奥美沙坦美多索米缓释片的设计、开发和体外评价

R. Gunda, Prasada Rao Manchineni, D. Dhachinamoorthi
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引用次数: 6

摘要

无论是快速给药系统还是新药给药系统,肠内给药途径都是最舒适、最广泛使用的给药途径。片剂是市场上最著名的固体制剂,是病人和医生的首选。在治疗慢性疾病条件的情况下,需要经常使用常规释放制剂,因此显示患者不遵守处方1然而,大多数药物的摄入表现为首次通过效应和/或首次通过肝脏代谢通过胃肠道降解的全身前消除,其结果是较低的全身生物利用度和较短的作用时间以及无活性或毒性转化产物的发展缓释(SR)剂型的目的是在较长时间内维持CSS水平。指定为修饰释放/定时释放的系统也可以被认为是实现延长药物递送的尝试。与立即释放制剂相比,3-6 SR制剂在给药频率上提供了更大的减少通过优化药物的生物药剂学、药代动力学和药效学特性,SR制剂比快速释放制剂具有优势。利用高分子聚合物等大分子调节药物释放速度已成为药物制剂产品开发的重要工具。多年来的大量报道表明,它们在各种药物从剂型中释放药物方面起着关键作用首选天然聚合物主要是因为它们经济、高药物容量、高热稳定性、非致癌性、黏附性、可生物降解、生物相容性、广泛的监管接受度和易压缩。各种胶和粘液被用于开发缓释制剂,如胶(黄原胶、黄原胶、瓜尔胶)、果胶、海藻酸盐等。纤维素衍生物如HPC、HPMC、CMC、SCMC已被广泛用作缓释剂型制剂的缓释剂。新型给药系统在时间药物治疗给药系统、黏附系统、时间药代动力学方法、靶向给药方法、颗粒系统等领域具有良好的应用前景。直接压缩法(DC)是一种简便易行的口服缓释制剂制备方法,具有快速、简便、制备过程中无降解作用、制剂依从性好等优点基于候选药物的生物药剂学、药代动力学和药效学特性的缓释系统的适宜性。文献中已经报道了大量关于其利用的研究
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Design, development, and in vitro evaluation of sustained release tablet formulations of olmesartan medoxomil
Enteral route is the most comfortable, extensively used route of administration for both prompt delivery systems and new drug delivery systems. Tablets are the most famous solid formulations available in the market and are preferred by patients and physicians alike. In case of treatment of chronic disease conditions, conventional release formulations are required to be administered in frequent manner and therefore shows patient non‒adherence to prescription.1 However, ingestion of majority of drugs shows first pass effect and/or first pass hepatic metabolism presystemic elimination by gastrointestinal degradation as a result of which low systemic bioavailability and shorter duration of action and development of non‒active or toxic transformed products.2 The objective of a sustained release (SR) dosage form is to maintain CSS levels for prolonged period. Systems that are designated as modified release/timed release can also be considered as attempts at achieving prolonged drug delivery.3‒6 SR formulations offers greater reduction in dosing frequency in comparison with immediate release formulations.7 SR formulations afford advantage over prompt release formulations by optimising biopharmaceutical, pharmacokinetic and pharmacodynamic properties of drug. The utilization of macromolecules like polymers in modulating the rate of drug release has turn to an essential tool in the product development of pharmaceutical formulations. Numerous reports over many years reveals that they play key role in the release of drugs from dosage form for various drugs.8 Natural polymers preferred primarily because they were economic, high drug holding capacity, high thermal stability, non‒carcinogenicity, mucoadhesivity, biodegradable, biocompatible, broad regulatory acceptance and ease of compression. Various gums and mucilages were used for the development of sustained release formulations in such as gums (xanthan, tragacanth, guar), pectin, alginates etc. cellulose derivatives such as HPC, HPMC, CMC, SCMC have been widely used as release retardants in the formulation of prolonged release dosage forms. The future of novel drug delivery systems (SR) is promising in arena like chronopharmacotherapeutic delivery system, mucoadhesive system, chronopharmacokinetic approach, targeted drug delivery approach, particulate system that provide high assurance and adoptability. Sustained release oral formulations by Direct Compression (DC) method was a simple approach due to its rapid production, Easer, No degradative effects occurred during manufacturing, compliance.7 The suitability of drug candidates for sustained release system based on biopharmaceutical, pharmacokinetic and pharmacodynamic properties of it. numerous studies have been reported in the literature regarding the utilisation
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