Yamaguchi T, Fukushima Y, Itai S, Hayashi H
Department of Pharmaceutics, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Biochim Biophys Acta. 1995 Jun 6;1256(3):381-6. doi: 10.1016/0005-2760(95)00085-q.
The rates of release of prostaglandin E1 (PGE1) from lipid particles into aqueous solution were obtained by the dialysis method, for parenteral lipid emulsion (Lipo-PGE1) diluted 10-times with buffered solutions of various pH. The findings, which were the rates of release of PGE1, were used to calculate the amount of PGE1 distributed in lipid particles when Lipo-PGE1, diluted 100-times with various pH levels of the buffered solution, was administered by intravenous drip infusion. More than 90% of PGE1 was retained in the lipid particles and intravenously infused when transfusion fluid pH was less than 5.5 and 2 ml of Lipo-PGE1 and 198 ml of transfusion fluid had been mixed and were administered over 2 h. Results from simulation showed that half of the PGE1 was retained in lipid particles and was infused, if Lipo-PGE1 was diluted 100-times with pH 8 transfusion fluid. Though PGE1 was sparingly soluble in an aqueous solution, these findings demonstrated that a significant amount of PGE1 was retained in lipid particles. Thus, this dosage form is expected to be highly effective for a drug delivery of PGE1 in clinical treatment.
通过透析法，获取了前列腺素E1（PGE1）从脂质颗粒释放到水溶液中的速率，该实验使用了用不同pH缓冲溶液稀释10倍的肠胃外脂质乳剂（前列地尔脂质微球）。当用不同pH值的缓冲溶液将前列地尔脂质微球稀释100倍后通过静脉滴注给药时，用这些作为PGE1释放速率的实验结果，来计算分布在脂质颗粒中的PGE1的量。当输液pH值小于5.5，将2ml前列地尔脂质微球与198ml输液混合并在2小时内给药时，超过90%的PGE1保留在脂质颗粒中并通过静脉输注。模拟结果显示，如果用pH值为8的输液将前列地尔脂质微球稀释100倍，一半的PGE1会保留在脂质颗粒中并被输注。尽管PGE1在水溶液中的溶解度很小，但这些结果表明大量的PGE1保留在脂质颗粒中。因此，这种剂型有望在临床治疗中对PGE1的药物递送具有高效性。
