Jain Vikas, Kare Pradeep, Jain Deepika, Singh Ranjit
School of Pharmaceutical Sciences, Shobhit University, NH-58, Modipuram, Meerut, Uttar Pradesh, 250110, India.
Acta Pol Pharm. 2011 Mar-Apr;68(2):273-8.
Mucoadhesive nanosuspension of ciprofloxacin was designed in order to improve the solubility, bioavailability and efficacy for the treatment of typhoid fever. The identity and purity of drug was established. The compatibility of drug with various excipients was ascertained by FTIR techniques, which indicated no interaction between the drug and excipients. Four different formulations were prepared by optimizing various parameters using different polymers like soya lecithin, pluronic F68, polyvinyl alcohol, and polyvinylpyrrolidone K30. Particle size and polydispersity index were determined by photon correlation spectroscopy. Average particle size of different formulations was found to be between 503-1844 nm. The zeta potential of all formulations was found to be around +/- 20 My indicating satisfactory physical stability. Scanning electron microscopy showed that process parameters affect the crystal morphology. The promising formulations prepared from combination of soya lecithin and pluronic F68 and those based on soya lecithin alone were subjected to dissolution profile studies. The later formulation exhibited fast dissolution rate as compared to the former. Thus nanosus-pension based on soya lecithin was incorporated into hydrogels prepared using different grades of carbopol 934 and 971 as mucoadhesive polymers. After 10 h, mucoadhesive nanosuspensions showed 45-56% release. The developed mucoadhesive nanosuspensions exhibited satisfactory physical stability. The studies indicated potential of these formulations as novel gastroretentive systems.
为提高环丙沙星在治疗伤寒热方面的溶解度、生物利用度和疗效,设计了环丙沙星黏膜黏附纳米混悬液。确定了药物的特性和纯度。通过傅里叶变换红外光谱(FTIR)技术确定了药物与各种辅料的相容性,结果表明药物与辅料之间无相互作用。使用大豆卵磷脂、泊洛沙姆F68、聚乙烯醇和聚乙烯吡咯烷酮K30等不同聚合物,通过优化各种参数制备了四种不同的制剂。通过光子相关光谱法测定粒径和多分散指数。发现不同制剂的平均粒径在503-1844nm之间。发现所有制剂的ζ电位约为±20mV,表明具有令人满意的物理稳定性。扫描电子显微镜显示工艺参数会影响晶体形态。对由大豆卵磷脂和泊洛沙姆F68组合制备的有前景的制剂以及仅基于大豆卵磷脂的制剂进行了溶出度研究。与前者相比,后一种制剂表现出更快的溶出速率。因此,将基于大豆卵磷脂的纳米混悬液加入到使用不同等级的卡波姆934和971作为黏膜黏附聚合物制备的水凝胶中。10小时后,黏膜黏附纳米混悬液显示出45-56%的释放率。所开发的黏膜黏附纳米混悬液表现出令人满意的物理稳定性。研究表明这些制剂作为新型胃滞留系统具有潜力。