کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2482394 | 1556265 | 2008 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Gamma irradiated micro system for long-term parenteral contraception: An alternative to synthetic polymers
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
An injectable system of levonorgestrel (LNG) was developed using biodegradable polymer of natural origin. The parenteral system was optimized for particle size and higher drug loading. The microparticulate system was characterised by scanning electron microscopy, encapsulation efficiency, moisture content, IR, DSC, XRD, residual solvent content, sterility testing, test of abnormal toxicity and test for pyrogens. The microparticles were sterilised by gamma irradiation (2.5 Mrad). The system was injected intramuscularly in rabbits and the blood levels of LNG were determined using radioimmunoassay technique. An optimized drug to polymer ratio of 0.3-1.0 (w/w ratio) gave improved drug loading of about 52%. In vivo studies in rabbits showed that the drug was released in a sustained manner for a period of 1 month. The AUC0-t was found to be 9363.6 ± 2340 pg/mL dayâ1 with MRT calculated to be about 16 days and Kel of 0.01 dayâ1. LNG levels were maintained between 200 and 400 pg/mL. In vivo release exhibited an initial burst effect which was not observed in the in vitro dissolution. This promising “Progestin-only” long-term contraceptive with improved user compliance is an alternative to the synthetic expensive polymeric carriers.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 35, Issue 4, 15 November 2008, Pages 307-317
Journal: European Journal of Pharmaceutical Sciences - Volume 35, Issue 4, 15 November 2008, Pages 307-317
نویسندگان
S. Puthli, P. Vavia,