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KMID : 0369820000300030173
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Jorunal of Korean Pharmaceutical Sciences
2000 Volume.30 No. 3 p.173 ~ p.178
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Preparation and Evaluation of PGE1 Transurethral Suppositories
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김종오/Kim JO
권기철/이종달/최한곤/용철순/Quan QZ/Rhee JD/Choi HG/Yong CS
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Abstract
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The purpose of this work is to develop a transurethral suppository containing prostaglandin E1(PGE1), which stabilizes the drug, gives no irritation to physiological body and enhances the erectile response of PGE1.PGE1 transurethral suppositories were prepared with various amounts of compositions such as saturated polyglycolysed glyceride (Suppocire®AP,SAP), polyoxyethylene hydrogenated castor oil (HCO-50) and ethanol. The melting points, viscosities and PGE1 release of the suppositories were investigated. Ocular irritation test was carried out after application of PGE1 suppository to rabbit's eye. The intracavernous pressure (ICP), penile length and duration of erectile response were determined after transurethral administration of PGE1 suppository and compared with those after intracavernosal injection of PGE1 solution to cats. HCO-50 hardly affected the melting points and viscosities of PGE1 suppositories. Additionally, PGE1 transurethral suppositories, whose melting point ranges was 34?35?C, was speedily melted in physiological body. HCO-50 significantly decreased the dissolution rates of PGE1 from the suppositories. Dissolution mechanism analysis showed the release of PGE1 was proportional to the square root of time, indicating that PGE1 might be released from the suppositories by Fickian diffusion. The release rate of PGE1 from PGE1 suppository [PGE1/SAP/HCO-50/ethanol (1/94.5/2.5/2%)] was about 80% within 2 h. This PGE1 suppository gave no significant irritation to the ocular tissue, expecting that it gave no irritation to the urethral tissue less sensive than ocular tissue. Furthermore, PGE1 in this suppository was stable at 4?C for 2 years. This suppository increased the ICP and penile erection similar to those of injectable PGE1 solution. However, it gave 2.5-fold increased duration of erectile response than injectable PGE1 solution. Our results suggested that it gave more effective erectile response than injectable PGE1 solution in cats. It is concluded that this PGE1 suppository with good safety, excellent stability and enhanced erectile response, could be a more effective and convenient transurethal delivery system of PGE1.
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KEYWORD
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Prostaglandin E1, Transurethral suppository, Stability, Irritation, Erectile dysfunction
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