Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release. Conclusion:The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

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“…Meloxicam characterization showed consistency with reported data of the crystalline nature of the pure drug [3,21,22].…”

Section: Discussionsupporting

confidence: 86%

Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Obaidat

Al-Taani

Al-quraan

2017

Int J Pharm Pharm Sci

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“…[23] Increased solubility may be due to the improved wettability of the CA particles in aqueous solution of Poloxamer 188. [24] Table 2 presents the values of the Gibbs free energy associated with the aqueous solubility of CA in the presence of poloxamer 188. The ΔGtr° values are all negative for poloxamer 188 at various concentrations, indicating the spontaneous nature of solubilization.…”

Section: Resultsmentioning

confidence: 99%

Improvement in Dissolution Rate of Cefuroxime Axetil by using Poloxamer 188 and Neusilin US2

Jammula¹,

Patra²,

Swain³

et al. 2013

Indian J Pharm Sci

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A combination of fusion and surface adsorption techniques was used to enhance the dissolution rate of cefuroxime axetil. Solid dispersions of cefuroxime axetil were prepared by two methods, namely fusion method using poloxamer 188 alone and combination of poloxamer 188 and Neusilin US2 by fusion and surface adsorption method. Solid dispersions were evaluated for solubility, phase solubility, flowability, compressibility, Kawakita analysis, Fourier transform-infrared spectra, differential scanning calorimetry, powder X-ray diffraction study, in vitro drug release, and stability study. Solubility studies showed 12- and 14-fold increase in solubility for solid dispersions by fusion method, and fusion and surface adsorption method, respectively. Phase solubility studies showed negative ΔG0tr values for poloxamer 188 at various concentrations (0, 0.25, 0.5, 0.75 and 1%) indicating spontaneous nature of solubilisation. Fourier transform-infrared spectra and differential scanning calorimetry spectra showed that drug and excipients are compatible with each other. Powder X-ray diffraction study studies indicated that presence of Neusilin US2 is less likely to promote the reversion of the amorphous cefuroxime axetil to crystalline state. in vitro dissolution studies, T50% and mean dissolution time have shown better dissolution rate for solid dispersions by fusion and surface adsorption method. Cefuroxime axetil release at 15 min (Q15) and DE15 exhibited 23- and 20-fold improvement in dissolution rate. The optimized solid dispersion formulation was stable for 6 months of stability study as per ICH guidelines. The stability was ascertained from drug content, in vitro dissolution, Fourier transform-infrared spectra and differential scanning calorimetry study. Hence, this combined approach of fusion and surface adsorption can be used successfully to improve the dissolution rate of poorly soluble biopharmaceutical classification system class II drug cefuroxime axetil.

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“…who reported that the total disappearance of the drug peak in the dissolved carrier indicates about the drug amorphization. [30]…”

Section: Resultsmentioning

confidence: 99%

In vitro dissolution study of atorvastatin binary solid dispersion

Jahan

Islam

Tanwir

et al. 2013

J Adv Pharm Technol Res

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The aim of the present study was to improve the solubility and dissolution rate of atorvastatin (ATV), a slight water-soluble drug, by solid dispersion (SD) technique using a hydrophilic carrier Poloxamer 188 (POL188). Physical mixing (PM) and solvent evaporation (SE) method were used to prepare ATV-SD where different drug-carrier ratios were used. Prepared formulations were characterized in their solid state by solubility study; differential scanning calorimetry, scanning electron microscopy, and Fourier transform infrared spectroscopy which demonstrated changes in the formulations supporting the improved solubility. Percent content of POL188 in the SD matrix was found to play the pivotal role in the improvement of dissolution property of ATV. In case of PM, highest enhancement in drug release was found for 1:3 ratio (P < 0.05, ANOVA Single factor) whereas in case of SE, 3:0.5 ratio of ATV-POL188 resulted the maximum enhancement in ATV release (P < 0.05, ANOVA Single factor). Analysis of dissolution data of optimized formula indicated the best fitting with Peppas-Korsmeyer model and the drug release kinetics was fickian diffusion. In conclusion, binary SD prepared by both PM and SE technique using POL188 could be considered as a simple, efficient method to prepare ATV solid dispersions with significant improvement in the dissolution rate.

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Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188

Cited by 80 publications

References 21 publications

Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Improvement in Dissolution Rate of Cefuroxime Axetil by using Poloxamer 188 and Neusilin US2

In vitro dissolution study of atorvastatin binary solid dispersion

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