Improved Dissolution Rate of Indomethacin by Adsorbents

Al-Saidan, Saleh M.; Alsughayer, Abdulhakeem A.; Eshra, A. G.

doi:10.3109/03639049809085635

Cited by 47 publications

(31 citation statements)

References 8 publications

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“…Many workers have designed a miniscular drug form using excipients with high surface area. 29,30 The reduction in peak intensity of XRPD spectra of agglomerates of batches IT-1 and IT-2 supported the observation (Figure 3). Decrease in peak intensities was due to dilution and formation of some plate-type crystals.…”

Section: Resultssupporting

confidence: 73%

Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

et al. 2004

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The purpose of this research work was to obtain directly compressible agglomerates of ibuprofen with talc by a novel crystallo-co-agglomeration (CCA) technique, which is an extension of spherical crystallization. Ibuprofen-talc agglomerates were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for ibuprofen as well as a bridging liquid for agglomeration of crystallized drug with talc. The agglomerates were characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy and were evaluated for tableting properties and for drug release. The process yielded spherical agglomerates containing ~95% to 96% wt/wt of ibuprofen. Agglomerates containing talc showed uniform distribution of hydroxypropylmethylcellulose and decreased crystallinity, and deformed under pressure. The miniscular form of ibuprofen and the hydrophobicity of talc governed the drug release rate. The batch containing a higher proportion of talc showed zeroorder kinetics and drug release was extended up to 13 hours. The CCA technique developed in this study is suitable for obtaining agglomerates of drug with talc as an excipient.

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Section: Resultssupporting

confidence: 73%

Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

et al. 2004

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“…MCC is known to cause deaggregation of powders, increasing the effective surface area in contact with the medium (Scheme 2; Cases 2 and 3). 8 Therefore, the dissolution rate enhancement is attributed to particle deaggregation in the dissolution medium. Microscopic examination revealed that the theophylline monohydrate particles formed during the dissolution run (Case 3 in Scheme 2) were much larger than the theophylline monohydrate in the granules (Case 2 in Scheme 2).…”

Section: Effect Of Processing With Microcrystalline Cellulosementioning

confidence: 99%

“…In addition to the active ingredient, the excipients in a dosage form can influence product performance. 8 Thus, product performance will be influenced by the solid state of the drug and excipients, as well as the processing conditions. These effects are of particular concern in case of drugs with low…”

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confidence: 99%

Influence of processing-induced phase transformations on the dissolution of theophylline tablets

Debnath

Suryanarayanan

2004

AAPS PharmSciTech

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INTRODUCTIONThe object of this investigation was to evaluate the influence of (1) processing-induced decrease in drug crystallinity and (2) phase transformations during dissolution, on the performance of theophylline tablet formulations. Anhydrous theophylline underwent multiple transformations (anhydrate → hydrate → anhydrate) during processing. Although the crystallinity of the anhydrate obtained finally was lower than that of the unprocessed drug, it dissolved at a slower rate. This decrease in dissolution rate was attributed to the accelerated anhydrate to hydrate transformation during the dissolution run. Water vapor sorption studies proved to be a good predictor of powder dissolution behavior. While a decrease in crystallinity was brought about either by milling or by granulation, the effect on tablet dissolution was pronounced only in the latter. Tablet formulations prepared from the granules exhibited higher hardness, longer disintegration time, and slower dissolution than those containing the milled drug. The granules underwent plastic deformation during compression resulting in harder tablets, with delayed disintegration. The high hardness coupled with rapid anhydrate → hydrate transformation during dissolution resulted in the formation of a hydrate layer on the tablet surface, which further delayed tablet disintegration and, consequently, dissolution. Phase transformations during processing and, more importantly, during dissolution influenced the observed dissolution rates. Product performance was a complex function of the physical state of the active and the processing conditions.The physicochemical properties of pharmaceuticals, including solubility and dissolution rate, can be influenced by the degree of crystallinity, solvation state, and crystal form. At room temperature, the anhydrate forms of ampicillin, theophylline, and glutethimide have a higher dissolution rate than their corresponding hydrates. 1 This difference in dissolution rate can be attributed to the difference in the free energy of hydration.1 Similarly, metastable forms, because of their higher free energy, are expected to dissolve more rapidly than their corresponding stable forms. This effect was observed with the metastable polymorphs of acetazolamide, carbamazepine, and indomethacin.2 However, this free energy difference between the stable and metastable forms can also provide the driving force for metastable → stable transformation in the dissolution medium. As a result, the observed difference in dissolution rate can be much lower than the predicted values. 3Although the physical form of a drug substance is carefully selected for dosage form manufacture, the processing conditions will determine the solid state of the drug in the final product. During tablet manufacture, processing steps may include milling, granulation, drying, and compression. Particle size as well as degree of crystallinity can be profoundly affected by milling as has been observed in case of griseofulvin. 4 The use of a binder solution for wet gra...

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“…Very few researchers have prepared miniscular dosage forms by using excipients with a large surface area [27,28]. Pawar et al designed a miniscular dosage form for ibuprofen-talc byCCA.…”

Section: Fig 5: X-ray Powder Diffraction Pattern Of Pure Linezolid Amentioning

confidence: 99%

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Kadam

Patil

2017

Int J App Pharm

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Objective: The purpose of current study was to improve physicochemical properties such as micrometric, compressibility and solubility of linezolid (LNZ) by preparing crystallo-co-agglomerates (CCA) in the presence of polymer for the enhancement of overall physicochemical performance. Methods:The process of agglomeration involves the use of dichloromethane (DCM) as a good solvent and chloroform as bridging liquid were used to prepare agglomerates. Agglomerates were characterised in the solid state using several techniques such as Scanning electronic microscopy(SEM), Fourier transformation infrared spectroscopy (FTIR), X-ray powder diffraction analysis (XRPD) The agglomerates obtained were evaluated for micrometric, mechanical, deformation, compressibility and drug release properties.Results: It was found that micrometric properties and dissolution characteristics of agglomerates were significantly improved than that of pure linezolid. Solubility was found to be increased than pure linezolid. The solubility of crystallo co-agglomerates was found an increase in 5 fold 3 fold and 3.7 fold for PVPK30 (0.5%), PVPK30 (0.25%) and PVPK30 (0.75%) respectively. The angle of repose for all batches was found between 22 ° to 30 °Carrs index was between 12.27±0.6 to 18.73±0.4 and Hausners ratio Near to 1, indicated good flow ability of agglomerates. The time required for drug release over a period of 60 min, is as LA1>LA2>LA3. LA3 shows fast drug release than LA1 and LA2, due to solubilization of drug due to more concentration of PVPK30 and less concentration of talc.Conclusion: Based on the above results, it was revealed that CCA of linezolid prepared with DCM and HPMC (Hydroxypropyl methyl cellulose)/PEG (Polyethylene glycol)/PVP (Polyvinylpyrrolidone) K30 exhibited improved micrometric properties, compressibility and in addition to improving solubility and dissolution rate.

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Improved Dissolution Rate of Indomethacin by Adsorbents

Cited by 47 publications

References 8 publications

Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

Influence of processing-induced phase transformations on the dissolution of theophylline tablets

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

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