Abstract
Objective: The main purpose of this study was to formulate and statistically evaluate 300 mg floating tablets of valsartan.
 Methods: Floating tablets of valsartan was prepared in 16 station rotary punching machine by considering 300 mg of valsartan as drug, 40-60 mg of hydroxypropyl methylcellulose (HPMC) K100M and 20-40 mg of poly (styrene-divinylbenzene) as polymers and 20 mg of sodium bicarbonate as gas generating agents. Since upper stomach has maximum therapeutic window for valsartan absorption, hence Gastroretentive Floating Tablets (GRFTs) was prepared by implementing Box-Bentham Design. The pre and post compression parameters were optimized using Statistica 10 software. From the in vitro buoyancy and drug release studies and interpretation of statistical outcomes viz. Akaike Information Criterion (AIC), Bayesian Information Criterion (BIC), Root Mean Squared Error (RMSE), Dissolution Efficiency (DE), Mean Dissolution Time (MDT), desirability study, it was concluded that batch VF5 formulation was found to be the most optimized formulation.
 Results: The floating time of VF5 was found to be 132±0.33 sec, in vitro buoyancy time was 18 h, Akaike Information Criterion (AIC) was 54.97, Bayesian Information Criterion (BIC) was 5.13, percentage dissolution efficacy was 56.39%, mean dissolution time was 5.19hr. Further, six-month stability study was performed as per ICH QIA guideline. After performing two-way ANOVA within stability study response variables, it was confirmed that the interaction was most significant.
 Conclusion: Valsartan floating drug delivery system was successfully developed by considering HPMC K100M and poly (styrene-divinylbenzene) as polymers. Among all the nine batches, VF5 was found to be the best-optimized batch.
Highlights
Valsartan is basically an angiotensin II receptor antagonist
All the batches blend has well to passable flow and micropolitics
The average thickness of all the tablets was recorded using vernier calliper, VF6 batch recorded 5.1±0.15 mm thickness; which was considered to be minimum among all the batches, where else VF7 recorded maximum thickness, which was recorded around 5.8±1.82 mm
Summary
Valsartan is basically an angiotensin II receptor antagonist. It has partial affinity for type I angiotensin receptor. Valsartan helps to reduce the blood pressure by blocking the action of angiotensin, which tenses to dilate blood vessels. It has versatile use in the treatment of Congestive Heart Failure (CHF), Post-Myocardial Infraction (MI). Valsartan has higher therapeutic window at upper stomach. To target the upper stomach, Gastro Retentive Drug Delivery System (GRDDS) is one of the best approaches for valsartan drug delivery [4]. Valsartan has only 3% oral bioavailability, which means improvement of its bioavailability by sustaining its duration of drug release could be a novel approach [5]. The basic interest of this research was to establish a proper statistical model and based on that optimizing best formulation
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