Nep E I, Mahdi M H, Adebisi A O, Ngwuluka N C, Conway B R, Smith A M, Asare-Addo K
a Department of Pharmacy , University of Huddersfield, Queensgate , Huddersfield , UK.
b Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Science , University of Jos , Jos , Nigeria.
Drug Dev Ind Pharm. 2018 Feb;44(2):251-260. doi: 10.1080/03639045.2017.1386209. Epub 2017 Oct 23.
Concomitant ingestion of alcohol and medications can greatly affect drug plasma concentrations as dose dumping or failure may occur as a result of the fact that formulation excipients may not always be resistant to alcohol. In this study, a natural polysaccharide (Sesamum radiatum gum) (SG) was extracted, characterized and used to formulate sustained release theophylline compacts to study the effect of varying alcohol concentrations (v/v) in dissolution media on drug release from these compacts. X-ray powder diffraction showed that the extracted gum was amorphous in nature with the powder having excellent compaction properties as observed with its compact being significantly harder than those prepared with pure hydroxypropyl methyl cellulose (HPMC) K4M. X-ray microtomography showed that the compacts produced were homogenous in nature, however, swelling studies showed failure of the compacts at the highest concentration of absolute ethanol used (40% v/v). Dissolution studies showed similarity at all levels of alcohol tested (f = 57-91) in simulated gastric (0.1 N HCl, pH 1.2) and intestinal fluids (phosphate buffer, pH 6.8) for the HPMC compacts whereas dissimilarity only occurred for the SG compacts at the highest alcohol concentration in both media (f = 35). The suitability of SG as a matrix former that can resist alcoholic effects therefore makes it suitable as an alternative polymer with wider applications for drug delivery.
酒精与药物同时摄入会极大地影响药物血浆浓度，因为由于制剂辅料可能并非总是对酒精具有抗性，可能会发生剂量倾泻或药物失效的情况。在本研究中，提取并表征了一种天然多糖（芝麻辐射胶）（SG），并将其用于制备茶碱缓释片，以研究溶解介质中不同酒精浓度（v/v）对这些片剂药物释放的影响。X射线粉末衍射表明，提取的胶本质上是无定形的，其粉末具有优异的压片性能，观察到其压制片明显比用纯羟丙基甲基纤维素（HPMC）K4M制备的压制片更硬。X射线显微断层扫描表明，所制备的片剂本质上是均匀的，然而，溶胀研究表明，在所使用的最高无水乙醇浓度（40% v/v）下，片剂出现了失效情况。溶出度研究表明，对于HPMC片剂，在模拟胃液（0.1 N HCl，pH 1.2）和肠液（磷酸盐缓冲液，pH 6.8）中，所有测试酒精水平下均具有相似性（f = 57 - 91），而对于SG片剂，仅在两种介质中的最高酒精浓度下出现不相似性（f = 35）。因此，SG作为一种能够抵抗酒精影响的基质形成剂的适用性使其适合作为一种具有更广泛药物递送应用的替代聚合物。
