Solubility Enhancement of Lornoxicam by Crystal Engineering

Gadade, Dipak D.; Kulkarni, Deepak; Rathi, P. B.; Pekamwar, Sanjay S.; Joshi, Suresh G.

doi:10.4172/pharmaceutical-sciences.1000226

Cited by 25 publications

(17 citation statements)

References 29 publications

(31 reference statements)

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“…(6-Chloro-4-hydroxy-2-methyl-N-2-pyridinyl-2H-thieno[2,3-e]-1,2thiazine-3-carboxamide 1,1-dioxide, C13H10ClN3O4S2, Fig.1) is a non-steroidal antiinflammatory drug (NSAID) that belongs to the "oxicam" class, which presents analgesic, anti-inflammatory and antipyretic properties [1,2,3]. It is used in musculoskeletal and joint disorders such as osteoarthritis and rheumatoid arthritis.…”

Section: Lornoxicammentioning

confidence: 99%

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Lornoxicam drug—A new study of thermal degradation under oxidative and pyrolysis conditions using the thermoanalytical techniques, DRX and LC-MS/MS

et al. 2019

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In the present work, the thermal behavior of Lornoxicam drug was studied under oxidizing (air) and pyrolysis (N2) atmospheres using simultaneous thermogravimetry and differential scanning calorimetry (TG-DSC), differential scanning calorimetry (DSC), Hot Stage Microscopy (HSM) and Evolved Gas Analysis (EGA) in the form of thermogravimetry coupled to infrared spectroscopy (TG-FTIR) and mass spectrometry (TG-MS). The thermal degradation product formed at different temperatures were examined using liquid chromatography coupled to mass spectrometry (LC-MS) and Powder X-Ray Diffraction (PXRD). The thermal study showed that the drug does not melt, partially amorphized on heating, it is thermally stable to 205 °C and undergoes thermal decomposition in two overlapping mass loss steps. Furthermore, the DSC and MS techniques suggest that thermal degradation processes are very complex, which occur with the release of gaseous products HCN, SO2, COS, CO2, N2O and CO and formation of three intermediate in the thermal residue.

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Section: Lornoxicammentioning

confidence: 99%

“…The thermal decomposition of Lornoxicam in pyrolytic and oxidative atmosphere has been previously reported [5,[13][14][15][16][17][18][19]. However, the thermal degradation products have not been previously investigated, and the thermal degradation mechanism of this drug is unknown.…”

Section: Lornoxicammentioning

confidence: 99%

Lornoxicam drug—A new study of thermal degradation under oxidative and pyrolysis conditions using the thermoanalytical techniques, DRX and LC-MS/MS

et al. 2019

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“…When two distinct layers were formed, they were separated and the solution was diluted and assay using UV-Spectroscopy by recording absorbance in triplicate. Concentration in both the phases was calculated using calibration equation and the partition coefficient was calculated for the cocrystal [38].…”

Section: Partition Coefficient Determinationmentioning

confidence: 99%

“…FTIR spectra and DSC thermograms of AVA cocrystal with IR tablet excipients -aerosil, MCC PH102, lactose and starch were recorded. The spectrums of cocrystal and cocrystal with excipients were matched for appearance or disappearance of any peak while the thermograms were matched for appearance or disappearance of any peak and enthalpy height [38].…”

Section: Ava Cocrystal -Excipient Compatibility Studymentioning

confidence: 99%

Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

Trivedi¹,

Borkar²,

Puranik³

2020

jrp

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The objective of the present work was to prepare cocrystals of poorly soluble drug Atorvastatin Calcium (AVA) with the aim of increasing its solubility and dissolution properties. Screening of 8 cocrystal formers (CCFs) was performed by Hansen solubility parameter (HSPs) using 4 methods-neat grinding, solvent drop grinding, solvent evaporation and sonocrystallization in equimolar ratio. Solubility of AVA cocrystal (1.9 fold increase) in comparison to plain AVA drug has been demonstrated with solubility experiments. FTIR spectra of AVA cocrystal showed disappearance of O-H group indicating the formation of hydrogen bond synthon between the drug and CCFs. DSC thermogram showed drastic reduction in melting point from 164.6°C to 71.9 °C indicating the reduction in cohesive energy and increase in solubility. XRD pattern showed new crystalline peaks at 2θ values of 9.858°, 15.201°, 22.907°, 25.407°, 29.496°. SEM analysis showed changes in the morphological characteristics as compared to drug and CCFs, indicating different crystalline nature. Experimental design was applied to optimize AVA cocrystal IR tablet for concentration of aerosil (X1) and MMC 102 (X2) and were evaluated for drug release (Y1) and friability (Y2). It was found that as the concentration of aerosil and MMC 102 increased friability decreased and %drug release increased. A drug release of 98.54±1.163% and friability of 0.515±0.090 % was obtained for optimized batch. Ex vivo diffusion study was carried out by isolating rat stomach tissue, exhibiting higher drug release (95.71±0.98 %) than plain AVA and marketed tablet. Thus formulating AVA cocrystal and its subsequent formulation in optimized IR tablet gives a promising opportunity for manufacturing a drug with increased bioavailability.

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“…Fourier transform infrared spectroscopy (FTIR) was employed for the vibrational spectroscopic analysis of the active pharmaceutical ingredient (API)-EFV and its cocrystals with a coformer-FA obtained by NG method 18 . The FTIR spectrums were recorded with the FTIR spectrophotometer with ATR attachment (Bruker; ALPHA-T) and the scanning range was in between 4000-660 cm -1 .…”

Section: Atr-fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Crystal Engineering of Antiviral Agent Efavirenz for Solubility Enhancement

Gadade¹,

Pekamwar

Shirsat³

2018

J. Drug Delivery Ther.

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In the current study, we attempted to improve the physicochemical properties of antiviral drug efavirenz through the cocrystal synthesis. The neat grinding performed to study the effect of coformer-fumaric acid (FA) on solubility and dissolution of efavirenz, which can serve as the green cocrystal synthesis approach. The prepared cocrystals were characterized for characteristics like powder flow properties, aqueous saturation solubility, in vitro powder dissolution study. The synthesized cocrystals were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction. The formation of a cocrystal of efavirenz and caffeine was confirmed by the characterization techniques which suggests the interactions between efavirenz and coformer-fumaric acid leads to cocrystal formation. The powder flow properties, solubility, and dissolution profile of efavirenz are significantly improved by its cocrystallization.

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Solubility Enhancement of Lornoxicam by Crystal Engineering

Cited by 25 publications

References 29 publications

Lornoxicam drug—A new study of thermal degradation under oxidative and pyrolysis conditions using the thermoanalytical techniques, DRX and LC-MS/MS

Lornoxicam drug—A new study of thermal degradation under oxidative and pyrolysis conditions using the thermoanalytical techniques, DRX and LC-MS/MS

Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

Crystal Engineering of Antiviral Agent Efavirenz for Solubility Enhancement

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