Abstract
Aim: The present research work was carried out to develop Valsartan and Amlodipine capsules using micro tablets and to evaluate the in-vitro drug release characteristics. The study was targeted to determine the systemic concentrations using in-vivo prediction.
 Study Design: The in vivo parameters along with the marketed Valsartan and Amlodipine product was predicted using WinNonlin® software external prediction method.
 Place and Duration of the Study: The present work was carried out at Pacific Academy of Higher Education and Research University, Udaipur between the duration of February-2019 to November-2019.
 Methodology: The dissolution studies were performed for test and reference products in 900ml Phosphate buffer (pH 6.8), and the USP Type II apparatus at 50 RPM with a sinker. The in vivo pharmacokinetic prediction was performed using WinNonlin® Software. A mechanistic oral absorption model was built in Phoenix® WinNonlin® 8.2 software (Certara, Princeton, NJ, 08540, USA).
 Results: The in-vitro dissolution studies were comparable between the test product and the reference product. The Similarity factor achieved was 61.7 and 84.8 for Amlodipine and Valsartan test product in comparison with the reference product. An average percent prediction error for Cmax and AUC for both Valsartan and Amlodipine achieved was less than 10% for all IVIVC models.
 Conclusion: The relatively low prediction errors for Cmax and AUC observed strongly suggest that the Valsartan and Amlodipine IVIVC models are valid. The average percent prediction error of less than 10% indicates that the correlation is predictive and allows the associated dissolution data to be used as a surrogate for bioavailability studies.
Highlights
Valsartan is an angiotensin-receptor blocker used to manage hypertension alone or in combination with other antihypertensive agents and to manage heart failure in patients who are intolerant to ACE inhibitors
*Corresponding author: E-mail: binurajkpharma@gmail.com; Binuraj et al.; JPRI, 33(46B): 335-349, 2021; Article no.JPRI.75660 and Area under the curve (AUC) for both Valsartan and Amlodipine achieved was less than 10% for all in-vivo correlation (IVIVC) models
Phoenix WinNonlin® IVIVC toolkit version 8.2 was used for the assessment of both Amlodipine and Valsartan absorption studies
Summary
Valsartan is an angiotensin-receptor blocker used to manage hypertension alone or in combination with other antihypertensive agents and to manage heart failure in patients who are intolerant to ACE inhibitors. Valsartan was initially approved in 1996 in Europe for the treatment of hypertension in adults. The structure of valsartan is shown in [Fig.1]. Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs. Valsartan is commonly used for the management of hypertension, heart failure, and Type 2 Diabetes-associated nephropathy, in patients who are unable to tolerate ACE inhibitors. ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization [1, 2]
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