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      Surface Solid Dispersion and Solid Dispersion of Meloxicam: Comparison and Product Development

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          Abstract

          Purpose: A comparative study was carried out between surface solid dispersion (SSD) and solid dispersion (SD) of meloxicam (MLX) to assess the solubility and dissolution enhancement approach and thereafter develop as patient friendly orodispersible tablet.

          Methods: Crospovidone (CPV), a hydrophilic carrier was selected for SSD preparation on the basis of 89% in- vitro MLX adsorption, 19% hydration capacity and high swelling index. SD on the other hand was made with PEG4000. Both were prepared by co-grinding and solvent evaporation method using drug: carrier ratios of 1:1, 1:4, and 1:8. Formulation SSDS3 (MLX: CPV in 1:8 ratio) made by solvent evaporation method showed t 50% of 28 min and 80.9% DE 50min which was higher in comparison to the corresponding solid dispersion, SDS3 (t 50% of 35min and 76.4% DE 50min). Both SSDS3 and SDS3 were developed as orodispersible tablets and evaluated.

          Results: Tablet formulation F3 made with SSD3 with a disintegration time of 11 secs, by wetting time= 6 sec, high water absorption of 78%by wt and cumulative drug release of 97% proved to be superior than the tablet made with SD3.

          Conclusion: Conclusively, the SSD of meloxicam has the potential to be developed as fast acing formulation that can ensure almost complete release of drug.

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          Most cited references21

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          Comparative evaluation of flow for pharmaceutical powders and granules.

          The objective of the present work was to carry out a systematic evaluation of flow of pharmaceutical powders and granules using compendial and non-compendial methods. Angle of repose, bulk density, tapped density, Carr's compressibility index, and Hausner ratios were evaluated. Additionally, flow was characterized using a powder rheometer in which a sensitive force transducer monitors the forces generated as a result of the sample displacement. The critical attributes such as cohesivity index, caking strength, and flow stability were determined for samples. The samples consisted of different grades of magnesium stearate powder including bovine, vegetable, and food grade, physical mixture powder blend consisting of a model formulation, granules prepared by various methods including slugging, high shear granulator, and fluid bed dryer. Lubricant efficiency was also determined for granules lubricated with various concentrations of magnesium stearate. It was observed that the compendial methods were often non-discriminating for minor variations in powder flow. The additional characterization such as cohesivity, and caking strength were helpful in understanding the flow characteristics of pharmaceutical systems. The flow stability test determined that the powders were not affected by the test conditions on the rheometer. The non-compendial tests were discriminating to even minor variations in powder flow.
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            Solid dispersions: a review.

            Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of hydrophobic drugs. This article reviews the various preparation techniques for solid dispersion and compiles some of the recent technology transfers. The different types of solid dispersions based on the molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier and methods of physicochemical characterization, along with an insight into the molecular arrangement of drugs in solid dispersions are also discussed. Finally, an in-depth rationale for limited commercialization of solid dispersions and recent revival has been considered.
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              Solubility enhancement of Cox-2 inhibitors using various solvent systems.

              This study examined the solubility enhancement of 4 cox-2 inhibitors, celecoxib, rofecoxib, meloxicam, and nimesulide, using a series of pure solvents and solvent mixtures. Water, alcohols, glycols, glycerol, and polyethylene glycol 400 (PEG 400) were used as solvents and water-ethanol, glycerol-ethanol, and polyethylene glycol-ethanol were used as mixed-solvent systems. A pH-solubility profile of drugs was obtained in the pH range 7.0 to 10.9 using 0.05 M glycine-sodium hydroxide buffer solutions. Lower alcohols, higher glycols, and PEG 400 were found to be good solvents for these drugs. The aqueous solubility of celecoxib, rofecoxib, and nimesulide could be enhanced significantly by using ethanol as the second solvent. Among the mixed-solvent systems, PEG 400- ethanol system had highest solubilization potential. In the case of meloxicam and nimesulide, solubility increased significantly with increase in pH value. Physico-chemical properties of the solvent such as polarity, intermolecular interactions, and the ability of the solvent to form a hydrogen bond with the drug molecules were found to be the major factors involved in the dissolution of drugs by pure solvents. The greater the difference in the polarity of the 2 solvents in a given mixed solvent, the greater was the solubilization power. However, in a given mixed-solvent system, the solubilization power could not be related to the polarity of the drugs. Significance of the solubility data in relation to the development of formulations has also been discussed in this study.
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                Author and article information

                Journal
                Adv Pharm Bull
                Adv Pharm Bull
                Adv Pharm Bull
                APB
                TBZMED
                Advanced Pharmaceutical Bulletin
                Tabriz University of Medical Sciences
                2228-5881
                2251-7308
                December 2017
                31 December 2017
                : 7
                : 4
                : 569-577
                Affiliations
                1Department of Pharmaceutics, Rajiv Academy for Pharmacy, Chattikkara, Mathura, India.
                2Department of Pharmaceutics, M M College of Pharmacy, Maharishi Markandeshwar University,Mullana, Ambala-133207, Haryana, India.
                3Department of Pharmaceutics, Pharmacy College Saifai, Uttar Pradesh University of Medical sciences, Saifai, Etawah , 206130, Uttar Pradesh, India.
                Author notes
                [* ] Corresponding author: Manish Kumar, Tel: 9719021160, manish_singh17@ 123456rediffmail.com
                Article
                10.15171/apb.2017.068
                5788211
                01678ac9-f403-4a76-8dea-7a6a600a965a
                ©2017 The Authors.

                This is an Open Access article distributed under the terms of the Creative Commons Attribution (CC BY), which permits unrestricted use, distribution, and reproduction in any medium, as long as the original authors and source are cited. No permission is required from the authors or the publishers.

                History
                : 14 May 2017
                : 01 December 2017
                : 04 December 2017
                Page count
                Figures: 6, Tables: 6, References: 23
                Categories
                Research Article

                surface solid dispersion,solid dispersion,dissolution,orodispersible tablet

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