Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
10
pubmed:dateCreated
1989-5-11
pubmed:abstractText
The purpose of this investigation was to first screen for potential effectiveness several rectal gels as insulin delivery systems and to select one promising dosage form as candidate for further evaluation in rabbits and man. Criteria for effectiveness were the "pharmacologic availability", determined as the ratio between the total area under the percent glucose reduction versus time curves upon rectal administration and the standard (I.V. for rabbits and S.C. for man), the maximum reduction in glucose blood concentration, the time to reach the maximum and the mean residence time of glucose reduction. The rectal gels consisted of emulsion systems prepared from pH 8 buffer solution containing insulin, an oleaginous phase, a surface active agent (bile salts, Myrj or Brij), and a viscosity increasing agent. The finally selected rectal gel was tested in rabbits both in a parallel and a crossover design in nondiabetic and diabetic animals. The selected rectal gel in nondiabetic and diabetic rabbits resulted in a pharmacologic availability of about 25%. By addition of Azone the pharmacologic availability was further increased, although not significantly (small n). In nondiabetic man the pharmacologic availability was about 32%, whereas the bioavailability (measured from plasma insulin) was only about 11%. Drugs undergoing hepatic first-pass metabolism and for which the liver is the biophase, should show increased pharmacologic availability with decreased bioavailability (if the latter one is due to first-pass effect).
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0379-0355
pubmed:author
pubmed:issnType
Print
pubmed:volume
10
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
645-56
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Rectal delivery system for insulin.
pubmed:affiliation
Division of Pharmaceutics and Drug Delivery Systems, University of Cincinnati Medical Center, OH.
pubmed:publicationType
Journal Article