新型协同加工超崩解剂制备氯沙坦钾速溶片

B. Hemalatha, P. Bhuvaneswari, G. Kalyani, N. K. Veni, K. Naga Durga, P. Yashwanthi, K. Padmalatha
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摘要

氯沙坦用于治疗高血压,也用于降低某些心脏病患者中风的风险。因此,本研究的目的是研制氯沙坦钾口服溶片,以提高其生物利用度,达到快速起效,提高患者依从性。由于氯沙坦钾的生物利用度较短,只有33%,为提高起效性,采用超崩解剂配制氯沙坦钾速溶片,以提高溶出速度,从而提高生物利用度。采用F1、F2、F3三种配方(分别为2%、4%和8% w/w),研究了交联棉糖钠浓度的影响。同样,研究了乙醇酸淀粉钠分别用3种配方(F4、F5和F6)对其影响。当超崩解剂质量分数为8%时,氯沙坦钾的释放速度明显快于其他浓度的交联棉糖钠和淀粉乙醇酸钠。与乙醇酸淀粉钠相比,以交联棉糖钠制备的氯沙坦钾释放速度相对较快。以超崩解剂(共加工混合物)、交联棉糖钠和淀粉乙醇酸钠为原料,采用直接压缩法制备了F7、F8和F9三种配方。与单个超崩解剂相比,含有共处理混合物的配方崩解时间更短。随后,我们可以得出结论,超崩解剂的性质、浓度以及超崩解剂的组合(共处理)对溶解速度有影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of Fast Dissolving Tablets of Losartan Potassium using Novel Co-processed Superdisintegrants
Losartan is used to treat high blood pressure (hypertension) and also used to lower the risk of stroke in certain people with heart disease. Therefore, the purpose of this study is to formulate mouth dissolving tablet of losartan potassium to improve its bioavailability, to attain fast onset of action and rise patient compliance. Owing to short bioavailability of 33% and to increase onset of action, fast dissolving tablets of Losartan Potassium were formulated using coprocessed superdisintegrants in order to improve the dissolution rate, in that way the bioavailability. The effect of concentration of the Croscarmellose sodium was studied by a set of three formulations (F1, F2, F3) with concentrations of 2%, 4% and 8% w/w respectively. Similarly, the impact of Sodium Starch Glycolate was studied by a set of three formulations (F4, F5 and F6) respectively. The formulation prepared with 8% w/w of superdisintegrant showed relatively rapid release of Losartan potassium when compared with other concentrations of Croscarmellose sodium and Sodium Starch Glycolate. The formulation prepared with Croscarmellose sodium had showed relatively fast release of Losartan Potassium when compared with Sodium Starch Glycolate. Three formulations (F7, F8 and F9) were prepared by including a combination of superdisintegrants (Co-processed Mixtures), Croscarmellose sodium and Sodium Starch Glycolate by direct compression method. Formulation containing Co-processed mixtures had less disintegration time as compared to the individual superdisintegrants. Subsequently, we can conclude that nature, concentration of the superdisintegrant in addition to combination of superdisintegrants (Co-processed) showed influence on the rate of dissolution.
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