Physicochemical characterization of solid dispersions of indomethacin with PEG 6000, Myrj 52, lactose, sorbitol, dextrin, and Eudragit E100.
The purpose of this study was to prepare and characterize solid dispersions of indomethacin with polyethylene glycol (PEG) 6000, Myrj 52, Eudragit E100, and different carbohydrates such as lactose, mannitol, sorbitol, and dextrin. Indomethacin is a class II substance according to the Biopharmaceutics Classification System. It is a poorly water soluble antirheumatic agent. The goal was to investigate whether the solid dispersion can improve the dissolution properties of indomethacin. The solid dispersions were prepared by three different methods depending on the type of carrier. The evaluation of the properties of the dispersions was performed using solubility measurements, dissolution studies, Fourier-transform infrared spectroscopy, and x-ray powder diffractometery. The results indicate that lactose, mannitol, sorbitol, and especially Myrj 52 are suitable carriers to enhance the in vitro dissolution rate of indomethacin at pH 7.2. Eudragit E100, Myrj 52, and mannitol increase the dissolution properties at pH 1.2. The data from the x-ray diffraction showed that the drug was still detectable in its solid state in all solid dispersions except solid dispersions with dextrin and high amounts of mannitol. However, the results from infrared spectroscopy together with those from x-ray diffraction showed well-defined drug-carrier interactions for dextrin coevaporates.
Valizadeh
Hadi
H
Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. hvalizadeh@noavar.com
Nokhodchi
Ali
A
Qarakhani
Nahid
N
Zakeri-Milani
Parvin
P
Azarmi
Shirzad
S
Hassanzadeh
Davood
D
Löbenberg
Raimar
R
D000179:Acrylates / Q000737:chemistry; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003912:Dextrins / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007213:Indomethacin / Q000737:chemistry*; D007785:Lactose / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D013012:Sorbitol / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013997:Time Factors; D014961:X-Ray Diffraction
D000179:Acrylates; D003912:Dextrins; D004337:Drug Carriers; C477020:Eudragit E100; D005079:Excipients; D011108:Polymers; D011092:Polyethylene Glycols; D013012:Sorbitol; D007785:Lactose; D007213:Indomethacin