不同超崩解剂对琥珀酸美托洛尔快速崩解片的制备及评价

M. Aruna, Samreen Sultana, S. Rasheed
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引用次数: 2

摘要

本研究的目的是研制一种快速崩解的琥珀酸美托洛尔固体口服剂型。快速溶解给药系统的概念源于为患者提供更传统的服药方式的愿望。与传统片剂相关的问题可以通过快速溶解片剂来解决,当片剂放在舌头上时,这些片剂会分解并迅速溶解在唾液中,而不需要饮用水。药物溶解度越高,吸收越快,临床疗效起效越快。预配制结果表明,活性药物成分的流动性能符合IP限制。为了进行药物-聚合物相容性,进行了傅里叶变换红外研究,观察到APl与辅料之间没有相互作用。制备了8种不同超级崩解剂配比的制剂,发现随着超级崩解剂用量的降低,药物释放率增加。在所有配方中,以CCS (F4)为超级崩解剂的配方较好地满足了各项参数。与其他制剂相比,它具有良好的体外崩解、体外溶出性。制备的片剂在几分钟内不需要水就能崩解;从而提高吸收,从而提高其生物利用度。结论:美托洛尔快速崩解片满足分散片的各项标准,可替代现有的常规片剂。制备的制剂在40℃、75%RH条件下,90 d内稳定。
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Formulation and evaluation of fast disintegrating tablets of metoprolol succinate using various superdisintegrants
The aim of present work is to develop a fast disintegrating solid oral dosage form of Metoprolol succinate. The concept of fast dissolving drug delivery system emerged from the desire to provide patient with more conventional means of taking their medication. Problems associated with conventional tablets can be resolved by means of fast dissolving tablets when put on tongue these tablets disintegrate and dissolve rapidly in saliva without need of drinking water. The faster the drug disintegrates in to solution, the quicker the absorption and onset of clinical effect. Preformulation results reveal that the flow properties of the active pharmaceutical ingredient were found to be excellent as per IP limits. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. Eight formulations were prepared with varying super disintegrating agent ratios and were found that as the level of super disintegrating agent decreased the drug release rates were found to be increased. Amongst all the formulations, formulation containing CCS (F4) as super disintegrant is fulfilling all the parameters satisfactorily. It has shown excellent in-vitro disintegration, in-vitro dissolution compared to other formulations. The prepared tablets disintegrate within few minutes without need of water; thereby enhance the absorption leading to its increased bioavailability. It was concluded that Fast Disintegrating tablets of Metoprolol can be prepared successfully as it satisfies all the criteria as a dispersible tablet and would be alternative to the currently available conventional tablets. Prepared formulations were stable during 90 days storage period at controlled 40°C and 75%RH.
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