胰岛素舌下粉剂的制备及其含量的测定
Azone,,胰岛素;Azone复合促进剂;舌下粉剂;紫外光谱,1实验材料与方法,2结果与讨论
摘 要 目的:研究含Azone复合促进剂的胰岛素舌下粉剂的制备及粉剂中胰岛素含量的测定。方法:根据含Azone复合促进剂的胰岛素乳液的最佳处方确定舌下粉剂的处方,根据该处方用β环糊精等包结或吸附Azone复合促进剂油状物,并用冷冻干燥法制备粉剂。用UV测定了粉剂中胰岛素的含量,并研究了该粉剂对糖尿病模型家兔的降血糖作用。结果:该舌下粉剂中胰岛素的回收率为100.5%, RSD为2.5%,含量为(66.6±3.3) u/250 mg, 该粉剂经糖尿病家兔舌下黏膜吸收后总降糖率(D%)达25.4%, 药理相对生物利用度(PA%)为20.2%。结论:该舌下粉剂中胰岛素含量确定,分布均匀,并且能有效降低实验动物的血糖。关键词 胰岛素;Azone复合促进剂;舌下粉剂;紫外光谱
Preparation of insulin sublingual powder and the determination of insulin in the powder
PENG Hong, GAO Qiuhua, HUANG Kaixun, XU Huibi
(Institute of Materia Medica, Huazhong University of Science and Technology, Wuhan, Hubei 430074)
Abstract Objective:To study the preparation of insulin sublingual powder with azone composite enhancer and to measure the content of insulin in the powder. Methods:Azone composite enhancer was included in βcyclodextrins, and insulin sublingual powder was prepared by freezing drier. The content of insulin in the powder was determined by UV, and the hypoglycemic effects of insulin sublingual powder on diabetic rabbits were also studied. Results:Recovery of insulin in the powder was (100.5±25)%, and the content of insulin in the powder was (66.6±3.3) u/250 mg. The total blood glucose decrease ratio(D) of the powder is 25.4%, and relative bioavailability is 20.2%. Conclusions:The results indicated that insulin was well dispersed in the powder, and the powder is very effective for insulin sublingual absorption. In addition UV is a good way to measure the content of insulin in the powder . ......
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