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Rani, Gampa Tulja
- Prediction of In-vivo Performance of Naproxen and Esomeprazole Magnesium Delayed-Release Tablets using Biorelevant Dissolution Tests
Authors
1 Department of Pharmacy, Annamalai University, Annamalai Nagar, Chidambaram − 608002, Tamil Nadu, IN
2 Malla Reddy Pharmacy College, Maisammaguda, Hyderabad − 500014, IN
Source
Asian Journal of Pharmaceutical Research and Health Care, Vol 12, No 2 (2020), Pagination: 63-74Abstract
Main objective of this research work was to develop a biorelevant dissolution method by correlating the in-vivo behavior of Naproxen and Esomeprazole magnesium delayed release tablets 500/20mg, when administered orally under pre-prandial condition. The target dissolution profile for bio-relevant dissolution media was derived, by deconvoluting mean blood plasma concentration time profile of Naproxen and Esomeprazole, achieved after oral administration under pre-prandial condition. The dissolution media volume and RPM were optimized using full factorial design of experiment. The dissolution profile observed with office of generic drugs recommended dissolution media was faster in release for Naproxen part and slower in release for Esomeprazole part in comparison to target release of bio-relevant dissolution method, with the F2 value of 31 for Naproxen and 29 for Esomeprazole. USP Apparatus-I with fasted state simulated gastro intestinal change over dissolution media were used for method development. Based on ANOVA results, for Naproxen part, 250ml of fasting change over dissolution medium, and 50RPM, with the desirability factor of 0.508 was concluded as bio relevant dissolution medium. For esomeprazole part, the 900ml of fasting change over dissolution medium, and 100RPM, with the desirability factor of 0.479 was concluded as bio-relevant dissolution medium. The F2 value observed between in-vitro and in-vivo dissolution profile is 64 and 63, the regression co-efficient (R2) value of 0.987 and 0.997 for Naproxen and Esomeprazole respectively demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition. The developed method shall be used as a predictive in-vitro tool for evaluation Naproxen from Naproxen and Esomeprazole magnesium delayed release tablets, and also gives the advantage for claiming bio-waiver for remaining strengths.
Keywords
Bio-Relevant, Delayed Release, Esomeprazole, Magnesium, Naproxen, Pre-Prandial.Full Text
References
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- Biorelevant Dissolution Method Development for Dutasteride and Tamsulosin Hydrochloride Modified Release Capsule - A Prognostic Tool for Oral Drug Absorption
Authors
1 Department of Pharmacy, Annamalai University, Annamalai Nagar, Chidambaram – 608002, Tamil Nadu, IN
2 Malla Reddy Pharmacy College, Maisammaguda, Hyderabad – 500014, Telengana, IN
Source
Asian Journal of Pharmaceutical Research and Health Care, Vol 12, No 4 (2020), Pagination: 177-188Abstract
The research work was aimed to develop a biorelevant dissolution method for fixed dose combination containing Dutasteride 0.5 mg in immediate-release form and Tamsulosin 0.4 mg in modified-release form. Mean plasma concentration achieved after oral administration to human under pre-prandial condition are deconvoluted using Wagner-Nelson deconvolution method, to achieve target dissolution profile. The dissolution profile observed using office of generic drugs recommended dissolution media was observed to be faster than the target dissolution profile. Tamsulosin being a modified-release multiparticulate system, biorelevant dissolution method was developed with Fasted state simulated change over dissolution media, using USP Apparatus 3 (reciprocating cylinder). Dutasteride being an immediate-release form, dissolution method was developed with single dissolution media, by extending the dissolution run time upto Cmax. Dissolution media, media volume and Dips Per Minute (DPM) are optimized by performing full factorial design of experiment. The ANOVA result interprets the biorelevant dissolution media for Tamsulosin part is 250 ml of Fasted state simulated change over dissolution media with 15 DPM, based on desirability factor of 0.7768 and for Dutasteride part 250 ml of pH 6.5 Fasted state simulated intestinal fluids with 7 DPM, based on desirability factor of 0.8988. The regression co-efficient (R2) value of 0.999 and 0.996 demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition for Tamsulosin and Dutasteride respectively. The developed method shall be used as a predictive in-vitro tool for evaluation of in-vivo performance under pre-prandial condition.
Keywords
Deconvolution, Dutasteride, Pre-prandial, TamsulosinFull Text
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