Forced degradation and its analysis play a crucial role in the development and production of pharmaceutical products at various stages. Such studies include the assessment of appropriate drug candidates, product development, as well as comparability studies, clarification of probable intermediates and identification of by-products, and the development of stability-indicating technologies. The stability of drugs can be analyzed with Forced degradation study, which gives perspective knowledge of the molecule's stability as well as the degradant that is produced during the drug's shelf life. In this review on stability-indicating methods for FDA approved antiretroviral drugs from such as Zidovudine
Background:
CCR5 and/or CXCR4 receptors on CD4+ T cell membranes are the active sites for HIV to bind. The different classes of drugs have unique mechanism of action to cease the virus but we are concentrating in the first class i.e. NNRTI that destroys the virus while it binds to the cell surface gp120 protein. The drugs are having several impurities that can be genotoxic and few are reported in the monographs.
Objective:
This study proposes the affinity of the impurities to the active site through molecular docking to a receptor (PDB ID 4MBS) from the library of analogues available for the antiretroviral drugs. As these drugs are taken for long term, this study will give a prominent idea for testing the impurities and its genotoxicity.
Method:
We have done molecular docking of 37 impurities and drugs with GLIDE module of schrodinger software for their binding affinities. In this study, receptor CCR5 and/or CXCR4 is selected containing glycoprotein that mediates virus binding to CD4+ T cell.
Results:
Didanosine E and Zidovudine D shows maximum and minimum score respectively. The selected impurities were interfering with the active binding site that may lead to any ADR or reduce the effect of API.
Conclusion:
Conclusively, a significant role is played by Protein-Ligand interaction in structural based designing. Summarizing that there might be genotoxicity effect due to competition between API and the impurities. The molecular docking was used to study the binding mechanism and to establish the docking score along with the activity. The outcome of the study can be used to design and development of novel compounds having genotoxicity.
Background: A hyphenated technique is blend or coupling of two distinctive analytical methods like chromatographic and spectral methods with appropriate interface.
Objective: This article describes about the various hyphenated techniques, a brief note on their instrumentation and working principles that are used in the current setup of industries. Like-wise their remarkable improvement and efficiency over the past decade. The techniques like single quadrupole inductively coupled mass spectrometry (ICP-Q-MS), ICP- Triple quadrupole mass spectrometry (ICP-QQQ), Liquid chromatography-Two -dimensional Gas chromatography mass spectrometry (LC-GCXGC-MS/MS), Two dimensional liquid chromatography (2D-LC), Fourier transform near infrared spectroscopy (FT-NIR) ,etc. are considered as recent improvements in this trend.
Conclusion: This development in the hyphenated techniques supports in different scientific fields, biomedical research, food and drug analysis. In addition to this improvement produced remarkable dimensional changes in the natural product analysis and elemental specifications.
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