Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Giza, Egypt.
Pharm Dev Technol. 2020 Feb;25(2):227-236. doi: 10.1080/10837450.2019.1687521. Epub 2019 Nov 21.
The physicochemical properties and absorption of a drug can be altered through cocrystallization with a suitable coformer. The aim of this study was to prepare and characterize Gabapentin (Gaba)-saccharine (sacch) sweet cocrystals for improvement of Gaba physicochemical properties, stability and absorption in addition to masking its taste. The prepared cocrystals were incorporated into oro-dispersible tablets as an attractive dosage form for pediatrics and adults. Gaba-sacch sweet cocrystals were prepared and characterized using FTIR, DSC, XRD and SEM analysis. They enhanced Gaba solubility and particle size distribution. Oro-dispersible tablets of the sweet cocrystals were prepared and evaluated in comparison to tablets prepared by Gaba-sacch physical mixture (PM). The tablets prepared by the cocrystals had lower wetting and disintegration time with enhanced drug release than those prepared with the physical mixture. The optimized formulation was evaluated for Gaba pharmacokinetics in rabbits in comparison to Gaba-sacch PM tablet and Gaba commercial oral capsules. This formulation had enhanced drug absorption through significant higher and AUC with shorter . The prepared Gaba-sacch sweet cocrystals oro-dispersible tablets, in addition to its enhanced and performance, can also enhance patient compliance through its palatable taste and ease of administration.
药物的物理化学性质和吸收可以通过与合适的共晶形成剂共结晶来改变。本研究旨在制备和表征加巴喷丁（Gaba）-糖精（sacch）甜味共晶，以改善 Gaba 的物理化学性质、稳定性和吸收，并掩盖其味道。所制备的共晶被掺入口腔分散片，作为儿科和成人的有吸引力的剂型。使用 FTIR、DSC、XRD 和 SEM 分析对 Gaba-sacch 甜味共晶进行了制备和表征。它们提高了 Gaba 的溶解度和粒度分布。与 Gaba-sacch 物理混合物 (PM) 制备的片剂相比，制备了甜味共晶的口腔分散片并进行了评估。与用物理混合物制备的片剂相比，共晶制备的片剂具有更低的润湿和崩解时间以及增强的药物释放。与 Gaba-sacch PM 片剂和 Gaba 商业口服胶囊相比，对该优化配方在兔体内的加巴喷丁药代动力学进行了评估。该配方通过显著提高和 AUC 以及缩短 来增强药物吸收。除了增强的 和 性能外，制备的 Gaba-sacch 甜味共晶口腔分散片还可以通过其可口的味道和易于给药来提高患者的依从性。
