کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485777 | 1114366 | 2012 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Evaluation of Drug Supersaturation by Thermodynamic and Kinetic Approaches for the Prediction of Oral Absorbability in Amorphous Pharmaceuticals
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Evaluation of Drug Supersaturation by Thermodynamic and Kinetic Approaches for the Prediction of Oral Absorbability in Amorphous Pharmaceuticals Evaluation of Drug Supersaturation by Thermodynamic and Kinetic Approaches for the Prediction of Oral Absorbability in Amorphous Pharmaceuticals](/preview/png/2485777.png)
چکیده انگلیسی
Supersaturation behavior of model drugs, danazol, griseofulvin, itraconazole, vemurafenib, and ER-34122, was analyzed by both thermodynamic and kinetic approaches to better understand the absorption characteristics of amorphous pharmaceuticals. For each amorphous drug, the extent of supersaturation during in vitro dissolution was proved to be similar to that in vivo, which was estimated from relative bioavailability data. The theoretical limit of supersaturation was thermodynamically calculated from several thermal properties and water sorption isotherms of amorphous solids. in vitro and in vivo supersaturation of amorphous vemurafenib was thermodynamically controlled and was in good agreement with the theoretical limit. On the contrary, the supersaturation ratio of the other four drugs was highly overestimated by the thermodynamic calculation. However, it was satisfactorily explained by considering supersaturation stability, which indicated how long supersaturation can be maintained without crystal nucleation. Supersaturation stability was evaluated by measuring the induction time for crystal nucleation kinetically. Concomitant use of thermodynamic and kinetic approaches is, therefore, invaluable in evaluating supersaturation behavior of amorphous materials and assessing development potential of poorly water-soluble drugs. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:4220-4230, 2012
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 11, November 2012, Pages 4220-4230
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 11, November 2012, Pages 4220-4230
نویسندگان
Shunsuke Ozaki, Ikuo Kushida, Taro Yamashita, Takashi Hasebe, Osamu Shirai, Kenji Kano,