دورية أكاديمية
Trimetazidine Dihydrochloride Pulsatile-Release Tablets for the Treatment of Morning Anginal Symptoms: Dual Optimization, Characterization and Pharmacokinetic Evaluation.
| العنوان: | Trimetazidine Dihydrochloride Pulsatile-Release Tablets for the Treatment of Morning Anginal Symptoms: Dual Optimization, Characterization and Pharmacokinetic Evaluation. |
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| المؤلفون: | Othman AI; Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Egyptian Russian University, Badr City, Po. Box 11829, Cairo, Egypt., Amin MM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Po. Box 11562, Cairo, Egypt., Abu-Elyazid SK; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Po. Box 11651, Cairo, Egypt., Abdelbary GA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Po. Box 11562, Cairo, Egypt. |
| المصدر: | Current drug delivery [Curr Drug Deliv] 2021; Vol. 18 (8), pp. 1182-1196. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Bentham Science Publishers Country of Publication: United Arab Emirates NLM ID: 101208455 Publication Model: Print Cited Medium: Internet ISSN: 1875-5704 (Electronic) Linking ISSN: 15672018 NLM ISO Abbreviation: Curr Drug Deliv Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Saif Zone, Sharjah, U.A.E. ; San Francisco, CA : Bentham Science Publishers, c2004- |
| مواضيع طبية MeSH: | Trimetazidine*, Animals ; Delayed-Action Preparations ; Drug Liberation ; Hypromellose Derivatives ; Rabbits ; Tablets |
| مستخلص: | Objective: This research work aimed to target the early morning peak symptoms of chronic stable angina through formulating antianginal drug, Trimetazidine (TMZ) in a pulsatile-release tablet. Methods: The core formulae were optimized using 22 .31 factorial design to minimize disintegration time (DT) and maximize drug release after 5 minutes (Q5min). Different ratios of Eudragit S100 and Eudragit L100 were used as a coating mixture for the selected core with or without a second coating layer of hydroxypropyl methylcellulose (HPMC E50). The different formulation variables were statistically optimized for their effect on lag time and drug release after 7 hours (Q7h) using BoxBehnken design. The optimized formula (PO) was subjected to stability study and pharmacokinetic assessment on New Zealand rabbits. Results: The optimal core (F8) was found to have 1.76 min disintegration time and 61.45% Q5min PO showed a lag time of 6.17 h with 94.80% Q7h and retained good stability over three months. The pharmacokinetics study confirmed the pulsatile-release pattern with Cmax of 206.19 ng/ml at 5.33 h (Tmax) and 95.85% relative bioavailability compared to TMZ solution. Conclusion: Overall pulsatile-release tablets of TMZ successfully released the drug after a desirable lag time, providing a promising approach for early morning anginal symptoms relief. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.) |
| فهرسة مساهمة: | Keywords: Box-Behnken; Trimetazidine dihydrochloride; chronic stable angina; dual optimization; in-vivo pharmacokinetic study.; pulsatile release |
| المشرفين على المادة: | 0 (Delayed-Action Preparations) 0 (Tablets) 3NXW29V3WO (Hypromellose Derivatives) N9A0A0R9S8 (Trimetazidine) |
| تواريخ الأحداث: | Date Created: 20210215 Date Completed: 20211217 Latest Revision: 20211217 |
| رمز التحديث: | 20231215 |
| DOI: | 10.2174/1567201818666210212095932 |
| PMID: | 33583377 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 1875-5704 |
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| DOI: | 10.2174/1567201818666210212095932 |