シクロデキストリン論文データベース検索システム

論文名	In-vitro prediction of bioavailability following extravascular injection of poorly soluble drugs: an insight into clinical failure and the role of delivery systems.
著者	Zimei Wu Dalia Hassan John P Shaw
キーワード
出版年月	1970年1月
発表先	J Pharm Pharmacol. 2013 Oct;65(10):1429-39.
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論文概要（和文）	溶解性の低い薬物の血管外注射後のバイオアベイラビリティのin vitro予測：臨床的失敗への洞察とデリバリーシステムの役割。
論文概要（英文）	Objectives: To investigate the feasibility of using an in-vitro model to simulate the incidence of post-injection drug precipitation (PDP), and to identify the roles of drug properties and delivery systems in its occurrence. Methods: A literature review on incomplete absorption following extravascular injection (subcutaneous and intramuscular) was conducted. Six model drugs in nine different formulations were studied for an in-vitro/in-vivo correlation. A rapid in-vitro dilution method using a 96-well plate was used for predicting PDP by dilution with a physiological buffer. New formulations based on hydroxypropyl-β-cyclodextrin (CD), with and without co-solvents or pH control, were developed and tested on the in-vitro model. Key findings: The occurrence of precipitation detected from the in-vitro dilution model appeared to be correlated with clinical reports and animal studies. The formulation components played an important role in determining the potential for drug precipitation on dilution or pH neutralization. CD was found to reduce the tendency for precipitation. The addition of co-solvents may reduce the effect of CD, depending on the solvent used. Conclusions: The in-vitro model can be used as a cost-effective screening tool in injectable formulation development for safe and effective delivery of poorly soluble drugs. PDP can be circumvented with a well-designed formulation.