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.
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.
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.
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.
Tadikonda R.R.,Avanthi institute of Pharmaceutical science
Journal of Applied Pharmaceutical Science | Year: 2014
Solid dispersion is one of the most widely used methods to enhance the solubility and dissolution rate of poor water soluble drugs. In the present study, flurbiprofen solid dispersions were prepared using solvent evaporation method by incorporating polyethylene glycol 20000 and evaluated for solubility studies, drug-carrier compatibility studies and in vitro dissolution studies. From the solubility studies, formulations F4 were selected to prepare in the form of tablets and compared with control tablets (conventional tablets using pure drug). From the results of in vitro dissolution study, tablets containing polyethylene glycol 20000 showed almost complete drug release within the 15 min. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F4 was 99.26±1.12%, 6.62%/min. These were very much higher compared to control tablets (34.95±1.29%, 2.33%/min). The relative dissolution rate was found to be 2.84 and dissolution efficiency was found to be 57.48 and it is increased by 3.5 fold with F4 formulation compared to control tablets (17.91). From the above results, it is concluded that the formulation of solid dispersions using polyethylene glycol 20000 is a suitable approach to improve the solubility and dissolution rate of flurbiprofen. © 2014 Bhaskar Daravath and Rama Rao Tadikonda et al.
Kumar S.K.,Jawaharlal Nehru Technological University |
Ramarao T.,Avanthi Institute of Pharmaceutical science |
Jayaveera K.N.,Jawaharlal Nehru University
International Journal of Pharma and Bio Sciences | Year: 2013
Tapentadol is a centrally acting synthetic analgesic, having biological half-life of 4 hours, its systemic bioavailability is 32%, is a suitable candidate for controlled release dosage form. The main aim of the present investigation was to formulate controlled release matrix tablets by using hydrophobic polymers like carnauba wax, eudragit L-100 and hydrogenated castor oil at different concentrations by using direct compression and melt granulation techniques, for an extended period of 24 hours to relieve moderate to chronic pain. Among all the formulations T-12 was selected as optimized one based on its physical parameters and in-vitro drug release profiles. The FTIR and DSC results of optimized formulation revealed that there is no incompatibility between drug and excipients used. For optimized formulation(T-12), the drug release mechanism was explored and explained by zero-order (r2=0.987), first-order (r2=0.947), Higuchi (r2=0.967) and Korsmeyer-peppas (r2=0.982 & n=0.855) equations, which explained the drug release follows zero-order and is fit for Higuchi equation & mechanism was anomalous diffusion i.e. diffusion and erosion. Biopharmaceutical study of the optimized (T-12) formulation in rabbit model showed 24 h prolonged drug release in-vivo. The results suggested that melt granulation technique, is a suitable method to formulate controlled release Tapentadol HCl and it can Perform therapeutically better than conventional immediate release dosage form.
Silpavathi L.,Avanthi Institute of Pharmaceutical science
Journal of Chemical and Pharmaceutical Sciences | Year: 2015
Metformin hydrochloride (MF.Hcl) is an anti-diabetic agent of biguanides class used for treating type-II diabetes. A number of generic tablets of MF. Hcl are available in global markets with diversified label claims nowadays. However, hardly any voluntary research organization takes the responsibility of checking the genuinely of the labels claimed by various manufacturers. The rationale of the present study was to quantify eight brands of MF. Hcl tablets marketed in India using non-aqueous titrimetry and UV-spectroscopic method and to ensure whether both the methods give similar results for all the brands as per their corresponding label claims such as uniformity of weight and percentage of purity. The result epitomizes that all the six brads out of eight had passed the assay specified in Indian Pharmacopoeia (IP), and the values obtained from uniformity of weight and weight variation tests were within the range as per the official standard. Nevertheless, the brands F2 and F3 had the highest and lowest percentage of purity respectively. However, the brand F5 failed the test. Thus, the study perhaps justified the fact that some volunteer organization should shoulder the responsibility of checking the pharmaceutical formulations available in the market to ensure that those are as per the prescribed standards of official monographs. © 2015, SPB Pharma Society. All rights reserved.
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.
PubMed | National Institute of Pharmaceutical Education and Research, Acharya Nagarjuna University and Avanthi Institute of Pharmaceutical science
Type: Journal Article | Journal: European journal of drug metabolism and pharmacokinetics | Year: 2016
Valsartan exhibits poor aqueous solubility and dissolution rate limited absorption. The lower solubility in the upper part of gastrointestinal tract (pH-dependant solubility) where its absorption window exists further contributes to the low oral bioavailability of valsartan.The present work was aimed to improve the in vivo pharmacokinetics of valsartan by preparing amorphous polymeric dispersions using Eudragit E 100 as carrier. Eudragit E 100 is a cationic polymer soluble in gastric fluid up to pH 5.0 and exhibits pH-dependent release. Hence, the dispersions prepared using Eudragit E 100 rapidly dissolves at lower pH presenting drug in molecularly dispersed and soluble form at its absorption site.Polymeric solid dispersions were prepared in different drug-to-carrier ratios. The prepared dispersions were evaluated for drug-carrier interactions, solid-state transitions and drug-release properties with the help of Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and in vitro dissolution studies. The optimized formulation containing valsartan was tested in rats for bioavailability and pharmacokinetic parameters and compared with that of valsartan pure drug.The results from FTIR studies indicated no interactions between drug and excipients. DSC studies confirmed reduction in crystallinity of drug. The dissolution studies performed in 0.1N HCl showed significant improvement (p<0.05) in the dissolution of valsartan. In vivo pharmacokinetic studies showed 199% relative bioavailability with significant improvement (p<0.05) in area under the curve compared to valsartan pure drug.Eudragit E 100 can be used to improve the dissolution of drugs that show low solubility at lower pH and thereby enhancing the bioavailability.
PubMed | National Institute of Pharmaceutical Education and Research and Avanthi Institute of Pharmaceutical science
Type: | Journal: Journal of drug delivery | Year: 2014
The objective of the present work was to obtain pH independent and improved dissolution profile for a poorly soluble drug, telmisartan using liquisolid compacts. Liquisolid compacts were prepared using Transcutol HP as vehicle, Avicel PH102 as carrier, and Aerosil 200 as a coating material. The formulations were evaluated for drug excipient interactions, change in crystallinity of drug, flow properties, and general quality control tests of tablets using Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), angle of repose, and various pharmacopoeial tests. In vitro dissolution studies were performed at three pH conditions (1.2, 4.5 and 7.4). Stability studies were performed at 40C and 75% RH for three months. The formulation was found to comply with Indian pharmacopoeial limits for tablets. FTIR studies confirmed no interaction between drug and excipients. XRD and DSC studies indicate change/reduction in crystallinity of drug. Dissolution media were selected based on the solubility studies. The optimized formulation showed pH independent release profile with significant improvement (P < 0.005) in dissolution compared to plain drug and conventional marketed formulation. No significant difference was seen in the tablet properties, and drug release profile after storage for 3 months.