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KMID : 0369820000300030167
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Jorunal of Korean Pharmaceutical Sciences
2000 Volume.30 No. 3 p.167 ~ p.172
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Preparation and Evaluation of Liquid Suppository Containing Prostaglandin E1-loaded Microemulsion
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김정환/Kim CH
이사원/박경미/최한곤/김종국/Lee SW/Park KM/Choi HG/Kim CK
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Abstract
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The purpose of this study is to develop a transurethral liquid suppository containing prostaglandin E1(PGE1)?loaded microemulsion, which undergoes a phase transition to gels at body temperature. The effects of oils, ethanol as solvent and HCl as pH-controlling agent on the physicochemical properties of liquid suppositories composed of poloxamer P 407, P 188 and carbopol was investigated. The stability of PGE1 and release of PGE1 from liquid suppository were evaluated. Oils such as Neobee and soybean oil significantly decreased the gelation temperature but increased the gel strength of liquid suppository due to their strongly binding with the components of liquid suppository base. However, ethanol slightly did the opposite. The pH of liquid suppositories hardly affected the gelation temperature and gel strength due to addition of very small HCl (0.005-0.01%). A liquid suppository [PGE1/P 407/P 188/carbopol/Neobee/ethanol/HCl (0.2/14/14/0.4/7/2/0.005%)], which had the gelation temperature (34.2±0.6?C) and gel strength (31.35±4.37sec) suitable for liquid suppository system, was easily administered and not leak out from the body. About 60% of PGE1 was released out within 2 h from this formulation. It was shown that the release of PGE1 was proportional to the square root of time, indicating that PGE1 might be released from the suppository by Fickian diffusion. It was stable at 4?C for at least 2 months. The results suggest that transurethral liquid suppository containing prostaglandin E1?loaded microemulsion is thought to be a convenient, safe and effective dosage form for PGE1. However, it should be further developed as a more convenient and stable dosage form for PGE1.
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KEYWORD
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Prostaglandin E1, Microemulsion, Liquid suppository, Gelation temperature, Gel strength
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