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68757

IN-VITRO TRANSFER, PERMEABILITY AND INCLUSION COMPLEXATION OF A NOVEL POTENT SYNTHETIC ANDROGEN, METHYL NORTESTOSTERONE ACETATE, COMPARED WITH TESTOSTERONE

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Last updated: 04 Jan 2025

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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.

DOI

10.21608/bfsa.1997.68757

Authors

First Name

Sayed

Last Name

Ahmed

MiddleName

M.

Affiliation

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

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Orcid

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Volume

20

Article Issue

2

Related Issue

10408

Issue Date

1997-12-01

Receive Date

1997-09-30

Publish Date

1997-12-31

Page Start

169

Page End

179

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 20_Issue 2_Pages 169-179.pdf

PDF . 686.4kB

Link

https://bpsa.journals.ekb.eg/article_68757.html

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https://bpsa.journals.ekb.eg/service?article_code=68757

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8

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Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

IN-VITRO TRANSFER, PERMEABILITY AND INCLUSION COMPLEXATION OF A NOVEL POTENT SYNTHETIC ANDROGEN, METHYL NORTESTOSTERONE ACETATE, COMPARED WITH TESTOSTERONE

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Article

Created At

22 Jan 2023