Immediate Release Formulation of Valsartan Capsule and Evaluation of its Compatibility by Nonthermal Methods (original) (raw)
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Valsartan is a BCS class II antihypertensive drug whose bioavailability is dissolution rate limited. Various capsule formulations of valsartan were prepared using micro crystalline cellulose and sodium lauryl sulfate. Their dissolution profiles were compared with commercial marketed formulations. Formulation J was found to have similar t 90 values to marketed brands statistically. Influence of sodium lauryl sulfate on the solubility of valsartan was studied and was found to increase with the concentration of sodium lauryl sulfate. Compatibility of valsartan with micro crystalline cellulose and sodium lauryl sulfate was studied by non-thermal methods like HPLC and IR.
Formulation and Dissolution Study of Valsartan Immediate Release Tablets
In the present study, design of oral immediate release tablets of Valsartan by direct compression technique was carried out. The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV'S) in different ratios. The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate. To determine the best fit dissolution profile for the dosage forms. Valsartan tablets were formulated by using microcrystalline cellulose (diluents), potato starch, acacia (binder) and magnesium stearate (lubricant). The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. The In-vitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.
P Study of Valsartan Immediate Release Formulation and Dissolution Tablets
In the present study, design of oral immediate release tablets of Valsartan by direct compression technique was carried out. The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV'S) in different ratios. The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate. To determine the best fit dissolution profile for the dosage forms. Valsartan tablets were formulated by using microcrystalline cellulose (diluents), potato starch, acacia (binder) and magnesium stearate (lubricant). The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. The In-vitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.
Compatibility and stability of valsartan in a solid pharmaceutical formulation
Brazilian Journal of Pharmaceutical Sciences, 2013
Valsartan (VAL) is a highly selective blocker of the angiotensin II receptor that has been widely used in the treatment of hypertension. Active pharmaceutical ingredient compatibility with excipients (crospovidone, hypromellose, magnesium stearate, microcrystalline cellulose and titanium dioxide) is usually evaluated in solid pharmaceutical development. Compatibility and stability can be evaluated by liquid chromatography. Studies were performed using binary mixtures of 1:1 (w/w) VAL/excipient; samples were stored under accelerated stability test conditions (40 ºC at 75% relative humidity). The results indicate that VAL is incompatible with crospovidone and hypromellose, which reduced the VAL content and gave rise to new peaks in the chromatogram due to degradation products.
FORMULATION AND EVALUATION OF VALSARTAN TABLETS BY USING DIFFERENT BINDING AGENTS
The present study has a design to evaluate the valsartan conventional tablets by using various binders like acacia, sucrose, starch, gelatin, hydroxypropyl methylcellulose (HPMC), and polyvinyl-pyrrolidone (PVP). Employing the above selected six binding agents, valsartan tablets were prepared by wet granulation technique. The prepared granules were evaluated for their physic-chemical characteristics. The prepared tablets also evaluated for post-compression parameters like drug content, hardness, friability, and disintegration time and dissolution rate.The prepared valsartan tablets follow zero order kinetics. Formulation F2 showed better dissolution rate (89.37%) among all the formulations along with lowest disintegration time(2.5 minutes),which contains sucrose as a binding agent. From the ANOVA study, it was observed that there is a significant differencein the dissolution rate among the formulations. So F2 formulation is considered as optimized formulation.
Formulation and Evaluation of Valsartan Oral Dispersible Tablets by Direct Compression Method
The objective of the present study is to develop a pharmaceutically stable, cost effective and quality improved robust formulation of Valsartan Immediate Release tablets. The aim of work is related to the formulation and evaluation of 10mg of dispersible tablet. Valsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Total nine formulations were prepared by direct compression method in which the concentration of the superdisintegrants is varied to evaluate the effect on the disintegration time of valsartan mouth dissolving tablets. The superdisintegrants, involved in preparation are Sodium starch glycolate, Avicel PH 102, Low HPC. The prepared batches of tablets were evaluated for micromeritic parameters, weight variation, hardness, friability, wetting time, In vitro dispersion time, drug content and In vitro dissolution studies. In Formulations F1, F2, F3, releases 89.83%, 91.10%, 96.20%, respectively, Formulation F4, F5, and F6, which release 85.11%, 88.71% and 90.44% respectively and. Formulation F7, F8, F9, releases 78.26%, 82.26%, 85.31%, respectively, at end of 15 minutes. Amongst all the developed formulations, valsartan mouth dissolving tablets formulated by using sodium starch glycolate as superdisintegrants, having hardness (3.7 Kg/cm 2 ), Friability (0.1356 %), Drug Content (9.9250.067 mg). and it is fulfilling all the parameters. It has shown good In vitro disintegration time (8.00 1.023 sec), In vitro dispersion time (14.33 1.24 sec), compared to other superdisintegrants. The optimized formulation (F3) containing Sodium starch glycolate, as superdisintegrant is producing best results compared to other formulations.
Formulation Optimization and In Vitro and In Vivo Preclinical Evaluation of Valsartan IR Tablets
The objective of the present study is optimization of Valsartan tablet formulation employing βCD, Starch 1500, and Soluplus by 2 3 factorial design to achieve NLT 85% dissolution in 10 min and to evaluate the optimized formulations by In Vitro and In Vivo (Preclinical) methods. Eight Valsartan tablet formulations were prepared using selected combinations of the three factors as per 2 3 factorial design. Valsartan tablets were prepared by direct compression method and were evaluated. The individual and combined effects of the three factors βCD, Starch 1500 and Soluplus are highly significant (P < 0.01) in influencing the dissolution rate of Valsartan tablets.Valsartan tablet formulations F b, F ab, F bc and F abc disintegrated rapidly and gave very rapid dissolution of Valsartan, 92.4%, 99.4% ,96.2% and 99.2% in 10 min respectively. The increasing order of dissolution rate (X 2 X 3 ) Based on the above equation, the formulation of optimized Valsartan tablets with NLT 85% dissolution in 10 min require βCD at 1:3.5 ratio of drug: βCD, Starch 1500 at 24.37% of drug and βCD content , and Soluplus at 1% of drug and βCD content. The optimized Valsartan tablet formulation gave 85.75% dissolution in 10min fulfilling the target dissolution requirement. The optimized Valsartan IR tablet formulation developed exhibited rapid absorption, higher plasma concentrations and higher bioavailability (123.5%) when compared to Valsartan market product. Hence formulation of Valsartan IR tablets with NLT 85% dissolution in 10 min could be optimized by 2 3 factorial design.
A statistical study on the formulation development of sustained release tablets for valsartan sodium
MOJ Drug Design Development & Therapy, 2018
Objective: The purpose of the current research work was to study effect of formulation variables in a statistical way for the SR formulations of Valsartan sodium. Methods: Valsartan sodium is an antihypertensive agent angiotensin‒II receptor blocker belongs to BCS class‒III agent. SR tablet formulations of Valsartan sodium were formulated using variable quantities of HPMCK100M and Xanthan Gum by direct compression method. quantities of polymers was chosen as independent variables, X1 and X2 respectively whereas, time required for dissolution 10%(t10%), 50%(t50%), 75%(t75%) and 90%(t90%) of drug from formulation were chosen as dependent variables. 9 formulations were prepared and evaluated for various pharmacopoeial tests. Results: The results reveals that all formulations were found to be with in the acceptable limits and release rate profiles of all formulations were fitted to kinetic models. The statistical parameters were determined. Polynomial equations were developed for dependent variables. Validity of them was checked by countercheck formulations (C1 ,C2 ). According to SUPAC guidelines, formulation (F4) containing mixture of 12% HPMCK100M and 16% Xanthan gum, was found to be identical formulation (dissimilarity factor f1 =1.763, similarity factor f2 =86.747 & No significant difference, t=0.0478) to marketed product (VALZAAR). Conclusion: Formulation F4 follows First order kinetics, Non‒Fickian Diffusion Anomalous Transport. (n=0.826). Keywords: valsartan sodium, 32 factorial design, sustained delivery, Hpmck100m, Xanthan gum, first order kinetics, anomalous transport.
Dissolution enhancement of valsartan using sublimating agent for the formulation of porous tablet
Der Pharmacia Lettre, , 2016
Valsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARB's). The drug has low bioavailability, it can be increased by enhancing solubility in gastric fluids using rapid disintegration. By that mechanism, the porous compacts of valsartan having improved solubility were prepared and the dissolution profile is noted. The valsartan loaded porous compacts are prepared using micro crystalline cellulose as carrier material, lactose as diluent, ammonium carbonate as subliming agent & talc as glidant. FT-IR was used to evaluate the drug-polymer interaction. The dry granules of valsartan were prepared in different concentrations of sublimating agent and compressed. The resultant compacts are evaluated for their actual drug content (assay), morphology, flow properties, disintegration &dissolution rate. The valsartan porous tablets shows better disintegration, and the best dissolution rates compared to normal tablets. The formulations (F 4 , F 5 , and F 6) dried at 75ºC for 8hr has shown better drug release than air dried formulations (F 1 , F 2 , F 3). The pre compression & post compression studies of prepared compacts is under limits. The average pore size distribution is found as 736nm.The formulation F6 and process can be easily scaled up and can be easily employed in large scale production because the process is simple, cost effective and precise and also yields reproducible good result.
The enhancement of aqueous solubility, physicochemical and micromeritics properties of poorly soluble drugs is of major concern in pharmaceutical formulation industries. It is observed in the drug industry that on average more than 1/3 of newly drugs are poorly water-soluble. Poor “drug like” properties of lead compounds lead to ineffective absorption from the site of administration, less bioavailability which has been designated as an important part of the high clinical failure. In the present work, Valsartan, nonpeptide, orally active and specific angiotensin II antagonist acting on the AT1 receptor subtype belongs to BCS class II drug (highly permeable and low soluble) is used as lead compound. A simultaneous DSC, FT-IR, SEM, XRPD micro spectroscopy, dissolution study and micromeritics properties studies was used to quickly investigate the Co-Crystal. Tablet formulation was developed by direct compression method and there evaluation was performed.