Tablet Formulation and Enhancement of Aqueous Solubility of Efavirenz by Solvent Evaporation Co-Crystal Technique

Rajurkar, Vikas G.; Sunil, Nagare Amit; Ghawate, Vilas

doi:10.4172/2161-0444.1000002

Cited by 18 publications

(16 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The latter characterizes the frictional force within a powder, and a value of 20–30° indicates good flow properties. 12 Ɵ was determined using Equation (1 ):…”

Section: Methodsmentioning

confidence: 99%

<p>Simvastatin-Nicotinamide Co-Crystals: Formation, Pharmaceutical Characterization and in vivo Profile</p>

Khan¹,

Ahmad²,

Idrees³

2020

DDDT

View full text Add to dashboard Cite

Purpose: To enhance the solubility and dissolution profile of simvastatin (SIM) through cocrystallization with varying ratios of nicotinamide (NIC) using various co-methods. Materials and Methods: Twelve SIM:NIC co-crystal formulations (F01-F12) were prepared using dry grinding, slurry, liquid-assisted grinding, and solvent-evaporation methods, and their properties compared. Optimized formulations were selected on the basis of dissolution profiles and solubility for in vivo studies. The angle of repose, Carr Index and Hausner ratio were calculated to evaluate flow properties. Differential light scattering (DLS) was used to estimate particle-size distribution. Scanning electron microscopy (SEM) was employed to evaluate surface morphology. Thermal analyses and Fourier-transform infrared (FTIR) spectroscopy were used to determine the ranges of thermal stability and physical interaction of formulated co-crystals. X-ray powder diffraction (XPD) spectroscopy was used to determine the crystalline nature. Solubility and dissolution studies were undertaken to determine in vitro drug-release behaviors. Results: Micromeritic analyses revealed the good flow properties of formulated co-crystals. DLS showed the particle size of co-crystals to be in the nanometer range. SEM revealed that the co-crystals were regular cubes. Thermal studies showed the stability of co-crystals at >300°C. FTIR spectroscopy revealed minor shifts of various peaks. XPD spectroscopy demonstrated cocrystal formation. The formulations exhibited an improved dissolution profile with marked improvements in solubility. In vivo studies showed a 2.4-fold increase in C max whereas total AUC (0-∞) was increased 4.75-fold as compared with that of SIM tablets. Conclusion: Co-crystallization with NIC improved the solubility and dissolution profile and, hence, the bioavailability of the poorly water-soluble drug SIM.

show abstract

“…The latter characterizes the frictional force within a powder, and a value of 20–30° indicates good flow properties. 12 Ɵ was determined using Equation (1 ):…”

Section: Methodsmentioning

confidence: 99%

<p>Simvastatin-Nicotinamide Co-Crystals: Formation, Pharmaceutical Characterization and in vivo Profile</p>

Khan¹,

Ahmad²,

Idrees³

2020

DDDT

View full text Add to dashboard Cite

show abstract

“…Previous studies reported attempts to improve solubility and dissolution of EFV by solid dispersion and drug milling 11,12 . It was also revealed that EFV shows improved pharmaceutical properties by cocrystallization with adipic acid 13 , lactic acid 14 , glutaric acid 15 .…”

Section: Issn: 2250-1177mentioning

confidence: 99%

Crystal Engineering of Antiviral Agent Efavirenz for Solubility Enhancement

Gadade¹,

Pekamwar

Shirsat³

2018

J. Drug Delivery Ther.

View full text Add to dashboard Cite

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.

show abstract

“…DSC analysis was performed using Linseis DSC PT1000. Approximately 5 mg of the powder sample was placed in an aluminum pan and heated at a rate of 10 °C/min, from 0 to 300 °C temperature range, under nitrogen stream [19,20].…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

The Development of Glibenclamide-Saccharin Cocrystal Tablet Formulations to Increase the Dissolution Rate of the Drug

et al. 2019

View full text Add to dashboard Cite

Objective: Cocrystallisation is a promising method in order to increase the solubility and dissolution of poorly water-soluble drugs. The aim of this study was to prepare, formulate and evaluate glibenclamide (GCM) cocrystal in direct compress tablet dosage form using saccharin (SAC) as the coformer. Methods: GCM cocrystal with various stoichiometric ratios were prepared by the solvent drop grinding method. The co-crystal was characterized by a saturated solubility test and dissolution rate test, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-Ray Diffraction (PXRD). The tablet dosage form of GCM was formulated and evaluated compare with the conventional dosage form. Results: The solubility and dissolution rate of GCM-SAC cocrystals increased significantly compared with pure GCM, especially for 1:2 of ratio. The dissolution rate of cocrystal with ratio 1:2 increased by almost 91.9% compared with pure GCM. Based on the FTIR analysis, it showed the shifting of characteristic bands of GCM in the spectrum and there was no chemical reaction in GCM cocrystal. In PXRD measurement, the new crystalline peak was detected in the crystal habit of cocrystal compared with pure GCM and coformer. The new single melting of GCM-SAC cocrystal also was detected in DSC measurement. The tablets of GCM-SAC cocrystal were successfully prepared by direct compression method which rapidly disintegrated (1 min) and has higher dissolution compared with its pure form (32.36% greater than glibenclamide after 45 min). Conclusion: The tablet dosage form of GCM cocrystal with SAC as coformer was successfully prepared, formulated and improved its solubility and dissolution rate.

show abstract

Tablet Formulation and Enhancement of Aqueous Solubility of Efavirenz by Solvent Evaporation Co-Crystal Technique

Cited by 18 publications

References 15 publications

<p>Simvastatin-Nicotinamide Co-Crystals: Formation, Pharmaceutical Characterization and in vivo Profile</p>

<p>Simvastatin-Nicotinamide Co-Crystals: Formation, Pharmaceutical Characterization and in vivo Profile</p>

Crystal Engineering of Antiviral Agent Efavirenz for Solubility Enhancement

The Development of Glibenclamide-Saccharin Cocrystal Tablet Formulations to Increase the Dissolution Rate of the Drug

Contact Info

Product

Resources

About