Gonjari I D, Hosmani A H, Karmarkar A B, Kadam S B, Godage A S, Khade T S
Government College of Pharmacy, Karad-415124, Dist. Satara, Maharashtra, India.
Drug Discov Ther. 2009 Aug;3(4):176-80.
The purpose of this research was to study mucoadhesive microspheres of tramadol hydrochloride compressed into tablet along with a loading dose. Microspheres containing tramadol hydrochloride were prepared by employing sodium alginate in combination with a mucoadhesive polymer, i.e., Carbopol 971P. An orifice-ionic gelation method was used to prepare the microspheres. A 3(2) factorial design was used to investigate the combined effect of two independent formulation variables in the preparation of microspheres. The concentration of sodium alginate (X(1)) and carbopol 971P (X(2)) were selected as independent variables. Nine batches were used in the experimental design and evaluated for swelling index, mucoadhesion, and drug entrapment efficiency. A surface plot is presented to graphically represent the effect of the independent variables on the evaluation parameters. The best batch exhibited drug entrapment efficiency of 70.12%, swelling index of 2.3 and mucoadhesion of 95.42%. Microspheres showing maximum drug entrapment were compressed with the loading dose and subjected to in vitro dissolution studies. Drug release from tablets was found to follow a matrix model. Initial burst release from these tablets indicated the release of the loading dose and then a sustained effect over the time. This modified approach to formulation of tablets was found to be effective in sustaining drug release.
本研究的目的是研究将盐酸曲马多粘膜粘附微球与负荷剂量一起压制成片剂。采用海藻酸钠与粘膜粘附聚合物（即卡波姆971P）结合制备含盐酸曲马多的微球。采用孔口离子凝胶法制备微球。采用3(2)析因设计研究微球制备中两个独立处方变量的联合效应。选择海藻酸钠(X(1))和卡波姆971P(X(2))的浓度作为自变量。实验设计中使用了9个批次，并对其溶胀指数、粘膜粘附性和药物包封率进行了评估。绘制了表面图以直观呈现自变量对评估参数的影响。最佳批次的药物包封率为70.12%，溶胀指数为2.3，粘膜粘附性为95.42%。将显示最大药物包封率的微球与负荷剂量一起压片，并进行体外溶出研究。发现片剂中的药物释放遵循基质模型。这些片剂的初始突释表明负荷剂量的释放，然后随着时间的推移产生持续效应。发现这种改良的片剂配方方法在维持药物释放方面是有效的。
