Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

V.R. Gupta, S. Mutalik, M.M. Patel, G.K. Jani

Research output: Contribution to journalArticle

64 Citations (Scopus)

Abstract

Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p <0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.
Original languageEnglish
Pages (from-to)173-184
Number of pages12
JournalActa Pharmaceutica
Volume57
Issue number2
DOIs
Publication statusPublished - 2007

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Celecoxib
Povidone
Differential Scanning Calorimetry
X-Ray Diffraction
Electron Scanning Microscopy
Solubility
Chloroform
Acetone
Drug Interactions
Pharmaceutical Preparations
Spectrum Analysis
Water
Drug Liberation

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@article{fa518536f4a74bf88a1373e58787fbc9,
title = "Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties",
abstract = "Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency ({\%} or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3{\%} (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p <0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10{\%}). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.",
author = "V.R. Gupta and S. Mutalik and M.M. Patel and G.K. Jani",
note = "Cited By :54 Export Date: 10 November 2017 CODEN: ACPHE Correspondence Address: Gupta, V.R.; Department of Pharmaceutics, N. E. T. Pharmacy College Navodaya Nagar, Mantralayam Road, Raichur-584103, India; email: vrmgupta_05@yahoo.co.in Chemicals/CAS: acetone, 67-64-1; celecoxib, 169590-42-5; chloroform, 67-66-3; povidone, 9003-39-8; water, 7732-18-5; celecoxib, 169590-42-5; Cyclooxygenase Inhibitors; Methylcellulose, 9004-67-5; Pharmaceutic Aids; Powders; Pyrazoles; Sulfonamides; Water, 7732-18-5 Manufacturers: Aurobindo, India; Fine Chemical Corporation, India References: Shangraw, R.F., Compressed Tablets by Direct Compression (1989) Pharmaceutical Dosage Forms: Tablets, 1, pp. 195-246. , Eds. H. A. Lieberman, L. Lachman and J. B. Schwartz, Marcel Dekker, New York; Kulkarni, P.K., Nagavi, B.G., Spherical crystallization (2002) Indian J, 36, pp. 66-71. , Pharm. Ed; Paradkar, A.R., Pawar, A.P., Mahadik, K.R., Kadam, S.S., Spherical crystallization: A novel particle design technique (1998) Indian Drugs, 31, pp. 229-233; Martindale, (1999) The Extra Pharmacopoeia, pp. 2-12. , 32nd ed, The Pharmaceutical Press, London; Babu, G.V.M.M., Shankar, V.G., Sankar, K.H., Seshasayana, A., Kumar, N.K., Murthy, K.V.R., Development of dissolution medium for a poorly water soluble drug, celecoxib (2002) Indian J. Pharm. Sci, 6, pp. 588-590; Nagarsenker, M.S., Joshi, M.S., Celecoxib-cyclodextrin systems: Characterization and evaluation of in vitro and in vivo advantages (2005) Drug Dev. Ind. Pharm, 31, pp. 169-178; Pawar, P.H., Pawar, A.P., Mahadik, K.R., Paradkar, A.R., Evalution of tableting properties of agglomerates obtained by spherical crystallisation of trimethoprim (1998) Indian J. Pharm. Sci, 60, pp. 24-28; Deshpande, M.C., Mahadik, K.R., Pawar, A.P., Paradkar, A.R., Evaluation of spherical crystallization as a particle size enlargement technique for aspirin (1997) Indian J. Pharm. Sci, 59, pp. 32-34; Sano, A., Kawashima, Y., Particle design of tolbutamide in the presence of soluble polymer or surfactant by the spherical crystallization technique: Improvement of dissolution rate (1987) J. Pharm. Sci, 76, pp. 471-474; Sano, A., Kuriki, T., Kawashima, Y., Takenchi, H., Hino, T., Niwa, T., Particle design of tolbutamide by the spherical crystallization technique. III. Micromeritic properties and dissolution rate of tolbutamide spherical agglomerates prepared by the quasi-emulsion solvent diffusion method and the solvent change method (1990) Chem. Pharm. Bull, 38, pp. 733-739; Paradkar, A.R., Pawar, A.P., Chordiya, J.K., Patil, V.B., Ketkar, A.R., Spherical crystallization of celecoxib (2002) Drug Dev. Ind. Pharm, 28, pp. 1213-1220; Martin, A., Bustamante, P., Chun, A., Micromeritics (2002) Physical Pharmacy - Physical Chemical Principles in the Pharmaceutical Sciences, pp. 423-452. , 4th ed, Lippincott Williams and Wilkins, Baltimore; Wells, J., Pharmaceutical preformulation, the physicochemical properties of drug substances (2002) Pharmaceutics - the Science of Dosage Form Design, pp. 113-138. , 2nd ed, Ed. M. E. Aulton, Churchill Livingstone, London; Kawashima, Y., Okumura, M., Takenaka, H., Spherical crystallization. Direct spherical agglomeration of salicylic acid crystals during crystallization (1982) Science, 216, pp. 1127-1128; Chourasia, M.K., Jain, N.K., Jasin, S., Jain, N.K., Jain, S.K., Preparation and characterization of agglomerates of flurbiprofen by spherical crystallization technique (2003) Indian J. Pharm. Sci, 3, pp. 287-290; DiMartino, P., Barthelemy, C., Piva, F., Joiris, E., Palmieri, G.F., Martelli, S., Improved dissolution behavior of fenbufen by spherical crystallization (1999) Drug Dev. Ind. Pharm, 25, pp. 1073-1081; Kawashima, S., Handa, T., Takenchi, H., Okumura, M., Katou, H., Nagai, O., Crystal modification of phenytoin with polyethylene glycol for improving mechanical strength, dissolution rate and bio-availability by a spherical crystallization technique (1986) Chem. Pharm. Bull, 34, pp. 3376-3383; Kapoor, A., Mujumdar, D.K., Yadav, M.R., Crystal forms of nimesulide - a sulfonanilide (non-steroidal anti-inflammatory drug) (1998) Indian J. Chem. B, 37, pp. 572-575; Mutalik, S., Venkatesh, M., Udupa, N., Fast analgesic activity from crystallized nimesulide and its solid dispersion (2002) Indian J. Physiol. Pharmacol, 1, pp. 115-118; Mutalik, S., Udupa, N., Pharmacological evaluation of membrane moderated transdermal system of glipizide (2006) Clin. Exp. Pharmacol. Physiol, 1-2, pp. 17-26",
year = "2007",
doi = "10.2478/v10007-007-0014-8",
language = "English",
volume = "57",
pages = "173--184",
journal = "Acta Pharmaceutica",
issn = "1330-0075",
publisher = "Croatian Pharmaceutical Society",
number = "2",

}

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties. / Gupta, V.R.; Mutalik, S.; Patel, M.M.; Jani, G.K.

In: Acta Pharmaceutica, Vol. 57, No. 2, 2007, p. 173-184.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

AU - Gupta, V.R.

AU - Mutalik, S.

AU - Patel, M.M.

AU - Jani, G.K.

N1 - Cited By :54 Export Date: 10 November 2017 CODEN: ACPHE Correspondence Address: Gupta, V.R.; Department of Pharmaceutics, N. E. T. Pharmacy College Navodaya Nagar, Mantralayam Road, Raichur-584103, India; email: vrmgupta_05@yahoo.co.in Chemicals/CAS: acetone, 67-64-1; celecoxib, 169590-42-5; chloroform, 67-66-3; povidone, 9003-39-8; water, 7732-18-5; celecoxib, 169590-42-5; Cyclooxygenase Inhibitors; Methylcellulose, 9004-67-5; Pharmaceutic Aids; Powders; Pyrazoles; Sulfonamides; Water, 7732-18-5 Manufacturers: Aurobindo, India; Fine Chemical Corporation, India References: Shangraw, R.F., Compressed Tablets by Direct Compression (1989) Pharmaceutical Dosage Forms: Tablets, 1, pp. 195-246. , Eds. H. A. Lieberman, L. Lachman and J. B. Schwartz, Marcel Dekker, New York; Kulkarni, P.K., Nagavi, B.G., Spherical crystallization (2002) Indian J, 36, pp. 66-71. , Pharm. Ed; Paradkar, A.R., Pawar, A.P., Mahadik, K.R., Kadam, S.S., Spherical crystallization: A novel particle design technique (1998) Indian Drugs, 31, pp. 229-233; Martindale, (1999) The Extra Pharmacopoeia, pp. 2-12. , 32nd ed, The Pharmaceutical Press, London; Babu, G.V.M.M., Shankar, V.G., Sankar, K.H., Seshasayana, A., Kumar, N.K., Murthy, K.V.R., Development of dissolution medium for a poorly water soluble drug, celecoxib (2002) Indian J. Pharm. Sci, 6, pp. 588-590; Nagarsenker, M.S., Joshi, M.S., Celecoxib-cyclodextrin systems: Characterization and evaluation of in vitro and in vivo advantages (2005) Drug Dev. Ind. Pharm, 31, pp. 169-178; Pawar, P.H., Pawar, A.P., Mahadik, K.R., Paradkar, A.R., Evalution of tableting properties of agglomerates obtained by spherical crystallisation of trimethoprim (1998) Indian J. Pharm. Sci, 60, pp. 24-28; Deshpande, M.C., Mahadik, K.R., Pawar, A.P., Paradkar, A.R., Evaluation of spherical crystallization as a particle size enlargement technique for aspirin (1997) Indian J. Pharm. Sci, 59, pp. 32-34; Sano, A., Kawashima, Y., Particle design of tolbutamide in the presence of soluble polymer or surfactant by the spherical crystallization technique: Improvement of dissolution rate (1987) J. Pharm. Sci, 76, pp. 471-474; Sano, A., Kuriki, T., Kawashima, Y., Takenchi, H., Hino, T., Niwa, T., Particle design of tolbutamide by the spherical crystallization technique. III. Micromeritic properties and dissolution rate of tolbutamide spherical agglomerates prepared by the quasi-emulsion solvent diffusion method and the solvent change method (1990) Chem. Pharm. Bull, 38, pp. 733-739; Paradkar, A.R., Pawar, A.P., Chordiya, J.K., Patil, V.B., Ketkar, A.R., Spherical crystallization of celecoxib (2002) Drug Dev. Ind. Pharm, 28, pp. 1213-1220; Martin, A., Bustamante, P., Chun, A., Micromeritics (2002) Physical Pharmacy - Physical Chemical Principles in the Pharmaceutical Sciences, pp. 423-452. , 4th ed, Lippincott Williams and Wilkins, Baltimore; Wells, J., Pharmaceutical preformulation, the physicochemical properties of drug substances (2002) Pharmaceutics - the Science of Dosage Form Design, pp. 113-138. , 2nd ed, Ed. M. E. Aulton, Churchill Livingstone, London; Kawashima, Y., Okumura, M., Takenaka, H., Spherical crystallization. Direct spherical agglomeration of salicylic acid crystals during crystallization (1982) Science, 216, pp. 1127-1128; Chourasia, M.K., Jain, N.K., Jasin, S., Jain, N.K., Jain, S.K., Preparation and characterization of agglomerates of flurbiprofen by spherical crystallization technique (2003) Indian J. Pharm. Sci, 3, pp. 287-290; DiMartino, P., Barthelemy, C., Piva, F., Joiris, E., Palmieri, G.F., Martelli, S., Improved dissolution behavior of fenbufen by spherical crystallization (1999) Drug Dev. Ind. Pharm, 25, pp. 1073-1081; Kawashima, S., Handa, T., Takenchi, H., Okumura, M., Katou, H., Nagai, O., Crystal modification of phenytoin with polyethylene glycol for improving mechanical strength, dissolution rate and bio-availability by a spherical crystallization technique (1986) Chem. Pharm. Bull, 34, pp. 3376-3383; Kapoor, A., Mujumdar, D.K., Yadav, M.R., Crystal forms of nimesulide - a sulfonanilide (non-steroidal anti-inflammatory drug) (1998) Indian J. Chem. B, 37, pp. 572-575; Mutalik, S., Venkatesh, M., Udupa, N., Fast analgesic activity from crystallized nimesulide and its solid dispersion (2002) Indian J. Physiol. Pharmacol, 1, pp. 115-118; Mutalik, S., Udupa, N., Pharmacological evaluation of membrane moderated transdermal system of glipizide (2006) Clin. Exp. Pharmacol. Physiol, 1-2, pp. 17-26

PY - 2007

Y1 - 2007

N2 - Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p <0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.

AB - Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p <0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.

U2 - 10.2478/v10007-007-0014-8

DO - 10.2478/v10007-007-0014-8

M3 - Article

VL - 57

SP - 173

EP - 184

JO - Acta Pharmaceutica

JF - Acta Pharmaceutica

SN - 1330-0075

IS - 2

ER -