A.U. College of Pharmaceutical Sciences, Division of Pharmaceutical Technology, Andhra University, Visakhapatnam, Andhra Pradesh, India
Curr Drug Deliv. 2017;14(7):955-967. doi: 10.2174/1567201813666161230130140.
Assessment of natural polymers in oral controlled drug delivery.
The objective of the present investigation was to assess of Araucaria gum (AHG) obtained from bark exudates of the Araucaria heterophylla (family: Araucariaceae) for the design of oral controlled release forms, in particular tablet dosage forms by using matrix systems. Diclofenac sodium was used as model drug and compared with the marketed formulation.
Matrix tablets were prepared by wet granulation technique and 5% w/v of AHG dispersion water was used as granulating agent for preparation of AHG matrix tablets.
AHD2 (3:20) was found to be the optimized formulation based on in vitro drug dissolution studies. FTIR and DSC studies performed on the optimized formulations indicated no drug-polymer interaction. AHD2 (3:20) was found to be stable after accelerated stability testing for 6 months as per ICH guidelines. Pharmacokinetic studies of the optimized formulation were performed in healthy Albino Wister rabbits in comparison with that of the pure drug by estimating pharmacokinetic parameters and mean residence time (MRT). It was found that there is a significant increase in the bioavailability of diclofenac sodium from AHD2 formulation which was evident from the high AUC and MRT values compared with the pure drug.
The above results clearly indicated that AHG gum can be used for the development of oral controlled release dosage forms by using matrix systems.
口服控释给药中的天然聚合物评估。
本研究旨在评估从南洋杉科南洋杉属(Araucaria heterophylla)树皮渗出物中获得的Araucaria 树胶(AHG),以设计口服控释制剂,特别是使用基质系统的片剂剂型。将双氯芬酸钠用作模型药物,并与市售制剂进行比较。
通过湿法制粒技术制备基质片剂,并使用 5% w/v 的 AHG 分散水作为造粒剂制备 AHG 基质片剂。
根据体外药物释放研究,发现 AHD2(3:20)是优化的配方。对优化配方进行的 FTIR 和 DSC 研究表明没有药物-聚合物相互作用。根据 ICH 指南,对 AHD2(3:20)进行 6 个月的加速稳定性测试后,发现其稳定。与纯药物相比,在健康白化兔中进行优化配方的药代动力学研究,通过估计药代动力学参数和平均驻留时间(MRT)。结果表明,与纯药物相比,AHD2 制剂中双氯芬酸钠的生物利用度显著增加,这从 AUC 和 MRT 值较高可以明显看出。
上述结果清楚地表明,AHG 树胶可用于通过使用基质系统开发口服控释剂型。