Characterization of a novel polymorphic form of celecoxib

Lu, Guang Wei; Hawley, Michael; Smith, Mark E.; Geiger, Brenda M.; Pfund, William P.

doi:10.1002/jps.20522

Cited by 88 publications

(93 citation statements)

References 17 publications

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“…This increase in systemic exposure, which was accompanied by lower T max values of Cx/bCN, indicates that this formulation was characterized by more rapid and efficient Cx dissolution in the GI tract. This outcome may stem from the fact that the Celebra ® formulation contained micron-sized crystalline drug (11,38) while Cx in Cx/bCN is nano-sized and amorphous (15). Enhanced dissolution rate and oral bioavailability of Cx in an amorphous nano-formulation was previously reported (12).…”

Section: Bioavailability Analysismentioning

confidence: 93%

Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Perlstein¹,

Bavli²,

Turovsky

et al. 2014

European Journal of Nanomedicine

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Beta-casein (bCN) micelles were developed as a platform for improved oral bioavailability (BA) of poorly water-soluble drugs. Here we demonstrate a proof-ofconcept using the NSAID celecoxib (Cx) loaded into bCN micelles (Cx/bCN). In a crossover pharmacokinetic (PK) study in pigs (n = 4), dosed intraduodenally with either the commercial Cx formulation Celebra ® or Cx/bCN, the C max obtained after administration of Cx/bCN was 2.3-fold higher and the T max was 1.57-fold faster, leading to a 1.76-fold increase in the BA of Cx, compared to the Celebra ® formulation. It is suggested that this BA enhancement was caused by improvement of Cx solubility in intestinal fluids by bCN micelles, which maintained their Cx cargo in an amorphous state.

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Section: Bioavailability Analysismentioning

confidence: 93%

Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Perlstein¹,

Bavli²,

Turovsky

et al. 2014

European Journal of Nanomedicine

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“…In HT solubility screening, the residual solids are rarely investigated systematically, although transitions to different solid forms in the presence of liquid pharmaceutical excipients or vehicles have been reported (7,10,11). Many drugs form polymorphs and solvates that can have different physicochemical properties such as melting point, enthalpy of fusion, vapor pressure, density, hardness, color, dissolution rate and that can differ considerably in solubility (12,13).…”

Section: Introductionmentioning

confidence: 99%

Miniaturized Assay for Solubility and Residual Solid Screening (SORESOS) in Early Drug Development

Wyttenbach

Alsenz

Grassmann³

2007

Pharm Res

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“…Sensitive analytical methods such as differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy and scanning electron microscopy have been used to characterize the various forms (11)(12)(13)(14)(15)(16)(17). Above all, much attention has been paid to utilization of the solution calorimeter, which generates data by dissolving a solid compound into a solvent, providing the enthalpy of solution which is a direct reflection of its lattice energy.…”

mentioning

confidence: 99%

Characterization of solvatomorphs of methotrexate using thermoanalytical and other techniques

Chadha¹,

Arora²,

Kaur³

et al. 2009

Acta Pharmaceutica

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Investigation of polymorphism and solvatomorphism in drug molecules is an important step in any pre-formulation program from both biopharmaceutical and technological point of view (1, 2). It is well known that polymorphs are different crystalline forms of the same compound whereas the inclusion of a solvent in a crystal lattice gives rise to pseudopolymorphs or solvatomorphs (2). One of the most relevant features among polymorphic modifications is the difference in their solubility and dissolution rate that affect their bioavailability (3-5).In crystal hydrates/solvates, the combination of intermolecular forces (hydrogen bonding) and crystal packing can produce very strong solvent-solid interactions leading to completely new properties in the solid state (6, 7). Some stable solvatomorphs require vigorous conditions for desolvation before melting, while others lose the solvent of crys- Identification and characterization of different forms of methotrexate were carried out by crystallization from different solvents. Five different forms of the drug were obtained. Appearance of a desolvation endotherm in the DSC accompanied by mass loss in TGA for forms I, II, IV and V showed these forms to be acetonitrile solvate hydrate (form I), trihydrate (forms II and IV) and dimethylformamide solvate (form V), respectively. However, the desolvation peak was absent in form III (obtained from methanol) indicating the absence of any solvent of crystallization. This form was found to be partially crystalline by its XRPD pattern. Solution calorimetry was further used to differentiate between the forms as they differ in lattice energy, resulting in different enthalpies of solution. The dissolution and solubility profiles were correlated with the enthalpy of solution and subsequently with crystallinity of all the forms; the least endothermic form (form III) had the highest dissolution rate.

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Characterization of a novel polymorphic form of celecoxib

Cited by 88 publications

References 17 publications

Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Beta-casein nanocarriers of celecoxib for improved oral bioavailability

Miniaturized Assay for Solubility and Residual Solid Screening (SORESOS) in Early Drug Development

Characterization of solvatomorphs of methotrexate using thermoanalytical and other techniques

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