Khaled Abdulhakim A A, Pervaiz Khalid, Karim Sabiha, Farzana Kalsoom, Murtaza Ghulam
Department of Mathematics, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
Acta Pol Pharm. 2013 Jul-Aug;70(4):743-7.
This study was aimed to develop level A, B and C in vitro-in vivo correlation (IVIVC) for encapsulated metoprolol tartrate (T1, T2 and T3 having metoprolol tartrate/polymer ratio of 1: 1, 1: 1.5 and 1: 2,w/w). The in vitro data were correlated with in vivo data. For level A IVIVC, drug absorption data were calculated using Wagner-Nelson method. In addition, convolution approach was used to approximate plasma drug levels from in vitro dissolution data. The coefficient of determination (R2) for level A IVIVC was 0.720, 0.905, 0.928 and 0.878 for Mepressor, T1, T2 andT3 formulations, respectively, with acceptable percent error (< 15%). The value of R2 for level B and C IVIVC was 0.231and 0.714, respectively. It is also concluded that level A IVIVC is a proficient mathematical model for biowaiver studies involving study parameters as those implemented for T1S (T1formulation tested for dissolution in the presence of sodium lauryl sulfate) revealing that IVIVC level A is dosage form specific, rather than to be drug specific.
本研究旨在建立包封型酒石酸美托洛尔（T1、T2和T3的酒石酸美托洛尔/聚合物比例分别为1:1、1:1.5和1:2，w/w）的A、B和C级体外-体内相关性（IVIVC）。将体外数据与体内数据进行关联。对于A级IVIVC，使用Wagner-Nelson方法计算药物吸收数据。此外，采用卷积法从体外溶出数据估算血浆药物水平。美托洛尔、T1、T2和T3制剂的A级IVIVC的决定系数（R2）分别为0.720、0.905、0.928和0.878，误差百分比可接受（<15%）。B级和C级IVIVC的R2值分别为0.231和0.714。还得出结论，A级IVIVC是一种用于生物豁免研究的有效数学模型，其研究参数与T1S（在十二烷基硫酸钠存在下测试溶出度的T1制剂）所采用的参数相同，这表明A级IVIVC是剂型特异性的，而非药物特异性的。
