Department of Pharmaceutics, V.L College of Pharmacy, Manik Prabhu Temple Road, Raichur, Karnataka, India.
Curr Drug Deliv. 2010 Apr;7(2):98-108. doi: 10.2174/156720110791011819.
The objective of the present study was to develop sustained release microcapsules of verapamil hydrochloride (VH) using biodegradable polymers. For this purpose microcapsules embedded verapamil hydrochloride were prepared using sodium alginate alone and also by incorporating some co polymers like methyl cellulose (MC), sodium carboxy methyl cellulose (SCMC) , poly vinyl pyrollidone (PVP) and xanthan gum by employing complex emulsion method of microencapsulation. Microcapsules were prepared in various core: coat ratios to know the effect of polymer and co polymers on drug release. Overall ten formulations were prepared and evaluated for flow behaviour, sieve analysis, drug entrapment efficiency, in vitro dissolution studies, stability studies, including scanning electron microscopy and DSC. The resulting microcapsules were discrete, large, spherical and also free flowing. The drug content in all the batches of microcapsules was found to be uniform. The release was depended on core: coat ratio and nature of the polymers. FTIR analysis revealed chemical integrity between Verapamil hydrochloride (VH), sodium alginate and between the copolymers. Among the four copolymers used methyl cellulose retarded the drug release more than the other three, hence the same formulation was subjected for in vivo studies. The drug release from the microcapsules was found to be following non fickian diffusion. Mechanism of drug release was diffusion controlled first order kinetics. Drug diffusion co efficient and correlation co efficient were also assessed by using various mathematical models. In vivo result analysis of pharmacokinetic parameters revealed that t max of reference and test formulations were almost same. From the study it was concluded that, sustained release Verapamil hydro chloride microcapsules could be achieved with success using sodium alginate alone and also in combination with other biodegradable polymers.
本研究的目的是开发盐酸维拉帕米(VH)的控释微囊,使用可生物降解的聚合物。为此,使用海藻酸钠单独,并通过将一些共聚物如甲基纤维素(MC)、羧甲基纤维素钠(SCMC)、聚维酮(PVP)和黄原胶嵌入维拉帕米盐酸盐微胶囊,采用复乳法微囊化。制备了不同核壳比的微胶囊,以了解聚合物和共聚物对药物释放的影响。共制备了十种制剂并进行了评价,包括流动行为、筛分分析、药物包封效率、体外溶出度研究、稳定性研究,包括扫描电子显微镜和差示扫描量热法。所得微囊为离散、大、球形且自由流动。所有批次的微囊药物含量均均匀。释放取决于核壳比和聚合物的性质。FTIR 分析表明盐酸维拉帕米(VH)、海藻酸钠和共聚物之间的化学完整性。在所使用的四种共聚物中,甲基纤维素比其他三种更能延缓药物释放,因此对同一制剂进行了体内研究。微胶囊中药物的释放遵循非菲克扩散。药物释放机制为扩散控制一级动力学。还通过使用各种数学模型评估了药物扩散系数和相关系数。体内药代动力学参数分析结果表明,参比制剂和试验制剂的 t max 几乎相同。从研究结果可以得出结论,使用海藻酸钠单独和与其他可生物降解聚合物组合,可以成功地实现盐酸维拉帕米的控释微囊。