文章基本信息

标题：Effect of Low-Molecular-Weight β-Cyclodextrin Polymer on Release of Drugs from Mucoadhesive Buccal Film Dosage Forms
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作者：Yotaro Arakawa ; Shigeru Kawakami ; Fumiyoshi Yamashita 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2005
卷号：28
期号：9
页码：1679-1683
DOI：10.1248/bpb.28.1679
出版社：The Pharmaceutical Society of Japan
摘要：We investigated the effect of low-molecular-weight β-cyclodextrin (β-CyD) polymer on in vitro release of two drugs with different lipophilicities ( i.e. , lidocaine and ketoprofen) from mucoadhesive buccal film dosage forms. When β-CyD polymer was added to hydroxypropylcellulose (HPC) or polyvinylalcohol (PVA) film dosage forms, the release of lidocaine into artificial saliva (pH 5.7) was reduced by 40% of the control. In contrast, the release of ketoprofen from the polymer film was enhanced by addition of β-CyD polymer to the vehicle. When lidocaine and ketoprofen was incubated with β-CyD polymer in the artificial saliva, concentration of free lidocaine molecules decreased in a β-CyD polymer concentration-dependent manner. The association constant with β-CyD polymer was 6.9±0.6 and 520±90 M ⁻¹ for lidocaine and ketoprofen, respectively. Retarded release of the hydrophilic lidocaine by β-CyD polymer might be due to the decrease in thermodynamic activity by inclusion complex formation, whereas enhanced release of the lipophilic ketoprofen by the β-CyD polymer might be due to prevention of recrystallization occurring after contacting the film with aqueous solution. Thus, effects of low-molecular-weight β-CyD polymer to the drug release rate from film dosage forms would vary according to the strength of interaction with and the solubility of active ingredient.
关键词：β-cyclodextrin polymer;buccal delivery;mucoadehive film dosage form;lidocaine;ketoprofen;hydroxypropylcellulose