Solid dispersion of meloxicam: Factorially designed dosage form for geriatric population

Pathak, Deepa; Dahiya, Sunita; Pathak, Kamla

doi:10.2478/v10007-007-0048-y

Cited by 37 publications

(22 citation statements)

References 7 publications

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“…So the reduction in the intensity of the PXRD peaks of meloxicam was due to dilution effect and not to conversion to an amorphous form because these carriers did not show any evidence of meloxicam conversion from crystalline to amorphous form. Also, SEM images showed partial inclusion of the crystalline drug inside the polymers in a particular manner (without aggregation) [34,35].…”

Section: Discussionmentioning

confidence: 99%

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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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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Section: Discussionmentioning

confidence: 99%

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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“…In recent years, interest in incorporating a surfaceactive carrier into solid dispersion has increased greatly and a high improvement in drug dissolution was reported (Serajuddin, 1999;Pathak et al, 2008). This approach has been reported to enhance the solubility, dissolution and bioavailability of many poorly water soluble drugs using various techniques including melting agglomeration and melting.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical characterization and solubility enhancement studies of allopurinol solid dispersions

Changdeo

Vinod

Shankar

et al. 2011

Braz. J. Pharm. Sci.

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Allopurinol is a commonly used drug in the treatment of chronic gout or hyperuricaemia associated with treatment of diuretic conditions. One of the major problems with the drug is that it is practically insoluble in water, which results in poor bioavailability after oral administration. In the present study, solid dispersions of allopurinol were prepared by solvent evaporation, kneading method, co-precipitation method, co-grinding method and closed melting methods to increase its water solubility. Hydrophilic carriers such as polyvinylpyrrolidone, polyethylene glycol 6000 were used in the ratio of 1:1, 1:2 and 1:4 (drug to carrier ratio). The aqueous solubility of allopurinol was favored by the presence of both polymers. These new formulations were characterized in the liquid state by phase solubility studies and in the solid state by differential scanning calorimetry, powder X-ray diffraction, UV and Fourier Transform Infrared spectroscopy. Solid state characterizations indicated that allopurinol was present as an amorphous material and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure allopurinol, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with polyvinylpyrrolidone showed highest improvement in wettability and dissolution rate of allopurinol. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer-Peppas model and the drug release kinetics primarily as Non-Fickian diffusion. Therefore, the present study showed that polyvinylpyrrolidone and polyethylene glycol 6000 have a significant solubilizing effect on allopurinol.Uniterms: Allopurinol. Polyethylene glycol 6000. Solid dispersions. Closed melting method. Dissolution enhancement.Alopurinol é fármaco comumente utilizado no tratamento de gota crônica ou hiperuricemia associada com o tratamento em condições diuréticas. Um dos maiores problemas com o fármaco é que este é praticamente insolúvel em água, o que resulta em baixa biodisponibilidade na administração oral. No presente estudo, dispersões sólidas de alopurinol foram preparadas pela evaporação do solvente, pelos métodos de amassamento, de coprecipitação, de comoagem e fusão fechada para aumentar sua solubilidade em água. Transportadores hidrofílicos, como polivinilpirrolidona, polietilenoglicol 6000 foram utilizados nas proporções de 1:1. 1:2 e 1:4 (fármaco: transportador). A solubilidade aquosa do alopurinol foi favorecida pela presença de ambos os polímeros. Estas novas formulações forma caracterizadas no estado líquido pelos estudos de solubilidade de fase e no estado sólido pela calorimetria diferencial de varredura, difração de Raio-X, espectroscopia de UV e de IV com transformada de Fourier. As caracterizações do estado sólido indicaram que o alopurinol estava presente como material amorfo e embebido em matriz polimérica. Ao contrário da velocidade de dissolução lenta do alopurinol puro, a dispersão do fármaco nos polímeros aumentou consideravelmente a taxa de d...

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“…The DSC thermogram of pure un-ground MX powder ( Figure 8 and Table 3) exhibited a sharp endothermic peak at 260.77 °C corresponding to its melting point, with a normalized energy of -140.64 J/g (Pathak et al, 2008), while the ground MX powder showed a sharper peak at almost the same melting endotherm (260.85 °C) with increased corresponding energy of -252.45 J/g, which might be an evident of the thermodynamic state variation (Glicksman, 2011).…”

Section: Dscmentioning

confidence: 99%

Nano-Crystalline Cellulose as a Novel Tablet Excipient for Improving Solubility and Dissolution of Meloxicam

Emara¹,

El-Ashmawy²,

Taha³

et al. 2016

J App Pharm Sci

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This study explored the effect of nano-crystalline cellulose (NCC) on Meloxicam (MX) solid dispersion (SD) prepared by co-grinding technique compared to micro-crystalline cellulose (MCC) in presence of lactose. MXtablets were prepared by direct compression of different co-ground SDs or physical mixtures. The solubility, dissolution, SEM and DSC of different preparations were studied. Flow-through cell apparatus (FTC) was used to study the dissolution of MX from tablets at pH 7.4. Generally, the results revealed that increasing NCC loadings showed a direct increase in both the solubility and dissolution of MX. MCC did not improve either the solubility or the dissolution of MX in the physical mixture, while, co-grinding dramatically decreased the dissolution rate of MX. It was interesting to find that grinding of MX-powder alone or in a mixture with lactose highly increased MX solubility and dissolution. SEM as well as DSC were found to be very good tools, without a single exception, to describe the observed solubility and dissolution of MX in these proposed preparations. SEM-images showed the particle size reduction upon grinding or co-grinding techniques. While DSC-data proved that the crystalline structure of MX has been changed to an amorphous state.

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Solid dispersion of meloxicam: Factorially designed dosage form for geriatric population

Cited by 37 publications

References 7 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

Physicochemical characterization and solubility enhancement studies of allopurinol solid dispersions

Nano-Crystalline Cellulose as a Novel Tablet Excipient for Improving Solubility and Dissolution of Meloxicam

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