Saunders L, Ingram D, Warrington S J
J Pharm Pharmacol. 1985 Nov;37(11):802-6. doi: 10.1111/j.2042-7158.1985.tb04971.x.
Experimental results of plasma concentration determinations and lowering of exercise heart rate for six subjects taking a conventional tablet and a sustained release preparation of oxprenolol have been analysed by a comprehensive computer simulation model. Individual plasma values were simulated using a lest squares procedure and the results were applied to evaluate individual release patterns following dosage with the sustained release preparation. Application of the model to the lowering of exercise heart rate indicated that the response is in a steady state with the plasma values and that the response-concentration relation is of the saturable, Emax, type. The parameters for this were evaluated for each subject for the results after a dose of a conventional tablet. These parameters were applicable to the results after dosage with a sustained release preparation. The method should be applicable to other sustained release preparations.
通过一个全面的计算机模拟模型,分析了六名服用常规片剂和氧烯洛尔缓释制剂的受试者的血浆浓度测定结果以及运动心率降低情况。使用最小二乘法模拟个体血浆值,并将结果用于评估服用缓释制剂后的个体释放模式。将该模型应用于运动心率降低情况表明,反应与血浆值处于稳态,且反应-浓度关系为饱和的Emax型。针对服用常规片剂后的结果,为每个受试者评估了这些参数。这些参数适用于服用缓释制剂后的结果。该方法应适用于其他缓释制剂。