کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2486875 | 1114396 | 2008 | 32 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Formulation and Statistical Optimization of a Novel Crosslinked Polymeric AntiâTuberculosis Drug Delivery System
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کلمات کلیدی
crosslinking - اتصال عرضیControlled release - انتشار کنترل شدهTuberculosis - بیماری سلMechanical properties - خواص مکانیکیTargeted drug delivery - دارورسانی هدفمندResponse surface methodology - روش سطح پاسخPolymeric drug delivery systems - سیستم های تحویل دارویی پلیمریMathematical model - مدل ریاضیPolyelectrolytes - پلی الکترولیت ها
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The crux of this research was the pragmatic investigation into the formulation of a reconstitutable multiparticulate antiâtuberculosis drug delivery system for facilitated administration for the attainment of segregated gastrointestinal (GI) delivery of rifampicin (RIF) and isoniazid (INH) in order to address issues of unacceptable RIF bioavailability on coadministration with INH. Ionotropically crosslinked polymeric enterospheres for delivery of INH to the small intestine were developed via a response surface methodology for the design and optimization of the formulation and processing variables. A 34 BoxâBehnken statistical design was constructed. The concentration of zinc sulfate saltingâout and crosslinking electrolyte, the crosslinking reaction time, the drying temperature (DT), and the concentration of triethyl citrate plasticizer were varied for determination of their effect on the molar amount of zinc (nZn) incorporated in the crosslinked enterosphere, drug entrapment efficiency (DEE), and mean dissolution time (MDT) at t2h in acidic media (0.1 M HCl). Complexometric determination of zinc cations (Zn2+) revealed that 23.70-287.89 mol of Zn2+ per mole of polymer were implicated in crosslink formation. DEE of 27.92% to 99.77% were obtained. Drug release at t2h ranged from 1.67% to 73.04%. The saltingâout and crosslinking agent significantly affected nZn (pâ=â0.034) and the DEE (pâ=â0.000), as did the concentration of plasticizer employed (pâ=â0.000 and 0.002, respectively). High DTs (>42.5°C) also significantly improved DEE (pâ=â0.029). ZnSO4 had a significant effect on the MDT (pâ=â0.000). A dry dispersible multiparticulate system incorporating the optimally designed INHâloaded enterospheres and RIF was developed. Bivariate regression analysis of UV spectrophotometric absorbance data allowed in vitro resolution of RIF and INH release at simulated gastric pH.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 97, Issue 6, June 2008, Pages 2176-2207
Journal: Journal of Pharmaceutical Sciences - Volume 97, Issue 6, June 2008, Pages 2176-2207
نویسندگان
Lisa Claire du Toit, Viness Pillay, Michael Paul Danckwerts, Clement Penny,