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Rama Rao T.,Avanthi Institute of Pharmaceutical science
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2014

Pioglitazone hydrochloride is an oral antidiabetic drug used in the treatment of Type-II diabetes. It is soluble in acidic pH and absorption occurs only in proximal intestine. The objective of the present investigation was to formulate a Gastroretentive dosage form of Pioglitazone Hydrochloride to prolong the residence of drug in its absorption area. Buoyant tablets were formulated by direct compression method using different concentrations of (10%, 20% and 30% w/w) HPMC K15M as matrix former and sodium bicarbonate in the concentration of (10%, 15% and 20% w/w) as gas generating agent. The effect of variation in the concentration of polymer and sodium bicarbonate on drug release profile and floating properties were investigated. Formulations were evaluated for various physical parameters like hardness, thickness, weight variation, friability, buoyancy studies, In-vitro dissolution and percentage swelling studies. All formulations are within Pharmacopoeial specifications for physical parameters. An In-vitro buoyancy study reveals that all batches of formulations floats instantaneously. In-vitro dissolution studies reveal that increasing the polymer concentration led to retardation of drug release. Percentage swelling studies revealed that increasing the polymer concentration increased % swelling. The drug release of optimized formulation (F9) follows the Higuchi kinetic model, and the mechanism is found to be Fickian according to Korsmeyer-Peppas model (n value is 0.68). The similarity factor (f2) is found to be 59 for the optimized formulation. FTIR, DSC study reveals that there is no drug-excipient interaction. Source

Chella N.,National Institute of Pharmaceutical Education and Research | Chella N.,Acharya Nagarjuna University | Tadikonda R.,Avanthi Institute of Pharmaceutical science
Drug Development and Industrial Pharmacy | Year: 2015

Solid dispersion (SD) technique is a promising strategy to improve the solubility and dissolution of BCS class II drugs. However, only few products are marketed till today based on SD technology due to poor flow properties and stability. The present work was intended to solve these problems by using combination approach, melt dispersion and surface adsorption technologies. The main aim of the present work is to improve the absorption in the stomach (at lower pH) where the absorption window exists for the drug by improving the dissolution, resulting in the enhancement of oral bioavailability of poorly soluble, weakly acidic drug with pH dependant solubility, i.e. valsartan. Melt dispersion granules were prepared in different ratios using different carriers (Gelucire 50/13, PEG 8000 and Pluronic F-68) and lactose as an adsorbent. Similarly, physical mixtures were also prepared at corresponding ratios. The prepared dispersion granules and physical mixtures were characterized by FTIR, DSC and in vitro dissolution studies. DSC studies revealed reduction in the crystallinity with a possibility of presence of amorphous character of drug in the dispersion granules. From dissolution studies, valsartan Gelucire dispersion (GSD4; 1:4 ratio) showed complete drug release in 30 min against the plain drug which showed only 11.31% of drug release in 30 min. Pharmacokinetic studies of optimized formulation in male Wistar rats showed 2.65-fold higher bioavailability and 1.47-fold higher Cmax compared to pure drug. The melt dispersion technology has the potential to improve dissolution and the bioavailability of BCS class II drugs. © 2014 Informa Healthcare USA, Inc. Source

Daravath B.,Acharya Nagarjuna University | Tadikonda R.R.,Avanthi Institute of Pharmaceutical science
Drug Development and Industrial Pharmacy | Year: 2015

Context: Development of solid dispersions is to improve the therapeutic efficacy by increasing the drug solubility, dissolution rate, bioavailability as well as to attain rapid onset of action. Objective: The present research deals with the development of solid dispersions of flurbiprofen which is poorly water soluble to improve the solubility and dissolution rate using gelucires. Materials and methods: In this study, solid dispersions were prepared following solvent evaporation method using gelucire 44/14 and gelucire 50/13 as carriers in different ratios. Then the formulations were evaluated for different physical parameters, solubility studies, DSC, FTIR studies and in vitro dissolution studies to select the best formulation that shows rapid dissolution rate and finally subjected to pharmacokinetic studies. Results and discussion: From the in vitro dissolution study, formulation F3 showed the better improvement in solubility and dissolution rate. From the pharmacokinetic evaluation, the control tablets produced peak plasma concentration (Cmax) of 9140.84 ± 614.36 ng/ml at 3 h Tmax and solid dispersion tablets showed Cmax = 11 445.46 ± 149.23 ng/ml at 2 h Tmax. The area under the curve for the control and solid dispersion tablets was 31 495.16 ± 619.92 and 43 126.52 ± 688.89 ng h/ml and the mean resident time was 3.99 and 3.68 h, respectively. Conclusion: From the above results, it is concluded that the formulation of gelucire 44/14 solid dispersions is able to improve the solubility, dissolution rate as well as the absorption rate of flurbiprofen than pure form of drug. © 2014 Informa Healthcare USA, Inc. All rights reserved. Source

Sahoo D.K.,Avanthi Institute of Pharmaceutical science
Journal of Liquid Chromatography and Related Technologies | Year: 2015

This paper demonstrates a chemometric-assisted RP-HPLC method for the simultaneous determination of azithromycin, secnidazole, and fluconazole using water:methanol (63:37% v/v) as mobile phase at a flow rate of 1.2 mL · min-1. The separation of the three drugs was achieved on an Xterra RP-18 column (250 × 4.6 mm ID, 5 μM) and the detection of the eluents was realized on a diode array detector at 210 nm wavelength. The combined effects of % methanol (organic phase) and flow rate, each at three levels influencing the chromatographic efficiency were investigated and optimized employing central composite design. Under the optimal condition, the percent relative standard deviations for precision study were in the range of 0.2-0.7% and 0.5-1.2% for standard and formulation, respectively. The limits of detection were 12.5, 0.62, and 1.7 μg · mL-1 and limits of quantification were found 37.5, 1.86, and 5.1 μg · mL-1 for azithromycin, secnidazole, and fluconazole, respectively. Consequently, the method has been effectively applied to their direct determination in the commercial formulation (combi-kit). © 2015 Copyright © Taylor & Francis Group, LLC. Source

Daravath B.,Acharya Nagarjuna University | Tadikonda R.R.,Avanthi Institute of Pharmaceutical science
Asian Journal of Pharmaceutical and Clinical Research | Year: 2014

Objective: The present research is aimed to investigate the effect of polyethylene glycol 4000 and 6000 as solid dispersion carriers on the solubility and dissolution rate of Meclizine hydrochloride. Methods: In this, meclizine hydrochloride solid dispersions were prepared by using solvent evaporation method and evaluated for solubility studies, drug-carrier compatibility studies and in vitro dissolution studies. Formulations F4 and F8 were selected to prepare the tablets and compared with control tablets (conventional tablets using pure drug). Results: From the in vitro dissolution studies, tablets containing polyethylene glycol 6000 showed almost complete drug release within the 20 min. The percent drug release in 20 min (Q20) and initial dissolution rate for formulation F8 was 99.26±1.62%, 4.96%/min. These were very much higher compared to control tablets (44.67±1.48%, 2.23%/min). The relative dissolution rate was found to be 2.22 and dissolution efficiency was found to be 57.94 and it is increased by 3.0 fold with F8 formulation when compared to control tablets (22.05). Conclusion: Formulation of the meclizine hydrochloride-polyethylene glycol solid dispersions is a suitable approach to improve the solubility and dissolution rate. Source

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