Journal of Bioequivalence & Bioavailability

Eprosartan mesylate cocrystals and their enhanced oral bioavailability studies

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Jaswanth Santosh Bhandaru and Raghuram R Akkinepally

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

Co-crystallization is a useful technique for the enhancement of the physicochemical properties of the molecules. The poor
physiochemical properties of the API’s tend to show low oral bioavailability which leads to enhanced dosage and consequent
adverse profiles of the drugs to the patients. Eprosartan mesylate (EM), an angiotensin II antagonist, is used in the treatment of
hypertension exhibits poor bioavailability (13%) due to low absorption window. Hence we recently reported pharmaceutical cocrystals
of EM (EM-SUC, EM-SAL & EM- PABA) with improved solubility and dissolution profiles. The present abstract focuses on
the study of enhanced oral bioavailability of the EM co-crystals. Pharmacokinetic studies of EM co-crystals were performed using
animal models (male Wister rats) to evaluate bioavailability of the drug. Four groups (n=6) of rodents were orally administered with
pure EM (API suspended in water) and EM co-crystals (12.3 mg/ kg body weight in aq. solution) respectively. Serial blood samples
were collected at predetermined time points and were analyzed for EM plasma concentration using a validated HPLC assay method.
Pharmacokinetic and statistical data analysis was performed using Kinetica 5.0 and GraphPad Prism software. The results suggested
that the EM co-crystals showed enhanced AUC and Cmax than the pure drug. Mean retention time of the cocrystals was observed to
be high with low clearance values which suggest the enhanced absorption window of the prepared co-crystals. EM-SUC showed more
than 3 times (3.4 fold) enhancement in the relative oral bioavailability than the pure EM suggesting that the succinic acid as preferred
coformer for the preparation of the EM co-crystals.

Biography :

Jaswanth Santosh Bhandaru has completed his Master’s degree in Pharmacy from Panjab University and has a 1.5 yr of industrial experience. He is currently doing his
Doctoral research work on multi- component systems and supramolecular chemistry, particularly pharmaceutical cocrystals. He developed co-crystals of few antihypertensive
drugs and proved their improved physicochemical properties. He is very enthusiastic in developing systems for improving the oral bioavailability of the molecules and studies
their industrial applicability. He also has good publications to his credit.