Research paper description Dr. ARM


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Uploaded on Jan 21, 2022

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Lopinavir is an antiviral drug, it has poor solubility as well as permeability in the gastrointestinal tract. The absorbed drug also is driven out of the cell by a cellular mechanism called P-GP efflux. All this leads to poor absorption and bioavailability. To escape Pg P efflux coadministration of another drug Ritonavir is done which preferentially undergoes PGP efflux and improves the bioavailability of lopinavir.

Category Education

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Research paper description Dr. ARM

Research paper of Dr. Ashwini Madgulkar for the month of April 2021 Title: Improvement of Oral Bioavailability of Lopinavir Without Co-administration of Ritonavir Using Microspheres of Thiolated Xyloglucan Authors: Ashwini R. Madgulkar, Mangesh R. Bhalekar, Ashwini A. Kadam Journal Details: American Association of Pharmaceutical Scientists PharmSci Tech (# 2017) Publisher: Cross mark Description: Lopinavir is an antiviral drug, it has poor solubility as well as permeability in gastrointestinal tract. The absorbed drug also is driven out of cell by a cellular mechanism called P-gp efflux. All this leads to poor absorption and bioavailability. To escape Pg P efflux coadministration of another drug Ritonavir is done which preferentially undergoes PgP efflux and improves bioavailability of lopinavir. This research was aimed at overcoming this limitation by formulating microspheres of lopinavir using thiolated xyloglucan (thiomer) as carrier. The thiomers are polymers which can improve permeation across intestinal cells and inhibit the Pg P efflux mechanism. This enabled 3.15 times enhancement of permeation of lopinavir from microspheres was enhanced. And improved bioavailability by 3.22-fold over combination of lopinavir and ritonavir in study done on experimental animals. Thus, thiomers not only improve bioavailability but also reduce the coadministration of ritonavir thus reducing cost and drug load in body. Photographs: