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KMID : 0369819960260040299
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Jorunal of Korean Pharmaceutical Sciences
1996 Volume.26 No. 4 p.299 ~ p.308
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Controlled Release of Propranolol Hydrochloride (PPH) from PPH-Solid Dispersion System--Polyvinyl Alcohol Hydrogel Hollow Type Suppository
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정진훈/Chung JH
이정연/구영순/Rhie JY/Ku YS
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Abstract
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In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours, respectively. In the relative strength test for PVA hydrogel, PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The Cmax, AUC0→8 and MRT of PPH powder hollow type suppository were 196.37±5.63ng/ml, 1105.26 ng/ml/min and 8.66 min, respectively. The Cmax, AUC0→8 and MRT of PPH-EC-SDS(PPH : EC=1:3) were $91.30{\pm]14.14\;ng/ml$, 554.69 ng/ml/min, 235.99 min, respectively.
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KEYWORD
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Hollow type suppository, Solid dispersion system, Release control, Hydrogel, Polyvinyl alcohol, Propranolol.HCl, Rectal absorption
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