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口服心得安可完全吸收,但全身利用度低且血浓度个体差异大,其肝提取率约80～90%,药物主要经肝代谢,由于口服后迅速代谢,因此需要多次给药及病人严格依从服药。本文主要评价心得安从各种亲水性基质的体外释放及透皮率,同时观察一些附加剂的影响。聚合物首先缓慢分散于预先加热至80℃的水,药物和附加剂预先溶解于50℃水,混匀放冷,然后加入聚合物溶液,混和。体外释放及透皮均用扩散池进行,用纤维素膜进行释放试验,用6～8周龄裸鼠的腹部皮肤进行透皮试验。
Oral experience Ankang completely absorbed, but the systemic utilization of low blood concentration and individual differences, the liver extraction rate of about 80 ~ 90%, the main drug by the liver metabolism, due to rapid metabolism after oral administration, which requires multiple administration and strict patient Follow the medication. This article mainly evaluates propranolol in vitro release and transdermal rate from a variety of hydrophilic matrix, while observing the impact of some additives. The polymer is first slowly dispersed in water pre-heated to 80 ° C. The drug and additives are pre-dissolved in water at 50 ° C, mixed and allowed to cool, then added to the polymer solution and mixed. In vitro release and transdermal diffusion cells were used to carry out release test with cellulose membrane, 6-8 weeks old nude mice abdominal skin transdermal test.