S. EL QOUATLI; R. T. NGONO; R. NAJIH; A. CHTAINI
A eugenol polymer immobilized electrode was developed for the assay of the carbocysteine compound. The electrochemical sensor was made by in situ electropolymerization of eugenol at titanium electrode. Cyclic voltamperometry at prepared electrode permitted to point out a reversible pattern for carbocysteine electrooxidation.
S. EL QOUATLI
Full Text Available A eugenol polymer immobilized electrode was developed for the assay of the carbocysteine compound. The electrochemical sensor was made by in situ electropolymerization of eugenol at titanium electrode. Cyclic voltamperometry at prepared electrode permitted to point out a reversible pattern for carbocysteine electrooxidation.
Full Text Available This study aimed to examine the effects of carbocysteine in OSAS patients.A total of 40 patients with moderate to severe obstructive sleep apnea syndrome (OSAS were randomly divided into two groups. One group was treated with 1500 mg carbocysteine daily, and the other was treated with continuous positive airway pressure (CPAP at night. Before treatment and after 6 weeks of treatment, all patients underwent polysomnography and completed questionnaires. Treatment compliance was compared between the two groups. Plasma was collected for various biochemical analyses. Endothelial function was assessed with ultrasound in the carbocysteine group.The proportion of patients who fulfilled the criteria for good compliance was higher in the carbocysteine group (n = 17 than in the CPAP group (n = 11; 100% vs. 64.7%. Compared with baseline values, the carbocysteine group showed significant improvement in their Epworth Sleepiness Scale score (10.18 ± 4.28 vs. 6.82 ± 3.66; P ≤ 0.01, apnea-hypopnea index (55.34 ± 25.03 vs. 47.56 ± 27.32; P ≤ 0.01, time and percentage of 90% oxygen desaturation (12.66 (2.81; 50.01 vs. 8.9 (1.41; 39.71; P ≤ 0.01, and lowest oxygen saturation level (65.88 ± 14.86 vs. 70.41 ± 14.34; P ≤ 0.01. Similar changes were also observed in the CPAP group. The CPAP group also showed a decreased oxygen desaturation index and a significant increase in the mean oxygen saturation after treatment, but these increases were not observed in the carbocysteine group. Snoring volume parameters, such as the power spectral density, were significantly reduced in both groups after the treatments. The plasma malondialdehyde level decreased and the superoxide dismutase and nitric oxide levels increased in both groups. The endothelin-1 level decreased in the CPAP group but did not significantly change in the carbocysteine group. Ultrasonography showed that the intima-media thickness decreased (0.71 ± 0.15 vs. 0.66 ± 0.15; P ≤ 0.05 but that flow
Manivannan, M.; Rajeshwaran, K.; Govindhan, R.; Karthikeyan, B.
Carbocysteine or carbocisteine having the empirical formula C5H9NO4S,is one of the most therapeutically prescribed expectorant, sold under the brand name viz., Mucodyne (UK and India), Rhinathiol and Mucolite. In pediatric respiratory pathology, it can relieve the symptoms of obstructive pulmonary disease (COPD) and bronchiectasis. On the consideration of its extensive pharmaceutical usage and medicinal value, we have investigated its chemical structure and composition by employing various spectral techniques like 1H, 13C NMR, FT-IR,Raman, UV-Visible spectroscopy and powder X-ray diffraction method. Density Functional Theoretical (DFT) studies on its electronic structure is also carried out. Drug docking studies were carried out to ascertain the nature of molecular interaction with the biological protein system. Furthermore theoretical Raman spectrum of this molecule has been computed and compared with the experimental Raman spectrum. The forbidden energy gap between its frontier molecular orbitals, viz., HOMO-LUMO is calculated and correlated with its observed λmax value. Atomic orbitals which are mainly contributes to the frontier molecular orbitals were identified. Molecular electrostatic potential diagram has been mapped to explain its chemical activity. Based on the results, a suitable mechanism of its protein binding mode and drug action has been discussed.
Josélia Larger Manfio
Full Text Available A carbocisteína é um agente mucolítico utilizado como adjuvante no tratamento de infecções do trato respiratório. A qualidade, segurança e eficácia do medicamento durante o seu prazo de validade são responsabilidades da indústria farmacêutica. A validade pode ser determinada através de estudos de estabilidade acelerados, nos quais fatores extrínsecos provocam a degradação do produto. De acordo com Arrhenius, existe uma relação entre temperatura e cinética química. Desta forma, amostras do produto foram expostas a condições drásticas: 40, 50, 60 e 70 ºC. O método de doseamento do xarope de carbocisteína foi validado podendo ser aplicado nas avaliações de rotina do controle de qualidade e no estudo de estabilidade deste produto. O prazo de validade proposto para o xarope de carbocisteína, calculado através da equação de Arrhenius, para a temperatura de 25 ºC foi de 240,9 dias. No entanto, foi observada diferença entre o prazo proposto e a validade usualmente praticada para este produto. Este estudo, ainda, demonstrou a presença de picos endógenos, que precisam ser melhor estudados a fim de se confirmar a presença de produtos de degradação.Carbocysteine is a mucolytic agent in adjunctive therapy of respiratory tract infections. The pharmaceutical industry is responsible for quality, safety and efficiency of the product during its shelf life. Shelf life can be determinated through an accelerated stability study where the degradation of the drug is managed with the extrinsic factors. According to Arrhenius, there is a relationship between temperature and chemical kinetic, so, the samples were exposed to drastic conditions at 40, 50, 60 and 70 ºC. The syrup assay method has been validated and it may be applied to analysis of carbocysteine syrup in routine quality control and stability studies. Through Arrhenius equation the proposed shelf life of carbocysteine syrup was 240.9 days when the dosage form is stored
Mantovani, Giovanni; Madeddu, Clelia; Macciò, Antonio; Gramignano, Giulia; Lusso, Maria Rita; Massa, Elena; Astara, Giorgio; Serpe, Roberto
Cancer-related anorexia/cachexia syndrome and oxidative stress play a key role in the progression and outcome of neoplastic disease. On the basis of our previously published studies and clinical experience, we have developed an innovative approach consisting of diet with high polyphenol content (400 mg), p.o. pharmaconutritional support enriched with n - 3 fatty acids (eicosapentaenoic acid and docosahexaenoic acid) 2 cans (237 mL each) per day, medroxiprogesterone acetate 500 mg/d, antioxidant treatment with alpha-lipoic acid 300 mg/d plus carbocysteine lysine salt 2.7 g/d plus vitamin E 400 mg/d plus vitamin A 30,000 IU/d plus vitamin C 500 mg/d, and selective cyclooxygenase-2 inhibitor Celecoxib 200 mg/d. The treatment is administered for 16 weeks. The following variables are evaluated: (a) clinical variables (stage and Eastern Cooperative Oncology Group performance status); (b) nutritional variables (lean body mass, appetite, and resting energy expenditure); (c) laboratory variables (serum levels of proinflammatory cytokines, C-reactive protein, and leptin and blood levels of reactive oxygen species and antioxidant enzymes); and (d) quality of life variables (European Organization for Research and Treatment of Cancer QLQ-C30, EQ-5Dindex, and EQ-5DVAS). A phase II nonrandomized study has been designed to enroll 40 patients with advanced cancer at different sites with symptoms of cancer-related anorexia/cachexia syndrome and oxidative stress. As of January 2004, 28 patients have been enrolled: 25 patients were evaluable and 14 of them have completed the treatment (20 patients have completed 2 months of treatment). As for clinical response, five patients improved, three patients remained unchanged, and six patients worsened. The Eastern Cooperative Oncology Group performance status (grade) 1 remained unchanged. As for nutritional/functional variables, the lean body mass increased significantly at 2 and 4 months. As for laboratory variables, reactive oxygen species
A phase II study with antioxidants, both in the diet and supplemented, pharmaconutritional support, progestagen, and anti-cyclooxygenase-2 showing efficacy and safety in patients with cancer-related anorexia/cachexia and oxidative stress.
Mantovani, Giovanni; Macciò, Antonio; Madeddu, Clelia; Gramignano, Giulia; Lusso, Maria Rita; Serpe, Roberto; Massa, Elena; Astara, Giorgio; Deiana, Laura
To test the efficacy and safety of an integrated treatment based on a pharmaconutritional support, antioxidants, and drugs, all given orally, in a population of advanced cancer patients with cancer-related anorexia/cachexia and oxidative stress. An open early-phase II study was designed according to the Simon two-stage design. The integrated treatment consisted of diet with high polyphenols content (400 mg), antioxidant treatment (300 mg/d alpha-lipoic acid + 2.7 g/d carbocysteine lysine salt + 400 mg/d vitamin E + 30,000 IU/d vitamin A + 500 mg/d vitamin C), and pharmaconutritional support enriched with 2 cans per day (n-3)-PUFA (eicosapentaenoic acid and docosahexaenoic acid), 500 mg/d medroxyprogesterone acetate, and 200 mg/d selective cyclooxygenase-2 inhibitor celecoxib. The treatment duration was 4 months. The following variables were evaluated: (a) clinical (Eastern Cooperative Oncology Group performance status); (b) nutritional [lean body mass (LBM), appetite, and resting energy expenditure]; (c) laboratory [proinflammatory cytokines and leptin, reactive oxygen species (ROS) and antioxidant enzymes]; (d) quality of life (European Organization for Research and Treatment of Cancer QLQ-C30, Euro QL-5D, and MFSI-SF). From July 2002 to January 2005, 44 patients were enrolled. Of these, 39 completed the treatment and were assessable. Body weight increased significantly from baseline as did LBM and appetite. There was an important decrease of proinflammatory cytokines interleukin-6 (IL-6) and tumor necrosis factor-alpha, and a negative relationship worthy of note was only found between LBM and IL-6 changes. As for quality of life evaluation, there was a marked improvement in the European Organization for Research and Treatment of Cancer QLQ-C30, Euro QL-5D(VAS), and multidimensional fatigue symptom inventory-short form scores. At the end of the study, 22 of the 39 patients were "responders" or "high responders." The minimum required was 21; therefore, the