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PubMed2001

Poloxamer 407 as a thermogelling and adhesive polymer for rectal administration of short-chain fatty acids.

OBJECTIVES: The purpose of the study was to gel a rectal solution of short-chain fatty acids to decrease the loss of active materials in the colonic lumen and thereby optimize their absorption. METHODS: Five thermogels were prepared with poloxamer 407 at concentrations ranging from 17% to 20%. Their viscosities were measured at room temperature and 37 degrees C, and their gelling temperatures were determined. The adhesive properties of each gel were assessed in vitro at 37 degrees C. Short-chain fatty acid release was studied using Guyot cells. RESULTS: From the threshold concentration of 17.5%, the solutions, Newtonian at room temperature (50-80 mPa x s), gelled at 37 degrees C. The higher the concentration, the higher the viscosity (1750 to 49,000 mPa x s), the lower the gelling temperature (27.6 degrees C to 23.4 degrees C), and the stronger the work of adhesion (2.2 to 4.5 mJ). Short-chain fatty acid release from the 18% polymer gel was decreased by 60% compared to the rectal solution. CONCLUSION: The 18% poloxamer 407 concentration provided a solution that was liquid at room temperature, that gelled at 37 degrees C, possessed adhesive properties, and controlled short-chain fatty acid release.

Absorption↗
PubMed1990

Pancreatitis after rectal administration of 5-aminosalicylic acid.

A patient treated with sulfasalazine for new-onset ulcerative colitis developed self-limited pancreatitis. Rechallenge with 5-aminosalicylic acid (5-ASA) in enema form (Rowasa) again induced pancreatitis. Recent case reports suggest that the salicylate component of sulfasalazine can lead to the development of pancreatitis with oral 5-ASA administration. This patient's course demonstrates further that rechallenge with 5-ASA in a rectal form may also lead to pancreatitis.

Administration, Rectal↗
PubMed1989

[Experience in the photochemotherapy of psoriasis with rectal administration of the photosensitizer].

The authors compare the efficacy and tolerance of rectal (in suppositories) and oral administration of puvalen in 117 patients. The therapy has been highly effective in both the groups; clinical remission has been achieved in 78% of Group 1 patients and in 80% of Group 2 ones. Rectal puvalen has been better tolerated; the incidence rate of side effects has been 4 times lower. This recommends the rectal route of puvalen administration for wide practice, particularly in patients with subclinical abnormalities of the liver and gastrointestinal system.

Administration, Oral↗
PubMed1990

Treatment of ureteric colic. Intravenous versus rectal administration of indomethacin.

A randomised multicentre clinical trial was undertaken to compare the effect on pain of indomethacin administered either intravenously or rectally to 116 patients with ureteric colic. Adverse reactions were also assessed. Of the patients receiving the intravenous injection, 48/53 (91%) achieved good pain relief (i.e. no supplementary analgesia was required) 30 min after administration, compared with 46/63 (73%) receiving the enema. Significantly more side effects occurred in the group treated intravenously. It was concluded that indomethacin administered as an enema was less effective than the intravenous form, but it should be regarded as a good alternative in the treatment of ureteric colic.

Administration, Rectal↗
PubMed1989

Biologic activity of 5'-deoxy-5-fluorouridine by rectal administration.

5'-Deoxy-5-fluorouridine (dFUR) is used orally to treat human malignancies. This study compared the antitumor activity and toxicity of rectally and orally administered dFUR. A 7-day treatment of dFUR (350 or 700 mg/kg/day) was infused rectally over 30 min or administered by oral gavage (500 mg/kg/day) to rats bearing transplanted dimethylhydrazine-induced colon tumors. The oral treatment was previously shown to produce a 82% cure of the tumor-bearing animals. The tumor weight after 7 day treatment was compared to that before treatment. The size of the tumor in the saline-treated control group (N = 6) increased by 55%. The maximum tumor size reductions by drug treatments were 40% for the 350-mg/kg rectal dose (N = 5), greater than 99% for the 700-mg/kg rectal dose (N = 10), and 100% for the 500-mg/kg oral dose (N = 4). The 350-mg/kg rectal dose did not produce any cures, while the 700-mg/kg rectal dose produced 80% cures and the 500-mg/kg oral dose 100% cures. The cured animals remained tumor-free during the observation period of 163 to 243 days. The tumor-bearing rats were euthanized between 46 and 132 days when they appeared moribund or when the tumor began to ulcerate. The 700-mg/kg rectal and 500-mg/kg oral treatments produced greater weight loss than saline suggesting a drug-induced intestinal toxicity. After rectal drug treatment, the animal weight returned to pretreatment level within 3 days, indicating a rapidly reversible intestinal toxicity. The oral group suffered a greater weight loss than the rectal group and took more than 10 days to recover.2+his suggests that the intestinal

Administration, Rectal↗
PubMed1996

Gastric mucosal injury and adaptation to oral and rectal administration of naproxen.

INTRODUCTION: Oral nonsteroidal anti-inflammatory drugs (NSAIDs) cause acute gastric mucosal injury but the relative importance of systemic and topical effect of NSAIDs to overall gastric damage remains uncertain. METHODS: Twenty-four healthy volunteers were allocated either oral or rectal naproxen 500 mg b.d. and gastroscoped before and during days 1, 7 and 28 of dosing. Macroscopic gastric damage was assessed using a modified Lanza score, mucosal blood flow recorded using laser Doppler flowmetry and prostaglandin E2 (PGE2) measured in antral mucosal biopsies. RESULTS: Maximal gastric damage occurred during the first 24 h in the oral naproxen group and was associated with a fall in antral mucosal blood flow (mean +/- S.E.M.) from 58.2 +/- 3.3 to 46.6 +/- 4.1 arbitrary units (a.u.) (P < 0.05). With continued administration of oral naproxen, gastric damage resolved and antral mucosal blood flow returned to baseline (54.2 +/- 3.7 a.u.). No macroscopic damage or significant changes in mucosal blood flow were observed during rectal administration. There was no significant difference between mucosal PGE2 concentrations in those receiving oral or rectal naproxen, falling from an initial level of 335 +/- 29 to 155 +/- 49 pg/mg at day 1 (P = 0.06) in those receiving oral naproxen and from 235 +/- 55 to 107 +/- 31 pg/mg at day 1 (P = 0.1) in those receiving rectal naproxen, and remaining suppressed throughout the study in both groups. CONCLUSIONS: These observations suggest that acute mucosal damage and changes in mucosal blood flow are caused by the topical rather than systemic actions of naproxen.

Administration, Oral↗
PubMed1988

Enhanced bioavailability of morphine after rectal administration in rats.

Plasma morphine levels and the area under the plasma concentration-time curve (AUC) after i.v. (10 mg kg-1), p.o. (100 mg kg-1) and rectal (unrestricted or restricted to 1.5 cm from the anus, 10 mg kg-1) administration of morphine hydrochloride were determined in 10 or 11-week-old male Wistar rats to compare bioavailability of morphine after the rectal dosage with that after oral administration. The AUC value after oral administration (15 micrograms min mL-1), which was normalized by the dose, was only one-tenth of that after i.v. dosing (151 micrograms min mL-1). In contrast, the AUC after rectal administration (unrestricted, 133 micrograms min mL-1; restricted, 142 micrograms min mL-1) was almost comparable with that after i.v. administration. From the comparison of these AUC values, the extent of systemic availability of morphine after rectal (unrestricted or restricted) and p.o. administration was estimated to be approximately 90 and 10%, respectively.

Administration, Oral↗
PubMed1990

[Measurement of portal systemic circulation by oral and per-rectal administration of I-123 iodoamphetamine].

In an earlier study, we measured the portal circulation noninvasively by Tc-99m pertechnetate per-rectal portal scintigraphy. This method makes it possible to see the portal circulation and to diagnose portal hypertension from the images of the liver and heart. However, the method mainly reflects circulation from the inferior mesenteric vein, the contribution of which to the portal circulation is less than that of the superior mesenteric vein. Here, we devised capsules of I-123 iodoamphetamine (IMP) that dissolve when the pH changes to evaluate the portal circulation arising from the superior mesenteric vein. I-123 IMP enclosed in an enteric-coated capsule was prepared and given orally, just before I-123 IMP was injected into the rectum. The per-rectal portal shunt index (RSI) and oral portal shunt index (OSI) were calculated from the count of radioactivity of the liver and lungs. The RSI and OSI of patients with cirrhosis were both higher than those of the patients with chronic hepatitis. In individual patients, the RSI was higher than the OSI. This noninvasive method seemed to be useful in evaluation of the portal systemic circulation in chronic liver diseases.

Administration, Oral↗
PubMed1996

Plasma concentration profiles after pre-operative rectal administration of a solution of paracetamol in children.

An exploratory study in paediatric surgical patients was performed to describe the behaviour of a rectal solution of paracetamol at 20 mg/kg. Four of six patients were able to complete the study. Peak concentration (Cmax) and time to peak concentration (tmax) found in the children are comparable to adults studied earlier. After 1.6 hrs (tmax) a peak concentration of 11.7 mg/l (Cmax) was reached. The area under the curve (AUC t = 6) and the mean residence time (MRT) were respectively 48.3 mghr/l and 5.2 hrs. The solution appears promising for further study in daily clinical practise.

Acetaminophen↗
PubMed2005

Protective effect of intra-rectal administration of rebamipide on dextran sulfate sodium-induced rat colitis.

BACKGROUND/AIM: Rebamipide, an anti-ulcer drug, has various actions including radical scavenging and mucus-stimulating as well as anti-inflammatory effects, and exhibits both mucosal protective and healing promoting actions in the stomach. In the present study, we examined the effect of rebamipide on an animal model of colitis induced by dextran sulfate sodium (DSS). METHODS: Experimental colitis was induced in rats by daily treatment with 3% DSS in drinking water for 7 days. Rebamipide (3-30 mg/kg), 5-aminosalicylic acid (5-ASA: 150 mg/kg) or metronidazole (10 and 30 mg/kg) was administered intra-rectally once daily for 6 days. The ulceration area, colon length, and mucosal myeloperoxidase (MPO) activity as well as thiobarbituric acid-reactive substance (TBARS) were measured on the 7th day after the onset of DSS treatment. The effects of rebamipide on the secretion of mucus in the colon was also examined. RESULTS: DSS treatment caused severe lesions in the colon, accompanied by an increase in MPO activity and TBARS as well as a decrease in body weight gain and colon length. Repeated administration of rebamipide dose-dependently suppressed the colon lesions and improved the pathological changes induced by DSS treatment. Rebamipide significantly increased the mucus contents in the colon. Both 5-ASA and metronidazole also reduced the severity of DSS-induced lesions. CONCLUSION: These results suggest that intra-rectal administration of rebamipide is effective against DSS-induced colitis. The protective effect of rebamipide may be attributable to both the radical scavenging action and the increase in the production of mucus in the colon, the latter presumably suppressing the process of intestinal bacterial infiltration.

Administration, Rectal↗
PubMed1997

Rectal administration of N-acetylcysteine in swine: a pilot study.

The purpose of this pilot study was to determine if N-acetylcysteine (NAC) administered via the rectal route in swine is absorbed into the systemic circulation. Fasting swine were anesthetized, intubated, monitored and i.v. access was obtained by femoral cutdown. NAC was administered into the rectal vault (2.0 g/kg) via a balloon-tipped Foley catheter inserted into the animals' rectum. NAC administered via the rectal route resulted in systemic absorption as determined by spectrophotometric methods in 5 of the 7 study animals. This study provides important information regarding the development of a potential alternative route for the administration of NAC.

Absorption↗
PubMed2001

Rectal administration of midazolam for conscious sedation of uncooperative children in need of dental treatment.

The aim of this study was to determine the effects of rectal midazolam on uncooperative children. The trial included 120 children at the age of 16 months to 10 years and six months (X = 4.5 years). The children were referred because behavioural management techniques alone had failed. On 225 treatment occasions the children received midazolam, 0.3 mg/kg body weight rectally 10 mins before treatment. The degree of sedation was assessed by the dentists after 10, 15, 20, 45 and 60 minutes. 60% of the treatments were fulfilled without difficulty. 39.6% of the treatments could be performed with some difficulty and with the help of parents preventive holding. Only one mentally handicapped patient showed non-acceptance. No side effects were noted during the treatments. After 107 treatments the parents were asked about the total time their children seemed sedated. After two hours 86 children were still considered sedated but after three hours only four of them seemed effected by the drug. Midazolam has shown in this follow-up to be an effective and safe drug for premedication of infants in the stressed dental situation. The advantage to for example diazepam lies mainly in the shorter period of time of sedation.

Administration, Rectal↗
PubMed1984

Rectal administration of sodium valproate in children.

A study of VPA based on a comparison of mean plasma levels, plasma peak latency times and plasma half-lives after rectal and oral administration was conducted in 9 children between 6 months and 10 years of age suffering from various forms of epileptic seizure, before they received chronic VPA treatment. Each child received an oral dose of 20 mg/kg and after two days a rectal dose of 20 mg/kg and the mean plasma concentrations were determined at intervals for both modes of administration. An identical plasma concentration for both after 24 h showed that the quantity of drug absorbed was the same. The mean half-life varied according to age: 11 +/- 2 h for children over 3 years of age and 9 +/- 1 h for those under 3. The results of the study, in line with the few other available published data, thus confirm the validity of rectal VPA administration.

Administration, Oral↗
PubMed1985

Enhanced bioavailability of insulin after rectal administration with enamine as adjuvant in depancreatized dogs.

Rectal absorption of insulin by depancreatized dogs was significantly enhanced by the coadministration of enamine as a suppository adjuvant and if this was followed by a further suppository containing enamine alone, the insulin absorption was even further enhanced. The additional enamine suppository resulted in high serum insulin concentrations for a longer time and effected a significant decrease in serum glucose concentrations. To decrease serum glucose concentrations effectively in depancreatized dogs, serum insulin levels had to remain high for a long period of time, rather than be transient.

Adjuvants, Pharmaceutic↗
PubMed1996

Pharmacokinetics and drug input characteristics for a diclofenac-codeine phosphate combination following oral and rectal administration.

In a single dose cross-over study with 12 healthy male volunteers the plasma concentrations of diclofenac (CAS 15307-86-5) and codeine (CAS 76-57-3) were determined after oral and rectal application of formulations containing 50 mg of each drug. For kinetic analysis of the concentration-time profiles non-compartmental as well as compartmental procedures were used. The compartment model included two disposition compartments supplemented by a dissolution and drug absorption step. For both compounds, the AUC0-infinity values of the two treatments were similar with only a slightly higher AUC for the suppositories, which was not found to be significantly different under the employed conditions (p > 0.05). Referring to the pharmacokinetic parameters Cmax and tmax typical differences between oral and rectal formulations were observed. For the suppositories, diclofenac and codeine average peak plasma concentrations were only half as high as for the tablets, whereas the respective tmax values were doubled. The results obtained show a similar extent of diclofenac and codeine bioavailability for both administration routes, but the rate of drug input was lower for the suppositories. The total mean input time (MITtot) was found to be significantly longer for the suppositories. This seems to be caused by a slow release from the dosage form or dissolution of the drugs, which is confirmed by a longer MITtot compared to the MRTsys in most of the volunteers.

Administration, Oral↗
PubMed2005

Modulation of the rheological and mucoadhesive properties of thermosensitive poloxamer-based hydrogels intended for the rectal administration of quinine.

The aim of this work was to formulate and characterize thermosensitive gels based on poloxamer 407, a thermosensitive polymer, and hydroxypropylmethylcellulose (HPMC), a bioadhesive polymer, intended for the rectal delivery of quinine in children. In order to avoid the macroscopic phase separation between the two polymers it was necessary to add propanediol-1,2. After the formulation of stable ternary systems, their rheological properties were studied as a function of temperature. It was thus possible to obtained the gelation temperature of the systems as well as their elastic modulus, G', at 37 degrees C. It appeared that HPMC in the presence of propanediol-1,2 had a synergistic effect on the gelation of poloxamer 407. Tests on the rabbit rectal mucous membrane, founded on a technique of traction of the adhesive/adhered joint, made it possible to characterize the bioadhesive properties of the gels by measuring the work of adhesion, W, and the maximum detachment force, F(max). Over small concentration ranges of poloxamer and HPMC, very important variations of the viscoelastic and mucoadhesives properties were observed. It was shown that the viscoelastic and the bioadhesive properties were tightly correlated. Indeed, an empirical equivalence relation was established between the shear frequency and the rate of deformation in traction and allowed to describe all our samples by a master curve. This master curve would make it possible to predict the values of W at various rates of traction by the simple non-destructive measurement of the elastic modulus, G', at an equivalent shear frequency.

Adhesiveness↗
PubMed1982

Ergotamine in plasma and CSF after i.m. and rectal administration to humans.

An attempt was made to study the kinetics of penetration of ergotamine across the blood-brain barrier. A single therapeutic dose of ergotamine was given to 18 hospitalized patients; eight patients received 0.5 mg i.m., three patients 4 mg rectally, and seven patients 2 mg rectally. Plasma samples were drawn between 0.25 and 72 h and one CSF sample was taken from each patient between 0.5 and 6.5 h after administration. The ergotamine concentrations were measured using a RIA method. The 0.5 mg intramuscular injection showed the highest plasma levels of ergotamine, with a mean peak concentration of 1.27 ng/ml reached at 0.5 h. The 4 mg rectal administration resulted in mean plasma ergotamine levels of 0.44 ng/ml in the time interval of 0.75-2 h. The 2 mg ergotamine rectally resulted in mean plasma levels of 0.15-0.17 ng/ml 1-8 h after administration of ergotamine. Neither the plasma samples taken after 10 h nor the CSF samples had ergotamine concentrations above the detection limit of the RIA method (0.1 ng ergotamine/ml).

Blood-Brain Barrier↗