Abstract：
The advent of HIV-Integrase inhibitors (IN) has marked a significant impact on the lives of HIV patients. Since the launch of the first anti retro-viral drug \"Azidothymidine\" to the recent advances of IN inhibitors, about 27.4 million people benefit by antiretroviral therapy (ART). The path had been challenging due to many crossroads, leading to the discovery of newer targets. One such recent ART target is Integrase. Use of Integrase inhibitors has surpassed the usage of all other ART owing to a strong barrier to resistance and have been reported to be the first-line therapy. Raltegravir, Elvitegravir, Dolutegravir and Bictegravir are US FDA approved IN inhibitors. The high usage of ART created an opportunity to study various analytical techniques for IN inhibitors. Hitherto, no review encompassing all IN inhibitors is presented. Herein, this review describes the analytical techniques employed for IN inhibitors estimation and quantification reported in the literature and official compendia. Literature suggests that most studies focus on LC-MS/MS and HPLC methods for drug estimation, and few reports suggest spectrophotometric, spectrofluorimetric and electrochemical methods. Furthermore, the review presents the techniques that describe the quantification of integrase drugs in various matrices. Although, antiretroviral drugs are extensively used but data suggests that limited studies have been conducted for determination of impurity profile and stability. This therefore, presents a scope to detect and validate impurities in order to meet ICH guidelines for their limits and further to improve the quality and safety of antiretroviral drugs.
摘要：
HIV-整合酶抑制剂(IN)的出现对HIV患者的生活产生了显著影响。自从第一个抗逆转录病毒药物“叠氮胸苷”推出以来，IN抑制剂的最新进展，约2740万人受益于抗逆转录病毒疗法（ART）。由于许多十字路口，这条路一直充满挑战，导致发现新的目标。一种这样的最近的ART靶标是整合酶。整合酶抑制剂的使用由于对抗性的强屏障而超过了所有其他ART的使用,并且已被报道为一线疗法。拉特格韦,Elvitegravir,Dolutegravir和Bictegravir是美国FDA批准的IN抑制剂。ART的大量使用为研究IN抑制剂的各种分析技术创造了机会。到目前为止，目前尚无涵盖所有IN抑制剂的综述。在这里，这篇综述描述了文献和官方汇编中报道的用于IN抑制剂评估和定量的分析技术。文献表明，大多数研究集中在LC-MS/MS和HPLC方法用于药物评估，很少有报告建议使用分光光度法，荧光光谱法和电化学方法。此外，该综述介绍了描述各种基质中整合酶药物定量的技术。虽然,抗逆转录病毒药物被广泛使用，但数据表明，对杂质谱和稳定性的测定进行了有限的研究。因此,提出了检测和验证杂质的范围，以满足ICH指南的限制，并进一步提高抗逆转录病毒药物的质量和安全性。
