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Formulation and Evaluation of Oro Dispersible Tablet of Desloratadine

机译:地氯雷他定口服分散片的研制与评价

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ABSTRACT Desloratadine is an antagonist at histamine H1 receptors, and an antagonist at all subtypes of the muscarinic acetylcholine receptor. It has a long-lasting effect and in moderate and low doses, does not cause drowsiness because it does not readily enter the central nervous system. The present study is an attempt to formulate and evaluate the fast dissolving tablets of  Desloratadine. Fast dissolving tablets were prepared by direct compression after masking the bitter taste of drug by solid dispersion method with the aid of superdisintegrants. Seven formulations were developed using two different superdisintegrants in varying concentrations in such a way that total weight of the tablet remains the same. The drug-polymer incompatibility was ruled out by FTIR studies. All the formulated tablets were subjected for pre and post-compression evaluation parameters. A comparison of in vitro drug release of best formulation along with F1 formulation having no superdisintegrants is carried out. All the formulated tablets were shown satisfactory results which complies with official limits. Among the seven formulations, F7 was selected as the best formulation as its wetting time was 33 seconds, disintegration time was 29 seconds and %CDR after 8 minutes was 100.1%. F7 was found to be stable at 25°C ± 2 °C,  60°C ± 5°C and 40 °C ± 2 °C and 75 ± 5 % RH . Formulated tablets containing high concentration of croscarmellose sodium are better and effective than conventional tablets to meet patient compliance, give fast relief from allergy and cost effective. Keywords: Desloratadine; H1 antagonist; Fast dissolving tablets; ODT; Superdisintegrant, croscarmellose sodium.
机译:摘要地氯雷他定是组胺H1受体的拮抗剂,也是毒蕈碱型乙酰胆碱受体所有亚型的拮抗剂。它具有长效作用,适度和低剂量也不会引起嗜睡,因为它不容易进入中枢神经系统。本研究是试图配制和评估去氯雷他定的速溶片剂。借助超分散剂通过固体分散法掩盖药物的苦味后,通过直接压制制备速溶片剂。使用两种不同的超级崩解剂以不同的浓度开发了七种制剂,使片剂的总重量保持不变。 FTIR研究排除了药物与聚合物的不相容性。对所有配制的片剂进行压缩前和压缩后的评估参数。进行了最佳制剂与不含超级崩解剂的F1制剂的体外药物释放比较。所有配制的片剂均显示令人满意的结果,符合官方规定的限值。在这7种配方中,F7被选为最佳配方,因为其润湿时间为33秒,崩解时间为29秒,而8分钟后的%CDR为100.1%。发现F7在25°C±2°C,60°C±5°C和40°C±2°C和75±5%RH的条件下稳定。含有高浓度交联羧甲基纤维素钠的配方片剂比常规片剂更好,更有效,可满足患者的依从性,可快速缓解过敏和成本效益。关键字:去氯雷他定; H1拮抗剂;快速溶解片剂; ODT;超崩解剂,交联羧甲基纤维素钠。

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