Solubility enhancement of celecoxib using β-cyclodextrin inclusion complexes

Rawat, Swati; Jain, Sanjay

doi:10.1016/j.ejpb.2003.10.020

Cited by 158 publications

(59 citation statements)

References 13 publications

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“…The most common causes of low oral bioavailability are poor solubility and low permeability of active pharmaceutical ingredient (API) [1] . Multiple approaches have been adopted to improve the solubility of poorly water soluble APIs including micronization [2] , complexation with cyclodextrins [3] , cosolvency [4,5] , solid dispersions [6] , salt forms [7] , nanoparticles [8] and surfactants [9] , etc. Cocrystals are a class of multicomponent molecular crystals demonstrated to enhance the solubility, bioavailability and/or stability of API, which has been proposed as a unique crystal engineering approach to alter the physicochemical properties of compounds [10][11][12] .…”

Section: Research Papermentioning

confidence: 99%

Solubility Enhancement of Lornoxicam by Crystal Engineering

Gadade¹,

Kulkarni²,

Rathi³

et al. 2017

Journal of Pharmaceutical Sciences

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Gadade, et al.: Crystal Engineering of LornoxicamAn attempt was made to improve the solubility and physicochemical properties of the poorly soluble lornoxicam by crystal engineering with different coformers. Nineteen different coformers were screened during this study. Cocrystals were prepared by neat grinding method. The prepared cocrystals were evaluated for solubility, powder characteristics, assay and in vitro dissolution study. The solid state property was characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction analysis and Raman spectroscopy. Maximum solubility and dissolution rate were observed with cocrystal prepared using saccharin sodium. Cocrystallization leads to increased solubility and improved in vitro dissolution of lornoxicam.

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Section: Research Papermentioning

confidence: 99%

Solubility Enhancement of Lornoxicam by Crystal Engineering

Gadade¹,

Kulkarni²,

Rathi³

et al. 2017

Journal of Pharmaceutical Sciences

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“…Hence, increasing the solubility of CXB may enhance its oral bioavailability. Although many researchers have been attempted to improve the solubility by various methods such as complexation with beta-cyclodextrin (20), self-emulsifying (21) and microemulsions (22)(23), conclusive evidence for the formulation of CXB in dosage forms with adequate solubility and bioavailability are rare. Dolenc Andrej et al (24) have produced CXB nanosuspensions existing as crystalline form by the emulsion-diffusion (solvent exchange) method but with a broad particle size distribution (PSD) of 0.14-1.29 μm.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of Dissolution Enhancement and Bioavailability of Poorly Water Soluble Celecoxib by Preparing Stable Amorphous Nanoparticles

Liu¹,

Sun²,

Hao³

et al. 2010

J Pharm Pharm Sci

110

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ABSTRACT-Purpose: Nanoparticle engineering offers promising methods for the formulation of poorly water soluble drug compounds. The aim of the present work was to enhance dissolution and oral bioavailability of poorly water-soluble celecoxib (CXB) by preparing stable CXB nanoparticles using a promising method, meanwhile, investigate the mechanism of increasing dissolution of CXB. Methods: CXB nanoparticles were produced by combining the antisolvent precipitation and high pressure homogenization (HPH) approaches in the presence of HPMC E5 and SDS (2:1, w/w). Then the CXB nanosuspensions were converted into dry powders by spray-drying. The effect of process variables on particle size and physical state of CXB were investigated. The physicochemical properties of raw CXB and CXB nanoparticles were characterized by scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), X-ray photoelectron spectra (XPS), fourier transform infrared (FT-IR) spectroscopy, diffrential scanning calorimetry (DSC), as well as, measuring the particle size and contact angle. Additionally, the studies of in-vitro drug dissolution and oral bioavailability in beagle dogs of nanoparticles were performed. Results: The images of SEM revealed spherical CXB nanoparticles. The DSC and XRPD results indicated that the antisolvent precipitation process led to the amorphization of CXB. Under storage, the amorphous CXB nanoparticles showed promising physical stability. The XPS data indicated the amorphous CXB nanoparticles exhibited different surface property compared to raw CXB. Hydrogen bonds were formed between the raw CXB and HPMC E5 as proven by the FT-IR spectra. CXB nanoparticles increased the saturation solubility of CXB fourfold. CXB nanoparticles completely dissolved in the dissolution medium of phosphate buffer (pH 6.8, 0.5% SDS) within 5 min, while there was only 30% of raw CXB dissolved. The C max and AUC 0-24h of CXB nanoparticles were approximately threefold and twofold greater than those of the Celecoxib Capsules, respectively. Conclusions: The process by combining the antisolvent precipitation under sonication and HPH was a promising method to produce small, uniform and stable CXB nanoparticles with markedly enhanced dissolution rate and oral bioavailability due to an increased solubility that is attributed to a combination of amorphization and nanonization with increased surface area, improved wettability and reduced diffusion pathway. _______________________________________________________________________________________

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“…[8] Azithromycin: β-CD (1:2) complexes showed maximum drug release; hence this complex was selected for the preparation of tablets. [9][10][11] …”

Section: Preparation Of Pm and Sd And In Vitro Dissolution Studiesmentioning

confidence: 99%

Untitled

Wadhwa¹

2017

AJP

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Aim: To increase the solubility of azithromycin by formulating solid dispersion (SD) and then SD tablets (SDT) were prepared from the best formulation of SDs. Material and Methods: SDs were prepared using polyethylene glycol 6000 and β-cyclodextrin (β-CD) by solvent evaporation method. To investigate drug-excipient interaction and for selection of suitable excipient for formulation differential scanning calorimetry study was done, and each excipient was selected for formulation development only if it showed compatible results. Results and Discussion: Tablets were prepared by direct compression technique using hydroxypropylmethylcellulose (HPMC)-K 100 and guar gum in different concentrations. SDs were evaluated for drug content, in vitro dissolution profiles, and developed SDT were evaluated for various pharmaceutical characteristics, viz., hardness, friability, weight variation, thickness, drug content, and in vitro drug release. Conclusion: Study indicates that among various formulations SDT of azithromycin: β-CD (1:2) complexes prepared using HPMC and guar gum in 1:4 combination showed maximum drug release.

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Solubility enhancement of celecoxib using β-cyclodextrin inclusion complexes

Cited by 158 publications

References 13 publications

Solubility Enhancement of Lornoxicam by Crystal Engineering

Solubility Enhancement of Lornoxicam by Crystal Engineering

Mechanism of Dissolution Enhancement and Bioavailability of Poorly Water Soluble Celecoxib by Preparing Stable Amorphous Nanoparticles

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