Preparation and comparative evaluation of liquisolid compacts and solid dispersions of Valsartan

Lakshmi, P. K.; Srinivas, Chava; Kalpana, B.

doi:10.3329/sjps.v4i2.10440

Cited by 8 publications

(3 citation statements)

References 6 publications

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“…Hence, improving the saturation solubility and dissolution rate of poorly water-soluble drugs is very important and significantly challenging to pharmaceutical researchers seeking to achieve optimum absorption of new drug candidates. [ 2 3 ] In this research work, we addressed this issue by taking ezetimibe as a model compound. We particularly focused on amorphous nanosuspensions to enhance the bioavailability of ezetimibe.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of amorphous ezetimibe nanosuspensions intended for enhancement of oral bioavailability

Thadkala

Nanam

Rambabu³

et al. 2014

Int J Pharma Investig

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Objective:The objective of this study was to prepare and investigate better and stable amorphous ezetimibe nanosuspensions for oral bioavailability enhancement.Materials and Methods:Nanosuspensions of ezetimibe were prepared by solvent-antisolvent precipitation technique using the surfactant, Tween 80 as stabilizer. The nanosuspension preparation was optimized for particle size by investigating two factors that is, solvent:antisolvent ratio and surfactant concentration, at three levels. The formulations were characterized for particle size, surface morphology, crystallinity, zeta potential, saturation solubility, in vitro drug release and in vivo drug absorption.Results:The nanosuspensions of ezetimibe were successfully prepared using solvent-antisolvent precipitation. The two factors solvent:antisolvent ratio and surfactant concentration influenced the particle size of the nanosuspensions prepared. Nanosuspensions were smooth and spherical. The X-ray powdered diffraction and differential scanning calorimetry results indicated that the antisolvent-solvent method led to the amorphization of ezetimibe. Under storage, the amorphous ezetimibe nanosuspensions demonstrated significant physical stability. Ezetimibe nanosuspensions increased the saturation solubility to an extent of 4-times. Ezetimibe nanosuspensions completely dissolved in the dissolution medium within 1 h, while pure drug was dissolved up to 42% during same time. The Cmax with ezetimibe nanosuspension was approximately 3-fold higher when compared with that of ezetimibe conventional suspensions administered orally.Conclusions:Stable amorphous ezetimibe nanosuspensions were successfully prepared and these nanosuspensions demonstrated dramatic improvement in oral bioavailability of the active.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterization of amorphous ezetimibe nanosuspensions intended for enhancement of oral bioavailability

Thadkala

Nanam

Rambabu³

et al. 2014

Int J Pharma Investig

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“…Percentage practical yield was calculated to know about per cent yield or efficiency of any method; thus, it helps in the selection of the appropriate method of production. Solid dispersion was collected and weighed to determine practical yield (PY) from the following equation [6]. PY (%) = practical mass (solid dispersion) / Theoretical mass x100…”

Section: Percent Practical Yieldmentioning

confidence: 99%

Formulation and Evaluation of Aripiprazole Oral Disintegrating Tablets

Navya

Damagundam²,

Jupally³

et al. 2022

JPRI

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Aim: This work aims to develop oral disintegrating tablets from solid dispersion of aripiprazole that are capable of enhancing solubility. Methodology: Aripiprazole an antipsychotic is a BCS class IV drug with Oral bioavailability of 87%. To enhance the solubility of this drug the solid dispersions were prepared by using a combination of β-Cyclodextrin and PVP K30 in 1:1, 1:2 by using a physical mixture and solvent evaporation method. The prepared solid dispersions were analyzed for all the physical parameters and drug excipient interactions. The solid dispersion was optimized for the preparation of oral disintegrating tablets by direct compression technique using different concentrations of various natural super disintegrants namely Tapioca starch, Amorphophallus campanulactus, and synthetic super disintegrants namely Sodium starch glycolate, crospovidone. Results: FTIR showed that the drug and excipients are compatible with each other. Among all the solid dispersion formulations SCD6 (Drug: β-cyclodextrin) shows a high percentage of drug release i.e., 98.58±0.28% for 45 min, and solubility was found to be 0.954±0.32mg/ml. Percentage practical yield was found to be 98.36±0.14% and drug content was found to be 97.31±0.04%. SCD6 formulation was optimized for the preparation of oral disintegrating tablets. The post-compression parameters of all the prepared tablets were within the limits. Among all, F3 formulations containing tapioca starch, 7.5% were found to possess a better disintegration time (28±1.52sec) and in-vitro dissolution (98.64±0.29% for 45min). Conclusion: It can be concluded that solid dispersions of Aripiprazole incorporated in oral disintegrating tablets are a very useful approach for better release of Aripiprazole in an efficient manner.

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“…The liquisolid compact weighing 250mg of sample was dissolved in methanol in 100ml volumetric flask. From the stock solution, 1ml was taken and diluted to 100ml with phosphate buffer pH 6.0 and the solution was analyzed spectrophotometrically at 482nm, using 13.5 mol/L sulfuric acid as color developing agent [16].…”

Section: Drug Contentmentioning

confidence: 99%

Formulation and evaluation of liquisolid compact of azithromycin dihydrate

Bhattacharyya¹,

Pasha²,

VERMA³

et al. 2019

Sanat

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Azithromycin dihydrate is a macrolide antibiotic and belongs to BCS class II drugs. The present study aims at the preparation of liquisolid compact of azithromycin dihydrate with an aim to improve the solubility of the drug. The liquid solid system uses a nonvolatile solvent to dissolve the drug. The solution or suspension of drug is converted into a free flowing dry and compressible powder in an admixture of coating and carrier material calculated mathematically. In this study Avicel PH102 and Aerosil 200 were used as carrier and coating material respectively. Propylene glycol was used as the nonvolatile solvent. Using different excipient ratio six formulations were made and evaluated for flowability and compressibility characteristics. Drug excipient interaction study was performed through Fourier transform infrared spectroscopy (FTIR). The formulations were subjected to statistical analysis. Optimization of the formulation was done through JMP V8.0 software. The optimized formulations were evaluated for flowability, compressibility study, thermal analysis by differential scanning calorimetry (DSC) and comparative dissolution study with pure drug. The optimized formulations showed a good flow property and compression characteristics. The FTIR study revealed no physical interaction of the drug with the excipient. The DSC thermograms proved the conversion of crystalline structure of the drug into its amorphous form. The comparative dissolution study of the optimized formulations with the pure drug revealed significant improvement of solubility of azithromycin dihydrate in liquid solid compact. Therefore, it can be concluded that a free flowing, non-adherent, dry and compressible powder of azithromycin dihydrate can be prepared using liquid solid compact technology.

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Preparation and comparative evaluation of liquisolid compacts and solid dispersions of Valsartan

Cited by 8 publications

References 6 publications

Preparation and characterization of amorphous ezetimibe nanosuspensions intended for enhancement of oral bioavailability

Preparation and characterization of amorphous ezetimibe nanosuspensions intended for enhancement of oral bioavailability

Formulation and Evaluation of Aripiprazole Oral Disintegrating Tablets

Formulation and evaluation of liquisolid compact of azithromycin dihydrate

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