Solubility enhancement of celecoxib using solidified Tween 80 for the formulation of tablet dosage forms

被引：6

作者：

Chakma S. ^{[1
]}

Khadka P. ^{[1
]}

Jo K. ^{[1
]}

Kim H. ^{[1
]}

Ro J. ^{[1
]}

Park K. ^{[1
]}

Karki S. ^{[1
]}

Barua S. ^{[1
]}

Lee J. ^{[1
]}

机构：

[1] College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul

来源：

Journal of Pharmaceutical Investigation | 2015年 / 45卷 / 5期

关键词：

Celecoxib; Fujicalin; Solidified Tween 80; Solubility enhancement; Water insoluble drug;

D O I：

10.1007/s40005-015-0192-1

中图分类号：

学科分类号：

摘要：

Celecoxib is a non-steroidal, anti-inflammatory drug used in the treatment of pain and inflammation associated with rheumatoid arthritis, and several other inflammatory disorders. It is a class II compound according to the Biopharmaceutics Classification System owing to its low water solubility and high membrane permeability. The objective of this study was to improve the solubility and dissolution rate of celecoxib using solid surfactant technology that might be useful in developing solid dosage forms. Solid surfactant was developed by mixing and grinding together a liquid surfactant (Tween 80) with various inorganic carriers like Fujicalin® (Dibasic Calcium Phosphate Anhydrous), Pineflow® (Porous-structured Maltodextrin), Neusilin® (Magnesium Alumino metasilicate) and Aerosil® (Colloidal Silicon dioxide) in a mortar and pestle in different ratios of liquid surfactant and the carrier to obtain solid surfactants. The celecoxib tablets prepared with solid surfactants were then evaluated for their solubility and dissolution properties. Among the fillers used, Fujicalin showed the highest solubilization capacity for celecoxib. The dissolution behaviors of various tablets prepared with solidified surfactants were compared to those of conventional celecoxib tablets in a simulated gastric fluid. Celecoxib tablets prepared using solidified surfactants showed improved dissolution behaviors when compared to the conventional counterparts. Fujicalin solidified Tween 80 was further analyzed by powder X-ray diffraction analysis, differential scanning calorimetry thermographs and reverse phase high performance liquid chromatography. © 2015, The Korean Society of Pharmaceutical Sciences and Technology.

引用

页码：449 / 460

页数：11

共 23 条

[1]

Amidon G.L., Lennernas H., Shah V.P., A theoretical basis for a biopharmaceutics drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability, Pharm Res, 12, pp. 413-420, (1995)

[2]

Balakrishnan A., Rege B.D., Amidon G.L., Polli J.E., Surfactant-mediated dissolution: contributions of solubility enhancement and relatively low micelle diffusivity, J Pharm Sci, 93, pp. 2064-2075, (2004)

[3]

Barzegar-jalali M., Valizadeh H., Dastmalchi S., Enhancing dissolution rate of carbamazepine via cogrinding with crospovidone and hydroxypropylmethylcellulose, Iran J Pharm Res, 6, pp. 159-165, (2007)

[4]

Cabral H.M., Hadgraft J., Kellaway I.W., Studies of cyclodextrin inclusion complexes. I. The salbutamol-cyclodextrin complex as studied by phase solubility and DSC, Int J Pharm, 63, pp. 259-266, (1990)

[5]

Clemett D., Goa K.L., Celecoxib: a review of its use in osteoarthritis, rheumatoid arthritis and acute pain, Drugs, 59, pp. 957-980, (2000)

[6]

Gupta V.R., Mutalik S., Patel M.M., Jani G.K., Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties, Acta pharm, 57, pp. 173-184, (2007)

[7]

Hu L., Zhang N., Yang G., Zhang J., Effects of Tween-80 on the dissolution properties of Daidzein solid dispersion in vitro, Int J Chem, 3, pp. 68-73, (2011)

[8]

Jallo L.J., Ghoroi C., Gurumurthy L., Patel U., Dave R.N., Improvement of flow and bulk density of pharmaceutical powders using surface modification, Int J Pharm, 423, pp. 213-225, (2012)

[9]

Lu G.W., Hawley M., Smith M., Geiger B.M., Pfund W., Characterization of a novel polymorphic form of celecoxib, J Pharm Sci, 95, pp. 305-317, (2006)

[10]

Morgen M., Bloom C., Beyerinck R., Bello A., Song W., Wilkinson K., Steenwyk R., Shamblin S., Polymeric nanoparticles for increased oral bioavailability and rapid absorption using celecoxib as a model of a low-solubility, high-permeability drug, Pharm Res, 29, pp. 427-440, (2012)

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