Preparation and characterization of co-grinded mixtures of aceclofenac and neusilin US2 for dissolution enhancement of aceclofenac.
The present study was carried out with a view to enhance the dissolution of poorly water-soluble BCS-class II drug aceclofenac by co-grinding with novel porous carrier Neusilin US(2.) (amorphous microporous granules of magnesium aluminosilicate, Fuji Chemical Industry, Toyama, Japan). Neusilin US(2) has been used as an important pharmaceutical excipient for solubility enhancement. Co-grinding of aceclofenac with Neusilin US(2) in a ratio of 1:5 was carried out by ball milling for 20 h. Samples of co-ground mixtures were withdrawn at the end of every 5 h. and characterized for X-ray powder diffraction, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. The analysis revealed the conversion of crystalline aceclofenac to its amorphous form upon milling with Neusilin US(2). Further, in vitro dissolution rate of aceclofenac from co-ground mixture was significantly higher compared to pure aceclofenac. The accelerated stability study of co-ground mixture was carried out at 40 degrees C/75%RH for 4 weeks, and it showed that there was no reversion from amorphous to crystalline form. Thus, it is advantageous to use a porous carrier like Neusilin US(2) in improvement of dissolution of poorly soluble drugs.
Vadher
Ambarish H
AH
A. R. College of Pharmacy and G. H. Patel Institute of Pharmacy, Vallabh Vidyanagar, 388 120, India.
Parikh
Jolly R
JR
Parikh
Rajesh H
RH
Solanki
Ajay B
AB
D017607:Aluminum Compounds; D000538:Aluminum Silicates / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D004008:Diclofenac / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D006860:Hydrogen Bonding; D008274:Magnesium / Q000737:chemistry*; D017616:Magnesium Compounds; D017640:Silicates; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
D017607:Aluminum Compounds; D000538:Aluminum Silicates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005079:Excipients; D017616:Magnesium Compounds; D017640:Silicates; D004008:Diclofenac; C033065:aluminum magnesium silicate; D008274:Magnesium; C056498:aceclofenac