Heinrich Heine University Duesseldorf, Universitaetsstrasse 1, 40225 Duesseldorf, Germany.
Eberhard Karls University Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
Eur J Pharm Sci. 2018 May 30;117:236-244. doi: 10.1016/j.ejps.2018.02.030. Epub 2018 Feb 27.
Various drug therapies require more than one active pharmaceutical ingredient (API) for an effective treatment. There are many advantages, e.g. to improve the compliance or pharmacodynamic response in comparison to a monotherapy or to increase the therapy safety. Until now, there are only a few products available for the paediatric population due to the lack of age appropriate dosage forms or studies proving the efficacy and safety of these products. This study aims to develop orodispersible films (ODFs) in a continuous solvent casting process as child appropriate dosage form containing both enalapril maleate (EM) and hydrochlorothiazide (HCT) separated in different film layers. Furthermore, they should be characterised and the API migration analysed by confocal Raman microscopy (CRM). ODFs were successfully produced in a continuous manufacturing process in form of double- and triple-layer formulations based on hydroxypropylcellulose (HPC) or a combination of HPC and polyvinyl alcohol (PVA). CRM revealed that both APIs migrate within the film layers shortly after manufacturing. PVA inhibits the migration inside the double-layer film, but is not able to prevent the API migration as an interlayer inside a triple-layer ODF. With increasing film layers, the content of residual solvents and the disintegration time increases (mono-layer films: <10 s, triple-layer films: 37 s). In conclusion, it was feasible to produce fixed-dose combinations in therapeutic doses up to 9 mg HCT and 3.5 mg EM for the double-layer film with adequate mechanical properties, which enable coiling up onto jumbo rolls directly after production. The best separation of the two APIs was achieved by casting a double-layer ODF consisting of different film forming polymers, which can be beneficial when processing two incompatible APIs.
各种药物疗法需要一种以上的活性药物成分 (API) 才能有效治疗。与单一疗法相比,这种疗法有许多优势,例如提高顺应性或药效反应,或提高治疗安全性。到目前为止,由于缺乏适合儿童的剂型或证明这些产品疗效和安全性的研究,儿科人群可用的产品寥寥无几。本研究旨在开发连续溶剂浇铸工艺中的口崩片 (ODF) 作为适合儿童的剂型,其中包含马来酸依那普利 (EM) 和氢氯噻嗪 (HCT),分别位于不同的膜层中。此外,还应对其进行表征,并通过共聚焦拉曼显微镜 (CRM) 分析 API 迁移情况。成功地以羟丙基纤维素 (HPC) 或 HPC 和聚乙烯醇 (PVA) 的组合为基础,以连续制造工艺生产出双层和三层配方的 ODF。CRM 显示,两种 API 都在制造后不久在膜层内迁移。PVA 抑制双层膜内的迁移,但不能防止 API 迁移作为三层 ODF 的夹层。随着膜层数量的增加,残留溶剂的含量和崩解时间增加(单层膜:<10s,三层膜:37s)。总之,以足够的机械性能生产出治疗剂量高达 9mg HCT 和 3.5mg EM 的固定剂量组合是可行的,这使得双层 ODF 可以在生产后直接卷成超大卷。通过浇铸由不同成膜聚合物组成的双层 ODF 可以实现两种 API 的最佳分离,这在处理两种不相容的 API 时可能是有益的。