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At least 181 records · Page 10Linked to original sources
PubMed1986

Pharmaceutical evaluation of hollow type suppositories. V. Preparation of valproic acid suppository and rectal absorption of valproic acid in rabbits.

Seven kinds of suppositories were constructed with oleaginous base materials (Witepsol H-15 (H-15) and E-85 (E-85]: a conventional type suppository containing valproic acid (VPA) mixed with E-85 (I), a conventional type suppository containing sodium salt of VPA (sodium valproate) (S-VPA) mixed with H-15 (II), hollow type suppositories containing VPA in the forms of oily liquid (free acid) (III), macrogol 1000 or 6000 mixture (IV or V), powder (S-VPA) (VI) and aqueous solution (S-VPA was dissolved in 0.9% NaCl solution) (VII) in each cavity. The content of VPA in type I was decreased considerably by volatility and type II was found to be hygroscopic. Therefore conventional type suppositories containing VPA or S-VPA were not of practical use, whereas III and VI prevented volatility of VPA and minimized the hygroscopic property of S-VPA. Plasma concentration of VPA was measured in rabbits after rectal administrations of III, IV, VI and VII. By using VI, the highest values of the mean of the peak plasma VPA concentration (Cmax) (49.8 +/- 2.6 micrograms/ml) and the mean of the area under the plasma concentration-time curve (AUC) (90.0 +/- 3.7 h X micrograms/ml) were obtained. The Cmax and the AUC estimated after administration of VII were not significantly different from those of VI. The Cmax and the AUC were lower with III than with IV, VI or VII but the extent of bioavailability (EBA) of III was about 80%.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMedDate not supplied

Absorption of rectally administered phenytoin: a pilot study.

OBJECTIVE: To test the hypothesis that rectally administered phenytoin is absorbed in healthy volunteers. DESIGN: This single-center, open-label crossover pilot study compared rectal absorption with intravenous administration of phenytoin injectable solution (7 mg/kg) in healthy volunteers. Twelve serial blood samples were taken from each volunteer beginning at time zero until 36 hours following administration. These were analyzed for presence of phenytoin by immunoassay. SETTING: The study took place at St. Paul's Hospital, a tertiary care center. PARTICIPANTS: Funding permitted for a sample size of five healthy participants, two men and three women, aged 21-45 years. Selection was by volunteer sample. Inclusion criteria were as follows: no known medical conditions, not receiving medication, no history of adverse drug reactions or allergies, not known to be pregnant, and normal liver function as determined per study protocol. MAIN OUTCOME MEASURES: Signs of absorption as indicated by presence of phenytoin in blood samples, maximum concentrations (Cmax), time to Cmax (tmax), AUC, and apparent bioavailability. RESULTS: Maximum mean concentrations of 2.4+/-1.1 mg/L (mean +/- SD) following rectal administration and 11.2+/-1.6 mg/L following intravenous administration were achieved during the first one to two hours (tmax in both treatment arms). Mean apparent bioavailability of the rectally administered phenytoin was 24.4+/-13.4% (15.8-44.1%). CONCLUSIONS: Results from this pilot study demonstrate that rectal absorption of phenytoin begins within 30 minutes following single-dose administration and was reported by four out of five volunteers to be the preferred route. Further studies are required before extrapolation can be made to the patient population.

Administration, Rectal↗
PubMed1989

The influence of a non-ionic surfactant on rectal absorption of virus particles.

A bacterial virus, suspended in three different vehicles, was introduced into the rectum of rabbits. The virus was detected in the circulating blood as early as 10 min after the administration. The quantity of virus found in blood and the duration of its presence, were enhanced when a non-ionic surfactant was used as vehicle of the virus.

Animals↗
PubMed1998

Nitric oxide donors enhance rectal absorption of macromolecules in rabbits.

PURPOSE: The objective of this investigation is to evaluate the potential of nitric oxide (NO) donors as a new class of absorption enhancers which may act on intestinal epithelial cells through epithelial actions of the chemical mediator, NO. METHODS: Suppositories containing NO donors and insulin were administered into the rabbit rectum. After administration of the suppository, blood samples were collected from the auricular vein. The plasma insulin and glucose concentrations were determined. RESULTS: The NO donor S-nitroso-N-acetyl-DL-penicillamine (SNAP, 4 mg) induced a significant increase in the rate of insulin absorption from the rectum. Administration of a suppository containing SNAP without insulin affected neither the plasma insulin nor the plasma glucose concentration. Other NO donors, NOR1 and NOR4, also induced increases in the insulin absorption. The absorption enhancement effect of SNAP was inhibited by coadministration of the NO scavenger carboxy-PTIO. SNAP also enhanced FITC-dextran (MW 4,000) absorption. Little cytotoxicity of SNAP (3.0 mg/ml) as assessed in terms of the rate of lactate dehydrogenase (LDH) release from Caco-2 cells was detected for 2 h of incubation. CONCLUSIONS: These findings suggest that NO enhanced macromolecular absorption from the rectum without mucosal cell damage, and that NO donors can act as potent absorption enhancers.

Animals↗
PubMed1979

Rectal absorption of short chain fatty acids in the absence of chloride.

The absorption of short chain fatty acids by the human rectum in the absence of chloride has been studied using a dialysis bag technique. Absorption rates of sodium, water, and short chain fatty acids were unchanged on replacing chloride with sulphate. Final concentrations of bicarbonate were 35.4 +/- 3.4 mmol/l in the presence of chloride and 37.1 +/- 5.2 mmol/l in the absence of chloride. The rates of movement of bicarbonate into the dialysates were similar. If bicarbonate is secreted in exchange for chloride then it also appears to be secreted in exchange for absorbed short chain fatty acids.

Adult↗