Rekdal Mikal, Pai Aravind, Bs Muddukrishna
Department of Chemical Engineering, Norwegian University of Science and Technology, 7491 Trondheim, Norway.
Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka 576104, India.
Data Brief. 2017 Nov 7;16:135-140. doi: 10.1016/j.dib.2017.11.019. eCollection 2018 Feb.
Etravirine is a drug used alongside other medication in the treatment of HIV and is a non-nucleoside reverse transcriptase inhibitor. It is a BCS class IV drug, having low solubility and high permeability (Drugbank, https://www.drugbank.ca/drugs/DB06414) [1]. As a result, large doses of the drug are required for treatment. Two pills have to be taken twice a day, making it a "pill burden" (Intelence, http://www.intelence.com/hcp/dosing/administration-options) [2]. Therefore, attempts of co-crystallizing Etravirine are attractive as the solubility of the drug tends to increase in this solid form (Schultheiss and Newman, 2009) [3]. In this study Etravirine co-crystals were synthesized in the molar ratios 1:1, 1:2 and 2:1 with L-tartaric acid as the co-former. Both slow evaporation and physical mixture was performed to mix the components. DSC values of final products are presented as well as FTIR spectra to observe the altered intermolecular interactions. A chemical stability test was performed after seven days using area under curve data from an HPLC instrument.
依曲韦林是一种与其他药物联合用于治疗艾滋病病毒（HIV）的药物，属于非核苷类逆转录酶抑制剂。它是一种BCS IV类药物，溶解度低但渗透性高（药物银行，https://www.drugbank.ca/drugs/DB06414）[1]。因此，治疗时需要大剂量用药。每天需服用两片，分两次服用，这成为了一种“服药负担”（英特龙，http://www.intelence.com/hcp/dosing/administration-options）[2]。因此，尝试将依曲韦林制成共晶体很有吸引力，因为该药物的溶解度在这种固体形式下往往会增加（舒尔特海斯和纽曼，2009年）[3]。在本研究中，以L-酒石酸作为共形成物，按照1:1、1:2和2:1的摩尔比合成了依曲韦林共晶体。采用缓慢蒸发和物理混合两种方法来混合各组分。给出了最终产物的差示扫描量热（DSC）值以及傅里叶变换红外光谱（FTIR），以观察分子间相互作用的变化。使用高效液相色谱（HPLC）仪器得到的曲线下面积数据，在七天后进行了化学稳定性测试。
