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Sample records for donepezil hydrochloride aricept

  1. Bioequivalence Study of Donepezil Hydrochloride Tablets in Healthy Male Volunteers

    OpenAIRE

    Supanimit Teekachunhatean; Sukit Roongapinun; Nutthiya Hanprasertpong; Siriluk Aunmuang; Noppamas Rojanasthien

    2012-01-01

    The objective of this study was to investigate the bioequivalence of two formulations of 5 mg donepezil HCL tablets: Tonizep as the test and Aricept as the reference. The two products were administered as a single oral dose according to a randomized two-phase crossover with a 3-week washout period in 20 healthy Thai Male volunteers. After drug administration, serial blood samples were collected over a period of 216 hours. Plasma donepezil concentrations were measured by high performance liqui...

  2. RP-HPLC analytical method development and optimization for quantification of donepezil hydrochloride in orally disintegrating tablet.

    Science.gov (United States)

    Liew, Kai Bin; Peh, Kok Khiang; Fung Tan, Yvonne Tze

    2013-09-01

    An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase. The method showed intraday precision and accuracy in the range of 0.24% to -1.83% and -1.83% to 1.99% respectively, while interday precision and accuracy ranged between 1.41% to 1.81% and 0.11% to 1.90% respectively. The standard calibration curve was linear from 0.125 μg/mL to 16 μg/mL, with correlation coefficient of 0.9997±0.00016. The drug solution was stable under room temperature at least for 6 hours. System suitability studies were done. The average plate count was > 2000, tailing factor method was used to assay donepezil hydrochloride in tablet and dissolution study of in-house manufactured donepezil orally disintegrating tablet and original Aricept.

  3. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride: P300 event related potential

    Directory of Open Access Journals (Sweden)

    Qiang Liu

    2016-01-01

    Full Text Available Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days, or combined with acupuncture at Shenting (DU24, Tianzhu (BL10, Sishencong (Extra, Yintang (Extra, Renzhong (DU26, Neiguan (PC6, Shenmen (HT7, Fengchi (GB20, Wangu (GB12 and Baihui (DU20 (once a day for 56 days. Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased amplitude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identified within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These findings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia.

  4. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride:P300 event related potential

    Institute of Scientific and Technical Information of China (English)

    Qiang Liu; Xiu-juan Wang; Zhe-cheng Zhang; Rong Xue; Ping Li; Bo Li

    2016-01-01

    Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days), or combined with acupuncture atShenting (DU24),Tianzhu (BL10),Sishencong (Extra), Yintang (Extra),Renzhong (DU26),Neiguan (PC6),Shenmen (HT7),Fengchi (GB20),Wangu (GB12) andBaihui (DU20) (once a day for 56 days). Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased ampli-tude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identiifed within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These ifndings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia.

  5. Recovery of cognitive dysfunction in a case of delayed encephalopathy of carbon monoxide poisoning after treatment with donepezil hydrochloride

    OpenAIRE

    Wang Pin; Zeng Tao; Chi Zhao-fu

    2009-01-01

    Delayed encephalopathy following carbon monoxide poisoning is a serious complication. Here, we report a patient with delayed encephalopathy who suffered from cognitive disorders and urinary incontinence after a temporal normal period of 15 days after acute intoxication, and his cognitive function recovered gradually following donepezil hydrochloride treatment. Now, he can undertake slight farming work.

  6. Recovery of cognitive dysfunction in a case of delayed encephalopathy of carbon monoxide poisoning after treatment with donepezil hydrochloride

    Directory of Open Access Journals (Sweden)

    Wang Pin

    2009-01-01

    Full Text Available Delayed encephalopathy following carbon monoxide poisoning is a serious complication. Here, we report a patient with delayed encephalopathy who suffered from cognitive disorders and urinary incontinence after a temporal normal period of 15 days after acute intoxication, and his cognitive function recovered gradually following donepezil hydrochloride treatment. Now, he can undertake slight farming work.

  7. Study on donepezil hydrochloride selective electrode%盐酸多奈哌齐药物电极的研究

    Institute of Scientific and Technical Information of China (English)

    任凌燕; 徐刚; 刘火安

    2009-01-01

    Objective:To prepare a polyvinyl chloride membrance donepezil hydrochloride selective electrode for assay of donepezil hydrochloride.Methods:To be made with sodium tetraphenylborate and donepezil hydrochloride ionophore as the electroactive material.Design with the electrode linear response range for the donepezil hydrochloride as the object function for optimization,the membrance composition was ionophore.PVC-membrance solvent di -n-octylphthalate(3.4:28.3:68.3,w/w).Then the donepezil hydrochloride selective electrode was prepared and its performance index was evaluated.Results:The electrode showed a linear Nernst response in the range of 1.78×10~(-6)-1.0×10~(-1)mol·L~(-1) in a buffer solution of pH 5 with a slope of 42 mV/pC at 10℃.The detection limit is 5.3×10~(-7) mol·L~(-1).Conclusion:The electrode has high selectivity,fast response and good reproducibility.Its result is accurate and reliable.It can be used to determine the donepezil hydrochloride.content in drugs.%目的:研制一种用于测定盐酸多奈哌齐含量的药物选择件电极.方法:采用四苯硼酸钠与盐酸多奈哌齐生成的离子缔合物为电活性物质,以电极响应范围为优化目标函数,按电活性物-PVC-邻苯二甲酸二正辛酯3.4:28.3:68.3(w/w)的比例制备PVC膜,研制盐酸多奈哌齐药物选择性电极,并对电极的性能指标进行评价.结果:在pH 5的盐酸-氢氧化钠溶液中,电极的线性范围为1.78×10~(-6)~1,0×10~(-1) mol·L~(-1),斜率为42 mV/pC(10℃),检出限为5.3×10~(-7) mol·L~(-1).结论:该电极选择性好,响应快,重现性好,测定结果准确可靠,可用于盐酸多奈哌齐药物的含量测定.

  8. Determination of donepezil hydrochloride in Donepezil Hydrochloride Tablets by HPLC%高效液相色谱法测定盐酸多奈哌齐片中的盐酸多奈哌齐

    Institute of Scientific and Technical Information of China (English)

    陈泊颖; 王博; 孟策; 陈欣怡; 任晓文

    2016-01-01

    Objective To develop an HPLC method for the content determination of donepezil hydrochloride in Donepezil Hydrochloride Tablets.Methods The HPLC analysis was performed on a Thermo ODS C18 column (250 mm × 4.6 mm,5 μμm);0.02 mol/L sodium 1-heptanesulfonate-acetonitrile-chlorine acid (50∶50∶1) was used as mobile phase;The detection wavelength was set at 271 nm and column temperature was maintained at 30 ℃;the flow rate was 1.0 mL/min and injection volume was 20 μL.Results The method showed a good linear relationship within the concentration range of 50-350 μg/mL (r =0.999 9),and the average recovery was 99.34% with RSD of 0.72% (n =9).Conclusion This method is convenient,rapid,accurate,and with good specificity and reproducibility,which could be used for quantitative determination of donepezil raw material drug and Donepezil Hydrochloride Tablets.%目的 建立高效液相色谱法测定盐酸多奈哌齐片中盐酸多奈哌齐的方法.方法 采用高效液相色谱法,用Thermo ODS C18色谱柱(250 mm×4.6mm,5 μm);以0.02 mol/L庚烷磺酸钠-乙腈-高氯酸(50∶50∶1)为流动相;波长271 nm;柱温30℃;体积流量为1.0 mL/min;进样体积20μL.结果 盐酸多奈哌齐在50~350 μg/mL与峰面积呈良好的线性关系,r=0.999 9(n=7);平均加样回收率为99.34%,RSD值为0.72%(n=9).结论 本法操作简便、准确,专属性强,重复性好,可用于盐酸多奈哌齐原料及盐酸多奈哌齐片的定量测定.

  9. Preparation Method of High Quality Donepezil hydrochloride%高质量盐酸多奈哌齐的制备方法

    Institute of Scientific and Technical Information of China (English)

    冯建鹏; 祝传宝; 胡丽娜; 王伟

    2012-01-01

    To provide a concise synthetic route of donepezil hydrochloride.Firstly,to choose 5,6-dimethoxy-2-(4-piperidinyl methylene)-2,3-dihydro-1H-inden-1-one as the starting material,to reduce pyridine to piperidine derivative,by PtO2 hydrogenization.Secondly to prepare donepezil hydrochloride,by the key Leuckart-Wallach reaction.Finally,by salification and refination,to obtain the high quality pharmaceutical grade donepezil hydrochloride by four step reaction with a overall yield of 69%.%提供了一条较为简洁的盐酸多奈哌齐合成路线,即以5,6-二甲氧基-2-(4-哌啶基甲基)-2,3-二氢-1H-茚酮为起始原料,PtO2催化氢化将吡啶还原为哌啶衍生物,以刘卡特-瓦拉赫反应为关键反应将胺基苄基取代制得盐酸多奈哌齐。再经过成盐和精制,以四步反应,69%的总收率得到了高质量的药用盐酸多奈哌齐。

  10. 盐酸多奈哌齐治疗老年痴呆的临床分析%Clinical Analysis on Donepezil Hydrochloride in Treatment of Senile Dementia

    Institute of Scientific and Technical Information of China (English)

    常嵘

    2015-01-01

    Objective Clinical effect of Donepezil Hydrochloride in treatment of senile dementia was to be studied.Methods Choose 48 elderly patients of senile dementia who are treated in hospital from January 2015 to November 2015 and separated 23 patients into control group that were given conventional treatment, while another 25 patients are taken into study group were given Donepezil Hydrochloride treatment and then observed and compared treatment effects between two groups.Results Patients’ treatment efficacy was much higher and their MMSE and ADL assessment scores were improved much more favorable in study group and patients’ side-effect incidence was much lower compared to that in control group; there was a differential between two groups and such a differential has statistic value(P<0.05). Conclusion Donepezil Hydrochloride was effective in treatment of senile dementia.%目的:分析盐酸多奈哌齐治疗老年痴呆的效果。方法研究2015年1月~2015年11月,纳入老年痴呆共48例,随机分组。常规治疗者有23例,为对照组;盐酸多奈哌齐治疗者有25例,为研究组。对比效果。结果两组中研究组的治疗有效率更高,MMSE和ADL评分改善更明显,不良反应率更低,有显著差异(P<0.05),且具统计学意义。结论盐酸多奈哌齐对老年痴呆治疗效果佳。

  11. 高压氧联合盐酸多奈哌齐治疗卒中后认知功能障碍%Hyperbaric Oxygen Combined with Donepezil Hydrochloride in the Treatment of Post-Stroke Cognitive Impair-ment

    Institute of Scientific and Technical Information of China (English)

    许颖; 杨坚; 高宁沁; 陈小平

    2015-01-01

    目的:分析高压氧联合盐酸多奈哌齐对卒中后认知功能障碍的疗效。方法:将90例住院治疗的卒中后认知功能障碍患者分为高压氧联合盐酸多奈哌齐10 mg组、盐酸多奈哌齐10 mg组、盐酸多奈哌齐5 mg组,每组各30例。采用简易精神状态量表(MMSE)及日常生活能力量表(ADL)评价3组患者治疗前后的认知功能。结果:高压氧联合盐酸多奈哌齐10 mg组患者治疗后MMSE和ADL评分较单用盐酸多奈哌齐组明显增加,差异有统计学意义(P<0.01)。结论:高压氧联合盐酸多奈哌齐(10 mg )对卒中后伴认知功能障碍患者的疗效较好。%Objective:To analyze the efficacy of hyperbaric oxygen combined with donepezil hydrochloride on post‐stroke cogni‐tive impairment .Methods:Ninety hospitalized patients with post‐stroke cognitive impairment were selected .They were divided into hyperbaric oxygen combined with donepezil hydrochloride 10 mg group ,donepezil hydrochloride 10 mg group and donepezil hydrochloride 5 mg group ,with 30 cases in each group .Cognitive functions in 3 groups before and after the treatment were e‐valuated with the mini mental state examination (MMSE) and the ability of daily living scale (ADL) .Results:The scores of MMSE and ADL of patients in hyperbaric oxygen combined with donepezil hydrochloride 10 mg group increased more than those in donepezil hydrochloride groups after treatment ,and the differences were statistically significant (P<0 .01) .Conclu‐sions:Hyperbaric oxygen combined with donepezil hydrochloride 10 mg shows superior efficacy on post‐stroke patients accom‐panied by cognitive impairment .

  12. Relevance of Donepezil in Enhancing Learning and Memory in Special Populations: A Review of the Literature

    Science.gov (United States)

    Yoo, J. Helen; Valdovinos, Maria G.; Williams, Dean C.

    2007-01-01

    This review discusses the laboratory and clinical research supporting the rationale for the efficacy of donepezil (Aricept[R] USA) in enhancing cognition in autism, Alzheimer disease, Down syndrome, traumatic brain injury, Attention Deficit Hyperactivity Disorder (ADHD), and schizophrenia. While preliminary animal models have shown effective,…

  13. 尼麦角林联合盐酸多奈哌齐治疗轻度血管性痴呆的临床疗效及对患者认知功能的影响%The clinical efficacy of nicergoline combined with donepezil hydrochloride in the treatment of mild vascular dementia and its influence on cognitive function

    Institute of Scientific and Technical Information of China (English)

    马淑媛; 白易欣

    2015-01-01

    目的:探讨尼麦角林联合盐酸多奈哌齐治疗轻度血管性痴呆的临床疗效及对患者认知功能的影响。方法将66例轻度血管性痴呆患者采用随机数字表法分为两组,每组33例。在常规综合对症治疗的基础上,对照组给予尼麦角林口服,观察组给予给予尼麦角林联合盐酸多奈哌齐片口服。两组均4周为1个疗程,连续治疗3个疗程。结果治疗后观察组简易智力状况检查表评分为(36.7±5.7)分,较治疗前和对照组均显著升高(t =10.137、11.236,均 P <0.05);观察组 ADL 评分为(35.8±16.2)分,较治疗前和对照组显著降低(t =10.825、11.415,均 P <0.05);观察组总有效率为78.9%,明显高于对照组的54.5%(χ2=9.24, P <0.05)。结论尼麦角林联合盐酸多奈哌齐治疗轻度血管性痴呆,能够明显提高认知功能量表评分,疗效显著,安全可靠。%Objective To investigate the clinical efficacy of nicergoline combined with donepezil hydrochlo-ride in the treatment of mild vascular dementia and its influence on cognitive function.Methods 66 patients with mild vascular dementia from neurology were divided into two groups by random numbers,33 cases in each group.On the based of the routine symptomatic treatment,the control group were given nicergoline,the observation group were treated with nicergoline combined with aricept.Four weeks was a course,both groups were continuously treated for 3 courses.Results The MMSE scores of the observation group after treatment was (36.7 ±5.7)points,which was significantly increased compared with before treatment(t =10.137,P <0.05)and the control group(t =11.236,P <0.05);The ADL score was(35.8 ±16.2)points,which was significantly lower compared with before treatment(t =10.825,P <0.05)and the control group(t =11.415,P <0.05);The total effective rate of the observation group was 78.9%,which was higher than 54

  14. Effects of Different Administration Protocols on the Plasma Concentration of Donepezil Hydrochloride in Dementia Patients with Stage 5 Chronic Kidney Disease

    Directory of Open Access Journals (Sweden)

    Chika Amano

    2013-06-01

    Full Text Available The prevalence of chronic kidney disease (CKD as well as Alzheimer's disease (AD increases with age. With the aging of the population in Japan, there is an increasing likelihood that patients with CKD will receive donepezil hydrochloride (DPZ, an antidementia drug, in the near future. Nevertheless, there have been few reports on how to use DPZ in patients with severe CKD. We report on 2 CKD stage 5 patients who received DPZ under different prescriptions. In case 1, 3 mg/day of DPZ was initially administered for 4 months, after which the dose was increased to 5 mg/day. In case 2, 5 mg was administered twice a week. The plasma concentration of DPZ was measured and the effectiveness was assessed using the Mini-Mental Health State Examination and the Hasegawa Dementia Rating Scale. We found that (1 only a slight increase in the plasma concentration of DPZ was observed with a dose of 3 mg daily, (2 there was a significant increase in the plasma concentration with a dose of 5 mg daily, and (3 when 5 mg of DPZ was administered twice a week, the plasma concentration did not differ significantly from healthy controls who had received 5 mg daily. Although cognitive function was improved best when the 5-mg dose was administered daily with no apparent side effects, the plasma concentration came close to reaching a toxic level at this dose. Careful follow-up may be essential when DPZ is used at 5 mg/day or greater in severe CKD patients.

  15. Effects of the cholinestrerase inhibitors donepezil and metrifonate on scopolamine-induced impairments in the spatial cone field orientation task in rats

    NARCIS (Netherlands)

    Staay, van der F.J.; Bouger, P.C.

    2005-01-01

    The aim of these experiments was to assess whether the clinically validated cognition enhancers donepezil (Aricept(TM), E2020) and metrifonate antagonize scopolamine-induced deficits in the cone field, a complex spatial discrimination task. The cone field task allows measurement of the effects of ex

  16. Effects of the cholinestrerase inhibitors donepezil and metrifonate on scopolamine-induced impairments in the spatial cone field orientation task in rats

    NARCIS (Netherlands)

    Staay, van der F.J.; Bouger, P.C.

    2005-01-01

    The aim of these experiments was to assess whether the clinically validated cognition enhancers donepezil (Aricept(TM), E2020) and metrifonate antagonize scopolamine-induced deficits in the cone field, a complex spatial discrimination task. The cone field task allows measurement of the effects of

  17. The Effect of Donepezil Hydrochloride in the Treatment of Senile Dementia%盐酸多奈哌齐治疗老年性痴呆疗效研究

    Institute of Scientific and Technical Information of China (English)

    金梅香

    2015-01-01

    Objective To investigate the effect of donepezil hydrochloride in the treatment of senile dementia. Methods 178 AD patients were collected which were treated in our department from June 2012 to June 2014, and were randomly divided into obser-vation group and control group with each of 89 cases. The observation group were given donepezil treatment, The control group was given the Laci Staw treatment, two groups of curative effect were compared. Results The total effective rate of observation group was 93.2%, the control group was 74.2%, The difference was statistically significant (P0.05). Conclusion Donepezil hydrochloride in the treatment of AD can significantly improve the cognitive function of patients, the effect is significant and worth to apply.%目的:探讨盐酸多奈哌齐治疗老年性痴呆的效果。方法整群选取该院2012年6月-2014年6月收治的AD患者178例,随机分为2组各89例,观察组给予盐酸多奈哌齐治疗,对照组给予吡拉西坦治疗,比较两组疗效。结果观察组总有效率为93.2%,对照组总有效率为74.2%,两组比较差异有统计学意义(P0.05)。结论盐酸多奈哌齐治疗AD可明显改善患者认知功能,效果显著,值得应用。

  18. 评价盐酸多奈哌齐治疗老年痴呆患者的临床疗效%Clinical Efficacy of Donepezil Hydrochloride in the Treatment of Elderly Patients With Dementia

    Institute of Scientific and Technical Information of China (English)

    秦栎媛

    2016-01-01

    目的:评价盐酸多奈哌齐治疗老年痴呆的临床效果。方法我院收治老年痴呆患者共80例作为调查对象。对照组40例患者接受常规治疗;观察组40例患者除了常规治疗外,联合盐酸多奈哌齐进行治疗,分析比较两组患者的临床治疗效果。结果治疗前,两组患者的MMSE评分及ADL评分比较差异无统计学意义(P>0.05);而治疗12周比较,观察组患者的MMSE评分及ADL评分改善优于对照组,组间差异有统计学意义(P<0.05)。结论盐酸多奈哌齐治疗老年痴呆效果优,安全性高。%Objective To evaluate the clinical effect of donepezil hydrochloride in the treatment of senile dementia.Methods Atotal of 80 cases of senile dementia were treated in our hospital. The control group(40 cases)were treated with conventional therapy,observation group of 40 patients in addition to conventional treatment,combined with donepezil hydrochloride treatment and between the two groups of patients with clinical therapeutic effect were compared.Results Before treatment,two groups of patients with the scores of MMSE and ADL score had no significant difference(P>0.05),and 12 weeks of treatment,the observation group of patients with the scores of MMSE and ADL score were better than the control group,the difference exist significant difference(P<0.05).Conclusion Donepezil hydrochloride in the treatment of senile dementia with obvious effect,high safety.

  19. 盐酸多奈哌齐在老年痴呆治疗中的应用研究%Application research of donepezil hydrochloride in the treatment of Alzheimer’s disease

    Institute of Scientific and Technical Information of China (English)

    李明

    2015-01-01

    Objective To investigate treatment method and effect by donepezil hydrochloride in the treatment of Alzheimer’s disease.Methods A total of 67 patients with Alzheimer’s disease were randomly divided into experimental group with 43 cases and control group with 24 cases. The experimental group received donepezil hydrochloride for treatment, and the control group received conventional treatment. Their curative effects were observed.Results The experimental group had total effective rate as 93.0%, and the control group had it as 75.0%. Their difference had statistical significance (P<0.05).Conclusion Application of donepezil hydrochloride in the treatment of Alzheimer’s disease patients can accelerate improvements of cognitive ability and ability of daily life in patients. This method provides remarkable effect, along with few adverse reactions. It is worthy wide promotion.%目的:探究老年痴呆患者采用盐酸多奈哌齐治疗的方法和效果。方法67例老年痴呆患者,随机分为实验组43例和对照组24例,实验组患者给予盐酸多奈哌齐治疗,对照组患者给予常规治疗,观察患者的治疗效果。结果实验组治疗总有效率为93.0%,对照组治疗总有效率为75.0%,差异有统计学意义(P<0.05)。结论老年痴呆患者采用盐酸多奈哌齐治疗,可促使患者认知能力和日常生活能力的提高,效果显著,不良反应少,可广泛推荐。

  20. 盐酸多奈哌齐在老年痴呆治疗中的应用研究%The Applied Research of Donepezil Hydrochloride in Treatment of Alzheimer

    Institute of Scientific and Technical Information of China (English)

    谢成玲

    2015-01-01

    目的:探究老年痴呆患者采用盐酸多奈哌齐治疗的方法和效果。方法选取2013年1月~2014年4月收治的86例老年痴呆患者进行治疗,随机分组,实验组49例患者采用盐酸多奈哌齐的治疗,对照组37例患者采取基础治疗,观察患者的治疗效果。结果实验组治疗有效率为85.71%,对照组治疗有效率为59.46%。两组患者的治疗效果差异显著,有统计学意义(P<0.05)。结论老年痴呆患者采用盐酸多奈哌齐的治疗,不良反应少,安全性高,缓解患者的身体症状。%Objective The treatment and efficiency of donepezil hydrochloride in Alzheimer are to be investigated. Methods Choose 86 patients with Alzheimer who are treated in hospital from January 2013 to April 2014 and separate them into control group and study group at random. 49 patients in study group are given donepezil hydrochloride treatment and 37 patients in control group are given elementary treatment. And then observe the treatment efficiency of two groups. Results The treatment efficiency in study group is up to 85.71%and treatment efficiency in control group is up to 59.46%,there is a treatment differential between the two groups,such a differential has statistic value(P<0.05).Conclusion Donepezil hydrochloride treatment is quite effective and safe to cure Alzheimer and relieve patients’ symptoms with less side-effect,which is worthy to be promoted and applied.

  1. Bioequivalence of Donepezil Hydrochloride Orally Disintegrating Tablets in Healthy Volunteers%盐酸多奈哌齐口腔崩解片人体生物等效性研究

    Institute of Scientific and Technical Information of China (English)

    宋薇; 杨静; 冯智军; 丁莉坤; 李雪晴; 周伦; 杨林; 文爱东

    2012-01-01

    目的:研究盐酸多奈哌齐口腔崩解片与盐酸多奈哌齐片人体的生物等效性.方法:20名男性健康志愿者随机交叉单剂量口服盐酸多奈哌齐口腔崩解片(受试制剂)与盐酸多奈哌齐片(参比制剂)5 mg,用液质联用法测定人血浆中多奈哌齐的浓度,用DAS 2.1软件计算药动学参数,并评价两制剂的生物等效性.结果:口服受试制剂和参比制剂药动学参数分别为Cmax(8.56±2.10)和(8.08±1.78) ng·ml-1,tmax(2.65±0.74)和(3.05±0.83)h,t1/2 (70.31±19.54)和(71.15±18.47)h,AUC0~216(373.76±94.15)和(353.04±81.42) ng·h·m1-1,AUC0~∞(420.30±110.99)和(399.80±108.56) ng·h·ml-1.受试制剂AUG~216的90%置信区间在参比制剂的等效范围内.结论:两种盐酸多奈哌齐制剂生物等效.%Objective; To study the bioequivalenee of donepezil hydrochloride orally disintegrating tablets and donepezil hydrochlo-ride tablets. Method: 20 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 5 mg orally disintegrating tablets (test preparation) or donepezil hydrochloride tablets ( reference preparation). Plasma concentrations of donepezil were determined by liquid chromatography tandem mass spectrometry method. The pharma-cokinetic parameters were calculated by DAS 2. 1 software. Result; The main pharmacokinetic parameters of test and reference preparations after oral administration were as follows;^ of (8.56 ±2. 10) and (8.08 ± 1.78) ng ml"' ,tmax of (2.65 ±0.74) and(3.05 ± 0.83) h,tI/2 of (70.31 ±19.54) and (71.15 ± 18.47) h,AUC0_m of (373.76 ±94.15) and (353.04 ± 81.42) ng -h -ml-', AUC0_, of (420. 30 ±110.99) and (399. 80 ± 108.56) ng -h ml"1. The 90% confidential intervals (CI) of AUC0_2]6 of the test preparation was in the bioequivalent range of the reference preparation. Conclusion; The two kinds of donepezil formulations are bio-equivalent.

  2. Memantine Combined with Hydrochloride Donepezil in Treating Alzheimer′s Disease%美金刚联合盐酸多奈哌齐治疗阿尔茨海默病疗效研究

    Institute of Scientific and Technical Information of China (English)

    蒋志宏; 蔡鸣; 谷新医; 马强

    2016-01-01

    目的:探讨美金刚联合盐酸多奈哌齐治疗阿尔茨海默病(AD)的疗效。方法选取医院2013年6月至2015年6月收治的AD患者98例,将其随机分为治疗组和对照组,各49例。对照组患者采用盐酸多奈哌齐治疗,治疗组患者在对照组治疗基础上加用美金刚治疗。比较两组患者的临床疗效、精神行为障碍、日常生活能力、不良反应等情况。结果治疗组总有效率为93.88%,显著高于对照组的79.59%( P﹤0.05);治疗后,两组痴呆病理行为评定量表( BEHAVE-AD )评分、蒙特利尔认知评估量表( MoCA )评分、简易智能精神状态检查量表( MMSE )评分及日常生活活动能力量表( ADL )评分均得到显著改善,且治疗组改善幅度更明显( P﹤0.05)。结论美金刚联合盐酸多奈哌齐能有效缓解和消除AD患者的精神行为障碍,全面改善和提升患者的日常生活能力。%Objective To probe into the efficacy of memantine combined with hydrochloride donepezil for patients with Alzheimer's disease. Methods 98 Alzheimer's disease patients from June 2013 to June 2015 were selected and randomly divided into the treatment group and control group,49 cases in each group. The control group was treated with hydrochloride donepezil,and the treatment group was treated with memantine combined with hydrochloride donepezil. The clinical efficacy,mental and behavioral disorders,activities of daily living,incidence of adverse reactions of the patients in two groups were compared and analyzed. Results The total effective rate in the treatment group was 93. 88%,which was significantly higher than 79. 59% of the control group( P ﹤ 0. 05);after treatment,the BEHAVE-AD scores,the MoCA scores,and the MMSE scores in the two groups were significantly increased,and the increase in the treatment group was more obvious ( P ﹤ 0. 05). Conclusion Memantine combined with hydrochloride donepezil could alleviate and e

  3. 多奈哌齐联合盐酸美金刚治疗阿尔茨海默病的临床研究%Clinical Study of Donepezil and Memantine Hydrochloride in the Treatment of Alzheimer's Disease

    Institute of Scientific and Technical Information of China (English)

    王雪

    2015-01-01

    目的:探讨多奈哌齐联合盐酸美金刚治疗阿尔茨海默病的的临床疗效和安全性。方法78例阿尔茨海默病患者随机分为观察组与对照组两组各39例,观察组患者采用多奈哌齐联合盐酸美金刚治疗,对照组患者采用多奈哌齐治疗,采用AD 评估量表-认知部分(ADAS-cog)、简易智能精神状态检查量表(MMSE)和日常生活活动能力量表(ADL)评定患者治疗前后的临床效果。结果治疗后,两组患者ADAS-cog、MMES和ADL量表评分与治疗前相比均有所改善(P<0.05);观察组患者改善效果好于对照组(P<0.05)。两组不良反应发生情况相比差异无统计学意义(P>0.05)。结论多奈哌齐联合盐酸美金刚治疗阿尔茨海默病疗效显著,能显著改善患者的认知功能和行为能力,并且具有良好的安全性。%Objective To explore the clinical effects and security of donepezil combined with memantine in the treatment of alzheimer’s disease. Methods78 cases of Alzheimer's disease patients were randomly divided into observation group and control group 39 cases in each group, the patients in the observation group with donepezil and memantine hydrochloride in the treatment and control group were treated with donepezil, table - cognitive (ADAS-cog), Mini Mental State Examination (MMSE) and activities of daily living ability scale (ADL) before and after treatment in patients with the clinical effect assessment by the assessment.ResultsAfter treatment, The scores of ADAS-cog, MMSE and ADL were improved in both groups (P0.05).Conclusion Donepezil combined with memantine in the treatment of alzheimer’s disease has signiifcant curative effect, can signiifcantly improve the patients' cognitive function and behavior ability, and good security.

  4. 丙戊酸镁缓释片联合盐酸多奈哌齐胶囊改善老年性痴呆患者认知行为的疗效观察%Magnesium Valproate Tablet Combined with Donepezil Hydrochloride Donepezil Capsules Improve Senile Dementia Cognitive Behavioral Effect Observed

    Institute of Scientific and Technical Information of China (English)

    范丽伟

    2013-01-01

    目的:评价丙戊酸镁缓释片联合盐酸多奈哌齐胶囊改善老年性痴呆(AD)患者认知行为的有效性及安全性.方法:对32例老年性痴呆患者采用丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗16 w,治疗前后用简易智能精神状态检查量表(MMSE)、AD评定量表(ADAS)及Blessed-Roth痴呆量表评价患者认知功能及痴呆严重程度、精神行为异常(ADAS non-cog)及日常生活自理能力(ADL),并进行安全性评价.结果:丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗后,老年性痴呆患者MMSE评价较治疗前提高(P<0.01),ADAS认知部分、ADAS non-cog及Blessed-Roth日常生活自理能力部分均有改善(P<0.01,P<0.05);1例出现轻度副作用.结论:丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗老年性痴呆患者有较好的疗效并安全性好,副作用小.%Objective:To evaluate magnesium valproate sustained-release tablets joint donepezil hydrochloride capsules improve the efficacy and safety of Alzheimer's disease (AD) patients with cognitive behavioral.Methods:32 cases of senile dementia patients with magnesium valproate sustained-release tablets joint donepezil hydrochloride capsules 16 weeks of treatment,before and after treatment with a simple mental state examination Scale (MMSE),AD Assessment Scale (ADAS) and Blessed-Roth The dementia scale evaluation of patients with cognitive function and dementia severity,behavioral and psychological abnormalities (ADAS non-cog)and activities of daily living ability (ADL),and the safety evaluation.Results:magnesium valpronte sustained-release tablets joint donepezil hydrochloride capsules treatment MMSE evaluation of patients with senile dementia than before treatment (P < 0.01),ADAS cognitive portion of the ADAS non-cog and the Blessed-Roth daily livingThe ability of parts were improved (P < 0.01,P <0.05) ; cases of mild side effects.Conclusion:The sustained-release tablets of magnesium valproate joint

  5. 丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗老年痴呆精神行为障碍的疗效观察%The Curative Effect of Magnesium Combined with Donepezil Hydrochloride Capsules in the Treatment of Patients with Behavioral and Psychiatric Disorders in Senile Dementia

    Institute of Scientific and Technical Information of China (English)

    孙平; 曲春晖; 王立钢

    2016-01-01

    目的:对老年痴呆(AD)患者联合应用丙戊酸镁缓释片与盐酸多奈哌齐胶囊的临床疗效进行观察。方法将我院收治的70例老年痴呆患者随机分为对照组与观察组,给予对照组单纯盐酸多奈哌齐胶囊治疗,观察组患者则在此基础上加用丙戊酸镁缓释片。对两组患者的治疗效果进行对比与评价。结果经过为期16周的治疗,观察组患者的MMSE评分显著高于对照组(P<0.05);观察组患者的ADAS和Blessed-Roth评分显著高于对照组(P<0.05)。结论通过对老年痴呆患者联合应用丙戊酸镁缓释片与盐a酸多奈哌齐胶囊进行治疗,可显著改善患者的精神行为障碍,促进其生活自理能力的提高,值得临床推广应用。%Objective To investigate the clinical of magnesium combined with donepezil hydrochloride capsules in the treatment of patients with behavioral and psychiatric disorders in senile dementia(AD).Methods 70 cases of senile dementiawith mental disorderwere divided into two groups, control group and observation group. The control group was treated with donepezil hydrochloride capsules, the observation group was treated with magnesium combined with donepezil hydrochloride capsules.The effect of the two groups were compared and evaluated. Results After 16 weeks of treatment, the MMSE score of the observation group was significantly higher than that of control group (P<0.05). The ADAS score and Blessed-Roth score of the observation group was significantly higher than that of control group (P<0.05).Conclusion Using magnesium combined with donepezil hydrochloride capsules to treat thepatients of behavioral and psychiatric disorders can significantly improve the patient’s mental and behavioral disorders, promote their self-care ability increase, it is worthy of clinical application.

  6. Comparison of the Effects of a Brand-name Drug and Its Generic Drug on the Quality of Life of Alzheimer's Disease Patients.

    Science.gov (United States)

    Sakakibara, Mikio; Kido, Mitsuhiko; Kuribayashi, Jun; Okada, Hiroshi; Igarashi, Ataru; Kamei, Hiroyuki; Nabeshima, Toshitaka

    2015-08-31

    The pharmacological effects of generic (GE) donepezil are the same as Aricept, its brand-name counterpart. However, little is known as to whether these two drugs provide the same quality of life (QOL). The study subjects were patients with Alzheimer's disease who were taking donepezil hydrochloride tablets, and were selected by visiting either the local pharmacies or the patients' homes. We chose the brand-name drug Aricept and its GE form donepezil to investigate, from a long-term caregiver's perspective, the influence of both drugs on the patients' QOL. An EuroQol-5 Dimension (EQ-5D) was used to assess the QOL of patients with Alzheimer's disease, before and after various Aricept and/or donepezil regimens. Patients were divided into four groups: first time users of Aricept (n=43), first time users of GE donepezil (n=45), users refilling previous prescriptions of Aricept (n=51), and users switching from Aricept to GE donepezil (n=51). The average change in the EQ-5D utility indices rose significantly in the patients starting a new regimen of Aricept and its GE drug. The patients continuing an existing regimen of Aricept showed no significant differences, even after Aricept was switched to a GE drug. The QOL of patients starting a new regimen of Aricept and its GE drug improved. The QOL was maintained upon switching to the GE drug form.

  7. 交泰丸联合盐酸多奈哌齐治疗血管性痴呆45例临床研究%Clinical research on Jiaotai Pill combined with Donepezil Hydrochloride in the treatment of 45 patients with vascular dementia

    Institute of Scientific and Technical Information of China (English)

    胡玉英; 胡跃强; 张青萍; 梁妮; 刘永辉

    2013-01-01

    目的 观察交泰丸联合盐酸多奈哌齐治疗血管性痴呆(vascular dementia,VD)的临床疗效.方法 90例VD患者按随机数字表法随机分为两组,治疗组 45例采用交泰丸0.02 g/(kg·d),2次/d,早晚饭后口服,同时予盐酸多奈哌齐5 mg每晚临睡前口服,共治疗4周.对照组45例采用盐酸多奈哌齐5 mg每晚临睡前口服,共治疗4周.观察治疗4周后的临床疗效,以及治疗4周后评价简易精神状况检查量表(MMSE)、日常生活能力(ADL)的变化.结果 治疗组治疗后的显效率和总有效率均明显高于对照组(P < 0.05);并且治疗组治疗后MMSE和ADL评分均明显高于对照组(P < 0.05).结论 交泰丸联合盐酸多奈哌齐治疗VD疗效显著,优于单独使用盐酸多奈哌齐.%Objective To observe the clinical efficacy on jiaotai Pill combined with Donepezil Hydrochloride in the treatment of vascular dementia (VD). Methods 90 patients with VD were randomly divided into treatment group and control group. 45 patients in the treatment group were given Jiaotai Pill 0.02 g/(kg?d), 2 time a day after breakfast and supper, meanwhile they were given 5 mg Donepezil Hydrochloride orally at bedtime every night. 45 patients in the control group were given 5 mg Donepezil Hydrochloride orally at. bedtime every night. Patients of two groups were treated for 4 weeks. The clinical efficacy after 4 weeks treatment and the changes of MMSE and ADL before and after 4 weeks treatment were observed. Results After treatment, the treatment group was better than the control group obviously in the aspect of apparent rate and the total effective rate (P < 0.05). The MMSE and ADL scores of treatment group were better than that of control group obviously (P < 0.05). Conclusion The Jiaotai Pill combined with Donepezil Hydrochloride in the treatment of vascular dementia (VD) is very effective in clinical efficacy. The clinical efficacy is better than using Donepezil Hydrochloride alone.

  8. Clinical observation of Reinhartdt and Sea Cucumber Capsule (RSC) combined and donepezil hydrochloride in treatment of alzheimer's disease%复方海蛇胶囊联合盐酸多奈哌齐治疗阿尔茨海默病临床观察

    Institute of Scientific and Technical Information of China (English)

    孔佳

    2012-01-01

    Objective It is to approach the efficacy and safety of Reinhartdt and Sea Cucumber Capsule ( RSC ) co-treatment of donepezil hydrochloride in alzheimer' s disease ( AD ). Methods Ninety-six patients with AD were randomly divided into RSC group ( 30 patients ), hydrochloric donepezil group ( 32 patients ) and combined treatment group ( 34 patients ). RSC group was treated with RSC by orally; hydrochloride donepezil group was treated with hydrochloric donepezil by orally; combined treatment group also oral RSC and hydrochloric donepezil; continuous medication for six-month-term. The mini-mental state examination ( MMSE ), activities of daily living scale ( ADL ), cognitive sub-scale ( ADAS - Cog ), clinical dementia rating scale ( CDR ) and side effects scale ( TESS ) assessment of the situation of three groups were observed. Results ①The MMSE scores in each group after treatment were greater than before, the ADL, ADAS - Cog, CDR score in each group after treatment were less than before treatment, there were significant different ( P 0. 05 ). Conclusion Combination use RSC and donepezil hydrochloride is safe and effective method in treatment of AD, the effect is better than a single drug, and the incidence of adverse reactions is low.%目的 探讨复方海蛇胶囊(RSC)联合盐酸多奈哌齐治疗阿尔茨海默病(AD)的有效性及安全性.方法 96例AD患者随机分为RSC组30例、盐酸多奈哌齐组32例和联合用药组34例,RSC组给予复方海蛇胶囊口服;盐酸多奈哌齐组给予盐酸多奈哌齐口服;联合用药组同时口服复方海蛇胶囊和盐酸多奈哌齐;连续用药6个月.观察3组患者治疗前后智能状态量表(MMSE)、日常生活能力量表(ADL)、认知次级量表(ADAS-Cog)、痴呆程度评定量表(CDR)以及副反应量表(TESS)评定情况.结果 治疗后各组MMSE评分均大于治疗前(P<0.05),ADL、ADAS-Cog、CDR评分均小于治疗前(P均<0.05);3组不良反应发生

  9. Effect of donepezil hydrochloride on changes of cognitive function and Montreal cognitive assessment scores in patients with mild cognitive impairment%盐酸多奈哌齐对MCI患者MoCA评分和认知功能的影响

    Institute of Scientific and Technical Information of China (English)

    赵继巍; 赵敬堃

    2012-01-01

    目的 探讨盐酸多奈哌齐对轻度认知障碍(MCI)患者蒙特利尔认知评估量表(MoCA)评分和认知功能的影响. 方法 哈尔滨医科大学附属第一医院神经内科自2010年9月至2011年3月共收治MCI患者50例,其中给予盐酸多奈哌齐治疗30例(盐酸多奈哌齐组),银杏叶片治疗20例(对照组),分析并比较2组患者治疗前、治疗12周、24周后MoCA评分的变化. 结果 盐酸多奈哌齐组患者治疗12、24周时MoCA评分高于治疗前,差异有统计学意义(P<0.05).治疗12周、24周时盐酸多奈哌齐组MoCA评分均高于对照组,差异有统计学意义(P<0.05);治疗12周时盐酸多奈哌齐组患者在数字广度、词语流畅性和延迟记忆方面的分项得分高于治疗前,差异有统计学意义(P<0.05). 结论 MoCA量表能够对MCI患者进行早期诊断,盐酸多奈哌齐对MCI患者进行早期治疗能延缓其进入AD的病程.%Objective To investigate the effect of donepezil hydrochloride on changes of cognitive functions and Montreal cognitive assessment (MoCA) scores in patients with mild cognitive impairment (MCI). Methods A total of 50 patients diagnosed as having MCI,admitted to our hospital from September 2010 to March 2011, were recruited; these patients were randomly assigned into treatment group (treated with donepezil hydrochloride,n=30) and control group (treated with Ginkgo biloba,n=20); the changes of MoCA scores were noted at 12 and 24 weeks after treatment.The data were analyzed by the statistical software SPSS 10.0. Results MoCA scores of treatment group 12 and 24 weeks after treatment were significantly higher than those before treatment (P<0.05); MoCA scores of treatment group were significantly higher than those of control group 12 and 24 weeks after treatment (P<0.05).Mann-Whitney rank sum test showed significant improvement in digit span,verbal fluency and delayed memory after the treatment of donepezil hydrochloride for 12 weeks as compared

  10. The Clinical Analysis of Donepezil Hydrochloride in the Treatment of Senile Dementia%盐酸多奈哌齐治疗老年痴呆的临床探析

    Institute of Scientific and Technical Information of China (English)

    祝鸿雁

    2015-01-01

    目的:探讨盐酸多奈哌齐治疗老年痴呆的临床探析。方法选取2013年11月到2014年12月我院接诊的42例老年痴呆患者,随机分为两组,实验组22例和对照组20例,对照组给予常规治疗,实验组在对照组的基础上给予盐酸多奈哌齐,观察两组患者的治疗效果。结果实验组患者的简易智能精神状态检查量表(MMSE)评分、日常生活能力量表(ADL)评分及不良反应的发生率明显优于对照组,差异显著,有统计学意义(P<0.05)。结论盐酸多奈哌齐治疗老年痴呆的效果显著,有效改善患者的精神状态,提高患者的日常生活能力,值得临床推广。%Objective To study the clinical analysis of senile dementia on donepezil HCL treatment. Methods To divide the 42 cases patients into control group (22 cases)and experimental group(20 cases). The patients’cases were chosen from November 2013 to December 2014,the control group adopted conventional treatment,the experimental group adopted the basis of the control group combine with donepezil HCL,to observe the two groups’ therapeutic effect. Results The date of experimental group patients from simple intel igence scale for mental state examination score(MMSE),daily life ability scale score(ADL)and the incidence of adverse reaction was better than control group,it was in a high treatment efficiency and obvious difference and the statistical y significant(P< 0.05). Conclusion Donepezil HCL treatment has significantly effectively on the patients' mental state and the ability of the patients' daily life. It is widely used in clinical promotion.

  11. Liquid chromatography and liquid chromatography-mass spectrometry analysis of donepezil degradation products

    Directory of Open Access Journals (Sweden)

    Mladenović Aleksandar R.

    2015-01-01

    Full Text Available This study describes the investigation of degradation products of donepezil (DP using stability indicating RP-HPLC method for determination of donepezil, which is a centrally acting reversible acetylcholinesterase inhibitor. In order to investigate the stability of drug and formed degradation products, a forced degradation study of drug sample and finished product under different forced degradation conditions has been conducted. Donepezil hydrochloride and donepezil tablets were subjected to stress degradation conditions recommended by International Conference on Harmonization (ICH. Donepezil hydrochloride solutions were subjected to acid and alkali hydrolysis, chemical oxidation and thermal degradation. Significant degradation was observed under alkali hydrolysis and oxidative degradation conditions. Additional degradation products were observed under the conditions of oxidative degradation. The degradation products observed during forced degradation studies were monitored using the high performance liquid chromatography (HPLC method developed. The parent method was modified in order to obtain LC-MS compatible method which was used to identify the degradation products from forced degradation samples using high resolution mass spectrometry. The mass spectrum provided the precise mass from which derived molecular formula of drug substance and degradation products formed and proved the specificity of the method unambiguously. [Projekat Ministarstva nauke Republike Srbije, br. 172013

  12. Effect of donepezil hydrochloride combined with comprehensive rehabilitation on memory impairment of patients after traumatic brain injury%盐酸多奈哌齐配合综合康复治疗对颅脑外伤后记忆障碍的疗效观察

    Institute of Scientific and Technical Information of China (English)

    冼庆林; 成慧慧; 肖永涛; 朱洁; 钟伟湘

    2011-01-01

    Objective To explore the treatment efficacy and safty of donepezil hydrochloride combined with comprehensive rehabilitation in memory impairment of patients after traumatic brain injury(TBI).Methods Seventy-six patients with TBI,admitted to our hospital from May 2008 to October 2010,were randomly divided into control group(n=38)and treatment group(n=38)using a case-control study method; patients from control group were given memory training,cognitive training and other comprehensive rehabilitation therapy while those from treatment group were given donepezil hydrochloride combined with comprehensive rehabilitation therapy for 3 months.Wechsler memory scale (WMS)was used to evaluate the efficacy and the drug adverse reactions were observed.Results As compared with those before treatment,the scores of forward counting in the long-term memory,scores of recall and recognition in short-term memory,scores of counting without looking in immediate memory and total scores of WMS were significantly higher in the cnntrol group after treatment(P<0.05); as compared with those before treatment,the scores of long term memory(forvard counting,backward counting and adding),and scores of recall,recognition and logic memory in short-term memory,scores of counting without looking in immediate memory,and total scores of W-MS were significantly higher in the treatment group after treatment(P<0.05); as compared with those in the control group after treatment,the scores of adding in long term memory,scores of logic memory in short-term memory and total scores of WMS were significantly higher in the treatment group after treatment(P<0.05); oral administration of donepezil hydrochloride showed no significant adverse reactions.Conclusion Donepezil hydrochloride therapy combined with memory training,cognitive training and other comprehensive rehabilitation program is more effective than comprehensive rehabilitation therapy alone for memory impairment of patients after TBI.%目的 探

  13. Study on the Effect of Different Types of Application of Donepezil Hydrochloride in the Treatment of Senile Dementia%不同类型老年痴呆应用盐酸多奈哌齐治疗的效果研究

    Institute of Scientific and Technical Information of China (English)

    刘颖

    2016-01-01

    Objective To investigate the donepezil hydrochloride in treating different types of dementia effect.Methods Simple-mental state examination (MMSE) and activities of daily living scale (ADL) to evaluate different types of alzheimer's patients to take effect ares treatment.Results After treatment, MMSE score mixed dementia, alzheimer's disease (AD) has significantly increased (P<0.05), after treatment, ADL blood of AD patients have signiifcantly decreased (P<0.05).Conclusion Ares treatment of senile dementia and mixed dementia has a good part of the effect, and vascular dementia largely ineffective.%目的:探讨盐酸多奈哌齐治疗不同类型老年痴呆的效果。方法用简易智能精神状态检查量表(MMSE)与日常生活活动能力量表(ADL)评估不同类型老年痴呆患者采取盐酸多奈哌齐治疗的效果。结果治疗后混合型痴呆、老年性痴呆(AD)MMSE评分增高(P<0.05);治疗后血AD患者ADL降低(P<0.05)。结论阿瑞斯治疗老年性痴呆与部分混合型痴呆有较好效果,而对血管性痴呆基本无效。

  14. Multi-target directed donepezil-like ligands for Alzheimer's disease

    Directory of Open Access Journals (Sweden)

    Mercedes eUnzeta

    2016-05-01

    Full Text Available Alzheimer's disease (AD, the most common form of adult onset dementia, is an age-related neurodegenerative disorder characterized by progressive memory loss, decline in language skills and other cognitive impairments. Although its etiology is not completely known, several factors including deficits of acetylcholine, β-amyloid deposits, τ-protein phosphorylation, oxidative stress and neuroinflammation are considered to play significant roles in the pathophysiology of this disease. For a long time, AD patients have been treated with acetylcholinesterase inhibitors such as donepezil (Aricept® but with limited therapeutic success. This might be due to the complex multifactorial nature of AD, a fact that has prompted the design of new Multi-Target-Directed Ligands (MTDL based on the one molecule, multiple targets paradigm. Thus, in this context, different series of novel multifunctional molecules with antioxidant, anti-amyloid, anti-inflammatory and metal-chelating properties able to interact with multiple enzymes of therapeutic interest in AD pathology including acetylcholinesterase, butyrylcholinesterase and monoamine oxidases A and B have been designed and assessed biologically. This review describes the multiple targets, the design rationale and an in-house MTDL library, bearing the N-benzylpiperidine motif present in donepezil, linked to different heterocyclic ring systems (indole, pyridine or 8-hydroxyquinoline with special emphasis on compound ASS234, an N-propargylindole derivative. The description of the in vitro biological properties of the compounds and discussion of the corresponding structure-activity-relationships allows us to highlight new issues for the identification of more efficient MTDL for use in AD therapy.

  15. Characterization of oral disintegrating film containing donepezil for Alzheimer disease.

    Science.gov (United States)

    Liew, Kai Bin; Tan, Yvonne Tze Fung; Peh, Kok Khiang

    2012-03-01

    The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity.

  16. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    DEFF Research Database (Denmark)

    Guo, Wenjia; Quan, Peng; Fang, Liang

    2015-01-01

    The purpose of this study was to develop a PLGA microspheres-based donepezil (DP) formulation which was expected to sustain release of DP for one week with high encapsulation efficiency (EE). DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion......-solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared...... was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model, which suggested the diffusion governing...

  17. Donepezil in the treatment of musical hallucinations.

    Science.gov (United States)

    Ukai, Satoshi; Yamamoto, Masakiyo; Tanaka, Michio; Shinosaki, Kazuhiro; Takeda, Masatoshi

    2007-04-01

    Musical hallucinations (MH) typically occur among elderly individuals and are associated with hearing impairment. The authors describe a patient with features of typical MH who was successfully treated with donepezil, a cholinesterase inhibitor, as a combination therapy and who has not shown any subsequent cognitive decline for approximately 5 years. The efficacy of donepezil in this patient indicates that age-dependent dysfunction of cholinergic neurons might be related to the development of MH.

  18. Glucosamine hydrochloride

    Science.gov (United States)

    ... combination of glucosamine hydrochloride, chondroitin sulfate, and manganese ascorbate. Some evidence suggests that this combination can improve ... combination of glucosamine hydrochloride, chondroitin sulfate, and calcium ascorbate twice daily reduces joint swelling and pain, as ...

  19. Donepezil

    Science.gov (United States)

    ... irregular, slow, or fast heartbeat, seizures; difficulty urinating; asthma;chronic obstructive pulmonary disease (a group of lung disease including chronic bronchitis or emphysema); or kidney, liver, or heart disease.tell your ...

  20. Role of Donepezil in Autism: Its Conduciveness in Psychopharmacotherapy

    Directory of Open Access Journals (Sweden)

    Rohit Kant Srivastava

    2011-01-01

    Full Text Available A woman consulted psychiatric Out-Patient Department (OPD for her 5-year and 2-month-old son presenting with typical autistic symptoms like social, behavioural, and communicational ineptitudeness. Subsequent treatment with Donepezil resulted in marked improvement in the aforementioned symptomatology. Recent studies in autistic child have shown diminished acetylcholine and nicotinic receptor activity, thus an acetylcholinergic enhancer, Donepezil, likely accounts for improvement in autistic symptoms. Evidently, the case report consolidates Donepezil role as a potentially useful agent in the treatment of cognitive and behavioural symptoms observed in this disorder.

  1. Drug: D00670 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available lipid metabolism hsa04725(43) Cholinergic synapse Enzyme: CYP2D6 [HSA:1565], CYP3A4 [HSA:1576] map07056 Agents for Alzheimer...14 415.9529 D00670.gif Alzheimer's disease treatment [adjunct]; Dementia symptoms treatment adjunct; Cogniti...D00670 Drug Donepezil hydrochloride (JP16/USAN); Aricept (TN) C24H29NO3. HCl 415.19

  2. Erlotinib hydrochloride.

    Science.gov (United States)

    Minna, John D; Dowell, Jonathan

    2005-05-01

    Erlotinib hydrochloride (Tarceva; OSI Pharmaceuticals/Genentech/Roche), a member of a class of targeted anticancer drugs that inhibit the activity of the epidermal growth factor receptor, was approved by the US FDA in November 2004 for the treatment of advanced non-small-cell lung cancer after failure of at least one prior chemotherapy regimen. It is the first such drug to demonstrate an increase in survival in Phase III trials in patients with advanced non-small-cell lung cancer.

  3. Donepezil prevents RANK-induced bone loss via inhibition of osteoclast differentiation by downregulating acetylcholinesterase

    Directory of Open Access Journals (Sweden)

    Tsuyoshi Sato

    2015-09-01

    Conclusions: AChE promotes osteoclast differentiation in vitro. Donepezil inhibits osteoclast function in vitro and prevents bone loss by suppressing bone resorption in vivo, suggesting the possibility that donepezil reduces fracture risk in patients with Alzheimer's disease.

  4. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    Directory of Open Access Journals (Sweden)

    Wenjia Guo

    2015-10-01

    Full Text Available The purpose of this study was to develop a PLGA microspheres-based donepezil (DP formulation which was expected to sustain release of DP for one week with high encapsulation efficiency (EE. DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared successfully with average diameter of 30 µm, drug loading of 15.92 ± 0.31% and EE up to 78.79 ± 2.56%. Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface. Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model, which suggested the diffusion governing release mechanism. After single-dose administration of DP microspheres via subcutaneous injection in rats, the plasma concentration of DP reached peak concentration at 0.50 d, and then declined gradually, but was still detectable at 15 d. A good correlation between in vitro and in vivo data was obtained. The results suggest the potential use of DP microspheres for treatment of Alzheimer's disease over long periods.

  5. Effect of donepezil on cognition in severe Alzheimer's disease: a pooled data analysis

    DEFF Research Database (Denmark)

    Cummings, Jeffrey; Jones, Roy; Wilkinson, David;

    2010-01-01

    To better characterize response to donepezil in patients with severe AD, Severe Impairment Battery (SIB) data were pooled from four donepezil clinical trials (N=904). Changes in SIB total and domain scores from baseline to week 24 were compared between placebo and donepezil treatment groups (obse...

  6. Effect of donepezil on cognition in severe Alzheimer's disease: a pooled data analysis

    DEFF Research Database (Denmark)

    Cummings, Jeffrey; Jones, Roy; Wilkinson, David

    2010-01-01

    To better characterize response to donepezil in patients with severe AD, Severe Impairment Battery (SIB) data were pooled from four donepezil clinical trials (N=904). Changes in SIB total and domain scores from baseline to week 24 were compared between placebo and donepezil treatment groups...... between donepezil- and placebo-treated patients in least squares (LS) mean change in SIB total scores from baseline to week 24 was 6.22 (p ... mean difference, 7.60; p donepezil for seven of nine domains (range, p = 0.0056 to p

  7. The combination of aricept with a traditional Chinese medicine formula, smart soup, may be a novel way to treat Alzheimer's disease.

    Science.gov (United States)

    Wang, Ying; Wang, Ying; Sui, Yi; Yu, Hongshuang; Shen, Xiaoheng; Chen, Shengdi; Pei, Gang; Zhao, Jian; Ding, Jianqing

    2015-01-01

    Alzheimer's disease (AD) is a common neurodegenerative disease affecting cognitive function in the elderly, which is characterized by the presence of extracellular deposits of insoluble amyloid-β plaques and neuronal loss. Modern pharmacology and drug development usually follow a single-target principle, which might contribute to the failure of most compounds in clinical trials against AD. Considering AD is a multifactorial disease, a combination therapeutic strategy that applies drugs with different mechanisms would be an alternative way. Smart Soup (SS), a Traditional Chinese Medicine formula, is composed of three herbaceous plants and has been applied in the treatment of amnesia in China for hundreds of years. In this work, we studied the clinical potency of the combination of SS and Aricept in AD therapy. In the in vivo model, both longevity and locomotive activity of AD transgenic Drosophila were improved remarkably in the combined medicine treated group. We also observed less amyloid-β deposition and retarded neuronal loss following the combined drug treatment. In the retrospective cohort study, we found the combination therapy exerted better therapeutic effect on AD patients. Our study revealed that combination therapy with multiple drug targets did have a better therapeutic outcome. It provides a new strategy to develop an optimum pharmaceutical approach against AD.

  8. Cartap Hydrochloride Poisoning.

    Science.gov (United States)

    Kalyaniwala, Kimmin; Abhilash, Kpp; Victor, Peter John

    2016-08-01

    Cartap hydrochloride is a moderately hazardous nereistoxin insecticide that is increasingly used for deliberate self-harm in India. It can cause neuromuscular weakness resulting in respiratory failure. We report a patient with 4% Cartap hydrochloride poisoning who required mechanical ventilation for 36-hours. He recovered without any neurological deficits. We also review literature on Cartap hydrochloride poisoning.

  9. Donepezil-induced response of Spirulina supplemented rat urinary bladder.

    Science.gov (United States)

    Nurullahoglu-Atalik, K E; Okudan, N; Gokbel, H; Nurullahoglu, Z U

    2013-01-01

    At present, very little is known about the effects of donepezil on vascular reactivity. The aim of the present study was to evaluate the responses of rat urinary bladder to donepezil (10-10-3x10-4 M) and the role of Spirulina supplementation in these effects. Animals were divided into the two groups of six animals in each group. The first group received only distilled water daily as vehicle for six weeks and served as the control. The second group received Spirulina 750 mg kg -1 orally, daily for six weeks and served as the spirulina group. Preparations of rat urinary bladder were used from both groups. Donepezil produced concentration dependent relaxation of rat urinary bladder preparations pre-contracted with KCl.The pIC50 value, but not the maximal response of donepezil, was significantly lower (pSpirulina supplemented group. These results demonstrated for the first time that spirulina treatment can affect urinary bladder activity (Fig. 1, Ref. 20).

  10. Research progress of donepezil for treating mild to moderate Alzheimer's disease

    Directory of Open Access Journals (Sweden)

    Xin-xin LI

    2017-02-01

    Full Text Available Donepezil is the second generation of cholinesterase inhibitors (ChEIs, which has a good effect on mild to moderate Alzheimer's disease (AD. In recent years, there were a lot of studies on the mechanism of donepezil. This paper mainly introduces the diagnosis and treatment situation of AD in China, and the action mechanism of donepezil in the treatment of mild to moderate AD. DOI: 10.3969/j.issn.1672-6731.2017.02.012

  11. Delirium Associated with Donepezil in a Patient with Alzheimer’s Disease: a Case Report

    Directory of Open Access Journals (Sweden)

    Kamyar Mollazadeh-Moghaddam

    2013-03-01

    Full Text Available Donepezil, a member of the acetylcholinesterase inhibitor family, is approved for management of cognitive impairments as well as behavioral complications in patients with neurodegenerative Alzheimer's disease. Generally, donepezil is regarded as a safe medication in patients with Alzheimer’s disease although there have been reports of several minor adverse events including gastrointestinal disturbances. Herein we describe a patient with Alzheimer’s disease who demonstrated delirious behavior upon treatment with donepezil.

  12. Effect of donepezil on emergence of apathy in mild to moderate Alzheimer's disease

    DEFF Research Database (Denmark)

    Waldemar, Gunhild; Gauthier, Serge; Jones, Roy;

    2011-01-01

    To determine whether donepezil treatment (10 mg/day over 24 weeks) is associated with delayed emergence of apathy in patients with mild to moderate Alzheimer's disease (AD) and to explore relationships between donepezil's effects on apathy and other Neuropsychiatric Inventory (NPI)-measured behav......To determine whether donepezil treatment (10 mg/day over 24 weeks) is associated with delayed emergence of apathy in patients with mild to moderate Alzheimer's disease (AD) and to explore relationships between donepezil's effects on apathy and other Neuropsychiatric Inventory (NPI...

  13. Effects of donepezil on behavioural manifestations of thalamic infarction: a single case observation

    Directory of Open Access Journals (Sweden)

    Rodrigo eRiveros

    2011-03-01

    Full Text Available Objective: To examine the effect of donepezil for the treatment of cognitive and behavioural disorders associated with thalamic lesions in a 45 years old male who suffered an infarct in the left thalamus. Background: Recent studies suggest that donepezil may improve executive functions impairments due to subcortical ischemic lesionsMethod: The crossover effects of donepezil were analyzed in a single case of thalamic infarction with cognitive and behavioural alterations. Results: Significant behavioural modifications related to improved performances in executive functions were observed with the treatment. Conclusions: The results suggest that donepezil may have significant effect on executive functions that can alter behavioural outcomes after thalamic infarctions

  14. Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

    OpenAIRE

    2011-01-01

    The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer’s disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro resul...

  15. Effect of donepezil on emergence of apathy in mild to moderate Alzheimer's disease

    DEFF Research Database (Denmark)

    Waldemar, Gunhild; Gauthier, Serge; Jones, Roy

    2011-01-01

    To determine whether donepezil treatment (10 mg/day over 24 weeks) is associated with delayed emergence of apathy in patients with mild to moderate Alzheimer's disease (AD) and to explore relationships between donepezil's effects on apathy and other Neuropsychiatric Inventory (NPI)-measured behav...

  16. PET Evidence of the Effect of Donepezil on Cognitive Performance in an Animal Model of Chemobrain

    Directory of Open Access Journals (Sweden)

    Ilhan Lim

    2016-01-01

    Full Text Available A considerable number of patients with breast cancer complain of cognitive impairment after chemotherapy. In this study, we showed that donepezil enhanced memory function and increased brain glucose metabolism in a rat model of cognitive impairment after chemotherapy using behavioral analysis and positron emission tomography (PET. We found that chemotherapy affected spatial learning ability, reference memory, and working memory and that donepezil improved these cognitive impairments. According to PET analysis, chemotherapy reduced glucose metabolism in the medial prefrontal cortex and hippocampus, and donepezil increased glucose metabolism in the bilateral frontal lobe, parietal lobe, and hippocampus. Reduced glucose metabolism was more prominent after treatment with doxorubicin than cyclophosphamide. Our results demonstrated the neural mechanisms for cognitive impairment after chemotherapy and show that cognition was improved after donepezil intervention using both behavioral and imaging methods. Our results suggested that donepezil can be employed clinically for the treatment of cognitive deficits after chemotherapy.

  17. Effectiveness of donepezil in reducing clinical worsening in patients with mild-to-moderate alzheimer's disease

    DEFF Research Database (Denmark)

    Wilkinson, David; Schindler, Rachel; Schwam, Elias

    2009-01-01

    donepezil) with mild-to-moderate AD [Mini-Mental State Examination (MMSE) score 10-27] were pooled from 3 randomized, double-blind placebo-controlled studies. Clinical worsening was defined as decline in (1) cognition (MMSE), (2) cognition and global ratings (Clinician's Interview-Based Impression of Change...... plus Caregiver Input/Gottfries-Bråne-Steen scale) or (3) cognition, global ratings and function (various functional measures). RESULTS: At week 24, lower percentages of donepezil-treated patients than placebo patients met the criteria for clinical worsening, regardless of the definition. The odds...... of declining were significantly reduced for donepezil-treated versus placebo patients (p donepezil-treated patients. CONCLUSION: In this population, donepezil treatment...

  18. Donepezil in the treatment of opioid-induced sedation: report of six cases.

    Science.gov (United States)

    Slatkin, N E; Rhiner, M; Bolton, T M

    2001-05-01

    Donepezil, an oral acetylcholinesterase inhibitor approved for the treatment of Alzheimer's disease, was given to 6 cancer pain patients having sedation related to the analgesic use of opioids. Each patient was taking more than 200 mg of oral morphine equivalents per day, and several were receiving complex analgesic regimens consisting of multiple adjuvant medications. Sedation improved at least moderately in 5 of the patients and mildly in 1 after they began taking donepezil. Patients reported a decrease in episodes of spontaneous sleeping during the day, fewer myoclonic twitches, improved daily function and greater social interaction. Several also reported improved sleep at night. Analgesia was not compromised by the use of donepezil, and in some cases it appeared improved. Donepezil may be a valuable alternative to psychostimulants in the treatment of opioid-induced sedation. A prospective controlled trial comparing the treatment effects of psychostimulants and donepezil on patients having opioid-induced sedation is underway.

  19. The Clinical Efficacy of Donepezil in the Treatment of Senile Dementia%盐酸多奈哌齐治疗老年痴呆的临床疗效

    Institute of Scientific and Technical Information of China (English)

    李克颖; 金海珠; 林萍

    2016-01-01

    Objective To discuss the clinical curative effect of senile dementia treated with donepezil.Methods The 78 cases of senile dementia patients were randomly divided into two groups, the control group Piracetam Tablets in the treatment, the observation group implementation of donepezil hydrochloride in the treatment.Results In the total effective rate, the observation group was 92.31%, significantly higher than the control group of 64.10% (P<0.05). After treatment, the two groups of patients with ADL, MMSE scores were significantly different (P<0.05). Conclusion The effect of donepezil hydrochloride in the treatment of senile dementia implementation signiifcantly, is adopted.%目的:评价老年痴呆实施盐酸多奈哌齐治疗的临床疗效。方法将78例老年痴呆患者随机分为两组,对照组实施吡拉西坦片治疗,观察组实施盐酸多奈哌齐治疗。结果在总有效率上,观察组为92.31%,明显比对照组64.10%高(P<0.05)。治疗后,两组患者ADL、MMSE评分均差异显著(P<0.05)。结论老年痴呆实施盐酸多奈哌齐治疗效果显著,值得采纳应用。

  20. Quantitation of Donepezil in Human Plasma by HPLC-MS%人血浆中盐酸多奈哌齐的HPLC-MS测定法

    Institute of Scientific and Technical Information of China (English)

    丁黎; 郝歆愚; 李丽敏; 卞晓洁; 张胜强

    2004-01-01

    目的:建立人血浆中盐酸多奈哌齐的HPC-MS法.方法:血样经饱和NaHCO3碱化后用乙酸乙酯提取,进行HPLC-MS分析,色谱柱为Hypersil ODS(5μm,250mm×4.6 mm),流动相为甲醇-水-三乙胺-冰醋酸(70:30:0.3:0.3),内标为盐酸非洛普,检测离子为m/z 380(多奈哌齐)、m/z 344(内标),裂解电压为120V.结果:在0.2~20ng/ml范围内多奈哌齐与内标峰面积比值与浓度线性关系良好(r=0.9996),最低可定量浓度为0.1 ng/ml,提取回收率为87.52%~90.91%.结论:本实验建立的分析方法灵敏、准确、简便.%AIM and METHOD:A highly sensitive method for quantitation of donepezil in human plasma was established by using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS),with phenopromlamine hydrochloride as the internal standard (I.S.).After alkalizing with saturated sodium bicarbonate,plasma was extracted with ethyl acetate and the extracts were separated by HPLC on a C18 reversed-phase column with methanol-water-acetic acid-triethylamine (70:30:0.3 :0.3,v/v ) as mobile phase.LC-ESI-MS was performed in the selected ion monitoring (SIM) mode using target ions at m/z 380 for donepezil and m/z 344 for the I.S..RESULT:Calibration curves,which were linear over the range of 0.2 to 20 ng/ ml,were established contemporaneously with the analyses of each batch of samples,along with low (0.2 ng/ml),medium (2 ng/ml) and high (20 rng/ml) quality control samples.The intra and inter-assay variability ranged from 1.25% to 9.84% for the low,medium and high quality control samples.The extraction recovery of donepezil from plasma was in the range of 87.5% ~ 91.9%.CONCLUSION:The method has been used successfully to study donepezil pharmacokinetics in human plasma.

  1. Efficiency and safety assessment of donepezil for treating mild and moderate Alzheimer disease%多奈哌齐治疗轻中度阿尔茨海默病的效能及其安全性评估

    Institute of Scientific and Technical Information of China (English)

    彭丹涛; 许贤豪; 王鲁宁

    2005-01-01

    BACKGROUND: As the second anti-Alzheimer disease drug approved by Food and Drug Administration(FDA), donepezil (Aricept) has been applied in European and American market. According to the regulation of Health Ministry of China, it needs conducting clinical trial of multiple center nationwide in order to come into Chinese market.OBJECTIVE: To evaluate the efficiency and safety of donepezil on treating mild and moderate Alzheimer disease (AD).DESIGN: Randomized, single blind and placebo control prospective study based on patients.SETTING: Neurological Department of Peking Hospital and Neurological Department of the 301 Hospital of Chinese PLA, and ect.PARTICIPANTS: Totally 188 patients with mild and moderate AD[with mini-mental state examination(MMSE) score of 10 to 24 points] from 15 big hospitals of Beijng, Shanghai and Guangzhou were conducted 12 weeks'clinical trial, among which 89 cases were of single blind and placebo control study while 99 cases were of self-controlled study. All the cases met the AD diagnostic standard of clinical neurology, linguistic dysfunction and stroke(NINCDS-ADRDA) and the 4th edition of Statistic Manual (DSM-IVR).INTERVENTIONS: Donepezil (5 rmg/tablet, ip, 5 rmg/time) or placebo with same color, shape, flavor and size with donepezil ( ip, 1 tablet/time)was taken orally for 12 consecutive weeks.MAIN OUTCOME MEASURES: MMSE, clinical dementia rating scale(CDR), activities of daily life scale(ADL), biochemical parameters, electrocardiograph(ECG) and chest x-ray were conducted once every 4 weeks before and after treatment.RESULTS: The random, single blind and placebo control study showed that the score of MMSE, CDR and ADL was greatly improved in donepezil group after 12 weeks' treatment when comparing with placebo group(P < 0. 01,0.05, 0.01 ). Self-controlled study showed that the score of MMSE, CRD and ADL in donepezil group after 12 weeks' treatment increased 3.5, 0.6 and 7.1 points respectively compared with those before treatment

  2. Trifluridine and Tipiracil Hydrochloride

    Science.gov (United States)

    This page contains brief information about trifluridine and tipiracil hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  3. Bivirkninger som årsag til seponering af donepezil ved Alzheimers demens

    DEFF Research Database (Denmark)

    Carøe, Tanja Korfitsen; Moe, Claus

    2009-01-01

    INTRODUCTION: The objective was to investigate the frequency of adverse events (AE) as a cause for discontinuation of donepezil treatment for Alzheimer's dementia (DAT) in a geriatric memory unit. MATERIAL AND METHODS: Five-year retrospective study of 123 donepezil-treated patients diagnosed...... with DAT or mixed dementia in a geriatric memory unit. The material covers all patients treated with donepezil and surveyed for 12 months in the memory unit during the period from 14th March 2001 to 7th April 2006. RESULTS: Among the 123 patients, 106 (86%) suffered from DAT and 17 (14%) suffered from...

  4. Safety and tolerability of donepezil 23 mg in moderate to severe Alzheimer's disease

    Directory of Open Access Journals (Sweden)

    Zou Heng

    2011-05-01

    Full Text Available Abstract Background Donepezil 23 mg/d, recently approved in the United States for treatment of moderate to severe Alzheimer's disease (AD, was developed to address the need for an additional treatment option for patients with advanced AD. This report, based on a pivotal phase 3 study, presents a detailed analysis of the safety and tolerability of increasing donepezil to 23 mg/d compared with continuing 10 mg/d. Method Safety analyses comprised examination of the incidence, severity, and timing of treatment-emergent adverse events (AEs and their relationship to treatment initiation; changes in weight, electrocardiogram, vital signs, and laboratory parameters; and the incidence of premature study discontinuation. The analysis population (n = 1434 included all randomized patients who took at least 1 dose of study drug and had a postbaseline safety assessment. To further examine the effect of transition from a lower to a higher donepezil dose, a pooled analysis of safety data from 2 phase 3 trials of donepezil 5 mg/d and 10 mg/d was also performed. Results The safety population comprised 1434 patients: donepezil 23 mg/d (n = 963; donepezil 10 mg/d (n = 471; completion rates were 71.1% and 84.7%, respectively. The most common AEs were nausea, vomiting, and diarrhea (donepezil 23 mg/d: 11.8%, 9.2%, 8.3%; donepezil 10 mg/d: 3.4%, 2.5%, 5.3%, respectively. AEs that contributed most to early discontinuations were vomiting (2.9% of patients in the 23 mg/d group and 0.4% in the 10 mg/d group, nausea (1.9% and 0.4%, diarrhea (1.7% and 0.4%, and dizziness (1.1% and 0.0%. The percentages of patients with AEs in the 23 mg/d group, as well as the timing, type, and severity of these AEs, were similar to those seen in previous donepezil trials with titration from 5 to 10 mg/d. Serious AEs were uncommon (23 mg/d, 8.3%; 10 mg/d, 9.6%. Discussion The 23 mg/d dose of donepezil was associated with typical cholinergic AEs, particularly gastrointestinal-related AEs

  5. Donepezil, an acetylcholinesterase inhibitor against Alzheimer's dementia, promotes angiogenesis in an ischemic hindlimb model.

    Science.gov (United States)

    Kakinuma, Yoshihiko; Furihata, Mutsuo; Akiyama, Tsuyoshi; Arikawa, Mikihiko; Handa, Takemi; Katare, Rajesh G; Sato, Takayuki

    2010-04-01

    Our recent studies have indicated that acetylcholine (ACh) protects cardiomyocytes from prolonged hypoxia through activation of the PI3K/Akt/HIF-1alpha/VEGF pathway and that cardiomyocyte-derived VEGF promotes angiogenesis in a paracrine fashion. These results suggest that a cholinergic system plays a role in modulating angiogenesis. Therefore, we assessed the hypothesis that the cholinergic modulator donepezil, an acetylcholinesterase inhibitor utilized in Alzheimer's disease, exhibits beneficial effects, especially on the acceleration of angiogenesis. We evaluated the effects of donepezil on angiogenic properties in vitro and in vivo, using an ischemic hindlimb model of alpha7 nicotinic receptor-deleted mice (alpha7 KO) and wild-type mice (WT). Donepezil activated angiogenic signals, i.e., HIF-1alpha and VEGF expression, and accelerated tube formation in human umbilical vein endothelial cells (HUVECs). ACh and nicotine upregulated signal transduction with acceleration of tube formation, suggesting that donepezil promotes a common angiogenesis pathway. Moreover, donepezil-treated WT exhibited rich capillaries with enhanced VEGF and PCNA endothelial expression, recovery from impaired tissue perfusion, prevention of ischemia-induced muscular atrophy with sustained surface skin temperature in the limb, and inhibition of apoptosis independent of the alpha7 receptor. Donepezil exerted comparably more effects in alpha7 KO in terms of angiogenesis, tissue perfusion, biochemical markers, and surface skin temperature. Donepezil concomitantly elevated VEGF expression in intracardiac endothelial cells of WT and alpha7 KO and further increased choline acetyltransferase (ChAT) protein expression, which is critical for ACh synthesis in endothelial cells. The present study concludes that donepezil can act as a therapeutic tool to accelerate angiogenesis in cardiovascular disease patients.

  6. The Effects of Donepezil on 15-Item Geriatric Depression Scale Structure in Patients with Alzheimer Disease

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    Youngsoon Yang

    2016-09-01

    Full Text Available Background/Aims: In Alzheimer disease (AD, depression is among the most common accompanying neuropsychiatric symptoms and has different clinical manifestations when compared with early-life depression. In patients with drug-naïve AD, we tried to explore the structure of the 15-item Geriatric Depression Scale (GDS15 and the effect of donepezil on these substructures. Methods: GDS15, cognitive function, and activities of daily living function tests were administered to 412 patients with probable AD who had not been medicated before visiting the hospital. Using principal component analysis, three factors were identified. The patients with AD who received only donepezil were retrospectively analyzed and we compared the change of cognition and GDS15 subgroup after donepezil medication. Results: Our study identified three factors and revealed that the GDS15 may be comprised of a heterogeneous scale. The Barthel index was significantly correlated with factor 1 (positively and factor 2 (negatively. The Korean version of the MMSE (K-MMSE was significantly correlated with factor 2 and factor 3. Compared to the baseline state, K-MMSE and GDS15 showed significant improvement after taking donepezil. Among GDS15 subgroups, factor 2 and factor 3 showed significant improvement after donepezil treatment. Conclusions: These results suggest that the GDS15 may be comprised of a heterogeneous scale and donepezil differentially affects the GDS15 subgroup in AD.

  7. The Effects of Donepezil on 15-Item Geriatric Depression Scale Structure in Patients with Alzheimer Disease

    Science.gov (United States)

    Yang, Youngsoon; Kwak, Yong Tae

    2016-01-01

    Background/Aims In Alzheimer disease (AD), depression is among the most common accompanying neuropsychiatric symptoms and has different clinical manifestations when compared with early-life depression. In patients with drug-naïve AD, we tried to explore the structure of the 15-item Geriatric Depression Scale (GDS15) and the effect of donepezil on these substructures. Methods GDS15, cognitive function, and activities of daily living function tests were administered to 412 patients with probable AD who had not been medicated before visiting the hospital. Using principal component analysis, three factors were identified. The patients with AD who received only donepezil were retrospectively analyzed and we compared the change of cognition and GDS15 subgroup after donepezil medication. Results Our study identified three factors and revealed that the GDS15 may be comprised of a heterogeneous scale. The Barthel index was significantly correlated with factor 1 (positively) and factor 2 (negatively). The Korean version of the MMSE (K-MMSE) was significantly correlated with factor 2 and factor 3. Compared to the baseline state, K-MMSE and GDS15 showed significant improvement after taking donepezil. Among GDS15 subgroups, factor 2 and factor 3 showed significant improvement after donepezil treatment. Conclusions These results suggest that the GDS15 may be comprised of a heterogeneous scale and donepezil differentially affects the GDS15 subgroup in AD.

  8. Concentration of Donepezil in the Cerebrospinal Fluid of AD Patients: Evaluation of Dosage Sufficiency in Standard Treatment Strategy

    OpenAIRE

    Valis, Martin; Masopust, Jiri; Vysata,Oldrich; Hort, Jakub; Dolezal, Rafael; Tomek, Jiri; Misik, Jan; Kuca, Kamil; Karasova, Jana Zdarova

    2016-01-01

    Although some studies have described the pharmacokinetics and pharmacodynamics of donepezil in the peripheral compartment, studies focused on drug transport across the blood–brain barrier are still very rare. To our knowledge, the fluctuation in the cerebrospinal fluid concentration of donepezil after administration of the drug has not been described in the literature so far. We recruited 16 patients regularly taking a standard therapeutic dose of donepezil (10 mg per day). All patients (Cauc...

  9. Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers

    Directory of Open Access Journals (Sweden)

    Kim YH

    2015-03-01

    Full Text Available Yo Han Kim,1 Hee Youn Choi,1 Hyeong-Seok Lim,1 Shi Hyang Lee,1 Hae Sun Jeon,1 Donghyun Hong,2 Seong Su Kim,2 Young Kweon Choi,2 Kyun-Seop Bae1 1Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Republic of Korea; 2iCure Pharmaceutical lncorporated, Anseong, Gyeonggi-do, Republic of Korea Background: Donepezil is an acetylcholinesterase inhibitor indicated for Alzheimer’s disease. The aim of this randomized, single-blind, placebo-controlled, single-dose, dose-escalation study was to investigate the safety, tolerability, and pharmacokinetics of the donepezil patch in healthy male subjects. Methods: Each healthy male subject received a single transdermal donepezil patch (72 hours patch-on periods of 43.75 mg/12.5 cm2, 87.5 mg/25 cm2, or 175 mg/50 cm2. Serial blood samples were collected up to 312 hours after patch application. The plasma concentrations of donepezil were determined by using a validated liquid chromatography–tandem mass spectrometry method. Pharmacokinetic parameters were obtained by noncompartmental analysis. Tolerability of the patches and performance of the patches (adhesion, skin irritation, residual donepezil content in the patch were assessed throughout the study. Results: The study was completed by 36 healthy subjects. After patch application, the maximal plasma donepezil concentration (Cmax and the area under the curve (AUC increased in a dose-proportional manner. Median time to Cmax was ~74–76 hours (~2–4 hours after patch removal, and mean t1/2ß was ~63.77–93.07 hours. The average donepezil residue in the patch after 72 hours was ~73.9%–86.7% of the loading dose. There were neither serious adverse events nor adverse events that lead to discontinuation. Skin adhesion of the patch was good in 97.2% of the subjects. All skin irritations after patch removal were mild and were resolved during the study period. Conclusion: The donepezil patch

  10. Safety and Efficacy of Donepezil in Children and Adolescents with Autism: Neuropsychological Measures

    Science.gov (United States)

    Johnson, Cynthia R.; McAuliffe-Bellin, Sarah; Murray, Patricia Jo; Hardan, Antonio Y.

    2011-01-01

    Abstract Objective There has been recent interest in the use of cognitive enhancing drugs, such as cholinesterase inhibitors, as a possible treatment for executive functioning (EF) deficits in autism spectrum disorder (ASD). The goal of this study was to assess the tolerability, safety, and efficacy of donepezil on EF in a sample of children and adolescents with ASD. Method Thirty-four children and adolescents with ASD (age range 8–17 years; IQ >75) were enrolled in a 10-week, double-blind, placebo-controlled trial of donepezil (doses of 5 and 10 mg), followed by a 10-week open label trial for placebo nonresponders. Results The effect of donepezil treatment on EF was examined. Despite improvement on a number of EF measures, no statistically significant between-group differences were found (with gains observed for both the placebo and donepezil groups). Conclusions The results suggest that short-term treatment with donepezil may have limited impact on cognitive functioning in ASD. Future controlled trials may need to consider a longer treatment period to detect significant gains on EF measures. PMID:21309696

  11. Donepezil for treatment of cognitive dysfunction in children with Down syndrome aged 10-17.

    Science.gov (United States)

    Kishnani, Priya S; Heller, James H; Spiridigliozzi, Gail A; Lott, Ira; Escobar, Luis; Richardson, Sharon; Zhang, Richard; McRae, Thomas

    2010-12-01

    The objective of this 10-week, randomized, double-blind, placebo-controlled multicenter study was to assess the efficacy and safety of donepezil for the treatment of cognitive dysfunction exhibited by children with Down syndrome (DS). Intervention comprised donepezil (2.5-10 mg/day) in children (aged 10-17 years) with DS of mild-to-moderate severity. The primary measures were the Vineland-II Adaptive Behavior Scales (VABS-II) Parent/Caregiver Rating Form (PCRF) the sum of nine subdomain standardized scores and standard safety measures. Secondary measures included the VABS-II/PCRF scores on the following domains and their respective individual subdomains: Communication (receptive, expressive, and written); Daily Living Skills (personal, domestic, and community); Socialization (interpersonal relationships, play and leisure time, and coping skills), and scores on the Test of Verbal Expression and Reasoning, a subject-performance-based measure of expressive language. At baseline, 129 participants were assigned treatment with donepezil or placebo. During the double-blind phase, VABS II/PCRF sum of the nine subdomain standardized scores, called v-scores, improved significantly from baseline in both groups (P < 0.0001), with no significant between-group differences. This trial failed to demonstrate any benefit for donepezil versus placebo in children and adolescents with DS, although donepezil appeared to be well tolerated. © 2010 Wiley-Liss, Inc.

  12. Effect of donepezil on reversal learning in a touch screen-based operant task.

    Science.gov (United States)

    Chen, Woei-Shin; Wong, Fong-Kuan; Chapman, Paul F; Pemberton, Darrel J

    2009-10-01

    Impairments in reversal learning, which are commonly observed in patients with psychiatric disorders, remain difficult to treat. There is still a debate over the beneficial effects of cholinergic enhancers on improving behavioural flexibility. The objective of this study was to investigate the effect of an acetylcholinesterase inhibitor, donepezil, on the performance of a rodent Probabilistic Reversal Learning task. Lister-Hooded rats were trained to retrieve food rewards by discriminating two computer-generated stimuli in an automated touch screen-based operant task. When a steady performance was achieved, the stimulus-reward rule was reversed. Each rat was given a 30-min training session daily for 24 days and donepezil was administered 30 min before each training session. Systemic treatment with donepezil had no effect on trial accuracy of the two-stimulus discrimination training. However, the donepezil group showed enhanced performance in the reversal learning. Our result showed that treatment with donepezil significantly enhanced Probabilistic Reversal Learning performance in healthy animals. On the basis of this finding, the inhibition of the central acetylcholinesterase would seem to be a potential therapeutic approach to treat behavioural inflexibility.

  13. Donepezil rescues spatial learning and memory deficits following traumatic brain injury independent of its effects on neurogenesis.

    Science.gov (United States)

    Yu, Tzong-Shiue; Kim, Ahleum; Kernie, Steven G

    2015-01-01

    Traumatic brain injury (TBI) is ubiquitous and effective treatments for it remain supportive largely due to uncertainty over how endogenous repair occurs. Recently, we demonstrated that hippocampal injury-induced neurogenesis is one mechanism underlying endogenous repair following TBI. Donepezil is associated with increased hippocampal neurogenesis and has long been known to improve certain aspects of cognition following many types of brain injury through unknown mechanisms. By coupling donepezil therapy with temporally regulated ablation of injury-induced neurogenesis using nestin-HSV transgenic mice, we investigated whether the pro-cognitive effects of donepezil following injury might occur through increasing neurogenesis. We demonstrate that donepezil itself enhances neurogenesis and improves cognitive function following TBI, even when injury-induced neurogenesis was inhibited. This suggests that the therapeutic effects of donepezil in TBI occur separately from its effects on neurogenesis.

  14. Broader Considerations of Higher Doses of Donepezil in the Treatment of Mild, Moderate, and Severe Alzheimer's Disease

    Directory of Open Access Journals (Sweden)

    Camryn Berk

    2012-01-01

    Full Text Available Donepezil, a highly selective acetylcholinesterase inhibitor (AChEI, is approved as a symptomatic treatment mild, moderate, and severe Alzheimer's disease (AD. Donepezil exerts its treatment effect through multiple mechanisms of action including nicotinic receptor stimulation, mitigation of excitotoxicity, and influencing APP processing. The use of donepezil at higher doses is justified given the worsening cholinergic deficit as the disease advances. Donepezil has been investigated in several clinical trials of subjects with moderate-to-severe AD. While the side effects are class specific (cholinergically driven, demonstrable benefit has been shown at the 10 mg dose and the 23 mg doses. Here, we review the clinical justification, efficacy, safety, and tolerability of use of donepezil in the treatment of moderate-to-severe AD.

  15. Donepezil rescues spatial learning and memory deficits following traumatic brain injury independent of its effects on neurogenesis.

    Directory of Open Access Journals (Sweden)

    Tzong-Shiue Yu

    Full Text Available Traumatic brain injury (TBI is ubiquitous and effective treatments for it remain supportive largely due to uncertainty over how endogenous repair occurs. Recently, we demonstrated that hippocampal injury-induced neurogenesis is one mechanism underlying endogenous repair following TBI. Donepezil is associated with increased hippocampal neurogenesis and has long been known to improve certain aspects of cognition following many types of brain injury through unknown mechanisms. By coupling donepezil therapy with temporally regulated ablation of injury-induced neurogenesis using nestin-HSV transgenic mice, we investigated whether the pro-cognitive effects of donepezil following injury might occur through increasing neurogenesis. We demonstrate that donepezil itself enhances neurogenesis and improves cognitive function following TBI, even when injury-induced neurogenesis was inhibited. This suggests that the therapeutic effects of donepezil in TBI occur separately from its effects on neurogenesis.

  16. APOE-ɛ4 Carrier Status and Donepezil Response in Patients with Alzheimer's Disease.

    Science.gov (United States)

    Waring, Jeffrey F; Tang, Qi; Robieson, Weining Z; King, David P; Das, Ujjwal; Dubow, Jordan; Dutta, Sandeep; Marek, Gerard J; Gault, Laura M

    2015-01-01

    Previous studies have investigated associations between apolipoprotein E (APOE)-ɛ4 allele status and acetylcholinesterase inhibitor treatment response in patients with Alzheimer's disease. The ability to draw definitive conclusions regarding the effect of APOE-ɛ4 genotype on treatment response has been hindered by inconsistent results among studies and methodological limitations that restrict interpretation of study findings. To determine whether APOE-ɛ4 carrier status influences the magnitude of change in 13-item Alzheimer's Disease Assessment Scale-Cognitive Subscale (ADAS-cog) score associated with acetylcholinesterase inhibitor treatment (i.e., donepezil). Analyses were performed using pooled data from the donepezil and placebo treatment arms of three consecutive, similarly designed, 12-week, multi-national, randomized clinical studies that enrolled patients with mild-to-moderate Alzheimer's disease. Correlations between APOE-ɛ4 carrier status and ADAS-cog scores were evaluated using analysis of covariance. No appreciable interaction between donepezil response and APOE-ɛ4 carrier status or copy number was detected. Both carriers and non-carriers of APOE-ɛ4 who received donepezil experienced significant improvements from baseline in ADAS-cog score versus placebo (p <  0.05). Change from baseline to final observation in the donepezil treatment group was - 2.95 for APOE-ɛ4 carriers and - 4.09 for non-carriers (p = 0.23). In contrast, non-carriers of APOE-ɛ4 in the placebo treatment group exhibited a greater improvement from baseline versus carriers (-2.38 versus - 0.60, p = 0.05). Within this population, APOE genotype had no statistically significant effect on cognitive response to donepezil treatment; however, APOE-ɛ4 allele status was associated with a difference in the magnitude of the change in ADAS-cog of placebo-treated patients.

  17. Treatment with Sildenafil and Donepezil Improves Angiogenesis in Experimentally Induced Critical Limb Ischemia

    Science.gov (United States)

    Constantinescu, Ioana M.; Bolfa, Pompei; Mironiuc, Aurel I.

    2017-01-01

    Objectives. In this study, we aimed to demonstrate the role of sildenafil (an antagonist of phosphodiesterase type 5 (PDE-5)) and donepezil (a specific and reversible inhibitor of acetylcholinesterase (Ach)) in increasing ischemia-induced angiogenesis. Method. Critical limb ischemia was induced by ligation of the common femoral artery followed by ligation of the common iliac artery. The operated animals were divided into 3 groups: receiving sildenafil, receiving donepezil, and surgery alone; the contralateral lower limb was used as a negative control. The results were controlled based on clinical score and Doppler ultrasound. Gastrocnemius muscle samples were taken from all animals, both from the ischemic and nonischemic limb and were used for histopathological and immunohistochemical examination for the evaluation of the number of nuclei/field, endothelial cells (CD31), dividing cells (Ki-67), and vascular endothelial growth factor (VEGFR-3). Results. An increasing tendency of the number of nuclei/field with time was observed both in the case of sildenafil and donepezil treatment. The formation of new capillaries (the angiogenesis process) was more strongly influenced by donepezil treatment compared to sildenafil or no treatment. This treatment significantly influenced the capillary/fiber ratio, which was increased compared to untreated ligated animals. Sildenafil treatment led to a gradual increase in the number of dividing cells, which was significantly compared to the negative control group and compared to the ligation control group. The same effect (increase in the number of Ki-67 positive cells) was more obvious in the case of donepezil treatment. Conclusion. Donepezil treatment has a better effect in ligation-induced ischemia compared to sildenafil, promoting angiogenesis in the first place, and also arteriogenesis.

  18. Effects of donepezil treatment on rat nicotinic acetylcholine receptor levels in vivo and in vitro.

    Science.gov (United States)

    Reid, Richard T; Sabbagh, Marwan N

    2003-12-01

    Research on acetylcholinesterase inhibitors (ChEIs) indicates that long term exposure increases the level of nicotinic acetylcholine receptors (nAChRs) but the effects of donepezil on nAChRs are not well studied. Therefore, we investigated the effects of sub-chronic donepezil administration on nAChRs in rats and rat pheochromocytoma PC-12 cells. Male Sprague Dawley rats were administered donepezil (0.7 and 2.4 micromoles/kg), nicotine (2.5 micromoles/kg) or saline subcutaneously twice daily for 14 days, PC-12 cells were incubated with 10(-6) to 10(-4) M donepezil for 72 hours and nAChR levels were determined by receptor binding assay using the nAChR ligands [3H]-epibatidine (EPI) for non-alpha 7 nAChRs and [3H]-methyllyconitine (MLA) for alpha 7 nAChRs. Chronic donepezil administration at 1.4 micromoles/kg/day and 4.8 micromoles/ kg/day significantly increased [3H]-epibatidine binding in the cortex to 126 +/- 1.3% and 127 +/- 3.2% of the saline control animals, respectively. [3H]-MLA binding in the cortex increased to 114 +/- 4.4% and 124 +/- 2.8% of the control group for the high and low dose groups, respectively. Hippocampal [3H]-EPI binding in the low dose and high dose groups significantly increased to 135 +/- 3.6% and 125 +/- 4.6% of the controls, respectively while there were no changes in the level of [3H]-MLA binding. In striatal homogenates, neither [3H]-EPI nor [3H]-MLA binding were significantly effected at either dose of donepezil. In PC-12 cells, [3H]-EPI binding was increased at the non-physiological 10(-4)M concentration only. There was no effect of donepezil on [3H]-MLA binding at any concentration examined. These results indicate that donepezil increases cortical alpha 7 and non-alpha 7 nAChRs, hippocampal non-alpha 7 nAChRs but does not influence striatal nAChR levels. Furthermore, the lack of an effect on the alpha 7-nAChRs in PC-12 cells suggests that the increase in cortical alpha 7 nAChRs may be an indirect effect of increased acetylcholine

  19. Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Samar I. Faggal

    2012-04-01

    Full Text Available New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl piperazin-1-ylacetylindoline-2,3-dione (IIId was found to be the most potent.

  20. Pharmacological evaluation of [{sup 11}c]donepezil as tracer for visualization of acetylcholinesterase by PET

    Energy Technology Data Exchange (ETDEWEB)

    Vos, F. de E-mail: filipx.devos@rug.ac.be; Santens, P.; Vermeirsch, H.; Dewolf, I.; Dumont, F.; Slegers, G.; Dierckx, R.A.; Reuck, J. de

    2000-11-01

    Donepezil is a highly potent and selective reversible acetylcholinesterase inhibitor. [{sup 11}C]Donepezil is prepared by methylation with [{sup 11}C]CH{sub 3}I of the corresponding 6'-O-desmethylprecursor. Tissue distribution in mice revealed a high uptake in brain and rapid clearance from the blood. Metabolization studies in mice indicated the formation of one {sup 11}C-labeled polar metabolite that didn't penetrate the blood-brain barrier. Regional brain distribution in rabbits didn't reflect the measured achetylcholinesterase distribution in rabbit brain.

  1. Donepezil in the treatment of early post-stroke aphasia:a randomized controlled trial%多奈哌齐治疗早期卒中后失语:随机对照研究

    Institute of Scientific and Technical Information of China (English)

    吴小琴; 刘晓加; 邢一兰; 王心宇

    2013-01-01

    Objective To investigate the effectiveness of donepezil in the treatment of early post-stroke aphasia (PSA).Methods PSA patients within one month after onset were randomly assigned into either a donepezil group or a control group.On the basis of conventional medication,the donepezil group was given hydrochloride donepezil 5 mg/d.The patients were followed-up after 4 week.The efficacy was evaluated by the Aphasia Battery of Chinese (ABC),the National Institute of Health Stroke Scale (NIHSS),the Stroke Aphasic Depression Questionnaire (SADQ),Chinese version,and the Treatment Emergent Symptom Scale (TESS) before and after treatment.Results A total of 48 PSA patients were enrolled in the study.Both the donepezil group and the control group had 24 patients and they all completed the study.There were no significant differences in age,years of education,NIHSS score,SADQ score,stroke duration,as well as the proportions of male,hypertension,diabetes,hyperlipidemia,heart disease,previous stroke or history of transient ischemic attack,smoking alcohol consumption,type of stroke,and lesion site (all P < 0.01).There were significant differences in each language score before and after treatment both in the donepezil group and in the control group (all P <0.01).The difference values of listening comprehension (47.8 ± 24.7 vs.22.0 ± 15.4; t =4.342,P =0.000)and reading comprehension (20.5 ± 14.0 vs.8.1 ± 10.5; t =3.483,P <0.01) scores before and after treatment in the donepezil group were significantly higher than those in the control group,while there were no significant differences in the information quantity of speech,fluency,series language,repetition,naming,and reading scores (all P >0.05).As compared with the control group,there were significant differences in the difference values of the SADQ scores before and after treatment in the donepezil group (6.2 ±6.0 vs.2.5 ±3.0; t =2.717,P=0.009).No serious adverse reactions were observed in both groups.Conclusions On

  2. Donepezil, anti-Alzheimer's disease drug, prevents cardiac rupture during acute phase of myocardial infarction in mice.

    Directory of Open Access Journals (Sweden)

    Mikihiko Arikawa

    Full Text Available BACKGROUND: We have previously demonstrated that the chronic intervention in the cholinergic system by donepezil, an acetylcholinesterase inhibitor, plays a beneficial role in suppressing long-term cardiac remodeling after myocardial infarction (MI. In comparison with such a chronic effect, however, the acute effect of donepezil during an acute phase of MI remains unclear. Noticing recent findings of a cholinergic mechanism for anti-inflammatory actions, we tested the hypothesis that donepezil attenuates an acute inflammatory tissue injury following MI. METHODS AND RESULTS: In isolated and activated macrophages, donepezil significantly reduced intra- and extracellular matrix metalloproteinase-9 (MMP-9. In mice with MI, despite the comparable values of heart rate and blood pressure, the donepezil-treated group showed a significantly lower incidence of cardiac rupture than the untreated group during the acute phase of MI. Immunohistochemistry revealed that MMP-9 was localized at the infarct area where a large number of inflammatory cells including macrophages infiltrated, and the expression and the enzymatic activity of MMP-9 at the left ventricular infarct area was significantly reduced in the donepezil-treated group. CONCLUSION: The present study suggests that donepezil inhibits the MMP-9-related acute inflammatory tissue injury in the infarcted myocardium, thereby reduces the risk of left ventricular free wall rupture during the acute phase of MI.

  3. Donepezil Adherence, Persistence and Time to First Discontinuation in a Three-Year Follow-Up of Older People

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    Henry C. Ndukwe

    2015-12-01

    Full Text Available Background: Donepezil is indicated for the management of mild to moderate dementia, particularly in Alzheimer's disease. Several studies have described low adherence rates with donepezil. Aim: To examine and measure donepezil adherence, persistence and time to first discontinuation in older New Zealanders. Methods: An inception cohort of 1,999 new users of donepezil, aged 65 years or older, were identified from the Pharmaceutical Collections and National Minimum Dataset from 1 November 2010 to 31 December 2013. Kaplan-Meier curves and Cox regression analysis were used to estimate the cumulative probability and risk of time to first discontinuation of donepezil therapy. Results: The mean age of the cohort was 79.5 ± 6.4 years and included 42.7% females. Adherence was high (89.0%, while the proportion of donepezil dispensings (81.0-32.5% declined between 6 and 36 months. Persistence between the 1st and 6th dispensing visit decreased by 19.0%, and 11.0% of the total cohort had a gap of 31 days or more. The adjusted risk of time to first discontinuation in the non-adherent group was 2.2 times (95% CI 1.9-2.6 that of the adherent group. Conclusions: The non-adherent new donepezil users, on average, discontinued faster than the adherent group. Time to first discontinuation in this study was higher compared to discontinuation rates observed in clinical trials.

  4. 多奈哌齐治疗卒中后失语的疗效观察%The efficacy of donepezil for post-stroke aphasia:a pilot case control study

    Institute of Scientific and Technical Information of China (English)

    陈莺; 李焰生; 王智樱; 徐群; 施国文; 林岩

    2010-01-01

    目的 评价多奈哌齐治疗急性卒中后失语的疗效.方法 将60例急性卒中后失语患者分为治疗组和对照组.所有患者接受规范化的脑血管病治疗,治疗组加用盐酸多奈哌齐5 mg/d,共12周.采用西部失语成套测验(WAB)评定疗效.结果 12周后,两组患者的WAB各亚项及失语指数(AQ)得分均较基线值有显著地提高,但治疗组的 AQ 改善程度得分比对照组更为显著[(34.14±17.70)分比(20.69±17.26)分,P=0.004];治疗组在自发言语、听理解、复述和命名各方面的改善程度均大于对照组,达到统计学意义(P<0.05);治疗组中有明显临床改善的患者达60%,而对照组仅为26.7%,差异显著(P=0.009).结论 卒中后3个月内失语患者有不同程度的自然恢复,加用多奈哌齐对自发言语、听理解、复述、命名的恢复可能有促进作用.%Objective To evaluate the efficacy of donepezil for post-stroke aphasia. Methods Sixty patients with acute post-stroke aphasia were divided into treatment group and a control group. All patients had been treated for secondary prevention according to the guideline. The treatment group received donepezil hydrochloride (5 mg/d) for 12 weeks. The efficacy of treatment was measured by comparing the changes of scores of Western Aphasia Battery ( WAB) between baseline and 12 weeks later. Results Compared with the baseline, the changes of scores of all items of WAB and Aphasia Quotient ( AQ) in both group after 12 weeks follow-up were great, however, the change of AQ was significantly greater in donepezil group (34. 14 ± 17. 70) than that in control group (20. 69± 17. 26) (P =0. 004). The patients in donepezil group also showed significant recovery in spontaneous speech, comprehension, repetition, and naming than those in control group (P <0. 05 ). The rate of significant improving in donepezil group was 60. 0% which was significantly greater than that in control group ( 26. 7% ) ( P = 0. 009 ). Conclusion There

  5. Combination treatment in Alzheimer's disease: results of a randomized, controlled trial with cerebrolysin and donepezil.

    Science.gov (United States)

    Alvarez, X Antón; Cacabelos, R; Sampedro, C; Couceiro, V; Aleixandre, M; Vargas, M; Linares, C; Granizo, E; García-Fantini, M; Baurecht, W; Doppler, E; Moessler, H

    2011-08-01

    Treatment with neurotrophic agents might enhance and/or prolong the effects of cholinesterase inhibitors (ChEIs) in Alzheimer's disease (AD). We compared the safety and efficacy of the neurotrophic compound Cerebrolysin (10 ml; n=64), donepezil (10 mg; n=66) and a combination of both treatments (n=67) in mild-to-moderate (mini-mental state examination-MMSE score 12-25) probable AD patients enrolled in a randomized, double-blind trial. Primary endpoints were global outcome (Clinician's Interview-Based Impression of Change plus caregiver input; CIBIC+) and cognition (change from baseline in AD Assessment Scale-cognitive subscale+; ADAS-cog+) at week 28. Changes in functioning (AD Cooperative Study-Activities of Daily Living scale, ADCS-ADL) and behaviour (Neuropsychiatric Inventory, NPI) were secondary endpoints. Treatment effects in cognitive, functional and behavioral domains showed no significant group differences; whereas improvements in global outcome favored Cerebrolysin and the combination therapy. Cognitive performance improved in all treatment groups (mean±SD for Cerebrolysin: -1.7±7.5; donepezil: -1.2±6.1; combination: -2.3±6.0) with best scores in the combined therapy group at all study visits. Cerebrolysin was as effective as donepezil, and the combination of neurotrophic (Cerebrolysin) and cholinergic (donepezil) treatment was safe in mild-to-moderate AD. The convenience of exploring long-term synergistic effects of this combined therapy is suggested.

  6. Study of effects of donepezil and aspirin on working memory in rats using electroconvulsive shock model

    Directory of Open Access Journals (Sweden)

    Rahul M. Manjare

    2014-12-01

    Conclusion: Neuroinflammation plays an important role in the pathophysiology of neurodegenerative disorder like AD. Combination of aspirin with donepezil increased the nootropic and neuroprotective effect of aspirin and thus may hold great clinical significance in such disorders. [Int J Basic Clin Pharmacol 2014; 3(6.000: 1012-1015

  7. A Rare Case of Acute Renal Failure Secondary to Rhabdomyolysis Probably Induced by Donepezil

    Directory of Open Access Journals (Sweden)

    Osman Zikrullah Sahin

    2014-01-01

    Full Text Available Introduction. Acute renal failure (ARF develops in 33% of the patients with rhabdomyolysis. The main etiologic factors are alcoholism, trauma, exercise overexertion, and drugs. In this report we present a rare case of ARF secondary to probably donepezil-induced rhabdomyolysis. Case Presentation. An 84-year-old male patient was admitted to the emergency department with a complaint of generalized weakness and reduced consciousness for two days. He had a history of Alzheimer’s disease for one year and he had taken donepezil 5 mg daily for two months. The patient’s physical examination revealed apathy, loss of cooperation, and decreased muscle strength. Laboratory studies revealed the following: urea: 128 mg/dL; Creatinine 6.06 mg/dL; creatine kinase: 3613 mg/dL. Donepezil was discontinued and the patient’s renal function tests improved gradually. Conclusion. Rhabdomyolysis-induced acute renal failure may develop secondary to donepezil therapy.

  8. Donepezil nanosuspension intended for nose to brain targeting: In vitro and in vivo safety evaluation.

    Science.gov (United States)

    Bhavna; Md, Shadab; Ali, Mushir; Ali, Rashid; Bhatnagar, Aseem; Baboota, Sanjula; Ali, Javed

    2014-06-01

    The present study was to develop donepezil loaded nanosuspension for direct olfactory administration which reaches the brain and determining safety profile in Sprague-Dawley rats. Nanosuspension was prepared by ionic-crosslinking method. The developed nanosuspension was intranasally instilled into the nostrils of rats with the help of cannula (size 18/20) so that drug reached into the brain directly via nose to brain pathway. The nanosuspension had an average size of 150-200nm with a polydispersity index of 0.341. The donepezil concentration was estimated in the brain homogenate using HPLC method. The Cmax showed concentration of donepezil in brain and plasma as 7.2±0.86 and 82.8±5.42ng/ml, respectively, for drug suspension and concentration of donepezil in brain and plasma as 147.54±25.08 and 183.451±13.45ng/ml, respectively, for nanosuspension at same dose of 0.5mg/ml when administered intranasally (pbrain.

  9. Electroanalytical determination of donepezil HCl in tablets and human serum by differential pulse and osteryoung square wave voltammetry at a glassy carbon electrode.

    Science.gov (United States)

    Golcu, A; Ozkan, S A

    2006-09-01

    Donepezil hydrochloride (DNP) is used for the treatment of mild to moderate dementia of the Alzheimer's type. The voltammetric behavior of DNP was studied at a glassy carbon electrode using cyclic, linear sweep, differential pulse (DPV) and square-wave (OSWV) voltammetric techniques. DNP exhibited irreversible anodic waves within the pH range 1.80 and 9.00 in different supporting electrolytes. The peak was characterized as being irreversible and diffusion-controlled. The possible mechanism of the oxidation process is discussed. The current-concentration plot was rectilinear over the range from 1 x 10(-6) to 1 x 10(-4) M in Britton-Robinson buffer at pH 7.0 with a correlation coefficient between 0.997 and 0.999 in supporting electrolyte and human serum samples using the DPV and SWV techniques. The repeatability and reproducibility of the methods for both media (supporting electrolyte and serum sample) were determined. Precision and accuracy of the developed methods were demonstrated by recovery studies. The standard addition method was used for the recovery studies. No electroactive interferences were found in biological fluids from endogenous substances or additives present in tablets. The methods developed were successfully applied to the determination of DNP in tablets and in spiked human serum.

  10. Psychoactive drugs and pilot performance: a comparison of nicotine, donepezil, and alcohol effects.

    Science.gov (United States)

    Mumenthaler, Martin S; Yesavage, Jerome A; Taylor, Joy L; O'Hara, Ruth; Friedman, Leah; Lee, Hana; Kraemer, Helena C

    2003-07-01

    The cholinergic system plays a major role in cognitive abilities that are essential to piloting an aircraft: attention, learning, and memory. In previous studies, drugs that enhance the cholinergic system through different pharmacologic mechanisms have shown beneficial effects on cognition; but dissimilar cognitive measures were used and samples were not comparable. A comparison within the same cognitive tasks, within comparable samples appears desirable. Toward this aim, we compared effect sizes (ES) of performance-enhancing doses of nicotine (a nicotinic receptor agonist) and donepezil (an acetylcholinesterase inhibitor) as found in our prior work on pilot performance. We also compared cholinergic ES to those of performance-impairing doses of alcohol. In three randomized, placebo-controlled trials, we assessed the flight performance of aircraft pilots in a Frasca 141 simulator, testing I: the acute effects of nicotine gum 2 mg; II: the effects of administration of 5 mg donepezil/day for 30 days; and III: the acute and 8 h-carryover effects of alcohol after a target peak BAC of 0.10%. We calculated the ES of nicotine, donepezil, and alcohol on a flight summary score and on four flight component scores. Compared to placebo, nicotine and donepezil significantly improved, while alcohol significantly impaired overall flight performance: ES (nicotine)=0.80; ES (donepezil)=1.02; ES (alcohol acute)=-3.66; ES (alcohol 8 h)=-0.82. Both cholinergic drugs showed the largest effects on flight tasks requiring sustained visual attention. Although the two tested cholinergic drugs have different pharmacologic mechanisms, their effects on flight performance were similar in kind and size. The beneficial effects of the cholinergic drugs on overall flight performance were large and the absolute (ie nondirectional) sizes were about one-fourth of the absolute ES of acute alcohol intoxication and roughly the same as the absolute 8 h-carryover ES of alcohol.

  11. Efficacy Of Rivastigmine And Donepezil On Cognitive Impairment Of Vascular Dementia - Some Preliminary Observations

    Directory of Open Access Journals (Sweden)

    Jha S

    2004-01-01

    Full Text Available Background: Vascular Dementia (VaD is common, global, disabling and a rather neglected, age related dementia. It is important to identify and treat it since cognitive impairment produces dysfunction in occupational and social life. Moreso, due to increase in geriatric population, incidence and prevalence of VaD is also increasing. Aim: We share our observations on efficacy of Rivastigmine and Donepezil (drugs advocated for improving cognition in dementia in patients of VaD. Material and Method: This was a non-randomized study based on clinical evaluation. We selected 53 patients suffering from VaD (as per clinical and radiological criteria. Their age range was 55-78 years (mean 65.3 + 6.2 yrs. Clinical, biochemical and radiological (Cranial CT and MRI evaluation was done to establish etiology. Cognition was measured using modified Mini Mental State Examination (MMSE which was repeated 2 times, at interval of 3 months. We observed the role of Rivastigmine in 14 and Donepezil in 19 patients of VaD. The change in MMSE score was compared with 20 control patients of VaD. The associated risk factors like hypertension, diabetes, hyperlipidemia etc. were managed. Acetyl Salicylic Acid (ASA in dose of 150mg/day was given as an antiplatelet agent to all 53 patients in this study. Results: At end of study, no statistically significant improvement was observed in MMSE score in any of the 53 patients. Improvement in MMSE score (though statistically insignificant was observed with Rivastigmine in 11 and with Donepezil in 14 patients. Progressive decline in MMSE score was observed in 14 (70% control patients of VaD who did not receive rivastigmine or donepezil. Conclusion - Rivastigmine and Donepezil are beneficial in halting deterioration of dementia in patients suffering from VaD.

  12. Conformational analysis and parallel QM/MM X-ray refinement of protein bound anti-Alzheimer drug donepezil.

    Science.gov (United States)

    Fu, Zheng; Li, Xue; Miao, Yipu; Merz, Kenneth M

    2013-12-03

    The recognition and association of donepezil with acetylcholinesterase (AChE) has been extensively studied in the past several decades because of the former's use as a palliative treatment for mild Alzheimer disease. Herein we examine the conformational properties of donepezil and we re-examine the donepezil-AChE crystal structure using combined quantum mechanical/molecular mechanical (QM/MM) X-ray refinement tools. Donepezil's conformational energy surface was explored using the M06 suite of density functionals and with the MP2/complete basis set (CBS) method using the aug-cc-pVXZ (X = D and T) basis sets. The donepezil-AChE complex (PDB 1EVE) was also re-refined through a parallel QM/MM X-ray refinement approach based on an in-house ab initio code QUICK, which uses the message passing interface (MPI) in a distributed SCF algorithm to accelerate the calculation via parallelization. In the QM/MM re-refined donepezil structure, coordinate errors that previously existed in the PDB deposited geometry were improved leading to an improvement of the modeling of the interaction between donepezil and the aromatic side chains located in the AChE active site gorge. As a result of the re-refinement there was a 93% reduction in the donepezil conformational strain energy versus the original PDB structure. The results of the present effort offer further detailed structural and biochemical inhibitor-AChE information for the continued development of more effective and palliative treatments of Alzheimer disease.

  13. Spectroscopic studies of solid-state forms of donepezil free base and salt forms with various salicylic acids

    Science.gov (United States)

    Brittain, Harry G.

    2014-12-01

    The polymorphic forms of donepezil free base have been studied using X-ray powder diffraction, Fourier transform infrared absorption spectroscopy, and differential scanning calorimetry. None of the free base crystal forms was observed to exhibit detectable fluorescence in the solid state under ambient conditions. Crystalline salt products were obtained by the reaction of donepezil with salicylic and methyl-substituted salicylic acids, with the salicylate and 4-methylsalicylate salts being obtained as non-solvated products, and the 3-methylsalicylate and 5-methylsalicylate salts being obtained as methanol solvated products. The intensity of solid-state fluorescence from donepezil salicylate and donepezil 4-methylsalicylate was found to be reduced relative to the fluorescence intensity of the corresponding free acids, while the solid-state fluorescence intensity of donepezil 3-methylsalicylate methanolate and donepezil 5-methylsalicylate methanolate was greatly increased relative to the fluorescence intensity of the corresponding free acids. Desolvation of the solvated salt products led to formation of glassy solids that exhibited strong green fluorescence.

  14. Cholinergic PET imaging in infections and inflammation using 11C-donepezil and 18F-FEOBV

    DEFF Research Database (Denmark)

    Jørgensen, Nis Pedersen; Alstrup, Aage Kristian Olsen; Mortensen, Frank Viborg

    2016-01-01

    of inflammation has not previously been investigated. Methods We performed positron emission tomography (PET) using the glucose analogue 18F-FDG, and 11C-donepezil and 18F-FEOBV, markers of acetylcholinesterase and the vesicular acetylcholine transporter, respectively. Mice were inoculated subcutaneously...... and remained stable. The 11C-donepezil and 18F-FEOBV uptake displayed progressive increase, and at 120–144 h was nearly at the FDG level. Moderate 11C-donepezil and slightly lower 18F-FEOBV uptake were seen in pig abscesses. PCR analyses suggested that the 11C-donepezil signal in inflammatory cells is derived...... from both acetylcholinesterase and sigma-1 receptors. In humans, very high 11C-donepezil uptake was seen in a lobar pneumonia and in peri-tumoral inflammation surrounding a non-small cell lung carcinoma, markedly superseding the 18F-FDG uptake in the inflammation. In a renal clear cell carcinoma no 11C-donepezil...

  15. Cholinergic PET imaging in infections and inflammation using 11C-donepezil and 18F-FEOBV

    DEFF Research Database (Denmark)

    Jørgensen, Nis Pedersen; Alstrup, Aage Kristian Olsen; Mortensen, Frank Viborg

    2017-01-01

    of inflammation has not previously been investigated. Methods We performed positron emission tomography (PET) using the glucose analogue 18F-FDG, and 11C-donepezil and 18F-FEOBV, markers of acetylcholinesterase and the vesicular acetylcholine transporter, respectively. Mice were inoculated subcutaneously...... and remained stable. The 11C-donepezil and 18F-FEOBV uptake displayed progressive increase, and at 120–144 h was nearly at the FDG level. Moderate 11C-donepezil and slightly lower 18F-FEOBV uptake were seen in pig abscesses. PCR analyses suggested that the 11C-donepezil signal in inflammatory cells is derived...... from both acetylcholinesterase and sigma-1 receptors. In humans, very high 11C-donepezil uptake was seen in a lobar pneumonia and in peri-tumoral inflammation surrounding a non-small cell lung carcinoma, markedly superseding the 18F-FDG uptake in the inflammation. In a renal clear cell carcinoma no 11C-donepezil...

  16. Clinical Recommendations for the Use of Donepezil 23 mg in Moderate-to-Severe Alzheimer's Disease in the Asia-Pacific Region

    Science.gov (United States)

    Sabbagh, Marwan; Han, SeolHeui; Kim, SangYun; Na, Hae-Ri; Lee, Jae-Hong; Kandiah, Nagaendran; Phanthumchinda, Kammant; Suthisisang, Chuthamanee; Senanarong, Vorapun; Pai, Ming-Chyi; Narilastri, Diatri; Sowani, Ajit M.; Ampil, Encarnita; Dash, Amitabh

    2016-01-01

    Background The ‘Asia-Pacific Expert Panel (APEX) for donepezil 23 mg’ met in November 2015 to review evidence for the recently approved high dose of donepezil and to provide recommendations to help physicians in Asia make informed clinical decisions about using donepezil 23 mg in patients with moderate-to-severe Alzheimer's disease (AD). Summary In a global phase III study (study 326) in patients with moderate-to-severe AD, donepezil 23 mg/day demonstrated significantly greater cognitive benefits versus donepezil 10 mg/day, with a between-treatment difference in mean change in the Severe Impairment Battery score of 2.2 points (p < 0.001) in the overall population and 3.1 points (p < 0.001) in patients with advanced AD. A subanalysis of study 326 demonstrated that the benefits and risks associated with donepezil 23 mg/day versus donepezil 10 mg/day in Asian patients with moderate-to-severe AD were comparable to those in the global study population. Key Message Donepezil 23 mg is a valuable treatment for patients with AD, particularly those with advanced disease. The APEX emphasized the importance of patient selection (AD severity, tolerability of lower doses of donepezil, and absence of contraindications), a stepwise titration strategy for dose escalation, and appropriate monitoring and counseling of patients and caregivers in the management of patients with AD. PMID:27703471

  17. Quantitation of donepezil and its active metabolite 6-O-desmethyl donepezil in human plasma by a selective and sensitive liquid chromatography-tandem mass spectrometric method

    Energy Technology Data Exchange (ETDEWEB)

    Patel, Bhavin N. [Chemistry Department, School of Sciences, Gujarat University, Navrangpura, Ahmedabad 380 009, Gujarat (India); Analytical Laboratory, BA Research India Ltd., Bodakdev, Ahmedabad 380 054, Gujarat (India); Sharma, Naveen [Analytical Laboratory, BA Research India Ltd., Bodakdev, Ahmedabad 380 054, Gujarat (India); Sanyal, Mallika [Chemistry Department, St. Xaviers' College, Navrangpura, Ahmedabad 380 009, Gujarat (India); Shrivastav, Pranav S. [Chemistry Department, School of Sciences, Gujarat University, Navrangpura, Ahmedabad 380 009, Gujarat (India)], E-mail: pranav_shrivastav@yahoo.com

    2008-11-23

    A sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay for the simultaneous determination of donepezil (D) and its pharmacologically active metabolite, 6-O-desmethyl donepezil (6-ODD) in human plasma is developed using galantamine as internal standard (IS). The analytes and IS were extracted from 500 {mu}L aliquots of human plasma via solid-phase extraction (SPE) on Waters Oasis HLB cartridges. Chromatographic separation was achieved in a run time of 6.0 min on a Waters Novapak C18 (150 mm x 3.9 mm, 4 {mu}m) column under isocratic conditions. Detection of analytes and IS was done by tandem mass spectrometry, operating in positive ion and multiple reaction monitoring (MRM) acquisition mode. The protonated precursor to product ion transitions monitored for D, 6-ODD and IS were at m/z 380.1 {yields} 91.2, 366.3 {yields} 91.3 and 288.2 {yields} 213.2, respectively. The method was fully validated for its selectivity, interference check, sensitivity, linearity, precision and accuracy, recovery, matrix effect, ion suppression/enhancement, cross-specificity, stability and dilution integrity. A linear dynamic range of 0.10-50.0 ng mL{sup -1} for D and 0.02-10.0 ng mL{sup -1} for 6-ODD was evaluated with mean correlation coefficient (r) of 0.9975 and 0.9985, respectively. The intra-batch and inter-batch precision (%CV, coefficient of variation) across five quality control levels was less than 7.5% for both the analytes. The method was successfully applied to a bioequivalence study of 10 mg donepezil tablet formulation in 24 healthy Indian male subjects under fasting condition.

  18. Donepezil: A cause of inadequate muscle relaxation and delayed neuromuscular recovery

    Directory of Open Access Journals (Sweden)

    Alka Bhardwaj

    2011-01-01

    Full Text Available A 74-year-old female with diabetes mellitus type II and Alzheimer′s disease, taking donepezil for 4 months was operated for right modified radical mastectomy under general anesthesia. During the procedure a higher dose of non-depolarizing muscle relaxant was required than those recommended for her age yet the muscle relaxation was inadequate intra-operatively. Residual neuromuscular blockade persisted postoperatively, due to the cumulative effect of large doses of non-depolarizing muscle relaxant, needing post-operative ventilatory assistance. After ruling out other causes of resistance to non-depolarizing muscle relaxants, we concluded that acetylcholinesterase inhibitor donepezil was primarily responsible for inadequate muscle relaxation and delayed post-operative neuromuscular recovery.

  19. GOOD or BAD Responder? Behavioural and Neuroanatomical Markers of Clinical Response to Donepezil in Dementia

    Directory of Open Access Journals (Sweden)

    Gabriella Bottini

    2012-01-01

    Full Text Available We explored the neuropsychological and neuromorphometrical differences between probable Alzheimer's disease patients showing a good or a bad response to nine months treatment with donepezil. Before treatment, the neuropsychological profile of the two patient groups was perfectly matched. By the ninth month after treatment, the BAD-responders showed a decline of the MMSE score together with a progressive impairment of executive functions. A voxel-based morphometry investigation (VBM, at the time of the second neuropsychological assessment, showed that the BAD-responders had larger grey and white matter atrophies involving the substantia innominata of Meynert bilaterally, the ventral part of caudate nuclei and the left uncinate fasciculus, brain areas belonging to the cholinergic pathways. A more widespread degeneration of the central cholinergic pathways may explain the lack of donepezil efficacy in those patients not responding to a treatment that operates on the grounds that some degree of endogeneous release of acetylcholine is still available.

  20. Olfactory Deficits in MCI as Predictor of Improved Cognition on Donepezil

    Science.gov (United States)

    2016-06-01

    analyses we will count donepezil dropouts with subsequent time -point assessments handled as planned originally under the intent-to-treat principle...Alzheimer’s Disease Assessment Scale- Cognitive subscale variants in mild cognitive impairment and mild Alzheimer’s disease: change over time and the effect...Award Number: W81XWH-12-1-0142 TITLE: “Olfactory Deficits in MCI as Predictor of Improved Cognition on Donepezil” PRINCIPAL INVESTIGATOR: Dr

  1. Donepezil Treatment of Older Adults with Cognitive Impairment and Depression (DOTCODE study): clinical rationale and design

    Science.gov (United States)

    Pelton, Gregory H.; Andrews, Howard; Roose, Steven P.; Marcus, Sue M.; D’Antonio, Kristina; Husn, Hala; Petrella, Jeffrey R.; Zannas, Anthony S.; Doraiswamy, P. Murali; Devanand, D. P.

    2014-01-01

    Treatment strategies for patients with depression and cognitive impairment (DEP-CI), who are at high risk to develop a clinical diagnosis of dementia, are not established. This issue is addressed in the donepezil treatment of cognitive impairment and depression (DOTCODE) pilot clinical trial. The DOTCODE study is the first long-term treatment trial that assesses differences in conversion to dementia and cognitive change in DEP-CI patients using a study design of open antidepressant medication plus add-on randomized, double-blind, placebo-controlled treatment with the acetylcholinesterase inhibitor donepezil. In Phase 1, DEP-CI patients receive optimized antidepressant treatment for 16 weeks. In Phase 2, antidepressant treatment is continued with the addition of randomized, double-blind treatment with donepezil or placebo. The total study duration for each patient is 78 weeks (18 months). Eighty DEP-CI outpatients (age 55 to 95 years) are recruited: 40 at New York State Psychiatric Institute/Columbia University and 40 at Duke University Medical Center. The primary outcome is conversion to a clinical diagnosis of dementia. The secondary outcomes are cognitive change scores in Selective Reminding Test (SRT) total recall and the modified Alzheimer’s Disease Assessment Scale (ADAS-cog). Other key assessments include the 24-item Hamilton Depression Rating Scale and antidepressant response; Clinical Global Impression (CGI) for depression, cognition, and global status; neuropsychological test battery for diagnosis; informant report of functional abilities (Pfeffer FAQ); Treatment Emergent Symptom Scale (TESS) for somatic side effects. Apolipoprotein E ε4 status, odor identification deficits, and MRI entorhinal/hippocampal cortex atrophy at baseline are evaluated as neurobiological moderators of donepezil treatment effects. PMID:24315979

  2. Isoflurane-induced spatial memory impairment in mice is prevented by the acetylcholinesterase inhibitor donepezil.

    Directory of Open Access Journals (Sweden)

    Diansan Su

    Full Text Available Although many studies have shown that isoflurane exposure impairs spatial memory in aged animals, there are no clinical treatments available to prevent this memory deficit. The anticholinergic properties of volatile anesthetics are a biologically plausible cause of cognitive dysfunction in elderly subjects. We hypothesized that pretreatment with the acetylcholinesterase inhibitor donepezil, which has been approved by the Food and Drug Administration (FDA for the treatment of Alzheimer's disease, prevents isoflurane-induced spatial memory impairment in aged mice. In present study, eighteen-month-old mice were administered donepezil (5 mg/kg or an equal volume of saline by oral gavage with a feeding needle for four weeks. Then the mice were exposed to isoflurane (1.2% for six hours. Two weeks later, mice were subjected to the Morris water maze to examine the impairment of spatial memory after exposure to isoflurane. After the behavioral test, the mice were sacrificed, and the protein expression level of acetylcholinesterase (AChE, choline acetylase (ChAT and α7 nicotinic receptor (α7-nAChR were measured in the brain. Each group consisted of 12 mice. We found that isoflurane exposure for six hours impaired the spatial memory of the mice. Compared with the control group, isoflurane exposure dramatically decreased the protein level of ChAT, but not AChE or α7-nAChR. Donepezil prevented isoflurane-induced spatial memory impairments and increased ChAT levels, which were downregulated by isoflurane. In conclusions, pretreatment with the AChE inhibitor donepezil prevented isoflurane-induced spatial memory impairment in aged mice. The mechanism was associated with the upregulation of ChAT, which was decreased by isoflurane.

  3. Protein Expression of BACE1 is Downregulated by Donepezil in Alzheimer's Disease Platelets.

    Science.gov (United States)

    Sarno, Tamires Alves; Talib, Leda Leme; Joaquim, Helena Passarelli Giroud; Bram, Jessyka Maria de França; Gattaz, Wagner Farid; Forlenza, Orestes Vicente

    2017-01-01

    Abnormal amyloid-β protein precursor (AβPP) metabolism is a key feature of Alzheimer's disease (AD). Platelets contain most of the enzymatic machinery required for AβPP processing, and correlates of intracerebral abnormalities have been demonstrated in platelets of patients with AD. Thus, AβPP-related molecules in platelets may be regarded as peripheral markers of AD. We sought to determine the protein expression of the AβPP secretases (ADAM10, BACE1, and PSEN1) and AβPP ratio in platelets of patients with mild or moderate AD compared to healthy controls. We further determined whether the protein expression of these markers might be modified by chronic treatment with donepezil. Platelet samples were obtained from patients and controls at baseline and after 3 and 6 months of continuous treatment with therapeutic doses of donepezil. The protein expression of platelet markers was determined by western blotting. AD patients had a significant decrease in AβPP ratio, ADAM10, and PSEN1 compared to controls at baseline, but these differences were not modified by the treatment. Nonetheless, a significant reduction in the protein expression of BACE1 was observed in patients treated with donepezil for 6 months. Our results corroborate previous findings from our group and others of decreased AβPP ratio and protein expression of ADAM10 in AD. We further show that PSEN1 is decreased in AD platelets, and that the protein expression of BACE1 is downregulated by chronic treatment with donepezil. This effect may be interpreted as evidence of disease modification.

  4. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  5. Evaluating the cost effectiveness of donepezil in the treatment of Alzheimer's disease in Germany using discrete event simulation

    Directory of Open Access Journals (Sweden)

    Hartz Susanne

    2012-02-01

    Full Text Available Abstract Background Previous cost-effectiveness studies of cholinesterase inhibitors have modeled Alzheimer's disease (AD progression and treatment effects through single or global severity measures, or progression to "Full Time Care". This analysis evaluates the cost-effectiveness of donepezil versus memantine or no treatment in Germany by considering correlated changes in cognition, behavior and function. Methods Rates of change were modeled using trial and registry-based patient level data. A discrete event simulation projected outcomes for three identical patient groups: donepezil 10 mg, memantine 20 mg and no therapy. Patient mix, mortality and costs were developed using Germany-specific sources. Results Treatment of patients with mild to moderately severe AD with donepezil compared to no treatment was associated with 0.13 QALYs gained per patient, and 0.01 QALYs gained per caregiver and resulted in average savings of €7,007 and €9,893 per patient from the healthcare system and societal perspectives, respectively. In patients with moderate to moderately-severe AD, donepezil compared to memantine resulted in QALY gains averaging 0.01 per patient, and savings averaging €1,960 and €2,825 from the healthcare system and societal perspective, respectively. In probabilistic sensitivity analyses, donepezil dominated no treatment in most replications and memantine in over 70% of the replications. Donepezil leads to savings in 95% of replications versus memantine. Conclusions Donepezil is highly cost-effective in patients with AD in Germany, leading to improvements in health outcomes and substantial savings compared to no treatment. This holds across a variety of sensitivity analyses.

  6. Normal Hearing Ability but Impaired Auditory Selective Attention Associated with Prediction of Response to Donepezil in Patients with Alzheimer's Disease

    Science.gov (United States)

    Ouchi, Yoshitaka; Meguro, Kenichi; Akanuma, Kyoko; Kato, Yuriko; Yamaguchi, Satoshi

    2015-01-01

    Background. Alzheimer's disease (AD) patients have a poor response to the voices of caregivers. After administration of donepezil, caregivers often find that patients respond more frequently, whereas they had previously pretended to be “deaf.” We investigated whether auditory selective attention is associated with response to donepezil. Methods. The subjects were40 AD patients, 20 elderly healthy controls (HCs), and 15 young HCs. Pure tone audiometry was conducted and an original Auditory Selective Attention (ASA) test was performed with a MoCA vigilance test. Reassessment of the AD group was performed after donepezil treatment for 3 months. Results. Hearing level of the AD group was the same as that of the elderly HC group. However, ASA test scores decreased in the AD group and were correlated with the vigilance test scores. Donepezil responders (MMSE 3+) also showed improvement on the ASA test. At baseline, the responders had higher vigilance and lower ASA test scores. Conclusion. Contrary to the common view, AD patients had a similar level of hearing ability to healthy elderly. Auditory attention was impaired in AD patients, which suggests that unnecessary sounds should be avoided in nursing homes. Auditory selective attention is associated with response to donepezil in AD. PMID:26161001

  7. Molecular imaging of cholinergic processes in prostate cancer using {sup 11}C-donepezil and {sup 18}F-FEOBV

    Energy Technology Data Exchange (ETDEWEB)

    Stokholm, Morten Gersel; Bender, Dirk; Jakobsen, Steen; Froekiaer, Joergen; Borghammer, Per [Aarhus University Hospital, Department of Nuclear Medicine and PET Centre, Aarhus C (Denmark); Hoeyer, Soeren [Aarhus University Hospital, Department of Histopathology, Aarhus C (Denmark); Borre, Michael [Aarhus University Hospital, Department of Urology, Aarhus C (Denmark)

    2016-05-15

    High-grade prostate cancer (PC) displays parasympathetic neoneurogenesis. We investigated the binding of two PET tracers that visualize cholinergic nerves in PC tissue using autoradiography. Prostatectomy tissue was subjected to autoradiography with {sup 11}C-donepezil and {sup 18}F-FEOBV and correlated with Gleason scores (GS). Regions of interest on the autoradiograms were defined and quantified. Tracer binding in cancer tissue regions was compared with that in normal tissue. We included 13 patients with biopsy-verified PC. In particular, {sup 11}C-donepezil uptake was higher in ''high-grade'' PC (GS ≥4 + 3) than in ''low-grade'' PC and benign hyperplasia. {sup 11}C-donepezil uptake ranged from a mean of 56 % higher (GS 3 + 3) to 409 % higher (GS 4 + 4), and {sup 18}F-FEOBV uptake ranged from 67 % higher (GS 3 + 3) to 194 % higher (GS 4 + 5). The uptake of both tracers was higher in PC with a high GS than in PC with a low GS, but the difference was significant only for {sup 11}C-donepezil (p = 0.003). Uptake of PET tracers binding to cholinergic nerves was markedly higher in PC with a high GS than in PC with a low GS. This finding implies that {sup 11}C-donepezil PET/CT may be able to differentiate between low-grade and high-grade PC. (orig.)

  8. Efficacy of Memantine, Donepezil, or Their Association in Moderate-Severe Alzheimer’s Disease: A Review of Clinical Trials

    Directory of Open Access Journals (Sweden)

    Ivana Molino

    2013-01-01

    Full Text Available Background. Acetylcholinesterase (AChE/cholinesterase (ChE inhibitors (Is and memantine are licensed for symptomatic treatment of mild-moderate and moderate-severe forms of Alzheimer’s disease (AD, respectively. High doses of the AChE-I donepezil were licensed in the USA for moderate-severe AD, and the association AChE/ChE-Is plus memantine was proposed for AD at this stage. Objectives. This paper has reviewed evidence from clinical trials of the effectiveness of memantine, donepezil, or the two drugs in association in managing moderate-severe AD. Method. Double-blind, placebo-controlled randomized trials (RCTs using memantine or donepezil alone or in association versus placebo in moderate-severe AD were reviewed. Analysis done in January 2013 considered the years 2007–2012. Results and Conclusion. Only 83 of the 941 papers selected were considered relevant, and only 13 met the criterion of “adequacy and representativeness.” Memantine and donepezil lead to improvements in moderate-to-severe AD and the choice between the compounds should be based on their contraindications more than on disease severity. No evidence was found of advantages of the association of memantine-donepezil. The heterogeneity of conditions explored by RCTs, the relatively short time of observation (24–52 weeks, and the different cognitive assessment tools used did not allow comparing properly different trials.

  9. Community Pharmacists’ Knowledge Regarding Donepezil Averse Effects and Self-Care Recommendations for Insomnia for Persons with AD

    Directory of Open Access Journals (Sweden)

    Marketa Marvanova

    2017-07-01

    Full Text Available Alzheimer’s disease (AD impacts millions of individuals worldwide. Since no cure is currently available, acetylcholinesterase inhibitors are symptomatic therapy. This study assessed community pharmacists’ knowledge regarding donepezil adverse effects (AEs and self-care recommendations for insomnia management for persons with AD treated with rivastigmine. This is a cross-sectional, standardized telephone survey of community pharmacists (n = 862 in three study areas: West Virginia, North Dakota/South Dakota, and Southern Oregon/Northern California. Pharmacists’ degree, sex, and pharmacists’ AD-related knowledge were assessed. In-stock availability of donepezil and rivastigmine formulations was assessed. Analyses were performed using Stata 10.1. Only 31.4% pharmacists were able to name ≥2 donepezil AEs. Only four donepezil AEs were named by at least 13% of pharmacists: nausea (36.1%, dizziness (25.1%, diarrhea (15.0%, and vomiting (13.9%. All other AEs were named by fewer than 7% of respondents. Only 62.9% of pharmacists (n = 542 provided appropriate recommendations: melatonin (40.3%, referral to physician (22.0%, or sleep hygiene (0.6%. Over 12% of pharmacists (n = 107 provided inappropriate recommendations (anticholinergic agent or valerian root and 21.5% of pharmacists were unable to provide any recommendation. We identified significant gaps in community pharmacists’ knowledge regarding donepezil AEs and non-prescription insomnia recommendation needing significant improvement to ensure high-quality AD-related care.

  10. Determination of donepezil in serum samples using molecularly imprinted polymer nanoparticles followed by high-performance liquid chromatography with ultraviolet detection.

    Science.gov (United States)

    Khansari, Mehdi Rajabnia; Bikloo, Shahrzad; Shahreza, Sara

    2016-03-01

    A molecularly imprinted polymer designed for the selective extraction of donepezil from serum samples was synthesized using a noncovalent molecular imprinting approach. The molecularly imprinted polymer was evaluated chromatographically and then its affinity for donepezil was confirmed by solid-phase extraction. The optimal conditions for solid-phase extraction were provided by cartridge conditioning using acidified water purified from a Milli-Q system, sample loading under basic aqueous conditions, clean-up using acetonitrile, and elution with methanol/tetrahydrofuran. Desirable molecular recognition properties of the molecularly imprinted polymer led to good donepezil recoveries (90-102%). The data indicated that the imprinted polymer has a perfect selectivity and affinity for donepezil and could be used for selective extraction and analysis of donepezil in human serum.

  11. Cholinergic PET imaging in infections and inflammation using {sup 11}C-donepezil and {sup 18}F-FEOBV

    Energy Technology Data Exchange (ETDEWEB)

    Joergensen, Nis Pedersen; Hoegsberg Schleimann, Mariane [Aarhus University Hospital, Department of Infectious Diseases, Aarhus (Denmark); Alstrup, Aage K.O.; Knudsen, Karoline; Jakobsen, Steen; Bender, Dirk; Gormsen, Lars C.; Borghammer, Per [Aarhus University Hospital, Department of Nuclear Medicine and PET Centre, Aarhus C (Denmark); Mortensen, Frank V. [Aarhus University Hospital, Department of Gastroenterology, Aarhus (Denmark); Madsen, Line Bille [Aarhus University Hospital, Department of Histopathology, Aarhus (Denmark); Breining, Peter [Aarhus University Hospital, Department of Endocrinology and Metabolism, Aarhus (Denmark); Petersen, Mikkel Steen [Aarhus University Hospital, Department of Clinical Immunology, Aarhus (Denmark); Dagnaes-Hansen, Frederik [Aarhus University, Department of Biomedicine, Aarhus (Denmark)

    2017-03-15

    Immune cells utilize acetylcholine as a paracrine-signaling molecule. Many white blood cells express components of the cholinergic signaling pathway, and these are up-regulated when immune cells are activated. However, in vivo molecular imaging of cholinergic signaling in the context of inflammation has not previously been investigated. We performed positron emission tomography (PET) using the glucose analogue 18F-FDG, and 11C-donepezil and 18F-FEOBV, markers of acetylcholinesterase and the vesicular acetylcholine transporter, respectively. Mice were inoculated subcutaneously with Staphylococcus aureus, and PET scanned at 24, 72, 120, and 144 h post-inoculation. Four pigs with post-operative abscesses were also imaged. Finally, we present initial data from human patients with infections, inflammation, and renal and lung cancer. In mice, the FDG uptake in abscesses peaked at 24 h and remained stable. The 11C-donepezil and 18F-FEOBV uptake displayed progressive increase, and at 120-144 h was nearly at the FDG level. Moderate 11C-donepezil and slightly lower 18F-FEOBV uptake were seen in pig abscesses. PCR analyses suggested that the 11C-donepezil signal in inflammatory cells is derived from both acetylcholinesterase and sigma-1 receptors. In humans, very high 11C-donepezil uptake was seen in a lobar pneumonia and in peri-tumoral inflammation surrounding a non-small cell lung carcinoma, markedly superseding the 18F-FDG uptake in the inflammation. In a renal clear cell carcinoma no 11C-donepezil uptake was seen. The time course of cholinergic tracer accumulation in murine abscesses was considerably different from 18F-FDG, demonstrating in the 11C-donepezil and 18F-FEOBV image distinct aspects of immune modulation. Preliminary data in humans strongly suggest that 11C-donepezil can exhibit more intense accumulation than 18F-FDG at sites of chronic inflammation. Cholinergic PET imaging may therefore have potential applications for basic research into cholinergic

  12. Pharmacist-based Donepezil Outpatient Consultation Service to improve medication persistence

    Directory of Open Access Journals (Sweden)

    Watanabe N

    2012-08-01

    Full Text Available Norio Watanabe,1,2 Keiko Yamamura,3 Yusuke Suzuki,4 Hiroyuki Umegaki,4 Katsuro Shigeno,5 Ryo Matsushita,1 Yoshimichi Sai,1 Ken-ichi Miyamoto,1 Kiyofumi Yamada61Department of Clinical Pharmacy, Graduate School of Natural Science and Technology, Kanazawa University, Kanazawa, Ishikawa, Japan; 2Department of Pharmacy, Hashima Municipal Hospital, Hashima, Gifu, Japan; 3Department of Clinical Pharmacy, School of Pharmacy, Aichi Gakuin University, Nagoya, Aichi, Japan; 4Department of Community Healthcare and Geriatrics, Nagoya University Graduate School of Medicine, Nagoya, Aichi, Japan; 5Department of Pharmacy Practice and Sciences, School of Pharmacy, Aichi Gakuin University, Nagoya, Aichi, Japan; 6Department of Neuropsychopharmacology and Hospital Pharmacy, Nagoya University Graduate School of Medicine, Nagoya, Aichi, JapanAim: Donepezil is widely used to delay the progression of cognitive dysfunction in patients with Alzheimer's disease (AD, but the efficacy of pharmacotherapy is often reduced by poor adherence to medication. In order to improve adherence by providing information about AD and the significance of pharmacotherapy, the Donepezil Outpatient Consultation Service (DOCS was set up. The influence of this service on medication persistence was assessed in the present study.Methods: Among outpatients starting donepezil therapy, we enrolled 59 patients between April 2008 and September 2010 before establishment of the DOCS (non-DOCS group and 52 patients between October 2010 and March 2012 who attended the DOCS (DOCS group. Each patient's and their caregiver's understanding about the clinical features of AD and pharmacotherapy with donepezil were also assessed. Their understanding was compared before and after the DOCS, and the 1-year medication persistence rate and the reasons for discontinuation were also investigated.Results: The 1-year medication persistence rate was significantly higher in the DOCS group than in the non-DOCS group (73

  13. Donepezil impairs memory in healthy older subjects: behavioural, EEG and simultaneous EEG/fMRI biomarkers.

    Directory of Open Access Journals (Sweden)

    Joshua H Balsters

    Full Text Available Rising life expectancies coupled with an increasing awareness of age-related cognitive decline have led to the unwarranted use of psychopharmaceuticals, including acetylcholinesterase inhibitors (AChEIs, by significant numbers of healthy older individuals. This trend has developed despite very limited data regarding the effectiveness of such drugs on non-clinical groups and recent work indicates that AChEIs can have negative cognitive effects in healthy populations. For the first time, we use a combination of EEG and simultaneous EEG/fMRI to examine the effects of a commonly prescribed AChEI (donepezil on cognition in healthy older participants. The short- and long-term impact of donepezil was assessed using two double-blind, placebo-controlled trials. In both cases, we utilised cognitive (paired associates learning (CPAL and electrophysiological measures (resting EEG power that have demonstrated high-sensitivity to age-related cognitive decline. Experiment 1 tested the effects of 5 mg/per day dosage on cognitive and EEG markers at 6-hour, 2-week and 4-week follow-ups. In experiment 2, the same markers were further scrutinised using simultaneous EEG/fMRI after a single 5 mg dose. Experiment 1 found significant negative effects of donepezil on CPAL and resting Alpha and Beta band power. Experiment 2 replicated these results and found additional drug-related increases in the Delta band. EEG/fMRI analyses revealed that these oscillatory differences were associated with activity differences in the left hippocampus (Delta, right frontal-parietal network (Alpha, and default-mode network (Beta. We demonstrate the utility of simple cognitive and EEG measures in evaluating drug responses after acute and chronic donepezil administration. The presentation of previously established markers of age-related cognitive decline indicates that AChEIs can impair cognitive function in healthy older individuals. To our knowledge this is the first study to identify

  14. Donepezil impairs memory in healthy older subjects: behavioural, EEG and simultaneous EEG/fMRI biomarkers.

    Science.gov (United States)

    Balsters, Joshua H; O'Connell, Redmond G; Martin, Mary P; Galli, Alessandra; Cassidy, Sarah M; Kilcullen, Sophia M; Delmonte, Sonja; Brennan, Sabina; Meaney, Jim F; Fagan, Andrew J; Bokde, Arun L W; Upton, Neil; Lai, Robert; Laruelle, Marc; Lawlor, Brian; Robertson, Ian H

    2011-01-01

    Rising life expectancies coupled with an increasing awareness of age-related cognitive decline have led to the unwarranted use of psychopharmaceuticals, including acetylcholinesterase inhibitors (AChEIs), by significant numbers of healthy older individuals. This trend has developed despite very limited data regarding the effectiveness of such drugs on non-clinical groups and recent work indicates that AChEIs can have negative cognitive effects in healthy populations. For the first time, we use a combination of EEG and simultaneous EEG/fMRI to examine the effects of a commonly prescribed AChEI (donepezil) on cognition in healthy older participants. The short- and long-term impact of donepezil was assessed using two double-blind, placebo-controlled trials. In both cases, we utilised cognitive (paired associates learning (CPAL)) and electrophysiological measures (resting EEG power) that have demonstrated high-sensitivity to age-related cognitive decline. Experiment 1 tested the effects of 5 mg/per day dosage on cognitive and EEG markers at 6-hour, 2-week and 4-week follow-ups. In experiment 2, the same markers were further scrutinised using simultaneous EEG/fMRI after a single 5 mg dose. Experiment 1 found significant negative effects of donepezil on CPAL and resting Alpha and Beta band power. Experiment 2 replicated these results and found additional drug-related increases in the Delta band. EEG/fMRI analyses revealed that these oscillatory differences were associated with activity differences in the left hippocampus (Delta), right frontal-parietal network (Alpha), and default-mode network (Beta). We demonstrate the utility of simple cognitive and EEG measures in evaluating drug responses after acute and chronic donepezil administration. The presentation of previously established markers of age-related cognitive decline indicates that AChEIs can impair cognitive function in healthy older individuals. To our knowledge this is the first study to identify the precise

  15. Treatment of post-electroconvulsive therapy delirium and agitation with donepezil.

    Science.gov (United States)

    Logan, Christopher J; Stewart, Jonathan T

    2007-03-01

    Delirium and agitation are commonly encountered after administration of electroconvulsive therapy (ECT). Management is generally fairly straightforward, although some patients may have a severe, prolonged, or refractory course. We recently cared for a 65-year-old man who consistently developed severe and very prolonged post-ECT delirium that did not respond to typical pharmacological agents; the duration of delirium was dramatically shortened by the addition of donepezil. Cholinesterase inhibitors may have a place in mitigating severe and prolonged post-ECT delirium.

  16. Cartap hydrochloride poisoning: A clinical experience

    OpenAIRE

    Hari K Boorugu; Anugrah Chrispal

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular to...

  17. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine... RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222b Ketamine.... Ketamine hydrochloride, (±),-2-(o-chlorophenyl)-2-(methylamino) cyclohexanone hydrochloride, with promazine...

  18. Thermoanalytical Investigation of Terazosin Hydrochloride

    OpenAIRE

    Mona Mohamed Abdel-Moety; Ali Kamal Attia

    2013-01-01

    Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (∆H*), entropy (∆S*) and Gibbs free energy change of the decomp...

  19. Clinical Recommendations for the Use of Donepezil 23 mg in Moderate-to-Severe Alzheimer's Disease in the Asia-Pacific Region

    Directory of Open Access Journals (Sweden)

    Marwan Sabbagh

    2016-09-01

    Full Text Available Background: The ‘Asia-Pacific Expert Panel (APEX for donepezil 23 mg' met in November 2015 to review evidence for the recently approved high dose of donepezil and to provide recommendations to help physicians in Asia make informed clinical decisions about using donepezil 23 mg in patients with moderate-to-severe Alzheimer's disease (AD. Summary: In a global phase III study (study 326 in patients with moderate-to-severe AD, donepezil 23 mg/day demonstrated significantly greater cognitive benefits versus donepezil 10 mg/day, with a between-treatment difference in mean change in the Severe Impairment Battery score of 2.2 points (p Key Message: Donepezil 23 mg is a valuable treatment for patients with AD, particularly those with advanced disease. The APEX emphasized the importance of patient selection (AD severity, tolerability of lower doses of donepezil, and absence of contraindications, a stepwise titration strategy for dose escalation, and appropriate monitoring and counseling of patients and caregivers in the management of patients with AD.

  20. 建立HPLC-ESI-SIM法测定盐酸多奈哌齐在血浆中的含量%To establish an HPLC-ESI-SIM method for the determination of donepezil in human plasma

    Institute of Scientific and Technical Information of China (English)

    李艳翠; 辛华; 高丽

    2012-01-01

    目的:研究盐酸多奈哌齐口服制剂在健康人体的药动学特征及生物等效性,建立HPLC-ESI-SIM方法测定血浆中的盐酸多奈哌齐浓度.方法:以乙哌立松为内标,待测血浆经碱化处理后,经乙酸乙酯进行液-液萃取,采用0DS-2C18柱(250mm×2.0mm,5μm),以甲醇-20mmol/L醋酸溶液(60:40)为流动相,流速0.8mL/min,柱温35℃.采用质谱电喷雾离子源正源(ESI+)将样品离子化,选择性离子监测(SIM)准分子离子峰.结果:多奈哌齐在0.10~ 20.0ng/mL内线性关系良好(r=0.9997),最低定量限为0.1ng/ml.方法回收率为92.9%~98.4%,提取回收率均大于80%,批内与批间RSD均小于10%.结论:该方法简单、快速、灵敏度高、专属性强,适用于人血浆中多奈哌齐浓度的测定及药动学研究.%Objective To study the pharmacokinetics and bioavailability of Donepezil Hydrochloride in healthy volunteers. To establish an HPLC-ESI-SIM method for the determination of donepezil in human plasma. Methods Alkalized plasma was extracted with ethyl acetate and Eperisone was used as internal standard .Solutes were separated on a ODS-2C18 column (250mm×2.0mm,5 μm)with a mobile phase of methanol-20mmol/L Acetic acid solution (60:40),The flow rate was 0.8mL/min and column was used with temperature of 35℃.Donepezil and internal standard were ionized in the eletrospray ionization (ESI+) with positive source of the mass spectrometer and detected in selected ioni2ation monitor (SIM) mode. Results The calibration curve was linear in the range of 0.1-20.0ng/mL (r= 0.9997) with the lower limit of quantitation, accuracy was within 92.9%~98.4%. The recovery of the extraction was more than 80%, intra-and inter-batch precision (RSD) were less than 10%. Conclusion The method is proved to be suitable for pharmacokinetics and determination of donepezil in human plasma with simple.quickness,sensitive and specificity.

  1. Evaluation of the binding characteristics of [5-{sup 11}C-methoxy]donepezil in the rat brain for in vivo visualization of acetylcholinesterase

    Energy Technology Data Exchange (ETDEWEB)

    Funaki, Yoshihito; Iwata, Ren; Ido, Tatsuo [Tohoku Univ., Sendai (Japan). Cyclotron and Radioisotope Center; Kato, Motohisa; Sakurai, Eiko; Tashiro, Manabu; Yanai, Kazuhiko [Tohoku Univ., Sendai (Japan). Graduate School of Medicine; Sakurai, Eiichi [Tohoku Coll. of Pharmacy, Sendai (Japan)

    2003-02-01

    Donepezil, an acetylcholinesterase (AChE) inhibitor, has not been evaluated for its binding characteristics using a radioactive tracer, although its inhibitory action on AChE has been studied. The aim of this research is to examine whether AChE can be visualized in vivo and in vitro with [{sup 11}C]donepezil. [5-{sup 11}C-methoxy]donepezil was synthesized by O-methylation using [{sup 11}C]methyl triflate. The binding of [{sup 11}C]donepezil to brain homogenates was higher in the brain stem and striatum, and it was lowest in the cerebellum. The in vitro autoradiographic study successfully demonstrated the specific binding of [{sup 11}C]donepezil to AChE in the rat brain. The IC{sub 50} value of binding was approximately 10 nM, which is comparable to the reported value for inhibiting enzyme activity (6 nM). Saturation experiments revealed that the B{sub max} and K{sub d} of [{sup 11}C]donepezil binding in vitro are 65 fmol/mg tissue and 39.8 nM, respectively. In accordance with the in vitro bindings, the in vivo distribution of [{sup 11}C]donepezil was heterogeneous in the rat brain. In the blocking experiments, the heterogeneous distribution disappeared in the presence of a large amount of unlabeled donepezil. These data suggest that [5-{sup 11}C-methoxy]donepezil can be potentially useful to image AChE non-invasively in the human brain by positron emission tomography. (author)

  2. Progressive cholinergic decline in Alzheimer's Disease: consideration for treatment with donepezil 23 mg in patients with moderate to severe symptomatology

    Directory of Open Access Journals (Sweden)

    Cummings Jeffrey

    2011-02-01

    Full Text Available Abstract Of the estimated 5.3 million people with Alzheimer's disease in the United States, more than half would be classified as having moderate or severe disease. Alzheimer's disease is a progressive disorder with the moderate to severe stages generally characterized by significant cognitive, functional, and behavioral dysfunction. Unsurprisingly, these advanced stages are often the most challenging for both patients and their caregivers/families. Symptomatic treatments for moderate to severe Alzheimer's disease are approved in the United States and include the acetylcholinesterase inhibitor donepezil and the glutamate receptor antagonist memantine. Progressive symptomatic decline is nevertheless inevitable even with the available therapies, and therefore additional treatment options are urgently needed for this segment of the Alzheimer's disease population. An immediate-release formulation of donepezil has been available at an approved dose of 5-10 mg/d for the past decade. Recently, the United States Food and Drug Administration approved a higher-dose (23 mg/d donepezil formulation, which provides more gradual systemic absorption, a longer time to maximum concentration (8 hours versus the immediate-release formulation (3 hours, and higher daily concentrations. Herein, we review (1 the scientific data on the importance of cholinergic deficits in Alzheimer's disease treatment strategies, (2 the rationale for the use of higher-dose acetylcholinesterase inhibitors in patients with advanced disease, and (3 recent clinical evidence supporting the use of higher-dose donepezil in patients with moderate to severe Alzheimer's disease.

  3. Low dose of donepezil improves gabapentin analgesia in the rat spared nerve injury model of neuropathic pain

    DEFF Research Database (Denmark)

    Folkesson, Anna; Honoré, Per Hartvig; Andersen, Lene Munkholm

    2010-01-01

    the effect of the cholinesterase inhibitor donepezil when administered (1) alone and (2) as low-dose in combination with the first-line recommendation gabapentin. The co-administration studies were performed following single and multiple dosing. Single, parenteral dosing of donepezil (1, 1.5 and 3 mg....../kg s.c.) produced a dose-dependent reversal of the neuropathic pain behaviour. Co-administration of a sub-effective dose of donepezil (0.5 mg/kg s.c.) and low doses of gabapentin (10 and 30 mg/kg s.c.) resulted in a three- to fourfold increase of the analgesic effect, in comparison with gabapentin administered...... alone. Following multiple, oral dosing, gabapentin (25 mg/kg p.o.) was administered once daily over 20 days. Addition of donepezil (1.5 mg/kg p.o.) from day 11 to day 20 resulted in improved analgesia during the period of combination therapy, in comparison with the gabapentin monotherapy period...

  4. Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.

    Science.gov (United States)

    Wu, Ming-Yu; Esteban, Gerard; Brogi, Simone; Shionoya, Masahi; Wang, Li; Campiani, Giuseppe; Unzeta, Mercedes; Inokuchi, Tsutomu; Butini, Stefania; Marco-Contelles, Jose

    2016-10-01

    Currently available drugs against Alzheimer's disease (AD) are only able to ameliorate the disease symptoms resulting in a moderate improvement in memory and cognitive function without any efficacy in preventing and inhibiting the progression of the pathology. In an effort to obtain disease-modifying anti-Alzheimer's drugs (DMAADs) following the multifactorial nature of AD, we have recently developed multifunctional compounds. We herein describe the design, synthesis, molecular modeling and biological evaluation of a new series of donepezil-related compounds possessing metal chelating properties, and being capable of targeting different enzymatic systems related to AD (cholinesterases, ChEs, and monoamine oxidase A, MAO-A). Among this set of analogues compound 5f showed excellent ChEs inhibition potency and a selective MAO-A inhibition (vs MAO-B) coupled to strong complexing properties for zinc and copper ions, both known to be involved in the progression of AD. Moreover, 5f exhibited moderate antioxidant properties as found by in vitro assessment. This compound represents a novel donepezil-hydroxyquinoline hybrid with DMAAD profile paving the way to the development of a novel class of drugs potentially able to treat AD.

  5. DOMINO-AD protocol: donepezil and memantine in moderate to severe Alzheimer's disease – a multicentre RCT

    Directory of Open Access Journals (Sweden)

    Lindesay James

    2009-07-01

    Full Text Available Abstract Background Alzheimer's disease (AD is the commonest cause of dementia. Cholinesterase inhibitors, such as donepezil, are the drug class with the best evidence of efficacy, licensed for mild to moderate AD, while the glutamate antagonist memantine has been widely prescribed, often in the later stages of AD. Memantine is licensed for moderate to severe dementia in AD but is not recommended by the England and Wales National Institute for Health and Clinical Excellence. However, there is little evidence to guide clinicians as to what to prescribe as AD advances; in particular, what to do as the condition progresses from moderate to severe. Options include continuing cholinesterase inhibitors irrespective of decline, adding memantine to cholinesterase inhibitors, or prescribing memantine instead of cholinesterase inhibitors. The aim of this trial is to establish the most effective drug option for people with AD who are progressing from moderate to severe dementia despite treatment with donepezil. Method DOMINO-AD is a pragmatic, 15 centre, double-blind, randomized, placebo controlled trial. Patients with AD, currently living at home, receiving donepezil 10 mg daily, and with Standardized Mini-Mental State Examination (SMMSE scores between 5 and 13 are being recruited. Each is randomized to one of four treatment options: continuation of donepezil with memantine placebo added; switch to memantine with donepezil placebo added; donepezil and memantine together; or donepezil placebo with memantine placebo. 800 participants are being recruited and treatment continues for one year. Primary outcome measures are cognition (SMMSE and activities of daily living (Bristol Activities of Daily Living Scale. Secondary outcomes are non-cognitive dementia symptoms (Neuropsychiatric Inventory, health related quality of life (EQ-5D and DEMQOL-proxy, carer burden (General Health Questionnaire-12, cost effectiveness (using Client Service Receipt Inventory and

  6. Clinically meaningful treatment responses after switching to galantamine and with addition of memantine in patients with Alzheimer’s disease receiving donepezil

    Directory of Open Access Journals (Sweden)

    Kano O

    2013-02-01

    Full Text Available Osamu Kano,1 Hirono Ito,1 Takanori Takazawa,1 Yuji Kawase,1 Kiyoko Murata,1 Konosuke Iwamoto,1 Tetsuro Nagaoka,1 Takehisa Hirayama,1 Ken Miura,1 Riya Nagata,1 Tetsuhito Kiyozuka,2 Jo Aoyagi,2 Ryuta Sato,2 Teruo Eguchi,3 Ken Ikeda,1 Yasuo Iwasaki11Department of Neurology, Toho University Omori Medical Center, 2Department of Neurology, Federation of National Public Service Personnel Mutual Aid Associations Mishuku Hospital, 3Sakura-kai Medical Group, Tokyo, JapanAbstract: Clinical trials have shown the benefits of acetylcholinesterase inhibitors, such as donepezil and galantamine, and an N-methyl-d-aspartate receptor antagonist, memantine, in patients with Alzheimer’s disease (AD. However, little is known regarding the effects of switching from donepezil 5 mg/day to galantamine 16 or 24 mg/day, or regarding the effects of adding memantine to established therapy compared with increasing the dose of donepezil. This report discusses two studies conducted to evaluate treatment with galantamine and memantine with respect to cognitive benefits and caregiver evaluations in patients with AD receiving donepezil 5 mg/day for more than 6 months. Patients with mild or moderate AD (scores 10–22 on the Mini-Mental State Examination were enrolled in the Galantamine Switch study and switched to galantamine (maximum doses 16 mg versus 24 mg. Patients with moderate to severe AD (Mini-Mental State Examination scores 3–14 were enrolled in the Donepezil Increase versus Additional Memantine study and either had their donepezil dose increased to 10 mg/day or memantine 20 mg/day added to their existing donepezil dose. Patients received the study treatment for 28 weeks and their Disability Assessment for Dementia, Mental Function Impairment Scale, Cohen-Mansfield Agitation Inventory, and Neuropsychiatric Inventory scores were assessed with assistance from their caregivers. For the Galantamine Switch study after 8 weeks, agitation evaluated by the Cohen

  7. EFFECTS OF 6-MONTHS TREATMENT WITH DONEPEZIL AND RIVASTIGMIN ON RESULTS OF NEUROPSYCHOLOGICAL TESTS OF MMSE, NPI, CLOCK AND BENDER IN PATIENTS WITH ALZHEIMER'S DISEASE

    Directory of Open Access Journals (Sweden)

    R. Abolfazli

    2008-05-01

    Full Text Available Alzheimer's disease is the most common degenerative disease of brain. Nowadays, the most common treatment being used to slow down disease progression, include Donepezil , Rivastigmine and Galantamine, which all of them act as inhibitors of acetyl cholinesterase. General purpose of our study was to show effects of treatment with Donepezil and Rivastigmine, as two drugs that commonly used for treatment of AD in Iran and to compare these effects between two drugs. Samples selected from patients who had Alzheimer` disease with DSM IV criteria and were candidate of receiving Donepezil or Rivastigmine, as treatment of AD, for the first time. We used four neuropsychological tests including MMSE, NPI, Clock and Bender to assess patient's cognitive and behavioral changes during treatment with two drugs. Patients divided to two groups (each group 35 cases; Patients with plan of taking Donepezil entered into one of the groups and patients with plan of taking Rivastigmine entered into another. The four tests were completed once before starting treatment and then, 1 month, 3 months and 6 months after treatment with Donepezil and Rivastigmine. MMSE, 6 months after treatment with Donepezil, improved from 20.63 before treatment to 21.83, which is statistically significant (P = 0.04. Also, MMSE, 6 months after treatment with Rivastigmine, improved from 20.03 before treatment to 22.71, which was statistically significant (P = 0.007. About Clock test, there was a significant improvement from 5.74 before treatment to 6.4 after 6 months of treatment with Rivastigmine; while this significant improvement was not seen in patients receiving Donepezil. In two other tests, no significant differences were seen before and after treatment. Also, No significant difference was detected between two groups and so no different effects on these tests between Donepezil and Rivastigmine in 6 months period of treatment.

  8. A survey of the consultative status of patients with Alzheimer disease and the efficacy and safety of donepezil treatment%阿尔茨海默病患者就诊状况及多奈哌齐治疗效果的调查

    Institute of Scientific and Technical Information of China (English)

    彭丹涛; 于普林

    2010-01-01

    目的 调查医院背景下阿尔茨海默病(AD)患者的就诊状况及多奈哌齐治疗的有效性.方法 由中华医学会老年医学分会立项,并与卫材(中国)药业有限公司共同组织全国40个城市60家大型医院,针对符合世界卫生组织国际疾病分类(ICD-10)及精神障碍诊断和统计工作手册第4版(DSM-Ⅳ)等痴呆诊断标准的患者进行首发症状、就诊时间和科室、诊断时间及多奈哌齐治疗至少3个月前后的认知、生活功能及精神行为变化进行调查.结果 调查痴呆患者808例,其中记忆力下降703例(87%)、精神行为症状250例(31%)、生活能力下降388例(48%),首次就诊时的病程9~16个月,平均(13.0±0.2)个月.首次作出痴呆诊断的科室神经内科占74%、精神科6%、老年科19%、其他科室1%.出现症状至首次确诊时间3~21个月,平均(14.4±0.3)个月.多奈哌齐治疗后痴呆患者的认知功能、日常生活自理能力及精神状况均有改善(P<0.05).结论 我国痴呆患者就诊率低,就诊及诊断时多为中重度患者,影响患者疾病的预后及生活能力的维持.多奈哌齐能有效改善患者的认知功能、日常生活自理能力及精神行为,在治疗过程中未出现严重不良反应.%Objective To investigate the consultative status of patients with Alzheimer Disease (AD), and to evaluate the efficacy and safety of donepezil (Aricept) in the treatment of AD.Methods This survey was initiated by Chinese society of Geriatrics, and was sponsored by Eisai (China) Inc. It was conducted in 60 hospitals of 40 cities in China. The diagnosis of dementia was made according to ICD-10 and DSM-Ⅳ criteria. The cognition, behavior and ability of daily living of the patients were compared before and after 3-month treatment with donepezil. Results A total of 808 dementia patients were recruited. The main reasons for patients' seeing doctors included memory problem (n= 703, 87%), behavioral and psychological

  9. Thermoanalytical Investigation of Terazosin Hydrochloride

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    Mona Mohamed Abdel-Moety

    2013-02-01

    Full Text Available Purpose: Thermal analysis (TGA, DTG and DTA and differential scanning calorimetry (DSC have been used to study the thermal behavior of terazosin hydrochloride (TER. Methods: Thermogravimetric analysis (TGA/DTG, differential thermal analysis (DTA and differential scanning calorimetry (DSC were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*, enthalpy (H*, entropy (S* and Gibbs free energy change of the decomposition (G* were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97% and specialized official method (99.85% indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 ºC, water content (7.49% and ash content (zero in comparison to what were obtained using official method: (272 ºC, (8.0% and (0.02% for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.

  10. Quantitative analysis of the effects of donepezil on regional cerebral blood flow in Alzheimer's disease by using an automated program, 3DSRT

    Energy Technology Data Exchange (ETDEWEB)

    Tateno, Masaru [Sapporo Medical University, Department of Neuropsychiatry, Sapporo, Hokkaido (Japan); Kobayashi, Seiju; Utsumi, Kumiko [Sunagawa City Medical Center, Department of Psychiatry, Sunagawa (Japan); Morii, Hidetoshi; Fujii, Kazuki [Sunagawa City Medical Center, Department of Radiology, Sunagawa (Japan)

    2008-08-15

    Donepezil, an acetylcholinesterase inhibitor, has been reported to have an effect that improves cerebral blood flow (CBF) alongside its primary effect on memory function. The aim of this study was to investigate the effects of long-term, low-dose donepezil therapy on blood perfusion in Alzheimer's disease (AD) by using a fully automated regional CBF quantification program named 3DSRT. Fifteen subjects with mild to moderate AD according to NINCDS/ADRDA criteria underwent 99mTc-ethylcysteinate dimer (ECD) brain perfusion single photon emission computed tomography (SPECT) twice with an interval of 55.1{+-}11.0 weeks. The dose of donepezil was fixed at 5 mg/day following the induction period (3 mg/day) of 2 weeks. Clinical efficacy of donepezil was assessed by using the Mini-Mental State Examination (MMSE). The results of SPECT imaging under exactly identical conditions were analyzed by 3DSRT, which enables us to perform a very objective assessment. Despite a decrease of the MMSE score from 20.9{+-}4.7 to 18.7{+-}5.7, CBF was increased in almost all cerebral areas except the left temporal segment. The increase was statistically significant in the left callosomarginal, right central, and bilateral pericallosal and lenticular nucleus segments. Thus far, no direct cerebrovascular effects have been reported for donepezil. We hypothesize that these CBF-promoting effects of donepezil might be related to increased neuronal activity and enhanced connection of neurons. (orig.)

  11. Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol

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    Yahya Ayhan Acar

    2014-01-01

    Full Text Available Benzydamine hydrochloride is a locally acting nonsteroidal anti-inflammatory drug. Benzydamine hydrochloride overdose can cause stimulation of central nervous system, hallucinations, and psychosis. We presented a young man with psychotic symptoms due to benzydamine hydrochloride abuse. He received a total dose of 1000 mg benzydamine hydrochloride with alcohol for its hallucinative effects. Misuse of benzydamine hydrochloride must be considered in differential diagnosis of first-episode psychosis and physicians should consider possibility of abuse in prescribing.

  12. Spectrophotometric simultaneous estimation of ranitidine hydrochloride and ondansetron hydrochloride from tablet formulation

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    Pillai S

    2007-01-01

    Full Text Available Three simple, accurate, economical and reproducible UV spectrophotometric methods for simultaneous estimation of two component drug mixture of ranitidine hydrochloride and ondansetron hydrochloride from combined tablet dosage form have been developed. First developed method involves formation and solving of simultaneous equations at 267.2 nm and 314.4 nm. Second method was developed making use of first order derivative spectroscopy using 340.8 nm and 276.0 nm as zero crossing points for estimation of ranitidine hydrochloride and ondansetron hydrochloride respectively. Third method is based on two wavelength calculation, wavelengths selected for estimation of ranitidine hydrochloride were 266.1 nm and 301.8 nm and for ondansetron hydrochloride 305.7 nm and 319.2 nm. The results of analysis have been validated statistically and by recovery studies.

  13. Spectrophotometric determination of diphenhydramine hydrochloride using dipicrylamine.

    Science.gov (United States)

    Shamsa, F A; Maghssoudi, R H

    1976-05-01

    A spectrophotometric procedure for the determination of diphenhydramine hydrochloride based on the reaction with dipicrylamine was developed. A yellow complex forms and is easily extractable by chloroform at pH 5. The mole ratio of diphenydramine hydrochloride to dipicrylamine in the complex is 1:3. The absorbance of the complex obeys Beer's law over the concentration range of 3-10 mug of diphenhydramine hydrochloride per ml of chloroform. This procedure can be carried out in the presence of other compounds without interference.

  14. Changes in cognitive domains during three years in patients with Alzheimer's disease treated with donepezil

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    Levander Sten

    2009-02-01

    Full Text Available Abstract Background The objective was to identify separate cognitive domains in the standard assessment tools (MMSE, ADAS-Cog and analyze the process of decline within domains during three years in Alzheimer's disease (AD patients with donepezil treatment. Method AD patients (n = 421 were recruited from a clinical multi-centre study program in Sweden. Patients were assessed every six months during three years. All patients received donepezil starting directly after study entry. After dropouts, 158 patients remained for analyses over three years. Data for the other patients were analysed until they dropped out (4 groups based on length in study. Results Factor analyses of all items suggested that there were three intercorrelated factors: a General, a Memory and a Spatial factor for which we constructed corresponding domains. Overall there was a cognitive improvement at six months followed by a linear drop over time for the three domains. Some group and domain differences were identified. Patients who remained longer in the study had better initial performance and a slower deterioration rate. The early dropouts showed no improvement at six months and many dropped out due to side effects. The other groups displayed a performance improvement at six months that was less pronounced in the Memory domain. Before dropping out, deterioration accelerated, particularly in the Spatial domain. Conclusion The course of illness in the three domains was heterogeneous among the patients. We were not able to identify any clinically relevant correlates of this heterogeneity. As an aid we constructed three algorithms corresponding to the cognitive domains, which can be used to characterize patients initially, identify rapid decliners and follow the course of the disease.

  15. Preparation, characterization, and in vivo evaluation of intranasally administered liposomal formulation of donepezil

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    Al Asmari AK

    2016-01-01

    Full Text Available Abdulrahman K Al Asmari,1 Zabih Ullah,1 Mohammad Tariq,1 Amal Fatani21Department of Research, Prince Sultan, Military Medical City, 2Department of Pharmacy, King Saud University, Riyadh, Saudi ArabiaAbstract: The adequate amount of drug delivery to the brain in neurological patients is a major problem faced by the physicians. Recent studies suggested that intranasal administration of liposomal formulation may improve the drug delivery to the brain. In the present study, an attempt was made to study the brain bioavailability of commonly used anti-Alzheimer drug donepezil (DNP liposomal formulation by intranasal route in rats. We adopted the thin layer hydration technique for the preparation of liposomes by using cholesterol, polyethylene glycol, and 1,2-distearyl-sn-glycero-3-phosphocholine (DSPC. The prepared liposomes were characterized by determining particle size, shape, surface morphology, zeta potential, encapsulation efficiency, and in vitro release of DNP. The pharmacokinetic parameters of liposomal DNP in plasma and brain of rats were determined following oral and nasal administration. The results of this study showed that the DNP liposomal formulation was stable with a consistent size (102±3.3 nm and shape. The prepared liposomes showed high encapsulation efficiency (84.91%±3.31% and sustained-release behavior. The bioavailability of DNP in plasma and brain increased significantly (P<0.05 after administration of liposomal formulation by the intranasal route. Histopathological examination showed that the formulation was safe and free from toxicity. It can be concluded that the nasal administration of liposomal preparation may provide an efficient and reliable mode of drug delivery to the central nervous system.Keywords: donepezil, intranasal, liposomes, bioavailability, blood–brain barrier

  16. Stability Indicating HPLC Method for Simultaneous Quantification of Trihexyphenidyl Hydrochloride, Trifluoperazine Hydrochloride and Chlorpromazine Hydrochloride from Tablet Formulation

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    P. Shetti

    2010-01-01

    Full Text Available A new, simple, precise, rapid, selective and stability indicating reversed-phase high performance liquid chromatographic (HPLC method has been developed and validated for simultaneous quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and chlorpromazine hydrochloride from combined tablet formulation. The method is based on reverse-phase using C-18 (250×4.6 mm, 5 μm particle size column. The separation is achieved using isocratic elution by methanol and ammonium acetate buffer (1% w/v, pH 6.5 in the ratio of 85:15 v/v, pumped at flow rate 1.0 mL/min and UV detection at 215 nm. The column is maintained at 30 °C through out the analysis. This method gives baseline resolution. The total run time is 15 min. Stability indicating capability is established buy forced degradation experiment. The method is validated for specificity, accuracy, precision and linearity as per International conference of harmonisation (ICH. The method is accurate and linear for quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and Chlorpromazine hydrochloride between 5 - 15 μg/mL, 12.5- 37.5 μg/mL and 62.5 - 187.5 μg/mL respectively.

  17. Acetylcholinesterase inhibitors for the treatment of Wernicke-Korsakoff syndrome--three further cases show response to donepezil.

    Science.gov (United States)

    Cochrane, Murray; Cochrane, Ashley; Jauhar, Pramod; Ashton, Elizabeth

    2005-01-01

    Three patients diagnosed with Wernicke-Korsakoff syndrome were treated with the acetylcholinesterase inhibitor, donepezil, for periods of 6 to 8 months. Cognitive testing [Alzheimer's disease assessment scale-cognitive subscale (ADAS-Cog), Mini-mental state examination (MMSE), Clock drawing test and six item 2 min recall] and carer questionnaires [Informant Questionnaire (IQ Code), Neuropsychiatric inventory scale (NPI)] were performed at baseline, mid- and endpoint of the treatment period and post-discontinuation. Progressive partial improvement occurred in cognitive measurements through the treatment period, some of which was sustained after discontinuing donepezil. Carer questionnaires also indicated improvement. Confounding factors necessitate caution when attributing improvements to the medication, but these cases suggest that this option merits further investigation.

  18. A Novel Synthesis of Difloxacin Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation,amination, cyclization, hydrolysis, decarbonylation and N-methylpiperazination. Additional four new intermediates are produced.

  19. A novel asymmetric synthesis of cinacalcet hydrochloride

    OpenAIRE

    Arava, Veera R; Laxminarasimhulu Gorentla; Pramod K. Dubey

    2012-01-01

    A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  20. A novel asymmetric synthesis of cinacalcet hydrochloride

    Directory of Open Access Journals (Sweden)

    Veera R. Arava

    2012-08-01

    Full Text Available A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  1. A novel asymmetric synthesis of cinacalcet hydrochloride

    Science.gov (United States)

    Gorentla, Laxminarasimhulu; Dubey, Pramod K

    2012-01-01

    Summary A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described. PMID:23019473

  2. Maintenance Treatment of Depression in Old Age: A Randomized, Double-blind, Placebo-Controlled Evaluation of the Efficacy and Safety of Donepezil Combined with Antidepressant Pharmacotherapy

    Science.gov (United States)

    Reynolds, Charles F.; Butters, Meryl A.; Lopez, Oscar; Pollock, Bruce G.; Dew, Mary Amanda; Mulsant, Benoit H.; Lenze, Eric J.; Holm, Margo; Rogers, Joan C.; Mazumdar, Sati; Houck, Patricia R.; Begley, Amy; Anderson, Stewart; Karp, Jordan F.; Miller, Mark D.; Whyte, Ellen M.; Stack, Jacqueline; Gildengers, Ariel; Szanto, Katalin; Bensasi, Salem; Kaufer, Daniel I.; Kamboh, M. Ilyas; DeKosky, Steven T.

    2010-01-01

    Context Cognitive impairment in late-life depression is a core feature of the illness. Objective to test whether donepezil + antidepressant is superior to placebo + antidepressant in (1) improving cognitive performance and instrumental activities of daily living and (2) reducing recurrences of depression over two years of maintenance treatment. Design Randomized, double-blind, placebo controlled maintenance trial. Setting university clinic Main Outcome Measures global neuropsychological performance, cognitive instrumental ADL, and recurrent depression. Results Donepezil + antidepressant temporarily improved global cognition (treatment by time interaction F = 3.78, df = 2, 126, p = .03), but effect sizes were small (Cohen’s d = 0.27: group difference at 1 year). A marginal benefit to cognitive instrumental ADL was also observed (treatment by time interaction; F = 2.94; df = 2, 137, p = 0.06). The donepezil group was more likely to experience recurrent major depression: 35% [95% CI: 24%, 46%] versus 19% [95% CI: 9%, 29%] (log rank chi squared = 3.97, p = .05); hazard ratio = 2.09 [95% CI: 1.00, 4.41]. Post-hoc subgroup analyses showed that, of 57 participants with mild cognitive impairment, 3/30 on donepezil (10%; 95% CI: 0, 21%) and 9/27 on placebo (33%; 95% CI: 16%, 51%) converted to dementia over two years (Fisher exact p = 0.05). The MCI subgroup had a 44 percent recurrence rate of major depression on donepezil verses 12% on placebo (LR=4.91, p=.03). The subgroup with normal cognition (n = 73) showed no benefit on donepezil or increase in recurrence of major depression. Conclusion Whether ChEI should be used as augmentation in the maintenance treatment of late-life depression depends upon a careful weighing of risks and benefits in those with MCI. In cognitively intact patients, donepezil appears to have no clear benefit for preventing progression to MCI/dementia or recurrence of depression. PMID:21199965

  3. Efficacy and Tolerability of a Combination Treatment of Memantine and Donepezil for Alzheimer’s Disease: A Literature Review Evidence

    Science.gov (United States)

    Riverol, Mario; Slachevsky, Andrea; López, Oscar L.

    2011-01-01

    INTRODUCTION Two types of drugs have been approved for the symptomatic treatment of Alzheimer’s disease (AD): the cholinesterase inhibitors (ChEIs) and memantine. There is a growing interest to know whether the combination of these drugs is safe and if it adds any clinical benefit to patients. OBJECTIVE To systematically review published medical literature assessing the efficacy and tolerability of a combination treatment of memantine and donepezil in AD patients. METHODS We searched PubMed for English and Spanish-language literature, using the terms “Alzheimer’s disease,” “cholinesterase inhibitors,” “donepezil,” and “memantine.” Our review focused on clinical trials and observational studies. RESULTS Eleven publications representing seven unique studies were selected for this review. Three were randomized double-blind, placebo-controlled trials and four were observational studies. CONCLUSIONS Available data revealed that the combination of memantine and donepezil slowed down cognitive decline, prolonged functional independence, and improved behavioral symptoms in patients with moderate to severe AD. The long-term use of the dual therapy decreased the risk of nursing home admission. More longitudinal studies are needed to further examine the role of combined therapy in the management of AD patients. PMID:25302109

  4. 78 FR 34108 - Determination That SUBOXONE (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Sublingual...

    Science.gov (United States)

    2013-06-06

    ... HUMAN SERVICES Food and Drug Administration Determination That SUBOXONE (Buprenorphine Hydrochloride and... (buprenorphine hydrochloride (HCl) and naloxone HCl) sublingual tablets, 2 milligrams (mg)/0.5 mg and 8 mg/2 mg... to approve abbreviated new drug applications (ANDAs) for buprenorphine HCl and naloxone...

  5. Normal Hearing Ability but Impaired Auditory Selective Attention Associated with Prediction of Response to Donepezil in Patients with Alzheimer’s Disease

    Directory of Open Access Journals (Sweden)

    Yoshitaka Ouchi

    2015-01-01

    Full Text Available Background. Alzheimer’s disease (AD patients have a poor response to the voices of caregivers. After administration of donepezil, caregivers often find that patients respond more frequently, whereas they had previously pretended to be “deaf.” We investigated whether auditory selective attention is associated with response to donepezil. Methods. The subjects were40 AD patients, 20 elderly healthy controls (HCs, and 15 young HCs. Pure tone audiometry was conducted and an original Auditory Selective Attention (ASA test was performed with a MoCA vigilance test. Reassessment of the AD group was performed after donepezil treatment for 3 months. Results. Hearing level of the AD group was the same as that of the elderly HC group. However, ASA test scores decreased in the AD group and were correlated with the vigilance test scores. Donepezil responders (MMSE 3+ also showed improvement on the ASA test. At baseline, the responders had higher vigilance and lower ASA test scores. Conclusion. Contrary to the common view, AD patients had a similar level of hearing ability to healthy elderly. Auditory attention was impaired in AD patients, which suggests that unnecessary sounds should be avoided in nursing homes. Auditory selective attention is associated with response to donepezil in AD.

  6. The Effects of an Uninterrupted Switch from Donepezil to Galantamine without Dose Titration on Behavioral and Psychological Symptoms of Dementia in Alzheimer's Disease

    Directory of Open Access Journals (Sweden)

    Shoichi Sasaki

    2014-05-01

    Full Text Available Aims: To elucidate the efficacy of galantamine on cognition and behavioral and psychological symptoms of dementia (BPSD in outpatients with mild cognitive impairment (MCI and Alzheimer's disease (AD who have switched from donepezil to galantamine. Materials and Methods: We performed an uninterrupted switch from donepezil to galantamine without a washout period or dose titration in 44 ambulatory outpatients with amnestic MCI (n = 12 or mild-to-moderate AD (n = 32. Three months after the switch, the efficacy of galantamine was evaluated with the Mini-Mental State Examination (MMSE, and the Neuropsychiatric Inventory (NPI and NPI Brief Questionnaire Form (NPI-Q, respectively, using the Wilcoxon signed-rank test. Results: NPI scores improved significantly on BPSD, especially on delusions, agitation and aberrant motor activity in AD patients (p = 0.027; improvement was remarkable in patients with moderate AD (MMSE score 10-19; p = 0.007, while insignificant in those with MCI (MMSE score ≥24; p = 0.648. The NPI-Q score also improved significantly regarding both the severity of the disease (p = 0.009 and caregiver distress (p = 0.012 in AD patients. MMSE scores hardly improved in either MCI (p = 0.394 or AD patients (p = 0.265. Conclusions: An uninterrupted switch from donepezil to galantamine could be a useful alternative treatment option for AD patients whose BPSD are unresponsive to donepezil, or whose caregivers are not satisfied with donepezil treatment.

  7. Octenidine hydrochloride in hydatid disease.

    Science.gov (United States)

    Altindis, Mustafa; Arikan, Yuksel; Cetinkaya, Zafer; Polat, Coskun; Yilmaz, Sezgin; Akbulut, Gökhan; Dilek, Osman Nuri; Gokce, Ozcan

    2004-01-01

    Hydatid disease is still endemic in many devoloping countries and continues to be an important cause of morbidity. The objective of this study was to determine the in vitro scolicidal effects of octenidine hydrochloride in different concentrations using different exposure times. After hydatid cyst liquid was left to precipitate for 1 h to obtain cystic sand, various concentrations of octenidine (undiluted, 1% and 0.1% diluted) were added to concentrated hydatid cyst sediments for 5, 10, 15, 20, 25, 30, 45, and 60 min, and scolicidal effects of octenidine were compared with 20% saline and control group for the same times. It was found that undiluted octenidine had a strong scolicidal effect at 15 min compared to saline at 20%. One percent octenidine had a scolicidal effect at 30 min. However, 0.1% octenidine did not have enough scolicidal effect in 1 h. It was concluded that undiluted and 1% diluted octenidine might be used for scolicidal purpose in the treatment of hydatid disease.

  8. Research of Genotoxic Impurities in Donepezil Hydrochloride%盐酸多奈哌齐中基因毒性杂质的研究

    Institute of Scientific and Technical Information of China (English)

    张佳; 陈峙; 丁现帅

    2016-01-01

    建立了液相色谱法测定盐酸多奈哌齐中的基因毒性杂质氯化苄的检测方法.该方法采用Waters Xterra RP18色谱柱,用甲酸水溶液和乙腈作为流动相,梯度洗脱,在0.04~40μg/mL范围内线性关系良好,方法准确可靠,且具有较小的定量限(LOQ=1.3 ppm).

  9. Compound list: fluoxetine hydrochloride [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available fluoxetine hydrochloride FLX 00158 ftp://ftp.biosciencedbc.jp/archive/open-tggates/...LATEST/Human/in_vitro/fluoxetine_hydrochloride.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/o...pen-tggates/LATEST/Rat/in_vivo/Liver/Single/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Single.zip ftp://ftp....biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Repeat.zip ...

  10. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  11. Utility of 11C-methionine and 11C-donepezil for imaging of Staphylococcus aureus induced osteomyelitis in a juvenile porcine model

    DEFF Research Database (Denmark)

    Afzelius, Pia; Alstrup, Aage Ko; Schønheyder, Henrik C

    2016-01-01

    The aim of this study was to compare (11)C-methionine and (11)C-donepezil positron emission tomography (PET) with (111)In-labeled leukocyte and (99m) Tc-DPD (Tc-99m 3,3-diphosphono-1,2-propanedicarboxylic acid) single-photon emission computed tomography (SPECT), and (18)F-fluorodeoxyglucose ((18)F...... in the right femoral artery with a porcine strain of Staphylococcus aureus. The sequential scan protocol included Computed Tomography, (11)C-methionine and (11)C-donepezil PET, (99m) Tc-DPD and (111)In-labelled leukocytes scintigraphy, and (18)F-FDG PET. This was followed by necropsy of the pigs and gross......-methionine in 79%, (11)C-donepezil in 58%, and (99m) Tc-DPD in none. Overall, (18)F-FDG PET was superior to (111)In-leukocyte SPECT and (11)C-methionine in marking infectious lesions....

  12. Compound Danshen tablets downregulate amyloid protein precursor mRNA expression in a transgenic cell model of Alzheimer's disease Effects and a comparison with donepezil

    Institute of Scientific and Technical Information of China (English)

    Ren'an Qin; Desheng Zhou; Jiajun Wang; Hua Hu; Yang Yang; Xiaoxuan Yao; Xiaopeng Sun

    2012-01-01

    After gene mutation, the pcDNA3.1/APP595/596 plasmid was transfected into HEK293 cells to establish a cell model of Alzheimer’s disease. The cell model was treated with donepezil or compound Danshen tablets after culture for 72 hours. Reverse transcription-PCR showed that the mRNA expression of amyloid protein precursor decreased in all groups following culture for 24 hours, and that there was no significant difference in the amount of decrease between donepezil and compound Danshen tablets. Our results suggest that compound Danshen tablets can reduce expression of the mRNA for amyloid protein precursor in a transgenic cell model of Alzheimer’s disease, with similar effects to donepezil.

  13. Utility of (11)C-methionine and (11)C-donepezil for imaging of Staphylococcus aureus induced osteomyelitis in a juvenile porcine model

    DEFF Research Database (Denmark)

    Afzelius, Pia; Alstrup, Aage Ko; Schønheyder, Henrik C;

    2016-01-01

    The aim of this study was to compare (11)C-methionine and (11)C-donepezil positron emission tomography (PET) with (111)In-labeled leukocyte and (99m) Tc-DPD (Tc-99m 3,3-diphosphono-1,2-propanedicarboxylic acid) single-photon emission computed tomography (SPECT), and (18)F-fluorodeoxyglucose ((18)F...... in the right femoral artery with a porcine strain of Staphylococcus aureus. The sequential scan protocol included Computed Tomography, (11)C-methionine and (11)C-donepezil PET, (99m) Tc-DPD and (111)In-labelled leukocytes scintigraphy, and (18)F-FDG PET. This was followed by necropsy of the pigs and gross......-methionine in 79%, (11)C-donepezil in 58%, and (99m) Tc-DPD in none. Overall, (18)F-FDG PET was superior to (111)In-leukocyte SPECT and (11)C-methionine in marking infectious lesions....

  14. A randomized, 4-week double-blind placebo control study on the efficacy of donepezil augmentation of lithium for treatment of acute mania

    Directory of Open Access Journals (Sweden)

    Chen J

    2013-06-01

    Full Text Available Jing Chen,1 Zheng Lu,1,2 Mingyuan Zhang,1 Jie Zhang,1 Xiaodong Ni,1 Xuefeng Jiang,1 Heding Xu,1 Anisha Heeramun-Aubeeluck,2 Qiaoyan Hu,3 Hua Jin,4 John M Davis31Shanghai Mental Health Center, Shanghai Jiaotong University School of Medicine, Shanghai, People’s Republic of China; 2Department of Psychiatry, Tongji Hospital of Tongji University, Shanghai, People’s Republic of China; 3University of Illinois at Chicago, Chicago, IL, USA; 4University of California at San Diego, San Diego, CA, USAIntroduction: A significant number of mania patients fail to respond to current pharmacotherapy, thereby there is need for novel augmentation strategies. The results of some early studies showed the effectiveness of cholinomimetics in the treatment of mania. One open case series suggested the efficacy of donepezil in the treatment of bipolar disorder. Our aim was to explore whether an oral cholinesterase inhibitor, donepezil, administered during a 4-week treatment period,would benefit patients with acute mania.Methods: We conducted a 4-week double-blind, placebo-controlled trial of donepezil as an adjunctive treatment to lithium in patients with acute mania. Eligible subjects were randomly assigned to receive donepezil or placebo in addition to lithium. Donepezil was started at 5 mg/day, and increased to 10 mg/day in the first week. Patients were rated with the Young Mania Rating Scale (YMRS and Brief Psychiatric Rating Scale (BPRS at baseline, day 1, week 1, week 2, and week 4.Results: Out of the 30 patients who were enrolled, 15 were on donepezil and 15 were on placebo. All patients completed the 4-week trial. On the first day, there was a difference of 1.97 units on the psychomotor symptoms scale of the YMRS in the donepezil group as compared to the placebo group (t = 2.39, P = 0.02. There was a difference of 0.57 units (t = 2.09, P = 0.04 in the speech item and a difference of 0.29 units in the sexual interest item (t = 2.11, P = 0.04 in the donepezil

  15. Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina

    Directory of Open Access Journals (Sweden)

    Cristiane Bezerra da Silva

    2016-01-01

    Full Text Available Dugesia tigrina is a non-parasitic platyhelminth, which has been recently utilized in pharmacological models, regarding the nervous system, as it presents a wide sensitivity to drugs. Our trials aimed to propose a model for an in vivo screening of substances with inhibitory activity of the enzyme acetylcholinesterase. Trials were performed with four drugs commercialized in Brazil: donepezil, tacrine, galantamine and rivastigmine, utilized in the control of Alzheimer’s disease, to inhibit the activity of acetylcholinesterase. We tested five concentrations of the drugs, with an exposure of 24 h, and the mortality and the inhibition of acetylcholinesterase planarian seizure-like activity (pSLA and planarian locomotor velocity (pLMV were measured. Galantamine showed high anticholinesterasic activity when compared to the other drugs, with a reduction of 0.05 μmol·min−1 and 63% of convulsant activity, presenting screw-like movement and hypokinesia, with pLMV of 65 crossed lines during 5 min. Our results showed for the first time the anticholinesterasic and convulsant effect, in addition to the decrease in locomotion induced by those drugs in a model of invertebrates. The experimental model proposed is simple and low cost and could be utilized in the screening of substances with anticholinesterasic action.

  16. Electrospun water soluble polymer mat for ultrafast release of Donepezil HCl

    Directory of Open Access Journals (Sweden)

    2010-12-01

    Full Text Available Electrostatic spinning (Electrospinning, ES was applied to prepare Donepezil HCl loaded nanofibers as a potential orally dissolving dosage form. Electrospinning of water solutions of different polymers were performed in order to fabricate a consistent and removable web on the collector with ultra-fast dissolution in water based media. Poly(vinyl-alcohol of low molecular weight was found to be the most appropriate for this purpose. Morphology of the prepared nanofibers was characterized by scanning electron microscope as a function of viscosity and drug content. Diameters of the fibers were between 100 and 300 nm with narrow distribution. In vitro drug release of the webs was immediate (less than 30 s after immersion independently of their drug content owing to the formed huge surface area, while cast films with the same compositions and commercial tablets needed 30 min or more for complete dissolution. The developed technology for the preparation of orally dissolving web (ODW formulations is a promising way for producing effective and acceptable dosage forms for children, older people and patients with dysphagia.

  17. Errorless practice as a possible adjuvant to donepezil in Alzheimer's disease.

    Science.gov (United States)

    Rothi, Leslie J Gonzalez; Fuller, Renee; Leon, Susan A; Kendall, Diane; Moore, Anna; Wu, Samuel S; Crosson, Bruce; Heilman, Kenneth M; Nadeau, Stephen E

    2009-03-01

    Six individuals with probable Alzheimer's disease (AD) participated in a phase 1 study employing a repeated measures, parallel baseline design testing the hypothesis that error-free experience during word production practice combined with an acetyl cholinesterase inhibitor would improve confrontation naming ability. While acetyl cholinesterase inhibitors are safe and delay cognition decline associated with AD, improvement over baseline cognition is less evident; clinically significant cognitive deficits persist and progress. Both animal and clinical research strongly implicate acetylcholine in learning, a form of neuroplasticity. In clinical practice, however, people with AD are given cholinergic medications without concomitant systematic/targeted retraining. In this study six participants with probable AD and taking donepezil participated in targeted word production practice using an errorless learning strategy. Results showed that combining behavioral enrichment training and an acetyl cholinesterase inhibitor resulted in significant improvements in verbal confrontation naming of trained items for three of six participants. Differences in baseline dementia severity, living conditions, and medications may have influenced the training response. Detection of substantial treatment effects in 50% of subjects suggests further language treatment studies in AD in combination with an acetyl cholinesterase inhibitor are warranted and provide useful information on inclusion/exclusion criteria for use in subsequent studies.

  18. The effect of a combination of gabapentin and donepezil in an experimental pain model in healthy volunteers: Results of a randomized controlled trial.

    Science.gov (United States)

    Boyle, Yvonne; Fernando, Disala; Kurz, Hazel; Miller, Sam R; Zucchetto, Mauro; Storey, James

    2014-12-01

    This double-blind, placebo-controlled, 3-period cross-over, 4-treatment option, incomplete block study (ClinicalTrials.gov number NCT01485185), with an adaptive design for sample size re-estimation, was designed to evaluate gabapentin plus donepezil in an established experimental model of electrical hyperalgesia. Thirty healthy male subjects aged 18-55 years were randomized to receive gabapentin 900 mg or gabapentin 900 mg+donepezil 5mg for 2 of the 3 treatment periods, with 50% of subjects randomized to receive placebo (negative control) and 50% to gabapentin 1800 mg (positive control) for the remaining period. Each treatment period was 14 days. Gabapentin or corresponding placebo was administered on Day 13 and the morning of Day 14. Donepezil or corresponding placebo was administered nocturnally from Day 1-13 and the morning of Day 14. Co-primary endpoints were the area of pinprick hyperalgesia (260 mN von Frey filament) and allodynia (stroking by cotton bud) evoked by electrical hyperalgesia on Day 14. Gabapentin 1800 mg (n=14) significantly reduced the area of allodynia vs placebo (n=14; -12.83 cm(2); 95% confidence interval [CI] -23.14 to -2.53; P=0.015) with supportive results for hyperalgesia (-14.04 cm(2); 95% CI -28.49-0.41; P=0.057), validating the electrical hyperalgesia model. Gabapentin+donepezil (n=30) significantly reduced the area of hyperalgesia vs gabapentin 900 mg (n=30; -11.73 cm(2); 95% CI -21.04 to -2.42; P=0.014), with supportive results for allodynia (-6.62 cm(2); 95% CI -13.29-0.04; P=0.052). The adverse event profile for gabapentin+donepezil was similar to the same dose of gabapentin. Data are supportive of further clinical investigation of a gabapentin-and-donepezil combination in patients with an inadequate response to gabapentin.

  19. Long-term safety and tolerability of donepezil 23 mg in patients with moderate to severe Alzheimer’s disease

    Directory of Open Access Journals (Sweden)

    Tariot Pierre

    2012-06-01

    Full Text Available Abstract Background Donepezil (23 mg/day is approved by the US Food and Drug Administration for the treatment of patients with moderate to severe Alzheimer’s disease (AD. Approval was based on results from a 24-week, randomized, double-blind study of patients who were stable on donepezil 10 mg/day and randomized 2:1 to either increase their donepezil dose to 23 mg/day or continue taking 10 mg/day. The objective of this study was to assess the long-term safety and tolerability of donepezil 23 mg/day in patients with moderate to severe AD. Methods Patients who completed the double-blind study and were eligible could enroll into a 12-month extension study of open-label donepezil 23 mg/day. Clinic visits took place at open-label baseline and at months 3, 6, 9, and 12. Safety analyses comprised examination of the incidence, severity, and timing of treatment-emergent adverse events (AEs; changes in weight, electrocardiogram, vital signs, and laboratory parameters; and discontinuation due to AEs. Results 915 double-blind study completers were enrolled in the open-label extension study and 902 comprised the safety population. Mean treatment duration in this study was 10.3 ± 3.5 months. In total, 674 patients (74.7% reported at least one AE; in 320 of these patients (47.5% at least one AE was considered to be possibly or probably study drug related. The majority of patients reporting AEs (81.9% had AEs of mild or moderate severity. There were 268 patients (29.7% who discontinued early, of which 123 (13.6% were due to AEs. Patients increasing donepezil dose from 10 mg/day in the double-blind study to 23 mg/day in the extension study had slightly higher rates of AEs and SAEs than patients who were already receiving 23 mg (78.0% and 16.9% vs 72.8% and 14.0%, respectively. The incidence of new AEs declined rapidly after the first 2 weeks and remained low throughout the duration of the study. Conclusion This study shows that long

  20. Subchronic treatment of donepezil rescues impaired social, hyperactive, and stereotypic behavior in valproic acid-induced animal model of autism.

    Science.gov (United States)

    Kim, Ji-Woon; Seung, Hana; Kwon, Kyung Ja; Ko, Mee Jung; Lee, Eun Joo; Oh, Hyun Ah; Choi, Chang Soon; Kim, Ki Chan; Gonzales, Edson Luck; You, Jueng Soo; Choi, Dong-Hee; Lee, Jongmin; Han, Seol-Heui; Yang, Sung Min; Cheong, Jae Hoon; Shin, Chan Young; Bahn, Geon Ho

    2014-01-01

    Autism spectrum disorder (ASD) is a group of pervasive developmental disorders with core symptoms such as sociability deficit, language impairment, and repetitive/restricted behaviors. Although worldwide prevalence of ASD has been increased continuously, therapeutic agents to ameliorate the core symptoms especially social deficits, are very limited. In this study, we investigated therapeutic potential of donepezil for ASD using valproic acid-induced autistic animal model (VPA animal model). We found that prenatal exposure of valproic acid (VPA) induced dysregulation of cholinergic neuronal development, most notably the up-regulation of acetylcholinesterase (AChE) in the prefrontal cortex of affected rat and mouse offspring. Similarly, differentiating cortical neural progenitor cell in culture treated with VPA showed increased expression of AChE in vitro. Chromatin precipitation experiments revealed that acetylation of histone H3 bound to AChE promoter region was increased by VPA. In addition, other histone deacetyalse inhibitors (HDACIs) such as trichostatin A and sodium butyrate also increased the expression of AChE in differentiating neural progenitor cells suggesting the essential role of HDACIs in the regulation of AChE expression. For behavioral analysis, we injected PBS or donepezil (0.3 mg/kg) intraperitoneally to control and VPA mice once daily from postnatal day 14 all throughout the experiment. Subchronic treatment of donepezil improved sociability and prevented repetitive behavior and hyperactivity of VPA-treated mice offspring. Taken together, these results provide evidence that dysregulation of ACh system represented by the up-regulation of AChE may serve as an effective pharmacological therapeutic target against autistic behaviors in VPA animal model of ASD, which should be subjected for further investigation to verify the clinical relevance.

  1. Subchronic treatment of donepezil rescues impaired social, hyperactive, and stereotypic behavior in valproic acid-induced animal model of autism.

    Directory of Open Access Journals (Sweden)

    Ji-Woon Kim

    Full Text Available Autism spectrum disorder (ASD is a group of pervasive developmental disorders with core symptoms such as sociability deficit, language impairment, and repetitive/restricted behaviors. Although worldwide prevalence of ASD has been increased continuously, therapeutic agents to ameliorate the core symptoms especially social deficits, are very limited. In this study, we investigated therapeutic potential of donepezil for ASD using valproic acid-induced autistic animal model (VPA animal model. We found that prenatal exposure of valproic acid (VPA induced dysregulation of cholinergic neuronal development, most notably the up-regulation of acetylcholinesterase (AChE in the prefrontal cortex of affected rat and mouse offspring. Similarly, differentiating cortical neural progenitor cell in culture treated with VPA showed increased expression of AChE in vitro. Chromatin precipitation experiments revealed that acetylation of histone H3 bound to AChE promoter region was increased by VPA. In addition, other histone deacetyalse inhibitors (HDACIs such as trichostatin A and sodium butyrate also increased the expression of AChE in differentiating neural progenitor cells suggesting the essential role of HDACIs in the regulation of AChE expression. For behavioral analysis, we injected PBS or donepezil (0.3 mg/kg intraperitoneally to control and VPA mice once daily from postnatal day 14 all throughout the experiment. Subchronic treatment of donepezil improved sociability and prevented repetitive behavior and hyperactivity of VPA-treated mice offspring. Taken together, these results provide evidence that dysregulation of ACh system represented by the up-regulation of AChE may serve as an effective pharmacological therapeutic target against autistic behaviors in VPA animal model of ASD, which should be subjected for further investigation to verify the clinical relevance.

  2. Rates of cognitive change in Alzheimer disease: Observations across a decade of placebo-controlled clinical trials with donepezil

    DEFF Research Database (Denmark)

    Jones, Roy W; Schwam, Elias; Wilkinson, David

    2009-01-01

    Treatment success in Alzheimer disease (AD) trials is generally based on benefits over placebo-treated controls. Consequently, variation in rates of decline among placebo-treated patients could impact outcomes from AD trials. In the present analyses, individual patient data [baseline Mini......-Mental State Examination (MMSE): 10 to 26] were pooled from randomized, placebo-controlled studies of donepezil for AD conducted during the 1990s, and grouped by initiation year-group 1: 1990 to 1994; group 2: 1996 to 1999. Changes in MMSE and Alzheimer's Disease Assessment Scale-cognitive subscale (ADAS...

  3. Cartap hydrochloride poisoning: A clinical experience

    Directory of Open Access Journals (Sweden)

    Hari K Boorugu

    2012-01-01

    Full Text Available Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [ 3 H]-ryanodine binding to the Ca 2+ release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca 2+ influx and induction of internal Ca 2+ release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  4. 21 CFR 556.350 - Levamisole hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs...

  5. Cartap hydrochloride poisoning: A clinical experience.

    Science.gov (United States)

    Boorugu, Hari K; Chrispal, Anugrah

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [(3)H]-ryanodine binding to the Ca(2+) release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca(2+) influx and induction of internal Ca(2+) release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  6. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food... chapter; meat products as defined in § 170.3(n)(29) of this chapter; milk products as defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  7. Combined administration of cerebrolysin and donepezil induces plastic changes in prefrontal cortex in aged mice.

    Science.gov (United States)

    Alcántara-González, Faviola; Mendoza-Perez, Claudia Rebeca; Zaragoza, Néstor; Juarez, Ismael; Arroyo-García, Luis Enrique; Gamboa, Citlalli; De La Cruz, Fidel; Zamudio, Sergio; Garcia-Dolores, Fernando; Flores, Gonzalo

    2012-11-01

    Cerebrolysin (Cbl) shows neurotrophic and neuroprotective properties while donepezil (Dnp) is a potent acetylcholinesterase (AChE) inhibitor, both drugs are prescribed for Alzheimer's disease (AD) treatment. Previous studies have shown that the Dnp and Cbl administered separately, modify dendritic morphology of neurons in the prefrontal cortex and hippocampus in senile rodents. Since the deficit of neurotrophic factor activity is implicated in the degeneration of cholinergic neurons of basal forebrain, a combination therapy of Dnp and Cbl has been tested recently in Alzheimer's patients. However, the plastic changes that may underlie this combined treatment have not yet been explored. We present here the effect of the combined administration of Cbl and Dnp on dendritic morphology in brain regions related to learning and memory in aged mice. The Golgi-Cox staining protocol and Sholl analysis were used for studying dendritic changes. Cbl and Dnp were administrated daily for 2 months to 9-months-old mice. Locomotor activity was assessed, as well as the dendritic morphology of neurons in several limbic regions was analyzed. Results showed that Cbl and Dnp induced an increase in locomotor activity without synergistic effect. The Cbl or Dnp treatment modified the dendritic morphology of neurons from prefrontal cortex (PFC), dorsal hippocampus (DH), dentate gyrus (DG), and the shell of nucleus accumbens (NAcc). These changes show an increase in the total dendritic length and spine density, resulting in an improvement of dendritic arborization. Prominently, a synergistic effect of Cbl and Dnp was observed on branching order and total dendritic length of pyramidal neurons from PFC. These results suggest that Dnp and Cbl may induce plastic changes in a manner independent of each other, but could enhance their effect in target cells from PFC.

  8. Effects of donepezil on activities of daily living: integrated analysis of patient data from studies in mild, moderate and severe Alzheimer's disease

    DEFF Research Database (Denmark)

    Gauthier, Serge; Lopez, Oscar Lopez; Waldemar, Gunhild

    2010-01-01

    We aimed to develop a standardization method to pool data recorded on different activities of daily living (ADL) scales in order to reduce variability of functional outcome data from Alzheimer's disease (AD) clinical trials and to better evaluate the effect of donepezil treatment on function...

  9. Dose-dependent sigma-1 receptor occupancy by donepezil in rat brain can be assessed with (11)C-SA4503 and microPET

    NARCIS (Netherlands)

    Kuzhuppilly Ramakrishnan, Nisha; Visser, Anniek K. D.; Schepers, Marianne; Luurtsema, Gert; Nyakas, Csaba J.; Elsinga, Philip H.; Ishiwata, Kiichi; Dierckx, Rudi A. J. O.; van Waarde, Aren

    2014-01-01

    RATIONALE: Sigma-1 receptor agonists are under investigation as potential disease-modifying agents for several CNS disorders. Donepezil, an acetylcholinesterase inhibitor used for the symptomatic treatment of Alzheimer's disease, is also a high-affinity sigma-1 agonist. OBJECTIVES: The objectives of

  10. Dose-dependent sigma-1 receptor occupancy by donepezil in rat brain can be assessed with (11)C-SA4503 and microPET

    NARCIS (Netherlands)

    Kuzhuppilly Ramakrishnan, Nisha; Visser, Anniek K. D.; Schepers, Marianne; Luurtsema, Gert; Nyakas, Csaba J.; Elsinga, Philip H.; Ishiwata, Kiichi; Dierckx, Rudi A. J. O.; van Waarde, Aren

    2014-01-01

    RATIONALE: Sigma-1 receptor agonists are under investigation as potential disease-modifying agents for several CNS disorders. Donepezil, an acetylcholinesterase inhibitor used for the symptomatic treatment of Alzheimer's disease, is also a high-affinity sigma-1 agonist. OBJECTIVES: The objectives of

  11. A Clinical Observation on the Effect of Aricept and Nicergoline in the Treatment of Alzheimer disease%盐酸多奈哌齐联合尼麦角林治疗轻中度阿尔茨海默病的临床观察

    Institute of Scientific and Technical Information of China (English)

    应爱娟; 陈龙法

    2007-01-01

    目的 评价盐酸多奈哌齐(Aricept)和尼麦角林(Nicergoline)治疗轻、中度阿尔茨海默病(Alzheimer disease,AD) 的有效性及安全性.方法 将184例轻、中度AD[简易智能状态量表(MMSE) 10~24分]患者随机分为对照组、盐酸多奈哌齐组、尼麦角林组及联合用药治疗组并进行12周临床试验研究.结果 盐酸多奈哌齐和尼麦角林及联合用药组均较对照组MMSE、临床痴呆程度量表(CDR) 及日常生活自理量表(ADL) 分数显著改善.联合用药组较盐酸多奈哌齐、尼麦角林组MMSE、CDR及ADL显著改善,而且随时间延长效果更加显著.盐酸多奈哌齐组与尼麦角林组比较从4周到12周MMSE分数显著改善(P均<0.01),而两组在CDR、ADL上无明显差异.盐酸多奈哌齐组1例、尼麦角林组1例及联合用药组2例发现轻微的头晕、恶心、轻度腹泻等,继续用药不良反应可消失,未见严重的副作用.结论 盐酸多奈哌齐、尼麦角林能有效治疗轻、中度AD 患者,对患者的认知功能、痴呆程度和日常生活自理能力均有改善, 耐受性好,安全性高.盐酸多奈哌齐在认知功能方面比尼麦角林疗效显著而在痴呆程度和日常生活自理能力无明显差异.联合应用两药可增加治疗效果,而未见明显副作用增加.

  12. Determination of Ivabradine Hydrochloride in Human Plasma by LC-MS/MS and Application in Pharmacokinetics Study%LC-MS/MS法测定人血浆盐酸依伐布雷定浓度及药动学研究

    Institute of Scientific and Technical Information of China (English)

    舒成仁; 卫乐乐

    2012-01-01

    Objective: To establish an LC-MS/MS method for the determination of ivabradine hydrochloride in human plasma and investigate the pharmacokinetics in human. Method: The samples were extracted with ether with donepezil hydrochloride as the internal standard. The CN column was used with the mobile phase of methanol-3% formic acid ( 40: 60 ) at a flow rate of 0. 3 ml ? Min~ . The detection was carried out by electrospray ionization mass spectremetry in positive ion mode. Multiple reactions monitoring ( MRM ) mode was used with the transition of m/z 469.0→177.0 and m/z 380. 5→243. 3 for ivabradine hydrochloride and the internal standard, respectively. Result: The calibration curve of ivabradine hydrochloride was linear within the concentration range of 0. 05 ~ 100 ng ? Ml~ . The average extraction recovery for low, medium and high concentration of ivabradine hydrochloride was 70. 87% , 76. 88% and 78. 31% , respectively. The RSDs of intra- and inter-day were less than 15% . Conclusion: LC-MS/MS method can be used for the pharmacokinetics research of ivabradine hydrochloride.%目的:建立LC-MS/MS法测定人血浆中盐酸依伐布雷定浓度,并用于药动学研究.方法:血浆经乙醚萃取处理,盐酸多奈哌齐为内标,采用氰基柱,以甲醇:0.3%甲酸水溶液(40:60)为流动相,流速0.3 ml·min-1,以ESI源正离子,多反应检测方式监测,选择离子反应为m/z469.0→177.0(盐酸依伐布雷定),m/z380.5→243.3 (内标).结果:盐酸依伐布雷定在0.05~100 ng·ml-1浓度范围内线性关系良好,低、中、高三种浓度平均提取回收率分别为70.87%、76.88%、78.31%,日内、日间相对标准差均小于15%.结论:该法可以用于盐酸依伐布雷定的药动学研究.

  13. Dose-dependent effect of donepezil administration on long-term enhancement of visually evoked potentials and cholinergic receptor overexpression in rat visual cortex.

    Science.gov (United States)

    Chamoun, Mira; Groleau, Marianne; Bhat, Menakshi; Vaucher, Elvire

    2016-09-01

    Stimulation of the cholinergic system tightly coupled with periods of visual stimulation boosts the processing of specific visual stimuli via muscarinic and nicotinic receptors in terms of intensity, priority and long-term effect. However, it is not known whether more diffuse pharmacological stimulation with donepezil, a cholinesterase inhibitor, is an efficient tool for enhancing visual processing and perception. The goal of the present study was to potentiate cholinergic transmission with donepezil treatment (0.5 and 1mg/kg) during a 2-week visual training to examine the effect on visually evoked potentials and to profile the expression of cholinergic receptor subtypes. The visual training was performed daily, 10min a day, for 2weeks. One week after the last training session, visual evoked potentials were recorded, or the mRNA expression level of muscarinic (M1-5) and nicotinic (α/β) receptors subunits was determined by quantitative RT-PCR. The visual stimulation coupled with any of the two doses of donepezil produced significant amplitude enhancement of cortical evoked potentials compared to pre-training values. The enhancement induced by the 1mg/kg dose of donepezil was spread to neighboring spatial frequencies, suggesting a better sensitivity near the visual detection threshold. The M3, M4, M5 and α7 receptors mRNA were upregulated in the visual cortex for the higher dose of donepezil but not the lower one, and the receptors expression was stable in the somatosensory (non-visual control) cortex. Therefore, higher levels of acetylcholine within the cortex sustain the increased intensity of the cortical response and trigger the upregulation of cholinergic receptors.

  14. Comparative studies of huperzine A,donepezil,and rivastigmine on brain acetylcholine,dopamine,norepinephrine,and 5-hydroxytryptamine levels in freely-moving rats

    Institute of Scientific and Technical Information of China (English)

    Yan-qi LIANG; Xi-can TANG

    2006-01-01

    Aim: To assess the effects of cholinesterase inhibitors huperzine A, donepezil and rivastigmine on cerebral neurotransmitters in the cortex and hippocampus in freely-moving rats. Methods: Double-probe cerebral microdialysis and HPLC with electrochemical detection were used to detect neurotransmitters. Results: Our results showed that huperzine A (0.25, 0.5, and 0.75 μmol/kg, po) dose-depen-dently elevated extracellular acetylcholine (Ach) levels in the medial prefrontal cortex (Mpfc) and hippocampus. Oral administration of donepezil (5.4 μmol/kg) or rivastigmine (1 μmol/kg) also elicited significant increases in Ach in the Mpfc and hippocampus. The time course of cortical acetylcholinesterase (AChE) inhibition with the 3 inhibitors mirrored the increases of Ach at the same dose. The marked elevation of Ach after oral administration of huperzine A (0.5 μmol/kg) and donepezil (5.4 μmol/kg) was associated with a significantly increased release of dopamine (DA) in the Mpfc or hippocampus. None of the 3 inhibitors affected norepinephrine (NE) and 5-hydroxytryptamine (5-HT) levels in the Mpfc and hippocampus. The effects of huperzine A and rivastigmine did not depend on the route of administration, but donepezil was less efficacious by the oral route than by ip injection. The ability of huperzine A to increase Ach levels was unchanged when tests were performed after multiple oral administration of the drug at 0.5 μmol/kg, once per day for 30 d. Conclusion: The present findings showed that, in molar terms, huperzine A had similar potency on increasing Mpfc Ach and DA levels as compared to the 11- and 2-fold dosages of donepezil and rivastigmine, respectively, and had longer lasting effects after oral dosing.

  15. [Antiseptics on the base of Octenidine Hydrochloride].

    Science.gov (United States)

    Malinovskií, N N; Reshetnikov, E A; Rubashnaia, I E; Mal'nikova, G N; Mitiukov, A P

    1997-01-01

    Comparative evaluation of laboratory and clinical investigation of antiseptic preparations on the base of octenidin-hydrochloride and bigluconate chlorhexidine in 537 patients was carried out. Statistically valid decrease in dissemination through the operation field and surgical wound after application of octenidin containing solutions was determined. It was established as well that these preparations were more effective fools of protection of the operation wound from its microbial contamination in comparison with antiseptic solutions widely spread to date in surgical practice.

  16. 抗抑郁药Duloxetine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    艾建国; 晋展

    2003-01-01

    @@ 日本Shionogi公司获得了Eli Lilly公司的授权,对其研制的一种对5-羟色胺(5-HT)和去甲肾上腺素(NE)的摄取有双重抑制作用的化合物Duloxetine Hydrochloride (Cymbalta(R),LY-264453,LY-248686)进行了进一步的开发.

  17. Effect of iptakalim hydrochloride on hemodynamics

    Institute of Scientific and Technical Information of China (English)

    Qing-leiZHU; HaiWANG; Wen-binXIAO

    2004-01-01

    AIM: To study the effect of iptakalim hydrochloride (Ipt) on hemodynamics. METHODS: Effect of Ipt on hemodynamics were studied in anesthetized nomotensive dogs, conscious nomotensive rats (NTR), and stroke prone spontaneously hypertensive rats (SHRsp), respectively. RESULTS: In pentobarbital anesthetized nomotensive dogs, Ipt at doses of 0.125, 0.25, 0.5,1.0, and 2.0 mg/kg iv could dose-dependently decrease blood pressure (BP), with the decrease of systolic BP equivalent

  18. Cartap hydrochloride poisoning: a case report

    OpenAIRE

    Sumesh Raj; Sheetal S.

    2014-01-01

    Cartap hydrochloride is a thiocarbamate insecticide used for control of chewing and sucking insects of all stages of development, on many crops. It is an analogue of nereistoxin. Poisoning with cartap is very rarely reported from India. We report a 46 year old man who consumed cartap with alcohol, presented with nausea & vomiting and improved with supportive measures. [Int J Res Med Sci 2014; 2(1.000): 360-361

  19. The 5-HT6 receptor antagonist idalopirdine potentiates the effects of donepezil on gamma oscillations in the frontal cortex of anesthetized and awake rats without affecting sleep-wake architecture.

    Science.gov (United States)

    Amat-Foraster, Maria; Leiser, Steven C; Herrik, Kjartan F; Richard, Nelly; Agerskov, Claus; Bundgaard, Christoffer; Bastlund, Jesper F; de Jong, Inge E M

    2017-02-01

    The 5-HT6 receptor is a promising target for cognitive disorders, in particular for Alzheimer's disease (AD). The high affinity and selective 5-HT6 receptor antagonist idalopirdine (Lu AE58054) is currently in development for mild-moderate AD as adjunct therapy to acetylcholinesterase inhibitors (AChEIs). We studied the effects of idalopirdine alone and in combination with the AChEI donepezil on cortical function using two in vivo electrophysiological methods. Neuronal network oscillations in the frontal cortex were measured during electrical stimulation of the brainstem nucleus pontis oralis (nPO) in the anesthetized rat and by an electroencephalogram (EEG) in the awake, freely moving rat. In conjunction with the EEG study, we investigated the effects of idalopirdine and donepezil on sleep-wake architecture using telemetric polysomnography. Idalopirdine (2 mg/kg i.v.) increased gamma power in the medial prefrontal cortex (mPFC) during nPO stimulation. Donepezil (0.3 and 1 mg/kg i.v.) also increased cortical gamma power and pretreatment with idalopirdine (2 mg/kg i.v.) potentiated and prolonged the effects of donepezil. Similarly, donepezil (1 and 3 mg/kg s.c.) dose-dependently increased frontal cortical gamma power in the freely moving rat and pretreatment with idalopirdine (10 mg/kg p.o.) augmented the effect of donepezil 1 mg/kg. Analysis of the sleep-wake architecture showed that donepezil (1 and 3 mg/kg s.c.) dose-dependently delayed sleep onset and decreased the time spent in both REM and non REM sleep stages. In contrast, idalopirdine (10 mg/kg p.o.) did not affect sleep-wake architecture nor the effects of donepezil. In summary, we show that idalopirdine potentiates the effects of donepezil on frontal cortical gamma oscillations, a pharmacodynamic biomarker associated with cognition, without modifying the effects of donepezil on sleep. The increased cortical excitability may contribute to the procognitive effects of idalopirdine in donepezil

  20. Stability of paclitaxel with ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site administration.

    Science.gov (United States)

    Burm, J P; Jhee, S S; Chin, A; Moon, Y S; Jeong, E; Nii, L; Fox, J L; Gill, M A

    1994-05-01

    The stability of paclitaxel with either ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site injection at room temperature was studied. Triplicate test solutions of paclitaxel 0.3 and 1.2 mg/mL were admixed 1:1 with ondansetron 0.03 and 0.3 mg/mL (as the hydrochloride salt) or ranitidine 0.5 and 2.0 mg/mL (as the hydrochloride salt). Also, paclitaxel 1.2 mg/mL was admixed 1:1:1 with ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL. The solutions were stored in glass containers at room temperature, and samples were removed at zero, one, two, and four hours for immediate assay. At the time of the assay and before any dilution, each sample was visually inspected for clarity, color, and precipitation, and the pH was determined. Drug concentrations were measured by stability-indicating high-performance liquid chromatographic procedures. Throughout the study, more than 90% of the initial concentrations of paclitaxel, ondansetron, and ranitidine remained in the solutions. No precipitates, color changes, or haziness was seen. The changes in pH were minor. Paclitaxel in concentrations of 0.3 and 1.2 mg/mL was stable when mixed with either ondansetron (0.03 or 0.3 mg/mL, as the hydrochloride salt) or ranitidine (0.5 or 2.0 mg/mL, as the hydrochloride salt) and stored in glass containers for four hours. Paclitaxel 1.2 mg/mL was also stable when mixed with both ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL and stored in glass containers for four hours.

  1. Simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride by reverse phase high performance liquid chromatography

    Directory of Open Access Journals (Sweden)

    Nalini C

    2006-01-01

    Full Text Available A reversed phase high performance liquid chromatographic method has been developed using Shimadzu HPLC-VP series, LC-10 ATV pump, SPD10 AVP and C8 column, for simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride in three marketed tablet formulations (extended release. The mobile phase consists of phosphate buffer of pH 7.0 and acetonitrile HPLC grade in the ratio of 1:1. The flow rate was maintained at 1 ml/min and the ultraviolet detection was done at 242 nm, which is the isosbestic point. Linearity coefficients, assay values, recovery studies and repeatability studies showed that the method is accurate and precise.

  2. Effect of matrine hydrochloride on liver injury

    Institute of Scientific and Technical Information of China (English)

    CHEN Li-bo; XU Feng; MA Wen-hui

    2008-01-01

    Objective Searching the function that the Injection of the matrine hydrochloride prevents and cures acute chemical liver injury of mice、 immunity liver injury of mice and chronic liver injury of rats. Methods Acute hepatic injury models of mice induced by Chemical poison carbon tetrachloride (CCl4), thioacetamide(TAA), D-galactosamine(D-GalN), immunity hepatic injury model of mice induced by BCG and fat polysaccharide (LPS), chronic liver injury model of rats induced by CCI, were introduced in the experiment. The serum ALT and AST were measured in acute hepatic injury experiments. Serum ALT, AST, AKP, ALB, TP, BiL-T, ereatinine, triglyceride, sialie acid, larninin, hyaluronic acid, type Ⅲ proeollagen and type Ⅳ collagen, hepatic hydroxyproline (HyP) of rats in chronic liver injury animals were determined after Injection of the matrine hydrochloride. Results The Injection of the matrine hydrochloride reduced serum ALT and AST level of acute chemical liver injury of mice induced by CCl4, TAA and D-GaIN. The index of the liver and the spleen of immunity liver injury of mice induced by BCG and LPS were decreased after the injection of matrine hydrochloride treatment. Compared with the model group, the injection may obviously inhibited serum ALT, AST, TP, AKP, TRI, BiL-T, creatinine, triglyceride, sialic acid, laminin , hyaluronic acid , type Ⅲ procollagen and type Ⅳ collagen activity of chronic liver injury of rats induced by CCl4, elevated ALB、A/G, reduced the liver HyP, decreased the index of the liver and the spleen. The liver visual observation, the pathology inspection and the HAI grading result showed the injection may reduce the inflammatory activity in liver tissue, restrain the liver cell damage, reduce the pseudolobuli formation. Conclusions The Injection of matrine hydrochloride had the protective function to acute chemical hepatic injury of mice induced by CCl4、TAA、D-GalN、immunity hepatic injury of mice induced by the BCG and LPS and

  3. The Efficacy of Licensed-Indication Use of Donepezil and Memantine Monotherapies for Treating Behavioural and Psychological Symptoms of Dementia in Patients with Alzheimer's Disease: Systematic Review and Meta-Analysis

    Science.gov (United States)

    Lockhart, I.A.; Orme, M.E.; Mitchell, S.A.

    2011-01-01

    Background/Aims Behavioural and psychological symptoms of dementia (BPSD) in Alzheimer's disease (AD) greatly increase caregiver burden. The abilities of donepezil and memantine to manage BPSD within their licensed indications in AD were compared. Methods A systematic review, random effects meta-analysis and Bucher indirect comparison were conducted. Results Six randomised controlled studies (4 donepezil and 2 memantine) reported use within the licensed indication and had Neuropsychiatric Inventory (NPI) data suitable for meta-analysis. BPSD showed significant improvement with donepezil compared with placebo [weighted mean difference (WMD) in NPI −3.51, 95% confidence interval (CI) −5.75, −1.27], whereas this was not the case for memantine (WMD −1.65, 95% CI −4.78, 1.49). WMD in NPI for donepezil versus memantine favoured donepezil but was not statistically significant (−1.86, 95% CI −5.71, 1.99; p = 0.34). Conclusion Within its licensed indication, donepezil is efficacious for the management of BPSD in AD compared with placebo. PMID:22163246

  4. The Efficacy of Licensed-Indication Use of Donepezil and Memantine Monotherapies for Treating Behavioural and Psychological Symptoms of Dementia in Patients with Alzheimer’s Disease: Systematic Review and Meta-Analysis

    Directory of Open Access Journals (Sweden)

    I.A. Lockhart

    2011-07-01

    Full Text Available Background/Aims: Behavioural and psychological symptoms of dementia (BPSD in Alzheimer’s disease (AD greatly increase caregiver burden. The abilities of donepezil and memantine to manage BPSD within their licensed indications in AD were compared. Methods: A systematic review, random effects meta-analysis and Bucher indirect comparison were conducted. Results: Six randomised controlled studies (4 donepezil and 2 memantine reported use within the licensed indication and had Neuropsychiatric Inventory (NPI data suitable for meta-analysis. BPSD showed significant improvement with donepezil compared with placebo [weighted mean difference (WMD in NPI –3.51, 95% confidence interval (CI –5.75, –1.27], whereas this was not the case for memantine (WMD –1.65, 95% CI –4.78, 1.49. WMD in NPI for donepezil versus memantine favoured donepezil but was not statistically significant (–1.86, 95% CI –5.71, 1.99; p = 0.34. Conclusion: Within its licensed indication, donepezil is efficacious for the management of BPSD in AD compared with placebo.

  5. 银杏叶片联合盐酸多奈哌齐治疗老年轻度认知功能障碍的临床研究%Clinical study on Ginkgo Biloba leaves extract tablets combined with donepezil in the treatment of mild cognitive impairment in the elderly

    Institute of Scientific and Technical Information of China (English)

    刘洋

    2015-01-01

    目的:探讨银杏叶片联合盐酸多奈哌齐在老年轻度认知功能障碍患者中的应用效果。方法:将我院门诊就诊的100例老年轻度认知功能障碍患者,随机分成治疗组与对照组,均50例,对照组患者采用盐酸多奈哌齐进行治疗,治疗组在盐酸多奈哌齐治疗的基础上联合银杏叶片进行治疗,对比两组患者治疗后的临床疗效。结果:治疗组患者总有效率为98.00%,与对照组患者的76.00%对比,差异有统计学意义( P<0.05),治疗组治疗后的脑电图(EEG )异常率为26.00%,显著低于对照组患者的48.00%,差异有统计学意义( P<0.05);两组患者治疗3个月简易智力状态检查量表(MMSE)评分均显著高于治疗前,治疗组治疗6个月、9个月的MMSE评分均显著高于对照组患者,差异均有统计学意义(P<0.05)。结论:在盐酸多奈哌齐治疗基础上联合银杏叶片治疗老年轻度认知功能障碍患者,可有效提高治疗质量,改善其认知功能与脑部活动状态,具备较高的应用价值。%Objective:To investigate the Ginkgo Biloba Leaves Extract Tablets combined with donepezil hydrochloride in the application effect of mild cognitive impairment in the elderly patients .Methods:100 cases of mild cognitive impairment in the elderly patients of our hospital ,were randomly divided into treatment group and control group ,all 50 cases ,patients in control group were treated by donepezil hydrochloride treatment ,treatment group were combined Ginkgo Biloba Leaves Extract Tablets based on donepezil hydrochloride on the treatment of treatment ,the clini‐cal efficacy were compared between two groups after treatment .Results:the patients in the treatment group the total ef‐fective rate was 98 .00% ,and the control of the 76 .00% groups were compared ,the difference was statistically significant (P<0 .05) ,the treatment group after

  6. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride capsules. 520.1660b Section 520.1660b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Oxytetracycline hydrochloride capsules. (a) Specifications. The drug is in capsule form with each capsule...

  7. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride capsules. 520.2345a... Tetracycline hydrochloride capsules. (a) Specifications. Each capsule contains 50, 100, 125, 250, or 500... as in paragraph (c) of this section: (1) No. 000009: 250 mg per capsule. (2) No. 000069: 125, 250, or...

  8. 21 CFR 520.1242f - Levamisole hydrochloride gel.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride gel. 520.1242f Section 520.1242f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Levamisole hydrochloride gel. (a) Specifications. The drug is a gel containing 11.5 percent...

  9. 21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride oral dosage forms. 520.1242 Section 520.1242 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242 Levamisole hydrochloride oral dosage...

  10. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242e Levamisole hydrochloride...

  11. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms. ...

  12. Vibrational spectra of pilocarpine hydrochloride crystals

    Energy Technology Data Exchange (ETDEWEB)

    Bento, R.R.F. [Universidade Federal de Mato Grosso (UFMT), Cuiaba, MT (Brazil). Inst. de Fisica; Freire, P.T.C. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Fisica]. E-mail: tarso@fisica.ufc.br; Teixeira, A.M.R.; Silva, J.H. [Universidade Regional do Cariri, Crato, CE (Brazil). Dept. Ciencias Fisicas e Biologicas; Lima Junior, J.A. [Universidade Estadual do Ceara (UECE), Limoeiro do Norte, CE (Brazil); Oliveira, M.C.F. de; Andrade-Neto, M. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Quimica Organica e Inorganica; Romero, N.R. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Farmacia; Pontes, F.M. [Universidade Estadual Paulista, Bauru, SP (Brazil). Faculdade de Ciencias

    2009-03-15

    Pilocarpine is a natural substance with potential application in the treatment of several diseases. In this work Fourier Transform (FT)-Raman spectrum and the Fourier Transform infra red (FT-IR) spectrum of pilocarpine hydrochloride C{sub 11} H{sub 17} N{sub 2} O{sup +}{sub 2} .Cl{sup -1} were investigated at 300 K. Vibrational wavenumber and wave vector have been predicted using density functional theory (B3LYP) calculations with the 6-31 G(d,p) basis set. A comparison with experiment allowed to assign most of the normal modes of the crystal. (author)

  13. The effect of stimulation therapy and donepezil on cognitive function in Alzheimer’s disease. A community based RCT with a two-by-two factorial design

    Directory of Open Access Journals (Sweden)

    Andersen Fred

    2012-07-01

    Full Text Available Abstract Background Progressive neurodegeneration in Alzheimer’s disease (AD induces cognitive deterioration, and there is controversy regarding the optimal treatment strategy in early AD. Stimulation therapy, including physical exercise and cholinesterase inhibitors are both reported to postpone cognitive deterioration in separate studies. We aimed to study the effect of stimulation therapy and the additional effect of donepezil on cognitive function in early AD. Method Design: A two-by-two factorial trial comprising stimulation therapy for one year compared to standard care to which a randomized double-blinded placebo controlled trial with donepezil was added. Setting: Nine rural municipalities in Northern Norway. Participants: 187 participants 65 years and older with a recent diagnosis of mild or moderate AD were included in the study of which 146 completed a one-year follow-up. INTERVENTIONS: In five municipalities the participants received stimulation therapy whereas participants in four received standard care. All participants were randomised double-blindly to donepezil or placebo and tested with three different cognitive tests four times during the one-year study period. Main outcome: Changes in MMSE sum score. Secondary outcome: Changes in ADAS-Cog and Clock Drawing Test. Results MMSE scores remained unchanged amongst AD participants receiving stimulation therapy and those receiving standard care. The results were consistent for ADAS-Cog and Clock Drawing Test. No time trend differences were found during one-year follow-up between groups receiving stimulation therapy versus standard care or between donepezil versus placebo. Conclusion In rural AD patients non-pharmacological and pharmacological therapy did not improve outcome compared with standard care but all groups retained cognitive function during one year follow-up. Other studies are needed to confirm these results. Trial registration ClinicalTrials.gov (Identifier: NCT00443014

  14. Protection by sigma-1 receptor agonists is synergic with donepezil, but not with memantine, in a mouse model of amyloid-induced memory impairments.

    Science.gov (United States)

    Maurice, Tangui

    2016-01-01

    Drugs activating the sigma-1 (σ1) chaperone protein are anti-amnesic and neuroprotective in neurodegenerative pathologies like Alzheimer's disease (AD). Since these so-called σ1 receptor (σ1R) agonists modulate cholinergic and glutamatergic systems in a variety of physiological responses, we addressed their putative additive/synergistic action in combination with cholinergic or glutamatergic drugs. The selective σ1 agonist PRE-084, or the non-selective σ1 drug ANAVEX2-73 was combined with the acetylcholinesterase inhibitor donepezil or the NMDA receptor antagonist memantine in the nontransgenic mouse model of AD-like memory impairments induced by intracerebroventricular injection of oligomeric Aβ25-35 peptide. Two behavioral tests, spontaneous alternation and passive avoidance response, were used in parallel and both protective and symptomatic effects were examined. After determination of the minimally active doses for each compound, the combinations were tested and the combination index (CI) calculated. Combinations between the σ1 agonists and donepezil showed a synergic protective effect, with CI1. Symptomatic effects appeared only additive for all combinations, with CI=1. A pharmacological analysis of the PRE-084+donepezil combination revealed that the synergy could be due to an inter-related mechanism involving α7 nicotinic ACh receptors and σ1R. These results demonstrated that σ1 drugs do not only offer a protective potential alone but also in combination with other therapeutic agents. The nature of neuromodulatory molecular chaperone of the σ1R could eventually lead to synergistic combinations.

  15. Risk Factors of Dementia after Cerebral Infarction and Therapeutic Effect of Donepezil%脑梗死后痴呆的危险因素分析及多奈哌齐的治疗效果研究

    Institute of Scientific and Technical Information of China (English)

    吴永斌; 赵丽; 杨昕

    2014-01-01

    Objective To explore the risk factors of dementia after cerebral infarction,and to study the therapeutic effect of donepezil. Methods A total of 150 patients with cerebral infarction who admitted to The First People′s Hospital of Shi-zuishan City,hospital from May 2009 to May 2012,were selected as study subjects,among whom 47 cases(31. 3% )had de-mentia. The risk factors of dementia after cerebral infarction were analyzed by univariate analysis and multivariate Logistic regres-sion analysis. The patients with dementia after cerebral infarction were divided into control group(22 cases)and observation group(25 cases),the control group was given conventional treatment,the observation group was given conventional treatment and donepezil hydrochloride tablets. After 9 months of follow - up,the therapeutic effect,cognitive function and activities of daily living were observed among patients with dementia after cerebral infarction. Results The dementia was related to age,de-gree of education,occupation,diabetes,smoking,hyperlipemia,hyperlipidemia and heart disease among patients with cere-bral infarction( P ﹤ 0. 05). According to Logistic regression analysis results,age,smoking,diabetes,and hyperlipidemia were the risk infactors for dementia after cerebral infarction and(OR = 1. 107、1. 961、1. 146、1. 148,P ﹤ 0. 05). After 9 months,the therapeutic effect of observation group was better than that of control group( P ﹤ 0. 05). After 6 months and 9 months of treatment,the scores of MoCA and MMSE in observation group were significantly higher than those in control group, the ADL score in observation group was significantly lower than that in control group(P ﹤ 0. 05). Conclusion Advanced age, diabetes,smoking and hyperlipemia were risk factors for dementia after cerebral infarction. Application of donepezil on the basis of routine treatment can obviously improve cognitive function and life function,and has better long - term therapeutic effects.%目的:探讨

  16. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)].

    Science.gov (United States)

    Fujii, Y; Ishii, Y; Suzuki, T; Murayama, S

    1979-10-01

    Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone.

  17. Neuroprotective effect of penehyclidine hydrochloride on focal cerebral ischemiareperfusion injury

    Institute of Scientific and Technical Information of China (English)

    Cuicui Yu; Junke Wang

    2013-01-01

    Penehyclidine hydrochloride can promote microcirculation and reduce vascular permeability. However, the role of penehyclidine hydrochloride in cerebral ischemia-reperfusion injury remains unclear. In this study, in vivo middle cerebral artery occlusion models were established in experimental rats, and penehyclidine hydrochloride pretreatment was given via intravenous injection prior to model establishment. Tetrazolium chloride, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling and immunohistochemical staining showed that, penehyclidine hydrochloride pretreatment markedly attenuated neuronal histopathological changes in the cortex, hippocampus and striatum, reduced infarction size, increased the expression level of Bcl-2, decreased the expression level of caspase-3, and inhibited neuronal apoptosis in rats with cerebral ischemia-reperfusion injury. Xanthine oxidase and thiobarbituric acid chromogenic results showed that penehyclidine hydrochloride upregulated the activity of superoxide dismutase and downregulated the concentration of malondialdehyde in the ischemic cerebral cortex and hippocampus, as well as reduced the concentration of extracellular excitatory amino acids in rats with cerebral ischemia-reperfusion injury. In addition, penehyclidine hydrochloride inhibited the expression level of the NR1 subunit in hippocampal nerve cells in vitro following oxygen-glucose deprivation, as detected by PCR. Experimental findings indicate that penehyclidine hydrochloride attenuates neuronal apoptosis and oxidative stress injury after focal cerebral ischemia-reperfusion, thus exerting a neuroprotective effect.

  18. Identification of polymorphism in ethylone hydrochloride: synthesis and characterization.

    Science.gov (United States)

    Maheux, Chad R; Alarcon, Idralyn Q; Copeland, Catherine R; Cameron, T Stanley; Linden, Anthony; Grossert, J Stuart

    2016-08-01

    Ethylone, a synthetic cathinone with psychoactive properties, is a designer drug which has appeared on the recreational drug market in recent years. Since 2012, illicit shipments of ethylone hydrochloride have been intercepted with increasing frequency at the Canadian border. Analysis has revealed that ethylone hydrochloride exists as two distinct polymorphs. In addition, several minor impurities were detected in some seized exhibits. In this study, the two conformational polymorphs of ethylone hydrochloride have been synthesized and fully characterized by FTIR, FT-Raman, powder XRD, GC-MS, ESI-MS/MS and NMR ((13) C CPMAS, (1) H, (13) C). The two polymorphs can be distinguished by vibrational spectroscopy, solid-state nuclear magnetic resonance spectroscopy and X-ray diffraction. The FTIR data are applied to the identification of both polymorphs of ethylone hydrochloride (mixed with methylone hydrochloride) in a laboratory submission labelled as 'Ocean Snow Ultra'. The data presented in this study will assist forensic scientists in the differentiation of the two ethylone hydrochloride polymorphs. This report, alongside our recent article on the single crystal X-ray structure of a second polymorph of this synthetic cathinone, is the first to confirm polymorphism in ethylone hydrochloride. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd.

  19. Capillary electrophoresis coupled with electrochemiluminescence for determination of cloperastine hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Objective To investigate the electrochemiluminescence (ECL) behavior of cloperastine hydrochloride. Methods ECL intensity of tris (2,2′-bipyridyl) rutheniumo(Ⅱ) was enhanced, the method for the determination of cloperastine hydrochloride was established using capillary electrophoresis (CE) coupled with electrochemilumolinescence (ECL) detection. Results Under the optimum conditions, ECL intensity varied linearly with cloperastine hydrochloride concentration from 7.0×10-6g/mL to 1.0×10-4g/mL. The detection l...

  20. COMPARISON OF DROTAVERINE HYDROCHLORIDE AND VALETHAMATE BROMIDE ON CERVICAL DILATATION

    Directory of Open Access Journals (Sweden)

    Mallika Selvaraj

    2016-06-01

    Full Text Available AIM To compare the two drugs drotaverine hydrochloride and valethamate bromide and their effects on cervical dilatation and labour duration. METHODOLOGY It is a prospective study undertaken at Government Rajaji Hospital on 150 randomly selected primigravidae patients. RESULTS The duration of active phase of first stage of labour was significantly reduced (p value 0.003, rate of cervical dilatation was higher (p value 0.0001 with drotaverine hydrochloride. CONCLUSION Drotaverine hydrochloride is a safe, potent and effective drug to be used in the active phase of labour.

  1. A novel formulation for mebeverine hydrochloride.

    Science.gov (United States)

    Abdel-Hamid, Sameh M; Abdel-Hady, Seham E; El-Shamy, Abdel-Hamid A; El-Dessouky, Hadir F

    2007-10-01

    The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time. Formulations were characterized in terms of drug release, mucoadhesion and rheology. Clinically, the selected formula has shown faster onset (p = 0.0156), longer duration (p = 0.0313), better film residence (p = 0.0313), and no foreign body sensation (p = 0.0313) in comparison to Solcoseryl dental paste. Histopathological examination showed no change in inflammatory cells count, concluding that this topical anesthetic is efficacious and safe orally.

  2. "Sustained release formulation of Metoclopramide Hydrochloride "

    Directory of Open Access Journals (Sweden)

    Dabbagh MA

    2000-08-01

    Full Text Available In this research, several formulations containing, an anti emetic agent (Metoclopramide hydrochloride, a hydrophilic polymer (hydroxypropylmethylcellulose and a hydrophobic polymer (ethylcellulose 10 cP were prepared by direct compression. Different factors such as: the effect of different ratios of the polymers, particle size, pressure force and differences of release in acidic and distilled water as media were investigated. After developing the ideal formulation, the effect of changing the ratio of drug in core: coating on the formulation was investigated. Coating of tablets with ethylcellulose, changed the release mechanism of drug and shifted it to near zero order release. The results showed that except when matrices were coated with ethylcellulose, drug release was proportioned to the square root of time, which might be due to the change of release pattern from matrix to reservoir system.

  3. Effect of sertraline hydrochloride on dialysis hypotension.

    Science.gov (United States)

    Dheenan, S; Venkatesan, J; Grubb, B P; Henrich, W L

    1998-04-01

    Hemodialysis hypotension (HH) is a very common disorder and has a multifactorial etiology. Autonomic dysfunction occurs in up to 50% of patients with end-stage renal disease (ESRD) and plays a key role in HH in some patients. Sertraline hydrochloride, a central nervous system serotonin reuptake inhibitor, has been shown to be an effective treatment of hypotension caused by autonomic dysfunction in disorders such as neurocardiogenic syncope and idiopathic orthostatic hypotension. This study sought to determine whether sertraline was effective in ameliorating HH. A retrospective chart analysis was performed that included nine consecutive patients (aged > or = 54 years, time on hemodialysis > or = 2.2 years) placed on sertraline (50 to 100 mg/d) for depression who also had HH (defined as prehemodialysis systolic blood pressure [SBP] or = 40 mm Hg decrease in SBP during hemodialysis, SBP sertraline. The data from a 6-week pre-sertraline period were compared with the data from a 6-week sertraline period (defined as 6 weeks after drug begun). Blood pressure medications were unchanged during the trial period of sertraline. However, nadir mean arterial pressure recorded during a given dialysis session in the pre-sertraline period (55+/-4 mm Hg) was significantly lower than that recorded in the sertraline period (68+/-5 mm Hg; P sertraline period was significantly lower than that during the pre-sertraline period (mean, 0.6+/-0.2 episodes per session v 1.4+/-0.3 episodes per session; P sertraline period was also significantly less than that during the pre-sertraline period (mean, 1.7+/-0.8 interventions v 11.0+/-3.0 interventions; P sertraline hydrochloride reduces HH in some patients with ESRD. A possible mechanism for this effect is sertraline-induced attenuation of the paradoxical sympathetic withdrawal that may underlie HH in some patients with ESRD.

  4. Dyeing Characteristics of Chitosan Biguanidine Hydrochloride Treated Wool Fabrics

    Institute of Scientific and Technical Information of China (English)

    ZHAO Xue; HE JIN-xin

    2010-01-01

    @@ Chitosan biguanidine hydrochloride(CGH)has been synthesized by the guanidineylation reaction of chitosan with dicyandiamide.The structures of CGH were characterized by Fourier transform infrared spectroscopy and 13CNMR spectra.

  5. Non-pigmented fixed drug eruption induced by eprazinone hydrochloride.

    Science.gov (United States)

    Tanabe, Kenichi; Tsuboi, Hiromi; Maejima, Hideki; Arai, Satoru; Katsuoka, Kensei

    2005-12-01

    A 68-year-old woman developed an upper respiratory tract infection in November 2002 and was treated with eprazinone hydrochloride, serrapeptase, carbocysteine and clarithromycin. Three days after the start of treatment, the patient noted erythema on her axilla, buttock and inguinal regions. The erythema subsided in 7 days although slight pigmentation remained. However, 7 days later the pigmentation completely disappeared. Oral eprazinone hydrochloride was given as a challenge, and 1 day later the erythema re-appeared in the same areas as on initial presentation (axilla, buttock, and inguinal regions). A fixed erythema without lasting pigmentation is attributed to eprazinone hydrochloride. Therefore, the patient was diagnosed as having a nonpigmented fixed drug eruption associated with eprazinone hydrochloride.

  6. Antifungal activity of hydrochloride salts of tylophorinidine and tylophorinine.

    Science.gov (United States)

    Dhiman, Mini; Parab, Rajashri R; Manju, Sreedharannair L; Desai, Dattatraya C; Mahajan, Girish B

    2012-09-01

    The antimicrobial efficacy of two phenanthroindolizidine alkaloids, tylophorinidine hydrochloride (TdnH) and tylophorinine hydrochloride (TnnH), isolated from the plant Tylophora indica (local name, Antamul) was evaluated. These were screened for in vitro antifungal and antibacterial activities. Both compounds exhibited potent antifungal activity displaying minimum inhibitory concentrations (MIC) in the range of 2-4 microg/mL for TdnH and 0.6-2.5 microg/mL for TnnH against Candida species.

  7. Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops

    OpenAIRE

    Eiichi Uchio

    2008-01-01

    Eiichi UchioDepartment of Ophthalmology, Fukuoka University School of Medicine, Fukuoka, JapanAbstract: Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H1 receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol®) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine...

  8. COMPARISON OF DROTAVERINE HYDROCHLORIDE AND VALETHAMATE BROMIDE ON CERVICAL DILATATION

    OpenAIRE

    Mallika Selvaraj; Sumathi

    2016-01-01

    AIM To compare the two drugs drotaverine hydrochloride and valethamate bromide and their effects on cervical dilatation and labour duration. METHODOLOGY It is a prospective study undertaken at Government Rajaji Hospital on 150 randomly selected primigravidae patients. RESULTS The duration of active phase of first stage of labour was significantly reduced (p value 0.003), rate of cervical dilatation was higher (p value 0.0001) with drotaverine hydrochloride. CONCLUS...

  9. Simultaneous Spectrophotometric Determination of Drotaverine Hydrochloride and Paracetamol in Tablet

    OpenAIRE

    Mahaparale Sonali; Telekone R; Raut R; Damle S; Kasture P

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamo...

  10. Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen.

    Science.gov (United States)

    Luo, Zonghua; Sheng, Jianfei; Sun, Yang; Lu, Chuanjun; Yan, Jun; Liu, Anqiu; Luo, Hai-Bin; Huang, Ling; Li, Xingshu

    2013-11-27

    A novel series of compounds obtained by fusing the cholinesterase inhibitor donepezil and the antioxidant ebselen were designed as multi-target-directed ligands against Alzheimer's disease. An in vitro assay showed that some of these molecules did not exhibit highly potent cholinesterase inhibitory activity but did have various other ebselen-related pharmacological effects. Among the molecules, compound 7d, one of the most potent acetylcholinesterase inhibitors (IC50 values of 0.042 μM for Electrophorus electricus acetylcholinesterase and 0.097 μM for human acetylcholinesterase), was found to be a strong butyrylcholinesterase inhibitor (IC50 = 1.586 μM), to possess rapid H2O2 and peroxynitrite scavenging activity and glutathione peroxidase-like activity (ν0 = 123.5 μM min(-1)), and to be a substrate of mammalian TrxR. A toxicity test in mice showed no acute toxicity at doses of up to 2000 mg/kg. According to an in vitro blood-brain barrier model, 7d is able to penetrate the central nervous system.

  11. Effects of memantine and donepezil on cortical and hippocampal acetylcholine levels and object recognition memory in rats.

    Science.gov (United States)

    Ihalainen, Jouni; Sarajärvi, Timo; Rasmusson, Doug; Kemppainen, Susanna; Keski-Rahkonen, Pekka; Lehtonen, Marko; Banerjee, Pradeep K; Semba, Kazue; Tanila, Heikki

    2011-01-01

    This preclinical study investigated the ability of memantine (MEM) to stimulate brain acetylcholine (ACh) release, potentially acting synergistically with donepezil (DON, an acetylcholinesterase inhibitor). Acute systemic administration of either MEM or DON to anesthetized rats caused dose-dependent increases of ACh levels in neocortex and hippocampus, and the combination of MEM (5 mg/kg) and DON (0.5 mg/kg) produced significantly greater increases than either drug alone. To determine whether ACh release correlated with cognitive improvement, rats with partial fimbria-fornix (FF) lesions were treated with acute or chronic MEM or DON. Acute MEM treatment significantly elevated baseline hippocampal ACh release but did not significantly improve task performance on a delayed non-match-to-sample (DNMS) task, whereas chronic MEM treatment significantly improved DNMS performance but only marginally elevated baseline ACh levels. Acute or chronic treatment with DON (in the presence of neostigmine to allow ACh collection) did not significantly improve DNMS performance or alter ACh release. In order to investigate the effect of adding MEM to ongoing DON therapy, lesioned rats pretreated with DON for 3 weeks were given a single intraperitoneal dose of MEM. MEM significantly elevated baseline hippocampal ACh levels, but did not significantly improve DNMS task scores compared to chronic DON-treated animals. These data indicate that MEM, in addition to acting as an NMDA receptor antagonist, can also augment ACh release; however, in this preclinical model, increased ACh levels did not directly correlate with improved cognitive performance.

  12. A Post Hoc Analysis of D-Threo-Methylphenidate Hydrochloride (Focalin) Versus D,l-Threo-Methylphenidate Hydrochloride (Ritalin)

    Science.gov (United States)

    Weiss, Margaret; Wasdell, Michael; Patin, John

    2004-01-01

    Objective: To evaluate clinical measures of the benefit/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH). Method: Data from a phase III clinical trial was used to compare equimolar doses of d-MPH and d,l-MPH treatment for…

  13. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse.

    Science.gov (United States)

    Provensi, Gustavo; Costa, Alessia; Passani, M Beatrice; Blandina, Patrizio

    2016-10-01

    Histaminergic H3 receptors (H3R) antagonists enhance cognition in preclinical models and modulate neurotransmission, in particular acetylcholine (ACh) release in the cortex and hippocampus, two brain areas involved in memory processing. The cognitive deficits seen in aging and Alzheimer's disease have been associated with brain cholinergic deficits. Donepezil is one of the acetylcholinesterase (AChE) inhibitor approved for use across the full spectrum of these cognitive disorders. We addressed the question if H3R antagonists and donepezil require an intact histamine neuronal system to exert their procognitive effects. The effect of the H3R antagonist ABT-239 and donepezil were evaluated in the object recognition test (ORT), and on the level of glycogen synthase kinase 3 beta (GSK-3β) phosphorylation in normal and histamine-depleted mice. Systemic administration of ABT-239 or donepezil ameliorated the cognitive performance in the ORT. However, these compounds were ineffective in either genetically (histidine decarboxylase knock-out, HDC-KO) or pharmacologically, by means of intracerebroventricular (i.c.v.) injections of the HDC irreversible inhibitor a-fluoromethylhistidine (a-FMHis), histamine-deficient mice. Western blot analysis revealed that ABT-239 or donepezil systemic treatments increased GSK-3β phosphorylation in cortical and hippocampal homogenates of normal, but not of histamine-depleted mice. Furthermore, administration of the PI3K inhibitor LY294002 that blocks GSK-3β phosphorylation, prevented the procognitive effects of both drugs in normal mice. Our results indicate that both donepezil and ABT-239 require the integrity of the brain histaminergic system to exert their procognitive effects and strongly suggest that impairments of PI3K/AKT/GSK-3β intracellular pathway activation is responsible for the inefficacy of both drugs in histamine-deficient animals.

  14. Simultaneous Estimation of Gemcitabine Hydrochloride and Capecitabine Hydrochloride in Combined Tablet Dosage Form by RP-HPLC Method

    Directory of Open Access Journals (Sweden)

    V. Rajesh

    2011-01-01

    Full Text Available A new reverse phase high performance liquid chromatography (RP-HPLC method has been developed for the simultaneous estimation of gemcitabine hydrochloride and capecitabine hydrochloride in combined tablet dosage form. An inertsil ODS-3 C-18 column having dimensions of 250×4.6 mm and particle size of 5 µm, with mobile phase containing a mixture of acetonitrile : water : triethyelamine in the ratio of (70 : 28 : 2v/v was used. The pH of mobile phase was adjusted to 4.0 with ortho-phosphoric acid. The flow rate was 1 mL/min and the column effluents were monitored at 260 nm. The retention time for gemcitabine hydrochloride and capecitabine hydrochloride was found to be 2.76 and 2.3 min respectively. The proposed method was validated in terms of linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The method was found to be linear in the range of 10-50 µg/mL and 4-24 µg/mL for gemcitabine hydrochloride and capecitabine hydrochloride, with regression coefficient r = 0.999 and r = 0.999, respectively.

  15. Differential effects of the muscarinic M1 receptor agonist RS-86 and the acetylcholine-esterase inhibitor donepezil on REM sleep regulation in healthy volunteers.

    Science.gov (United States)

    Nissen, Christoph; Nofzinger, Eric A; Feige, Bernd; Waldheim, Bernhard; Radosa, Marc-Philipp; Riemann, Dieter; Berger, Mathias

    2006-06-01

    Broad evidence from preclinical and clinical research indicates that cholinergic neurotransmission contributes significantly to the generation of rapid eye movement (REM) sleep. However, a potential role of different acetylcholine receptor (AChR) subtypes for the regulation of three main aspects of REM sleep, (1) REM onset, (2) REM maintenance, and (3) generation of REMs, are not clear. In the present double-blind, randomized and placebo-controlled study, we investigated the differential effects of the M1 muscarinic AChR (mAChR) agonist RS-86 and the ACh-esterase inhibitor donepezil to further specify the AChR subtype function on REM sleep regulation in n = 20 healthy volunteers. We found that RS-86 selectively shortened REM latency (multivariate analysis of variance post hoc contrast p = 0.024 compared to placebo, not significant for donepezil) and that donepezil specifically enhanced the duration of REM sleep (% sleep period time, p = 0.000 compared to placebo; p = 0.003 compared to RS-86) and the number of REMs (p = 0.000 compared to placebo; p = 0.000 compared to RS-86). These results provide evidence that the onset of REM sleep is, in part, mediated by M1 mAChR activity, whereas the maintenance of REM sleep and the number of REMs are mediated by non-M1, but presumably M2 mAChR activity. These findings are of interest for the understanding of sleep regulation and of neuropsychiatric disorders, such as Alzheimer's dementia and depressive disorders, whose etiopathology may involve alterations in cholinergic neurotransmission.

  16. A double-blind placebo-controlled randomized trial of Melissa officinalis oil and donepezil for the treatment of agitation in Alzheimer's disease.

    Science.gov (United States)

    Burns, Alistair; Perry, Elaine; Holmes, Clive; Francis, Paul; Morris, Julie; Howes, Melanie-Jayne R; Chazot, Paul; Lees, George; Ballard, Clive

    2011-01-01

    Behavioural and psychological symptoms (BPSD) are frequent in people with Alzheimer's disease and cause considerable stress to patients and their carers. Antipsychotics have been widely used as a first-line treatment, resulting in an estimated 1,800 excess strokes and 1,600 excess deaths in the UK alone. Safe and effective alternatives are urgently needed. Based upon preliminary evidence from clinical trials, aromatherapy with melissa oil may be such an alternative, but initial studies have been modest in size, and adequate blinding has been problematic. Our objective was to assess the efficacy of melissa aromatherapy in the treatment of agitation in people with Alzheimer's disease in an adequately powered and robustly blinded randomized controlled trial comparing it with donepezil, an anticholinesterase drug used with some benefit to treat BPSD. The study was a double-blind parallel-group placebo-controlled randomized trial across 3 specialist old age psychiatry centres in England. Participants had probable or possible Alzheimer's disease, were resident in a care home, had clinically significant agitation (defined as a score of 39 or above on the Cohen Mansfield Agitation Inventory) and were free of antipsychotics and/or anticholinesterase for at least 2 weeks. Participants were allocated to 1 of 3 groups: placebo medication and active aromatherapy; active medication and placebo aromatherapy or placebo of both. The primary outcome measure was reduction in agitation as assessed by the Pittsburgh Agitation Scale (PAS) at 4 weeks. This is an observational scale, and raters were required to wear nose clips to ensure that full blinding was maintained. The PAS, Neuropsychiatric Inventory (NPI; another measure of BPSD) and other outcome measures were completed at baseline, 4-week and 12-week follow-ups. 114 participants were randomized, of whom 94 completed the week 4 assessment and 81 completed the week 12 assessment. Aromatherapy and donepezil were well tolerated

  17. Distinctive Effect of Donepezil Treatment on P300 and N200 Subcomponents of Auditory Event-Related Evoked Potentials in Alzheimer Disease Patients

    OpenAIRE

    2015-01-01

    Background Latency of P300 subcomponent of event-related potentials (ERPs) increases in Alzheimer disease (AD) patients, which correlate well with cognitive impairment. Cholinesterase inhibitors (ChEIs) reduce P300 latency in AD patients with parallel improvement in cognition. It is not known whether N200 response to ChEIs is similar to that of P300. The aim of this study was to evaluate and compare characteristics of P300 and N200 in AD patients, treatment-naïve and on stable donepezil treat...

  18. Stability of cefozopran hydrochloride in aqueous solutions.

    Science.gov (United States)

    Zalewski, Przemysław; Skibiński, Robert; Paczkowska, Magdalena; Garbacki, Piotr; Talaczyńska, Alicja; Cielecka-Piontek, Judyta; Jelińska, Anna

    2016-01-01

    The influence of pH on the stability of cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions.

  19. Interaction of articaine hydrochloride with prokaryotic membrane lipids.

    Science.gov (United States)

    Lygre, Henning; Moe, Grete; Nerdal, Willy; Holmsen, Holm

    2009-01-01

    Local anesthetics are the most commonly used drugs in dentistry, with a wide range of effects, including antimicrobial activity. High antimicrobial effects have recently been reported on oral microbes from articaine hydrochloride, revealed by the minimum inhibitory concentration and minimal bactericidal concentration. Additionally, articaine has recently been used as an alkaline component in endodontic materials with a proposed antibacterial activity. However, the detailed mechanisms of action have not been discussed. We determined the Langmuir surface pressure/molecular area isotherms of prokaryotic lipid monolayers, as well as the phospholipid phase transitions, by employing differential scanning calorimetry on unilamellar prokaryotic liposomes (bilayers). Articaine hydrochloride was found to interact with the prokaryotic membrane lipids in both monolayers and bilayers. An increase of the phospholipid molecular area of acidic glycerophospholipids as well as a decrease in phase transition temperature and enthalpy were found with increasing articaine hydrochloride concentration. The thermodynamic changes by adding articaine hydrochloride to prokaryotic membrane lipids are potentially related to the effects observed from antimicrobial peptides resulting from membrane insertion, aggregate composition, pore formation, and lysis. Interaction of articaine hydrochloride with prokaryotic membrane lipids is indicated. Hence, further research is necessary to gain insight into where these compounds exert their effects at the molecular level.

  20. Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin.

    Science.gov (United States)

    Al-Khalili, Mohammad; Meidan, Victor M; Michniak, Bozena B

    2003-01-01

    The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05 to 0.1 mA/cm2 resulted in doubling of the iontophoretic flux of buspirone hydrochloride, while increasing drug concentration from 1% to 2% had no effect on flux. Using phosphate buffer to adjust the pH of the drug solution decreased the buspirone hydrochloride iontophoretic flux relative to water solutions. Incorporating buspirone hydrochloride into ethanol:water (50:50 vol/vol) based gel formulations using carboxymethylcellulose and hydroxypropylmethylcellulose had no effect on iontophoretic delivery. Incorporation of three terpene enhancers (menthol, cineole, and terpineol) into the gel resulted in a synergistic effect when combined with iontophoresis. Menthol was the most active enhancer, and when combined with iontophoresis it was possible to deliver 10 mg/cm2/day of buspirone hydrochloride.

  1. Free radical scavenging effect of donepezil as the possible contribution to its memory enhancing activity in mice.

    Science.gov (United States)

    Umukoro, S; Adewole, F A; Eduviere, A T; Aderibigbe, A O; Onwuchekwa, C

    2014-05-01

    Donepezil (DP) is the major drug currently used for enhancing memory function in patients with Alzheimer's disease (AD), an action ascribed to the elevation of central cholinergic neurotransmission. However, there are indications that DP may protect neurons against injury through the prevention of free radical-mediated neuroinflammation that has been implicated in the pathology of AD. Thus, this study was carried out to examine the effect of DP on memory impairment and on biomarkers of oxidative stress induced by scopolamine (SC) and lipopolysaccharide (LP) in mice.Mice were treated with DP (0.5-4 mg/kg, i. p.) 30 min prior to i. p. injection of SC or LP once daily for 7 days before assessing for memory function utilizing the Y-maze paradigm and levels of biomarkers of oxidative stress using standard biochemical procedures.DP (0.5-2 mg/kg) significantly reversed the memory impairment produced by SC (1 mg/kg) or LP (250 µg/kg) in mice, indicating memory enhancing effect. The increased brain levels of malondialdehyde (MDA) evoked by SC (1 mg/kg) or LP (250 µg/kg), was significantly inhibited by DP (0.5-4 mg/kg), suggesting antioxidant property. Further, DP (0.5-4 mg/kg) significantly inhibited glutathione (GSH) depletion caused by SC (1 mg/kg) or LP (250 µg/kg) in mice brains, which suggest free radical scavenging property.These findings suggest that DP has antioxidant effect, which might be playing a significant role in its memory enhancing activity in mice. However, more detailed studies are necessary to confirm the relevance of this finding and its implications in clinical settings.

  2. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions.

    Science.gov (United States)

    Polonini, H C; Silva, S L; Cunha, C N; Brandão, M A F; Ferreira, A O

    2016-04-01

    A challenge with compounding oral liquid formulations is the limited availability of data to support the physical, chemical and microbiological stability of the formulation. This poses a patient safety concern and a risk for medication errors. The objective of this study was to evaluate the compatibility of the following active pharmaceutical ingredients (APIs) in 10 oral suspensions, using SyrSpend SF PH4 (liquid) as the suspending vehicle: cholecalciferol 50,000 IU/mL, haloperidol 0.5 mg/mL, imipramine hydrochloride 5.0 mg/mL, levodopa/carbidopa 5.0/1.25 mg/mL, lorazepam 1.0 mg/mL, minocycline hydrochloride 10.0 mg/mL, tacrolimus monohydrate 1.0 mg/mL, terbinafine 25.0 mg/mL, tramadol hydrochloride 10.0 mg/mL and valsartan 4.0 mg/mL. The suspensions were stored both refrigerated (2 - 8 degrees C) and at controlled room temperature (20 - 25 degrees C). This is the first stability study for these APIs in SyrSpend SF PH4 (liquid). Further, the stability of haloperidol,ilmipramine hydrochloride, minocycline, and valsartan in oral suspension has not been previously reported in the literature. Compatibility was assessed by measuring percent recovery at varying time points throughout a 90 days period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV). Given the percentage of recovery of the APIs within the suspensions, the beyond-use date of the final preparations was found to be at least 90 days for most suspensions both refrigerated and at room temperature. Exceptions were: Minocycline hydrochloride at both storage temperatures (60 days), levodopa/carbidopa at room temperature (30 days), and lorazepam at room temperature (60 days). This suggests that compounded suspensions of APIs from different pharmacological classes in SyrSpend SF PH4 (liquid) are stable.

  3. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Science.gov (United States)

    2013-01-11

    ... (Tramadol Hydrochloride) Tablets AGENCY: U.S. Customs and Border Protection, Department of Homeland Security... (tramadol hydrochloride) tablets. Based upon the facts presented, CBP has concluded in the final determination that India is the country of origin of the Rybix (tramadol hydrochloride) tablets for purposes of...

  4. Spectrophotometric determination of meclizine hydrochloride and pyridoxine hydrochloride in laboratory prepared mixtures and in their pharmaceutical preparation

    Science.gov (United States)

    Ibrahim, Maha M.; Elzanfaly, Eman S.; El-Zeiny, Mohamed B.; Ramadan, Nesreen K.; Kelani, Khadiga M.

    2017-05-01

    In this paper, three rapid, simple, accurate and precise spectrophotometric methods were developed for the determination of meclizine hydrochloride in the presence of pyridoxine hydrochloride without previous separation. The methods under study are dual wavelength (DWL), ratio difference (RD) and continuous wavelet transform (CWT). On the other hand, pyridoxine hydrochloride (PYH) was determined directly at 291 nm. The methods obey Beer's law in the range of (5-50 μg/mL) for both compounds. All the methods were validated according to the ICH guidelines where the accuracy was found to be 98.29, 99.59, 100.42 and 100.62% for DWL, RD, CWT and PYH; respectively. Moreover the precision of the methods were calculated in terms of %RSD and it was found to be 0.545, 0.372, 1.287 and 0.759 for DWL, RD,CWT and PYH; respectively. The selectivity of the proposed methods was tested using laboratory prepared mixtures and assessed by applying the standard addition technique. So, they can be used for the routine analysis of pyridoxine hydrochloride and meclizine hydrochloride in quality-control laboratories.

  5. Stability of ranitidine hydrochloride in total parenteral nutrient solution.

    Science.gov (United States)

    Walker, S E; Bayliff, C D

    1985-03-01

    The stability of ranitidine hydrochloride was studied in a standard total parenteral nutrition (TPN) solution. The Canadian formulation of ranitidine hydrochloride (25 mg/mL) was added in 100-, 200-, and 300-mg doses to approximately 1200 mL of a TPN solution and allowed to stand at room temperature (23 degrees C) for seven days. During this time, samples were drawn at least once a day, and the ranitidine concentration was determined by high-performance liquid chromatography. The ranitidine concentration declined at roughly the same rate regardless of the initial concentration. During the study period, each of the three different concentrations declined to less than 70% of the initial concentration. Approximately 10% of the initial concentration was lost in 48 hours. Ranitidine hydrochloride admixtures were stable for up to 48 hours at room temperature in this standard TPN solution.

  6. Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride

    Science.gov (United States)

    Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei

    2013-04-01

    Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a β 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.

  7. Spectrophotometric estimation of pioglitazone hydrochloride in tablet dosage form

    Directory of Open Access Journals (Sweden)

    Basniwal Pawan

    2008-01-01

    Full Text Available Two simple, rapid, and precise methods - linear regression equation (LRE and standard absorptivity - were developed and validated for the estimation of pioglitazone hydrochloride in tablet dosage form. The maximum absorbance (lmax of pioglitazone hydrochloride was found to be 269.8 nm in methanol:water:hydrochloric acid (250:250:1. Beer-Lambert law was obeyed in the concentration range of 10-50 µg/ml, and the standard absorptivity was found to be 253.97 dl/g/cm. Both the methods were validated for linearity, accuracy, precision (days, analysts, and instrument variation, and robustness (solvent composition. The numerical values for all parameters lie within the acceptable limits. Pioglitazone hydrochloride was estimated in the range of 99.58-99.97% by LRE method and 100.25-100.75% by standard absorptivity method. At 99% confidence limit, the F-test value for the methods was found to be 1.8767.

  8. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet.

    Science.gov (United States)

    Mahaparale, Sonali; Telekone, R S; Raut, R P; Damle, S S; Kasture, P V

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer's law was obeyed in the concentration range 5-50 mug/ml for drotaverine and 5-60 mug/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm) and lambda(max) of paracetamol (243.5 nm). In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  9. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet

    Directory of Open Access Journals (Sweden)

    Mahaparale Sonali

    2010-01-01

    Full Text Available Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm and λmax of paracetamol (243.5 nm. In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  10. 多奈哌齐和维生素E对轻度认知功能障碍的疗效评价%Donepezil and Vitamin E for the Treatment of Mild Cognitive Impairment

    Institute of Scientific and Technical Information of China (English)

    黄智恒; 王丽娟

    2005-01-01

    @@ 1文献类型 治疗. 2证据水平 1b. 3文献来源 Petersen RC, Thomas RG, Grundman M, et al.Vitamin E and Donepezil for the treatment of mild cognitive impairment [J]. N Engl J Med, 2005,352:2379-2388.

  11. Therapeutic effect of donepezil on the post-stroke aphasia%多奈哌齐对脑卒中后失语的治疗效果评价

    Institute of Scientific and Technical Information of China (English)

    罗红波; 杨金升; 石向群; 于伟玲

    2011-01-01

    目的 探讨多奈哌齐治疗脑卒中后失语的疗效和安全性.方法 脑卒中后失语患者随机分为对照组(38例)及治疗组(38例).对照组给予常规治疗,治疗组在常规治疗的基础上给予多奈哌齐5mg,1次/d,共4周.采用西方成套测验( WAB)并计算失语商(AQ)评定患者语言功能.结果 治疗后,两组的WAB、AQ评分均有所提高,但治疗组WAB中的口语表达、听理解、复述等方面评分与对照组相比明显增高,差异有统计学意义(P<0.05).多奈哌齐对运动性失语、感觉性及传导性失语中的复述言语障碍改善作用明显,但对命名性失语无明显疗效.未见明显药物不良反应.结论多奈哌齐治疗脑卒中后失语有效且较安全.%Objective To study the efficacy and safety of donepezil in the treatment of post-stroke aphasia. Methods Patients with post-stroke aphasia were randomly divided into twogroups; donepezil treated and control (n = 38, each). The control group received a conventional treatment. Beside the conventional treatment, the patients in treated group were given 5 mg donepezil once a day for 4 weeks. The language function of patients was evaluated by western aphasia battery (WAB) and aphasia quotient (AQ). Results The WAB and AQ scores in the two groups increased after treatment. The WAB scores ( oral expression, auditory comprehension and retelling) in the donepezil treated group were significantly higher than those in the control group (P <0. 05) 4 weeks after treatment. Donepezil had obvious effects on retelling in speech disorders of anandia, sensoryaphasia and conduction aphasia, but anomicaphasia. No significant adverse effects of donepezil were observed. Conclusions Donepezil is effective and safety in the treatment of post-stroke aphasia.

  12. 多奈哌齐缓释微球的制备及家兔体内药动学研究%Preparation of Donepezil Sustained Release Microspheres and Pharmacokinetic Research in Rabbits

    Institute of Scientific and Technical Information of China (English)

    皮佳鑫; 王浩; 栾瀚森; 杨莉

    2013-01-01

    目的 通过超声波技术制备多奈哌齐缓释微球.方法 应用超声波装置制备多奈哌齐缓释微球,进行载药量、粒径、体外释放实验等体外评价,并用LC-MS/MS研究多奈哌齐微球家兔体内的药动学.结果 应用超声波装置制备多奈哌齐缓释微球,载药量为12.1%,粒径分布在40 ~ 130 μm,体外可累计释药一个月,经家兔皮下单剂量30.0 mg·kg-1注射给药,主要药动学参数为:ρmax=40.63 μg·L-1,tmax=2.47 d,MRT=14.81 d,AUC0→∞=646.96μg·d·L-1.结论 应用超声波技术成功制备具有明显缓释特性的多奈哌齐微球.%OBJECTIVE To prepare and evaluate donepezil sustained-release microspheres by ultrasound technique.METHODS Preparation technology of donepezil biodegradable microspheres by ultrasound technique was established and optimized.In vitro evaluation of donepezil microspheres was carried out.The pharmacokinetics of donepezil microspheres was investigated by LC-MS/MS after subcutaneous injection in rabbits at a dose of 30.0 mg · kg-1.RESULTS Donepezil microspheres with drug loading of 12.1% and mean particle size between 40 to 130 μm were successfully prepared by ultrasound technique.The donepezil microspheres displayed a one-month sustained-release character in vitro.The pharmacokinetic parameters were as follows:ρmax 40.63 μg · L-1,tmax 2.47 d,MRT 14.81 d,and AUC0→∞ 646.96 μg · d · L-1.CONCLUSION Ultrasound technique is successfully applied in the preparation of donepezil sustained-release microspheres.

  13. Comparative Effect of Donepezil and Nimodipine on Vascular Dementia%盐酸多奈哌齐与尼莫地平治疗血管性痴呆的疗效观察

    Institute of Scientific and Technical Information of China (English)

    王忠功; 彭爱学; 张广慧; 孙奉辉; 胡文立

    2009-01-01

    Objective To compare the effect of donepezil and nimodipine on vascular dementia. Methods Thirty-six patients with vascular dementia were randomly divided into donepezil group ( n = 20 ) and nimodipine group ( n = 16 ). Donepezil group were treated with donepazil at a dose of 5 mg daily for 12 weeks. Nimodipine group were treated with nimodipine at a dose of 30 mg three times daily for 12 weeks. Before and after the treatment, mini-mental state examination (MMSE)and activities of daily living(ADL) were appraised. Results Donepezil significantly improved cognitive function and activities of daily living in patients with vascular dementia. Compared with donepezil, nimodipine had less effect on improvement of cognitive function, and had no effect on activities of daily living in patients with vascular dementia. Conclusion Both donepezil and nimodipine have effect on vascular dementia, but donepezil are more effective than nimodipine.%目的 观察盐酸多奈哌齐与尼莫地平治疗血管性痴呆的疗效.方法 将36例At管性痴呆患者随机分为盐酸多奈哌齐组20例,给予盐酸多奈哌齐5 mg,每日1次口服,疗程12周;尼莫地平组16例,给予尼莫地平组30 mg,每日3次口服,疗程12周.观察用药前后认知功能(MMSE)及日常生活能力(ADL)改善程度.结果 盐酸多奈哌齐可明显改善认知功能和日常生活能力,尼莫地平可改善认知功能障碍,但疗效不如盐酸多奈哌齐,且不能提高日常生活能力.结论 盐酸多奈哌齐与尼莫地平均可用于治疗血管性痴呆,盐酸多奈哌齐疗效优于尼莫地平.

  14. Spectrophotometric determination of ritodrine and isoxsuprine hydrochlorides using 4-aminoantipyrine.

    Science.gov (United States)

    Revanasiddappa, H D; Manju, B G

    2000-01-01

    A simple, accurate, and rapid method for the quantitative determination of ritodrine hydrochloride (RTH) and isoxsuprine hydrochloride (ISH) in both pure and dosage forms, is described. The method is based on the development of pink colored product as a result of the condensation of 4-aminoantipyrine with phenols in the presence of an alkaline oxidizing agent. The resulting products are measured at 510 nm for both drugs, with molar absorptivities of 0.98 x 10(4) and 1.20 x 10(4) L/mol x cm for RTH and ISH, respectively. A study of the effect of commonly associated excipients revealed that they did not cause interference.

  15. Enantiomeric Separation of Meptazinol Hydrochloride by Capillary Electrophoresis

    Institute of Scientific and Technical Information of China (English)

    YUYun-qiu; CHENYan; LINi; QIUZhui-bai

    2004-01-01

    Aim To establish a capillary electrophoresis method for enantiomerie separation of meptazinol hydrochloride. Methods The separation conditions such as cyclodextrin(CD)type, buffer pH, concentration of 2,3,6-O-triInethyl-β-cyclodextrin and organic additives were optimized. An optimum concentration was 30 mmol·L-1 phosphate (pH 7.02)with 10% (W/V) TM-β-CD and 2% acetonitrile. Results Basehne resolution of the enantiomer was readily achieved using 2,3,6-O-trimethyl-β-cyclodextrin. Conclusion This is a convenient method for fast enantiomeric resolution of meptazinol hydrochloride.

  16. [Effect of topical exhedrine hydrochloride on muco-ciliary transport].

    Science.gov (United States)

    Grammatica, L; Fiorella, R

    1983-07-30

    The time of nasal M.C.T. (Mucus Ciliar Transport) was studied by the indirect objective method of bleu-sky in 30 healthy subjects before and after the application of efedrina hydrochloride in water solution associated with timolo, eucaliptolo, mentolo essence of canfora monobramata and clorbutamolo. The time of nasal M.C.T., regular in the 87% of the subjects during the first determination was found extended in almost all of the cases after the application of vasoconstrictor (85%). This experimental data may be caused both by a direct effect of efedrina hydrochloride and by the substances associated in the solution and their physical characteristics.

  17. Meta-analysis of curative effect of Donepezil on post-stroke aphasia%多奈哌齐治疗卒中后失语疗效的Meta分析

    Institute of Scientific and Technical Information of China (English)

    吴哲; 张雪娟; 罗晓光

    2011-01-01

    目的 应用Meta分析方法评价多奈哌齐治疗卒中后失语的疗效.方法 检索多奈哌齐治疗卒中后失语症的随机对照研究文献,以失语商(AQ)为效应指标,对检索出的文献按固定效应模式通过Revman 4.2统计软件评价和分析多奈哌齐治疗卒中后失语的疗效.结果 12篇文献被纳入,仅3篇为高质量文献.与安慰剂组比较,治疗后多奈哌齐组在西部失语症成套测验中部分项目的评分如书写、复述、理解、流畅性、命名、信息内容、阅读明显改善(均P =0.001).多奈哌齐组AQ整体效应值的加权均数差(WMD)为3.48(95%CI:3.11 ~3.86);10 mg/d组为4.55(95% CI:3.90 ~5.21),5 mg/d组为2.96(95% CI:2.50~3.42);与安慰剂组比较,差异有统计学意义(均P <0.001).结论 多奈哌齐治疗卒中后失语症有效,多奈哌齐10mg/d比5 mg/d的疗效更好.%Objective To assess the curative effect of Donepezil on post-stroke aphasia by means of Meta-analysis. Methods The literatures about randomized controlled trials of Donepezil treated post-stroke aphasia were retrieved. With.aphasia quotient (AQ) as a effect index, the curative effect of Donepezil treated post-stroke aphasia in retrieved literatures were evaluated and analyzed by the statistic soft wear Revman 4. 2 using the fixed effects model. Results Twelve retrieved literatures were included in this study, but only 3 of them were high quality literatures. Compared with placebo group, after treatment the some projects scores of West Aphasia Battery such as writing, repeating, understanding, fluency, denominating, information content and reading in Donepezil group were significantly improved (all P = 0. 001 ). The AQ overall effect value of weighted mean difference ( WMD ) in Donepezil group was 3.48(95% CI:3.11 - 3. 86) ; which was 4. 55 (95% CI:3. 90 - 5. 21) in Donepezil 10 mg/d group and 2.96(95%CI:2.50 -3.42) in Donepezil 5 mg/d group. Compared with placebo group, the differences had

  18. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride

    Directory of Open Access Journals (Sweden)

    Y. Ankamma Chowdary

    2014-01-01

    Full Text Available In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms.

  19. Diffusion Coefficients ofl-Lysine Hydrochloride and l-Arginine Hydrochloride in Their Aqueous Solutions at 25℃

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    The diffusion coefficients** ofl-lysine hydrochloride andl-arginine hydrochloride in their aqueous solu- tions at 25℃ were determined by the metallic diaphragm cell method which is characterized by accuracy, promptness and convenience. Meanwhile, the densities and viscosities of the solutions were also determined. Based on all these data a semi-empirical model for correlating the diffusion coefficients of solid organic salts in their aqueous solutions at 25℃ was proposed. The fitting result of this model is comparatively satisfactory. Compared to a former model, Gordon Model, this model can avoid a number of difficulties and arduous work.

  20. Release Characteristics of Diltiazem Hydrochloride Wax-Matrix ...

    African Journals Online (AJOL)

    Michael Horsfall

    diltiazem hydrochloride-wax matrix granules with sintering. ... The drug release was by Higuchi controlled diffusion mechanism and it followed ... of plastic matrix tablets. Polymer films with different permeability have been .... More so, with increase in temperature and ..... characterization of ibuprofen-cetyl alcohol beads by.

  1. Study on the syhthesis process of tetracaine hydrochloride

    Science.gov (United States)

    Li, Wenli; Zhao, Jie; Cui, Yujie

    2017-05-01

    Tetrachloride hydrochloride is a local anesthetic with long-acting ester, and it is usually present in the form of a hydrochloride salt. Firsleb first synthesized the tetracaine by experiment in 1928, which is one of the recognized clinical potent anesthetics. This medicine has the advantages of stable physical and chemical properties, the rapid role and long maintenance. Tetracaine is also used for ophthalmic surface anesthesia as one of the main local anesthetic just like conduction block anesthesia, mucosal surface anesthesia and epidural anesthesia. So far, the research mainly engaged in its clinical application research, and the research strength is relatively small in the field of synthetic technology. The general cost of the existing production process is high, and the yield is low. In addition, the reaction time is long and the reaction conditions are harsh. In this paper, a new synthetic method was proposed for the synthesis of tetracaine hydrochloride. The reaction route has the advantages of few steps, high yield, short reaction time and mild reaction conditions. The cheap p-nitrobenzoic acid was selected as raw material. By esterification with ethanol and reaction with n-butyraldehyde (the reaction process includes nitro reduction, aldol condensation and hydrogenation reduction), the intermediate was transesterified with dimethylaminoethanol under basic conditions. Finally, the PH value was adjusted in the ethanol solvent. After experiencing 4 steps reaction, the crude tetracaine hydrochloride was obtained.

  2. Surface tension of compositions of polyhexametyleneguanidine hydrochloride - surfactants

    Directory of Open Access Journals (Sweden)

    S. Kumargaliyeva

    2012-12-01

    Full Text Available We made up songs bactericidal polyhexamethyleneguanidine hydrochloride (metacyde with the surface-active substances - anionic sodium dodecylsulfate, cationic cetylpyridinium bromide, and nonionic Tween-80 and measured the surface tension of water solutions. The study showed that the composition metacyde with surface-active agents have a greater surface activity than the individual components.

  3. 21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Proparacaine hydrochloride ophthalmic solution. 524.1982 Section 524.1982 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... longterm toxicity of proparacaine is unknown. Prolonged use may possibly delay wound healing. (d...

  4. Acute generalized exanthematous pustulosis caused by terazosin hydrochloride.

    Science.gov (United States)

    Speck, Laura M; Wilkerson, Michael G; Perri, Anthony J; Kelly, Brent C

    2008-04-01

    Acute generalized exanthematous pustulosis (AGEP) is a rare cutaneous eruption mainly provoked by drugs. A case of AGEP in a 74-year-old male that was attributed to the ingestion of terazosin hydrochloride is presented. This is the first reported case of this association in medical literature. The history, clinical presentation, and pathogenesis of AGEP are discussed.

  5. Cradle-to-gate life cycle inventory of vancomycin hydrochloride.

    Science.gov (United States)

    Ponder, Celia; Overcash, Michael

    2010-02-15

    A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections.

  6. Asymmetric Synthesis of (+)-(11 R,12S)-Mefloquine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    The asymmetric synthesis of (+)-(11R,12S)-mefloquine hydrochloride, an antimalarial drug, was accomplished from commercially available 2-trifluoromethylaniline, ethyl 4,4,4-trifluoroacetoacetate and cyclopentanone in 7 steps with a 14% overall yield. The key steps were proline-catalyzed asymmetric direct aldol reaction and Beck-mann rearrangement. The absolute configuration was assigned by a Mosher's method.

  7. Amitriptyline-related peripheral neuropathy relieved during pyridoxine hydrochloride administration.

    Science.gov (United States)

    Meadows, G G; Huff, M R; Fredericks, S

    1982-11-01

    Tricyclic antidepressants rarely cause peripheral neuropathy. In fact, this class of drugs has been used to control the symptoms of pain and paresthesia that accompany peripheral neuropathy. We report peripheral paresthesias that occurred in a 39-year-old female during five years of amitriptyline administration. The patient's symptoms were relieved by oral pyridoxine hydrochloride, associated with elevated plasma pyridoxal phosphate.

  8. Micellization behavior of mixtures of amphiphilic promazine hydrochloride and cationic aniline hydrochloride in aqueous and electrolyte solutions

    Energy Technology Data Exchange (ETDEWEB)

    Rub, Malik Abdul; Azum, Naved; Asiri, Abdullah M. [King Abdulaziz University, Jeddah (Saudi Arabia); Khan, Farah [Aligarh Muslim University, Aligarh (India); Al-Sehemi, Abdullah G. [Research Center for Advanced Materials Science, King Khalid University, Abha (Saudi Arabia)

    2015-10-15

    We studied the influence of cationic hydrotrope aniline hydrochloride on the micellization behavior of cationic amphiphilic phenothiazine drug promazine hydrochloride in the presence and absence of 50mmol kg{sup -1} NaCl. The experimental critical micelle concentration (CMC) values came out to be lower than ideal CMC (CMCid) values, signifying attractive interactions between the two components in mixed micelles. NaCl further decreases the CMC of pure PMZ and aniline hydrochloride as well as their mixture due to screening of the electrostatic repulsion among the polar head groups. The bulk properties of solution were examined by using different theoretical models for justification and comparison of results. The micellar mole fraction of aniline hydrochloride (X{sup Rub}{sub ,} X{sup M}{sub 1}, X{sup Rod}{sub 1} and X{sup id}{sub 1}) was evaluated by different proposed models, showing greater contribution of hydrotrope in mixed micelle. The negative values of interaction parameter (β) indicate synergistic interactions and negative values of β further decrease by the addition of salt in mixed systems. From the CMC values as a function of temperature, various thermodynamic properties have been evaluated and discussed in detail.

  9. Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values.

    Science.gov (United States)

    Veeraselvam, M; Sridhar, R; Perumal, P; Jayathangaraj, M G

    2014-01-01

    The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg) per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P sloth bears for appropriate line treatment.

  10. Chemical Immobilization of Sloth Bears (Melursus ursinus with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values

    Directory of Open Access Journals (Sweden)

    M. Veeraselvam

    2014-01-01

    Full Text Available The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV, hemoglobin (Hb, red blood cell count (RBC, erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN, creatinine, alkaline amino-transferase (ALT, aspartate amino-transferase (AST, and so forth were estimated in 11 (5 males and 6 females apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P<0.05 and mean corpuscular hemoglobin concentration (MCHC (P<0.05. The study might help to evaluate health profiles of sloth bears for appropriate line treatment.

  11. 天麻素联合多奈哌齐治疗血管性痴呆疗效分析%Clinical efficacy of gastrodin and donepezil on vascular dementia

    Institute of Scientific and Technical Information of China (English)

    何小波; 王晓燕

    2014-01-01

    Objective To observe the therapeutic effect of gastrodin and donepezil on vascular dementia. Methods Forty-eight elderly patients were divided into two groups ( the donepezil group vs the donepezil plus gastrodin group) randomly.The mini-mental state examination(MMSE), activity of daily living(ADL), Hachinski ischemic score and the EEG expression were evaluated and the adverse effect was observed. Results The cognitive function, the ability of activity of daily living, and the EEG expression were improved in two groups after treatment. The donepezil plus gastrodin group has even more better therapeutic effect compared with the donepezil group, which were inflected in higher score in MMSE, lower score in ADL, and higherαband relative power value and lowerθandδband relative power value in quanti-tative EEG. Conclusions Donepezil plus gastrodin have even more better effect on vascular dementia.%目的:观察天麻素与多奈哌齐联合治疗血管性痴呆的临床治疗效果。方法我们采用随机、对照研究的方法,将48例老年血管性痴呆患者分为多奈哌齐组(对照组)、多奈哌齐联合天麻素治疗组(联合治疗组),观察2组患者简易智能量表、日常生活功能量表、Hachinski缺血量表及脑电图等指标的变化,并观察不良反应。结果研究显示2组痴呆量表评分、生活质量评分及脑电图表现均有明显改善,而药联合治疗组改善更明显,与对照组比较有统计学差异。结论天麻素联合多奈哌齐能改善血管性痴呆患者生活质量及脑功能。

  12. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure.

    Science.gov (United States)

    Wojnarowska, Z; Swiety-Pospiech, A; Grzybowska, K; Hawelek, L; Paluch, M; Ngai, K L

    2012-04-28

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M(")(f) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across T(g). The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  13. Disposable screen-printed sensors for determination of duloxetine hydrochloride

    Directory of Open Access Journals (Sweden)

    Alarfaj Nawal A

    2012-01-01

    Full Text Available Abstract A screen-printed disposable electrode system for the determination of duloxetine hydrochloride (DL was developed using screen-printing technology. Homemade printing has been characterized and optimized on the basis of effects of the modifier and plasticizers. The fabricated bi-electrode potentiometric strip containing both working and reference electrodes was used as duloxetine hydrochloride sensor. The proposed sensors worked satisfactorily in the concentration range from 1.0 × 10-6-1.0 × 10-2 mol L-1 with detection limit reaching 5.0 × 10-7 mol L-1 and adequate shelf life of 6 months. The method is accurate, precise and economical. The proposed method has been applied successfully for the analysis of the drug in pure and in its dosage forms. In this method, there is no interference from any common pharmaceutical additives and diluents. Results of the analysis were validated statistically by recovery studies.

  14. [Clinical evaluation of roxatidine acetate hydrochloride injection as preanesthetic medication].

    Science.gov (United States)

    Kawanishi, M; Enomoto, A; Shimada, Y; Kurokawa, Y

    1991-09-01

    The effects of single intravenous administration of roxatidine acetate hydrochloride 75 mg on the volume and pH of gastric juice were investigated in 43 patients undergoing elective surgery under general anesthesia. The drug was given 1 hour before anesthesia. The percentages of patients with gastric pH above 2.5 and gastric juice volume under 25 ml were 95.3% and 97.7% at the time of induction of anesthesia and at the time of extubation, respectively. As for overall assessment on gastric secretion, 93.0% was judged as very effective. In 2 cases, pricking sensations were observed at the time of injection, but these symptoms disappeared without any treatment within a few minutes. No other adverse reactions nor abnormal laboratory test findings were observed. In conclusion, roxatidine acetate hydrochloride administered intravenously 1 hour prior to anesthesia is thought to be useful to prevent acid aspiration pneumonitis.

  15. Thermal Analysis Applied to Verapamil Hydrochloride Characterization in Pharmaceutical Formulations

    Directory of Open Access Journals (Sweden)

    Maria Irene Yoshida

    2010-04-01

    Full Text Available Thermogravimetry (TG and differential scanning calorimetry (DSC are useful techniques that have been successfully applied in the pharmaceutical industry to reveal important information regarding the physicochemical properties of drug and excipient molecules such as polymorphism, stability, purity, formulation compatibility among others. Verapamil hydrochloride shows thermal stability up to 180 °C and melts at 146 °C, followed by total degradation. The drug is compatible with all the excipients evaluated. The drug showed degradation when subjected to oxidizing conditions, suggesting that the degradation product is 3,4-dimethoxybenzoic acid derived from alkyl side chain oxidation. Verapamil hydrochloride does not present the phenomenon of polymorphism under the conditions evaluated. Assessing the drug degradation kinetics, the drug had a shelf life (t90 of 56.7 years and a pharmaceutical formulation showed t90 of 6.8 years showing their high stability.

  16. Linear scleroderma after contusion and injection of mepivacaine hydrochloride.

    Science.gov (United States)

    Ueda, Takashi; Niiyama, Shiro; Amoh, Yasuyuki; Katsuoka, Kensei

    2010-05-15

    A 36-year-old woman initially was treated for a contusion by local injection of mepivacaine hydrochloride into the left dorsum of the foot. Approximately 3 months after the injury and injection, linear sclerotic plaques originating from the site of contusion and injection were recognized. These progressed in extent and severity over a period of 3 years, when she presented to our clinic. By biopsy, swelling of collagen fibers in the lower dermis was revealed and the condition was diagnosed as linear scleroderma. Our present case had multiple linear sclerotic plaques of the left lower extremity, the distribution of which was consistent with Blaschko lines. It was also revealed that the initial sclerotic plaque was at the site of the contusion and local mepivacaine hydrochloride injection. Our present case is interesting in that the findings suggest a correlation between linear scleroderma plaque occurrence and the contusion or injection of mepivacaine.

  17. Synthesis of /sup 14/C-Bucromarone succinate and hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Nicolas, C.; Verny, M.; Maurizis, J.-C.; Payard, M.; Faurie, M.

    1986-08-01

    /sup 14/C-Bucromarone, 2-(4-(3-N,N dibutylamino propoxy) 3,5-dimethyl benzoyl) chromone, was synthesized from (U-/sup 14/C) oxalic acid. The labelling takes place at the first step of the synthesis, giving /sup 14/C-Bucromarone succinate (specific activity 7.45 mCi/mmol) and /sup 14/C-Bucromarone hydrochloride (specific activity 7.5 mCi/mmol).

  18. Enantiospecific synthesis of (1- sup 3 H)-(+)-pseudoephedrine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Hill, J.A.; Scharver, J.D. (Burroughs Wellcome Co., Research Triangle Park, North Carolina (USA). Chemical Development Labs.)

    1990-06-01

    The naturally occurring dextrorotary enantiomer (+)-pseudoephedrine was synthesized in the ({sup 3}H)-labelled form with specific activity 17.5 Ci/mmol suitable for development of a radioimmunoassay procedure. The chirally specific route from L-alanine to (1-{sup 3}H)-d-pseudoephedrine hydrochloride was based on the use of {alpha}-amino acids as chiral educts for asymmetric products. (author).

  19. OPTIMIZATION OF CONCENTRATION OF POLYHEXANIDE HYDROCHLORIDE IN MULTIPURPOSE SOLUTION.

    OpenAIRE

    Arora, A.; Ali, A.; M.T.Zzaman; Chauhan, S.; V.Handa

    2010-01-01

    There are a number of foreign pathogenic microorganisms like viruses, bacteria, yeast, fungi and protozoa which can inadvertently be introduced into eye via contact lens and hence disinfection is a vital part. Multifunctional solutions are generally intended to combine the action of cleaning disinfecting, rinsing lubricating deproteinising and soaking in one single product.In order to optimization of concentration of Polyhexanide hydrochloride in multipurpose solution some microbiological stu...

  20. FORMULATION AND EVALUATION OF FLOATING TABLETS OF TIZANIDINE HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Adimoolam Senthil

    2011-08-01

    Full Text Available The objective of the present investigation was to develop floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34–40% and short biological half life (4.2 h. Tizanidine hydrochloride floating tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropylmethylcellulose (HPMC K4M and K15M. Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility throughout the length of the gastrointestinal tract. Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in-vitro drug release characteristics in 12 hours. Drug release from floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there was no drug and excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. The optimized formulation (F9 released 75% of drug at the end of 10 hours by in-vitro release study.

  1. Clinical effect of venlafaxine combined with methylphenidate hydrochloride on narcolepsy

    Directory of Open Access Journals (Sweden)

    YAN Bin

    2013-11-01

    Full Text Available This study aims to explore the clinical effect of venlafaxine sustained-release capsules combined with methylphenidate hydrochloride tablets on narcolepsy. Thirty-eight cases of narcoleptic patients were randomly divided into venlafaxine combined with methylphenidate hydrochloride treatment group (observation group, N = 19 and methylphenidate hydrochloride and clomipramine treatment group (control group, N = 19. After a total of 12-week treatment, clinical curative effect and adverse drug reactions were observed in 2 groups of patients. The results showed that effective rate of the treatment for excessive daytime sleepiness (EDS in observation group was higher than that of the control group (15/19 vs 8/19, P = 0.044, and effective rate of the treatment for cataplexy in observation group was higher than that of the control group (13/19 vs 6/19, P = 0.048. The rate of adverse drug reactions in observation group was lower than that in the control group (χ2 = 8.889, P = 0.003. It was indicated that venlafaxine combined with methylphenidate had good curative effect on narcolepsy with EDS and cataplexy symptoms.

  2. Mucoadhesive microspheres of propranolol hydrochloride for nasal delivery

    Directory of Open Access Journals (Sweden)

    Dandagi P

    2007-01-01

    Full Text Available Gelatin A microspheres of propranolol hydrochloride for intranasal systemic delivery were developed with the aim to avoid first pass metabolism, to improve the patient compliance, to use an alternative therapy to conventional dosage form, to achieve controlled blood level profiles, and to improve the therapeutic efficacy of propranolol hydrochloride in the treatment of various cardiovascular disorders and as a prophylactic for migraine. Gelatin A microspheres were prepared by emulsion crosslinking method using glutaradehyde as a crosslinking agent. Gelatin and chitosan were used as polymer and co polymer respectively. All the prepared microspheres were evaluated for physical characteristics, such as particle size, incorporation efficiency, swelling index, in vitro bioadhesion using rat jejunum and in vitro drug release in pH 6.6 phosphate buffer. Average particle size of microspheres was found to be in the size range 1-50 mm. Increase in drug and polymer concentration in the formulation increased incorporation efficiency. All the microsphers showed good bioadhesive properties and swelling indices and good sustained release of drug. The data indicates that propranolol hydrochloride release followed Higuchi′s matrix and Peppa′s model. Stability studies showed stability of formulation at all the conditions to which they were subjected.

  3. A novel kind of TSV slurry with guanidine hydrochloride

    Science.gov (United States)

    Jiao, Hong; Yuling, Liu; Baoguo, Zhang; Xinhuan, Niu; Liying, Han

    2015-10-01

    The effect of a novel alkaline TSV (through-silicon-via) slurry with guanidine hydrochloride (GH) on CMP (chemical mechanical polishing) was investigated. The novel alkaline TSV slurry was free of any inhibitors. During the polishing process, the guanidine hydrochloride serves as an effective surface-complexing agent for TSV CMP applications, the removal rate of barrier (Ti) can be chemically controlled through tuned selectivity with respect to the removal rate of copper and dielectric, which is helpful to modifying the dishing and gaining an excellent topography performance in TSV manufacturing. In this paper, we mainly studied the working mechanism of the components of slurry and the skillful application guanidine hydrochloride in the TSV slurry. Project supported by the Major National Science and Technology Special Projects (No. 2009ZX02308), the Fund Project of Hebei Provincial Department of Education, China (No. QN2014208), the Natural Science Foundation of Hebei Province, China (No. E2013202247), and Colleges and Universities Scientific research project of Hebei Province, China (No. Z2014088).

  4. Spectrophotometric estimation of betahistine hydrochloride in tablet formulations

    Directory of Open Access Journals (Sweden)

    Amit Kumar

    2010-01-01

    Full Text Available Aim: The study aims to develop simple, sensitive, rapid, accurate and precise spectrophotometric method for estimation of Betahistine hydrochloride in tablet dosage forms. Materials and Methods: For method I and II, in a series of 10 ml volumetric flask, aliquots of standard drug solution (100 μg/ml in double distilled water were transferred and diluted with same so as to give several dilutions in concentration range of 15-90 μg/ml and 10-80 μg/ml respectively of betahistine hydrochloride. To 5 ml of each dilution taken in a separating funnel, (5 ml of methyl orange for method I and 5 ml of bromo phenol blue for method II reagent and 5 ml of chloroform was added. Reaction mixture was shaken gently for 5 min and allowed to stand so as to separate aqueous and chloroform layer. Absorbance maxima measured at 421.6 nm and 412 nm for method I and II respectively. Results: The recovery studies were found close to 100 % that indicates accuracy and precision of the proposed methods. The statistical analysis was carried out and results of which were found satisfactory. Standard deviation values were found low that indicated reproducibility of the proposed methods. Conclusion: Based on results the developed methods could be used for routine estimation of betahistine hydrochloride from tablet formulations.

  5. Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of wild leopards (Panthera pardus fusca) in emergency situations.

    Science.gov (United States)

    Belsare, Aniruddha V; Athreya, Vidya R

    2010-06-01

    In India, leopards (Panthera pardus fusca) inhabit human-dominated landscapes, resulting in encounters that require interventions to prevent harm to people, as well as the leopards. Immobilization is a prerequisite for any such intervention. Such emergency field immobilizations have to be carried out with limited tools, often amidst large uncontrollable crowds. An effective and practicable approach is discussed, based on 55 wild leopard immobilizations undertaken between January 2003 and April 2008. A xylazine hydrochloride (1.4 +/- 0.3 mg/kg)--ketamine hydrochloride (5 +/- 2 mg/kg) mixture was used for immobilization of leopards, based on estimated body weight. When weight could not be estimated, a standard initial dose of 50 mg of xylazine--150 mg of ketamine was used. Supplemental doses (50-75 mg) of only ketamine were used as required. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization.

  6. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis

    Science.gov (United States)

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-01-01

    Background: Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. Materials and Methods: Samples were divided into eight experimental groups: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. Results: In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Conclusion: Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound

  7. Stability of ranitidine hydrochloride and amino acids in parenteral nutrient solutions.

    Science.gov (United States)

    Bullock, L; Parks, R B; Lampasona, V; Mullins, R E

    1985-12-01

    The stability of ranitidine hydrochloride in parenteral nutrient (PN) solutions and the effect of ranitidine hydrochloride on the amino acids in the PN solutions were studied. Six PN solutions (three each with amino acid contents of 2.125 and 4.25%) were prepared. Each PN solution also contained dextrose 25%, electrolytes, trace elements, vitamins, and heparin sodium. Ranitidine hydrochloride injection was added to four of the PN samples. Of the final samples, two contained no ranitidine, two contained ranitidine hydrochloride 50 micrograms/mL, and two contained ranitidine hydrochloride 100 micrograms/mL. Admixtures of ranitidine hydrochloride at the two concentrations in 0.9% sodium chloride injection were also prepared. Samples were observed for color change and tested for pH during storage at room temperature. Concentrations of amino acids were measured after 24 hours in samples without ranitidine and in samples containing ranitidine hydrochloride 100 micrograms/mL. Ranitidine hydrochloride content was determined by high-performance liquid chromatography at 12, 24, and 48 hours. No visual changes or pH changes occurred by 24 hours. All PN solutions became darker by 48 hours. The presence of ranitidine hydrochloride did not substantially affect amino acid concentrations. At 24 hours, at least 90% of the initial ranitidine concentrations remained in all samples. In three of the four PN samples at 48 hours, less than 90% of initial ranitidine concentrations remained. Ranitidine hydrochloride in concentrations of 50 and 100 micrograms/mL in parenteral nutrient solutions containing 4.25 and 2.125% crystalline amino acids is stable for 24 hours at room temperature. Under these conditions, concentrations of the amino acids contained in the PN solutions were not affected by the addition of ranitidine hydrochloride.

  8. High-performance liquid chromatographic determination of memantine hydrochloride in rat plasma using sensitive fluorometric derivatization.

    Science.gov (United States)

    Xie, Mei-Fen; Zhou, Wei; Tong, Xin-Yi; Chen, Yi-Le; Cai, Yi; Li, Yan; Duan, Geng-Li

    2011-02-01

    In this study, we investigated a simple, sensitive and reliable liquid chromatography-fluorescence detection method for the determination of memantine hydrochloride in rat plasma which was based on derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). For the first time, FMOC-Cl was introduced into derivatization of memantine hydrochloride in rat plasma. The amino groups of memantine hydrochloride and amantadine hydrochloride (internal standard) were trapped with FMOC-Cl to form memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions, which can be very compatible for LC-FLD. Precipitation of plasma proteins by acetonitrile was followed by vortex mixing and centrifugation. Chromatographic separation was performed on a C(18) column (DIAMONSIL 150 × 4.6 mm, id 5 μm) with a mobile phase consisting of acetonitrile and water at a flow rate of 1.0 mL/min. The retention times of memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions were 23.69 and 40.27 min, respectively. Optimal conditions for the derivatization of memantine hydrochloride were also described. The limit of quantification (LOQ) was 25 ng/mL for memantine hydrochloride in plasma, the linear range was 0.025-5.0 μg/mL in plasma with a correlation coefficient (r) of 0.9999. The relative standard deviations (RSDs) of intra-day and inter-day assays were 4.46-12.19 and 5.23-11.50%, respectively. The validated method was successfully applied to the determination of memantine hydrochloride in rat plasma samples.

  9. 多奈哌齐联合尼莫地平治疗阿尔茨海默病患者的疗效观察%Efficacy observation of Donepezil combined with Nimodipine in treatment of Alzheimer's Disease

    Institute of Scientific and Technical Information of China (English)

    徐燕

    2015-01-01

    Objective:To observe effects of Donepezil combined with Nimodipine in treatment of Alzheimer's Disease ( AD) . Methods:96 AD patients were randomly divided into control group and study group, 48 for each group. The control group was treated with just Donepezil, while the study group was given Donepezil plus Nimodipine. The ADAS-Cos', MMSEs and efficacies after the treatment of the two groups were compared. Results:The two groups were significantly improved. After the treatment, the ADAS-Cos score of study group was significantly lower than that of control group, while the MMSE score was significantly higher than that of con-trol group (P<0. 01). The total effective rate of study group was higher than that of control group (P<0. 05). Conclusions:The effi-cacy of Donepezil and Nimodipine is better than single Donepezil for the patients with AD.%目的::观察多奈哌齐联合尼莫地平治疗阿尔茨海默病( AD)患者的效果。方法:将AD患者96例随机分为对照组和研究组,每组各48例。对照组患者应用多奈哌齐治疗,研究组患者在对照组基础上加用尼莫地平,比较两组患者治疗后AD评定量表-认知部分(ADAS-Cos)、MMSE及疗效。结果:研究组患者治疗后ADAS-Cos评分显著低于对照组,MMSE评分显著高于对照组(P<0.01)。研究组患者的总有效率高于对照组(P<0.05)。结论:多奈哌齐联合尼莫地平治疗阿尔茨海默病患者的效果优于单纯多奈哌齐治疗效果。

  10. 78 FR 27971 - Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not...

    Science.gov (United States)

    2013-05-13

    ... HUMAN SERVICES Food and Drug Administration Determination That REV-EYES (Dapiprazole Hydrochloride... determined that REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, was not withdrawn from sale... refer to a listed drug. REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, is the...

  11. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Science.gov (United States)

    2010-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  12. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242b Levamisole hydrochloride tablet...

  13. 21 CFR 520.1242c - Levamisole hydrochloride and piperazine dihydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride and piperazine dihydrochloride. 520.1242c Section 520.1242c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242c Levamisole hydrochloride...

  14. Effects of metomindate hydrochloride and tricaine methanesulfonate on the short term cortisol response in channel catfish

    Science.gov (United States)

    The effects of metomidate hydrochloride and tricaine methanesulfonate (MS-222) on cortisol stress response of channel catfish, Ictalurus punctatus, were examined during 10 minutes of sedation. Channel catfish were assigned to three treatments: 1. Metomidate hydrochloride (12.5 mg/L), 2. MS-222 (100...

  15. A practical synthesis of sarpogrelate hydrochloride and in vitro platelet aggregation inhibitory activities of its analogues

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.

  16. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Science.gov (United States)

    2010-07-01

    ... Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of...—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This method was specifically developed for water-soluble phenolic resins that have a relatively high free-formaldehyde...

  17. Liquid Chromatographic Methods for the Determination of Vildagliptin in the Presence of its Synthetic Intermediate and the Simultaneous Determination of Pioglitazone Hydrochloride and Metformin Hydrochloride

    OpenAIRE

    El-Bagary, Ramzia I.; Elkady, Ehab F.; Ayoub, Bassam M.

    2011-01-01

    Two reversed-phase liquid chromatographic (RP-LC) methods are described for the determination of two binary mixtures of hypoglycemic agents. In the first method, vildagliptin (VDG) was determined in the presence of 3-amino-1-adamantanol (AAD), a synthetic intermediate and impurity of VDG. In the second method, pioglitazone hydrochloride (PGZ) and metformin hydrochloride (MET) were simultaneously determined in their binary mixture. Chromatographic separation in the two methods was achieved on ...

  18. Chitosan coated vancomycin hydrochloride liposomes: Characterizations and evaluation.

    Science.gov (United States)

    Yang, Zhenlei; Liu, Junli; Gao, Jinhua; Chen, Shilei; Huang, Guihua

    2015-11-10

    The present work evaluated the feasibility of chitosan coated liposomes (c-Lips) for the intravenous delivery of vancomycin hydrochloride (VANH), a water-soluble antibiotic for the treatment of gram-positive bacterial infections like osteomyelitis, arthritis, endocarditis, pneumonia, etc. The objective of this research was to develop a suitable drug delivery system in vivo which could improve therapeutic efficacy and decrease side effects especially nephrotoxicity. Firstly, the vancomycin hydrochloride liposomes (VANH-Lips) were prepared by modified reverse phase evaporation method, then the chitosan wrapped vancomycin hydrochloride liposomes (c-VANH-Lips) nanosuspension was formulated by the method of electrostatic deposition. Based on the optimized results of single-factor screening experiment, the c-VANH-Lips were found to be relatively uniform in size (220.40 ± 3.56 nm) with a narrow polydispersity index (PI) (0.21 ± 0.03) and a positive zeta potential (25.7 ± 1.12 mV). The average drug entrapment efficiency (EE) and drug loading (DL) were 32.65 ± 0.59% and 2.18 ± 0.04%, respectively. The in vitro release profile of c-VANH-Lips possessed a sustained release Characterization and the release behavior was in accordance with the Weibull equation. Hemolysis experiments showed that its intravenous injection had preliminary safety. In vivo, after intravenous injection to mice, c-VANH-Lips showed a longer retention time and higher AUC values compared with the VANH injection (VANH-Inj) and VANH-Lips. In addition, biodistribution results clearly demonstrated that c-VANH-Lips preferentially decreased the drug distribution in kidney of mice after intravenous injection. These results revealed that injectable c-VANH-Lips may serve as a promising carrier for VANH to increase therapeutic efficacy on gram-positive bacterial infections and reduce nephrotoxicity, which provides significantly clinical value for long-term use of VANH.

  19. Multicomposite ultrathin capsules for sustained ocular delivery of ciprofloxacin hydrochloride.

    Science.gov (United States)

    Bhadra, Dipankar; Gupta, Girish; Bhadra, Sulekha; Umamaheshwari, R B; Jain, Narendra

    2004-07-16

    The present work is intended to develop a sustained bioadhesive drug delivery system for delivery of Ciprofloxacin Hydrochloride in Cul-de-Sac for sustained and effective antimicrobial chemotherapy. For this, ultrathin multicomposite capsular systems were selected. Multicomposite ultrathin capsules are molecular assemblies of tailored architecture having layer-by-layer adsorption of oppositely charged macromolecules onto colloidal particles. In the present study colloidal calcium phosphate core and gluateraldehyde fixed RBCs were used as core on which alginate (-vely charged) and polyallylamine hydrochloride (+vely charged) polyelectrolyte coating was deposited alternatively upto 10th layer. The coating in each subsequent layer was determined by changes in zeta potential. Ciprofloxacin hydrochloride was loaded in the capsules by incubation with the capsules suspended in phosphate buffer saline pH 7.4. The cores of the capsules were then removed by treatment with 0.1N HCl for calcium phosphate core and by sodium hypochlorite for RBC cored capsules. The hollow ciprofloxacin HCl loaded capsules were the evaluated in-vitro for pattern of layer-by-layer drug loading, drug release, stability at various temperatures and ionic concentrations and corneal retention. The core removal process was found to have minimal effects on drug loading in capsules. The drug loading was found to be higher for RBC cored hollow capsules and hence release rate was lower as compared to calcium cored hollow capsules. Draize test for corneal irritancy proved that the capsules were not irritating. The capsules were found to deliver the ciprofloxacin in cul-de-sac of rabbit's eyes for prolonged period. Based on corneal retention studies and tear drug concentration, the capsules can be considered for suitable and safe use for sustained ocular delivery of drugs.

  20. Indirect Electrochemical Oxidation of 4-Amino-dimethyl-aniline Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The indirect electrochemical oxidation of 4-amino-dimethyl-aniline hydrochloride containing wastewater generated from vanillin production is presented. Experiments were conducted at a constant current density of 30 mA/cm2 via a Ti/Ru-Ti-Sn ternary oxide coated anode and an undivided reactor. During the various stages of the electrolysis, parameters such as the values of chemical oxygen demand (COD) and total organic carbon (TOC) were determined in order to evaluate the feasibility of the electrochemical treatment. The energy consumption and the current efficiency during the electrolysis were calculated. The present study proves the effectiveness of the electrochemical treatment for wastewater resulted from vanillin production.

  1. Verapamil hydrochloride release characteristics from new copolymer zwitterionic matrix tablets.

    Science.gov (United States)

    Kostova, Bistra; Kamenska, Elena; Ivanov, Ivo; Momekov, George; Rachev, Dimitar; Georgiev, George

    2008-01-01

    The aim of this study was to synthesize stable copolymer (vinyl acetate-co-3-dimethyl[methacryloyloxyethyl] ammonium propane sulfinate) zwitterionic latex with different compositions for the first time by emulsifier-free emulsion copolymerization. Throughout the course of the study, a proposal was made for the explanation of the relationship between the "overshooting" phenomenon (a swelling kinetics with a maximum) and the specific self-association of the zwitterionic copolymers. The zwitterionic monomer unit mole fraction, pH, and ionic strength effects on this relationship, on the swelling kinetics of the zwitterionic copolymers, and on the sustained verapamil hydrochloride release from the model tablets were established by the study's authors.

  2. FINANCIAL AVAILABILITY OF IN-HOME MEDICAL TREATMENT OF PATIENTS WITH ALZHEIMER’S DISEASE

    Directory of Open Access Journals (Sweden)

    Mariana Arnaoudova

    2016-07-01

    Full Text Available Background: Alzheimer's disease (AD is a progressive neurodegenerative disorder and presents a great burden for the person, family and society as a whole. Since 2012, in Bulgaria, AD is accepted as a disorder of a great socio-economic significance and the drugs for home treatment are included in the reimbursement list of the National Health Insurance Fund (NHIF. Objective: To trace the access to treatment of Alzheimer’s in-home patients, as a result of generic substitution on the base of share distribution of the original and generic products. Methods: We collected data for the sales of pharmaceutical products (PP’s, containing donepezil hydrochloride and memantine hydrochloride from a distributor for the Northeast region of Bulgaria (Varna in the period 2014-2015. An analysis of the percentage share distribution of the original and generic products was conducted. Results: According to our results original product Aricept accounts for only 4%, while the market share for its generics is 96%. In this group the share to be paid from NHIF is 25%, the remaining 75% from the cost is paid by the patients. The original product Axura occupies 8% market share, the generics- 92%. In this group the share to be paid from NHIF is 50% for generics, while Axura was removed from the Positive reimbursement list. We comment the significant differences in the sale shares in several directions. Conclusion: The reduction of expenses, with the use of generics, would help more patients to receive an optimal treatment and the savings could be redirected for other costly treatments.

  3. Clinical Efficacy of Donepezil in the Treatment of Senile Dementia%盐酸多奈哌齐治疗老年痴呆的疗效研究

    Institute of Scientific and Technical Information of China (English)

    杨红; 朱德生

    2013-01-01

    Objective To evaluate the clinical efficacy of Donepezil in the treatment of senile dementia. Methods A total of 106 senile dementia patients admitted to our hospital were randomly divided into treatment group ( n = 53 ) and control group ( n =53 ). The two groups were both given primary treatment, and the treatment group was given additional Donepezil treatment. Clinical symptoms, physical signs, MMSE score and ADL score were compared between the two groups before treatment, three months and two years after treatment. Results Among the 106 senile dementia patients, 44 cases were male ( 41. 5% ) and 62 cases were female ( 58. 5% ); the patients were aged from 60 to 90, and 82 cases were from 60 to 75 ( 77. 3% ) and 24 cases were from 76 to 90 ( 22.7% ); 73 cases were under college degree ( 68. 87% ) and 33 cases were college degree or above ( 31. 13% ); 72 cases had Alzheimer's disease ( AD ) ( 67. 9% ), 23 cases had vascular dementia ( VaD ) ( 21. 7% ) and 11 cases had other dementia ( 10. 4% ). 92 cases were followed up and 14 cases lost following up during the two - year follow up. The MMSE score and ADL score before treatment and on three - month following up between the two groups showed no statistically significant difference ( P > 0. 05 ), but showed statistically significant differences on two - year following up ( P 0. 05 ). Conclusion Donepezil is safe and effective treatment for senile dementia with little adverse reaction. Donepezil may be regarded as one of best treatments for senile dementia.%目的 探讨盐酸多奈哌齐治疗老年痴呆患者的临床疗效.方法 选择2009年1月-2010年9月106例本院就诊的老年痴呆患者,随机分为治疗组53例及对照组53例,两组均给予基础治疗,治疗组在此基础上给予盐酸多奈哌齐治疗.选择治疗前、随访3个月时及2年时患者的临床症状、体征及简易精神状况检查表(MMSE)评分、日常生活能力量表(ADL)评分进行分析比较.结果 106

  4. Pharmacokinetic and Bioavailability of Donepezil Orally Disintegrating Tablet in Healthy Volunteers%盐酸多奈哌齐口腔崩解片人体药物代谢动力学和生物等效性试验

    Institute of Scientific and Technical Information of China (English)

    余勤; 向瑾; 冯萍; 王颖; 梁茂植; 苗佳; 南峰; 沈奇; 秦永平

    2012-01-01

    目的 采用高效液相色谱-质谱联用法研究盐酸多奈哌齐口腔崩解片的人体药物代谢动力学,并评价其生物等效性.方法 2009年9月-11月对22例健康男性受试志愿者单次交叉口服盐酸多奈哌齐口腔崩解片(试验制剂)和盐酸多奈哌齐普通片(参比制剂),测定给药后不同时间点血浆中多奈哌齐经时血药浓度,采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价.结果 受试者单次口服试验制剂与参比制剂后,达峰时间分别为(2.95±1.16)、(3.19±0.98)h,峰浓度分别为(9.98±2.93)、(9.13±2.05)ng/mL,药时曲线下面积(0-t)分别为(470.76±142.64)、(446.57±137.30) ng/mL·h;药时曲线下面积(0-∞)分别为(517.74±169.79)、(489.47±162.13)ng/mL·h.试验制剂与参比制剂的生物等效性结果为104.7%,其90%置信区间为(98.4%,111.4%).结论 盐酸多奈哌齐口腔崩解片与普通片生物等效.%Objective To study the pharmacokinetic and bioavaiiabiiity of donepezi! orally disintegrating tabiet in healthy volunteers with high performance liquid chromatography-mass spectrometry (HPLC-MS). Methods Twenty-two healthy male volunteers were enrolled in the study between September and November 2009. The subjects orally took a single dose of 5 mg donepezil test or reference preparation. The concentrations of donepezil plasma were assessed and data were analyzed automatically with DAS 2.0 pharmacokinetic program. The relative bioavailability of donepezil test or reference preparation was calculated. Results The parameters of donepezil test and reference preparation were as following: the peak time (Tmax) was (2.95 ±1.16) h and (3.19 ±0.98) h; the peak concentration (Cmax) was (9.98 ±2.93) ng/mL and (9.13 ±2.05) ng/mL; the area under the curve (AUC)(0-t) was (470.76 ±142.64) ng/mL Objective To study the pharmacokinetic and bioavaiiabiiity of donepezi! orally disintegrating tabiet in healthy volunteers with high

  5. [Examination of effectiveness of olopatadine hydrochloride in atopic dermatitis].

    Science.gov (United States)

    Shimizu, Tadamichi; Mashiko, Maki; Shimizu, Hiroshi

    2005-02-01

    Subjective/objective symptoms (itching, papula, erythema, lichenification, desquamation, scratching, erosion) and the levels of IgE, LDH, interleukin (IL) -6, thymus and activation-regulated chemokine (TARC) were compared before and after administering olopatadine hydrochloride (ALLELOCK tablets) to 17 atopic dermatitis (AD) patients. Subject/objective symptoms improved significantly after administering the agent, and the total dosage of the combined topical steroids was also significantly decreased after administration (p<0.05), although IgE, IL-6 and LDH levels did not change, TARC was significantly decreased (p<0.05). The correlation between the levels of IgE, IL-6, LDH and TARC before and after the administration was examined. There was a positive correlation between IgE and TARC (r=0.62, p<0.01) and between IL-6 and TARC (r=0.78, p<0.01). Olopatadine hydrochloride is therefore useful in improving the symptoms in AD, and TARC may be used as an indicator of the symptom improvement.

  6. Growth of glycine ethyl ester hydrochloride and its characterizations

    Science.gov (United States)

    Venkatesan, G.; Pari, S.

    2016-11-01

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV-Vis-NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV-Vis-NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV-Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  7. SPECTROPHOTOMETRIC, ATOMIC ABSORPTION AND CONDUCTOMETRIC ANALYSIS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Sara M. Anis

    2011-09-01

    Full Text Available Six simple and sensitive spectroscopic and conductometric procedures (A-F were developed for the determination of tramadol hydrochloride. Methods A, B and C are based on the reaction of cobalt (II thiocyanate with tramadol to form a stable ternary complex, which could be measured by spectrophotometric (method A, atomic absorption (method B or conductometric (method C procedures. Methods D and E depend on the reaction of molybdenum thiocyanate with tramadol to form a stable ternary complex, measured by spectrophotometric means (method D or by atomic absorption procedures (method E, while method F depends on the formation of an ion pair complex between the studied drug and bromothymol blue which is extractable into methylene chloride. Tramadol hydrochloride could be assayed in the range of 80-560 and 40-–220 μg ml-1, 1-15 mg ml-1 and 2.5-22.5, 1.25-11.25 and 5-22 μg ml-1 using methods A,B,C,D,E and F, respectively. Various experimental conditions were studied. The results obtained showed good recoveries. The proposed procedures were applied successfully to the analysis of tramadol in its pharmaceutical preparations and the results were favorably comparable with the official method.

  8. FORMULATION AND DISSOLUTION STUDY OF DILTIAZEM HYDROCHLORIDE IMMEDIATE RELEASE TABLETS

    Directory of Open Access Journals (Sweden)

    BRAHMAIAH BONTHAGARALA

    2014-08-01

    Full Text Available Objective: The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S in different ratios. Methods: In the present study, design of oral immediate release tablets of Diltiazem hydrochloride by direct compression technique was carried out. Results: The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate . To determine the best fit dissolution profile for the dosage forms. Diltiazem hydrochloride tablets were formulated by using microcrystalline cellulose (diluent, potato starch, acacia (binder and magnesium stearate (lubricant. The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. Conclusion: The Invitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.

  9. Modulation of venlafaxine hydrochloride release from press coated matrix tablet

    Directory of Open Access Journals (Sweden)

    Gohel M

    2008-01-01

    Full Text Available The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3 2 full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion. The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  10. TRIMETAZIDINE HYDROCHLORIDE TRANSDERMAL PATCH: FORMULATION AND IN-VITRO EVALUATION

    Directory of Open Access Journals (Sweden)

    Sarfaraz Md

    2012-07-01

    Full Text Available The present study was carried out to formulate and evaluate matrix-type transdermal formulations containing trimetazidine hydrochloride with polymers such as carboxymethyl chitosan and hydroxypropylmethylcellulose (HPMC 5cps by solvent evaporation technique with glycerin, as plasticizer. The prepared patches were tested for their physicochemical characteristics such as thickness, weight variation, drug content uniformity, folding endurance and tensile strength. The partition coefficient study was performed using n-octanol as the organic phase and phosphate buffer pH 7.4 as an aqueous phase and it was found to be 1.01. In-vitro release studies of trimetazidine hydrochloride-loaded patches in phosphate buffer (pH, 7.4 exhibited drug release in the range of 89.40 to 92.10 % in 24 hrs. The parameter flux (J was calculated and it was in the range of 1.325 to 2.898 mg/cm2/hr. Based on optimization studies, patches containing carboxymethyl chitosan patches were chosen as optimized formulation. Skin irritation studies were performed on optimized transdermal patch and were found to be free of irritation. The patches were subjected to short term stability studies and were found stable. FTIR studies revealed no interactions between drug and excipients. Data of in vitro release from optimized patches were fit in to different equations and kinetic models such as zero order, first-order, Higuchi and Korsmeyer-Peppas models to explain release kinetics.

  11. 维拉佐酮盐酸盐%vilazodone hydrochloride

    Institute of Scientific and Technical Information of China (English)

    李赛

    2011-01-01

    由Trovis Pharma LLC制药公司研制的维拉佐酮盐酸盐(vilazodone hydrochloride)于2011年1月21日由FDA批准上市,商品名为Viibryd,用于治疗成年人重度抑郁症(major depressive disorder,MDD)[1].Viibryd将以10 mg、20 mg和40 mg片剂上市.Viibryd中文化学名称:5-[4-[4-(5-氰基-1H-吲哚-3-基)丁基]-1-哌嗪基]-2-苯并呋喃草酰胺盐酸盐;英文化学名称:5-[4-[4-(5-cyano-1 H-indol-3-yl)butyl]-1 -piperaz-inyl]-2-benzofurancarboxamide hydrochloride;分子式:C26-H27N5O2 ·HCl;分子量:477.99;CAS登记号:163521-08-2.

  12. Structural characterisation and dehydration behaviour of siramesine hydrochloride.

    Science.gov (United States)

    Zimmermann, Anne; Tian, Fang; de Diego, Heidi Lopez; Frydenvang, Karla; Rantanen, Jukka; Elema, Michiel Ringkjøbing; Hovgaard, Lars

    2009-10-01

    In this study the crystal structures of siramesine hydrochloride anhydrate alpha-form and siramesine hydrochloride monohydrate were determined, and this structural information was used to explain the physicochemical properties of the two solid forms. In the crystal structure of the monohydrate, each water molecule is hydrogen bonded to two chloride ions, and thus the water is relatively strongly bound in the crystal. No apparent channels for dehydration were observed in the monohydrate structure, which could allow transmission of structural information during dehydration. Instead destructive dehydration occurred, where the elimination of water from the monohydrate resulted in the formation of an oily phase, which subsequently recrystallised into one or more crystalline forms. Solubility and intrinsic dissolution rate of the anhydrate alpha-form and the monohydrate in aqueous media were investigated and both were found to be lower for the monohydrate compared to the anhydrate alpha-form. Finally, the interactions between water molecules and chloride ions in the monohydrate as well as changes in packing induced by water incorporation could be detected by spectroscopic techniques.

  13. OPTIMIZATION OF CONCENTRATION OF POLYHEXANIDE HYDROCHLORIDE IN MULTIPURPOSE SOLUTION.

    Directory of Open Access Journals (Sweden)

    A. Arora

    2010-01-01

    Full Text Available There are a number of foreign pathogenic microorganisms like viruses, bacteria, yeast, fungi and protozoa which can inadvertently be introduced into eye via contact lens and hence disinfection is a vital part. Multifunctional solutions are generally intended to combine the action of cleaning disinfecting, rinsing lubricating deproteinising and soaking in one single product.In order to optimization of concentration of Polyhexanide hydrochloride in multipurpose solution some microbiological studies were performed by taking five microorganisms which are more prevalent in the infected eye condition. The nutrient agar and sabourad's agar media were used for bacteria and yeast mould respectively. The media were prepared as per I.P and sterilised by autoclaving and poured into Petri plates. The media when cooled to 42°C, 0.5 ml of the culture was added.The optimum concentration of Polyhexanide hydrochloride is 0.0002% which is an effective concentration against five microorganisms that are most prevalent in the infected eye condition.It was concluded that the multipurpose solution containing 2.0 g/ml of polyhexanide were found to be better in terms of antimicrobial activity

  14. Modulation of venlafaxine hydrochloride release from press coated matrix tablet.

    Science.gov (United States)

    Gohel, M C; Soni, C D; Nagori, S A; Sarvaiya, K G

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  15. Formulation and evaluation of transdermal patches of papaverine hydrochloride

    Directory of Open Access Journals (Sweden)

    Shah Samip

    2010-01-01

    Full Text Available Transdermal patches of papaverine hydrochloride were prepared by the solvent casting method using ethyl cellulose: PVP, PVA: PVP and Eudragit RL-100: Eudragit RS-100 using different ratios. The physicochemical parameters such as flexibility, thickness, smoothness, weight variation, moisture content, hardness and tensile strength were evaluated for the prepared patches. The formulation exhibited flexibility, uniform thickness and weight, smoothness, good drug content (92 to 96%, and little moisture content. The in vitro diffusion studies were carried out using modified Keshery-Chein cell using cellophane as the diffusion membrane and the formulation followed the Higuchi diffusion mechanism. The formulation containing PVA: PVP as polymers showed faster release rate (hydrophilic polymers compared to Eudragit RL-100: Eudragit RS-100 (hydrophobic polymers or combination of hydrophilic and hydrophobic polymers (ethyl cellulose and PVP. The stability studies indicated that all the patches maintained good physicochemical properties and drug content after storing the patches in different storage conditions. Compatibility studies indicated that there was no interaction between the drug and polymers. In vivo studies showed that papaverine hydrochloride helps in decreasing the effect of isoproterenol-induced myocardial necrosis. Hence, the aim of the present study was to prepare the sustained release formulation (Transdermal patches of the drug using different blend of polymers. The formulated patches containing the hydroplilic polymers showed best release rate of drug.

  16. [Clinical evaluation of roxatidine acetate hydrochlorides as a preanesthetic medication].

    Science.gov (United States)

    Namba, M; Chihara, E; Ibuki, T; Ashida, H; Fukushima, H; Tanaka, Y

    2001-02-01

    Roxatidine acetate hydrochloride capsule is slowly absorbed from the gastrointestinal tract, and its acid suppressive effect on the stomach is long-lasting compared with other H2-blockers. The reduction of gastric juice in perioperative period is considered advantageous for patients not only because it decreases the risk for aspiration pneumonia but also because it reduces the risk of bronchial spasm induced by gastroesophageal reflux of acidic gastric content. The effects of single oral administration of roxatidine acetate hydrochloride 150 mg at night before the operation on the volume and pH of gastric juice were investigated during anesthesia using two types of anesthetic agents (isoflurane and propofol) in 93 patients of three age groups (group Y: age 20-40, group M: age 41-64, group O: age 65 roxatidine on reduction of gastric juice was found at the time of anesthetic induction and 2 hours after the induction in any age group with either anesthetic agent. The serum concentration of roxatidine at the time of induction was much higher in group O. The value of residual concentration of roxatidine 20 hours after oral intake was estimated from the intraoperative measurements of serum concentration. The results suggest that single administration at night before the operation is sufficient for the oldest group, but an additive dose is recommended for the younger groups.

  17. Formulation and evaluation of tramadol hydrochloride rectal suppositories

    Directory of Open Access Journals (Sweden)

    Saleem M

    2008-01-01

    Full Text Available Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time. In vitro release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters. In vitro drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000 with high molecular weight (4000 and 6000 in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base.

  18. A novel and rapid microbiological assay for ciprofloxacin hydrochloride

    Institute of Scientific and Technical Information of China (English)

    Edith Cristina Laignier Cazedey; Hérida Regina Nunes Salgado

    2013-01-01

    The present work reports a simple, fast and sensitive microbiological assay applying the turbidimetric method for the determination of ciprofloxacin hydrochloride (CIPRO HCl) in ophthalmic solutions. The validation method yielded good results and included excellent linearity, precision, accuracy and specificity. The bioassay is based on the inhibitory effect of CIPRO HCl upon the strain of Staphylococcus epidermidis ATCC 12228 used as the test microorganism. The results were treated statistically by analysis of variance (ANOVA) and were found to be linear (r¼0.9994, in the range of 14.0-56.0 mg/mL), precise (intraday RSD%¼2.06;interday RSD%¼2.30) and accurate (recovery ¼ 99.7%). The turbidimetric assay was compared to the UV spectrophotometric and HPLC methods for the same drug. The turbidimetric bioassay described on this paper for determination of ciprofloxacin hydrochloride in ophthalmic solution is an alternative to the physicochemical methods disclosed in the literature and can be used in quality control routine.

  19. Growth of glycine ethyl ester hydrochloride and its characterizations

    Energy Technology Data Exchange (ETDEWEB)

    Venkatesan, G.; Pari, S., E-mail: sparimyur@gmail.com

    2016-11-15

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV–Vis–NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV–Vis–NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV–Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  20. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Hideki Toyoda

    2016-02-01

    Full Text Available The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis.

  1. Structural characterization of anhydrous naloxone- and naltrexone hydrochloride by high resolution laboratory X-ray powder diffraction and thermal analysis.

    Science.gov (United States)

    Sugimoto, Kunihisa; Dinnebier, Robert E; Zakrzewski, Marek

    2007-12-01

    The crystal structures of the analgesic compounds anhydrous naloxone and naltrexone hydrochloride were determined ab initio from high resolution laboratory X-ray powder diffraction data. Both compounds crystallize in the orthorhombic space group P2(1)2(1)2(1) with lattice parameters of a = 14.6588(10) A, b = 17.4363(9) A, c = 7.96200(22) A, and V = 2035.06(23) A(3) for naloxone hydrochloride and a = 15.4560(5) A, b = 14.9809(4) A, c = 7.84121(18) A, and V = 1815.58(11) A(3) for naltrexone hydrochloride. The crystal structure of anhydrous naloxone hydrochloride forms one-dimensional chains through hydrogen bonds. In the crystal structure of anhydrous naltrexone hydrochloride, two-dimensional sheets are formed by hydrogen bonds. The dehydration processes of naloxone hydrochloride dehydrate and naltrexone hydrochloride tetrahydrate was analyzed by DTA, DSC, TG, and MG.

  2. 多奈哌齐联合天智颗粒治疗轻中度阿尔茨海默病的临床研究%Study on donepezil combined with Tianzhi granule in treating mild to moderate Alzheimer ’s disease

    Institute of Scientific and Technical Information of China (English)

    赖福生; 焦冬生; 卢少军; 钱时德; 李惠俊; 王燕燕; 赵全

    2014-01-01

    目的:观察多奈哌齐与天智颗粒联合治疗轻、中度阿尔茨海默病(Alzheimer’s disease ,AD)的临床疗效。方法选择简易智能量表(MMSE)评分在10~24分的轻、中度AD患者84例,随机分成2组。联合治疗组43例给予多奈哌齐5%Objective To investigate the curative effect of donepezil combined with Tianzhi granule on mild to moderate Alzheimer’s disease(AD).Methods Eighty-four patients with mild to moderate AD (Mini Mental State Examination(MMSE) total scores between 10 and 24) were randomly divided into two groups :combined treatment group (n= 43) ,treated with donepezil 5 mg once a day and Tianzhi granule 5 g three times a day ;control group (n=41) treated with donepezil 5 mg ,once a day.The treatment lasted for 12 weeks. MMSE and Activity of Daily Living Scale (ADL) were used to evaluate clinical effica-cy.Results MMSE and ADL scores were improved significantly after treatments in two groups (P< 0.01). The scores of combined treatment goup were improved more significantly than that of control group (P< 0.05). There were 4 patients (9.3% )with mild diarrhea in treatment group ;1 patient (2.4% )with mild diarrhea and 5 patients(12.2% )with excitation and insomnia in control group.Conclusion Donepezil combined with Tianzhi granule is effective on patients with mild and moderate AD. It could produce improvements in cognition and ability of daily life.Clinical effects of Donepezil combined with Tianzhi granule are batter than that of Donepezil.

  3. Efficacy of benzydamine hydrochloride dripping at endotracheal tube cuff for prevention of postoperative sore throat.

    Science.gov (United States)

    Nimmaanrat, Sasikaan; Chokkijchai, Kedsirin; Chanchayanon, Thavat

    2013-10-01

    Postoperative sore throat (POST) is a frequent consequence following ETT intubation, which may negatively affect the postoperative course and patient satisfaction. Benzydamine hydrochloride is a topically-applied non-steroidal anti-inflammatory drug (NSAID). The authors evaluated the analgesic effect of benzydamine hydrochloride dripping on the ETT cuff on POST. Eighty-six patients participated in this randomized controlled trial. They were assigned into either the benzydamine hydrochloride or the control group. The whole ETT cuff was dripped either with 3 ml (4.5 mg) of benzydamine hydrochloride or nothing five minutes prior to anesthesia induction. The incidence and severity of POST at 0, 2, 4, 6, 12 and 24 hours postoperatively were assessed. The potential adverse effects of benzydamine hydrochloride (throat numbness throat burning sensation, dry mouth, and thirst) were also evaluated. Twenty-five patients (58.14%) in each group had POST (p-value = 1). The severity of POST (calculated from affected patients) in both groups at different time points was not significantly different. Patients in the benzydamine hydrochloride group did not have a higher incidence of adverse effects. We found that dripping benzydamine hydrochloride on the ETT cuff neither reduced the incidence of POST nor increased the incidence of adverse effects in comparison with no intervention.

  4. Developmental rates of immatures of three Chrysomya species (Diptera: Calliphoridae) under the effect of methylphenidate hydrochloride, phenobarbital, and methylphenidate hydrochloride associated with phenobarbital.

    Science.gov (United States)

    Rezende, Fábio; Alonso, Marcela A; Souza, Carina M; Thyssen, Patrícia J; Linhares, Arício X

    2014-05-01

    Entomotoxicology is focused on obtaining data on necrophagous entomofauna, for criminal investigations purposes. This study aimed to evaluate the effect of different concentrations of methylphenidate hydrochloride, phenobarbital, and their association on the developmental rate, larval and pupal survivorship, and the interval of emergence of adults of Chrysomya albiceps (Wiedemann), Chrysomya megacephala (Fabricius), and Chrysomya putoria (Wiedemann) (Diptera: Calliphoridae). Considering the therapeutic dose (TD) of methylphenidate hydrochloride (0.29 mg/Kg), the concentrations tested were 10× TD, 50× TD, and 100× TD. For phenobarbital, the concentrations used were 1× TD (=150 mg/Kg), 3.3× TD, and 6.7× TD. For the association of the drugs, the combinations used were 10× TD-methylphenidate hydrochloride plus 1× TD-phenobarbital, 50× TD-methylphenidate hydrochloride plus 3.3× TD-phenobarbital, and 100× TD-methylphenidate hydrochloride plus 6.7× TD-phenobarbital. The control group, without addition of drug, was maintained under the same conditions of temperature (25 ± 1 °C), humidity (70 ± 10%), and photoperiod (12 h). Specimens of each group were weighed every 12 h until pupariation. The developmental rate of the three Chrysomya species immatures was monitored. For C. albiceps the developmental time was delayed in 24 h for methylphenidate hydrochloride group and in 12 h for the phenobarbital and the drugs association groups. The effect was observed only at specific ages for C. megacephala, without altering the developmental time. For C. putoria, the developmental time was delayed in 12 h for methylphenidate hydrochloride group and in 24 h for the phenobarbital and the drugs association groups. The emergence interval was similar among all experimental groups, but larval and pupal viabilities were affected in different ways.

  5. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples.

    Science.gov (United States)

    Abdel-Ghani, N T; Rizk, M S; Mostafa, M

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL(-1), using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ≥0.995 (n=6) with a relative standard deviation (RSD) ≤1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  6. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples

    Science.gov (United States)

    Abdel-Ghani, N. T.; Rizk, M. S.; Mostafa, M.

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL-1, using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ⩾0.995 (n = 6) with a relative standard deviation (RSD) ⩽1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  7. Comparative effects of zilpaterol hydrochloride and ractopamine hydrochloride on live performance and carcass characteristics of calf-fed Holstein steers.

    Science.gov (United States)

    Brown, T R; Sexten, A K; Lawrence, T E; Miller, M F; Thomas, C L; Yates, D A; Hutcheson, J P; Hodgen, J M; Brooks, J C

    2014-09-01

    Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no β-agonists, 2) a diet that contained zilpaterol hydrochloride (ZH; 8.3 mg/kg [100% DM basis]) for 20 d with a 3-d withdrawal period before harvest, and 3) a diet that contained ractopamine hydrochloride (RH; 30.1 mg/kg [100% DM basis]) for 28 d before harvest. No differences (P ≥ 0.18) were detected between treatments for initial BW, BW at d 28, or DMI. Final BW, BW gain for the last 28 d, total BW gain, ADG for the last 28 d, and overall ADG were greater (P Feeding either β-agonist to calf-fed Holstein steers increased live performance through increased BW, BW gain, and ADG. Furthermore, supplementing calf-fed Holstein steers with ZH provides greater improvements in HCW, LM area, and yield grade components, with a slight decrease in quality grade when compared to calf-fed Holstein steers supplemented with RH.

  8. 多奈哌齐治疗老年痴呆症的疗效及安全性分析%Analysis of the efficacy and safety of donepezil in the treatment of senile dementia

    Institute of Scientific and Technical Information of China (English)

    李志云

    2016-01-01

    目的:探讨多奈哌齐治疗老年痴呆症的疗效及安全性。方法:收治老年痴呆症患者68例,随机分为观察组和对照组,对照组采用常规治疗,观察组在对照组基础上加用多奈哌齐,比较两组治疗效果。结果:治疗后,观察组的MMSE及ADL评分均明显高于对照组(P<0.01)。结论:多奈哌齐治疗老年痴呆症的疗效显著,安全性较高。%Objective:To explore the efficacy and safety of donepezil in the treatment of senile dementia.Methods:68 elderly patients with dementia were selected.They were randomly divided into the observation group and the control group.The control group was treated by routine method.The observation group was treated with donepezil on the basis of the control group.We compared the therapeutic effect of two groups.Results:After treatment,the MMSE and ADL scores of the observation group were significantly higher than those in the control group(P<0.01).Conclusion:The efficacy of donepezil in the treatment of senile dementia was significant,and the security was higher.

  9. The effect of Donepezil on senile dementia complicated with psychosis%多奈哌齐对老年痴呆并发精神异常的疗效观察

    Institute of Scientific and Technical Information of China (English)

    朱军

    2012-01-01

    目的 研究多余哌齐对老年痴呆并发精神异常的治疗效果.方法 52例老年痴呆并发精神异常的患者随机分为观察组与对照组,观察组患者予多奈哌齐5 mg qd;对照组予吡拉西坦800 mg tid.3月后评估患者的生活、精神以及认知功能,并记录不良反应.结果 观察组治疗效果显著,对照组的疗效并不明显,2组不良反应发生率无显著差异.结论 多奈哌齐可有效改善老年痴呆并发精神异常患者的精神症状,提高患者的认知能力与生活自理能力.%Objective To observe the effect of donepezil on senile dementia complicated with psychosis. Methods 52 cases of senile dementia with concurrent psychiatric disorders were divided into observation group and control group, gave donepezil 5 mg qn to observation group, and piracetam 800 mg tid to control group, then evaluate the activity of daily living, psychiatric symptoms and cognition, and record the adverse reactions after 3 months. Results The observation group achieved better therapeutic effect, but the effect of control group was not obvious, and the incidence of adverse reactions of the two groups has no statistical significance. Conclusion The donepezil has obvious effect on the psychiatric abnormalities of senile dementia, and can improve patients' cognitive ability and the ability of daily life.

  10. 舍曲林联合多奈哌齐治疗对脑卒中后功能恢复的影响%The effect of sertraline joint donepezil for stroke recoyery

    Institute of Scientific and Technical Information of China (English)

    张明兴; 黄旭明; 石艺华; 李可一; 杨杏萍; 林恒凯

    2014-01-01

    Objectiye:To study the effect of sertraline joint donepezil for stroke recovery. Methods:81 patiets were divided into group treated with sertraline joint donepezil(n = 25),group treated with sertraline(n = 27)and control group(n =29). They were evaluated with Hamiltonˊs Depression Scale(HAMD),mini-mental state examination(MMSE),the na-tional institutes of health stroke scale(NIHSS)and Barthel index before treatment,4 weeks and 8 weeks after treatment. The results of the three groups were compared. Results:There was no statistically significant difference in the scores of HAMD,MMSE,NIHSS and Barthel index of the three groups before treatment( > 0. 05). The scores of HAMD of group treated with sertraline joint donepezil and group treated with sertraline were lower than that of control group after 4 weeks ( 0. 05). The scores of MMSE of group treated with sertraline joint donepezil and group treated with sertraline were higher than that of control group after 8 weeks( 0.05)。治疗4周舍曲林+多奈哌齐组及舍曲林组 HAMD 评分低于对照组(0.05)。治疗8周舍曲林+多奈哌齐组及舍曲林组 MMSE 评分高于对照组(<0.001,<0.05)。治疗8周舍曲林+多奈哌齐组及舍曲林组 NIHSS 评分低于对照组(<0.01,<0.05)。治疗8周舍曲林+多奈哌齐组 Barthel 评分高于舍曲林组及对照组(<0.05,<0.001),舍曲林组 Barthel 指数评分高于对照组(<0.05)。结论:联合使用舍曲林与多奈哌齐可明显促进脑卒中患者病后功能恢复。

  11. Effect of Donepezil Timingof Medication Administration on Sleep Quality of Patients with Alzheimer's Disease%多奈哌齐服药时间对阿尔茨海默病患者睡眠质量的影响

    Institute of Scientific and Technical Information of China (English)

    焦燕; 李宗国; 包广亮

    2016-01-01

    Objective:Through the influence of observation of donepezil taking medicine at different time on quality of sleep in patients with Alzheimer's disease to provide guidance for the clinical application of the drug.Methods:The April 2013 to June 201 5 in our hospital,1 50 cases of sleep disorders associated with Alzheimer's patients as research subjects were randomly divided into three groups,each group 50 cases,group A taking galantamine,group B taking donepezil at night,group C taking donepezil in the moring.Detection Pittsburgh Sleep Quality Index(PSQI),Epworth index were tested after 8 weeks of treatment.Results:After treatment,the PSQI index of group C was significantly different with that of A group(t =12.14,P 0.05 ).Conclusion:In the morning, taking donepezil may improve sleep better in Alzheimer's patients.%目的::观察多奈哌齐不同服药时间对阿尔茨海默病患者睡眠质量的影响,为该药的临床应用提供指导。方法:将2013年4月至2015年6月于我院就诊的150例伴有睡眠障碍的阿尔茨海默病患者作为研究对象,随机分为3组,每组各50例,A 组服用加兰他敏,B 组晚间服多奈哌齐,C 组早晨服多奈哌齐。治疗8周后检测匹兹堡睡眠质量指数(Pittsburgh sleep quality index,PSQI)、Epworth 日间嗜睡量表指数。结果:经过治疗后,C 组 PSQI 指数与 A 组、B 组比较差异有统计学意义(t =12.14,32.50;P 0.05)。结论:在早晨服用多奈哌齐可以更好改善阿尔茨海默病患者的睡眠状态。

  12. 高压氧并盐酸多奈哌齐治疗血管性痴呆的疗效观察%Hyperbaric oxygen combined with donepezil in the treatment of vascular dementia

    Institute of Scientific and Technical Information of China (English)

    王水平; 陶珍; 丁素菊; 程晋成; 余本松; 王轶群

    2009-01-01

    目的 观察高压氧(HBO)并盐酸多奈哌齐治疗血管性痴呆(VD)的效果.方法 将64例VD患者随机分为观察组和对照组,每组32例.观察组用HBO并盐酸多奈哌齐治疗,对照组单用盐酸多奈哌齐治疗,均治疗12周,治疗前、后2组均采用简易精神状态量表(MMSE)及长谷川痴呆量表(HDS)进行评定.结果 观察组及对照组治疗后MMSE、HDS分数均有明显提高,差异有统计学意义(P<0.05);观察组改善情况明显优于对照组,两者比较差异有统计学意义(P<0.05).结论 HBO并用盐酸多奈哌齐治疗VD效果更佳.%Objective To investigate the efficacy of hyperbaric oxygen combined with donepezil in the treat-ment of patients with vascular dementia(VD). Methods Sixty-four patients with VD were randomly divided into a control group(donepezil group,n=32)and a treatment group(hyperbaric oxygen combined with donepezil,n=32).The course of treatment was 12 weeks.All patients were tested using the Mini-Mental State Examination(MMSE)and Hasegawa's dementia scale(HDS)before and after treatment. Results After 12 weeks of treatment,the MMSE scores and HDS scores of patients increased significantly in both the control and treatment groups.There were signifi-cant differences between the control and treatment groups in terms of MMSE and HDS scores.Conclusion Hyperbar-ic oxygen combined with donepezil could significantly improve cognition in VD patients.

  13. 高压氧联合多奈哌齐治疗血管性痴呆疗效观察%Hyperbaric oxygen joint donepezil in the treatment of vascular dementia in clinical efficacy

    Institute of Scientific and Technical Information of China (English)

    王永盛; 王苹; 吴志鹏; 赵元琛

    2014-01-01

    目的:评价高压氧联合多奈哌齐治疗血管性痴呆的疗效及安全性。方法70例血管性痴呆患者随机分成观察组和对照组各35例。两组均使用多奈哌齐治疗1次/日,观察组在上述治疗的基础上联合高压氧治疗,每日1次,治疗前及治疗8周后应用简易智力状态检查量表( MMSE)和Barthel指数评分评定疗效。结果观察组总有效率82.9%,对照组总有效率62.8%,两组比较有统计学差异(χ2=3.540,P<0.05)。治疗后患者MMSE评分及Bar-thel指数评分较前明显增加,观察组增加更明显(均P<0.05)。结论高压氧联合多奈哌齐治疗血管性痴呆可明显改善患者智能障碍和生活能力,安全性好,优于单用多奈哌齐。%Objective To evaluate the safety and efficacy of hyperbaric oxygen combined with donepezil in the treatment of vasculardementia.Method 70patientswithvasculardementiawererandomlydividedintotreatmentgroupandcontrol group 35 cases each.The two groups were the use of donepezil in the treatment of 1 time /day, the treatment group based on the treatment of combined with use of hyperbaric oxygen in the treatment of 1 time /day.Before and 8 weeks after treatment application scale simple mental state examination ( MMSE) and Barthel index score evaluation of curative effect . Results Treatment group total effectiveness 82.9%, control group total effective rate 62.8%, two groups are statistically significant (P<0.05).After treatment, MMSE score and Barthel index scores were significantly increased , The treatment group increased significantly, with statistically significant difference compared with the control group (P <0.05). Conclusion hyperbaric oxygen combined with donepezil in the treatment of patients with vascular dementia could obviously improve intelligence disorder and living ability , good security , better than use donepezil .

  14. 多奈哌齐联合认知康复训练治疗认知障碍%Effects of Rehabilitation Training Combined with Donepezil on the Cognitive Impairment Patients

    Institute of Scientific and Technical Information of China (English)

    沈慧萍

    2012-01-01

    [目的]:探讨多奈哌齐联合认知康复训练治疗轻度认知障碍的临床疗效.[方法]:90例轻度认知障碍患者随机分为2组,联合治疗组口服多奈哌齐联合认知康复训练治疗,对照组仅口服多奈哌齐,跟踪观察6个月,治疗前后均进行简易精神状态检查表(MMSE)评分与临床记忆量表检查,并对结果进行统计分析.[结果]:治疗后联合治疗组的MMSE评分和临床记忆量表测定中指向记忆、联想学习、人像特点联系回忆及总分等方面评分明显优于对照组,差异有统计学意义(P<0.05).[结论]:治疗后两组患者认知功能均有改善,多奈哌齐联合认知康复训练治疗明显优于单用口服多奈哌齐治疗.%Objective:To explore the clinical efficacy rehabilitation training combined with the donepezil on the cognitive impairment patients with mild cognitive disorders. Methods:90 cases of mild cognitive impairment patients were randomly divided into two groups: combined therapy group and only donepezil group, therapy tracking observed for 6 months. The efficacy were assessed with mini-mental state to check the table ( MMSE) and clinical memory scale before and after treatment, and the results were statistically analyzed. Results:MMSK score , determination of point to memory , associative learning , portrait characteristic associate memories and total score of clinical memory scale of the combined treatment group were significantly better than the control group after treatment(P <0.05) . Conclusion:The cognitive function in patients shows some improvements after treatment. The efficacy of rehabilitation practice combined with the donepezil is significantly belter than only donepezil trealment .

  15. Donepezil adjunctive treatment to risperdone for the cognitive impairments in schizophrenia%利培酮合并盐酸多奈哌齐对精神分裂症认知功能的影响

    Institute of Scientific and Technical Information of China (English)

    陈庆红; 徐西嘉; 张启权; 曹伟

    2011-01-01

    目的:研究盐酸多奈哌齐改善精神分裂症认知功能的效果.方法:将50例未服过抗精神病药的精神分裂症患者,随机分为利培酮(4 mg/d)联合盐酸多奈哌齐组((5~10 mg/d)研究组,23例)和利培酮(4 mg/d)联合安慰剂组(对照组,24例),治疗12周.于治疗前和治疗6周末及12周末测定认知功能,用阳性和阴性症状量表(PANSS)于治疗前和治疗12周末评定临床疗效.结果:治疗12周末,两组各认知测验和PANSS分较治疗前均有改善,差异有统计学意义(P<0.05或P<0.01);数字广度测验、视觉再生测验和连线A测验总分变化值研究组高于对照组(P<0.05或P<0.01).结论:盐酸多奈哌齐可以改善精神分裂症的记忆功能,建议大样本的研究进一步证实.%Objective:To evaluate the effects of donepezil on cognitive impairments in patients with schizophrenia.Method:We conducted a 12-week, double-blind, placebo-controlled trial of donepezil as adjunctive treatment to risperidone on 50 patients with schizophrenia.The study group was given with risperidone (4 mg/d) and donepezil (5 ~ 10 mg/d) ,and the control group was given with risperidone (4 mg/d) and placebo during 12 weeks treatment period.Results:The scores of all cognitive measures and PANSS in endpoint were significantly reduced compared with baseline in both groups (P < 0.05).However,the study group demonstrated greater improvement in the visual reproduction test,trail making tests part A and digit span than did the control group(P < 0.05 or P < 0.01 ).Conclusion: Donepezil as adjunctive therapy may improve memory function of patients with schizophrenia, and future studies require large sample sizes to achieve sufficient power.

  16. Physical and Chemical Characterization of Poly(hexamethylene biguanide Hydrochloride

    Directory of Open Access Journals (Sweden)

    Luiz Henrique C. Mattoso

    2011-06-01

    Full Text Available We present the characterization of commercially available Poly(hexamethylene biguanide hydrochloride (PHMB, a polymer with biocidal activity and several interesting properties that make this material suitable as a building block for supramolecular chemistry and “smart” materials. We studied polymer structure in water solution by dynamic light scattering, surface tension and capacitance spectroscopy. It shows typical surfactant behavior due to amphiphilic structure and low molecular weight. Spectroscopic (UV/Vis, FT-NIR and thermal characterization (differential scanning calorimetry, DSC, and thermogravimetric analysis, TGA were performed to give additional insight into the material structure in solution and solid state. These results can be the foundation for more detailed investigations on usefulness of PHMB in new complex materials and devices.

  17. β-Cyclodextrin-promazine hydrochloride interaction: Conductometric and viscometric studies

    Directory of Open Access Journals (Sweden)

    Mohd. Sajid Ali

    2015-01-01

    Full Text Available Herein we have studied the interaction of β-cyclodextrin (β-CD with the amphiphilic drug promazine hydrochloride (PMZ by using conductimetry and viscometry. From the observed results it was concluded that critical micelle concentration (cmc of the pure drug was lower than the apparent critical micelle concentration (cmc∗ of the drug in the presence of β-CD. The cmc∗ increased on increasing the concentration of β-CD due to the encapsulation of the amphiphilic drug to the hydrophobic cavities of the β-CD which delayed the micelle formation. Viscosity of the solution decreased drastically on the addition of β-CD which further increased on increasing the drug solution. Free energies of micellization (ΔGmic were calculated with the help of degrees of micelle ionization and cmc obtained from the specific conductivity−[PMZ] plots. Micellization was found to be less spontaneous in the presence of cyclodextrin.

  18. Permanent-wave dermatitis: contact allergy to cysteamine hydrochloride.

    Science.gov (United States)

    Landers, Maeran C; Law, Sandra; Storrs, Frances J

    2003-09-01

    Cysteamine hydrochloride (CHC) is a newly recognized sensitizer found in permanent-wave solutions. We report the case of a hairdresser who was found to be allergic to CHC. Our allergic patient was patch-tested to various chemicals found in permanent-wave solutions, including CHC (1.0% in petrolatum). Patch-test reactions were positive to CHC, glyceryl thioglycolate, diglyceryl thioglycolate, p-phenylenediamine (PPD), and PPD through a piece of latex glove. Sixty-four controls to CHC (1.0% in petrolatum) had negative results. Household-weight latex gloves were protective against CHC allergy. Persons with CHC-waved hair were not allergic. CHC contained in "neutral" permanent-wave preparations has been used in American beauty salons since 1993. We briefly discuss the introduction and significance of CHC in permanent waves.

  19. Betahistine hydrochloride in Méniére's disease.

    Science.gov (United States)

    Frew, I J; Menon, G N

    1976-08-01

    A double-blind, placebo-controlled, cross-over clinical trial was performed to assess the effect of betahistine hydrochloride (Serc) in Ménière's disease. The diagnosis was based on paroxysmal attacks of rotational vertigo, with tinnitus, and a fluctuating sensori-neural deafness, together with the results of auditory and vestigular tests. Twenty-eight patients were admitted to the trial over 3 years. Twenty-two patients completed the trial. In total, they received betahistine 32 mg daily, for a period of 16 weeks, and placebo also for the same length of time, preceded in every case by a 4-week pre-treatment period. Daily symptom score cards were kept. There was a statistically significant improvement in favour of the drug with regard to vertigo, tinnitus and deafness. Vertigo was the most responsive symptom. No adverse reactions were observed.

  20. [Characteristics and selectivity of photocatalytic-degradation of tetracycline hydrochloride].

    Science.gov (United States)

    Song, Chen-Yi; Yin, Da-Qiang

    2014-02-01

    The photocatalytic-degradation behavior of tetracycline hydrochloride (TTC) was studied. The catalyst used was photosensitive semiconductor titanium dioxide (TiO2). The results showed that the photocatalytic degradation of TTC was well fitted to first order reaction kinetics model, and the adsorption was the control step of the whole photocatalytic-degradation process, indicating that the main degradation path was the photocatalytic reaction of TTC adsorbed on the surface of TiO2. Besides, through photocatalytic-degradation of the mixed solution of TTC and sulfamethoxazole or amoxicillin, the degradation of the two antibiotics showed obvious selectivity when the pH, TiO2 dosage and other conditions were changed.

  1. FORMULATION AND EVALUATION OF SUSTAINED RELEASE PELLETS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Baskara Haripriya

    2013-02-01

    Full Text Available The aim of the present research is to develop and evaluate a better sustained release multiple unit pellets (MUP formulation of Tramadol hydrochloride. Dissolution and diffusion controlled systems have classically been of primary importance in oral delivery of medication because of their relative ease of production and cost compared with other methods of sustained or controlled delivery. Most of these systems are solids, although a few liquids and suspension have been recently introduced. The present work aimed at developing SR pellets of Tramadol HCl by Wurster process. FTIR studies showed no unacceptable extra peaks which confirm the absence of chemical interaction between the drug and polymer. Angle of repose, tapped density, bulk density values for the formulations were within the range which indicates that pellets prepared by Wurster process were satisfactory for further studies. The percentage drug content of Tramadol was determined by extraction with methanol and analyzed by using UV-visible spectrophotometer at 271nm.

  2. Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride.

    Science.gov (United States)

    Alekya, Thota; Narendar, Dudhipala; Mahipal, Donthi; Arjun, Narala; Nagaraj, Banala

    2017-09-26

    Rheumatoid arthritis is an auto immune disease which requires chronotherapy as it occurs during early morning. Tramadol hydrochloride (TH) is an analgesic drug, used to treat rheumatoid arthritis. The aim of the present investigation was to develop chronomodulated drug delivery system of tramadol hydrochloride such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of TH, initially core tablets of TH were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit S100 was optimized and coating tablets of TH was prepared. The prepared coated tablets were evaluated for weight variation, hardness, drug content and in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 7.5% of coating solution (ES2) had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. DSC studies revealed that no interaction between core and coated materials with drug was observed. Thus, chronomodulated drug delivery system of TH was formulated and assuming that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am. © Georg Thieme Verlag KG Stuttgart · New York.

  3. Sinomenine Hydrochloride Protects against Polymicrobial Sepsis via Autophagy

    Directory of Open Access Journals (Sweden)

    Yu Jiang

    2015-01-01

    Full Text Available Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs. The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl is widely used to treat rheumatoid arthritis (RA. However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3 puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM. 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  4. Sinomenine hydrochloride protects against polymicrobial sepsis via autophagy.

    Science.gov (United States)

    Jiang, Yu; Gao, Min; Wang, Wenmei; Lang, Yuejiao; Tong, Zhongyi; Wang, Kangkai; Zhang, Huali; Chen, Guangwen; Liu, Meidong; Yao, Yongming; Xiao, Xianzhong

    2015-01-23

    Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs). The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN) is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl) is widely used to treat rheumatoid arthritis (RA). However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP) in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA) was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3) puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS)-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM). 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  5. Formulation optimization of propranolol hydrochloride microcapsules employing central composite design

    Directory of Open Access Journals (Sweden)

    Shivakumar H

    2008-01-01

    Full Text Available A central composite design was employed to produce microcapsules of propranolol hydrochloride by o/o emulsion solvent evaporation technique using a mixture of cellulose acetate butyrate as coat material and span-80 as an emulsifier. The effect of formulation variables namely levels of cellulose acetate butyrate (X 1 and percentage of Span-80 (X 2 on encapsulation efficiency (Y 1 , drug release at the end of 1.5 h (Y 2 , 4 h (Y 3 , 8 h (Y 4 , 14 h (Y 5 , and 24 h (Y 6 were evaluated using the F test. Mathematical models containing only the significant terms were generated for each response parameter using multiple linear regression analysis and analysis of variance. Both the formulation variables exerted a significant influence (P < 0.05 on Y 1 whereas the cellulose acetate butyrate level emerged as the lone factor which significantly influenced the other response parameters. Numerical optimization using desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , and Y 6 for the optimized formulation was found to be 92.86±1.56% w/w, 29.58±1.22%, 48.56±2.56%, 60.85±2.35%, 76.23±3.16% and 95.12±2.41%, respectively which were in close agreement with those predicted by the mathematical models. The drug release from microcapsules followed first order kinetics and was characterized by Higuchi diffusion model. The optimized microcapsule formulation developed was found to comply with the USP drug release test-1 for extended release propranolol hydrochloride capsules.

  6. Biowaiver monographs for immediate release solid oral dosage forms: ciprofloxacin hydrochloride.

    Science.gov (United States)

    Olivera, M E; Manzo, R H; Junginger, H E; Midha, K K; Shah, V P; Stavchansky, S; Dressman, J B; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of new multisource and reformulated immediate release (IR) solid oral dosage forms containing ciprofloxacin hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. Ciprofloxacin hydrochloride's solubility and permeability, its therapeutic use and index, pharmacokinetics, excipient interactions and reported BE/bioavailability (BA) problems were taken into consideration. Solubility and BA data indicate that ciprofloxacin hydrochloride is a BCS Class IV drug. Therefore, a biowaiver based approval of ciprofloxacin hydrochloride containing IR solid oral dosage forms cannot be recommended for either new multisource drug products or for major scale-up and postapproval changes (variations) to existing drug products.

  7. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement

    National Research Council Canada - National Science Library

    Wairkar, Sarika; Gaud, Ram

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg...

  8. Myocardial perfusion imaging with higenamine hydrochloride stress studies in diagnosis of coronary artery disease

    Institute of Scientific and Technical Information of China (English)

    周维

    2013-01-01

    Objective To evaluate the stress test efficacy and safety of higenamine hydrochloride,MPI studies were performed in patients with coronary artery disease. Methods Sixty-eight patients with suspected coronary artery

  9. Synthesis of 2-Heterocyclomethyl-5-diphenylmethylenecyclopentanone Hydrochlorides and their Inhibitory Effect on Tumor Cell Growth

    Institute of Scientific and Technical Information of China (English)

    Yun Hai ZHANG; Lin Xiang ZHAO; Zhen Jun BIAN; Rui WANG; Fu Yuan SUN

    2006-01-01

    Sixteen new 2-heterocyclomethyl-5-diphenylmethylenecyclopentanone hydrochlorides were designed and synthesized. The growth inhibitory effect of these compounds in vitro was conducted using a MTT assay in human breast cancer T47D cells.

  10. The effect of tramadol hydrochloride on early life stages of fish.

    Science.gov (United States)

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Berankova, Petra; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Vecerek, Vladimir; Svobodova, Zdenka

    2016-06-01

    The aim of this study was to perform the fish embryo acute toxicity test (FET) on zebrafish (Danio rerio) and the early-life stage toxicity test on common carp (Cyprinus carpio) with tramadol hydrochloride. The FET was performed using the method inspired by the OECD guideline 236. Newly fertilized zebrafish eggs were exposed to tramadol hydrochloride at concentrations of 10; 50; 100 and 200μg/l for a period of 144h. An embryo-larval toxicity test on C. carpio was performed according to OECD guideline 210 also with tramadol hydrochloride at concentrations 10; 50; 100 and 200μg/l for a period of 32 days. Hatching was significantly influenced in both acute and subchronic toxicity assays. Subchronic exposure also influenced early ontogeny, both morphometric and condition characteristics and caused changes in antioxidant enzyme activity. The LOEC value was found to be 10μg/l tramadol hydrochloride.

  11. Effects of drotaverine hydrochloride on viability of rat cultured cerebellar granulocytes.

    Science.gov (United States)

    Demushkin, V P; Zhavoronkova, E V; Khaspekov, L G

    2012-02-01

    The neurocytotoxic effect of drotaverine hydrochloride was studied in culture of rat cerebellar granulocytes. Incubation of cells with 100 and 250 μM drotaverine reduced neuronal survival to 60 and 4%, respectively.

  12. Thiamine hydrochloride: An efficient catalyst for one-pot synthesis of quinoxaline derivatives at ambient temperature

    Indian Academy of Sciences (India)

    Omprakash B Pawar; Fulchand R Chavan; Venkat S Suryawanshi; Vishnu S Shinde; Narayan D Shinde

    2013-01-01

    Quinoxaline derivatives have been synthesized in high to excellent yields in the presence of thiamine hydrochloride (VB1) as an inexpensive, non-toxic and metal ion free catalyst at ambient temperature.

  13. Hippocampal P3-like auditory event-related potentials are disrupted in a rat model of cholinergic degeneration in Alzheimer's disease: reversal by donepezil treatment.

    Science.gov (United States)

    Laursen, Bettina; Mørk, Arne; Kristiansen, Uffe; Bastlund, Jesper Frank

    2014-01-01

    P300 (P3) event-related potentials (ERPs) have been suggested to be an endogenous marker of cognitive function and auditory oddball paradigms are frequently used to evaluate P3 ERPs in clinical settings. Deficits in P3 amplitude and latency reflect some of the neurological dysfunctions related to several psychiatric and neurological diseases, e.g., Alzheimer's disease (AD). However, only a very limited number of rodent studies have addressed the back-translational validity of the P3-like ERPs as suitable markers of cognition. Thus, the potential of rodent P3-like ERPs to predict pro-cognitive effects in humans remains to be fully validated. The current study characterizes P3-like ERPs in the 192-IgG-SAP (SAP) rat model of the cholinergic degeneration associated with AD. Following training in a combined auditory oddball and lever-press setup, rats were subjected to bilateral intracerebroventricular infusion of 1.25 μg SAP or PBS (sham lesion) and recording electrodes were implanted in hippocampal CA1. Relative to sham-lesioned rats, SAP-lesioned rats had significantly reduced amplitude of P3-like ERPs. P3 amplitude was significantly increased in SAP-treated rats following pre-treatment with 1 mg/kg donepezil. Infusion of SAP reduced the hippocampal choline acetyltransferase activity by 75%. Behaviorally defined cognitive performance was comparable between treatment groups. The present study suggests that AD-like deficits in P3-like ERPs may be mimicked by the basal forebrain cholinergic degeneration induced by SAP. SAP-lesioned rats may constitute a suitable model to test the efficacy of pro-cognitive substances in an applied experimental setup.

  14. Synthesis of imidazol-1-yl-acetic acid hydrochloride: A key intermediate for zoledronic acid

    OpenAIRE

    Singh, Santosh Kumar; Manne, Narendra; Ray, Purna Chandra; Pal, Manojit

    2008-01-01

    A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid.

  15. Synthesis of imidazol-1-yl-acetic acid hydrochloride: A key intermediate for zoledronic acid

    Science.gov (United States)

    Manne, Narendra; Ray, Purna Chandra

    2008-01-01

    Summary A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid. PMID:19104672

  16. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    OpenAIRE

    Zhi-Gang Cheng; Xu-Yong Dai; Li-Wei Li; Qiong Wan; Xiang Ma; Guang-Ya Xiang

    2014-01-01

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR)...

  17. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    OpenAIRE

    Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya

    2014-01-01

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). ...

  18. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement.

    Science.gov (United States)

    Wairkar, Sarika; Gaud, Ram

    2016-06-01

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg) and Metformin hydrochloride (500 mg) COAM, as a dose ratio, were prepared by ball-milling technique. COAMs were characterized for saturation solubility, amorphism and physicochemical interactions (X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR)), SEM, in vitro dissolution, and stability studies. Solubility studies revealed a sevenfold rise in solubility of Nateglinide from 0.061 to 0.423 mg/ml in dose ratio of COAM. Solid-state characterization of COAM suggested amorphization of Nateglinide after 6 h of ball milling. XRPD and DSC studies confirmed amorphism in Nateglinide, whereas FTIR elucidated hydrogen interactions (proton exchange between Nateglinide and Metformin hydrochloride). Interestingly, due to low energy of fusion, Nateglinide was completely amorphized and stabilized by Metformin hydrochloride. Consequently, in vitro drug release showed significant increase in dissolution of Nateglinide in COAM, irrespective of dissolution medium. However, little change was observed in the solubility and dissolution profile of Metformin hydrochloride, revealing small change in its crystallinity. Stability data indicated no traces of devitrification in XRPD of stability sample of COAM, and % drug release remained unaffected at accelerated storage conditions. Amorphism of Nateglinide, proton exchange with Metformin hydrochloride, and stabilization of its amorphous form have been noted in ball-milled COAM of Nateglinide-Metformin hydrochloride, revealing enhanced dissolution of Nateglinide. Thus, COAM of Nateglinide-Metformin hydrochloride system is a promising approach for combination therapy in diabetic patients.

  19. SIMULTANEOUS ESTIMATION OF DICLOFENAC SODIUM AND TOLPERISONE HYDROCHLORIDE IN COMBINED PHARMACEUTICAL FORMULATION

    OpenAIRE

    Bhavesh Gevriya* and R.C. Mashru

    2013-01-01

    Three simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Tolperisone Hydrochloride (TOL) and Diclofenac Sodium (DIC) in their combined dosage form. Method A, Simultaneous equation method (Vierodt’s method) applies measurement of absorptivities at two wavelengths, 261.00 nm (λmax of Tolperisone Hydrochloride) and 279.00 nm, (λmax of Diclofenac Sodium) in zero order spectra. The concentrations can be calculated from the derived equati...

  20. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF TOLPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    OpenAIRE

    Patel Satish A; Hariyani Kaushik P

    2012-01-01

    The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Diclofenac sodium and Tolperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Tolperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in...

  1. The effect of L-ornithine hydrochloride ingestion on human growth hormone secretion after strength training

    OpenAIRE

    2010-01-01

    This study aimed to examine the effect of L-ornithine hydrochloride ingestion on serum growth hormone secretion response after strength training in young men who did not regularly engage in high intensity exercise. Ten healthy young males without workout habits (age: 22.2 +/- 1.0 yr). Subjects performed biceps curl strength training after L-ornithine hydrochloride and placebo ingestions. They participated in both of the above conditions randomly with a week interval in between. Serum growth h...

  2. 多奈哌齐对Aβ25~35诱导神经毒性的保护作用%Neuroprotective effect of donepezil on β-amyloid25~35-induced neurotoxicity

    Institute of Scientific and Technical Information of China (English)

    杨红旗; 李学; 蒋秋焕; 马建军; 徐军

    2012-01-01

    Objective To investigate the neuroprotective effect of cholinesterase inhibitor donepezil on β-amyloid25~35 (Aβ25~35)-induced neurotoxicity and its related mechanism.Methods PC12 cells were conventionally cultured.Serial concentrations of Aβ25~35 and donepezil (0,0.5,1,5,10,20 and 50 μmol/L) were added to PC 12 cells and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) staining was then employed to detect their effects on PC12 cell viability; pretreatments with 1,5,10,20 and 50 μmol/L donepezil were given to the PC12 cells 2 h before adding 20 μmol/L Aβ25~35 as pretreatment groups A,B,C,D and E,and normal control group Ⅰ and 20 μmol/L Aβ25-35 treatment group were chosen; MMT assay was again used to detect the PC12 cell viability and level of lactate dehydrogenase (LDH).Pretreatment with 10 μmol/L GF109203X (protein kinase C [PKC] antagonist) given to the PC12 cells 30 min before adding 10 μmol/L donepezil was carried out as pretreatment group F,and normal control group Ⅱ,10 μmol/L GF109203X treatment group and 10 μmol/L donepezil treatment group were chosen; the expressions ofphosphorylation-PKC (P-PKC) and its major substrate phosphorylated myristoylated alanine-rich protein C kinase substrate (P-MARCKS) were measured by Western blotting; the effect of donepezil on PKCα and PKCε isoforms subcellular distribution were detected by immunofluorescence staining.Results Aβ25-35 (5,10,20 and 50 μmol/L) treatment for 24 h could decrease the cell viability in PC12 cells in a dose-dependent manner (P<0.05); as compared with PC12 cells in the control group,the 20 μmol/L Aβ25 ~35 treatment group enjoyed lower PC12 cell viability and higher release of LDH.As compared with 20 μmol/L Aβ25~35 treatment group,pretreatment groups B,C,D and E enjoyed increased cell viability and decreased LDH release (P<0.05).Western blotting indicated that 10 μmol/L donepezil treatment can promote PKC and MARCKS phosphorylation as compared

  3. Direct, preparative enantioselective chromatography of propranolol hydrochloride and thioridazine hydrochloride using carbon dioxide-based mobile phases.

    Science.gov (United States)

    Geiser, F; Schultz, M; Betz, L; Shaimi, M; Lee, J; Champion, W

    1999-12-31

    In this paper, we describe the direct, preparative enantioselective chromatography of racemic (rac)-propranolol hydrochloride (HCI) and rac-thioridazine.HCl using Chiralpak AD chiral stationary phase and mobile phase systems containing carbon dioxide and methanol without the use of basic or acidic additives. Isolated fractions of propranolol.HCl were positively identified by mass spectrometry, Beilstein flame test, melting point, and chemical analysis to be HCI enantiomers of propranolol-HCl salts exhibited characteristic mass spectra peaks at 36 and 38 mass-to-charge ratio in the expected 3:1 isotopic ratio for the solute that were absent in the mass spectra for the free-base forms. To our knowledge, the direct, preparative enantioselective isolation of HCI enantiomeric salts of rac-propranolol and of rac-thioridazine have not been previously demonstrated and published.

  4. A Randomized Clinical Trial of Berberine Hydrochloride in Patients with Diarrhea-Predominant Irritable Bowel Syndrome.

    Science.gov (United States)

    Chen, Chunqiu; Tao, Chunhua; Liu, Zhongchen; Lu, Meiling; Pan, Qiuhui; Zheng, Lijun; Li, Qing; Song, Zhenshun; Fichna, Jakub

    2015-11-01

    We aimed to evaluate clinical symptoms in diarrhea predominant irritable bowel syndrome (IBS-D) receiving berberine hydrochloride in a randomized double-blind placebo-controlled clinical trial. Overall, 196 patients with IBS-D were recruited for this study; consequently, 132 patients randomized to receive daily 400 mg of berberine hydrochloride, delivered twice daily or placebo for 8 weeks followed by a 4-week washout period. After a 2-week run-in period, diarrhea, abdominal pain, urgent need for defecation frequency and any adverse events were recorded daily. Prior to administration of the medication and after completing the treatment, assessment of IBS symptom scores, depression and anxiety scale scores and the IBS scale for quality of life (QOL) was carried out. The effects of berberine hydrochloride on IBS-D, defined by a reduction of diarrhea frequency (P = 0.032), abdominal pain frequency (P berberine group than the placebo group in the 8 weeks of treatment. A trend of improvement (P berberine hydrochloride for IBS symptom score, depression score and anxiety score and the IBSQOL, compared with placebo. At last, berberine hydrochloride was well tolerated. So we concluded that berberine hydrochloride is well tolerated and reduces IBS-D symptoms, which effectively improved patients QOL.

  5. Using crystal structure prediction to rationalize the hydration propensities of substituted adamantane hydrochloride salts.

    Science.gov (United States)

    Mohamed, Sharmarke; Karothu, Durga Prasad; Naumov, Panče

    2016-08-01

    The crystal energy landscapes of the salts of two rigid pharmaceutically active molecules reveal that the experimental structure of amantadine hydrochloride is the most stable structure with the majority of low-energy structures adopting a chain hydrogen-bond motif and packings that do not have solvent accessible voids. By contrast, memantine hydrochloride which differs in the substitution of two methyl groups on the adamantane ring has a crystal energy landscape where all structures within 10 kJ mol(-1) of the global minimum have solvent-accessible voids ranging from 3 to 14% of the unit-cell volume including the lattice energy minimum that was calculated after removing water from the hydrated memantine hydrochloride salt structure. The success in using crystal structure prediction (CSP) to rationalize the different hydration propensities of these substituted adamantane hydrochloride salts allowed us to extend the model to predict under blind test conditions the experimental crystal structures of the previously uncharacterized 1-(methylamino)adamantane base and its corresponding hydrochloride salt. Although the crystal structure of 1-(methylamino)adamantane was correctly predicted as the second ranked structure on the static lattice energy landscape, the crystallization of a Z' = 3 structure of 1-(methylamino)adamantane hydrochloride reveals the limits of applying CSP when the contents of the crystallographic asymmetric unit are unknown.

  6. RP-HPLC estimation of imipramine hydrochloride and diazepam in tablets

    Directory of Open Access Journals (Sweden)

    D Srikantha

    2015-01-01

    Full Text Available A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 μg/ml for imipramine hydrochloride (r 2 =0.999 and in the range 5-30 μg/ml for diazepam (r 2 =0.9994, respectively. The limits of detection and quantitation were 0.03 and 0.1 μg/ml for imipramine hydrochloride and 0.02 and 0.07 μg/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam studies, intraday and interday precision (<2% and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets.

  7. HPLC method validation for modernization of the tetracycline hydrochloride capsule USP monograph

    Directory of Open Access Journals (Sweden)

    Emad M. Hussien

    2014-12-01

    Full Text Available This paper is a continuation to our previous work aiming at development and validation of a reversed-phase HPLC for modernization of tetracycline-related USP monographs and the USP general chapter . Previous results showed that the method is accurate and precise for the assay of tetracycline hydrochloride and the limit of 4-epianhydrotetracycline impurity in the drug substance and oral suspension monographs. The aim of the current paper is to examine the feasibility of the method for modernization of USP tetracycline hydrochloride capsule monograph. Specificity, linearity, accuracy and precision were examined for tetracycline hydrochloride assay and 4-epianhydrotetracycline limit. The method was linear in the concentration range from 80% to 160% (r>0.9998 of the assay concentration (0.1 mg/mL for tetracycline hydrochloride and from 50% to 150% (r>0.997 of the acceptance criteria specified in tetracycline hydrochloride capsule monograph for 4-epianhydrotetracycline (NMT 3.0%. The recovery at three concentration levels for tetracycline hydrochloride assay was between 99% and 101% and the RSD from six preparations at the concentration 0.1 mg/mL is less than 0.6%. The recovery for 4-epianhydrotetracycline limit procedure over the concentration range from 50% to 150% is between 96% and 102% with RSD less than 5%. The results met the specified acceptance criteria.

  8. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF TOLPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    Directory of Open Access Journals (Sweden)

    Patel Satish A

    2012-09-01

    Full Text Available The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Diclofenac sodium and Tolperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Tolperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in the concentration range of 2-20 μg/ml and 2-20 μg/ml for Diclofenac sodium and Tolperisone hydrochloride, respectively. The concentrations of the drugs were determined by using simultaneous equations at both the wavelengths. The mean recovery was 100.6 ± 0.41 and 99.64 ± 0.50 for Diclofenac sodium and Tolperisone hydrochloride, respectively. The method was successfully applied to laboratory prepared synthetic mixture because no interference from the mixture excipients was found. The suitability of this method for the quantitative determination of Diclofenac sodium and Tolperisone hydrochloride was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of Diclofenac sodium and Tolperisone hydrochloride in combination. The results of analysis have been validated statistically and by recovery studies.

  9. Stability-indicating HPLC method for simultaneous determination of montelukast and fexofenadine hydrochloride

    Directory of Open Access Journals (Sweden)

    Mona Pankhaniya

    2013-01-01

    Full Text Available A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher ® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v, pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 μg/ml and 24-120 μg/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations.

  10. Comparison between lignocaine hydrochloride and ropivacaine hydrochloride as lumbosacral epidural anaesthetic agents in goats undergoing laparoscopy assisted embryo transfer

    Directory of Open Access Journals (Sweden)

    Anubhav Khajuria

    2014-10-01

    Full Text Available Goats (n=12 undergoing laparoscopy assisted embryo transfer were randomly allotted to two groups (I and II and injected lignocaine hydrochloride (4mg/kg or ropivacaine hydrochloride (1mg/kg at the lumbosacral epidural space. The animals were held with raised hind quarters for first three minutes following injection. Immediately after induction of regional anaesthesia, they were restrained in dorsal recumbency in Trendelenburg position in a cradle. Laparoscopy was performed after creating pneumoperitoneum using filtered room air. The mean (± S.E induction time in animals of group I was significantly shorter (5.33 ± 0.61 min than those belonging to group II (12.66 ±1.99 min. Complete analgesia developed throughout the hind quarters and abdomen for 30 min and 60 min in group I and II animal’s respectively. Unlike animals of group I, group II goats continued to show moderate analgesia for 180 minutes. The motor activity returned after a lapse of 130.00 ± 12.64 min and 405.00 ± 46.31 min respectively. Occasional vocalization and struggling was noticed in two goats one from each group irrespective of the surgical manipulations during laparoscopy. The rectal temperature and respiration rates showed only non-significant increase, but the heart rate values were significantly higher (P < 0.5 up to 150 min in animals of both the groups when compared to their baseline values. From this study, it was concluded that both anaesthetic agents produced satisfactory regional anaesthesia in goats undergoing laparoscopy. However, considering the very long delay in regaining the hind limb motor activity, the use of ropivacaine may not be recommended for this purpose. Supplementation of sedative/tranquilizer with lumbosacral epidural anaesthesia needs evaluation.

  11. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: verapamil hydrochloride, propranolol hydrochloride, and atenolol.

    Science.gov (United States)

    Vogelpoel, H; Welink, J; Amidon, G L; Junginger, H E; Midha, K K; Möller, H; Olling, M; Shah, V P; Barends, D M

    2004-08-01

    Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumption was made that these tablets were bioequivalent to the innovator product. The development of a database with BCS-related data is announced by the International Pharmaceutical Federation (FIP).

  12. An enantioselective synthesis of S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride, an important metabolite of fluoxetine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Wheeler, W.J. (Lilly (Eli) and Co., Indianapolis, IN (United States). Lilly Research Labs.)

    1992-06-01

    The S-enantiomer of [gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride has been prepared in eight steps from acetophenone-[carbonyl-[sup 14]C]. The key step in the synthesis involved the enantioselective reduction of R-2-chloroacetophenone-[1-[sup 14]C]with (-)-diisopinocampheyl-chloroborane in an 86.5% yield. The chlorohydrin was converted to R-phenyloxirane-[1-[sup 14]C], which was subsequently converted to the corresponding R-cyanohydrin by reaction with TMS-CN/CaO. Borane reduction and arylation, followed by salt formation yielded S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride. (author).

  13. The effectiveness and cost-effectiveness of donepezil, galantamine, rivastigmine and memantine for the treatment of Alzheimer's disease (review of Technology Appraisal No. 111): a systematic review and economic model.

    Science.gov (United States)

    Bond, M; Rogers, G; Peters, J; Anderson, R; Hoyle, M; Miners, A; Moxham, T; Davis, S; Thokala, P; Wailoo, A; Jeffreys, M; Hyde, C

    2012-01-01

    Alzheimer’s disease (AD) is the most commonly occurring form of dementia. It is predominantly a disease of later life, affecting 5% of those over 65 in the UK. Review and update guidance to the NHS in England and Wales on the clinical effectiveness and cost-effectiveness of donepezil, galantamine, rivastigmine [acetylcholinesterase inhibitors (AChEIs)] and memantine within their licensed indications for the treatment of AD, which was issued in November 2006 (amended September 2007 and August 2009). Electronic databases were searched for systematic reviews and/or metaanalyses, randomised controlled trials (RCTs) and ongoing research in November 2009 and updated in March 2010; this updated search revealed no new includable studies. The databases searched included The Cochrane Library (2009 Issue 4, Cochrane Database of Systematic Reviews and Cochrane Central Register of Controlled Trials), MEDLINE, MEDLINE In-Process & Other Non-Indexed Citations, EMBASE, PsycINFO, EconLit, ISI Web of Science Databases--Science Citation Index, Conference Proceedings Citation Index, and BIOSIS; the Centre for Reviews and Dissemination (CRD) databases--NHS Economic Evaluation Database, Health Technology Assessment, and Database of Abstracts of Reviews of Effects. The clinical effectiveness systematic review was undertaken following the principles published by the NHS CRD. We included RCTs whose population was people with AD. The intervention and comparators depended on disease severity, measured by the Mini Mental State Examination (MMSE). mild AD (MMSE 21-26)--donepezil, galantamine and rivastigmine; moderate AD (MMSE 10-20)--donepezil, galantamine, rivastigmine and memantine; severe AD (MMSE costs and cost-effectiveness. Where appropriate, data were pooled using pair-wise meta-analysis, multiple outcome measures, metaregression and mixedtreatment comparisons. The decision model was based broadly on the structure of the three-state Markov model described in the previous technology

  14. Effects of donepezil combined with nimodipine on cognition impairment in patients with Parkinson's disease%多奈哌齐联合尼莫地平治疗帕金森病伴认知障碍

    Institute of Scientific and Technical Information of China (English)

    韩健; 郭富强

    2012-01-01

    目的 观察多奈哌齐联合尼莫地平治疗帕金森病伴认知障碍(PD-CIND)的疗效.方法 120例PD-CIND患者分为试验组、对照组各60例.就诊1 wk内,在PD的常规治疗基础上,试验组予尼莫地平片30 mg tid,多奈哌齐片5 mg qn;对照组单用多奈哌齐片5 mg qn.2组均连续使用3 mo.用药前、用药3 mo后进行蒙特利尔认知评估量表(MoCA)进行评估.结果 2组治疗后MoCA各条目及总分均较治疗前有明显提高,其中试验组与治疗前比较有非常显著意义(P<0.01),对照组有延迟回忆、定向力2个条目与治疗前比较无显著意义(P>0.05);2组间治疗后得分比较,除注意、抽象两个条目外,余条目及总分试验组均高于对照组(P<0.05).结论 多奈哌齐联合尼莫地平对改善PD-CIND是有效的,且优于单用多奈哌齐.%AIM To explore the effects of donepezil combined with nimodipine on cognition impairment in the patients with Parkinson's disease (PD). METHODS A total of 120 patients with PD and cognitive impairment without dementia (PD-CIND) were randomly divided into trial group (60 patients administered with donepezil 30 mg, tid. and nimodipine 5 mg, qn. for 3 months) and control group (60 patients administered with donepezil 5 mg, qn. for 3 months). To assess the cognitive state, we tested the patients using Chinese version of Montreal Cognitive Assessment Scale (MoCA) at baseline and after 3 months. RESULTS Compared with baseline values, the score of MoGA after 3 months in the two groups increased significantly on all items (P 0.05) in the control group. After the treatment, there was significant difference in the MoCA scores between the two groups except the items of attention and abstract ( P < 0.05) . CONCLUSION Donepezil combined with nimodipine is effective in the treatment of PD-CIND, and is superior to the single use of donepezil.

  15. 多奈哌齐对血管性痴呆小鼠海马caspase-3表达的影响%Effect of donepezil on caspase-3 expression in hippocampus of mice with vascular dementia

    Institute of Scientific and Technical Information of China (English)

    杜江; 张德军; 王勇; 王运杰

    2012-01-01

    Objective To study the effect of donepezil on the expression change of cysteinyl aspirate specific-proteinase 3 (caspase-3) in the hippocampus of mice with vascular dementia (VD). Methods The models of VD mice were established through three times of ischemia-reperfusion in bilateral common carotid arteries. 90 Kunming mice were randomly divided into sham operation(30) ,model (30)and treatment groups (treated with donepezil). The behavioral scores were investigated by step-down and water maze tests at days 29 and 30 respectively. The expression of caspase-3 in the hippocampus of mice was examined by immunohistochemistry and western blot. Results The grades of learning and memory of mice treated with donepezil was obviously increased than those of VD mice(P<0. 05). The expression of caspase-3 in the hippocampus of mice treated with donepezil was lower than in VD mice(P<0. 05). Conclusion Donepezil can down-regulate the expression of caspase-3 in the hippocampus of mice with vascular dementia.%目的 探讨盐酸多奈哌齐对血管性痴呆(VD)小鼠海马半胱氨酸蛋白酶-3(cysteinyl aspirate specific-proteinase 3,caspase-3)表达的调节作用.方法 采用双侧颈总动脉反复缺血-再灌注法制备小鼠VD模型.90只雄性昆明小鼠随机分为3组,假手术组(30只)、模型组(30只)及盐酸多奈哌齐治疗组(30只).在术后第29天、第30天,经跳台试验和水迷宫试验进行行为学测试,用免疫组化和western blot方法检测各组小鼠海马caspase-3的表达变化.结果 盐酸多奈哌齐治疗组小鼠的学习和记忆成绩明显高于VD模型组小鼠(P<0.05);免疫组化和Western blot结果发现,盐酸多奈哌齐治疗组小鼠海马CA1区caspase-3蛋白阳性表达的平均光密度值显著低于VD模型组(P<0.05).结论 盐酸多奈哌齐能够降低VD小鼠海马caspase-3的表达.

  16. A system review of efficacy of donepezil in treatment of vascular dementia%多奈哌齐治疗血管性痴呆临床疗效的系统评价

    Institute of Scientific and Technical Information of China (English)

    马卓; 陈月; 冯婉玉

    2013-01-01

    Objective: To evaluate the clinical efficacy of donepezil in treating vascular dementia. Methods : CNKI, CMCC, Medline, PubMed and Embase database were searched for articles about donepezil in treating vascular dementia between January 1997 and February 2012. Forest plot with meta-analysis was drawn by RevMan 5.0. Results; Twenty-two literatures met inclusion creteria. Meta-analysis of 17 included studies revealed that the patients treated with donepezil had better mini-mental state examination (MMSE) scale score than before treatment and the placebo group [ MD = 3. 45 , 95% CI = ( 2. 85 , 4. 04 ) , ( P < 0. 05 ) ] ; the patients treated with donepezil had improved daily living ( ADL) scale score than before treatment and the placebo group [ MD = -7.09,, 95% CI = ( -7.90, -6. 29) , (P < 0. 05) ] in 15 included studies. A total of four articles reported MMSE scores change [MD=0.68,95% CI = (0.40, 0.95), (P<0.05)] and AD AS-Cog scores change [MD =- 1, 34, 95% CI = ( -1.77, -0.90), (P<0.05)] compared with placebo group. Conclusion; The results of existing self-control studies and placebo-control studies proved that donepezil can significantly improve the cognitive function and daily Chinese Journal of New Drugs 2013,22(5) living ability of patients with VD.%目的:评价多奈哌齐治疗血管性痴呆(vascular dementia,VD)的临床疗效.方法:检索CNKI,CMCC,Medline,PubMed,Embase数据库,检索从1997年1月至2012年2月公开发表的多奈哌齐治疗血管性痴呆的研究,对符合纳入标准的文献,运用RevMan 5.0软件对文献数据进行Meta分析,绘制森林图.结果:共纳入文献22篇.Meta分析结果显示,在改善血管性痴呆患者简易精神状态检查量表(mini-mental state examination,MMSE)评分值方面,共纳入文献17篇,[MD =3.45,95% CI:2.85~4.04,P<0.05],多奈哌齐治疗后优于治疗前及安慰剂组;在改善血管性痴呆日常生活能力量表(activities of daily living,ADL)评分值方面,共纳入文献15

  17. Stability-indicating HPTLC determination of ambroxol hydrochloride in bulk drug and pharmaceutical dosage form.

    Science.gov (United States)

    Jain, P S

    2010-01-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for the analysis of ambroxol hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed HPTLC aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of methanol-triethylamine (4:6 v/v). The system was found to give a compact spot for ambroxol hydrochloride (R(f) value of 0.53 +/- 0.02). Densitometric analysis of ambroxol hydrochloride was carried out in the absorbance mode at 254 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r(2) = 0.9966 +/- 0.0013 with respect to peak area in the concentration range 100-1000 ng/spot. The mean value +/- standard deviation of slope and intercept were 164.85 +/- 0.72 and 1168.3 +/- 8.26 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantitation were 10 and 30 ng/spot, respectively. Ambroxol hydrochloride was subjected to oxidation and thermal degradation. The drug undergoes degradation under oxidation and heat conditions. This indicates that the drug is susceptible to oxidation and heat. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of said drug. Stability indicating of new chemical entities is an important part for the drug development of ambroxol hydrochloride and for its estimation in plasma and other biological fluids; the novel Statistical analysis proves that the method is repeatable and selective for the analysis of ambroxol hydrochloride as bulk drug and in pharmaceutical formulations. The proposed developed HPTLC method can be applied for identification and quantitative determination of ambroxol hydrochloride in bulk drug and dosage forms. This work is to determine the purity of the drug available from the various sources by detecting

  18. SYNTHESIS OF 2, 6-DIAMINO-3-PHENYLAZOPYRIDINE-1-OXIDE AND ITS HYDRO-CHLORIDE

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    Ganesh Babu Talagadadeevi, Ramakrishna Muvva, Bangar Reddy Vancha and Madhusudana Rao Jampani*

    2013-11-01

    Full Text Available The compound 2, 6-diamino-3-phenylazopyridine hydrochloride salt is a genito-urinary antiseptic drug under the trade name Pyridinium. This study is directed towards the occurrence of an oxidation reaction to convert the tertiary amine present in 2, 6-diamino-3-phenylazopyridine hydrochloride to form an N-oxide derivative as an impurity in the process for its preparation. This was done by the independent synthesis of 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride salt by two independent routes. The presence of three amine functions in the molecule required first to protect the primary amine groups by derivatisation so that oxidation occurs exclusively at the tertiary amino group of the pyridine ring. 2, 6-diamino-3-phenylazopyridine was acetylated to get 2, 6-diacetamido-3-phenylazopyridine whose structure was confirmed from 1H NMR and mass spectral data. The oxidation of diacetyl derivative with peracetic acid resulted not only in the N-oxide formation but also in the cleavage of one of the acetamido group to give 2(6-acetamido-6(2amino-3-phenylazopyridine-1-oxide. The alkaline hydrolysis of the N-oxide form gave 2, 6-diamino-3-phenylazopyridine-1-oxide which on treatment with hydrochloric acid gave 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride. In yet another route the N-oxide was prepared by the coupling reaction between benzene diazonium chloride and 2, 6-diaminopyridine-1-oxide in aqueous hydrochloric acid medium. This reaction resulted in the formation of 2, 6-diamino-3- phenylazopyridine-1-oxide hydrochloride as an insoluble salt. The structure of the N-oxide was confirmed from 1H NMR and mass spectral data. A co-injection HPLC analysis showed the complete absence of 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride in 2, 6-diamino-3-phenylazopyridine hydrochloride in its manufacturing process.

  19. High Performace Liquid Chromtographic Determination of Nicardipine Hydrochloride in Human Plasma

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    Y. S. R. Krishnaiah

    2004-01-01

    Full Text Available A sensitive high-performance liquid chromatographic method was developed for the estimation of nicardipine hydrochloride in human plasma. Varying amount of nicardipine hydrochloride (2.5 to 150 ng/0.5 mL and fixed quantity (100 ng/0.5 mL of nifedipine (internal standard was added to blank human plasma, and a single step extraction was carried out with ethyl acetate. The mixture was centrifuged, ethyl acetate layer separated, dried and reconstituted with 100 μL of acetonitrile. Twenty microliters of this solution was injected into a reverse phase C-18 column using a mobile phase consisting of acetonitrile: 0.02 M potassium dihydrogen phosphate (pH 4.0 in the ratio of 60:40 v/v and the eluents were monitored at 239 nm. The method was validated for its linearity, precision and accuracy. The calibration curve was linear in the range of 5-150 ng/0.5 mL of plasma and the lower detection limit was 2.5 ng/0.5 mL of plasma. The intra- and inter-day variation was found to be less than 2.5% indicating that the method is highly precise. The mean recovery of nicardipine hydrochloride from plasma samples was 89.6±2.60%. The proposed HPLC method was applied for the estimation of nicardipine hydrochloride in human plasma after oral administration of an immediate release nicardipine hydrochloride capsule (dose 30 mg to 6 adult male volunteers. There was no interference of either the drug metabolites or other plasma components with the proposed HPLC method for the estimation of nicardipine hydrochloride in human plasma. Due to its simplicity, sensitivity, high precision and accuracy, the proposed HPLC method may be used for biopharmaceutical and pharmacokinetic evaluation of nicardipine hydrochloride and its formulations in humans

  20. Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium.

    Science.gov (United States)

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2015-01-01

    In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.

  1. HPLC Determination of Propranolol Hydrochloride,Verapamil Hydrochloride and Propafenone Hydrochloride Ilegally Mixed into Wenxin Granules%高效液相色谱法测定稳心颗粒中非法添加药物的含量

    Institute of Scientific and Technical Information of China (English)

    张士勇; 程军; 叶云

    2012-01-01

    Objective To set up a method for the determination of propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride illegally mixed into Wenxin Granules by HPLC. Methods The HPLC method was used. The Inertsil ODS - SP C18 column (250 mm × 4. 6 mm, 5 μm) was used with the mobile phase of phosphate buffer (adding water to dissolve potassium dihydrogen phosphate 6. 8 g and sodium 1 - octanesulfonate 1. 3 g, and diluting to 1 000 mL, adjusting pH value to 3.0 with phosphoric acid ) -methanol(40: 60). The flow rate was 0.8 mL/min, the detection wavelength was set at 223 nm and the column temperature was 25 ℃. Results The calibration curve showed the good linearity for propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride in the range of 00. 019 76-2.47 μg( r = 1) ,0. 01-2. 5 μg(r = l) and 0.009 948-2.487 μg( r = 1) respectively;the average recovery rates (n = 6) were 97. 11% , 97. 63% and 98. 88% , respectively; RSD were 1. 85% , 1. 92% and 1. 46% , respectively. Conclusion This method is accurate and reproducible, which can be used for the determination of propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride illegally mixed into Wenxin Granules.%目的 建立检测稳心颗粒中非法添加的盐酸普萘洛尔、盐酸维拉帕米和盐酸普罗帕酮含量的高效液相色谱法.方法 采用lnertsil ODS-SP C18色谱柱(250 mm×4.6 mm,5μm),流动相为磷酸盐缓冲液(取磷酸二氢钾6.8 g,辛烷磺酸钠1.3 g,加水溶解并稀释至1 000 mL,用磷酸调节pH至3.0)-甲醇(40:60),流速为0.8 mL/min,检测波长为223 nm,柱温为25℃.结果 盐酸普萘洛尔、盐酸维拉帕米和盐酸普罗帕酮进样量的线性范围分别为0.019 76~2.47 μg(r=1),0.01~2.5μg(r=1)和0.009 948~2.487μg(r=1);平均回收率分别为97.11%,97.63%和98.88%,RSD分别为1.85%,1.92%和1.46%(n=6).结论 该方法准确、重现性好,可作为稳心颗粒中非法添加盐酸普萘洛尔、

  2. Distribution of intravenously administered acetylcholinesterase inhibitor and acetylcholinesterase activity in the adrenal gland: 11C-donepezil PET study in the normal rat.

    Directory of Open Access Journals (Sweden)

    Tadashi Watabe

    Full Text Available PURPOSE: Acetylcholinesterase (AChE inhibitors have been used for patients with Alzheimer's disease. However, its pharmacokinetics in non-target organs other than the brain has not been clarified yet. The purpose of this study was to evaluate the relationship between the whole-body distribution of intravenously administered (11C-Donepezil (DNP and the AChE activity in the normal rat, with special focus on the adrenal glands. METHODS: The distribution of (11C-DNP was investigated by PET/CT in 6 normal male Wistar rats (8 weeks old, body weight  = 220 ± 8.9 g. A 30-min dynamic scan was started simultaneously with an intravenous bolus injection of (11C-DNP (45.0 ± 10.7 MBq. The whole-body distribution of the (11C-DNP PET was evaluated based on the Vt (total distribution volume by Logan-plot analysis. A fluorometric assay was performed to quantify the AChE activity in homogenized tissue solutions of the major organs. RESULTS: The PET analysis using Vt showed that the adrenal glands had the 2nd highest level of (11C-DNP in the body (following the liver (13.33 ± 1.08 and 19.43 ± 1.29 ml/cm(3, respectively, indicating that the distribution of (11C-DNP was the highest in the adrenal glands, except for that in the excretory organs. The AChE activity was the third highest in the adrenal glands (following the small intestine and the stomach (24.9 ± 1.6, 83.1 ± 3.0, and 38.5 ± 8.1 mU/mg, respectively, indicating high activity of AChE in the adrenal glands. CONCLUSIONS: We demonstrated the whole-body distribution of (11C-DNP by PET and the AChE activity in the major organs by fluorometric assay in the normal rat. High accumulation of (11C-DNP was observed in the adrenal glands, which suggested the risk of enhanced cholinergic synaptic transmission by the use of AChE inhibitors.

  3. Distribution of intravenously administered acetylcholinesterase inhibitor and acetylcholinesterase activity in the adrenal gland: 11C-donepezil PET study in the normal rat.

    Science.gov (United States)

    Watabe, Tadashi; Naka, Sadahiro; Ikeda, Hayato; Horitsugi, Genki; Kanai, Yasukazu; Isohashi, Kayako; Ishibashi, Mana; Kato, Hiroki; Shimosegawa, Eku; Watabe, Hiroshi; Hatazawa, Jun

    2014-01-01

    Acetylcholinesterase (AChE) inhibitors have been used for patients with Alzheimer's disease. However, its pharmacokinetics in non-target organs other than the brain has not been clarified yet. The purpose of this study was to evaluate the relationship between the whole-body distribution of intravenously administered (11)C-Donepezil (DNP) and the AChE activity in the normal rat, with special focus on the adrenal glands. The distribution of (11)C-DNP was investigated by PET/CT in 6 normal male Wistar rats (8 weeks old, body weight  = 220 ± 8.9 g). A 30-min dynamic scan was started simultaneously with an intravenous bolus injection of (11)C-DNP (45.0 ± 10.7 MBq). The whole-body distribution of the (11)C-DNP PET was evaluated based on the Vt (total distribution volume) by Logan-plot analysis. A fluorometric assay was performed to quantify the AChE activity in homogenized tissue solutions of the major organs. The PET analysis using Vt showed that the adrenal glands had the 2nd highest level of (11)C-DNP in the body (following the liver) (13.33 ± 1.08 and 19.43 ± 1.29 ml/cm(3), respectively), indicating that the distribution of (11)C-DNP was the highest in the adrenal glands, except for that in the excretory organs. The AChE activity was the third highest in the adrenal glands (following the small intestine and the stomach) (24.9 ± 1.6, 83.1 ± 3.0, and 38.5 ± 8.1 mU/mg, respectively), indicating high activity of AChE in the adrenal glands. We demonstrated the whole-body distribution of (11)C-DNP by PET and the AChE activity in the major organs by fluorometric assay in the normal rat. High accumulation of (11)C-DNP was observed in the adrenal glands, which suggested the risk of enhanced cholinergic synaptic transmission by the use of AChE inhibitors.

  4. Cinchocaine hydrochloride determination by atomic absorption spectrometry and spectrophotometry.

    Science.gov (United States)

    Abdel-Ghani, Nour T; Youssef, Ahmed F A; Awady, Mohamed A

    2005-05-01

    Two sensitive spectrophotometric and atomic absorption spectrometric procedures have been developed for determination of cinchocaine hydrochloride (Cin.Cl) in pure form and in pharmaceutical formulation. The spectrophotometric method was based on formation of an insoluble colored ion-associate between the cited drug and tetrathiocyanatocobaltate (CoTC) or hexathiocyanatochromate (CrTC) which dissolved and extracted in an organic solvent. The optimal experimental conditions for quantitative extraction such as pH, concentration of the reagents and solvent were studied. Toluene and iso-butyl alcohol proved to be the most suitable solvents for quantitative extraction of Cin-CoTC and Cin-CrTC ion-associates with maximum absorbance at 620 and 555 nm, respectively. The optimum concentration ranges, molar absorptivities, Ringbom ranges and Sandell sensitivities were also evaluated. The atomic absorption spectrometric method is based on measuring of the excess cobalt or chromium in the aqueous solution, after precipitation of the drug, at 240.7 and 357.9 nm, respectively. Linear application ranges, characteristic masses and detection limits were 57.99-361.9, 50.40 and 4.22 microg ml(-1) of Cin.Cl, in case of CoTC, while 37.99-379.9, 18.94 and 0.81 microg ml(-1) in case of CrTC.

  5. Dyeing Characteristics of Chitosan Biguanidine Hydrochloride Treated Wool Fabrics

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    Chitosan biguanidine hydrochloride(CGH) has been synthesized by the guanidineylation reaction of chitosan with dicyandiamide.The structures of CGH were characterized by Fourier transform infrared spectroscopy and 13CNMR spectra.In this paper,we used citric acid(CA) as a crosslinking agent,mixed with CGH to perform a pad-drycure treatment on wool fabric to study reaction mechanism during crosslinking with the help of Fourier transform infrared spectroscopy(FT-IR) and scanning electron microscopy(SEM).Dyeing characteristics of CGH treated wool fabric was assessed.The effects of CGH concentration,curing temperature,dipping time,pH value on color yield of reactive dyes on wool fibres were investigated.Fastness properties of the modified wool fabric to laundering and crocking have also been discussed.Fourier transform infrared spectroscopy(FT-IR) showed that CA produce esterification with the-OH group of the wool and transamidation with the-NH2 group of the CGH to form a crosslink.Scanning electron microscopy(SEM) analysis showed the CGH firmly attached to the surface of wool fibre.It was found that the CGH pretreated wool fabrics had significantly improved dyeability characteristics.It is worthwhile to mention that the CGH treated samples have antibacterial potential due to the antibacterial property of chitosan molecules and guanidinium salts.

  6. DESIGN OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF DILTIAZEM HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    L. K. Omray

    2014-02-01

    Full Text Available Gastro retentive drug delivery system of diltiazem hydrochloride was designed and evaluated for its effectiveness for the management of mild to moderate hypertension. Gastro retentive drug delivery system were prepared using polyvinyl alcohol and sodium carboxy methyl cellulose as the polymers and sodium bicarbonate as a gas generating agent for the reduction of floating lag time. Gastro retentive drug delivery system tablets were prepared by wet granulation method by compression in tablet compression machine. Formulations DL1, DL2, DL3, DL4 and DL5 were developed which differed in the ratio of polyvinyl alcohol and sodium carboxy methyl cellulose polymers. All the formulations were evaluated for hardness, weight variation, friability, drug content, swelling index, buoyancy studies and in vitro drug release study. In vitro drug release study was performed using United State Pharmacopoeia 23 type 2 dissolution test apparatus employing paddle stirrer at 50 r/pm. Dissolution medium was 900 ml of 0.1N hydrochloric acid at 37ºC ± 3ºC. Formulations DL3 was found to be better as compared to other formulation.

  7. Prednisone and vardenafil hydrochloride for refractory levamisole-induced vasculitis.

    Science.gov (United States)

    Mandrell, Joshua; Kranc, Christina L

    2016-08-01

    Levamisole is an immunomodulatory drug that was previously used to treat various medical conditions, including parasitic infections, nephrotic syndrome, and colorectal cancer. Over the last few years, increasing amounts of levamisole have been used as an adulterant in cocaine. Levamisole-cut cocaine has become a concern because it is known to cause a necrotizing purpuric rash, autoantibody production, and life-threatening leukopenia. Mixed histologic findings of vasculitis and thrombosis are characteristic of levamisole-induced purpura. The recommended management of levamisole-induced vasculitis currently involves withdrawal of the culprit along with supportive treatment. We describe a patient with levamisole-induced vasculitis who continued to develop skin lesions despite self-reported cocaine cessation. Complete resolution of cutaneous disease occurred with the addition of oral prednisone and vardenafil hydrochloride, suggesting the possibility of a new treatment option in patients with refractory disease. In addition, we review the clinical presentation, disease course, diagnostic approach, laboratory findings, histology, and management of levamisole-induced vasculitis. The harmful effects of levamisole-cut cocaine are serious enough that public alerts have been issued to increase awareness. Clinicians should consider the possibility of levamisole exposure in cocaine users presenting with any combination of fever, neutropenia, and necrotic skin lesions, especially in acral areas including the ears.

  8. Conformation and interactions of dopamine hydrochloride in solution

    Energy Technology Data Exchange (ETDEWEB)

    Callear, Samantha K.; Imberti, Silvia [ISIS Facility, STFC Rutherford Appleton Laboratory, Harwell Oxford, Didcot OX11 0QX (United Kingdom); Johnston, Andrew; McLain, Sylvia E. [Biochemistry Department, University of Oxford, South Parks Road, Oxford OX1 3QU (United Kingdom)

    2015-01-07

    The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and π interactions also playing a significant role in determining the arrangement of adjacent molecules.

  9. FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Chilvalvar Sapnil

    2013-10-01

    Full Text Available The objective of this research work was to develop extended release tablets (Twice in a day of Tramadol Hydrochloride using different Hydrophilic polymers like HPMC K15M, HPMC K4M, Metalose 60SH50, Carbopol 971P, Sodium alginate, Xanthan gum by direct compression method. Various amounts of polymers was used in the twenty four proposed formulations (F1 to F24 for the study of release rate retardant effect at 10 %, 15 %, 20 %, 25 % of total weight of tablet matrix respectively. Then the tablets were evaluated in terms of their physical parameters (weight variation, hardness, friability and thickness, drug content and in-vitro release studies. All the formulations showed compliance with pharmacopoeial standards. The in-vitro dissolution study were conducted using USP dissolution apparatus type-II (paddle method in 900 ml 0.1 N HCl for first 2 h and remaining 10 h performed in 6.8 pH phosphate buffer at 100 rpm for a total period of 12 h. Based on the dissolution data comparison with innovator product, formulation F14 was found as the best formulation. The drug release of formulation F14 followed First Order kinetic model and the mechanism was found to be non-Fickian/anomalous according to Korsmeyer-Peppas equation.

  10. FORMULATION DEVELOPMENT OF ISOXSUPRINE HYDROCHLORIDE MODIFIED RELEASE MATRIX TABLETS

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    Ketan Patel

    2012-01-01

    Full Text Available The objective of the present investigation was to study the effect of critical formulation parameters affecting release of isoxsuprine hydrochloride from matrix tablets using combination of polyethylene oxide (PEO and dicalcium phosphate (DCP. The powder blend consisting of drug and excipients was analyzed for angle of repose, Carr’s index and Hausner’s ratio. The tablets were prepared by direct compression method. To assess the compressional behavior of the drug-excipient blend, the tablets were analyzed for friability and crushing strength. The in vitro drug release study was carried out in distilled water. The powder blend exhibited satisfactorily flow as measured by angle of repose, Carr’s index and Hausner’s ratio. The formulation ingredients showed satisfactory tableting properties (friability <1%, crushing strength ≥ 4 kgf. The drug release was modified on addition of PEO and DCP. Addition of 5 to 25% DCP in the formulation of matrix tablets caused apparent difference in the drug dissolution in distilled water. However, the difference was insignificant as analyzed by analysis of variance (ANOVA and similarity factor ( f2. The drug release from the tablets was best explained by Weibull model. Unified Weibull model was evolved to predict drug release from the formulated batches. The findings of this investigation can be extended to industry to cut down the cost of formulation and to by-pass the existing patents employing hydrophilic matrixing agents, at least for selective drugs.

  11. Solvent screening and crystal habit of metformin hydrochloride

    Science.gov (United States)

    Benmessaoud, Ibtissem; Koutchoukali, Ouahiba; Bouhelassa, Mohamed; Nouar, Abderrahim; Veesler, Stéphane

    2016-10-01

    A multi-well setup with video-microscopy was used to study the influence of solvent on solubility, nucleation, and crystallization of an Active Pharmaceutical Ingredient (API): metformin hydrochloride (MET.HCl). Starting with 13 solvents covering a wide variety of polarity and proticity, we found 63 crystallization medium for MET.HCl solid generation: good solvents, good co-solvents and anti-solvent systems. For toxicological reasons, we limited the number of crystallization medium to 18: 3 good solvents (class 3), 3 good co-solvent systems and 12 anti-solvent systems. In order to study the influence of crystallization medium on nucleation temperature, crystal habit and polymorphism of MET.HCl, crystallization was studied by a cooling temperature method. Different crystal habits were observed by optical and scanning electron microscopies, and solid phase were characterized by X-ray powder diffraction, indicating that all the crystals correspond to the thermodynamic stable polymorphic form A of MET.HCl. Finally, the enthalpy of fusion and the melting temperature of MET.HCl were determined by DSC and confirmed the X-ray powder diffraction results.

  12. Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride

    Science.gov (United States)

    Amin, A. S.; Dessouki, H. A.

    2002-10-01

    A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 μg ml -1, respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml -1 for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method.

  13. Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.

    Science.gov (United States)

    Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

    2015-01-01

    Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24 h and pulsed delivery of drug for 3 days (8 h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs.

  14. [POLYHEXAMETHYLENE BIGUANID HYDROCHLORIDE (BIGUANELLE) THERAPY OF BACTERIAL VAGINOSIS].

    Science.gov (United States)

    Kovachev, S; Ganovska, A; Sultanov, E; Ivanova, S; Gizdov, N; Nikolova, L; Iliev, V

    2016-01-01

    The aim of our study was to determine the efficacy and tolerability of local therapy with polyhexamethylene biguanid hydrochloride (BIGUANELLE) in women with anaerobic vaginal infection. We include in our study 23 women (18-50) with established by AMSEL criteria bacterial vaginosis. In all of the women at the beginning and at the end of the survey was performed gynecological examination and microbiological research (AMSEL). The therapeutic scheme at all women is with a single vaginal application of gynecological solution BIGUANELLE. Effectiveness of the treatment was evaluated according to clinical complaints and microbiological research (Amsel criteria: Ph 4.5 >; KOH (+); "clue cells"; specific vaginal fluorine). Tolerability of patients to treatment was assessed by questionnaire. Clinical complaints of patients after the therapy decreased as follows: vaginal fluorine with 73.9%; odor--75%; pruritus--50%; discomfort--90%. Microbiological research and their evaluation by AMSEL, showed the therapeutic efficacy of the therapy in 16 (69.6%) of all (n-23) patients. At 7 (30.4%) women, the treatment remained without effect. At questionnaire answers, 73.9% patients were satisfied with the application of BIGUANELLE, 95.6% of them have implemented it easily, 95.6% of women believe that BIGUANELLE is more convenient to use in comparison with similar products which have a daily application, and none of the patients (100%) have any complaints in applying this gynecological solution. BIGUANELLE showed good clinical efficacy in the treatment of bacterial vaginosis. It is easily applied and well tolerated by the patients.

  15. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride.

    Science.gov (United States)

    Bathool, Afifa; Gowda, D V; Khan, Mohammed S; Ahmed, Ayaz; Vasudha, S L; Rohitash, K

    2012-04-01

    Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS), a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS) used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  16. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride

    Directory of Open Access Journals (Sweden)

    Afifa Bathool

    2012-01-01

    Full Text Available Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS, a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  17. SIMULTANEOUS ESTIMATION OF MEFENAMIC ACID AND DICYCLOMINE HYDROCHLORIDE BY SPECTROSCOPIC METHODS

    Directory of Open Access Journals (Sweden)

    D.N. Prajapati et al

    2012-10-01

    Full Text Available A novel, simple, accurate, sensitive, reproducible, economical spectroscopic method was developed and validated for the determination of Mefenamic acid and Dicyclomine hydrochloride in combined dosage form. Three different analytical methods, Absorption correction method, Differential derivative method, Simultaneous equation method were developed for estimation of Dicyclomine hydrochloride(10mg and Mefenamic acid (250mg in tablet dosage form. wavelength for estimation was 223nm for Dicyclomine hydrochloride and 308.60nm for Mefenamic acid in absorption correction method. 211.60nm was Zero crossing point of Mefenamic acid and 308.80nm was Zero crossing point of Dicyclomine hydrochloride which can estimate in differential derivative method. Simultaneous equation method was developed in NaOH which was linear in the range of 1-6µg/ml for Dicyclomine hydrochloride and 25-150µg/ml for Mefenamic acid, the correlation coefficient obtained was nearer to one. The method was validated for linearity, accuracy and precision as per ICH guidelines. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage form.

  18. RP-HPLC estimation of venlafaxine hydrochloride in tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Baldania S

    2008-01-01

    Full Text Available A simple, specific, accurate, and precise reverse phase high performance liquid chromatographic method was developed and validated for the estimation of venlafaxine hydrochloride in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250 x 4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: 0.05 M potassium dihydrogen orthophosphate (70:30, v/v; pH 6.2 was used. The flow rate was 1.0 ml/min and effluents were monitored at 226 nm. Carbamazepine was used as an internal standard. The retention time of venlafaxine hydrochloride and carbamazepine were 3.7 min and 5.3 min, respectively. The method was validated for specificity, linearity, accuracy, precision, limit of quantification, limit of detection, robustness and solution stability. Limit of detection and limit of quantification for estimation of venlafaxine hydrochloride were found to be 100 ng/ml and 300 ng/ml, respectively. Recoveries of venlafaxine hydrochloride in tablet formulations were found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of venlafaxine hydrochloride in tablet dosage forms.

  19. FORMULATION AND EVALUATION OF S-(--AMLODIPINE BESYLATE AND NEBIVOLOL HYDROCHLORIDE TABLETS

    Directory of Open Access Journals (Sweden)

    Shaikh S.A

    2010-06-01

    Full Text Available The objective of the present study was to develop a tablet formulation of S-(-- amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity.The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  20. Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride

    Directory of Open Access Journals (Sweden)

    S Vidyadhara

    2013-01-01

    Full Text Available In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303. The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler, swellable filler (starch 1500, microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve (0-t and area under first moment curve (0-t were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h.

  1. 奥氮平联合多奈哌齐治疗脑器质性精神障碍疗效观察%Efficacy of olanzapine plus donepezil in the treatment of brain organic psychosis

    Institute of Scientific and Technical Information of China (English)

    潘振山; 魏冬

    2014-01-01

    Objective To explore the efficacy of olanzapine plus donepezil in the treatment of brain organic psychosis (BOP) .Methods Eighty-two BOP patients were randomly divided into 2 groups ,both groups received conventional therapy for brain organic disease and took orally olanzapine ,on this basis research group was plus donepezil .Efficacies and adverse reac-tions were assessed with the Brief Psychiatric Rating Scale (BPRS) ,Positive and Negative Syndrome Scale (PANSS) and Activities of Daily Living (ADL) before and after treatment .Results After treatment all scales scores lowered more significantly compared with pretreatment (P0 .05) .Conclusion Olanzapine plus donepezil has an evident effect and higher safety compared with single olanzapine in the treatment of brain organic psychosis .%目的:探讨奥氮平联合多奈哌齐治疗脑器质性精神障碍的临床疗效和安全性。方法将82例脑器质性精神障碍患者随机分为两组,均接受脑器质性疾病常规治疗及口服奥氮平治疗,研究组在此基础上联合多奈哌齐治疗。于治疗前后采用简明精神病量表、阳性与阴性症状量表、日常生活能力量表评定临床疗效及不良反应。结果治疗后两组各量表评分均较治疗前显著降低(P<0.01),研究组显著低于对照组(P<0.01);两组不良反应发生率比较差异无显著性(P>0.05)。结论奥氮平联合多奈哌齐治疗脑器质性精神障碍临床疗效显著,安全性高,优于单用奥氮平治疗。

  2. Application of near-infrared reflectance spectrometry to the analytical control of pharmaceuticals: ranitidine hydrochloride tablet production.

    Science.gov (United States)

    Dreassi, E; Ceramelli, G; Corti, P; Perruccio, P L; Lonardi, S

    1996-02-01

    The possibility of applying near-infrared reflectance spectrometry to the control of the production cycle of ranitidine hydrochloride tablets was investigated. The results were good for the identification of ranitidine hydrochloride drug substance, mixtures for tablets, cores and coated tablets. The determination of the compound and of its water content also gave satisfactory results.

  3. 75 FR 31790 - Determination That Cysteine Hydrochloride Injection, USP, 7.25%, Was Not Withdrawn From Sale for...

    Science.gov (United States)

    2010-06-04

    ... HUMAN SERVICES Food and Drug Administration Determination That Cysteine Hydrochloride Injection, USP, 7... determination that Cysteine Hydrochloride Injection, USP, 7.25% (Cysteine HCl), was not withdrawn from sale for... applications (ANDAs) for Cysteine HCl if all other legal and regulatory requirements are met. FOR...

  4. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Science.gov (United States)

    2010-07-01

    ... Insulation Resins by the Hydroxylamine Hydrochloride Method A Appendix A to Subpart DDD of Part 63 Protection... Part 63—Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method 1. Scope The method in this appendix was specifically developed for water-soluble phenolic resins that...

  5. Biowaiver monographs for immediate release solid oral dosage forms: amitriptyline hydrochloride.

    Science.gov (United States)

    Manzo, R H; Olivera, M E; Amidon, G L; Shah, V P; Dressman, J B; Barends, D M

    2006-05-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing amitriptyline hydrochloride are reviewed. Its therapeutic uses, its pharmacokinetic properties, the possibility of excipient interactions and reported BE/bioavailability (BA) problems are also taken into consideration. Literature data indicates that amitriptyline hydrochloride is a highly permeable active pharmaceutical ingredient (API). Data on the solubility according to the current Biopharmaceutics Classification System (BCS) were not fully available and consequently amitriptyline hydrochloride could not be definitively assigned to either BCS Class I or BCS Class II. But all evidence taken together, a biowaiver can currently be recommended provided that IR tablets are formulated with excipients used in existing approved products and that the dissolution meets the criteria defined in the Guidances.

  6. Identification of impurities and statistical classification of methamphetamine hydrochloride drugs seized in the China

    Science.gov (United States)

    Zhang, Jian Xin; Zhang, Da Ming; Han, Xu Guang

    2008-01-01

    A total of 48 methamphetamine hydrochloride samples from eight seizures were analyzed using gas chromatography–mass spectrometry (GC–MS) and a flame ionization detector (GC–FID). Major impurities detected include 1,2-dimethyl-3-phenylaziridine, Ephedrine/pseudoephedrine, 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene. These data are suggestive of ephedrine/pseudoephedrine as the main precursor of the methamphetamine hydrochloride samples seized during 2006–2007. Additionally the presence of 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene is indicative that six seizures were synthesized via the more specific ephedrine/hydriodic acid/red phosphorus method. In addition, five impurities were found for the first time in methamphetamine hydrochloride samples. Seventeen impurity peaks were selected from the GC–FID chromatograms. The peak areas of the selected peaks were then grouped for cluster analysis. PMID:19008060

  7. Synthesis, spectral, and anti-microbial studies of thioiminium iodides and amine hydrochlorides.

    Science.gov (United States)

    Britto, Sebastian; Renaud, Philippe; Nallu, Maruthai

    2014-01-01

    To avoid the undesired deprotonation during the addition of organolithium and organomagnesium reagents to ketones, the thioiminium salts, easily prepared from lactams and amides are converted into 2,2-disubstituted and 2-monosubstituted amines by reaction with simple nucleophiles such as organocerium and organocopper reagents. The reaction of thioiminium iodides with organocerium reagents derived by transmetalation of corresponding lithium reagents with anhydrous cerium(III) chloride has been investigated. These thioiminium iodides act as good electrophiles and accept alkylceriums towards bisaddition. The newly synthesized amines have been characterized by 1H and 13C NMR, IR and mass spectra. The amines have been converted into their hydrochlorides and characterized by COSY. These hydrochlorides have been subjected to antimicrobial screening with clinically isolated microorganisms, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi and Candida albicans. The hydrochlorides show quite good activity against these bacteria and fungus. Copyright © 2013 Elsevier B.V. All rights reserved.

  8. The effects of clomipramine hydrochloride in cats with psychogenic alopecia: a prospective study.

    Science.gov (United States)

    Mertens, Petra A; Torres, Sheila; Jessen, Carl

    2006-01-01

    A double-blind, placebo-controlled clinical trial was conducted to determine the efficacy of clomipramine hydrochloride in cats with psychogenic alopecia. Twenty-five cats were randomly assigned to receive clomipramine hydrochloride (0.5 mg/kg orally q 24 hours) or placebo for 56 days. Eleven cats in each group completed the trial. The results of this study showed that clomipramine hydrochloride failed to demonstrate significant changes in the number of grooming bouts, hair regrowth, and the area of alopecia in cats with psychogenic alopecia when compared to a placebo. It was uncertain whether these results reflected a lack of drug efficacy, insufficient treatment duration, or an insufficient number of cases enrolled.

  9. Protective effects of glucosamine hydrochloride against free radical-induced erythrocytes damage.

    Science.gov (United States)

    Jamialahmadi, Khadijeh; Arasteh, Omid; Matbou Riahi, Maryam; Mehri, Soghra; Riahi-Zanjani, Bamdad; Karimi, Gholamreza

    2014-07-01

    Glucosamine (GlcN) is an important precursor in the biochemical synthesis of glycosylated proteins and lipids in human body. It gains importance because of its contribution to human health and its multiple biological and therapeutic effects. In this study, the in vitro oxidative hemolysis of rat erythrocyte was used as a model to study the potential protective effect of glucosamine hydrochloride against free radical-induced damage of biological membranes. Glucosamine hydrochloride exhibited dose-dependent DPPH antioxidant activity. Oxidative hemolysis and lipid/protein peroxidation of erythrocytes induced by a water-soluble free radical initiator 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH) were significantly suppressed by GlcN in a time and dose dependent manner. GlcN also prevented the depletion of cytosolic antioxidant glutathione (GSH) in erythrocytes. These results indicated that glucosamine hydrochloride efficiently protected erythrocytes against free radicals and it could be recommended as a pharmaceutical supplement to alleviate oxidative stress.

  10. Simultaneous determination of salbutamol sulphate and bromhexine hydrochloride in tablets by reverse phase liquid chromatography

    Directory of Open Access Journals (Sweden)

    Pai P. N. S.

    2009-01-01

    Full Text Available A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of salbutamol sulphate and bromhexine hydrochloride. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and phosphate buffer, pH 4 in the ratio 60:20:20 v/v. The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 224 nm. The described method was linear over a concentration range of 10-110 µg/ml and 20-140 µg/ml for the assay of salbutamol sulphate and bromhexine hydrochloride, respectively. The mean recovery was found to be 95-105% for salbutamol sulphate and 96.2-102.1% for bromhexine hydrochloride when determined at five different levels.

  11. Management of attention-deficit hyperactivity disorder in adults: focus on methylphenidate hydrochloride

    Directory of Open Access Journals (Sweden)

    Rajasree Nair

    2009-08-01

    Full Text Available Rajasree Nair, Shannon B MossBaylor Family Medicine Residency at Garland, Garland, Texas, USAAbstract: Attention-deficit hyperactivity disorder (ADHD is one of the most common psychiatric disorders in young adults and causes significant psychosocial impairment and economic burden to society. Because of the paucity of long-term evidence and lack of national guidelines for diagnosis and management of adult ADHD, most of the data are based on experience derived from management of childhood ADHD. This article reviews the current evidence for the diagnosis and management of adult ADHD with special emphasis on the role of methylphenidate hydrochloride preparations in its treatment. Methylphenidate hydrochloride, a stimulant that acts through the dopaminergic and adrenergic pathways, has shown more than 75% efficacy in controlling the symptoms of adult ADHD. Although concern for diversion of the drug exists, recent data have shown benefits in preventing substance use disorders in patients with adult ADHD.Keywords: adult ADHD, treatment, stimulants, methylphenidate hydrochloride

  12. Multi-walled carbon nanotubes based catalyst plasmon resonance light scattering analysis of tetracycline hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    It was found that multi-walled carbon nanotubes (MWNTs) could catalyze the redox reaction between chlorauric acid (HAuCl4) and reductive drugs such as tetracycline hydrochloride (TC), producing gold nanoparticles (Au NPs). By measuring the plasmon resonance light scattering (PRLS) signals of the resulting Au NPs, tetracycline hydrochloride can be detected simply and rapidly with a linear range of 4―26 μmol/L, a correlated coefficient (r ) of 0.9955, and a limit of detection (3σ) of 6.0 nmol/L. This method has been successfully applied to the detection of tetracycline hydrochloride tablets in clinic with the recovery of 101.9% and that of fresh urine samples with the recovery of 98.3%―102.0%.

  13. HPLC Method for the Determination of Tamsulosin Hydrochloride in Sustained Release Tablets

    Institute of Scientific and Technical Information of China (English)

    齐美玲; 王鹏; 耿颖姝; 顾峻岭

    2003-01-01

    The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% phosphoric acid solution (20∶30∶50,V/V/V) at a flow rate of 1.0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0.81-8.10 μg/mL. The mean recovery was 99.8% (SR=0.7%, n=9), and the precision was found to be 0.45% (n=9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.

  14. Formulation and evaluation of S-(--Amlodipine besylate and nebivolol hydrochloride tablets

    Directory of Open Access Journals (Sweden)

    S A Shaikh

    2010-01-01

    The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  15. Thermal Analysis Investigation of Dapoxetine and Vardenafil Hydrochlorides using Molecular Orbital Calculations.

    Science.gov (United States)

    Attia, Ali Kamal; Souaya, Eglal R; Soliman, Ethar A

    2015-11-01

    Thermal analysis techniques have been used to study the thermal behavior of dapoxetine and vardenafil hydrochlorides and confirmed using semi-empirical molecular orbital calculations. Thermogravimetric analysis, derivative thermogravimetry, differential thermal analysis and differential scanning calorimetry were used to determine the thermal behavior and purity of the drugs under investigation. Thermodynamic parameters such as activation energy, enthalpy, entropy and Gibbs free energy were calculated. Thermal behavior of DAP and VAR were confirmed using by semi-empirical molecular orbital calculations. The purity values were found to be 99.97% and 99.95% for dapoxetine and vardenafil hydrochlorides, respectively. The purity of dapoxetine and vardenafil hydrochlorides is similar to that found by reported methods according to DSC data. Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs.

  16. Formulation, Development and Evaluation of delayed release capsules of Duloxetine Hydrochloride made of different Enteric Polymers

    Directory of Open Access Journals (Sweden)

    Pallavi Yerramsetty

    2012-03-01

    Full Text Available Delayed release systems have acquired a centre stage in the arena of pharmaceutical research and development. The present study involves formulation and evaluation of Duloxetine Hydrochloride delayed release capsules. Duloxetine Hydrochloride is an acid labile drug. It degrades in the acidic environment of the stomach thus leading to therapeutic inefficacy. Therefore it is necessary to bypass the acidic pH of the stomach which can be achieved by formulating delayed release dosage form by using different enteric polymers. Protection of drug from acidic environment is done by coating the drug with enteric polymers by using suspension layering technique in Fluidized bed processor (FBP with different enteric polymers like HPMCAS (Hydroxy Propyl Methyl Cellulose Acetate Succinate, Acryl EZE and HPMCP (Hydroxy propyl methyl cellulose phthalate.The formulation (E12 of delayed release capsules of Duloxetine Hydrochloride containing HPMCP (HP-55: HP- 50 as enteric polymer can be taken as optimized

  17. Compatibility of verapamil hydrochloride injection in commonly used large-volume parenterals.

    Science.gov (United States)

    Cutie, M R; Lordi, N G

    1980-05-01

    The visual and chemical compatibilities of verapamil hydrochloride injection in 10 commonly used large-volume solutions packaged in glass, polyolefin, or polyvinyl chloride containers were studied. The mixtures, each containing 40 mg/liter of verapamil hydrochloride, were stored away from light for up to 48 hours at 25 degrees C. The solutions were examined visually for haze, precipitate formation, color change, and evolution of gas immediately after mixing and at 0.25, 1, 3, 8, 24, and 48 hours. Spectrophotometry and thin-layer chromatography were used to test for drug decomposition or chemical incompatibilities. All test methods used showed that no significant degradation of verapamil hydrochloride had taken place in the solutions or through contact with the containers. Slightly higher spectrophotometric readings for dextrose-containing solutions, though within experimental error, could have indicated the presence of dextrose degradation products. Evidence from this study suggests that verapamil hydrocholoride is compatible with the large-volume parenterals studied.

  18. DEVELOPMENT AND VALIDATION OF SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS DETERMINATION OF PROPRANOLOL HYDROCHLORIDE AND FLUNARIZINE DIHYDROCHLORIDE IN THEIR COMBINED DOSAGE FORMULATION

    Directory of Open Access Journals (Sweden)

    A.K. Doshi*, B.N. Patel and C.N. Patel

    2012-06-01

    Full Text Available A simple, accurate and precise spectrophotometric method has been developed for simultaneous estimation of Propranolol hydrochloride and Flunarizine dihydrochloride in combined dosage form. Simultaneous equation method is employed for simultaneous determination of Propranolol hydrochloride and Flunarizine dihydrochloride from combined dosage forms. In this method, the absorbance was measured at 289 nm for Propranolol hydrochloride and 253 nm for Flunarizine dihydrochloride. Linearity was observed in range of 24-64 μg/ml and 6-16 μg/ml for Propranolol hydrochloride and Flunarizine dihydrochloride respectively. Recovery studies confirmed the accuracy of proposed method and results were validated as per ICH guidelines. The method can be used for routine quality control of pharmaceutical formulation containing Propranolol hydrochloride and Flunarizine dihydrochloride.

  19. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography].

    Science.gov (United States)

    Xuan, Xueyi; Huang, Lina; Pan, Xiaoling; Li, Ning

    2013-02-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase consisted of methanol, 0.05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 degrees C. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths: 0-6 min, 280 nm; 6-7 min, 257 nm; 7-14 min, 280 nm; 14 min, 233 nm. The separation of the five cold medicine ingredients in the tablets was achieved in 25.5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 -0.998 g/L, 0.053-0.946 g/L, 0.007-0.129 g/L, 0.035-0.622 g/L and 0.002-0.039 g/L, respectively, with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97.9%-102.8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets.

  20. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation

    Institute of Scientific and Technical Information of China (English)

    Bayoumy I Eassa; Mohamed A El-Shazly

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder.It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated.The aim of this study is to evaluate the efficacy,safety,tolerability,undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE.A total of 300 patients who presented with lifelong (primary) PE were included in this study.The study was performed for 28 weeks,in which placebo (starch tablet) was given for 4 weeks,and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks.Patients were divided into three equal groups,each consisting of 100 patients.The first group (A) was given tramadol hydrochloride capsule 25 mg.The second group (B) was given tramadol hydrochloride capsule 50 mg.The third group (C) was given tramadol hydrochloride capsule 100 mg.All of the 300 participants included completed the study voluntarily.The age of the patients varied from 25 to 50 years.After the treatment period,the recorded data were collected for each group and analysed.The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001).We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective,safe and tolerable,with minimal undesirable effects,and approval for this indication should be sought.

  1. BRAIN TARGETING OF FLUNARIZINE HYDROCHLORIDE BY SOLID LIPID NANOPARTICLES FOR PROPHYLAXIS OF MIGRAINE

    Directory of Open Access Journals (Sweden)

    Mandal Surjyanarayan

    2011-09-01

    Full Text Available Flunarizine hydrochloride, a piperazine derivative, is a selective Ca++ channel blocker coupled with its antihistaminic property claimed to be effective in prophylaxis of migraine. Oral bioavailability of Flunarizine hydrochloride is very low (less then 18% due to poor water solubility and extensive first pass metabolism. Hence the aim of the present study was to develop Flunaruzine hydrochloride loaded sold lipid nanoparticles to improve drug diffusion profile and hence the oral bioavailability. Flunarizine hydrochloride nanosuspension stabilised by poloxamer F-68 was first prepared by high speed homogenization and was lyophilized to obtain nanoparticle using mannitol (1:1 w/v as cryoprotectant. Developed nanoparticle was characterized for its particle size and size distribution, drug content and % drug entrapment. In vitro dissolution study using dissolution bag (12000 D and ex vivo study in rat ileum were carried out using simulated intestinal fluid as dissolution medium. Droplet size, Zeta potential, % drug content and % drug entrapment of the nanoparticles of the Flunarizine hydrochloride were found to be 282±50nm with PdI=0.424±0.028, 34.9±7.36mV, 98.3±0.26% and 67±0.55% respectively. In vitro, ex vivo permeation study revealed that cumulative percentage drug permeated was found to be 75.66±0.9% and 69±1.4% in 8 hrs. Data of the ex vivo release study indicated that drug release was controlled by combination of lipid swelling, erosion and diffusion through the hydrated lipid matrix. From the results it could be considered that the developed Flunarizine hydrochloride nanoparticles may be an alternative for the prophylaxis of migraine.

  2. Effect of Clenbuterol Hydrochloride on the in vitro Development of Mouse Embryo

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Objective To investigate the effect of clenbuterol hydrochloride on the in vitro devel-opment of both 1-cell and 2-cell mouse embryos.Methods The cultural systems of both 1-cell and 2-cell mouse embryo were used todetermine the effect of clenbuterol hydrochloride at doses of 1 ng/mL, 3 ng/mL, and10 ng/mL on developmental rates of mouse embryos.Results When 1-cell embryos cultured with 1 ng/mL of clenbuterol hydrochloride,developmental rates from the 4-cell stage to blastocyst stage were significantly lowerthan those in the control group (P< 0. 05), but on dosages of 3 ng/mL and 10ng/mL,the inhibiting effects on embryo development were significantly increased (P< 0. 01).When 2-cell embryos cultured with 1 ng/mL of clenbuterol hydrochloride, obvious dif-ferences in developmental rates were not found between the 2-cell embryo group and thecontrol (P> 0. 05). However, at levels of 3 ng/mL and 10 ng/mL, significant de-crease of developmental rates in 2-cell embryos was observed from the 4-cell and fromthe 8-cell stage, respectively (P< 0. 05). Embryos cultured with clenbuterol hydrochlo-ride appeared to have more granules, fragments and degeneration than those in thecontrol.Conclusion Clenbuterol hydrochloride has a toxic effect on the mouse embryos, and theeffect is in a dose-dependent. 1-cell mouse embryos cultured with clenbuterolhydrochloride could be easily inhibited at 2-cell stage, but the effect of clenbuterolhydrochloride on development of the late 2-cell embryos would be reduced.

  3. SIMULTANEOUS ESTIMATION OF DICLOFENAC SODIUM AND TOLPERISONE HYDROCHLORIDE IN COMBINED PHARMACEUTICAL FORMULATION

    Directory of Open Access Journals (Sweden)

    Bhavesh Gevriya* and R.C. Mashru

    2013-01-01

    Full Text Available Three simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Tolperisone Hydrochloride (TOL and Diclofenac Sodium (DIC in their combined dosage form. Method A, Simultaneous equation method (Vierodt’s method applies measurement of absorptivities at two wavelengths, 261.00 nm (λmax of Tolperisone Hydrochloride and 279.00 nm, (λmax of Diclofenac Sodium in zero order spectra. The concentrations can be calculated from the derived equations. Method B, Q-Absorbance equation method. It involves formation of Q-absorbance equation at 233.50 nm (isoabsorptive point and 261.00 nm (λmax of Tolperisone Hydrochloride in zero order spectra. Method C, Zero crossing first derivative spectrophotometry involves measurement of absorbance at 249.20 nm (for Tolperisone Hydrochloride and 227.40 nm (for Diclofenac Sodium in first derivative spectra. Developed methods were validated according to ICH guidelines. The calibration graph follows Beer’s law in the range of 6.0 to 18.0 μg/ml for Tolperisone Hydrochloride and 2.0 to 6.0 μg/ml for Diclofenac Sodium with R square value greater than 0.999. Accuracy of all methods was determined by recovery studies and showed % recovery between 98 to 102%. Intraday and interday precision was checked for all methods and mean %RSD was found to be less than 2 for all the methods. The methods were successfully applied for estimation of Tolperisone Hydrochloride and Diclofenac Sodium in marketed formulation.

  4. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride.

    Science.gov (United States)

    Ranpise, Nisharani S; Korabu, Swati S; Ghodake, Vinod N

    2014-04-01

    Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. The aim of this study was to design lercanidipine hydrochloride-loaded nanostructured lipid carriers to investigate whether the bioavailability of the same can be improved by oral delivery. Lercanidipine hydrochloride nanostructured lipid carriers were prepared by the method of solvent evaporation at a high temperature and solidification by freeze drying. The nanostructured lipid carriers were evaluated for particle size analysis, zeta potential, entrapment efficiency, in vitro drug diffusion, ex vivo permeation studies and pharmacodynamic study. The resultant nanostructured lipid carriers had a mean size of 214.97 nm and a zeta potential of -31.6 ± 1.5 mV. More than 70% lercanidipine hydrochloride was entrapped in the NLCs. The SEM studies indicated the formation of type 2 nanostructured lipid carriers. The in vitro release studies demonstrated 19.36% release in acidic buffer pH 1.2 indicating that the drug entrapped in the nanostructured lipid carriers remains entrapped at acidic pH. The ex vivo studies indicated that the drug release was enhanced from 10% to 60.54% at blood pH in 24h. The in vivo pharmacodynamic study showed that NLCs released lercanidipine hydrochloride in a controlled manner for a prolonged period of time as compared to plain drug. These results clearly indicate that nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension. Copyright © 2013 Elsevier B.V. All rights reserved.

  5. Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.

    Science.gov (United States)

    Nanjwade, Basavaraj K; Deshmukh, Rucha V; Gaikwad, Kishori R; Parikh, Kemy A; Manvi, F V

    2012-06-01

    The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.

  6. Progress in Related Single Nucleotide Polymorphism in the Therapeutic Response of Donepezil in Patients with Alzheimer′s Disease%多奈哌齐治疗阿尔茨海默病的疗效相关基因多态性研究进展

    Institute of Scientific and Technical Information of China (English)

    卢进; 万丽丽; 郭澄

    2016-01-01

    目的:综述多奈哌齐治疗轻中度阿尔茨海默病(AD)的疗效相关基因多态性的研究进展,为其疗效相关研究及临床合理使用提供参考。方法检索PubMed及CNKI等数据库中关于影响多奈哌齐治疗AD相关疗效的影响因素,分析与多奈哌齐疗效相关的基因多态性特征。结果与结论多奈哌齐临床治疗个体差异大的主要原因可能与遗传因素密切相关。其中CYP2D6,CY3A4,APOE,ESR1,BCHE, PON-1,CHRNA7及CHAT的基因多态性与多奈哌齐疗效有关,未来可能成为多奈哌齐治疗轻中度AD的遗传标记物。%Objective To summarize the progress in related single nucleotide polymorphism in the clinical efficacy of donepezil in pa-tients with Alzheimer's disease, to provide evidence to related study and clinical applications of donepezil. Methods Using databases such as PubMed and CNKI to analyze the genetic influencing factor and the clinical efficacy of donepezil for treating Alzheimer's dis-ease. Results and Conclusion The rate of clinical efficacy of patients to donepezil varies, most likely because of their genetic back-ground. The polymorphism of CYP2D6, CY3A4, APOE, ESR1, BCHE, PON-1, CHRNA7 and CHAT were closely related to the therapeutic response of donepezil in patient with Alzheimer's disease. They can be taken in consider to become the future biomarker in clinical therapy of donepezil.

  7. Clinical Research of Donepezil on the Security of Cardiovascular System in the Patients with Alzheimer’s Disease%多奈哌齐片对阿尔茨海默病患者心血管系统安全性的临床研究

    Institute of Scientific and Technical Information of China (English)

    杨春伍; 刘爱举; 丁玉; 顾汉印

    2013-01-01

    目的:探讨多奈哌齐片对阿尔茨海默病(AD)患者心血管系统影响。方法:60例确诊AD患者,先后给予多奈哌齐片5 mg/d、10 mg/d,各4周的序贯治疗,分别测定治疗前、治疗4周和治疗8周时患者心电图和血压,并进行统计学分析。结果:60例患者5例中途退出;治疗4周、8周时患者的心率、P-R间期、Q-T间期、QRS波及血压与治疗前比较均无统计学差异(P>0.05)。结论:多奈派齐对老年患者心血管系统影响较小,相对安全。%Objective: To investigate Donepezil Tablets on the cardiovascular system of patients with Alzheimer’s disease (AD).Method:Sixty diagnosed AD patients were orally given donepezil 5mg/d for 4 weeks and subsequently 10 mg/d for another 4 weeks. Electrocardiography and blood pressure of the enrolled patients were measured before donepezil intaking and after 4 weeks and 8 weeks treatment and then the data were analyzed statistically.Result: 5 patients with 60 cases dropped out. After 4 weeks and 8 weeks donepezil treatment, the heart rate, PR interval, QT interval, QRS wave and blood pressure of the enrolled AD patient were not statistically different compared to those of prior donepezil treatment (P>0.05).Conclusion:Donepezil has little adverse effect on cardiovascular system of the elderly patients and is relatively safe to patients.

  8. Multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer’s disease: design, synthesis, biochemical evaluation, ADMET, molecular modeling, and QSAR analysis of novel donepezil-pyridyl hybrids

    Directory of Open Access Journals (Sweden)

    Bautista-Aguilera OM

    2014-10-01

    Full Text Available Oscar M Bautista-Aguilera,1,* Gerard Esteban,2,* Mourad Chioua,1 Katarina Nikolic,3 Danica Agbaba,3 Ignacio Moraleda,4 Isabel Iriepa,4 Elena Soriano,5 Abdelouahid Samadi,1 Mercedes Unzeta,2 José Marco-Contelles1 1Laboratory of Medicinal Chemistry (Institute of General Organic Chemistry [IQOG], National Research Council [CSIC], Madrid, Spain; 2Department of Biochemistry and Molecular Biology, Institute of Neurosciences, Autonomous Barcelona University, Barcelona, Spain; 3Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia; 4Department of Organic Chemistry, Faculty of Pharmacy, University of Alcalá, Ctra Barcelona, Alcalá de Henares, Spain; 5Synthesis, and Structure of Organic Compounds (SEPCO (IQOG, CSIC, Madrid, Spain *These authors have equally contributed to this work Abstract: The design, synthesis, and biochemical evaluation of donepezil-pyridyl hybrids (DPHs as multipotent cholinesterase (ChE and monoamine oxidase (MAO inhibitors for the potential treatment of Alzheimer’s disease (AD is reported. The 3D-quantitative structure-activity relationship study was used to define 3D-pharmacophores for inhibition of MAO A/B, acetylcholinesterase (AChE, and butyrylcholinesterase (BuChE enzymes and to design DPHs as novel multi-target drug candidates with potential impact in the therapy of AD. DPH14 (­Electrophorus electricus AChE [EeAChE]: half maximal inhibitory concentration [IC50] =1.1±0.3 nM; equine butyrylcholinesterase [eqBuChE]: IC50 =600±80 nM was 318-fold more potent for the inhibition of AChE, and 1.3-fold less potent for the inhibition of BuChE than the reference compound ASS234. DPH14 is a potent human recombinant BuChE (hBuChE inhibitor, in the same range as DPH12 or DPH16, but 13.1-fold less potent than DPH15 for the inhibition of human recombinant AChE (hAChE. Compared with donepezil, DPH14 is almost equipotent for the inhibition of hAChE, and 8.8-fold more potent for h

  9. 观察盐酸多奈哌齐治疗阿尔兹海默病的疗效%Efifcacy of Donepezil in the Treatment of Alzheimer disease

    Institute of Scientific and Technical Information of China (English)

    王霞萍; 潘会玲

    2015-01-01

    目的:探讨盐酸多奈哌齐治疗阿尔兹海默病患者的疗效。方法选择2012年5月~2014年5月本院就诊的阿尔兹海默病患者150例,随机均分为治疗组及对照组,各75例。两组均给予基础治疗,治疗组在此基础上给予盐酸多奈哌齐治疗。结果150例老年痴呆患者中男68例,女82例,年龄60~90岁,60~75岁120例,76~90岁30例,大学学历以下128例,大学及大学以上学历22例。随访2年期间失访10例,实访140例。两组均有不良反应发生,给予对症处理后好转,且两组不良反应发生率比较,差异无统计学意义(x2=1.38,P>0.05)。结论盐酸多奈哌齐治疗老年痴呆安全有效,不良反应较少,值得临床推广。%Objective To evaluate the clinical efifcacy of Donepezil in the treatment of Alzheimer disease. Methods A total of 150 Alzheimer disease patients admitted to our hospital were randomly divided into treatment group (n=75) and control group (n=75). The two groups were both given primary treatment,and the treatment group was given additional Donepezil treatment. Clinical symptoms,physical signs, and ADL score were compared between the two groups before treatment, six months and two years after treatment. Results Among the 150 Alzheimer disease patients,68cases were male and 82 cases were female,the patients were aged from 60 to 90, and 120cases were from 60 to 75 and 30 cases were from 76 to 90,128 cases were under college degree and 22 cases were college degree or above,140 cases were followed up and 10 cases lost following up during the two-year follow up.ADL score before treatment and on six-month following up between the two groups showed statistically statistically signiifcant difference (P0.05). Conclusion Donepezil is safe and effective treatment for Alzheimer disease with little adverse reaction.Donepezil may be regarded as one of best treatments for Alzheimer disease.

  10. Efficacy of combined use of oxiracetam and donepezil in the treatment of elderly vascular dementia%奥拉西坦联合多奈哌齐治疗高龄血管性痴呆的疗效

    Institute of Scientific and Technical Information of China (English)

    张炳山; 王滨; 万鹤鸣

    2016-01-01

    目的:观察奥拉西坦联合多奈哌齐治疗高龄血管性痴呆(VD )的临床疗效。方法老年VD患者96例随机均分为两组:B组每天口服多奈哌齐5 mg ,连续6个月;A组加用奥拉西坦4 g ,加入生理盐水250 ml中静脉滴注,每天1次,21 d为1个疗程,每3个月治疗1个疗程。于治疗前和治疗6个月后进行蒙特利尔认知评估量表(MoCA)、简易精神状态量表(MMSE)和日常生活能力量表(ADL )评分,比较两组疗效。结果两组患者治疗6个月后,M oCA评分和M M SE评分均较治疗前增加(P<0.05),ADL评分降低(P<0.05)。治疗6个月后,A组 MoCA和 MMSE评分高于B组,ADL评分低于B组(P<0.05)。A组有效率为89.58%,高于B组的68.75%(P<0.05)。两组患者治疗前后的肝肾功能均无明显变化(P>0.05)。结论奥拉西坦复合多奈哌齐治疗老年VD的疗效优于多奈哌齐单药治疗。%Objective To observe the efficacy of combined use of oxiracetam and donepezil in the treatment of elderly vascular dementia (VD ) .Methods Ninety-six elderly VD patients were equally and randomly divided into two groups .The patients in group B were treated with oral donepezil 5 mg daily for 6 months ,and those in group A were given additional oxiracetam 4 g in 250 ml normal saline ,which was infused once a day for 21 days as a therapy course in every 3 months .The efficacy was evaluated with the scores of Montreal cognitive assessment (MoCA ) ,minimental state examination (MMSE) and activities of daily living (ADL) before and in 6 months after treatment . Results Compared to before ,MoCA and MMSE scores were significantly higher and ADL score was lower in 6 months after treatment in both groups(P0 .05 ) .Conclusion The efficacy of combined use of oxiracetam and donepezil in the treatment of elderly VD is better than donepezil alone .

  11. Therapeutic effect of Donepezil combined nimodipine treatment in 45 cases with vascular dementia%多奈哌齐片联合尼莫地平治疗血管性痴呆45例的疗效

    Institute of Scientific and Technical Information of China (English)

    林小娟; 杨凌杰

    2015-01-01

    Objective:To observe the therapeutic effect of donepezil combined nimodipine on vascular dementia. Methods:A total of 45 patients with vascular dementia aging 54~76 years were randomly divided into donepezil +nimodipine group (n= 24)and huperzine + piracetam group (n= 21).Scores of mini-mental state examination (MMSE)and activity of daily living (ADL)were examined in two groups before and after treatment,and therapeu-tic effect was compared between two groups.Results:Compared with before treatment,after treatment,MMSE score [(15.8±6.3)scores vs.(21.6±7.4)scores]significantly rose and ADL score [(50.3±6.4)scores vs.(40.2 ±7.1)scores]significantly reduced in donepezil + nimodipine group;MMSE score [(14.6±6.9)scores vs.(18.5 ±7.2)scores]significantly rose,ADL score [(49.3±7.8)scores vs.(43.5±8.2)scores]significantly reduced in huperzine + piracetam group,P <0.01 all;but there were no significant difference between two group after treat-ment (P =0.08,0.07).Conclusion:Therapeutic effect of donepezil combined nimodipine on vascular dementia is quite to huperzine + piracetam.%目的:观察多奈哌齐联合尼莫地平治疗血管性痴呆的临床疗效。方法:45例年龄在54~76岁的血管性痴呆患者被随机分为多奈哌齐+尼莫地平组(24例)和石杉碱甲+吡拉西坦组(21例),测定两组患者治疗前后的简明精神状态检查表(MMSE)评分和日常生活活动评分(ADL),并进行两组疗效的比较。结果:与治疗前比较,治疗后多奈哌齐+尼莫地平组的 MMSE 评分[(15.8±6.3)分比(21.6±7.4)分]显著提高,ADL 评分[(50.3±6.4)分比(40.2±7.1)分]显著下降,石杉碱甲+吡拉西坦组 MMSE 评分[(14.6±6.9)分比(18.5±7.2)分]显著提高,ADL 评分[(49.3±7.8)分比(43.5±8.2)分]显著下降,P 均<0.01;但两组治疗后无显著差异(P=0.08,0.07)。结论:多奈哌齐联合尼莫地平治疗血管性痴呆的疗效

  12. Donepezil and rehabilitation training for patients' with Alzheimer's disease%多奈哌齐联合康复训练治疗老年痴呆患者的临床效果探讨

    Institute of Scientific and Technical Information of China (English)

    王廷玉; 何秀贞; 邓淑芳; 陈章凡; 郭庆忠

    2014-01-01

    Objective To study the clinical efficacy of donepezil and rehabilitation training for patients with Alzheimer' s disease.Methods 144 patients with Alzheimer' s disease were chosen from our hospital from June,2010 to June,2013 and then were randomly and averagely divided into a treatment group and a control group.The control group were treated with donepezil for 8 weeks.And the treatment group were given donepezil and rehabilitation training for 8 weeks.The clinical efficacies were observed.Results 63 patients responded to the treatment well,7 just responded to,and 2 did not in the treatment group,with a efficacy of 97.2%.42 patients responded the treatment well,24 just responded to,and 6 did not in the control group,with a efficacy of 91.7%.The values of MMES and BEHAVE-AD were improved more in the treatment group than in the control group.Conclusions Donepezil and rehabilitation training for patients with Alzheimer' s disease is effective,can improve the patients' mental status and cognitive function,and is worth being clinically generalized.%目的 探讨多奈哌齐联合康复训练治疗老年痴呆患者的临床效果.方法 选取2010年6月至2013年6月我院收治的老年痴呆患者144例,随机将其平均分为实验组及对照组,均口服多奈哌齐,实验组再行康复训练,均治疗8周,并观察两组治疗效果.结果 治疗后实验组显效63例,有效7例,无效2例,总有效率97.2%;对照组显效42例,有效24例,无效6例,总有效率91.7%.实验组总有效率高于对照组,而且实验组MMES评分、BEHAVE-AD评分改善情况优于对照组,差异均具有统计学意义(P<0.05).结论 多奈哌齐联合康复训练治疗老年痴呆临床效果显著,可有效改善患者精神状态及认知功能,并建议在临床治疗中推广应用.

  13. 多萘哌齐联用奥氮平治疗老年期痴呆认知功能临床观察%Donepezil Plus Olanzapine in the Treatment of Cognitive Impairments in Senile Dementia

    Institute of Scientific and Technical Information of China (English)

    陈彩霞; 刘丹

    2015-01-01

    Objective:To compare the effect of combination therapy of Donepezil and Olanzapine and only Donepezil therapy in the treatment of cognitive function in senile dementia .Methods:A total of 65 senile dementia patients were randomly divided into two groups ,Donepezil group ( single group ) and Done-pezil combined with Olanzapine group ( combination group ) ,receiving treatment for 8 weeks.The Mini-mental State Examination(MMSE),was used to assess before treatment ,and at 4 weekend and 8 week-end.Results:Before treatment,there was no significant difference in MMSE score in both two groups .In 4 weeks after treatment ,there was no significant difference in MMSE score in both two groups .At 8 week-end,the significant difference was found in both two groups (t=4.786~7.825,P<0.05).In addition,to compare the two groups ,in 4 weeks after treatment ,there was no significant difference in MMSE score ,At 8 weekend,the significant difference was found in MMSE between the two groups (t=2.59,P<0.05). Conclusion:Both groups can improve the cognitive function in senile dementia , but combination group can more effectively improve the cognitive function in senile dementia.%目的:比较多萘哌齐联用奥氮平与单独使用多萘哌齐治疗老年期痴呆认知功能的临床疗效。方法:共65例老年期痴呆患者随机分为联合使用组与单独使用组,针对两组病人,双盲对照治疗,治疗过程以8周为一个疗程,分别在治疗前、治疗第4周末、治疗第8周末用简易智能精神状态量表( MMSE)测评临床疗效,评估认知功能。结果:在治疗前联合使用组与单独使用组MMSE评分无显著差异。临床治疗第4周末与治疗前比较,联合使用组及单独使用组MMSE评分均无显著差异。疗程第8周末,单独使用组及联合使用组分别与治疗前比较MMSE评分均有显著差异(t=4.786~7.825;P<0.05)。此外,联合使用组与单独使用组在治疗第4周

  14. Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride.

    Science.gov (United States)

    Kortejärvi, H; Yliperttula, M; Dressman, J B; Junginger, H E; Midha, K K; Shah, V P; Barends, D M

    2005-08-01

    Literature and experimental data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate release (IR) solid oral dosage forms containing ranitidine hydrochloride are reviewed. According to the current Biopharmaceutics Classification System (BCS), ranitidine hydrochloride should be assigned to Class III. However, based on its therapeutic and therapeutic index, pharmacokinetic properties and data related to the possibility of excipient interactions, a biowaiver can be recommended for IR solid oral dosage forms that are rapidly dissolving and contain only those excipients as reported in this study.

  15. Development and validation of a dissolution test for diltiazem hydrochloride in immediate release capsules

    Directory of Open Access Journals (Sweden)

    Taciane Ferreira Mendonça

    2011-01-01

    Full Text Available This work describes the development and validation of a dissolution test for 60 mg of diltiazem hydrochloride in immediate release capsules. The best dissolution in vitro profile was achieved using potassium phosphate buffer at pH 6.8 as the dissolution medium and paddle as the apparatus at 50 rpm. The drug concentrations in the dissolution media were determined by UV spectrophotometry and HPLC and a statistical analysis revealed that there were significant differences between HPLC and spectrophotometry. This study illustrates the importance of an official method for the dissolution test, since there is no official monograph for diltiazem hydrochloride in capsules.

  16. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    Directory of Open Access Journals (Sweden)

    Zhi-Gang Cheng

    2014-01-01

    Full Text Available Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm. All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR. The identification of these impurities should be useful for quality control in the manufacture of barnidipine.

  17. Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance.

    Science.gov (United States)

    Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya

    2014-01-21

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm×4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). The identification of these impurities should be useful for quality control in the manufacture of barnidipine.

  18. High performance thin layer chromatographic method for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride

    Directory of Open Access Journals (Sweden)

    Chitlange S

    2008-01-01

    Full Text Available High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F 254 plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively.

  19. Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride

    OpenAIRE

    Gaurav Bhatia; Banga, Ajay K.

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determi...

  20. Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.

    Science.gov (United States)

    2002-01-01

    Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate

  1. Effect of Donepezil and Atrovastatin on moderate or severe Alzheimer disease and its safety%多奈哌齐联合阿托伐他汀治疗中重度阿尔茨海默病的疗效和安全性

    Institute of Scientific and Technical Information of China (English)

    赵晓玲; 刘艳

    2011-01-01

    Objective To explore the efficacy and safety of Donepezil combined with Atrovastatin on patients with moderate or severe Alzheimer disease.Methords Forty-four patients with moderate or severe Alzheimer disease were randomly divided into combination ( Donepezil combined with Atrovstatin ) group and Donepezil group.Results of blood lipid level, Mini-Mental State Examination ( MMSE), activity of daily living(ADL) and global deterioration scale(GDS) were compared respectively between the two groups before and after treatment.Results There was significant difference in the blood lipid level of combination group before and after treatment ( P <0.05 ) ,while not of Donepezil group ( P > 0.05 ).There were significant differences in scores of MMSE, ADL and GDS of the two groups before and after treatment ( P < 0.05 ).Improvements in scores of MMSE, ADL and GDS were significantly greater in combination group than those in Donepezil group statistically ( P < 0.05 ).Conclusions Donepezil can improve effectively the cognitive and daily living skills of moderate or severe Alzheimer disease.The combination of Donepezil and Atrovstatin with high safety is superior to single use of Donepezil.%目的 探讨多奈哌齐联合阿托伐他汀治疗中、重度阿尔茨海默病(Alzheimer disease,AD)患者的疗效及安全性.方法 44例中、重度AD患者采用随机数字表法分为联合用药组和多奈哌齐组.治疗前和治疗24周后分别进行血脂水平、简易精神状态量表(Mini-Mental State Examination,MMSE)、日常生活能力量表(activity of daily living,ADL)及全面衰退量表(global deterioration scale,GDS)的检测和评分,并进行比较.结果 联合用药组治疗前后的血脂水平差异有统计学意义(P0.05);每组治疗前后的MMSE、ADL及GDS评分比较,差异均有统计学意义(P<0.05);两组治疗后的各项评分比较,差异同样有统计学意义(P<0.05).结论 多奈哌齐联合阿托伐他汀能有效改善中、重

  2. Study of the combination of donepezil and compound haishe capsule in therapy of Alzheimer's disease%盐酸多奈哌齐和复方海蛇胶囊联合治疗阿尔茨海默病的研究

    Institute of Scientific and Technical Information of China (English)

    支胜利; 陈科; 潘新根; 任列; 吴杰

    2013-01-01

    Objective To investigate the improvement of cognitive function and behavioral abilities in Alzheimer's disease after treatment with donepezil and Compound Haishe Capsule. Methods 90 patients with Alzheimer's disease were randomized into 3 groups: patients in combined group (30 cases) were treated with the combination of donepezil and Compound Haishe Capsule, patients in donepezil group(30 cases) were treated with donepezil, and patients in control group(30 cases) without any medicine. MMSE and ADL scale were assessed in patients before treatment and 3 months after. Results The cognitive function and behavioral abilities improved significantly in the donepezil group and combined group compared with control group(P<0.01), and the improvement of cognitive function was even more in the combined group than donepezil group (P<0.01). The behavioral abilities were improved markedly in the donepezil group and combined group (P<0.01). Conclusion Congnitive function and behavioral abilities in patients with Alzheimers's disease improved markedly after treatment with the combination of donepezil and compound Haishe Capsule.%目的:探讨联合应用盐酸多奈哌齐和复方海蛇胶囊对阿尔茨海默病(AD)患者认知功能和行为能力的改善作用。方法收集AD患者90例,依就诊顺序分为3组,盐酸多奈哌齐和复方海蛇胶囊联合治疗组30例,盐酸多奈哌齐治疗组30例,正常对照组30例。3组患者分别在治疗前和治疗3个月后进行简易精神状态检查表(MMSE)、日常生活活动能力(ADL)量表的测评。结果盐酸多奈哌齐和复方海蛇胶囊联合治疗组患者治疗后认知功能、行为能力较盐酸多奈哌齐治疗组改善明显(P<0.01)。盐酸多奈哌齐和复方海蛇胶囊联合治疗组治疗后认知功能、行为能力较治疗前改善明显(P<0.01)。结论盐酸多奈哌齐和复方海蛇胶囊联合治疗对AD患者认知功能、行为能力有显著改善作用。

  3. Spotlight on anagrelide hydrochloride for the treatment of essential thrombocythemia

    Directory of Open Access Journals (Sweden)

    Sarma A

    2017-01-01

    Full Text Available Anita Sarma,1 Donal P Mclornan,1,2 Claire N Harrison2 1Department of Haematology, King’s College Hospital NHS Foundation Trust, 2Department of Haematology, Guy’s and St Thomas’ NHS Foundation Trust, London, UK Abstract: Anagrelide (ANA hydrochloride is an oral imidazoquinazoline registered as an orphan drug in Europe. It is indicated as a second-line agent for the reduction of thrombocytosis in high-risk essential thrombocythemia (ET in Europe and in any myeloproliferative neoplasm-associated thrombocytosis and for the amelioration of thrombo-hemorrhagic events in the context of myeloproliferative neoplasm in the USA and Japan. The compound has been in clinical use for almost two decades with approval in the European Union (EU for over a decade. The licensed indication encompasses the apparently specific action of the drug to reduce the platelet count; however, the precise mode of action of ANA remains unclear. Here, we review the current data from two large phase 3 studies, PT-1 and ANAHDRET, and a phase 4 post-approval observational study EXELS. All of these studies were conducted in the EU and therefore pertain to ET as the only licensed indication. Data from these studies suggest that ANA is on the whole as effective as the most commonly used agent hydroxycarbamide (HC. Although ANA, when compared to HC, appears to be slightly less effective in preventing arterial thrombosis and myelofibrotic transformation, it is associated with lower risk of venous thrombosis. Since the initial data from the PT-1 study, a caution has been recommended for the combined use of ANA and aspirin as this may provoke excess hemorrhage. ET is a clinically and biologically heterogeneous condition, and these biological variations may in part explain some of the clinical differences observed in various studies in response to specific treatments. No new toxicities of ANA have emerged in the past decade, which means that clinicians and patients can be reassured

  4. Pharmaceutical development of an amorphous solid dispersion formulation of elacridar hydrochloride for proof-of-concept clinical studies.

    Science.gov (United States)

    Sawicki, E; Schellens, J H M; Beijnen, J H; Nuijen, B

    2017-04-01

    A novel tablet formulation containing an amorphous solid dispersion (ASD) of elacridar hydrochloride was developed with the purpose to resolve the drug's low solubility in water and to conduct proof-of-concept clinical studies. Elacridar is highly demanded for proof-of-concept clinical trials that study the drug's suitability to boost brain penetration and bioavailability of numerous anticancer agents. Previously, clinical trials with elacridar were performed with a tablet containing elacridar hydrochloride. However, this tablet formulation resulted in poor and unpredictable absorption which was caused by the low aqueous solubility of elacridar hydrochloride. Twenty four different ASDs were produced and dissolution was compared to crystalline elacridar hydrochloride and a crystalline physical mixture. The formulation with highest dissolution was characterized for amorphicity. Subsequently, a tablet was developed and monitored for chemical/physical stability for 12 months at +15-25 °C, +2-8 °C and -20 °C. The ASD powder was composed of freeze dried elacridar hydrochloride-povidone K30-sodium dodecyl sulfate (1:6:1, w/w/w), appeared fully amorphous and resulted in complete dissolution whereas crystalline elacridar hydrochloride resulted in only 1% dissolution. The ASD tablets contained 25 mg elacridar hydrochloride and were stable for at least 12 months at -20 °C. The ASD tablet was considered feasible for proof-of-concept clinical studies and is now used as such.

  5. Carbon dioxide-water oxygen isotope fractionation factor using chlorine trifluoride and guanidine hydrochloride techniques

    Energy Technology Data Exchange (ETDEWEB)

    Dugan, J.P. Jr.; Borthwick, J.

    1986-12-01

    A new value for the CO/sub 2/-H/sub 2/O oxygen isotope fractionation factor of 1.04145 +/- 0.000 15 (2sigma) has been determined. The data have been normalized to the V-SMOW/V-SLAP scale and were obtained by measuring isotopic compositions with the guanidine hydrochloride and chlorine trifluoride techniques.

  6. 77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...

    Science.gov (United States)

    2012-09-04

    ...) Capsules, 0.5 Milligram (Base), Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness AGENCY... determined that ALOXI (palonosetron hydrochloride (HCl)) Capsules, 0.5 milligram (mg) (base), were not... abbreviated new drug applications (ANDAs) for palonosetron HCl capsules, 0.5 mg (base), if all other legal and...

  7. Biowaiver monographs for immediate release solid oral dosage forms: mefloquine hydrochloride.

    Science.gov (United States)

    Strauch, S; Jantratid, E; Dressman, J B; Junginger, H E; Kopp, S; Midha, K K; Shah, V P; Stavchansky, S; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release solid oral dosage forms containing mefloquine hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. The solubility and permeability data of mefloquine hydrochloride as well as its therapeutic use and therapeutic index, its pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability studies were taken into consideration. Mefloquine hydrochloride is not a highly soluble API. Since no data on permeability are available, it cannot be classified according to the Biopharmaceutics Classification System with certainty. Additionally, several studies in the literature failed to demonstrate BE of existing products. For these reasons, the biowaiver cannot be justified for the approval of new multisource drug products containing mefloquine hydrochloride. However, scale-up and postapproval changes (HHS-FDA SUPAC) levels 1 and 2 and most EU type I variations may be approvable without in vivo BE, using the dissolution tests described in these regulatory documents.

  8. An investigation on in vitro and in vivo antimicrobial properties of the antidepressant: amitriptyline hydrochloride

    Directory of Open Access Journals (Sweden)

    Anurup Mandal

    2010-10-01

    Full Text Available The antidepressant drug amitriptyline hydrochloride was obtained in a dry powder form and was screened against 253 strains of bacteria which included 72 Gram positive and 181 Gram negative bacteria and against 5 fungal strains. The minimum inhibitory concentration (MIC was determined by inoculating a loopful of an overnight peptone water culture of the organism on nutrient agar plates containing increasing concentrations of amitriptyline hydrochloride (0, 10 µg/mL, 25 µg/mL, 50 µg/mL, 100 µg/mL, 200 µg/mL. Amitriptyline hydrochloride exhibited significant action against both Gram positive and Gram negative bacteria at 25-200 µg/mL. In the in vivo studies it was seen that amitriptyline hydrochloride at a concentration of 25 µg/g and 30 µg/g body weight of mouse offered significant protection to Swiss strain of white mice when challenged with 50 median lethal dose (MLD of a virulent strain of Salmonella typhimurium NCTC 74. The in vivo data were highly significant (p<0.001 according to the chi-square test.

  9. Oral Midodrine Hydrochloride for Prevention of Orthostatic Hypotension during Early Mobilization after Hip Arthroplasty

    DEFF Research Database (Denmark)

    Jans, Øivind; Mehlsen, Jesper; Kjærsgaard-Andersen, Per

    2015-01-01

    or older and scheduled for total hip arthroplasty under spinal anesthesia to either 5 mg midodrine hydrochloride or placebo orally 1 h before mobilization at 6 and 24 h postoperatively. The primary outcome was the prevalence of OH (decrease in systolic or diastolic arterial pressures of > 20 or 10 mm...

  10. DENATURATION OF NATIVE AND DEGLYCOSYLATED α-GALACTOSIDASES FROM Penicillium canescens BY GUANIDINE HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Borzova N. V.

    2015-08-01

    Full Text Available The aim of this work was the study of native and galactosidases from Penicillium canescens under denaturing conditions caused by guanidine hydrochloride. Calculation of kinetics and constants of enzymes inactivation was carried out on using experimental kinetic curves of enzyme denaturation. We observed significant differences in the kinetics of inactivation of native and deglycosylated α-galactosidases from P. canescens caused by guanidine hydrochloride. Native enzyme was stable within the selected range of guanidine hydrochloride concentrations (from 0.1 to 3.0 M, retaining no less than 50% of the initial enzyme activity for 3 days. Deglycosylated enzyme preparations were less stable and they lost their activity within 5–30 minutes, when they were treated with guanidine hydrochloride in concentrations above 1 M. Dissociation rate constant of native and deglycosylated forms of the enzyme differed by 10 to 100 folds. It was shown that subunit interactions play a major role in the process of inactivation of the enzyme, and the carbohydrate component is essential for stabilizing of subunit bonds and maintaining conformational stability of the enzyme under denaturing conditions of chemical agents.

  11. Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

    Science.gov (United States)

    Uzunović, Alija; Vranić, Edina

    2007-08-01

    Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

  12. Efficacy of epinastine hydrochloride for antigen-provoked nasal symptoms in subjects with orchard grass pollinosis.

    Science.gov (United States)

    Gotoh, Minoru; Hashiguchi, Kazuhiro; Okubo, Kimihiro

    2011-03-01

    Among the gramineae species, orchard grass is a typical causative pollen that provokes seasonal rhinitis. The purpose of this study was to examine the protective efficacy of epinastine hydrochloride for signs and symptoms caused by repeated nasal provocation with discs containing orchard grass pollen. A single-dose, placebo-controlled, double-blind, crossover clinical study was conducted in subjects with orchard grass pollinosis. The pollen challenge was conducted with the use of provocation discs containing orchard grass pollen. Epinastine hydrochloride suppressed nasal symptoms caused by nasal provocation tests using orchard grass pollen discs. Among the nasal symptoms, the number of sneezing was significantly inhibited 30 minutes and 60 minutes after the administration of epinastine hydrochloride, as compared with placebo. There were no adverse reactions to the study drugs. Our results suggest that nasal provocation tests with discs containing orchard grass pollen is a useful method for evaluating the onset of action of antiallergic drugs. As compared with placebo, epinastine hydrochloride decreased early-phase sneezing and the total nasal symptom score after repeated nasal provocations with orchard grass pollen discs.

  13. 77 FR 14810 - Determination That DURANEST (Etidocaine Hydrochloride) Injection, 0.5%, and Five Other DURANEST...

    Science.gov (United States)

    2012-03-13

    ... contains the same active ingredient in the same strength and dosage form as the ``listed drug,'' which is a.... Drug Applicant date NDA 17-751...... DURANEST AstraZeneca August 30, 1976. (epinephrine Pharmaceutical.... (epinephrine Pharmaceutical. bitartrate; etidocaine hydrochloride) Injection 1.5%. The drug products listed...

  14. 1,2-Bis (pyridin-2-ylmethyl)sulfanyl ethane and its dimorphic hydrochloride salt

    DEFF Research Database (Denmark)

    Lennartson, A.; McKenzie, C. J.

    2011-01-01

    and are held together by C-H center dot center dot center dot N and C-H center dot center dot center dot S interactions, resulting in the formation of a three-dimensional network structure. In addition, two polymorphs of the corresponding hydrochloride salt, 2-[(2-[(pyridin-1-ium-2-ylmethyl...

  15. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  16. A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).

    Science.gov (United States)

    Villegas, Orlando; And Others

    This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…

  17. Minocycline hydrochloride as a soft sclerotizing agent for symptomatic simple renal and hepatic cysts.

    Science.gov (United States)

    Danza, F M; Falcione, M; Bordonaro, V; Infante, A; Paladini, A; Bonomo, L

    2017-01-01

    To present the results of our ten-year case series in simple hepatic and renal cysts sclerosis using minocycline hydrochloride as a sclerotizing agent, evaluating the effectiveness, the safety and the feasibility of this agent for percutaneous sclerotherapy for symptomatic cysts. We retrospectively evaluated our archives of patients treated (54 patients with 60 renal cysts, 21 patients with 24 hepatic cysts) for symptomatic abdominal cysts. These patients were treated with ultrasound guided drainage and subsequent minocycline hydrochloride instillation. In large or recurrent cysts, we repeated the treatment for the second time. The patients were evaluated at 6 and 12 months; some patients underwent later, additional examinations and we also reviewed these exams for any eventual long-term relapse. The percentage of sclerosis success was found to be 100% for hepatic cysts and 86% for renal cysts. We also found that minimal complications were encountered. Minocycline hydrochloride has proven to be an effective sclerotizing agent. In our cases, symptoms disappeared in 100% of patients with hepatic cysts and in 93% of patients with renal cysts. It is also a safe sclerotizing agent, as demonstrated by the few complications encountered. Percutaneous sclerosis with Minocycline hydrochloride is a very effective and promising nonsurgical treatment for patients with symptomatic simple cysts, and it can be performed without major complications.

  18. The Impact of Hydrochloride Heroin on Mental Flexibility, Abstract Reasoning, Impulsivity, and Attention

    Directory of Open Access Journals (Sweden)

    Zahra Alam Mehrjerdi

    2011-04-01

    Full Text Available Introduction: Drug addiction could lead to severe impairments in executive and neurocognitive functions but study on the impact of hydrochloride heroin on executive functions has remained in infancy in Iran. The aim of this study was to examine the relationship between addiction to hydrochloride heroin and executive functioning in several cognitive domains including mental flexibility, abstract reasoning, impulsivity, and attention. Methods: A total of 60 cases of young male addicts aged 18 to 21 were recruited from outpatient addiction clinics in Karaj city and were matched with 60 non-drug using controls. A test battery including the Wisconsin Card Sorting Test (WCST, Porteus Maze Test (PMQS, Serial Seven Subtraction Test (SSST, and Color Trails Test (CTT were administered respectively. Results: The patient group showed more problems in impulse control compared with the control group, while mental flexibility, abstract reasoning and attention were not affected. Discussion: The findings indicated that addiction to hydrochloride heroin had a negative effect on impulse control. This issue could reflect the role of impaired inhibitory control on drug-seeking behaviors and relapse. Special treatment programs must be tailored to control impulsivity among addicts to hydrochloride heroin during treatment.

  19. Solubility, dissolution rate and phase transition studies of ranitidine hydrochloride tautomeric forms.

    Science.gov (United States)

    Mirmehrabi, M; Rohani, S; Murthy, K S K; Radatus, B

    2004-09-10

    Understanding the polymorphic behavior of pharmaceutical solids during the crystallization process and further in post-processing units is crucial to meet medical and legal requirements. In this study, an analytical technique was developed for determining the composition of two solid forms of ranitidine hydrochloride using two peaks of Fourier transform infrared (FTIR) spectra without the need to grind the samples. Solubility studies of ranitidine hydrochloride showed that Form 2 has a higher solubility than Form 1. Solution-mediated transformation is very slow and occurs from Form 2 to Form 1 and not the reverse. No solid-solid transformation was observed due to grinding or compressing the pure samples of either forms and of a 50/50 wt.% mixture. Grinding was found to be a proper technique for increasing the bulk solid density of the ranitidine hydrochloride without the risk of solid-solid transformation. Dissolution rate found to be equally fast for both forms. The solubility data were modeled using the group contribution parameters and UNIversal QUAsi-Chemical (UNIQUAC) theory. There was a good agreement between the experimental solubility data of ranitidine hydrochloride and the results of UNIQUAC equation.

  20. SPECTROPHOTOMETRIC ESTIMATION OF BUSPIRONE HYDROCHLORIDE IN BULK AND ITS PHARMACEUTICAL FORMULATION

    Directory of Open Access Journals (Sweden)

    B.DHANDAPANI,

    2010-05-01

    Full Text Available Three simple, accurate, rapid and sensitive methods developed for the determination of buspirone hydrochloride in bulk drug and in its tablets by UV Spectroscopy (Method – A – Water as a Solvent, UV Spectroscopy (Method – B – Methanol as a Solvent, and Colorimetry (Method - C. In Method A buspirone hydrochloride estimated at 236 nm using distilled water as a solvent. The linearity was observed in the concentration range of 5 – 25 μg/ml with correlation co efficient of 0.9866. In Method B methanol used as a solvent. The linearity wasobserved in the concentration range of 10 – 50 μg/ml with correlation co efficient of 0.9905. In Method C buspirone hydrochloride is a colorless compound undergoes oxidation with 0.005M Potassium ermanganate Solution in the presence of 0.5M Sodium Hydroxide gives Pink color. The intensity of color directly proportional to theconcentration of buspirone hydrochloride and its found that intensity of color stable for 20mins and the absorbance was measured at 610 nm with different time intervals with the linearity range and correlation co -efficient of 10 – 50 μg/ml and 0.9924. The result of analysis for all the methods was validated statistically and by ecovery studies.

  1. Complexation of roxatidine acetate hydrochloride with beta-cyclodextrin: NMR spectroscopic study.

    Science.gov (United States)

    Ali, S M; Maheshwari, A; Asmat, F

    2004-08-01

    A NMR spectroscopic study of mixtures of varying ratios of roxatidine acetate hydrochloride (RAH) and beta-cyclodextrin (beta-CD) in D2O revealed the formation of a 1:1 inclusion compound. The aromatic ring of RAH selectively penetrates the beta-CD cavity in preference to the piperidine ring.

  2. Usefulness of vernakalant hydrochloride injection for rapid conversion of atrial fibrillation

    DEFF Research Database (Denmark)

    Pratt, Craig M.; Roy, Dennis; Torp-Pedersen, Christian

    2010-01-01

    The objective of the present study was to assess the safety and effectiveness of vernakalant hydrochloride injection (RSD1235), a novel antiarrhythmic drug, for the conversion of atrial fibrillation (AF) or atrial flutter to sinus rhythm (SR). Patients with either AF or atrial flutter were random...

  3. 1,2-Bis (pyridin-2-ylmethyl)sulfanyl ethane and its dimorphic hydrochloride salt

    DEFF Research Database (Denmark)

    Lennartson, A.; McKenzie, C. J.

    2011-01-01

    and are held together by C-H center dot center dot center dot N and C-H center dot center dot center dot S interactions, resulting in the formation of a three-dimensional network structure. In addition, two polymorphs of the corresponding hydrochloride salt, 2-[(2-[(pyridin-1-ium-2-ylmethyl...

  4. Interactions of biocidal guanidine hydrochloride polymer analogs with model membranes: a comparative biophysical study

    Institute of Scientific and Technical Information of China (English)

    Zhongxin Zhou; Anna Zheng; Jianjiang Zhong

    2011-01-01

    Four synthesized biocidal guanidine hydrochloride polymers with different alkyl chain length,including polyhexamethylene guanidine hydrochloride and its three new analogs,were used to investigate their interactions with phospholipids vesicles mimicking bacterial membrane.Characterization was conducted by using fluorescence dye leakage,isothermal titration calorimetry,and differential scanning calorimetry.The results showed that the gradually lengthened alkyl chain of the polymer increased the biocidal activity,accompanied with the increased dye leakage rate and the increased binding constant and energy change value of polymer-membrane interaction.The polymer-membrane interaction induced the change of pretransition and main phase transition (decreased temperature and increased width) of phospholipids vesicles,suggesting the conformational change in the phospholipids headgroups and disordering in the hydrophobic regions of lipid membranes.The above information revealed that the membrane disruption actions of guanidine hydrochloride polymers are the results of the polymer's strong binding to the phospholipids membrane and the subsequent perturbations of the polar headgroups and hydrophobic core region of the phospholipids membrane.The alkyl chain structure significantly affects the binding constant and energy change value of the polymer-membrane interactions and the perturbation extent of the phospholipids membrane,which lead to the different biocidal activity of the polymer analogs.This work provides important information about the membrane disruption action mechanism of biocidal guanidine hydrochloride polymers.

  5. Coupling of Carbon Dioxide with Epoxides Catalyzed by Amino Acid Hydrochloride Salts

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Using amino acid hydrochloride salt as a catalyst, the coupling reaction of CO2 with epoxides could proceed smoothly to give cyclic carbonates in very good yields and high selectivity. The reaction conditions such as the pressure of carbon dioxide, reaction temperature, time and catalyst loading were carefully investigated.

  6. Zilpaterol hydrochloride affects cellular muscle metabolism and lipid components of ten different muscles in feedlot heifers

    Science.gov (United States)

    This study determined if zilpaterol hydrochloride (ZH) altered muscle metabolism and lipid components of ten muscles. Crossbred heifers were either supplemented with ZH (n = 9) or not (Control; n = 10). Muscle tissue was collected (adductor femoris, biceps femoris, gluteus medius, infraspinatus, lat...

  7. Spectrophotometric and HPLC methods for simultaneous estimation of pseudoephedrine hydrochloride and loratadine from tablets

    Directory of Open Access Journals (Sweden)

    Singhvi I

    2006-01-01

    Full Text Available Two simple, accurate, economical and reproducible UV spectrophotometric and one HPLC method for simultaneous estimation of two-component drug mixture of pseudoephedrine hydrochloride and loratadine in combined tablet dosage form have been developed. The first developed method employs multiwavelength spectroscopy using seven mixed standards and 257.0 nm and 283.0 nm as two wavelengths for estimation. The second method involves first derivative spectroscopy using 308.6 nm and 263.0 nm as zero crossing points for pseudoephedrine hydrochloride and loratadine respectively. For both spectrophotometric methods, 0.2 M hydrochloric acid was used as solvent. Linearity was observed in concentration range of 0-40 mg/ml of loratadine and 0-800 mg/ml of pseudoephedrine hydrochloride. Developed HPLC method is reverse-phase chromatographic method using Inertsil C 18 column and methanol:ammonium acetate buffer in ratio of 80:20 pH 7.5 as mobile phase. Nimesulide was used as internal standard for HPLC method. For HPLC method, linearity was observed in concentration range of 0-200 mg/ml of loratadine and 100-2000 mg/ml of pseudoephedrine hydrochloride. Results of analysis were validated statistically and by recovery studies.

  8. Vernakalant hydrochloride for rapid conversion of atrial fibrillation - A phase 3, randomized, placebo-controlled trial

    DEFF Research Database (Denmark)

    Roy, D.; Pratt, C.M.; Torp-Pedersen, C.;

    2008-01-01

    Background - The present study assessed the efficacy and safety of vernakalant hydrochloride ( RSD1235), a novel compound, for the conversion of atrial fibrillation ( AF). Methods and Results - Patients were randomized in a 2: 1 ratio to receive vernakalant or placebo and were stratified by AF du...

  9. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma.

    Science.gov (United States)

    El-Saharty, Y S; Metwaly, F H; Refaat, M; El-Khateeb, S Z

    2006-06-07

    The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro-PTA) or ammonium reineckate (Dro-R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors, which were evaluated according to IUPAC recommendations, reveal a fast, stable and linear response for drotaverine over the concentration range 10(-5) to 10(-2) M with cationic slopes of 49.55 and 51.36 mV per concentration decade. The direct potentiometric determination of drotaverine hydrochloride using the proposed sensors gave average recoveries of 99.95+/-0.71 and 100.04+/-0.60 for Dro-PTA and Dro-R, respectively. The sensors are used for determination of drotaverine hydrochloride in tablets, in its mixture with caffeine and paracetamol and in plasma. Validation of the method shows suitability of the proposed sensors for use in the quality control assessment of drotaverine hydrochloride. The developed method was found to be simple, accurate and precise when compared with a reported HPLC method.

  10. Effect of carrier excipient and processing on stability of indorenate hydrochloride/excipient mixtures.

    Science.gov (United States)

    Villalobos-Hernández, J R; Villafuerte-Robles, L

    2001-11-01

    The purpose of this investigation was to determine the solid-state chemical stability of a model drug, indorenate hydrochloride, as a function of carrier excipient and mixing process. Physical mixtures and granules were prepared by tumble mixing and alcoholic granulation with and without binder. Stability of the mixtures was estimated using differential scanning calorimetry and isothermal degradation studies at 40, 50, and 60 degrees C. Average first-order degradation constants at 25 degrees C, extrapolated from isothermal studies, were much lower for indorenate hydrochloride after tumbling mixing with microcrystalline cellulose (3.45 x 10(-5) day-1) than those obtained after tumbling mixing with lactose (112.0 x 10(-5) day-1). Distribution of the drug on the excipient's surface, through granulation with and without Povidone, increased the average drug degradation rates in granules with microcrystalline cellulose (36.2 x 10(-5) day-1) as well as in granules with lactose (326 x 10(-5) day-1). Partially amorphous lactose (spray-dried lactose) showed higher average degradation rates (310.5 x 10(-5) day-1) than crystalline lactose (199.3 x 10(-5) day-1). It appears that the amorphous portion of the drug as well as that of reacting excipients play a major role in affecting the reaction rate. The calorimetric studies showed a strong solid-solid interaction between indorenate hydrochloride and lactose, suggesting chemical incompatibility. This strong solid-solid interaction was characterized by disappearance of typical transition peaks of lactose at temperatures above 200 degrees C and the development of new peaks at about 130-170 degrees C. No major changes in transition peaks were observed in mixtures of microcrystalline cellulose and indorenate hydrochloride, suggesting chemical compatibility. Calorimetric results allow the prediction of the chemical incompatibility between indorenate hydrochloride and lactose observed in isothermal degradation studies.

  11. Stability-Indicating TLC-densitometric determination of nebivolol hydrochloride in bulk and pharmaceutical dosage form.

    Science.gov (United States)

    Shirkhedkar, Atul A; Bugdane, Prasad M; Surana, Sanjay J

    2010-02-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for densitometric determination of nebivolol hydrochloride both as a bulk drug and in formulation was developed and validated as per the international conference on harmonization guidelines (ICH). The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of toluene-methanol-triethylamine (3.8:1.2:0.2 v/v/v). Densitometry analysis of nebivolol hydrochloride was carried out in the absorbance mode at 281 nm. The system was found to give compact spot for nebivolol hydrochloride (R(f) value of 0.33 +/- 0.02). The linear regression analysis data for the calibration plots showed good relationship with r(2)= 0.9994 +/- 0.0002 in the concentration range 500-3000 ng/spot. The mean value +/- SD of slope and intercept were 3.761 +/- 0.017 and 127.39 +/- 19.53 with respect to peak area. The limits of detection (LOD) and limit of quantitation (LOQ) were 63.10 ng/spot and 191.23 ng/ spot, respectively. Nebivolol hydrochloride was subjected to acid and alkali hydrolysis, oxidation, thermal degradation, and photodegradation. All the peaks of degradation products were well-resolved from the standard drug with significantly different R(f) values. Statistical analysis proves that the method is repeatable, selective and accurate for the estimation of said drug. The proposed developed HPTLC method can be applied for identification and quantitative determination of nebivolol hydrochloride in the bulk and pharmaceutical dosage form.

  12. Toxicity of naproxen sodium and its mixture with tramadol hydrochloride on fish early life stages.

    Science.gov (United States)

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Fiorino, Emma; Faggio, Caterina; Svobodova, Zdenka

    2017-08-31

    Pharmaceuticals occur in water bodies as a consequence of their incomplete removal during waste water treatment processes. The occurence of pharmaceuticals in surface waters as well as their possible impact on aquatic vertebrates have received considerable attention in recent years. However, there is still a lack of informations on the chronic effects of widely used drugs as well as their possible mixture toxicity on non-target aquatic vertebrates as well as their possible mixture toxicity. The aim of this study was to assess the effects of naproxen sodium on early life stages of fish and evaluate its mixture toxicity with tramadol hydrochloride, which was assessed in our earlier study as a single substance. Two embryo-larval toxicity tests with common carp (Cyprinus carpio) were performed according to the OECD guideline 210 (Fish, Early-life Stage Toxicity Test) in order to assess the subchronic toxicity of naproxen sodium and tramadol hydrochlorid-naproxen sodium mixture at the concentrations of 10; 50; 100 and 200 μg/L. These experiments were conducted for 32 days. The subchronic exposure to naproxen sodium and naproxen sodium and tramadol hydrochloride mixture had a strong effect on the early life stages of common carp. Hatching, developmental rate, morphology, histopathology and, in the case of the naproxen sodium and tramadol hydrochloride mixture, mortality were influenced. The bioindicators of oxidative stress were also influenced. The LOEC was determined at 10 μg/L for both naproxen sodium and naproxen sodium and tramadol hydrochloride mixture. Copyright © 2017. Published by Elsevier Ltd.

  13. The protecting effects and mechanism of betaine hydrochloride on hepatic ischemia-reperfusion injury in rats

    Institute of Scientific and Technical Information of China (English)

    XIN Xiao-ming; MA Lian-long; GAO Yong-feng; WANG Hao; WANG Xiao-dan; ZHU Yu-yun; GAO Yun-sheng

    2008-01-01

    Objective To study the protecting effects and mechanism of betaine hydrochloride on hepatic ischemia-reperfusion injury in rats. Methods Fourty SD rats were randomly divided into 5 groups (8 animals in each group) : sham-operated control group (A), hepatic ischemia-reperfusion group (B), 200 mg·kg-1 400 mg·kg-1 800 mg·kg-1 betaine hydrochloride + hepatic ischemia-reperfusion group (C、D、E). betaine hydrochloride was administered to animals byoral route in group C、D、E for 7 days before ischemia. A、B group was administered with NS. Made the animal model of part hepatic ischemia-reperfusion. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) levels in the blood and themalondialdehyde (MDA), superoxide dismutase (SOD), protein content in hepatic tissue were determined after the liver had been reperfused for 24 hours; the hepatic tissue was examined under lightmieroscope and the cell apoptosis was demonstrated with flow cytometry. Results ALT, AST, MDA increased and SOD decreased significantly in B group when compared those in the A group (P<0.05), Hepatic apoptosis was significantly increased; ALT, AST, MDA decreased and SOD increased significantly in betaine hydrochloride 200 mg·kg-1(C) group when compared those in the B group(P<0.05). Hepatic apoptosis was significantly lower, The histologic changes of the liver tissue under lightmicroscope in the C group was more easer than in the I/R group (B). Conclusions Betaine hydrochloride has the ability to scavenge oxygen free radical (OFR), reduce lipid peroxidation and inhibition of apoptosis. So it can protect the rats liver damaged by ischemia-reperfusion.

  14. Utility of 11C-donepezil and 11C-methionine for imaging of Staphylococcus aureus induced osteomyelitis in a juvenile porcine model: Comparison to autologous 111In-labelled leukocytes, 18F-FDG, and 99mTc-MPD

    DEFF Research Database (Denmark)

    Afzelius, Pia; Alstrup, Aage Kristian Olsen; Schønheyer, Henrik C.

    2016-01-01

    The aim of this study was to compare 11C-methionine and 11C-donepezil positron emission tomography (PET) with 111In-labeled leukocyte and 99mTc-MDP single-photon emission computed tomography (SPECT), and 18F-fluorodeoxyglucose (18F-FDG) PET to improve detection of osteomyelitis. The tracers...... a sequential scan protocol with 18F-FDG, 11C-methionine, 11C-donepezil, 99mTc- methylene diphosphonate (MDP), and 111In-labelled autologous leukocytes. This was followed by necropsy of the pigs and gross pathology, histopathology, and microbial examination. The pigs developed a total of 22 osteomyelitis...... lesions, 5 lesions characterized as abscesses and pulmonary abscesses in one pig. By comparing the 22 osteomyelitic lesions, 18F-FDG accumulated in 100%, 111In-leukocytes in 86%, 11C-methionine in 86%, 11C-donepezil in 63%, and 99mTc-MDP in none. Overall, 18F-FDG PET was slightly superior to 111In...

  15. Utility of 11C-methionine and 11C-donepezil for imaging of Staphylococcus aureus induced osteomyelitis in a juvenile porcine model: comparison to autologous 111In-labelled leukocytes, 99mTc-DPD, and 18F-FDG

    Science.gov (United States)

    Afzelius, Pia; Alstrup, Aage KO; Schønheyder, Henrik C; Borghammer, Per; Jensen, Svend B; Bender, Dirk; Nielsen, Ole L

    2016-01-01

    The aim of this study was to compare 11C-methionine and 11C-donepezil positron emission tomography (PET) with 111In-labeled leukocyte and 99mTc-DPD (Tc-99m 3,3-diphosphono-1,2-propanedicarboxylic acid) single-photon emission computed tomography (SPECT), and 18F-fluorodeoxyglucose (18F-FDG) PET to improve detection of osteomyelitis. The tracers’ diagnostic utility where tested in a juvenile porcine hematogenously induced osteomyelitis model comparable to osteomyelitis in children. Five 8-9 weeks old female domestic pigs were scanned seven days after intra-arterial inoculation in the right femoral artery with a porcine strain of Staphylococcus aureus. The sequential scan protocol included Computed Tomography, 11C-methionine and 11C-donepezil PET, 99mTc-DPD and 111In-labelled leukocytes scintigraphy, and 18F-FDG PET. This was followed by necropsy of the pigs and gross pathology, histopathology, and microbial examination. The pigs developed a total of 24 osteomyelitic lesions, 4 lesions characterized as contiguous abscesses and pulmonary abscesses (in two pigs). By comparing the 24 osteomyelitic lesions, 18F-FDG accumulated in 100%, 111In-leukocytes in 79%, 11C-methionine in 79%, 11C-donepezil in 58%, and 99mTc-DPD in none. Overall, 18F-FDG PET was superior to 111In-leukocyte SPECT and 11C-methionine in marking infectious lesions. PMID:28078182

  16. Utility of (11)C-methionine and (11)C-donepezil for imaging of Staphylococcus aureus induced osteomyelitis in a juvenile porcine model: comparison to autologous (111)In-labelled leukocytes, (99m) Tc-DPD, and (18)F-FDG.

    Science.gov (United States)

    Afzelius, Pia; Alstrup, Aage Ko; Schønheyder, Henrik C; Borghammer, Per; Jensen, Svend B; Bender, Dirk; Nielsen, Ole L

    2016-01-01

    The aim of this study was to compare (11)C-methionine and (11)C-donepezil positron emission tomography (PET) with (111)In-labeled leukocyte and (99m) Tc-DPD (Tc-99m 3,3-diphosphono-1,2-propanedicarboxylic acid) single-photon emission computed tomography (SPECT), and (18)F-fluorodeoxyglucose ((18)F-FDG) PET to improve detection of osteomyelitis. The tracers' diagnostic utility where tested in a juvenile porcine hematogenously induced osteomyelitis model comparable to osteomyelitis in children. Five 8-9 weeks old female domestic pigs were scanned seven days after intra-arterial inoculation in the right femoral artery with a porcine strain of Staphylococcus aureus. The sequential scan protocol included Computed Tomography, (11)C-methionine and (11)C-donepezil PET, (99m) Tc-DPD and (111)In-labelled leukocytes scintigraphy, and (18)F-FDG PET. This was followed by necropsy of the pigs and gross pathology, histopathology, and microbial examination. The pigs developed a total of 24 osteomyelitic lesions, 4 lesions characterized as contiguous abscesses and pulmonary abscesses (in two pigs). By comparing the 24 osteomyelitic lesions, (18)F-FDG accumulated in 100%, (111)In-leukocytes in 79%, (11)C-methionine in 79%, (11)C-donepezil in 58%, and (99m) Tc-DPD in none. Overall, (18)F-FDG PET was superior to (111)In-leukocyte SPECT and (11)C-methionine in marking infectious lesions.

  17. Multimorphologies of hydrochloride polyaniline synthesized by conventional and interfacial polymerization

    Science.gov (United States)

    Ferreira, André A.; Sanches, Edgar A.

    2017-09-01

    The aim of this paper is to analyze the structure and morphology of the hydrochloride Polyaniline Emeraldine-salt form (PANI-ES) synthesized by conventional (PANI-ES/C1 and PANI-ES/C2) and interfacial (PANI-ES/I1 and PANI/ES/I2) polymerization using HCl 1 M and 2 M. The X-ray diffraction patterns (XRD) of PANI-ES/I1 and PANI-ES/I2 have presented higher crystallinity. Furthermore, the peak located at 2θ = 18.3° has not been reported in scientific literature. PANI-ES/C1 and PANI-ES/C2 presented closed crystallinity percentage around 50 (±2) %, while PANI-ES/I1 and PANI-ES/I2 presented, respectively, 55 (±2) % and 63 (±2) % of crystallinity. However, PANI-ES/C2, PANI-ES/I1 and PANI-ES/I2 have presented larger ;b; unit cell parameter, from 8.9021 Å (PANI-ES/C1) to ∼16.2931 Å, due to the more efficient doping of the chloride ions. Fourier-transform Infrared Spectroscopy technique (FTIR) was useful to evaluate significant changes in the quinoid (Q) and benzenoid (B) bands: PANI-ES/C1 and PANI-ES/C2 presented the ratio Q/B, respectively, 0.4 and 0.6, indicating that the doping level by exposure to a higher dopant concentration has increased. An even more intense dopant action was verified in PANI-ES/I1 and PANI-ES/I2, presenting Q/B ratios of 0.7 and 0.9, respectively. These results reveal the more efficient doping level provided by the interfacial polymerization. Scanning Electron Microscopy (SEM) images showed that PANI-ES/C1 presented short nanofibers, while PANI-ES/C2 showed nanofibers length and diameter, respectively, around 61% and 13% higher than those found in PANI-ES/C1. However, PANI-ES/I1 and PANI-ES/I2 presented four different types of morphologies (nanoplates, nanorods, nanofibers and nanoflowers) due to the peculiarity of this polymerization method. The difference of length and diameter between PANI-ES/C1 and PANI-ES/I2 nanofibers reaches 64% and 52%, respectively. Thermogravimetric Analysis (TGA) showed that the event related to the dopant release

  18. Does yohimbine hydrochloride facilitate fear extinction in virtual reality treatment of fear of flying? A randomized placebo-controlled trial

    NARCIS (Netherlands)

    Meyerbroeker, K.; Powers, M.B.; van Stegeren, A.; Emmelkamp, P.M.G.

    2012-01-01

    BACKGROUND: Research suggests that yohimbine hydrochloride (YOH), a noradrenaline agonist, can facilitate fear extinction. It is thought that the mechanism of enhanced emotional memory is stimulated through elevated noradrenaline levels. This randomized placebo-controlled trial examined the

  19. Antioxidant and antimicrobial activity of Maillard reaction products from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems.

    Science.gov (United States)

    Wu, Shuping; Hu, Jiao; Wei, Liuting; Du, Yumin; Shi, Xiaowen; Zhang, Lina

    2014-04-01

    The structure, UV absorbance, browning intensity, fluorescence changes, antioxidant activity and antimicrobial assessment of Maillard reaction products (MRPs) derived from xylan with chitosan, chitooligomer, glucosamine hydrochloride and taurine model systems were evaluated. The results revealed that all MRPs had similar infrared spectra and molecular structures. MRPs from different model systems on the UV absorbance at 294 nm after heated 90 min and browning intensity at 420 nm showed the similar law: xylan-taurine > xylan-glucosamine hydrochloride > xylan-chitooligomer > xylan-chitosan, and the order of DPPH scavenging activity of MRPs was as follows: xylan-chitosan > xylan-chitooligomer > xylan-glucosamine hydrochloride > xylan-taurine, which revealed that the properties of MRPs were closely related to molecular weight of model systems. Moreover, the highest radical scavenging activity of MRPs from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems was 65.9%, 63.7%, 46.4% and 42.5%, respectively.

  20. 盐酸美金刚联合多奈哌齐治疗中、重度阿尔茨海默病的临床研究%Clinical research of memantine and donepezil on the treatment of moder-ate and severe Alzheimer ’s disease

    Institute of Scientific and Technical Information of China (English)

    糜屈; 第五永长

    2014-01-01

    Objective To discuss the effects and security of memantine and donepezil in the treatment of moderate to severe Alzheimer’s disease(AD). Methods Eighty-six AD patients were randomly divided into two groups, the obser-vation group was treated by memantine and donepezil, while the control group was treated by donepezil. The mini-mental state examination (MMSE), ADAS-cog, ADL, NPI were used to evaluate the clinical effects before and after treatment 24 weeks. Results The scores of ADAS-cog,ADL,NPI and MMSE were great significant(P0.05). Conclusion Both of the two groups have clinical effect on treatment of AD,but memantine and donepezil is better efficacy than donepezil in NPI, and they are all safe.%目的:探讨盐酸美金刚联合多奈哌齐治疗中、重度阿尔茨海默病(AD)的临床疗效及安全性。方法将86例AD 患者随机分为盐酸美金刚联合多奈哌齐组(实验组)和多奈哌齐组(对照组),在治疗前、治疗后24周末分别利用简易智能状态检查(MMSE)评分量表、AD评估量表-认知部分(ADAS-cog)、日常生活能力(ADL)量表和神经精神症状问卷(NPI)评估。结果实验组和对照组在治疗前后ADAS-cog、ADL和NPI及MMSE差异均有统计学意义(P0.05)。结论实验组和对照组对AD认知功能均有改善,但前者对NPI的改善更明显,两组治疗均具有良好的安全性。

  1. The curative effect of donepezil combined with mouse nerve growth factor on treating patients with Alzheimer’s disease%多奈哌齐联合鼠神经生长因子治疗阿尔茨海默病48例临床观察

    Institute of Scientific and Technical Information of China (English)

    李晴; 秦琴保

    2014-01-01

    目的:探讨多奈哌齐联合鼠神经生长因子联合治疗阿尔茨海默病的临床疗效。方法48例患者随机分为2组,分别接受多奈哌齐或多奈哌齐联合鼠神经生长因子治疗,总疗程12周,根据MMSE、ADL、ADAS‐cog量表评价2组治疗前后认知功能及生活能力变化。结果2组在日常生活能力及缓解认知功能的减退方面,显示有效;且联合治疗组较单纯使用多奈哌齐组在MMSE和ADL评分上改善更为显著。结论多奈哌齐联合鼠神经生长因子治疗能有效改善AD患者的认知、行为能力,并且具有良好安全性。%Objective To investigate the curative effect of donepezil combined with mouse nerve growth factor on treating patients with Alzheimer’s disease (AD). Methods 48 patients with AD were divided into donepezil group (treated with done‐pezil) and combined treatment group (treated with donepezil combined with mouse nerve growth factor ). 12 weeks after treat‐ment, the cognitive function and viability of two groups were evaluated by the Mini‐Mental State Examination (MMSE), Ac‐tivities of Daily Living(ADL),Alzheimer’s disease Assessment Scale cognitive subscale(ADAS‐cog). Results function and viability of two groups were significantly improved,and the MMSE and ADL score of combined treaTthmeencotggnriotiuvpe were better than these of donepezil group. Conclusion Donepezil combined with mouse nerve growth factor can effectively improve the cognitive function and viability of AD patients and have better safety.

  2. Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans

    Directory of Open Access Journals (Sweden)

    Min JS

    2016-09-01

    Full Text Available Jee Sun Min,1 Doyun Kim,1 Jung Bae Park,1 Hyunjin Heo,1 Soo Hyeon Bae,2 Jae Hong Seo,1 Euichaul Oh,1 Soo Kyung Bae1 1Integrated Research Institute of Pharmaceutical Sciences, College of Pharmacy, The Catholic University of Korea, Bucheon, 2Department of Pharmacology, College of Medicine, The Catholic University of Korea, Seocho-gu, Seoul, South Korea Background: Evaluating the potential risk of metabolic drug–drug interactions (DDIs is clinically important. Objective: To develop a physiologically based pharmacokinetic (PBPK model for sarpogrelate hydrochloride and its active metabolite, (R,S-1-{2-[2-(3-methoxyphenylethyl]-phenoxy}-3-(dimethylamino-2-propanol (M-1, in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine. Methods: The PBPK model was developed, incorporating the physicochemical and pharmacokinetic properties of sarpogrelate hydrochloride, and M-1 based on the findings from in vitro and in vivo studies. Subsequently, the model was verified by comparing the predicted concentration-time profiles and pharmacokinetic parameters of sarpogrelate and M-1 to the observed clinical data. Finally, the verified model was used to simulate clinical DDIs between sarpogrelate hydrochloride and sensitive CYP2D6 substrates. The predictive performance of the model was assessed by comparing predicted results to observed data after coadministering sarpogrelate hydrochloride and metoprolol. Results: The developed PBPK model accurately predicted sarpogrelate and M-1 plasma concentration profiles after single or multiple doses of sarpogrelate hydrochloride. The simulated ratios of area under the curve and maximum plasma concentration of metoprolol in the presence of sarpogrelate hydrochloride to baseline were in good agreement with the observed ratios. The predicted fold-increases in the area under the curve ratios of metoprolol

  3. A randomized, crossover design study of sevelamer carbonate powder and sevelamer hydrochloride tablets in chronic kidney disease patients on haemodialysis

    OpenAIRE

    Fan, Stanley; Ross, Calum; Mitra, Sandip; Kalra, Philip; Heaton, Jeremy; Hunter, John; Plone, Melissa; Pritchard, Nick

    2009-01-01

    Background. Sevelamer carbonate is an improved, buffered form of sevelamer hydrochloride developed for the treatment of hyperphosphataemia in CKD patients. Sevelamer carbonate formulated as a powder for oral suspension presents a novel, patient-friendly alternative to tablet phosphate binders. This study compared the safety and efficacy of sevelamer carbonate powder with sevelamer hydrochloride tablets in CKD patients on haemodialysis. Methods. This was a multi-centre, open-label, randomized,...

  4. The Clinical Effect Observation of Nimodipine and Donepezil for the Patients with Subcortical Ischemic Vascular Cognitive Impairment%尼莫地平与多奈哌齐治疗皮质下缺血性血管性认知功能障碍患者的临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    吴修信; 李立新; 黄志勇; 廖品君

    2012-01-01

    目的 比较尼莫地平与多奈哌齐对皮质下缺血性血管性认知障碍(SIVCI)患者的临床疗效.方法 将90例SIVCI患者,随机分成3组,每组30例患者入选,2个实验组,分别为盐酸多奈哌齐组(给予多奈哌齐5 mg,每日1次,睡前口服)、尼莫地平组(尼莫地平30 mg,每日3次口服)及对照组.3组均使用基础药物治疗,基础药物为阿司匹林肠溶片100 mg每日1次 ;银杏叶提取物片,40 mg,每日3次.观察各组患者用药24周后各组间MoCA评分变化.结果 与对照组比较,尼莫地平组患者服药24周后,MoCA评分提高1.60(P <0.05),有显著差异 ;与对照组比较,多奈哌齐组患者服药24周后MoCA评分提高4.26(P <0.0001),有显著差异.与尼莫地平组比较,多奈哌齐组患者服药24周后,MoCA评分平均提高2.51(P <0.0001),有显著差异.结论 多奈哌齐与尼莫地平,均可用于治疗SIVCI,多奈哌齐疗效优于尼莫地平.%Objective To compare nimodipine and donepezil for their clinical effect on the patients with subcortical ischemic vascular cognitive impairment (SIVCI). Methods 90 cases with SIVCI, randomly e-venly divided into 3 groups,are treated with aspirin(100 mg qd,po)and ginkgo biloba extract tablets(40 mg tid po) ;2 experimental groups,hydrochloric donepezil group(5 mg/d donepezil,qn, po) and nimodipine group (30 mg Nimodipine tid po). To observe the variety of MoCA score among groups after 24 weeks treatment. Results To compare with the control group, the MoCA score of nimodipine and donepezil group increases 1.60 (P<0. 05) ,4. 26 (P <0.0001 ) , repectively, with significant differences. To compare with the nimodipine group,the MoCA score of donepezil group increases 2. 51 (P <0. 0001) with significant differences. Conclusion Both nimodipine and donepezil can be used to treat the patients with subcortical ischemic vascular cognitive impairment( SIVCI). And donepezil is more effective than nimodipine on cognitive impairment.

  5. Berberine hydrochloride attenuates lipopolysaccharide-induced endometritis in mice by suppressing activation of NF-κB signal pathway.

    Science.gov (United States)

    Fu, Kaiqiang; Lv, Xiaopei; Li, Weishi; Wang, Yu; Li, Huatao; Tian, Wenru; Cao, Rongfeng

    2015-01-01

    Endometritis is a common disease in animal production and influences breeding all over the world. Berberine is one of the main alkaloids isolated from Rhizoma coptidis. Previous reports showed that berberine has anti-inflammatory potential. However, there have been a limited number of published reports on the anti-inflammatory effect of berberine hydrochloride on LPS-induced endometritis. The purpose of the present study was to investigate the effects of berberine hydrochloride on LPS-induced mouse endometritis. Berberine hydrochloride was administered intraperitoneally at 1h before and 12h after LPS induction. Then, a biopsy was performed, and uterine myeloperoxidase (MPO) and nitric oxide (NO) concentrations were determined. Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels in the uterus homogenate were measured by ELISA. The extent of IκB-α and P65 phosphorylation was detected by Western blot. The results showed that berberine hydrochloride significantly attenuated neutrophil infiltration, suppressed myeloperoxidase activity and decreased NO, TNF-αand IL-1βproduction. Furthermore, berberine hydrochloride inhibited the phosphorylation of the NF-κB p65 subunit and the degradation of its inhibitor, IκBα. These findings suggest that berberine hydrochloride exerts potent anti-inflammatory effects on LPS-induced mouse endometritis and might be a potential therapeutic agent for endometritis.

  6. Formulation and evaluation of hydroxyzine hydrochloride sustained release microspheres by ionotropic gelation technique using Carbopol 934P

    Directory of Open Access Journals (Sweden)

    Soumyadeep Ghosh

    2014-01-01

    Full Text Available Preparation of sustained release microspheres of hydroxyzine hydrochloride by ionotropic gelation technique and evaluation. Microspheres of hydroxyzine hydrochloride were prepared by ionotropic gelation method using sodium alginate, Carbopol 934P and calcium chloride. The powders were evaluated for their flow properties. Hydroxyzine hydrochloride microspheres were characterized by Fourier transform infrared and in vitro dissolution studies. The drug release study of hydroxyzine hydrochloride microspheres was evaluated using basket type dissolution test apparatus. The release rate of Hydroxyzine hydrochloride microspheres was studied for 12 h in pH 7.4 phosphate buffer media. From the five batches F5 batch showed good release behavior 91.08% of drug is released over 12 h, and r2 = 0.987 in zero-order kinetics. The microspheres were prepared without the use of organic solvents. Microspheres of hydroxyzine hydrochloride decrease the incidence of side effects and also improve patient compliance by reducing the number of dosing and by reducing the fluctuations of drug in the blood. This entire attributed attitude proves that microsphere technology from novel drug delivery can be very much effective in reducing dosage frequency, dose dumping, and better patient compliance and economical to the patient. In the future, natural, biodegradable polymers can be used to improve therapeutic efficacy of the drug and further minimizing side-effects.

  7. [A prospective multicenter randomized controlled clinical study on the efficacy and safety of Guaifenesin compound pseudoephedrine hydrochloride oral solution].

    Science.gov (United States)

    Lu, Quan

    2010-03-01

    To evaluate efficacy and safety of Guaifenesin compound pseudoephedrine hydrochloride oral solution for the treatment of cough, expectoration, nasal congestion and runny nose in children. This was a prospective multicenter randomized single-blind, parallel-controlled clinical study. A total of 10 centers participated in this study, the actual number of cases in line with the program was 412, of whom 205 cases in trial group were treated with Guaifenesin compound pseudoephedrine hydrochloride oral solution, and 207 cases in control group with ambroxol hydrochloride oral solution, treatment of both groups persisted for 7 days. The improvement rate of each single symptom and the combined symptoms and the overall effective rate were compared between the two groups. The adverse drug reactions and compliance were assessed as well. The treatment of both groups showed efficacy. Except sputum stickiness, the improvement of all symptoms in trial group was superior to that in the control group on the 3rd day after treatment (P Guaifenesin compound pseudoephedrine hydrochloride oral solution was 82.9% and the overall efficacy rate was 89.3%. Guaifenesin compound Pseudoephedrine hydrochloride oral solution had higher compliance and its adverse event rate was merely 0.92%. Guaifenesin compound pseudoephedrine hydrochloride oral solution showed significant efficacy and safety in children for treatment of cough, expectoration, nasal congestion and runny nose caused by common cold or acute tracheobronchitis.

  8. Spectrophotometric determination of procaine hydrochloride in pharmaceutical products using 1,2-naphthoquinone-4-sulfonic acid as the chromogenic reagent

    Science.gov (United States)

    Xu, Li Xiao; Shen, Yun Xiu; Wang, Huai You; Jiang, Ji Gang; Xiao, Yan

    2003-11-01

    Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with 1,2-naphthoquinone-4-sulfonic acid in pH 3.60 buffer solution to form a salmon pink compound, and its maximum absorption wavelength is at 484 nm, ɛ 484=5.22×10 3.The absorbance for procaine hydrochloride from 0.30 to 100 μg ml -1 obeys Beer's law. The linear regression equation of the calibration graph is C=19.23A-0.03, with a linear regression correlative coefficient is 0.9996, the detection limit is 0.28 μg ml -1; recovery is from 98.0 to 105.2%. Effects of pH, surfactant, organic solvent, foreign ions, and standing time on the determination of procaine hydrochloride have been examined. This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. The results obtained by this method agreed with those by the official method (dead-stop titration).

  9. Determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets by HPLC%HPLC法测定盐酸伊伐布雷定片含量

    Institute of Scientific and Technical Information of China (English)

    杨晓莉; 张琼; 李辉

    2012-01-01

    Objective To establish an HPLC method for the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets. Methods The column C18 Inertsil ODS-3(250 mm ×4. 6 mm,5 μm) was used. The mobile phase consisted of buffer phos-phate(pH7. 6)- acetonitrile(60 : 40) ,flow rate was 1. 0 mL o min-1 ,the detection wavelength was set at 286 nm,and the column temperature was 25 ℃. Results The linearity of peak area was good when the sample content was in the range of 2. 32-16. 25 μg(r= 0. 999 9). The average recovery was 101. 3% with RSD 1. 2%(n = 9). Conclusions The method is accurate,reliable and simple,and it can be used in the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets.%目的 建立HPLC法测定盐酸伊伐布雷定片的含量.方法 采用C18 Inertsil ODS-3(250 mm ×4.6 mm,5 μm)色谱柱,流动相为磷酸盐缓冲液(pH7.6)-乙腈(60∶40),流速为1.0 mL·min-1,检测波长为286 nm,柱温25 ℃.结果 盐酸伊伐布雷定线性范围为2.32~16.25 μg,峰面积与进样量线性关系良好(r=0.999 9);平均回收率为101.3%,其RSD为1.2% (n=9).结论 该方法准确、可靠、简便,适用于盐酸伊伐布雷定片的含量测定.

  10. Advanced structure-activity relationships applied to Mentha spicata L. subsp. spicata essential oil compounds as AChE and NMDA ligands, in comparison with donepezil, galantamine and memantine - new approach in brain disorders pharmacology.

    Science.gov (United States)

    Avram, Speranta; Maria, Mernea; Bagci, Eyup; Hritcu, Lucian; Borcan, Livia-Cristina; Mihailescu, Dan

    2017-01-13

    Alzheimer's disease (AD) therapy is based on several natural and synthetic compounds that act as acetylcholinesterase (AChE) and N-methyl-D-aspartate receptor (NMDA) ligands that have limited efficiency in relieving AD symptoms. Recent studies show that inhibitors isolated from Mentha spicata L. subsp. spicata are promising for AD therapy. We aimed to identify novel and more potent phytopharmaceutical compounds for AD treatment by taking into account the compounds from Mentha spicata L. subsp. spicata essential oil. We generated structure-activity relationship (SAR) models that predict the biological activities of 14 Mentha spicata L. subsp. spicata compounds on AChE and NMDA by comparing their molecular features with those of the three conventional ligands: donepezil, galantamine and memantine. The most relevant descriptors for predicting the biological activities of considered compounds are solvent accessible area and their subdivided, hydrophobicity, energy of frontier molecular orbitals and counts of the aromatic ring and rotatable bounds. 1,8-cineole, the main compound from Mentha spicata L. subsp. spicata essential oil, resulted to be similar with memantine and dissimilar with donepezil in respect to hidrophobicity (logP1,8-cineole=2.95, logPmemantine=2.81, logPdonepezil=4.11), the energy of LUMO (eLUMO1,8-cineole=3.01 eV, eLUMOmemantine=3.35 eV, eLUMOdonepezil=-0.35 eV) and the solvent accessible surface areas over all hydrophobic (SA_H1,8-cineole= 350 Å2, SA_Hmemantine= 358 Å2, SA_Hdonepezil= 655 Å2) or polar atoms (SA_P1,8-cineole= 4 Å2, SA_Pmemantine=10 Å2, SA_Pdonepezil=44.62 Å2). Our results point towards 1,8-cineole as a good candidate for NMDA antagonism, with a weaker AChE inhibitory effect. Our results may be useful in establishing new therapeutic strategies for neurological disorders.

  11. Preparation and characterisation of mucoadhesive nasal gel of venlafaxine hydrochloride for treatment of anxiety disorders

    Directory of Open Access Journals (Sweden)

    Shyamoshree Basu

    2012-01-01

    Full Text Available The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug.

  12. SIMULTANEOUS ESTIMATION & VALIDATION OF PARACETAMOL, PHENYLEPHRINE HYDROCHLORIDE AND CHLORPHENIRAMINE MALEATE IN TABLETS BY SPECTROPHOTOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    R. SAWANT, R. JOSHI, P. LANKE L. BHANGALE

    2013-09-01

    Full Text Available The present work describes two methods for simultaneous estimation of phenylephrine hydrochloride and chlorpheniramine maleate in pure and solid dosage forms. First method employs the application of simultaneous equation and second, is a multi-wavelength spectrophotometric analysis method. Both methods utilize 0.1N NaOH as solvent. Simultaneous equation develops using 256.8 nm, 236.8 nm and 222.4 nm as the max of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate respectively. Calibration curves were linear over the concentration ranges of 0-35 μg/mL for all drugs. The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation < 1 %, while being simple, cheap and less time consuming, and hence can be suitably applied for simultaneous determination of three drugs in laboratory prepared mixtures and in commercial tablet preparation.

  13. Electron paramagnetic resonance and FT-IR spectroscopic studies of glycine anhydride and betaine hydrochloride

    Science.gov (United States)

    Halim Başkan, M.; Kartal, Zeki; Aydın, Murat

    2015-12-01

    Gamma irradiated powders of glycine anhydride and betaine hydrochloride have been investigated at room temperature by electron paramagnetic resonance (EPR). In these compounds, the observed paramagnetic species were attributed to the R1 and R2 radicals, respectively. It was determined that the free electron interacted with environmental protons and 14N nucleus in both radicals. The EPR spectra of gamma irradiated powder samples remained unchanged at room temperature for two weeks after irradiation. Also, the Fourier Transform Infrared (FT-IR), FT-Raman and thermal analyses of both compounds were investigated. The functional groups in the molecular structures of glycine anhydride and betaine hydrochloride were identified by vibrational spectroscopies (FT-IR and FT-Raman).

  14. Double-blind study of benzydamine hydrochloride, a new treatment for sore throat.

    Science.gov (United States)

    Wethington, J F

    1985-01-01

    Forty-four patients with sore throat participated in a placebo-controlled, double-blind clinical trial of benzydamine hydrochloride administered as a gargle. After medical evaluation and throat culture, 21 patients were treated with a solution containing benzydamine and 23 patients with a placebo solution. Statistical analysis of scores from patients' diaries showed that benzydamine solution afforded significantly greater (P less than 0.001) relief of pain and dysphagia at 24 hours than did the placebo solution. Physician evaluations at 24 hours showed that the benzydamine solution had significantly greater effect than did placebo on hyperemia (P less than 0.004) and edema (P less than 0.005). Side effects were minimal and of no clinical significance. The findings indicate that benzydamine hydrochloride is safe and effective therapy for the signs and symptoms of sore throat.

  15. Development and Evaluation of Extended Release Formulation of Tramadol Hydrochloride Based on Osmotic Technology

    Directory of Open Access Journals (Sweden)

    Patel JB

    2013-05-01

    Full Text Available Extended release formulation of Tramadol Hydrochloride based on osmotic technology was developedand evaluated. Target release profile was selected and different variables were optimized to achieve it.Formulation variables such as osmotic agent, plasticizer and coating thickness of semi-permeablemembrane were found to markedly affect drug release. Tramadol hydrochloride release was directlyproportional to the level of osmogent and plasticizer but inversely proportional to the level of coatingthickness of semi-permeable membrane. Drug release from developed formulation was independent ofpH and agitation intensity but dependent on osmotic pressure of release media. The optimizedformulation was compared with marketed product CONTRAMAL SR and accelerated stability studywas also carried out for 6 months.

  16. Spectroscopic Study on Interaction of β-Cyclodextrin with Triprolidine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    ALI Syed Mashhood; ASMAT Fahmeena

    2006-01-01

    The complexation of triprolidine hydrochloride (TRP) and β-cyclodextrin (β-CD) in deuterium oxide was investigated by 400 MHz 1H NMR spectroscopy. The 800 MHz 2D ROESY data reveaed that two 1 : 1 and one 2: 1β-CD-TRP inclusion complexes were formed. Both aromatic moieties (p-tolyl and pyridyl ring) has entered into the β-CD cavity, confirming the existence of two different equilibria for 1: 1 inclusion complexes in which p-tolyl ring of the guest is more tightly held by the host cavity. The ROE intermolecular interactions provided the plausible structures of these 1: 1 and 2: 1 stoichiometric inclusion complexes of β-CD-triprolidine hydrochloride in solution.

  17. Esterification of pseudoephedrine hydrochloride by citric acid in a solid dose pharmaceutical preparation.

    Science.gov (United States)

    Goel, Alok; Zhao, Zhicheng; Sørensen, Dan; Zhou, Jay; Zhang, Fa

    2016-09-10

    Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40°C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary reaction in the presence of minor level of water at elevated temperature to generate three isomeric esters. The structures of the pseudoephedrine citric acid esters were elucidated using high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy (NMR). Occurrence of esterification in solid state, instead of amidation which is generally more favorable than esterification, is likely due to remaining HCl salt form of solid pseudoephedrine hydrochloride to protect its amino group from amidation with citric acid. In contrast, the esterification was not observed from solution reaction between PSE and citric acid.

  18. Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

    Science.gov (United States)

    Hathout, Rania M; Nasr, Maha

    2013-10-01

    Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride.

  19. Formulation and evaluation of bilayer tablet for bimodal release of venlafaxine hydrochloride

    OpenAIRE

    2015-01-01

    The aim of the present research was to develop a bilayer tablet of venlafaxine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore fenugreek mucilage (FNM) for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioadhesive polymers like hydroxy propyl methyl cellulose (HPMC), Carbopol, and Xanthan Gum. The formulations were evaluated for swelling Index, ex vivo bioadhesion, water uptake studies, in vit...

  20. Derivatives of benzimidazole: vasodilator activity of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride. Preliminary study.

    Science.gov (United States)

    Demenge, P; Carraz, G; Luu Duc, C; Silice, C

    1979-01-01

    The effects of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride (HBBPC) have been studied in the rabbit and rat. Most of these studies were performed comparatively with reference vasodilators and papaverine. HBBPC vasodilator activity is nearly the same as that of papaverine in the isolated rabbit ear. The characteristic of the vasoactive action of HBBPC seems to reside in its duration. The mechanism of action of HBBPC seems of peripheral type, that is to say it acts on the vascular smooth muscle.

  1. Pupil Dilation with Intracameral Epinephrine Hydrochloride during Phacoemulsification and Intraocular Lens Implantation

    Science.gov (United States)

    Yu, A-Yong; Guo, Hua; Wang, Qin-Mei; Bao, Fang-Jun; Huang, Jing-Hai

    2016-01-01

    Objective. To investigate mydriatic effect of intracamerally injected epinephrine hydrochloride during phacoemulsification and intraocular lens (IOL) implantation. Methods. Eighteen cataract patients for bilateral phacoemulsification were enrolled. To dilate pupil, one eye was randomly selected to receive intracamerally 1 mL epinephrine hydrochloride 0.001% for 1 minute after corneal incision (intracameral group), and the contralateral eye received 3 drops of compound tropicamide 0.5% and phenylephrine 0.5% at 5-minute intervals 30 minutes before surgery (topical group). Pupil diameters were measured before corneal incision, before ophthalmic viscoelastic device (OVD) injection, after OVD injection, before IOL implantation, and at the end of surgery. Results. At each time point, the mean pupil diameter in the intracameral group was 2.20 ± 0.08, 5.09 ± 0.20, 6.76 ± 0.19, 6.48 ± 0.18, and 5.97 ± 0.24 mm, respectively, and in the topical group it was 7.98 ± 0.15, 7.98 ± 0.15, 8.53 ± 0.14, 8.27 ± 0.16, and 7.93 ± 0.20 mm, respectively. The topical group consistently had larger mydriatic effects than the intracameral group (P < 0.05). The onset of mydriatic effect was rapid in the intracameral group. There was no difference in surgical performance or other parameters between groups. Conclusions. Intracameral epinephrine hydrochloride appears to be an alternative to the mydriatic modalities for phacoemulsification and IOL implantation. In comparison with topical mydriatics, intracameral epinephrine hydrochloride offers easier preoperative preparation, more rapid pupil dilation, and comparable surgical performance. PMID:26904274

  2. A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations

    OpenAIRE

    Badr, Jihan M.

    2013-01-01

    Background: Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. Materials and Method: In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Ha...

  3. Evaluation of gum damar as a novel microencapsulating material for ibuprofen and diltiazem hydrochloride

    OpenAIRE

    Morkhade D; Joshi S

    2007-01-01

    A natural gum, damar was investigated as a novel microencapsulating material for sustained drug delivery. Microparticles were prepared by oil-in-oil emulsion solvent evaporation method. Ibuprofen and diltiazem hydrochloride were used as model drugs. Microparticles were evaluated for particle size, encapsulation efficiency and in vitro drug release kinetics. Images of the microparticles were obtained by bright field microscopy. The effect of different gum:drug ratios and solubility of drug on ...

  4. DEVELOPMENT AND EVALUATION OF MICROBALLOONS OF PIOGLITAZONE HYDROCHLORIDE USING EUDRAGIT S-100

    OpenAIRE

    Nishant S. Gandhi et al.

    2012-01-01

    ABSTRACTKeywords:Pioglitazone hydrochloride,Eudragit S-100,Solvent diffusion evaporation,Floating microspheres,Polymer: Drug ratioCorrespondence to Author:Nishant GandhiOld Power House Road, Ramnagar, Gondia, Maharashtra, IndiaVarious approaches have been used to retain the dosage form in the stomach as a way of increasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems;...

  5. Ion activated in situ gel system for ophthalmic delivery of moxifloxacin hydrochloride

    OpenAIRE

    Mali, Mahesh N.; Ashok A. Hajare

    2010-01-01

    Rapid precorneal elimination of drug is a major limitation of conventional ophthalmic formulations. An ion activated in situ gel forming systems of an antibacterial agent moxifloxacin hydrochloride for instillation as drops into eye undergoing a sol to gel transition in the cul-de-sac was formulated. Sodium alginate was used as the gelling agent in combination with hydroxypropylmethyl cellulose. Formulations were evaluated for gelling capacity, pH, in vitro release, rheological study, Draize ...

  6. Investigation of olopatadine hydrochloride under stress conditions by hydrophilic interaction liquid chromatography

    Directory of Open Access Journals (Sweden)

    Maksić Jelena Đ.

    2016-01-01

    Full Text Available The purpose of the present research was to conduct stress degradation studies on the olopatadine hydrochloride, an antiallergic drug, using the hydrophilic interaction liquid chromatography (HILIC. HILIC requires the utilization of polar and moderately polar stationary phases and aqueous-organic mobile phase usually containing more than 70% of organic solvent. In this study, olopatadine hydrochloride was subjected to acid and base hydrolysis, oxidation and termolytic degradation in order to estimate its stability under different stress conditions recommended by ICHQ1A (R2 guideline. Degree of degradation was followed by HILIC method. The chromatographic conditions were: column Betasil Cyano (100 mm × 4.6 mm, 5 mm particle size, mobile phase consisted of acetonitrile and ammonium acetate 5 mM (pH adjusted to 4.50 in ratio 85:15 V/V, flow rate was 1 mL min-1, column temperature was set at 30°C and detection was performed at 257 nm. Results obtained for stress studies indicated that olopatadine hydrochloride underwent transformation under acidic and oxidative (30% w/v hydrogen peroxyde conditions showing high degree of degradation. Furthermore, it was found that olopatadine hydrochloride is relatively stable when exposed to thermal (60°C and basic (1 M NaOH conditions. Therewith, kinetics of degradation reaction was determined with an aim to define the corresponding reaction rate constants and half-lives. Firstly, the order of the reaction was evaluated experimentally using the integral method. Based on the calculated values of the correlation coefficients, it was shown that the acidic, basic and oxidative degradation are the second-order reaction. High stability under basic conditions was achieved on the basis of the great degradation half-life values. Also, it has been verified that acidic degradation is the fastest reaction. [Projekat Ministarstva nauke Republike Srbije, br. 172052

  7. Formulation and development of industry feasible proniosomal transdermal drug delivery system of granisetron hydrochloride

    OpenAIRE

    Bhushan Arun Patil; Prashant Keshav Puranik; Shankar Dadasaheb Pol; Prajakta Kalidas Khobragade; Pritee Shamrao Ramteke; Rajashree Gopal Palasakar; Nitiraj Ransing-Patil

    2015-01-01

    Proniosomes gel is semisolid liquid crystal products of nonionic surfactants, which converted into niosomes upon hydration. A proniosome based transdermal drug delivery system of granisetron hydrochloride (GRA HCL) developed by coacervation phase separation method. Formulation optimized by use of 3 2 full factorial design. Span 60 and cholesterol selected as independent variables, while entrapment efficiency (EE) and flux selected as dependent variables. Proniosomes evaluated for EE, in vitro...

  8. Development and In Vitro Characterization of Sustained Release Pellets of Venlafaxine Hydrochloride

    OpenAIRE

    P.REMYA; N. Damodharan; Dinesh Kumar, S.; V. Sowjanya

    2012-01-01

    The present study was undertaken with development and in-vitro characterization of sustained release pellets of venlafaxine hydrochloride by wruster process technique .which release the drug in sustained manner over a period of 20 hours. The different viscosity grades of polymers are HPMC-E6, Ethyl cellulose 7cps, MCC-101 were preparation of granules or pellets by wurster coating .The granules were prepared and evaluated for Angle of repose, bulk density, tapped density, cars index, moisture ...

  9. Effects of 1% cyclopentolate hydrochloride on anterior segment parameters obtained with Pentacam in young adults

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    Ceyhun Arici

    2014-08-01

    Full Text Available Purpose: To investigate the effects of topically applied 1% cyclopentolate hydrochloride on anterior segment parameters obtained with a Pentacam rotating Scheimpflug camera in healthy young adults. Methods: Anterior segment analyses of 25 eyes from 25 young adults (Group 1, before and after 45 min of 1% cyclopentolate hydrochloride application, were performed. For a control group (cycloplegia-free, Group 2, 24 eyes of 24 age- and sex-matched healthy cases were evaluated twice at 45 min intervals. The results obtained from the groups were compared statistically. Results: The mean ages of the groups were 23.04 ± 3.42 (range, 18-29 and 22.4 ± 2.05 (range, 18-27 years for Groups 1 and 2, respectively (p=0.259. In Group 1, measurements between the two analyses were significantly different for the values of anterior chamber depth (ACD, anterior chamber angle (ACA, and anterior chamber volume (ACV (p<0.05, whereas no statistical difference was found for the central corneal thickness (CCT and keratometry (K1, K2 measurements. In Group 2, none of these parameters were statistically different between the two analyses. Conclusions: Topically applied 1% cyclopentolate hydrochloride caused an increase in the ACD and ACV values, and a decrease in the ACA value. However, it had no significant effect on the CCT and keratometry measurements. It is important to consider these effects when using the Pentacam device on young adults with cycloplegia and when applying it for various reasons.

  10. The Efficacy of Levobupivacaine Hydrochloride-Dexamethasone Infiltration for Post-Tonsillectomy Pain in Adults.

    Science.gov (United States)

    Bayram, Ali; Doğan, Murat; Cihan, Celalettin; Karataş, Duran; Gökahmetoğlu, Günhan; Özcan, Ibrahim

    2015-10-01

    The aim of the study is to evaluate the efficacy of peritonsillar infiltration of a levobupivacaine hydrochloride and dexamethasone combination for post-tonsillectomy pain in adult patients. A total of 40 patients were included in this double-blind, randomized, and placebo-controlled study. The patients were equally randomized into 2 groups by means of sealed envelopes. The study group (SG) received peritonsillar levobupivacaine hydrochloride and dexamethasone infiltration and the control group (CG) received peritonsillar saline infiltration. Pain scores at the second, fourth, eighth, 12th, 16th, and 24th hours and the second to seventh days after operation were recorded by the patients in each group using a visual analog scale. Duration of surgery and the total amount of blood loss during the surgery were also recorded for each patient. All pain scores in the SG were lower than those in the CG; however, the difference was significant at the second, 12th, and 16th hours, and the second and third day (P fever, halitosis, and bleeding were similar between the 2 groups. Total amount of analgesic consumption in the SG was significantly lower than in the CG on each day of the week after tonsillectomy. Peritonsillar infiltration of a levobupivacaine hydrochloride and dexamethasone combination may provide pain reduction and decrease analgesic consumption in the postoperative period after adult tonsillectomy.

  11. Ultraviolet spectrophotometric method for analytical determination of mianserin hydrochloride in coated tablets and comparison with LC

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    Letícia Lenz Sfair

    2015-12-01

    Full Text Available abstract Ultraviolet spectrophotometric (UV and Liquid Chromatographic (LC methods for the determination of mianserin hydrochloride in pharmaceutical formulation were developed and validated. The various parameters, such as specificity, linearity, precision and accuracy were studied according to International Conference on Harmonization (ICH, 2005. For UV method, mianserin hydrochloride was determinate at 278 nm using HCl 0.1 M as the solvent. The response was linear in the concentration range of 20.0 - 140.0 µg/mL (r = 0.9998. Precision data evaluated by relative standard deviation was lower than 2%. The UV method was simple, rapid and low cost. Chromatographic analyses were performed in an Ace C18 column and the mobile phase was composed of methanol, 50 mM monobasic potassium phosphate buffer and 0.3% triethylamine solution adjusted to pH 7.0 with phosphoric acid 10% (85:15. LC method was specific, linear, precise, exact and robust. The results confirmed that the both methods are valid and useful to the routine quality control of mianserin hydrochloride in coated tablets. Statistical analysis by Student´s t-test showed no significant difference between the results obtained by UV and LC methods.

  12. Xylometazoline hydrochloride nasal spray combined with laser artificial nasolacrimal duct implantation for nasolacrimal duct obstruction

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    Xiao-Zhao Yang

    2017-02-01

    Full Text Available AIM: To study the role of xylometazoline hydrochloride nasal spray in combination therapy of nasolacrimal duct obstruction and to investigate the effect of nasal inflammation on nasolacrimal duct obstruction. METHODS: Totally 279 patients with nasolacrimal duct obstruction were collected, who received lacrimal passage irrigation, CT angiography for lacrimal passage and nasal endoscope before treated by lacrimal laser forming and artificial nasolacrimal duct implantation combined with xylometazoline hydrochloride nasal spray. In group A, 137 patients were treated with antibiotic eye drop and non-steroidal anti-inflammatory drugs after operations. In group B, 142 patients were treated with xylometazoline hydrochloride nasal spray besides the same treatment for group A. RESULTS:In the 279 patients 217(77.8%, in which 105 cases(76.6%were in group A and 112 cases(78.9%were in group B, were suffered with nasal inflammation, including nasal mucosal hyperemia, inferior turbinate hypertrophy, middle turbinate hypertrophy. At 3mo after the ducts were drawn, efficacy of group B was 95.8%, which was significant better than that of group A(86.1%, PCONCLUSION: Nasal inflammation was an important factor in the incidence of nasolacrimal duct obstruction, which shoud pay more attention in the process of diagnosis and treatment. Combination therapy could improve the cure rate of nasolacrimal duct obstruction.

  13. Guanidine hydrochloride embedded polyurethanes as antimicrobial and absorptive wound dressing membranes with promising cytocompatibility

    Energy Technology Data Exchange (ETDEWEB)

    Sahraro, Maryam; Yeganeh, Hamid, E-mail: h.yeganeh@ippi.ac.ir; Sorayya, Marziyeh

    2016-02-01

    Preparation and assessments of novel absorptive wound dressing materials with efficient antimicrobial activity as well as very good cytocompatibility were described in this work. An amine terminated poly(hexamethylene guanidine hydrochloride) was prepared and used as curing agent of different epoxy-terminated polyurethane prepolymers. The structures of prepared materials were elucidated by evaluation of their {sup 1}H NMR and FTIR spectra. The recorded tensile strength of membranes confirmed the excellent dimensional stability of the film type dressings even at fully hydrated conditions. Therefore, these dressings could protect the wound bed from external forces during the healing period. The structurally optimized dressing membranes could preserve the desired moist environment over the wounded area, as a result of their balanced equilibrium, water absorption and water vapor transmission rate. Therefore, a very good condition for stimulation of self-healing of wound bed was attained. Also, owing to the presence of guanidine hydrochloride moieties embedded into the structure of dressings, efficient antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans were detected. In vitro cytotoxicity assay of the prepared dressings revealed cytocompatibility of these materials against fibroblast cells. Therefore, they could support cell growth and proliferation at the wounded area. - Highlights: • New polyurethane wound dressings with guanidine hydrochloride based antimicrobials • Maintaining moist and warm wound environment for accelerating healing • Proper tensile strength of dressings even at fully hydrated state • Excellent biocompatibility index due to proper selection of starting materials.

  14. Effect of binders on 500mg metformin hydrochloride tablets produced by wet granulation

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    LUCIANA CATIA BLOCK

    2009-12-01

    Full Text Available Metformin hydrochloride (MH is an oral hypoglycemic agent and a high-dose drug that has poor flow and compression properties. In this study, the feasibility of developing adequate, low cost 500mg tablets of metformin hydrochloride by wet granulation was tested with several binders (Starch / PVP K30®; Starch 1500® /PVP K30®, PVP K30® and PVP K90® in a simple tablet press of the type used in small pharmaceutical laboratories. The drug powder was tested for ability to flow, by determining Carr’s Index (CI and the Hausner ratio (HR. Differential scanning calorimetry and thermogravimetric analysis were carried out on isolated MH and 1:1 (w/w binary mixtures with the excipients. The size distribution, friability, flow properties and drug content of the granules were analyzed, as were the hardness, friability, disintegration, dissolution and uniformity of the dosage form. The drug powder showed CI > 22% and HR > 1.25, characteristic of a poor flow powder, and no significant incompatibilities with the excipients. All the granules showed adequate flow properties and were suitable for pressing into tablets, all of which complied with pharmacopeial specifications. The starch /PVP K30® and starch 1500® /PVP K30® mixtures were best for producing 500 mg MH tablets. Keywords: Metformin hydrochloride. Tablets. Wet granulation. Binders.

  15. METHOD DEVELOPMENT AND VALIDATION OF DULOXETINE HYDROCHLORIDE IN BULK AND FORMULATION USING UV SPECTROPHOTOMETRIC METHOD

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    Kishore Methuku

    2012-06-01

    Full Text Available New, simple and cost effective UV-spectrophotometric method was developed for the estimation of Duloxetine hydrochloride in bulk formulations. Duloxetine hydrochloride was estimated at 290 nm in 20% Acetonitrie. Linearity range was found to be 10–50 μg ml–1 (regression equation: 0.017 + 0.016; r2 = 0.999. The apparent molar absorptivity was found to be 5.922×10-3 mol−1 cm−1 in 20% Acetonitrile. These methods were tested and validated for various parameters according to ICH guidelines and USP. The quantitation limits were found to be 0.2405 μg ml–1 and 0.7289 μg ml–1 in 20% Acetonitrile respectively. The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation < 2%, while being simple, cheap and less time consuming and can be suitably applied for the estimation of Duloxetine hydrochloride in different dosage forms and dissolution studies.

  16. FORMULATION AND EVALUATION OF TIZANIDINE HYDROCHLORIDE MICROSPHERES BY USING 32 FULL FACTORIAL DESIGNS

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    Adimoolam Senthil

    2011-09-01

    Full Text Available Tizanidine hydrochloride is a centrally acting α-2 adrenergic agonist muscle relaxant. In the present study an attempt has been made to formulate and evaluate tizanidine hydrochloride microspheres by using hydroxypropylmethylcellulose K4M and carboxymethyl cellulose as polymers. Tizanidine hydrochloride microspheres were prepared by simple emulsification phase separation technique using glutaraldehyde as a cross-linking agent. Twenty preliminary trial batches, B1-B20 batches of microspheres were prepared by using different volume (2 to 10 ml of glutaraldehyde as cross-linking agent, cross-linking time 1 to 4 hours and 3:1 ratio of polymer-to-drug with two different polymers. From these twenty batches of each polymer, the optimized formulation is selected based on the percentage of mucoadhesion, drug entrapment efficiency and sphericity of microspheres. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X1, and stirring speed (X2 on dependent variables percentage of mucoadhesion, drug entrapment efficiency, swelling index and in-vitro drug release study. The drug polymer compatibility studies were carried out using FTIR. Among the two polymers hydroxypropylmethyl cellulose K4M exhibited a high drug entrapment efficiency of 79% and a swelling index 1.260, percentage of mucoadhesive after 1hour was 80% and the drug release was also sustained for more than 10 hours.

  17. Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human.

    Science.gov (United States)

    Teramura, T; Watanabe, T; Higuchi, S; Hashimoto, K

    1995-11-01

    1. The pharmacokinetics of a new calcium antagonist barnidipine hydrochloride, a stereochemically pure enantiomer, was studied after intravenous and oral dosing to the rat and dog, and oral to man. 2. After intravenous dosing, plasma concentrations of barnidipine hydrochloride declined bi-exponentially with the terminal half-lives of 0.6 h in the rat and 4.1 h in the dog. The blood clearance was 5.2 l/h/kg in the rat and 3.3 l/h/kg in the dog, and was comparable with hepatic blood flow in both species. 3. After oral dosing, plasma concentrations of barnidipine hydrochloride peaked rapidly (0.3-0.4 h in the rat and dog, 1.0-1.6 h in man). Cmax and AUC rose non-linearly with increasing doses in all three species. 4. The absolute bioavailability was low (11-18% in the rat and 6-9% in the dog), suggesting a marked first-pass metabolism.

  18. Development of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres: Formulation optimization, characterization, and vitro release.

    Science.gov (United States)

    Lin, Qiang; Huo, Qing; Qin, Yingzhe; Zhao, Zhuo; Tao, Fengyun

    2017-01-02

    This study investigates the preparation of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres. This experiment investigates effects of the ratio of carboxymethyl chitosan and collagen blend, water to oil ratio, stirring speed, and other factors on the microsphere properties. The experiment had the following conditions: a 1:2 proportion of carboxymethyl chitosan and collagen, a 1:2 proportion of drugs and materials, a 5:1 proportion of oil phase and water phase, 0.5% of span80, a 600r/min stirring speed, 3 ml of a cross-linking agent, 3 h of cross-linking curing, 1.25 ± 0.05 mm diameter LTH microcapsules, a 54.08% envelop rate, and a 14.16% carrier rate. The microspheres release rate reached 66% within 1 h, then steadily released within 5 h in vitro. The experimental results showed that the ligustrazine hydrochloride microsphere production process was stable and exhibited a good release effect compared with other ligustrazine hydrochloride tablets and pills.

  19. FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF PIOGLITAZONE HYDROCHLORIDE USING A NATURAL POLYMER

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    Mobeen Mohd.

    2015-04-01

    Full Text Available The objective of the present investigation was to design a controlled release dosage form for a thiazolidinedione oral hypoglycemic drug i.e., pioglitazone hydrochloride employing a natural polymer. The present study was also aimed to increase the biological half-life by developing it in the form of sustained release microspheres. The present study aimed at employing a natural polymer in formulating the mucoadhesive microspheres and estimate its effect over the controlled release of the drug from the formulation. The microspheres of pioglitazone hydrochloride were prepared by employing sodium alginate as a cell forming polymer and by using a natural bio-adhesive polymer viz. goru gum in the ratios of 1:1, 1:1.5 and 1:2, by orifice ion gelation method with varying concentrations of calcium chloride. Six batches of microspheres (MS1 – MS6 were prepared. The microspheres were evaluated for various micromeritic properties and it was observed that all the batches exhibited free-flowing properties. Scanning electron microscopy results showed that the microspheres were almost spherical in shape and discrete. The FTIR results showed that there were no interactions between the drug and the excipients. The in vitro release profile indicated that all the batches of microspheres showed controlled and prolonged drug release over an extended period, with acceptable release kinetics. The work demonstrated that among all the formulations of microspheres, the microspheres of the formulation MS4 are promising candidates for the sustained release of pioglitazone hydrochloride.

  20. Pharmacokinetic study of benfotiamine and the bioavailability assessment compared to thiamine hydrochloride.

    Science.gov (United States)

    Xie, Feifan; Cheng, Zeneng; Li, Sanwang; Liu, Xingling; Guo, Xin; Yu, Peng; Gu, Zhenkun

    2014-06-01

    Benfotiamine is a lipid-soluble thiamine precursor which can transform to thiamine in vivo and subsequently be metabolized to thiamine monophosphate (TMP) and thiamine diphosphate (TDP). This study investigated the pharmacokinetic profiles of thiamine and its phosphorylated metabolites after single- and multiple-dose administration of benfotiamine in healthy Chinese volunteers, and assessed the bioavailability of orally benfotiamine administration compared to thiamine hydrochloride. In addition, concentration of hippuric acid in urine which is produced in the transformation process of benfotiamine was determined. The results showed that thiamine and its phosphorylated metabolites exhibited different pharmacokinetic characteristics in plasma, blood and erythrocyte, and one-compartment model provided the best fit for pharmacokinetic profiles of thiamine. The transformation process of benfotiamine to thiamine produced large amount of hippuric acid. No accumulation of hippuric acid was observed after multiple-dose of benfotiamine. Compared to thiamine hydrochloride, the bioavailability of thiamine in plasma and TDP in erythrocyte after oral administration of benfotiamine were 1147.3 ± 490.3% and 195.8 ± 33.8%, respectively. The absorption rate and extent of benfotiamine systemic availability of thiamine were significantly increased indicating higher bioavailability of thiamine from oral dose of benfotiamine compared to oral dose of thiamine hydrochloride.