IN-VITRO AND IN-VIVO EVALUATION OF SUSTAINED-RELEASE SUPPOSITORIES CONTAINING THEOPHYLLINE MICROSPHERES | ||||
Bulletin of Pharmaceutical Sciences Assiut University | ||||
Article 5, Volume 38, Issue 1, 2015, Page 91-98 PDF (438.49 K) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/bfsa.2015.63177 | ||||
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Authors | ||||
Gamal M. Mahrous1; Gamal A. Shazly* 1, 2; Sayed H. Auda1, 3; Hesham M. Tawfeek2 | ||||
1Department of Pharmaceutics, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia | ||||
2Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University 71526, Assiut, Egypt | ||||
3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy,Al-zhar University, Assiut, Egypt | ||||
Abstract | ||||
The sustained release microspheres of theophylline were formulated using non-solvent addition technique. The in-vitro dissolution of the drug from the fabricated microspheres that having size ranges of 300-600, 600-800 and 800-1000 µm was tested. The release of theophylline was extended over 8 hrs and it was found that the drug release decreased nonsignificantly as the particle size increased (p≥ 0.05). Incorporating theophylline-containing microspheres into suppository formulation using polyethylene glycol base resulted in a slight increase in dissolution rate, but still in a sustained release pattern over 8 hrs. In-vivo study of the prepared suppositories on beagle dogs revealed that the peak of theophylline serum concentration Cmax (mean±S.D) was 11.1+0.3 µg/mL. It was also found that AUC(0–24hrs) value averaged 154.7±20.3 µg-h/ml. The median peak time (Tmax) was 3.0 hrs and MRT was 13 hrs indicating a sustained effect. | ||||
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