Percutaneous Absorption of Dexamethasone Acetate and Palmitate, and the Plasma Concentration

To investigate quantitatively the percutaneous absorption of dexamethasone acetate (DA) and palmitate (DP), gel and petrolatum ointments were prepared and applied to rat skin. DA in the presence of absorption enhancers (Azone® and sorbitan monooleate) was rapidly absorbed, in the form of dexamethaso...

Full description

Saved in:
Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 35; no. 10; pp. 4263 - 4270
Main Authors OGISO, TARO, ITO, YOSHIMASA, IWAKI, MASAHIRO, ATAGO, HIDEHIKO, TANAKA, CHIKAKO, MANIWA, NORIKO, ISHIDA, SADAHIRO
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1987
Maruzen
Japan Science and Technology Agency
Subjects
absorption enhancer
Animals
Applied sciences
Azone
Dexamethasone - analogs & derivatives
Dexamethasone - blood
Dexamethasone - pharmacokinetics
dexamethasone acetate
dexamethasone palmitate
Exact sciences and technology
gel ointment
in vitro release rate
Male
Other techniques and industries
percutaneous absorption
petrolatum ointment
plasma concentration
rat
Rats
Rats, Inbred Strains
Skin Absorption
Online AccessGet full text

Cover

More Information
Summary:To investigate quantitatively the percutaneous absorption of dexamethasone acetate (DA) and palmitate (DP), gel and petrolatum ointments were prepared and applied to rat skin. DA in the presence of absorption enhancers (Azone® and sorbitan monooleate) was rapidly absorbed, in the form of dexamethasone, through the skin, whereas the absorption after application of DA ointment without enhancers was relatively poor. DP was also efficiently absorbed in the presence and absence of enhancers, with bioavailability of 5.3 and 4.1%, respectively. The absorbed DP was slowly hydrolyzed in the systemic circulation. The percutaneous absorption of drugs from the petrolatum ointments with enhancers was slower than that from the gel ointments. The in vitro release rates of DA and DP from the gel ointments with enhancers were 7.3 and 6.1 mg/h1/2, respectively and were much higher than those from the petrolatum ointments. The partition coefficient of DP was much larger than that of DA. Thus, it is suggested that DA and DP gel ointments with enhancers are effective in terms of high absorption into the circulation.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.35.4263