Influence of Solid Fat Index in Triglyceride Suppository Bases on Drug Release
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概要
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In order to elucidate the factors affecting drug release characteristics from triglyceride suppositories, we have measured the solid fat index (SFI) of triglyceride suppository bases by the differential scanning calorimetry method. When Witepsol H15,widely used for suppository bases, was stored at 30℃ for 2 weeks, an increase in the SFI value of Witepsol H15 occurred, resulting in decreases in the release rate of morphine hydrochloride from stored suppositories. However, the degree of increase in SFI of stored Witepsol H15 was found to be different among some lots. To further investigate the relation between SFI and drug release rate in triglyceride bases, mixed bases of Witepsol H15 and Witepsol E85,which have various SFI values, were prepared. The addition of Witepsol E85 to Witepsol H15 resulted in an increase in SFI of the Witepsol H15-Witepsol E85 (H15-E85) mixed base. The increase of SFI brought about changes in some physicochemical properties of the H15-E85 mixed base such as increases in the melting point and the apparent viscosity. The release profiles of brilliant blue as a model drug from the H15-E85 mixed base could be expressed by Jander's equation. The logarithms of the release rate constants of brilliant blue from the H15-E85 mixed base, as well as those of morphine hydrochloride from stored Witepsol H15,were found to have a linear relation with SFI. These results indicate that SFI, which is considered to directly represent the melting state of suppository bases, is closely correlated with the drug release rate from triglyceride suppository bases.
- 公益社団法人日本薬学会の論文
- 1994-07-15
著者
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中村 康彦
Department Of Formulation Research Dainippon Pharmaceutical Co. Ltd.
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東 敏郎
大日本製薬株式会社製品研究所
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中村 康彦
Pharmaceutical Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
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斎藤 博幸
Pharmaceutical Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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北村 健三
Pharmaceutical Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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東 敏郎
Pharmaceutical Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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Nakamura Yoshihide
Technical Department Fuji Chemical Industries Co. Ltd.
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Nakamura Y
Department Of Pharmacognosy Tohoku Pharmaceutical University
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