Minzi Omary M S, Massele Amosy, Justin-Temu Mary, Ericsson Orjan, Gustafsson Lars L
Department of Medicinal Chemistry, School of Pharmacy, Muhimbili University College of Health Sciences, Dar es Salaam.
Trop Doct. 2006 Apr;36(2):93-7. doi: 10.1258/004947506776593512.
The main objective of this work was to assess the relative bioavailability of two tablet formulations containing sulfadoxine/pyrimethamine (SP) and marketed in Tanzania. Twelve healthy volunteers were randomized to receive a single oral dose of three SP tablets each containing 500 mg sulfadoxine (SDX) and 25 mg pyrimethamine (PYR) in a form of either A (a locally manufactured SP tablet formulation, manufactured by a local pharmaceutical industry in Tanzania) or B (Fansidar), Hoffmann La Roche, Basel, Switzerland, an innovator's SP) after an overnight fasting. Serial blood samples (100 microL) were collected from a finger prick in duplicate up to 10 days and dried on Whatman filter paper. The samples were assayed for SDX and PYR using high-performance liquid chromatographic methods. Pharmacokinetic parameters of SDX and PYR were estimated by single compartment method. The pharmacokinetics of formulation A--maximum plasma concentration, the areas under the plasma concentration--time curve and the relative bioavailability (A versus B) were significantly lower than those of formulation B (P < 0.1). These observed differences indicate bioinequivalence between the two products.
这项工作的主要目的是评估在坦桑尼亚销售的两种含磺胺多辛/乙胺嘧啶（SP）的片剂制剂的相对生物利用度。12名健康志愿者被随机分组，在禁食过夜后，单次口服三种SP片剂，每种片剂含500毫克磺胺多辛（SDX）和25毫克乙胺嘧啶（PYR），剂型为A（坦桑尼亚当地一家制药企业生产的本地制造的SP片剂制剂）或B（Fansidar，瑞士巴塞尔霍夫曼·罗氏公司生产的创新型SP）。从手指采血，每次采集100微升，重复采集直至10天，并在Whatman滤纸上干燥。使用高效液相色谱法对样品中的SDX和PYR进行测定。采用单室模型法估算SDX和PYR的药代动力学参数。制剂A的药代动力学参数——最大血浆浓度、血浆浓度-时间曲线下面积以及相对生物利用度（A相对于B）显著低于制剂B（P<0.1）。观察到的这些差异表明这两种产品存在生物不等效性。
