• YAKHAK HOEJI
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• v.35 no.3
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• pp.197-202
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• 1991

In order to study drug release from the suppository, three types of hollow suppositories and one conventional suppository were prepared using indomethacin(IDM) as a model drug and Witepsol H-15 as a base. The 4 types of suppository prepared are as follows: type I, conventional suppository containing 50 mg of IDM powder, type II, hollow supository containing 50 mg of IDM powder in the cavity, type III, hollow suppository containing 25 mg of IDM powder in the base and IDM microcapsules (25 mg as IDM powder) in the cavity, and type IV, hollow suppository containing IDM microcapsules (25 mg as IDM powder) in the base and 0.5 ml of 5%(w/v) IDM-PEG 300 solution in the cavity. The drug amount released(%) from type II and I within 24 hrs was 46.7% and 66.9%, respectively. Comparing with the drug amount released from four types of suppository within initial 2 hrs and 24 hrs, that of type IV was high as 32.7% and 76.6%, respectively. IDM-ethycellulose microcapsules passed through 270 mesh sieve and the IDM content was 20.95%.

• YAKHAK HOEJI
• /
• v.40 no.4
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• pp.400-410
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• 1996

In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.