Sildenafil vaginal suppositories: preparation, characterization, in vitro and in vivo evaluationopen access
- Authors
- Shanmugam, Srinivasan; Kim, Young-Hun; Park, Jeong-Hee; Im, Ho Taek; Sohn, Young Taek; Kim, Kyeong Soo; Kim, Yong-Il; Yong, Chul Soon; Kim, Jong Oh; Choi, Han-Gon; Woo, Jong Soo
- Issue Date
- Jun-2014
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Intravaginal delivery; PK/biodistribution; release kinetics; sildenafil; vaginal suppositories
- Citation
- DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, v.40, no.6, pp.803 - 812
- Indexed
- SCIE
SCOPUS
- Journal Title
- DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
- Volume
- 40
- Number
- 6
- Start Page
- 803
- End Page
- 812
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/22847
- DOI
- 10.3109/03639045.2013.788011
- ISSN
- 0363-9045
- Abstract
- Aim: The main objective was to investigate the in vitro release profile/kinetics, and in vivo plasma pharmacokinetics (PK) and organ biodistribution (BD) of the prepared sildenafil vaginal suppositories (SVS). Methods: Suppositories containing 25 mg of sildenafil were prepared by the cream melting technique using Witepsol H-15 as a suppository base. The suppositories were characterized for weight variation, content uniformity, hardness, disintegration time and crystallinity change. The in vitro dissolution in pH 4.5, and in vivo plasma PK and organ BD of sildenafil from SVS in female Sprague Dawley rats, were also investigated. Results: The mean weight variation, content uniformity, hardness and disintegration time of the prepared SVS were 1.127 +/- 0.020 g, 98.25 +/- 2.50%, 2.5 +/- 0.08 kg and 9 +/- 1.0 min, respectively. The release of sildenafil from the SVS was more than 90% at 30 min, with a release kinetic of Hixson-Crowell model and non-Fickian diffusion (n = 0.464). The plasma PK study demonstrated a significantly lower C-max (similar to 10 times) and AUC(0-24) (h) (similar to 13 times) of sildenafil in plasma following intravaginal (IVG) administration of suppositories compared to oral (PO) administration of sildenafil solution. Nevertheless, the organ BD study showed a phenomenally higher C-max (similar to 40 times) and AUC(0-24 h) (similar to 20 times) of sildenafil in uterus following IVG administration of suppositories than PO administration of sildenafil solution. Conclusion: This study demonstrated enhanced sildenafil exposure in the uterus following IVG administration of SVS, which could be used to target the uterus for therapeutic benefits.
- Files in This Item
-
Go to Link
- Appears in
Collections - COLLEGE OF PHARMACY > DEPARTMENT OF PHARMACY > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/22847)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.