کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5820934 | 1557411 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Comparative studies on physicochemical stability of cyclosporine A-loaded amorphous solid dispersions
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کلمات کلیدی
DSCSqdSIRPXRDESIHPCAmorphous - آمورفCSA - ایالات مؤتلفهٔ آمریکاTem - این استANOVA - تحلیل واریانس Analysis of varianceone-way analysis of variance - تحلیل واریانس یک راههStability - ثباتRelative humidity - رطوبت نسبیCyclosporine A - سیکلوسپورینAselected ion recording - ضبط یون انتخاب شدهSolid solution - محلول جامدTransmission electron microscopy - میکروسکوپ الکترونی عبوریHydroxypropyl cellulose - هیدروکسی پروپیل سلولزPowder X-Ray Diffraction - پراش اشعه ایکسSolid dispersion - پراکندگی جامدDifferential scanning calorimetry - کالریمتری روبشی افتراقیelectrospray ionization - یونیزاسیون الکترو اسپری
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
The present study aimed to evaluate the physical stability on amorphous solid dispersion (SD) of cyclosporine A (CsA) employing hydroxypropyl cellulose (HPC). SD formulations (5-30% CsA) of CsA such wet-milled SD (WM/SD) and freeze-dried SD (FD/SD) were prepared, and both SD formulations were stored at 40 °C/75% relative humidity for 8 weeks. Transitions in morphology, dissolution behavior, crystallinity and thermal behavior of CsA were evaluated. There was at least 84-fold improvement in initial dissolution rate of SD formulations compared with that of amorphous CsA powder, although their dissolution rate was gradually decreased under accelerated conditions. In particular, aged FD/SD with a drug load of 30% exhibited highly limited dissolution as evidenced by 40% reduction of solubility after 8 weeks of storage. In contrast, aged WM/SD exhibited less reduction in dissolution rate compared with FD/SD. No significant changes were seen in crystallinity and thermal behavior after aging of SD formulations for 8 weeks; however, electron microscopic observations revealed aggregation of drug molecules/particles in the aged FD/SD, possibly leading to the reduced dissolution. From these findings, stability on CsA-loaded SD might be variable depending on the preparation methodology, and the wet-milling approach could be a viable option for preparing efficacious SD formulations with improved stability.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 426, Issues 1â2, 15 April 2012, Pages 302-306
Journal: International Journal of Pharmaceutics - Volume 426, Issues 1â2, 15 April 2012, Pages 302-306
نویسندگان
Hideyuki Sato, Yohei Kawabata, Kayo Yuminoki, Naofumi Hashimoto, Yukinori Yamauchi, Kumiko Ogawa, Takahiro Mizumoto, Shizuo Yamada, Satomi Onoue,