Pharmaceutics and Pharmacokinetics Division, CSIR-CDRI, Lucknow, India.
Academy of Scientific and Innovative Research, New Delhi, India.
Curr Pharm Des. 2019;25(9):987-1020. doi: 10.2174/1381612825666190130110653.
Bioavailability, one of the prime pharmacokinetic properties of a drug, is defined as the fraction of an administered dose of unchanged drug that reaches the systemic circulation and is used to describe the systemic availability of a drug. Bioavailability assessment is imperative in order to demonstrate whether the drug attains the desirable systemic exposure for effective therapy. In recent years, bioavailability has become the subject of importance in drug discovery and development studies.
A systematic literature review in the field of bioavailability and the approaches towards its enhancement have been comprehensively done, purely focusing upon recent papers. The data mining was performed using databases like PubMed, Science Direct and general Google searches and the collected data was exhaustively studied and summarized in a generalized manner.
The main prospect of this review was to generate a comprehensive one-stop summary of the numerous available approaches and their pharmaceutical applications in improving the stability concerns, physicochemical and mechanical properties of the poorly water-soluble drugs which directly or indirectly augment their bioavailability.
The use of novel methods, including but not limited to, nano-based formulations, bio-enhancers, solid dispersions, lipid-and polymer-based formulations which provide a wide range of applications not only increases the solubility and permeability of the poorly bioavailable drugs but also improves their stability, and targeting efficacy. Although, these methods have drastically changed the pharmaceutical industry demand for the newer potential methods with better outcomes in the field of pharmaceutical science to formulate various dosage forms with adequate systemic availability and improved patient compliance, further research is required.
生物利用度是药物的主要药代动力学特性之一，定义为给药剂量中未改变的药物部分到达体循环并用于描述药物的全身可用性。为了证明药物是否达到了有效治疗所需的理想全身暴露量，评估生物利用度是至关重要的。近年来，生物利用度已成为药物发现和开发研究中的重要课题。
我们对生物利用度及其增强方法领域进行了系统的文献综述，纯粹专注于近期的论文。使用 PubMed、Science Direct 等数据库和常规谷歌搜索进行了数据挖掘，对收集到的数据进行了详尽的研究和总结。
本次综述的主要目的是生成一个全面的一站式摘要，其中包括许多现有的方法及其在改善稳定性问题、物理化学和机械性质方面的药物应用，这些方法直接或间接地提高了水溶性差的药物的生物利用度。
新型方法的应用，包括但不限于纳米制剂、生物增强剂、固体分散体、基于脂质和聚合物的制剂等，不仅提高了生物利用度差的药物的溶解度和渗透性，而且提高了它们的稳定性和靶向效果。虽然这些方法极大地改变了制药行业对具有更好结果的新型潜在方法的需求，但在药物科学领域中，为了制定具有足够全身可用性和提高患者依从性的各种剂型，仍需要进一步的研究。
