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PubMed1979

Rectal aspirin--absorption and antipyretic effect.

Rectal acetylsalicylic acid was given to 14 children who had undergone open heart surgery. The effect on their temperatures was similar whether 15--30 or 30--50 mg/kg was given. Either dose was more effective than no treatment. The greatest fall in temperature occurred after 4 or 5 hours. Rectal aspirin in a triglyceride base is effective in lowering postoperative temperature. It should also be of use in treating other fevers. A dose of 20--25 mg/kg is suggested.

Adolescent↗
PubMedDate not supplied

Rectal versus oral absorption of codeine phosphate in man.

Rectal absorption of codeine phosphate from various dosage forms was studied in man. The rectal dosage forms included aqueous solutions and fatty suppositories. A comparison was made with an orally administered solution. The plasma concentrations of codeine were measured by means of HPLC analysis after a single dose of 60 mg codeine phosphate in a cross-over study in 7 volunteers. Compared with oral dosing rectal absorption from an aqueous solution or a fatty suppository produced an almost identical plasma concentration profile with similar interindividual variations. Comparing the absorption rate characteristics it appeared that rectal absorption from an alkaline solution containing codeine phosphate proceeded significantly (P less than 0.05) more rapid than after oral dosing. No essential difference in bioavailability was observed between the various rectal and oral dosage forms.

Administration, Oral↗
PubMed1989

3-Amino-1-hydroxypropylidene-1,1-diphosphonate (APD): a novel enhancer of rectal cefoxitin absorption in rats.

The promoting action of the calcium chelating compound EDTA on intestinal drug absorption is supposed to be based on Ca2+ depletion, inducing widening of tight junctions. The aim of the present study was to evaluate the effects of the calcium-binding agent 3-amino-1-hydroxypropylidene-1,1-diphosphonate disodium salt (APD) on rectal cefoxitin absorption in rats. The extent of rectal cefoxitin absorption was enhanced by 0.5 to 6% w/v of APD, on rectal infusion as well as on bolus delivery, the latter regimen tending to result in lower bioavailabilities. A maximal cefoxitin bioavailability of 85 +/- 10% was achieved by infusion with 4% w/v of APD, compared with 14 +/- 12% without APD.

Animals↗
PubMed1987

Evidence for large intestinal control of potassium homoeostasis in uraemic patients undergoing long-term dialysis.

1. The role of the large intestine in the maintenance of K+ balance in uraemic patients established on long-term dialysis was studied with a rectal dialysis technique in 14 normal subjects, ten normokalaemic patients undergoing chronic ambulatory peritoneal dialysis (CAPD), and seven patients undergoing haemodialysis. Dietary K+ intakes in the normal subjects, CAPD patients and haemodialysis patients were 80-100 mmol/24 h, 70-80 mmol/24 h and 60-70 mmol/24 h, respectively. 2. At an initial intraluminal K+ concentration of 45 mmol/l, rectal K+ secretion in the CAPD patients (2.4 +/- 0.4 mumol h-1 cm-2) was greater than in normal subjects (1.2 +/- 0.2 mumol h-1 cm-2, P less than 0.02). Under similar conditions, rectal K+ secretion was also greater in the haemodialysis patients than in normal subjects, both predialysis (3.7 +/- 0.4 mumol h-1 cm-2, P less than 0.001) and postdialysis (2.4 +/- 0.5 mumol h-1 cm-2, P less than 0.05), even though haemodialysis decreased plasma K+ concentration from 5.3 +/- 0.1 mmol/l to 3.5 +/- 0.2 mmol/l (P less than 0.001). 3. There were no significant differences in rectal Na+ absorption, rectal potential difference, plasma aldosterone concentration, or total body K+ content (measured by whole-body counting of 40K), between the normal subjects and either the CAPD or the haemodialysis patients. 4. These results indicate that K+ homoeostasis is maintained in uraemic patients undergoing long-term dialysis by a combination of K+ losses during dialysis, and enhanced large intestinal K+ excretion.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1993

Excretion in the house cricket: stimulation of rectal reabsorption by homogenates of the corpus cardiacum.

1. We describe an in vitro perfused preparation of Acheta domesticus rectum which allows direct comparison of Malpighian tubule secretion and rectal absorption under identical conditions. Rectal absorption is stimulated four- to sixfold by corpora cardiaca (CC) homogenates and the stimulated rate is sufficiently rapid to account for all the fluid secreted by the tubules. 2. The time course for increased fluid absorption is similar to that required to stimulate electrogenic chloride transport in locusts and grasshoppers. Chloride is rapidly absorbed by the rectum under all conditions, along with lesser amounts of Na+ and K+. Unlike the situation in locusts, K+ uptake is unaffected by CC homogenates and the stimulated absorbate is NaCl-rich, similar in composition to the NaCl-rich tubule fluid produced under stimulated conditions. The absorbate is always slightly hypo-osmotic to the perfusate, reaching a maximum differential of approximately 15 mosmol l-1 following CC stimulation. 3. The antidiuretic factor that reduces tubule secretion does not promote fluid reabsorption by the rectum.

Absorption↗
PubMed1989

The effect of local anaesthetics on epinephrine absorption following rectal mucosal infiltration.

This study was undertaken to investigate the effects of lidocaine and bupivacaine on epinephrine absorption following rectal mucosal infiltration, to assess the cardiovascular and metabolic effects of the absorbed epinephrine and to compare the systemic absorption of the local anaesthetics employed. Three groups of five greyhounds received 1.5 micrograms.kg-1 of epinephrine 1:200,000 in lidocaine 0.5 per cent, bupivacaine 0.5 per cent or 0.9 per cent saline. Plasma epinephrine, lidocaine, bupivacaine, lactate, glucose and potassium concentrations were measured at 1, 2, 5, 10, 15 and 30 minutes following infiltration. Plasma epinephrine concentrations were significantly higher in the lidocaine group at one and two minutes following infiltration. Plasma bupivacaine concentrations were significantly higher than plasma lidocaine concentrations throughout the study period. There were no significant differences in metabolic or biochemical indices within or between the three groups. A local vasodilatory action of lidocaine may enhance epinephrine absorption. Differences in hepatic uptake and rate of metabolism may explain the increased plasma bupivacaine measured. Lidocaine may be the local anaesthetic of choice for ano-rectal procedures, especially when large volumes of local anaesthetic are being infiltrated.

Absorption↗
PubMed1979

Rectal and oral absorption of methylprednisolone acetate.

Rectal absorption of methylprednisolone acetate and oral absorption of methylprednisolone and methylprednisolone acetate were investigated in a single-dose 3-way crossover study of 12 normal male volunteers. The median value of bioavailability (relative to oral dose) of methylprednisolone acetate based on unchanged methylprednisolone plasma levels was 14.2% after rectal administration, suggesting that the drug exerts its therapeutic effect topically rather than systemically. In contrast, the median of total radioactivity in urine (as a percentage of rectal dose) was 34.3% (range, 4.52% to 58.8%), suggesting partial bacterial metabolism in the rectum prior to absorption. Mean bioavailability (relative to oral administration of methylprednisolone acetate) of methylprednisolone after oral administration was 89.9%, indicating somewhat better systemic availability of the ester than the alcohol. The average apparent elimination rate constant for methylprednisolone after oral administration of both ester and alcohol was 0.290 hr-1, corresponding to a half-life of 2.39 hr.

Absorption↗
PubMed1991

The relationship of salicylate lipophilicity to rectal insulin absorption enhancement and relative lymphatic uptake.

The sodium salts of the 3,5-dichloro, 3,5-dibromo-, 3,5-diiodo-, and 5-methoxy- analogs of salicylic acid have been evaluated as enhancers of rectal insulin absorption. A relationship was found between adjuvant potency and relative lipophilicity. Maximal adjuvant activity was obtained with 0.1 M 3,5-dichlorosalicylate. Higher concentrations (0.15 M) of 3,5-diiodosalicylate produced a decline in adjuvant activity, which may be associated with extraction of specific cellular proteins. This may indicate the existence of an optimal salicylate lipophilicity for adjuvant efficacy. Relative adjuvant activity was found to be related to the lymph:plasma absorption ratio of [125I]insulin. Lymphatic uptake of insulin was not related to lymph flow rate.

Animals↗
PubMed1997

Absorption of oligodeoxynucleotide by suppository from rat rectal route.

Rectal absorption of 32-mer phosphorothioate deoxynucleotides (S-Oligo) in the rat was attempted with the aid of a suppository containing oleic acid and a surfactant. Although, the suppository without adjuvant did not show detectable blood levels, that containing over 10% oleic acid enabled the absorption of S-Oligo with tmax at 2 h postdosing.

Administration, Rectal↗
PubMed1980

Availability of oxyphenbutazone from different suppository formulations.

The in vitro release of oxyphenbutazone as well as its rectal absorption in rabbits from different suppository formulations were investigated. It was proved that polyethylene glycol base gave higher medicament release than adeps solidus base. Incorporation of nonionic surfactants in Witepsol H 15 increased or decreased oxyphenbutazone release while incorporation of hydrophilic aerosil caused a reduction in the released amount of the medicament. A mixture of Witepsol H 15 or H 12 and Brij 58 (85:5) gave the highest in vitro release and the highest rectal absorption of the medicament. A correlation was found to exist between the in vitro release of oxyphenbutazone and its rectal absorption in rabbits.

Animals↗
PubMed1995

Regional rectal perfusion: a new in vivo approach to study rectal drug absorption in man.

BACKGROUND: In vivo permeability measurements of drugs in the colonic/rectal region in humans are difficult. A new instrument for the perfusion of a defined and closed segment in the colon/rectum was developed. The objective of this study was to evaluate its use for studying drug absorption mechanisms in the human rectum and to investigate the effect of transmucosal water absorption on drug permeability. Six healthy subjects participated at 2 separate occasions by using a modified system for segmental rectal perfusion. The system consisted of a multichannel tube with inflatable balloons and was endoscopically introduced into the rectum. The technique was considered acceptable by the following criteria; (a) high and reproducible recovery of PEG 4000, (b) stable residence time of the solution within the test segment, (c) flux of electrolytes that agrees with previous reports, (d) mass-balance absorption of antipyrine across the rectal barrier, (e) and good acceptability to the subjects. The permeability of antipyrine in the rectal region was increased by inducing net water absorption. D-glucose was not absorbed during any study periods. The present technique is valuable for studying drug absorption from the human rectum.

Antipyrine↗
PubMed1997

The enhancing mechanism of capric acid (C10) from a suppository on rectal drug absorption through a paracellular pathway.

Capric acid (C10) enhanced the absorption of cefoxitin sodium in a concentration-dependent manner following the rectal administration as a suppository in rats. The optimal concentration of C10 was 13%. C10 administered as a suppository also reduced rectal membrane resistance (Rm), showing that the above enhancing effect was induced by widening the paracellular pathway. Both the enhancing effect on the absorption and the reducing effect on Rm were inhibited by W7, an inhibitor of myosin light chain kinase. These results supported that, as shown in the in vitro Caco-2 cell system, the C10 effect on the paracellular pathway is due to activating the contraction of Ca(2+)-calmodulin-dependent actin filament.

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine↗
PubMed1981

Absorption of levodopa after rectal administration.

Absorption of levodopa was studied after administration by mouth and rectum. Given by mouth, levodopa benefited all 12 patients studied, and levodopa blood levels rose significantly (p less than 0.01). When it was given rectally, there was no rise in levodopa concentration in the blood and no clinical benefit. Rectally administered levodopa is therefore of no value in the management of postoperative parkinsonian patients who cannot take oral medication.

Absorption↗
PubMed1991

Enhanced rectal and nasal absorption of human epidermal growth factor by combined use of the absorption promoter and the synthetic polymer in rats.

Previously, the presence of sodium carboxymethylcellulose (CMC Na) in addition to an absorption promoter, sodium caprate (C10 Na), in the dosing solution was found to be necessary for the enhancement of the rectal absorption of human epidermal growth factor (hEGF). In the present study, other synthetic polymers and absorption promoters were examined for their ability to enhance the rectal and nasal absorption of hEGF in rats. The effect of polymers in combined use with 100 mM C10 Na on the rectal absorption of hEGF was in the following order: 1% methylcellulose 1% hydroxypropylmethylcellulose 0.1% polyacrylic acid 1% CMC Na. Other absorption promoters such as N-lauroyl-alanine (C12-A) and dihydroxy-bile salts also enhanced the rectal absorption of hEGF in combined use with CMC Na. In order to confirm the increased rectal absorption of hEGF, the disappearance of hEGF from the rectal loop was examined. When hEGF in a 1% CMC Na solution (200 ug/kg) was administered in the rectal loop, the disappearance percent of hEGF during 60 min was 13.9% of the dose, although hEGF was not detected in the plasma. The presence of promoters such as 10 mM C10 Na or 15 mM C12-A in 1% CMC Na increased the disappearance percent to about 50% in a dosing range of hEGF from 100 to 500 ug/kg. On the other hand, a markedly enhanced nasal absorption of hEGF by 100 mM C10 Na was observed even in the absence of any polymer in a dising solution. However, addition of CMC Na into the dosing solution accelerated the rate of nasal absorption of hEGF in early phase.(ABSTRACT TRUNCATED AT 250 WORDS)

Acrylic Resins↗
PubMed1989

Effectiveness and absorption of rectal hydrocortisone acetate foam in nonspecific proctocolitis.

A 3-week open trial of rectal hydrocortisone acetate foam (Colifoam, Stafford Miller, UK) was conducted in 19 patients with active, nonspecific distal proctocolitis. Complete or near complete remission was observed in nine patients (47.4%). Absorption of hydrocortisone acetate from Colifoam was evaluated in 13 patients by measuring early morning serum cortisol before treatment and 12 and 36 h after the final dose. Normal cortisol values were observed in every instance, suggesting that the steroid component of Colifoam was not significantly absorbed. Colifoam seems to be an effective remedy for distal proctocolitis. Its specific advantages include ease of retention and apparent nonabsorption of the active component.

Administration, Rectal↗