Dipartimento di Ingegneria Industriale, Università degli Studi Salerno, Fisciano, Italy.
Eur J Pharm Biopharm. 2011 Oct;79(2):382-91. doi: 10.1016/j.ejpb.2011.04.003. Epub 2011 Apr 16.
In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtained evolutions with time of plasma concentration were presented and used to assess the effectiveness of the commercial pharmaceutical products. The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized.
在这项工作中，我们回顾了现有的各种仪器，这些仪器可用于模拟药物（或食物）在摄入后的变化。同样，我们还简要回顾了用于模拟给予生物体的药物命运的各种模型。然后，我们在常规溶解测试器（USP 装置 2，方法 A）以及修改后的仪器中测定了双氯芬酸钠的控释制剂从市售肠溶包衣片中的释放动力学，该仪器可以更接近实际情况而不是 USP 建议的 pH 变化来复制给定的 pH 变化。报告并讨论了这两种实验释放曲线，因此，它们被用作先前提出的药代动力学模型的输入函数。给出了随时间变化的血浆浓度的演变，并用于评估市售药物产品的有效性。因此，强调了正确的体外模拟对于药物剂型设计的重要性。
