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

14th International Conference on Science, Engineering and Technology

自然科学;工业技术

Vadlamudi, Manoj Kumar^1,2 ; Dhanaraj, Sangeetha^1

School of Advanced Sciences, VIT University, Vellore, Tamil Nadu

632 014, India^1

Analytical Research and Development, Ashland India Private Limited, Hyderabad, Telangana

500 078, India^2

关键词: Aqueous solubility;    Bioavailability enhancements;    Degree of absorption;    Hydroxypropyl cellulose;    Hydroxypropyl methylcellulose;    Inclusion complexation;    Poorly water-soluble drugs;    Solvent evaporation;   

Others  :  https://iopscience.iop.org/article/10.1088/1757-899X/263/2/022023/pdf
DOI  :  10.1088/1757-899X/263/2/022023

来源: IOP

【 摘 要 】

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 drug 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.