IN-VITRO TRANSFER, PERMEABILITY AND INCLUSION COMPLEXATION OF A NOVEL POTENT SYNTHETIC ANDROGEN, METHYL NORTESTOSTERONE ACETATE, COMPARED WITH TESTOSTERONE | ||
| Bulletin of Pharmaceutical Sciences Assiut University | ||
| Article 8, Volume 20, Issue 2, December 1997, Pages 169-179 PDF (670.29 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/bfsa.1997.68757 | ||
| Author | ||
| Sayed M. Ahmed | ||
| Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt | ||
| Abstract | ||
| The solubility, dissolution, in-vitro transfer from aqueous to organic phase, and in-vitro permeability of a potent nortestosterone ester, methyl nortestosterone acetate (NTA), compared with testosterone (T) in the absence and in the presence of hydroxypropyl-b-cyclodextrin (HP-b-CD) were investigated. The phase solubility diagrams of both drugs revealed the formation 1:1 inclusion complexes with HP-b-CD of AL-type at 30°, 70° and 45°C. The solubility of NTA and T were increased approximately 7000 fold and 500 fold, respectively, in the presence of 0.12 M HP-b-CD at 37°C. NTA interacted more strongly with HP-b-CD than T, a fact that led to a much better enhancement in the dissolution rate. Such inclusion complexation led to noticeable decrease in the transfer rate of both androgens from the aqueous to the organic phase compared with the drug alone. Finally, it was found that HP-b-CD enhanced the in-vitro permeability of NTA and T from Klucel gel formulations. | ||
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