Department of Organic Chemistry, Ghent University, Ghent, Belgium
Macromol Rapid Commun. 2012 Oct 15;33(19):1701-7. doi: 10.1002/marc.201200332. Epub 2012 Aug 14.
Here we evaluate poly(2-ethyl-2-oxazoline)s (PEtOx) as a matrix excipient for the production of oral solid dosage forms by hot melt extrusion (HME) followed by injection molding (IM). Using metoprolol tartrate as a good water-soluble model drug we demonstrate that drug release can be delayed by HME/IM, with the release rate controlled by the molecular weight of the PEtOx. Using fenofibrate as a lipophilic model drug we demonstrate that relative to the pure drug the dissolution rate is strongly enhanced by formulation in HME/IM tablets. For both drug molecules we find that solid solutions, i.e. molecularly dissolved drug in a polymeric matrix, are obtained by HME/IM.
在这里,我们评估了聚(2-乙基-2-恶唑啉)(PEtOx)作为一种基质赋形剂,通过热熔挤出(HME)和注塑成型(IM)来生产口服固体制剂。我们以酒石酸美托洛尔为水溶性良好的模型药物,证明了药物释放可以通过 HME/IM 来延迟,释放速率可以通过 PEtOx 的分子量来控制。我们以非诺贝特为亲脂性模型药物,证明与纯药物相比,在 HME/IM 片剂中药物的溶解速率得到了极大的提高。对于这两种药物分子,我们发现通过 HME/IM 得到的是固溶体,即药物分子溶解在聚合物基质中。