Formulation And Evaluation Of Liquisolid Compacts Of Lornoxicam

Objective: Objective of the present investigation was to enhance the solubility and dissolution rate of poorly water-soluble drug lornoxicam using liquisolid technique with comparative determination of in vitro release profile of liquisolid compacts and conventional formulation of lornoxicam. Methods: Formulation was prepared by a liquisolid technique using different drug concentration in a liquid vehicle and different carrier/coating ratio. Prepared liquisolid compact was evaluated for Fourier transform infrared (FTIR) spectra analysis, differential scanning calorimetry (DSC), X-ray diffraction (P-XRD), scanning electron microscopy (SEM) and in vitro dissolution study. Results: The result showed that liquisolid compacts of lornoxicam displayed significantly higher drug release rate as compared to pure drug and conventional tablet prepared. The results of both DSC and X-ray crystallography indicated loss of crystallinity of the drug upon formulated into the liquisolid compact. Conclusion: Dissolution rate of the drug from liquisolid compacts was affected by changing the drug concentration and excipient ratio. The liquisolid technique appeared to be a promising approach for improving the dissolution of poorly soluble drug lornoxicam.

Improvement of physicochemical parameters of acyclovir using cocrystallization approach

ABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may result in improvement of bioavailability. Hansen solubility approach was used as a tool to predict the cocrystal formation of a drug with selected coformer. Cocrystals of acyclovir with various coformers were screened in order to enhance their water solubility. Cocrystals of the drug were prepared using various methods like solvent evaporation, wet grinding, and antisolvent addition. Formation of cocrystals by solvent evaporation method was found to be better method amongst all. Optimization of cocrystal formation was carried out by employing different solvents as well as the stoichiometric ratio of acyclovir with that of coformer. Synthesis of cocrystals was optimized using water as a solvent system resulted in good agreements. The potential cocrystal formation of acyclovir was characterized by IR, PXRD and DSC techniques. An in-vitro dissolution study was performed to determine the dissolution rate of cocrystals. The results suggest that acyclovir forms cocrystals with tartaric acid and the initial dissolution rate of synthesized cocrystals were considerably faster as compared to pure acyclovir.

In vitro-in vivo studies of the quantitative effect of calcium, multivitamins and milk on single dose ciprofloxacin bioavailability / 药物分析学报

Ciprofloxacin, commonly used in India as an anti-microbial for prolonged use in chronic and non-specific indications, may affect the bioavailability of the drug. The drug prescribed is commonly taken with multivitamins, calcium and milk. A simple and reliable analytical methodology obtaining a correlation with in vivo urinary excretion studies using UV and HPLC and in vitro dissolution studies (IVIVC) has shown a significant increase in elimination rate of ciprofloxacin co-administered with multivitamins, calcium and milk. Appreciable IVIVC results proved that dissolution studies could serve as an alternative to in vivo bioavailability and also support bio-waivers.

RP-HPLC-PDA method development and validation for the analysis of Tadalafil in bulk, pharmaceutical dosage forms and in-vitro dissolution samples.

The present work describes the development and validation of a simple, rapid, selective and reproducible RPHPLC method for the Analysis of Tadalafil in Bulk, tablets and In-Vitro Dissolution Samples. Analysis was performed on an Agilent, EclipseC18 column (150 mm × 4.6 mm, 5 􀟤m) with the mobile phase consisting of ammonium acetate (10 mM):methanol (35:65v/v) at a flow rate of 1.0 mL/min. UV detection was performed at 280 nm and the retention time for TDL was 4.6 minutes. The dissolution media composed of 0.5% SLS, using USP II (Paddle) Dissolution apparatus, at 50 RPM and temperature maintained 37.0 ± 0.5ͦ C. The method was validated according to ICH guidelines. The method was validated for specificity, accuracy, precision, ruggedness, limit of quantification, limit of detection and linearity. The system suitability parameters, such as , tailing factor, theoretical plate and relative standard deviation (RSD) for assay of five standard replicates, were well within the limits. The results of the studies showed that the proposed RP-HPLC method is simple, rapid, precise and accurate. Hence the method can be used for the routine Dissolution Profiling of Tadalafil as well as its assay in bulk and tablets.

Formulation and Evaluation of Oxcarbazepine Suspension: In vitro/In vivo Correlation.

Aims: Oxcarbazepine was formulated as suspension in order to perk up the palatability, augment bioavailability of the product, furthermore extended to estimate good degree of in vitro in vivo correlation (IVIVC). Study Design: Formulation and Evaluation of Oxcarbazepine Suspension: In Vitro/In Vivo Correlation Place and Duration of Study: Birla Institute of Technological Sciences- Hyderabad, India between July 2011 to January 2012 Methodology: Oxcarbazepine had poor aqueous solubility, thus the solubility was increased by hydrotropes then formulated into suspension using taragum as viscosity enhancer. Further validity of dissolution study was extended by In vitro/In vivo correlation using level A method. Results: These suspensions were observed for in vitro dissolution profile and studied for in vivo pharmacokinetic profile, from the obtained values, a level A IVIVC modeling was observed, interestingly from the results attained suspension showed almost 98% drug release (FDR) and 85% drug absorbed (FDA) in 90min. Fascinatingly, from the correlation between FDR and FDA, slope and regression co-efficient obtained was near to 1.0 indicated good linearity. Conclusion: In conclusion, a point-to-point link from the level A which was a keystone of acceptable and reliable correlation was achieved.

Prepraration of PLGA-PLL-PEG Nanoparticles Simultaneously Loaded with Daunorubicin and Tetrandrine / 中国药学杂志

OBJECTIVE: To prepare PLGA-PLL-PEG nanoparticles simultaneously loaded with daunorubicin (DNR) and tetrandrine (Tet).

Formulation and Evaluation of sustained release matrix tablets of Glipizide.

The aim of present investigation was to enhance the solubility of glipizide (BCS Class II). Glipizide is an oral antidiabetic agent with relatively short elimination half life. Inclusion complex of Glipizide with -cyclodextrin was prepared by kneading method and evaluated for its in-vitro release. Phase solubility studies were performed according to method reported by Higuchi and Connors which was classified as AL type characterized by apparent 1:1 stability constant. The Glipizide & Beta Cyclodextrin found to be compatible which was observed from FTIR spectra of Glipizide - CD Complex. The dissolution study of Glipizide - CD complex shows significant increase in the drug release than pure drug. Matrix Glipizide - CD complex tablet complex equivalent to 10 mg Glipizide were prepared by using Hydroxy propyl methyl cellulose (HPMC), Carboxy methyl cellulose sodium (NaCMC) and Microcrytalline cellulose (MCC). The tablets were evaluated for various tests like hardness, friability, disintegration and in-vitro dissolution studies.

HPLC method development for the simultaneous analysis of amlodipine and valsartan in combined dosage forms and in vitro dissolution studies

A simple, rapid and reproducible HPLC method was developed for the simultaneous determination of amlodipine and valsartan in their combined dosage forms, and for drug dissolution studies. A C18 column (ODS 2, 10 μm, 200 x 4.6 mm) and a mobile phase of phosphate buffer (pH 3.6 , 0.01 mol L-1):acetonitrile: methanol (46:44:10 v/v/v) mixture were used for separation and quantification. Analyses were run at a flow-rate of 1 mL min-1 and at ambient temperature. The injection volume was 20 μL and the ultraviolet detector was set at 240 nm. Under these conditions, amlodipine and valsartan were eluted at 7.1 min and 3.4 min, respectively. Total run time was shorter than 9 min. The developed method was validated according to the literature and found to be linear within the range 0.1 - 50 μg mL-1 for amlodipine, and 0.05 - 50 μg mL-1 for valsartan. The developed method was applied successfully for quality control assay of amlodipine and valsartan in their combination drug product and in vitro dissolution studies.

Desenvolveu-se método de HPLC rápido e reprodutível para a determinação simultânea de anlodipino e valsartana em suas formas de associação e para os estudos de dissolução dos fármacos. Utilizaram-se coluna C18 (ODS 2, 10 μm, 200 x 4,6 mm) e fase móvel tampão fosfato (pH 3,6, 0,01 mol L-1):acetonitrila: metanol para a separação e a quantificação. As análises foram efetuadas com velocidade de fluxo de 1 mL min-1 e à temparatura ambiente O volume de injeção foi de 20 μL e utilizou-se detector de ultravioleta a 240 nm. Sob essas condições, anlodipino e valsartana foram eluídas a 7,1 min e 3,4 min, respectivamente. O tempo total de corrida foi menor que 9 min. O método desenvolvido foi validado de acordo com a literatura e se mostrou linear na faixa de 0,1-50 μg mL-1 para anlodipino e de 0,05-50 μg mL-1 para valsartana. O método desenvolvido foi aplicado com sucesso para ensaios de controle de qualidade de associações de anlodipino e valsartana e nos estudos de dissolução in vitro.