The use of spray-drying to enhance celecoxib solubility

被引:62
作者
Fouad, Ehab A. [1 ,2 ]
EL-Badry, Mahmoud [1 ,2 ]
Mahrous, Gamal M. [1 ]
Alanazi, Fars K. [1 ,3 ]
Neau, Steven H. [4 ]
Alsarra, Ibrahim A. [1 ,5 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia
[2] Assiut Univ, Fac Pharm, Dept Pharmaceut, Assiut, Egypt
[3] King Saud Univ, Coll Pharm, Kayyali Chair Pharmaceut Ind, Riyadh 11451, Saudi Arabia
[4] Allegheny Univ Hlth Sci, Philadelphia Coll Pharm, Dept Pharmaceut Sci, Philadelphia, PA 19102 USA
[5] King Saud Univ, Ctr Excellence Biotechnol Res, Riyadh 11451, Saudi Arabia
关键词
Spray-drying; celecoxib; Kollicoat IR (R); polyvinyl alcohol; polyethylene glycol; dissolution rate; IN-VITRO; SOLID DISPERSIONS; DRUG; DELIVERY; FORMS; STATE; CLASSIFICATION; CRYSTALLINE; DISSOLUTION; FORMULATION;
D O I
10.3109/03639045.2011.587428
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The present research investigates the enhancement of the dissolution rate of celecoxib by using spray-drying to prepare a solid dispersion with various polymers, namely Kollicoat IR (R) (Kollicoat), polyvinyl alcohol (PVA) 22000, or polyethylene glycol 6000 (PEG). The investigated drug-to-polymer mass ratios were 1:1, 1:2, and 1:4 by weight. Hydroalcoholic or methylene chloride solvent systems were used. The obtained yields ranged from 65% to 78%, whereas the entrapment efficiencies were between 68% and 82%. The results revealed an increase in the dissolution rate of the prepared particles up to 200% within 20 min. The prepared particles were investigated using differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The increased dissolution rate was attributed to hydrogen bond formation between celecoxib and each polymer together with the reduced size of the formed particles offering a greater overall surface area. It was concluded that spray-drying may be considered a successful one-step technique to improve the dissolution rate of celecoxib when using Kollicoat, PVA, or PEG as the carrier polymer.
引用
收藏
页码:1463 / 1472
页数:10
相关论文
共 35 条
[1]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[2]   Single periocular injection of celecoxib-PLGA microparticles inhibits diabetes-induced elevations in retinal PGE2,VEGF, and vascular leakage [J].
Amrite, AC ;
Ayalasomayajula, SP ;
Cberuvu, NPS ;
Kompella, UB .
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, 2006, 47 (03) :1149-1160
[3]   Retinal delivery of celecoxib is several-fold higher following subconjunctival administration compared to systemic administration [J].
Ayalasomayajula, SP ;
Kompella, UB .
PHARMACEUTICAL RESEARCH, 2004, 21 (10) :1797-1804
[4]   Modification of the crystal habit of celecoxib for improved processability [J].
Banga, Sheere ;
Chawla, Garima ;
Varandani, Deepak ;
Mehta, B. R. ;
Bansal, Arvind K. .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 2007, 59 (01) :29-39
[5]  
Biswal S, 2009, TROP J PHARM RES, V8, P417
[6]   Characterization of solid-state forms of celecoxib [J].
Chawla, G ;
Gupta, P ;
Thilagavathi, R ;
Chakraborti, AK ;
Bansal, AK .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2003, 20 (03) :305-317
[7]  
Davies N M, 2001, Expert Opin Pharmacother, V2, P139, DOI 10.1517/14656566.2.1.139
[8]  
DEV RV, 1999, ACTA CRYSTALLOGRAP C, V0055
[9]  
Dixit R. P., 2007, Indian Journal of Pharmaceutical Sciences, V69, P370
[10]   PREFORMULATION STUDIES ON SOLID DISPERSIONS CONTAINING TRIAMTERENE OR TEMAZEPAM IN POLYETHYLENE GLYCOLS OR GELUCIRE 44 14 FOR LIQUID FILLING OF HARD GELATIN CAPSULES [J].
DORDUNOO, SK ;
FORD, JL ;
RUBINSTEIN, MH .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1991, 17 (12) :1685-1713