PREPARATION AND EVALUATION OF PHENYLTOLOXAMINE CITRATE MICROSPHERES

Document Type : Original Article

Authors

1 Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt

2 Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

3 Department of Physiology, Faculty of Medicine, Assiut University, Assiut, Egypt

Abstract

Microspheres of phenyltoloxamine citrate (PTC) with cellulose acetate butyrate (CAB) were prepared using an emulsion-solvent evaporation technique. Good reproducibility in microspheres preparation was observed. The recovery of drug from different microspheres varied between 87 and 94 %. The release rates of the drug from these microsphres were decreased as compared with that from the drug powder. Different release characteristics were obtained by changing the drug-to-polymer ratio and varying the particle size of micro spheres. As the polymer to drug ratio increased, the microsphere size distribution shifted to the smaller size and the release of the drug decreased. The release of the drug showed pH-dependence. The release kinetics of the drug from CAB microspheres were studied. The antihistamine and the analgesic activities of PTC alone and PTC microspheres were evaluated in vivo. The antihistamine and analgesic activities of the tested microspheres in vivo were found to be greater and more prolonged than that of the intact drug.