氯诺昔康固体分散体快速崩解片的研制与评价

H. Mohammadi, H. V, R. S, B. D. V. R. N.
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引用次数: 1

摘要

氯诺昔康是奥昔康类非甾体抗炎药(NSAID)。它属于BCS类物质,具有低溶解度和高渗透性。本研究的目的是制备含氯诺昔康固体分散体的快速崩解片,以提高氯诺昔康的溶出率和溶解度,并使其更快起效。固体分散体由聚合物如Kolliwax GMS, Soluplus和HPMC以三种不同的比例(1:1:1,1:2:1和1:3:1)制备。利用傅里叶变换红外光谱(FTIR)对配方进行了药物含量研究、药物释放研究和药物-聚合物相互作用的表征。固体分散体可以通过体外溶出研究来评估。利用优化后的固体分散体SD9,采用33响应面法(3变量、3级超崩解剂),设计实验软件,以刺槐豆胶、枸杞胶、车前草等超崩解剂为原料,直接压缩制备快速崩解片。预压缩参数的评估值在规定的范围内,表明良好的自由流动性能。压缩后的重量变化、硬度、脆度、含量均匀性、崩解时间(33秒)、释药率等指标均在10 min内达到最高值(99.21±1.87%),优于市售制剂(87.27±0.27%)。从体内生物利用度研究来看,最佳配方的Tmax为1.0 h,与市售配方的2.5 h相比显著(P < 0.05)。采用单因素方差分析评估其统计学意义。因此,体内研究表明,加入氯诺昔康快速崩解片的固体分散体可以成功地改善溶出度,导致更快的起效。由此可见,采用氯诺昔康固体分散体的快速崩解片可提高患者的依从性,并可立即采取有效的治疗疼痛和炎症。
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Development and Evaluation of Fast Disintegrating Tablets of Lornoxicam Solid Dispersions
Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.
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