Chakraborti Chandra Kanti, Sahoo Subhashree, Behera Pradipta Kumar
Department of Pharmaceutics, Kanak Manjari Institute of Pharmaceutical Sciences, Rourkela 769015, Orissa, India.
School of Chemistry, Sambalpur University, Jyoti Bihar 768019, Orissa, India.
Saudi Pharm J. 2015 Apr;23(2):195-201. doi: 10.1016/j.jsps.2014.08.003. Epub 2014 Aug 9.
Considering the importance of drug permeation from formulations, in vitro and ex vivo drug permeation characteristics of three oral mucoadhesive suspensions of Ofloxacin were designed and compared. Three suspensions of Ofloxacin were prepared by taking two grades of Carbopol polymer such as Carbopol 934 (C934) and Carbopol 940 (C940); and Hydroxypropyl methylcellulose. The permeability study was performed by using a Franz diffusion cell through both synthetic cellulose acetate membrane and excised goat gastrointestinal membranes in acidic as well as alkaline pH. To know the permeability of the drug from control/formulations through different membranes in acidic/alkaline pH, cumulative percentage drug permeation, apparent permeability (Papp) and flux (J) were calculated. In addition, enhancement ratio (ER) of each formulation was also determined. From our results, it is evident that formulation containing C940 was the best suspension considering Papp and J values of all formulations. Moreover, it was the most beneficial formulation for improving permeation and diffusivity of Ofloxacin even after 16 h. Hence, this suspension was probably the most suitable formulation to obtain prolonged release action of the drug. The ER values of all formulations through the excised goat intestinal mucus membrane in alkaline pH were higher than those formulations through the goat stomach mucosal membrane in acidic pH. ER values of those formulations indicate that the permeability of the drug was more enhanced by the polymers in the intestinal part, leading to more bioavailability and prolonged action in that portion of the gastrointestinal tract. It may also be concluded from our results that in addition to formulation containing C940, other formulations may also show effective controlled release action.
考虑到药物从制剂中渗透的重要性，设计并比较了三种氧氟沙星口服粘膜粘附性混悬液的体外和离体药物渗透特性。通过使用两种等级的卡波姆聚合物（如卡波姆934（C934）和卡波姆940（C940））以及羟丙基甲基纤维素制备了三种氧氟沙星混悬液。使用Franz扩散池通过合成醋酸纤维素膜和切除的山羊胃肠道膜在酸性和碱性pH条件下进行渗透性研究。为了了解对照品/制剂中的药物在酸性/碱性pH条件下通过不同膜的渗透性，计算了药物累积渗透百分比、表观渗透率（Papp）和通量（J）。此外，还测定了每种制剂的增强率（ER）。从我们的结果可以明显看出，考虑到所有制剂的Papp和J值，含有C940的制剂是最佳混悬液。此外，即使在16小时后，它也是改善氧氟沙星渗透性和扩散性最有益的制剂。因此，这种混悬液可能是获得药物长效释放作用最合适的制剂。所有制剂在碱性pH条件下通过切除的山羊肠粘膜的ER值高于在酸性pH条件下通过山羊胃粘膜的制剂。这些制剂的ER值表明，聚合物在肠道部分对药物渗透性的增强作用更大，从而导致在胃肠道该部分的生物利用度更高和作用时间更长。从我们的结果还可以得出结论，除了含有C940的制剂外，其他制剂也可能显示出有效的控释作用。
