Controlled release matrix tablets for diclofenac sodium were developed in this study. Five matrix-tablet formulations were prepared by granulating two viscosity grades of HPMC (hydroxylpropylmethylcellulose) in varying ratios with water in the planetary mixer. The in-vitro dissolution tests indicate that all five matrix formulations prolong the release of diclofenac sodium. The main factors controlling drug release were the HPMC viscosity grade and the amount of HPMC used. The larger the amount of high viscosity grade HPMC used, the slower the resultant release rate of diclofenac sodium. There was no significant degradation of diclofenac sodium or change in drug release rate in any of the five formulations during a three-month period of stability testing. The sustained release ability of four formulations was further demonstrated in an in-vivo study in six healthy subjects. There were in-vitro/in-vivo correlations between Cmax, AUC0-14, and the time for 50 or 80% drug to be released.

The effect of grinding on the physicochemical properties of ground mixtures of crystalline drugs (acetaminophen, warfarin, indomethacin, diazepam and hydrocortisone acetate) with B-cyclodextrin was studied by IR analysis, x-ray diffraction method and thermal analysis. The crystallinities of drugs decreased with increasing grinding time and became amorphous or nearly amorphous, which depended on drug moiety and cavity size of B-cyclodextrin. The result indicates that acetaminophen became amorphous and only formed an inclusion complex in the ground mixture with B --J

No abstract

No abstract