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Significance of excipients to enhance the bioavailability of poorly water-soluble drugs in oral solid dosage forms: A Review

机译:赋形剂在口服固体剂型中增强水溶性药物的生物利用度的重要性:综述

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Nowadays most of the drug substances are coming into the innovation pipeline with poor water solubility. Here, the influence of excipients will play a significant role to improve the dissolution of poorly aqueous soluble compounds. The drug substance needs to be dissolved in gastric fluids to get the better absorption and bioavailability of an orally administered drug. Dissolution is the rate-controlling stage for drugs which controls the rate and degree of absorption. Usually, poorly soluble oral administrated drugs show a slower dissolution rate, inconsistent and incomplete absorption which can lead to lower bioavailability. The low aqueous solubility of BCS class II and IV drugs is a major challenge in the drag development and delivery process. Several technologies have been used in an attempt to progress the bioavailability of poorly water-soluble drug compounds which include solid dispersions, lipid-based formulations, micronization, solvent evaporation, co-precipitation, ordered mixing, liquid-solid compacts, solvent deposition inclusion complexation, and steam aided granulation. In fact, most of the technologies require excipient as a carrier which plays a significant role in improving the bioavailability using Hypromellose acetate succinate, Cyclodextrin, Povidone, Copovidone, Hydroxypropyl cellulose, Hydroxypropyl methylcellulose, Crospovidone, Starch, Dimethylacetamide, Polyethylene glycol, Sodium lauryl sulfate, Polysorbate, Poloxamer. Mesoporous silica and so on. This review deliberates about the excipients significance on bioavailability enhancement of drug products in a single platform along with pragmatically proved applications so that user can able to select the right excipients as per the molecule.
机译:如今大多数药物都进入了创新管道,水溶解度差。这里,赋形剂的影响将发挥重要作用以改善含水溶性化合物差的溶解。需要将药物溶解在胃液中以获得口服药物的更好吸收和生物利用度。溶解是控制吸收速度和吸收度的药物的速率控制阶段。通常,可溶性口服施氮药物差异较低,溶解速率较慢,不一致和不完全吸收,这可能导致生物利用度降低。 BCS II类和IV药物的低水溶性是阻力发育和交付过程中的主要挑战。几种技术已经试图被用来进步水难溶性药物化合物,其包括固体分散体,基于脂质的制剂,微粉化,溶剂蒸发,共沉淀的生物利用度,有序混合,液 - 固形体,溶剂沉积包合配合和蒸汽辅助造粒。事实上,大部分的技术都需要赋形剂作为在使用提高的生物利用度羟丙甲纤维素乙酸琥珀酸酯,环糊精,聚维酮,共聚维酮,羟丙基纤维素,羟丙基甲基纤维素,交聚维酮,淀粉,二甲基乙酰胺,聚乙二醇,月桂基硫酸钠起着显著作用的载体,聚山梨醇酯,泊洛沙姆。介孔的二氧化硅等。本篇审查刻意对单个平台中药品增强的赋形剂具有重要意义以及务实证明的应用,使用户可以根据分子选择正确的赋形剂。

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