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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >In vivo evaluation os submicron emulsions with pilocarpine:the effect of pH and chemical form of the drug
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In vivo evaluation os submicron emulsions with pilocarpine:the effect of pH and chemical form of the drug

机译：含毛果芸香碱的亚微米乳剂的体内评估：pH和药物化学形式的影响

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Submicron emulsions containing 2.0% w/v pilocarpine as pilocarpine HCl, soybean oil (10% w/v) and egg lecithin (1.2% w/v) were formulated. Emulsions at pH 5.0, 6.5 and 8.5 were applied to the rabbit’s eye, and the reduction in pupil diameter was measured for 6 h. The miotic effect was compared with that obtained with aqueous solutions at the same pH. A prolonged miotic effect was observed when the submicron emulsion was used as a vehicle. After application of emulsions at pH 5.0, 6.5 or 8.5, the time when 20% reduction of pupil diameter was still observed was 3.9 ± 1.1 h, 4.3 1 1.3 h and 5.3 ± 0.8 h, respecti-vely, while, after application of a solution, this parameter was shorter by 30— 40%. AUC0 6h values were larger after application of the submicron emulsions in comparison to aqueous solutions; however, statistically significant differences were only observed for emulsions at pH 6.5. Although the bioavailability of the drug is pH dependent, emulsions at higher pH cannot be considered for clinical use because of pilocarpine degradation which occurs with a similar rate as in aqueous solutions. Introduction of pilocarpine into the oily phase in the form of pilocarpine base or its oleate did not improve either the physicochemical or the pharmacological properties of the formulations. Irrespective of the pH and chemical form of pilocarpine used for emulsion preparation, practically all drug was found in the aqueous phase of the emulsion; thus, partitioning to the oily phase was negligible.
机译：配制含有2.0％w / v毛果芸香碱作为盐酸毛果芸香碱，大豆油（10％w / v）和卵卵磷脂（1.2％w / v）的亚微米乳剂。将pH 5.0、6.5和8.5的乳剂涂在兔子的眼睛上，并测量6小时瞳孔直径的减小。将模仿效果与在相同pH值下使用水溶液获得的效果进行了比较。当亚微米乳剂用作载体时，观察到延长的模拟效果。在施加pH 5.0、6.5或8.5的乳剂后，仍观察到瞳孔直径减小20％的时间分别为3.9±1.1 h，4.3 1 1.3 h和5.3±0.8 h。解决方案中，该参数缩短了30％至40％。与水溶液相比，在施用亚微米乳液后，AUC0 6h值更大;但是，仅在pH 6.5的乳液中观察到统计学上的显着差异。尽管药物的生物利用度取决于pH值，但由于毛果芸香碱的降解速度与水溶液相似，因此无法考虑将较高pH的乳剂用于临床。以毛果芸香碱碱或其油酸酯的形式将毛果芸香碱引入油相不会改善制剂的物理化学或药理学性质。不管用于乳液制备的毛果芸香碱的pH值和化学形式如何，实际上所有的药物都在乳液的水相中发现。因此，分配至油相可忽略不计。

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