Enhancing dissolution, serum concentrations and hypoglycemic effect of glibenclamide using solvent deposition technique

Enhancing dissolution, serum concentrations and hypoglycemic effect of glibenclamide using solvent deposition technique


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دانشگاه علوم پزشکی تبریز
دانشگاه علوم پزشکی تبریز

نویسندگان: سیاوش دستمالچی

کلمات کلیدی: excipient; glibenclamide; glucose; microcrystalline cellulose; solvent

نشریه: 18341 , 2 , 8 , 2005

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نویسنده ثبت کننده مقاله سیاوش دستمالچی
مرحله جاری مقاله تایید نهایی
دانشکده/مرکز مربوطه مرکز تحقیقات بیوتکنولوژی(زیست فناوری)
کد مقاله 59352
عنوان فارسی مقاله Enhancing dissolution, serum concentrations and hypoglycemic effect of glibenclamide using solvent deposition technique
عنوان لاتین مقاله Enhancing dissolution, serum concentrations and hypoglycemic effect of glibenclamide using solvent deposition technique
ناشر 8
آیا مقاله از طرح تحقیقاتی و یا منتورشیپ استخراج شده است؟ بلی
عنوان نشریه (خارج از لیست فوق)
نوع مقاله Original Article
نحوه ایندکس شدن مقاله ایندکس شده سطح یک – ISI - Web of Science
آدرس لینک مقاله/ همایش در شبکه اینترنت https://www.ncbi.nlm.nih.gov/pubmed/16124928

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Purpose: Glibenclamide is practically insoluble in water and its GI absorption is limited by its dissolution rate. Therefore, to enhance the drug dissolution, serum concentrations and its hypoglycemic effects, it was formulated as solid dispersions and evaluated the relevant in vitro and in vivo parameters. Methods: The drug solid dispersions were prepared by solvent deposition technique using microcrystalline cellulose as the carrier in different ratios and their dissolution rates were compared to those of pure drug and its physical mixture with carrier. Drug serum concentrations and hypoglycemic effects in rabbits of pure drug, a physical mixture and the corresponding solid dispersion were investigated. In order to elucidate the observed in vitro and in vivo differences, IR spectroscopy and x-ray diffraction patterns of the formulations were studied. Results: The solid dispersion with the drug to carrier ratio of 1:19 showed the highest dissolution rate with the dissolution efficiency (DE) of 44.42 in comparison to pure drug (DE = 3.82), physical mixture (DE = 4.91) and other solid dispersions (DE between 13.85-39.94) and also produced higher drug serum concentrations (more than 4 times at 6th hour post dose) as well as enhanced hypoglycemic effects relative to pure drug and its corresponding physical mixture. Conclusions: Solvent deposition technique was proved an effective tool of increasing dissolution probably due to enhanced wettability and reduced drug particle size, which in turn led to enhance drug serum concentrations and its hypoglycemic effects. Strong quantitative correlations were established between dissolution parameter and parameters related to serum concentrations as well as hypoglycemic effects. Copyright © 1998 by the Canadian Society for Pharmaceutical Sciences.

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سیاوش دستمالچیاول

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