Celecoxib-Cyclodextrin Systems: Characterization and Evaluation of In Vitro and In Vivo Advantage

Nagarsenker, Mangal S.; Joshi, M. S.

doi:10.1081/ddc-200047795

Cited by 49 publications

(21 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The physical mixtures (PM) were prepared by geometric mixing of drug and β-CD or HP β-CD in a mortar and pestle with simple trituration for 15-20 min and then passing the mixture through a 60# sieve (15).…”

Section: Preparation Of Solid Dispersions By Kneading Techniquementioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

View full text Add to dashboard Cite

Solid dispersions (SDs) and physical mixtures (PMs) of valsartan in β-cyclodextrin (β-CD), hydroxypropyl β-cyclodextrin (HP β-CD), and polyvinyl pyrollidone (PVP K-30) were prepared to increase its solubility characteristics. The drug formulations were characterized in the solid state by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). By these physical determinations, drug-polymer interactions were found. Both the solubility and the dissolution rate of the drug in these formulations were increased. Drug contents were determined by UV spectrophotometry at a λ max of 249.5 nm. The phase solubility behavior of valsartan in various concentrations of β-CD, HP β-CD, and PVP K-30 (0.25-1.0% w/v) in distilled water was obtained at 37 ± 2 °C. The dissolution of valsartan is increased with increasing amounts of the hydrophilic carriers (i.e., β-CD, HP β-CD, and PVP K-30). Gibbs free energy (ΔG o tr ) values were all negative, indicating the spontaneous nature of valsartan solubilization. The SDs of valsartan with β-CD and HP β-CD were prepared at 1:1, 1:3, and 1:5 drug/carrier ratios by a kneading method, and PVP K-30 SDs were prepared at the same ratios (i.e., 1:1, 1:3 and 1:5 drug/carrier) by a lyophilization technique. The FTIR spectroscopic studies show the stability of valsartan and the absence of well-defined drug-polymer interaction. Compared with β-CD, HP β-CD showed better enhancement of dissolution rate; compared with HP β-CD, PVP K-30 showed better solubility and dissolution enhancement.

show abstract

Section: Preparation Of Solid Dispersions By Kneading Techniquementioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

View full text Add to dashboard Cite

show abstract

“…It is used mainly for osteoarthritis, rheumatoid arthritis, and dysmenorrhea (8)(9)(10). Celecoxib is practically insoluble in water (0.003 mg/mL), and peak blood levels are reached between 2 and 3 h after oral administration.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Characterization, and Optimization of Fast-Dissolve Tablets Containing Celecoxib Solid Dispersion

Pandya¹,

Patel²,

Patel³

et al. 2009

Dissolution Technol.

View full text Add to dashboard Cite

Celecoxib is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of the present investigation was to increase the solubility and dissolution rate of celecoxib by preparing a solid dispersion with polyvinyl pyrrolidone K30 (PVP-K30) using a solvent-evaporation method. The dissolution profiles of developed formulations in distilled water containing 1% SLS were studied. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). For the preparation of celecoxib fast-dissolve tablets, a 1:2 solid dispersion with PVP-K30 was used with croscarmellose sodium as a superdisintegrant and Pearlitol 200SD (pearlitol) as a pore-forming agent. A 3 2 full-factorial design was employed to study the effect of independent variables, the amounts of croscarmellose sodium (X 1 ) and pearlitol (X 2 ), on dependent variables, disintegration time, percentage friability, wettability, and percentage of drug released after 20 min (Q 20 ). The results show that a dispersion of the drug in polymer considerably enhanced the dissolution rate. The drug-to-carrier ratio is the controlling factor for dissolution improvement. FTIR spectra show no chemical incompatibility between the drug and PVP-K30. FTIR and DSC data indicate that celecoxib was in the amorphous form, which explains the faster dissolution rate of the drug from its solid dispersions. Concerning the optimization study, multiple regression analysis reveals that an optimum concentration of croscarmellose sodium and a higher percentage of pearlitol are required for obtaining rapidly disintegrating tablets.

show abstract

“…Also, celecoxib shows incomplete and poor oral bioavailability due to low aqueous solubility (5). Hence, the improvement of aqueous solubility in such a case is a valuable goal to improve therapeutic efficacy (6). Apart from particle enlargement, this technique has also been applied for various purposes such as taste masking and particle size enlargement (7)(8)(9)(10).…”

mentioning

confidence: 99%

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

Gupta¹,

Mutalik

Patel³

et al. 2007

Acta Pharmaceutica

View full text Add to dashboard Cite

Direct tabletting of pharmaceutical materials is desirable to reduce the cost of production (1). However, compressing a high-dosed drug directly requires good micromeritic properties, such as flowability, and good and reproducible compression behavior. Spherical crystallization technique transforms directly the fine particles produced in crystallization or in the reaction process into a spherical shape. Agglomerates exhibit improved secondary characteristics, like flowability and compressibility, so that direct tabletting or coating is possible without further processing (mixing, agglomeration, sieving, etc.) (2, 3). Celecoxib, a non-steroidal anti-inflammatory drug (NSAID), is the first selective cyclooxygenase-2 inhibitor used in the treatment of osteoarthritis and rheumatoid arthritis in adult patients (4). Celecoxib exhibits poor flow and compression charac- 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.

show abstract

Celecoxib-Cyclodextrin Systems: Characterization and Evaluation of In Vitro and In Vivo Advantage

Cited by 49 publications

References 11 publications

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Formulation, Characterization, and Optimization of Fast-Dissolve Tablets Containing Celecoxib Solid Dispersion

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

Contact Info

Product

Resources

About