Abstract
What is it? Darunavir is a protease inhibitor used in the treatment of HIV infection. It is an important drug of therapy cocktail for patients infected with the virus. On the market there are darunavir ethanolate tablets of 75, 150, 300, 400, 600 and 800mg, because this is the most stable form. It is commercialized by Janssen-Cilag with the name PrezistaTM.Why we started? This drug has low water solubility and poor bioavailability, therefore requires administration in doses relatively high to the success of the therapeutic effect. The complexation of drugs by using cyclodextrin is welcome in this respect to improve the solubility and hence increase the dissolution rate of poorly soluble drugs. A monograph about this compound has not been described, thus it is an extremely important quality control of darunavir to demonstrate its effectiveness and safety.What we did? Some existing analytical techniques have been discussed in this manuscript, focusing on bioanalytical and pharmaceutical quality control applications.What we found? This review showed the published analytical methods reported for the determination of darunavir and discuss about its characteristics and complexation with cyclodextrin.
Highlights
Protease inhibitors were a major therapeutic advance in the mid-1990s for the treatment of HIV infection, which resulted in increased life expectancy for patients who had failed therapies in earlier
Validation is an important part of the quality assurance program and aims to demonstrate that the analytical method is suitable for the intended proposal and that it is safe to be executed [19], being the procedures included in the standards of Good Manufacturing Practices (GMP) required by U.S FDA, and applied in pharmaceutical industries and should occur according to good laboratory practice (GLP) [20]
We performed a literature search on methods for analysis of darunavir and were found to detect the drug in tablets by thin layer chromatography (TLC), UV spectrophotometry, infrared spectroscopy (IR) and high performance liquid chromatography (HPLC) [21,22], in plasma by HPLC [3,15], ultra efficiency liquid chromatography coupled to mass spectrometry (UHPLC-MS) [23] and HPLC coupled with mass spectrometry (HPLC-MS) [4]
Summary
Protease inhibitors were a major therapeutic advance in the mid-1990s for the treatment of HIV infection, which resulted in increased life expectancy for patients who had failed therapies in earlier. The newest protease inhibitors, is a non-peptide synthetic analogue of amprenavir [1], which was approved by the U.S.FDA in June 2006 and in February 2007 the European Commission approved its marketing [2] It is effective in patients with experiments in antiretroviral treatments, such as those with HIV-1 strains that are resistant to more than one protease inhibitors [3]. The affinity of this union is 100 times higher than that of amprenavir, another protease inhibitor [4]. This review will examine the published analytical methods reported for determination of darunavir and discuss about its characteristics, complexation to β-cyclodextrin and methods of analysis of darunavir
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