School of Pharmaceutical Sciences, SOA University, Bhubaneswar 751003, India.
AAPS PharmSciTech. 2009;10(3):928-34. doi: 10.1208/s12249-009-9289-z. Epub 2009 Jul 23.
Glibenclamide (GL)-loaded microcapsules (MC) and transdermal patches (TDP) were formulated and in vitro and in vivo parameters compared to find out the best route of drug administration. The formulation TDP1 having a drug-polymer ratio 1:1 showed comparatively higher GL release and better permeation across mice skin (p < 0.05). From the comparative study, it was concluded that the transdermal system of GL produced better improvement compared to oral microcapsule administration (p < 0.05). The transdermal system exhibited comparatively slow and continuous supply of GL at a desired rate to systemic circulation avoiding metabolism, which improved day-to-day glycemic control in diabetic subjects. Transdermal system of GL exhibited better control of hyperglycemia and prolonged plasma half-life by transdermal systems (9.6 +/- 1.2 h) in comparison with oral microcapsule (5.84 +/- 2.1 h), indicating that the drug, when administered by transdermal systems, will remain in the body for a longer period. From the glucose tolerance test, transdermal route effectively maintained the normoglycemic levels in contrast to the oral group (MC1), which produced remarkable hypoglycemia ranging from -12.6 +/- 2.1% to -18 +/- 2.3%. The significantly high (p < 0.05) area under the curve values observed with transdermal system (1,346.2 +/- 92.3 ng ml(-1) h(-1)) also indicate increased bioavailability of the drug from these systems compared to the oral route (829.8 +/- 76.4 ng ml(-1) h(-1)).
格列本脲(GL)载药微囊(MC)和透皮贴剂(TDP)被制备并进行了体外和体内参数比较,以找出最佳的给药途径。药物-聚合物比为 1:1 的 TDP1 制剂显示出相对较高的 GL 释放率和更好的透过小鼠皮肤的能力(p < 0.05)。通过比较研究,得出结论,GL 的透皮系统比口服微囊给药产生了更好的改善(p < 0.05)。透皮系统以期望的速率在系统循环中以相对缓慢和持续的方式提供 GL,避免了代谢,从而改善了糖尿病患者的日常血糖控制。与口服微囊(5.84 +/- 2.1 h)相比,GL 的透皮系统显示出更好的控制高血糖和延长血浆半衰期(9.6 +/- 1.2 h),表明当通过透皮系统给药时,药物将在体内停留更长时间。从葡萄糖耐量试验来看,与口服组(MC1)相比,透皮给药途径有效地维持了正常血糖水平,口服组产生了显著的低血糖,范围从-12.6 +/- 2.1%到-18 +/- 2.3%。透皮系统观察到的显著高(p < 0.05)曲线下面积值(1,346.2 +/- 92.3 ng ml(-1) h(-1))也表明与口服途径相比,这些系统增加了药物的生物利用度(829.8 +/- 76.4 ng ml(-1) h(-1))。