Topic
Rectal Absorption
About: Rectal Absorption is a research topic. Over the lifetime, 247 publications have been published within this topic receiving 4423 citations.
Papers published on a yearly basis
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Papers
Journal Article•
TL;DR: Log dose/effect curves were established for i.m. insulin in adult male rats, and administration in a solution containing 5% sodium glycocholate, an absorption-promoting adjuvant, increased insulin efficacy by each route.
Abstract: The purpose of this investigation was to develop a method to quantitate insulin absorption, and to compare insulin absorption from various noninjection sites of administration. Log dose/effect curves were established for i.m. insulin in adult male rats. The effects measured were the maximum change in plasma glucose concentration and the cumulative percentage of change in plasma glucose concentrations from 0 to 4 hr. Both log dose/effect curves gave similar results when calculating the efficacy of other routes, relative to i.m. Nasal, buccal, sublingual and rectal absorption sites were isolated by ligation procedures or with physical barriers. Rectal insulin was more efficacious than nasal, buccal and sublingual insulin, when administered without an absorption-promoting adjuvant. However, the efficacy relative to i.m. insulin was low for each route, probably due to a combination of slow membrane permeation and metabolism at the absorption site. Administration in a solution containing 5% sodium glycocholate, an absorption-promoting adjuvant, increased insulin efficacy by each route. The rank order was nasal greater than rectal greater than buccal greater than sublingual, with nasal and rectal insulin being roughly half as efficacious as i.m. insulin. Orally administered insulin, at doses 5 times higher than administered by other routes, and with Na glycocholate, produced no hypoglycemic response.
189 citations
TL;DR: Laureth-9, a nonionic surfactant which irreversibly removes membrane proteins or lipids, promoted insulin absorption from each site, and the enhancing effects of Na salicylate and Na2EDTA, which have reversible mechanisms of permeability enhancement, were specific for rectal absorption.
Abstract: The site dependence of the absorption-promoting actions of laureth-9, Na salicylate, Na2EDTA, and aprotinin was studied in rats. Insulin absorption was estimated on the basis of the cumulative hypo-glycemic response from 0 to 4 hr postdose, relative to that after intramuscular insulin. Insulin was administered with or without adjuvants to isolated rectal, nasal, and buccal absorption sites. Laureth-9, a nonionic surfactant which irreversibly removes membrane proteins or lipids, promoted insulin absorption from each site. The rectal, nasal, and buccal routes were 30% as effective as the i.m. route. The enhancing effects of Na salicylate and Na2EDTA, which have reversible mechanisms of permeability enhancement, were specific for rectal absorption. With these adjuvants, rectal insulin was 30–40% as effective as i.m. insulin, but nasal and buccal doses were less than 5% as effective as i.m. doses. This specificity can be at least partly explained by considering the site-to-site differences in membrane histology, although differences in pore size and membrane biochemistry might also contribute. The protease inhibitor aprotinin was ineffective in increasing insulin efficacy via each route, either alone or in combination with laureth-9.
161 citations
TL;DR: In Part II of this article, this discussion is extended to drugs which act peripherally and to methods of enhancing rectal drug absorption.
Abstract: Part I of this article, which appeared in the previous issue of the Journal, covered general considerations, the physiology of the rectum, spreading of drugs into the colon, rectal absorption, partial avoidance of first-pass elimination, rate-controlled rectal delivery of drugs, irritation of the rectal mucosa and clinical applications of rectal administration, and discussed centrally acting drugs. In Part II, this discussion is extended to drugs which act peripherally and to methods of enhancing rectal drug absorption. The overall summary appeared in Part I.
121 citations
TL;DR: In this article, the rectal absorption of diazepam was studied in man and compared with intravenous, intramuscular and oral administration, and it was calculated that the drug will not exhibit measurable first pass metabolism.
88 citations
TL;DR: The salt is probably a dihydrate as judged by microanalytical data and its infrared spectrum which showed absorption bands at 3200 (NH), 3420 and 1640 (H,O) and 21 10 cm-I (+N&).
Abstract: J. Pharm. Pharmacol. 1981.33: 334-335 Communicated November 25, 1980 and melted at 58'40 \"C by capillary and 123\"-125 \"C by hot-stage (Reichart) procedures. The salt is probably a dihydrate as judged by microanalytical data (Found: C, 28.12; H, 9-09; N, 22.02; CI, 28.36. Calc. for CeHloN,C1,.2H,0; C, 28.24; H, 9.4; N, 21.96; C1, 27.84%) and its infrared spectrum (paraffin mull, probable assignments in parentheses) which showed absorption bands at 3200 (NH), 3420 and 1640 (H,O) and 21 10 cm-I (+N&). I thank Mr Robert Shaw (Principal Pharmacist for Quality Control. East Anglia Regional Health Authority) for promoting my interest in TETA and providing samples and Mr F. Sels (Janssen Pharmaceutica, Beerse) for the microanalytical data.
87 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2021 | 1 |
| 2019 | 3 |
| 2017 | 1 |
| 2015 | 1 |
| 2014 | 2 |
| 2012 | 3 |