各種PGE_1 リポソームの性質と効力
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概要
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Alprostadil (PGE<SUB>1</SUB>) shows potent vasodilating effect and anti-platelet effect and its clinical usefulness has been confirmed. But it is known that plasma half life of PGE<SUB>1</SUB> is very short because it is easily metabolized very rapidly mainly in lung. It is considered that avoiding the rapid enzymatic attack is important point to make a effective formulation of PGE<SUB>1</SUB>. We studied two liposomal formulations of PGE<SUB>1</SUB>, liposome with pH gradient and liposome composed of hydrogenated egg phophatidylcholine (H-EPC). Both liposomal preparations showed higher plasma concentration of PGE<SUB>1</SUB> than PGE<SUB>1</SUB> solution when these preparations were administered intravenously to rats. Pharmacological effect of liposomal preparations was also stronger than that of PGE<SUB>1</SUB> solution. The effect was in proportion to plasma concentration of PGE<SUB>1</SUB>. Liposomal PGE<SUB>1</SUB> with pH gradient was presumed to be stable for 2 years below 10° after lyophilization. It is concluded that these liposomal preparations of PGE<SUB>1</SUB> could be promising candidates for human use.
- 日本膜学会の論文
- 1995-07-01
著者
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- 各種PGE_1 リポソームの性質と効力