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PubMed2005

Pharmacokinetics of theophylline after administration of suppositories formulation.

Asthma is a public health problem for developed countries. It attacks all age groups but often starts in childhood. Theophylline ethanoate of piperazine in a suppository form is one of the treatments of asthmatic children. The pharmacokinetics of theophylline were evaluated in 24 healthy male subjects after administration of theophylline ethanoate of piperazine suppositories (PR) (Minophylline 500 mg. Alexandria Co.) and single injection intravenous (IV) of theophylline ethanoate of piperazine (Minophylline ampoules 500 mg Alexandria Co.). The theophylline serum levels were determined by an ELISA method. Peak theophylline plasma concentration, Cmax, (mean +/- S.D) was 21.5 +/- 2.10 microg/mL & 14 +/- 0.90 microg/mL; AUC(0-t), values were 80.9 and 67. 4 microg x ml x hr for the reference IV preparation and suppositories, respectively. The median peak time, Tmax, was 0.5 hr for theophylline rectal administration. The above mentioned results demonstrate the possibilities of using theophylline (Minophylline Suppositories--500 mg Alexandria Co.) in asthmatic children in rural and desert areas away from health care personnel.

Administration, Rectal↗
PubMed2000

Sustained release of diclofenac from polymer-containing suppository and the mechanism involved.

Sustained release of diclofenac sodium (DcNa) from suppositories composed of triglycerides and polymer was investigated by dissolution testing through an artificial membrane. DcNa was slowly released from a suppository containing carboxyvinyl polymer (CVP), and the extent of the release decreased with the amount of CVP added. Little effect was noted with the addition of other water-soluble polymers, such as hydroxyethylcellulose (HEC), xanthan gum, and polyvinylalcohol (PVA). When sodium benzoate was used instead of DcNa, a similar result was obtained with the addition of CVP. The result of release rate analysis together with the viscosity and pH in these cases showed that the reduction of solubility and diffusion due to sodium exchange between DcNa and CVP played an important role in the sustained release from the suppository. Also, in comparison with the results when CVP was not used, the plasma concentration profile of diclofenac after the administration of CVP suppository displayed a twofold longer half-life time.

Animals↗
PubMed1999

Relative hypoglycemia of rectal insulin suppositories containing deoxycholic acid, sodium taurocholate, polycarbophil, and their combinations in diabetic rabbits.

In this study, insulin suppositories containing 50 U insulin incorporated with 50 mg of deoxycholic acid, sodium taurocholate, or both were placed in the rectum of alloxan-induced hyperglycemic rabbits. A large decrease in plasma glucose concentrations was observed, and the relative hypoglycemias were calculated to be 38.0%, 34.9%, and 44.4%, respectively, compared with insulin subcutaneous (s.c.) injection (40 U). Insulin suppositories containing 50 mg polycarbophil alone or mixed with 50 mg deoxycholic acid produced relative hypoglycemia of 43.1% and 42.2%, respectively. The most pronounced effect was observed with the addition of polycarbophil to the suppository formulation containing a combination of deoxycholic acid and sodium taurocholate, which produced a 56% relative hypoglycemia compared with subcutaneous injection. These suppository formulations could be very promising alternatives to the current insulin injections, being roughly half as efficacious as subcutaneous injection.

Acrylic Resins↗
PubMed2002

Rectal administration of propylthiouracil in hyperthyroid patients: comparison of suspension enema and suppository form.

Previous studies have described the therapeutic effects of propylthiouracil (PTU) and methimazole in normal subjects after rectal suppositories. The goal of our study was to compare the pharmacokinetic and pharmacologic effects of a suppository and suspension form of PTU given per rectum. Fifteen newly diagnosed hyperthyroid patients of both genders (ages 21 to 55 years) were randomly given the drug as follows: group 1 (n = 7), a single enema (400 mg of PTU in 90 mL of sterile water) and group 2 (n = 8), two suppositories of polyethylene glycol base (200 mg of PTU in each). The pharmacokinetic study revealed earlier time to peak levels (T(max)) and significantly greater maximal peak levels (C(max)) in group 1 than in group 2, (85.71 +/- 12.12 minutes vs. 172.5 +/- 26.24 minutes for T(max) and 3.89 +/- 0.34 vs. 2.01 +/- 0.38 microg/mL, p < 0.05 for C(max), respectively). However, the area under the curve (635.16 +/- 105.71 vs. 377.87 +/- 68.09 microg x min/mL) was not statistically different between both groups. Both forms induced a significant decrease in serum free triiodothyronine (FT(3)) levels and an increase in serum rT(3) levels shortly after administration. Four subjects reported a bitter taste 5-10 minutes after receiving the drug. PTU can be effectively absorbed via the rectal route. The enema form appeared to provide better bioavailability than the suppository form. However, both preparations exhibited comparable therapeutic effect.

Administration, Rectal↗
PubMed2005

Analgesic efficacy of caudal block versus diclofenac suppository and local anesthetic infiltration following pediatric laparoscopy.

AIM: To compare the analgesic efficacy of caudal block with diclofenac suppository and local anesthetic infiltration in children undergoing laparoscopy. METHODS: We studied 50 children undergoing laparoscopy for diagnostic and therapeutic purposes. Their ages ranged from 3 to 13 years, and all belonged to American Society of Anesthesiologists (ASA) class I or II. Anesthesia was carried out using the standard procedure. Patients were randomly assigned to one of two groups. Group 1 received caudal block with bupivacaine 1 mL/kg after anesthetic induction. Group 2 received diclofenac suppository 3 mg/kg postinduction and local anesthetic infiltration at the port sites at the end of the procedure. Pain was assessed using the Hannallah objective pain scale at 15, 30, 60, 120, and 360 minutes postextubation. RESULTS: The pain scores were comparable in both groups at all times. Twelve percent of caudal block patients and 20% of diclofenac patients needed rescue analgesic, a statistically insignificant difference. In 2 patients, caudal block was technically difficult and they were excluded from the study. The incidence of side effects was low in our study. CONCLUSION: We find the analgesic efficacy of diclofenac suppository combined with local anesthetic infiltration at port sites comparable to caudal block. Given the necessarily invasive nature of caudal block, we suggest the combined use of diclofenac suppository with local anesthetic infiltration at port sites as a useful and more economical alternative for analgesia following pediatric laparoscopy.

Adolescent↗
PubMed1999

Analgesic effect of salmon calcitonin suppositories in patients with acute pain due to recent osteoporotic vertebral crush fractures: a prospective double-blind, randomized, placebo-controlled clinical study.

OBJECTIVE: To evaluate the analgesic efficacy of calcitonin suppositories (200 IU) in comparison with bed rest and paracetamol tablets, as a rescue analgesic. DESIGN: A prospective, double-blind, randomized, placebo-controlled, clinical trial. PATIENTS: Forty patients (8 men and 32 postmenopausal women), who had recently (within the last 5 days) suffered a nontraumatic osteoporotic vertebral fracture. SETTING AND INTERVENTIONS: All patients were admitted to the hospital, divided randomly into two groups and received either one calcitonin or placebo suppository once a day, respectively, for 28 days. All patients were allowed to take paracetamol tablets (500 mg), with a maximum dose of six tablets daily. OUTCOME MEASURES: Spinal pain evaluation was performed at the beginning of the study (before the initiation of treatment) and then daily until the end of the study (day 28) using the Huskinsson's visual analog scale (VAS) and a painmeter device, by direct pressure on the fractured vertebra. Pain was evaluated with the patients attempting or performing four different locomotor functions, e.g., bed rest, sitting, standing, and walking functions. Biochemical urine and plasma measurements were carried out before the initiation of treatment and on days 14 and 28. RESULTS: All calcitonin-treated patients experienced an overall statistically significant (all p values < 0.001) decrease of spinal pain as assessed by the VAS and the painmeter device. Pain relief allowed for early mobilization and the gradual restoration of the locomotive functions in the calcitonin-treated group. Placebo-treated patients remained in bed for almost the whole of the observation period. At the end of the study (28th day), fasting osteocalcin, hydroxyproline/creatinine, and calcium/creatinine ratio values were statistically significantly (all p values < 0.001), lower in the calcitonin-treated than in the placebo-treated patients. In the placebo group these values showed a gradual increase. In the calcitonin-treated group side effects mainly included dizziness and enteric irritation caused by the suppositories. Enteric irritation was also present in the placebo-treated group. CONCLUSIONS: Salmon calcitonin suppositories (200 IU daily) caused a dramatic decrease in spinal pain in patients with recent osteoporotic vertebral fractures and influenced the early mobilization and the gradual restoration of their locomotor functions.

Acute Disease↗
PubMedDate not supplied

Bioavailability of metronidazole in rabbits after administration of a rectal suppository.

The bioavailability of metronidazole in rabbits was studied using plasma concentration measurements after the administration of the drug in a hydrophilic (glycerogelatin) suppository form. The peak in the plasma concentration time curve occurred about 1 hour after administration, indicating that the rate of absorption is fast and equivalent to that observed in humans after oral administration. There was rapid elimination of the drug, as indicated by a relatively high elimination rate constant and low plasma half-life. The in vitro dissolution profile of the suppositories further confirms rapid absorption of the drug from the suppositories in the rectum. The presence of Tween 80 enhanced the in vitro release of metronidazole, but the presence of a hydrogenated vegetable oil lubricant (Lubritab) caused retardation in the drug release from the suppositories.

Administration, Rectal↗
PubMed2005

Efficacy and safety of mesalamine 1 g HS versus 500 mg BID suppositories in mild to moderate ulcerative proctitis: a multicenter randomized study.

BACKGROUND: Ulcerative proctitis (UP) usually presents as fresh rectal bleeding. Successful treatment using topical mesalamine 5-aminosalicyclic acid (5-ASA) 500 mg BID suppository led to developing a once-a-day formulation that could contribute to better acceptability and ease of use by patients. The objective of this randomized trial, conducted in 18 centers, was to compare efficacy of 2 modes of treatment with 5-ASA suppositories. METHODS: Ninety-nine patients with mild or moderate UP limited to 15 cm of the anal margin, evidenced by a disease activity index (DAI) between 4 and 11, were randomized to 5-ASA 500 mg suppository (Canasa; Axcan Pharma) BID or 1 g at bedtime (HS) for 6 weeks. The study used a noninferiority hypothesis based on the mean difference in DAI values after 6 weeks of treatment on an intent-to-treat basis using analysis of covariance. DAI was derived from a composite of the measures of stool frequency, rectal bleeding, mucosal visualization at endoscopy, and general well being. RESULTS: There was no difference between groups at baseline for demographic and clinical parameters. Mean DAIs fell from 6.6 +/- 1.5 (SD) to 1.6 +/- 2.3 in the 500 mg BID group (n = 48) and from 6.1 +/- 1.5 to 1.3 +/- 2.2 in the 1 g HS group (n = 39). There was no significant difference (P = 0.74) in mean DAI at week 6 between the 2 groups. Both groups showed a significant reduction (P < 0.0001) in DAI over the course of the 6 weeks. Both formulations showed effectiveness in reducing each individual component of the DAI. There was no significant difference between treatments in adverse events, and both groups had an overall drug compliance of greater than 95%. CONCLUSION: This study showed that 1 g HS and 500 mg BID mesalamine suppository treatments of UP patients were equivalent in all facets of efficacy, safety, and compliance in a 6-week trial.

Adult↗
PubMed1990

A pharmacokinetic study of high-dose metoclopramide suppositories.

The pharmacokinetics of high-dose rectal metoclopramide have been studied in nine patients after administration of 150-mg suppositories. The results have been compared to the pharmacokinetics of the drug in five patients who received the same dose of metoclopramide intravenously. Administration of a metoclopramide suppository achieved plasma drug concentrations that are associated with the effective treatment of cytotoxic drug-induced nausea and vomiting. In three patients who received the drug by both routes the systemic availability of the suppository appeared to be complete. High-dose metoclopramide suppositories are convenient and may be advantageous in the treatment of medical oncology out-patients.

Administration, Rectal↗
PubMed1984

Comparison of paracetamol and pentazocine suppositories for pain relief after tonsillectomy in adults.

The pain-relieving effect of paracetamol 500 mg or pentazocine 50 mg suppositories was studied in 91 voluntary adult patients after tonsillectomy in halothane or enflurane anaesthesia. Both suppositories were studied after both anaesthetics. Thus the patients were randomly allocated to four study groups. At 60 min after administration of coded suppositories, 46-50% of the patients in various groups needed extra analgesic and received pethidine 1 mg/kg i.m. Thereafter, the pain relief was satisfactory in all groups until the end of the observation period (120 min). The incidence of vomiting, the most common side effect, ranged from 5 to 14% in the groups. Bleeding from the operation site was most common (14%) in the patients treated with pentazocine after enflurane anaesthesia and did not occur in the patients treated with pentazocine after halothane anaesthesia. The incidence of bleeding in both paracetamol groups was 9%. In all cases, bleeding stopped without any special treatment. The results suggest that both paracetamol 500 mg and pentazocine 50 mg suppositories in the doses used were weak analgesics for throat pain after tonsillectomy in adults in the early postoperative period. The incidence of side effects was relatively low.

Acetaminophen↗
PubMed1986

Prostaglandin synthetase inhibition with indomethacin rectal suppositories in the treatment of acute and chronic urinary calculus obstruction.

The effect of indomethacin suppositories on both acute urinary colic and urinary calculus, resistant or refractory to conventional therapy with analgesics and spasmolytics was investigated. Fifty-five patients with acute urinary colic refractory to treatment with repeated injections of antispasmodics and analgesics had dramatic or complete pain relief after receiving indomethacin suppositories (100 mg) (P less than 0.01). Fifteen of the 55 patients passed urinary stones within 30 days of treatment with indomethacin. Three out of 30 other patients with renal or ureteric stones were treated with indomethacin suppositories (100 mg) twice daily. Twenty-one of the 30 patients passed their stones within 30 days of treatment. It is concluded that indomethacin suppositories can relieve acute urinary colic resistant to treatment with analgesic/antispasmodic drugs, and facilitate expulsion of urinary calculi. The mechanism of action of indomethacin is discussed in terms of its analgesic and anti-inflammatory effects and its prostaglandin synthesis inhibition.

Adolescent↗
PubMed1995

High dose loperamide suppositories: a novel approach for improving clinical function after restorative proctocolectomy.

The effect of loperamide suppositories on patients following restorative proctocolectomy was studied by means of a randomized, double-blind, crossover trial comparing active suppositories (20 mg b.d. x 1 week) with placebo. Ten patients (8 male, 2 female; 7 J pouch, 3 W pouch; 8 ulcerative colitis, 2 familial adenomatous polyposis) were studied 3-60 months (median, 31.5) after ileostomy closure. Ages ranged from 24 to 63 years (medium, 41.5). All patients kept a diary of their bowel habits and eight underwent a standardized test of pouch compliance. Urgency volume (UV) and maximum tolerable volumes (MTV) and the volume at onset of large isolated pouch contractions (LIC) were recorded. Statistical analysis was by the Wilcoxon test for paired data. Mean daily stool frequency during the placebo phase ranged from 3.7 to 7.8. It was reduced during the active phase in only seven patients (P > 0.1) but was reduced in all six patients whose placebo phase stool frequency was five or more. Urgency volume was increased by use of active suppositories in six of the eight patients tested (P > 0.01). There was no consistent effect on MTV. Large isolated pouch contractions were not seen in either test in one patient. In all of the remaining seven patients LIC were recorded after the placebo phase. After the active phase LIC first appeared at higher volumes in three but were not seen at all in four patients. High dose loperamide suppositories suppress pouch contractions and tend to lower stool frequency especially when high initially. They represent a novel therapeutic approach to high stool frequency in pouch patients.

Adult↗
PubMed2004

Rectal analgesia for the relief of perineal pain after childbirth: a randomised controlled trial of diclofenac suppositories.

OBJECTIVE: To evaluate rectal diclofenac in the relief of perineal pain after trauma during childbirth. DESIGN: A randomised, double-blind trial. SETTING: Delivery Suite, Women's and Children's Hospital, South Australia. POPULATION: Women with a second-degree (or greater) perineal tear or episiotomy. METHODS: Women were randomly allocated to either diclofenac or placebo suppositories (Anusol), using a computer-generated randomisation schedule with stratification for parity and mode of birth. Treatment packs contained two x 100 mg diclofenac or two placebo suppositories, the first being inserted when suturing was complete, and the second 12-24 hours after birth. Women were asked to complete questionnaires at 24 and 48 hours after birth relating to their degree of perineal pain using the validated Short Form McGill Pain Questionnaire. MAIN OUTCOME MEASURES: Pain scores at 24 and 48 hours after birth. RESULTS: A total of 133 women were recruited, with 67 randomised to diclofenac suppositories and 66 to placebo. Women in the diclofenac group were significantly less likely to experience pain at 24 hours while walking (RR 0.8; 95% CI 0.6 to 1.0), sitting (RR 0.8; 95% CI 0.6 to 1.0), passing urine (RR 0.6; 95% CI 0.4 to 1.0) and on opening their bowels (RR 0.6; 95% CI 0.2 to 0.9) compared with those women who received placebo. These differences were not sustained 48 hours after birth. CONCLUSIONS: The use of rectal non-steroidal anti-inflammatory drug suppositories is a simple, effective and safe method of reducing the pain experienced by women following perineal trauma within the first 24 hours after childbirth.

Administration, Rectal↗
PubMed2000

A prospective randomized placebo-controlled double-blinded pilot study of misoprostol rectal suppositories in the prevention of acute and chronic radiation proctitis symptoms in prostate cancer patients.

OBJECTIVE: Radiation proctitis is a known complication of radiation therapy for prostate cancer. Available medical treatment is usually ineffective and has focused on relieving symptoms after damage has occurred. Our study aimed at evaluating the use of misoprostol rectal suppositories in the prevention of acute as well as chronic radiation proctitis symptoms. METHODS: A prospective, randomized, placebo-controlled, double-blinded trial was conducted in patients with recently diagnosed stages B and C prostate cancer who underwent external beam irradiation. Patients received either a misoprostol or a placebo suppository 1 h before each radiation session. Misoprostol suppositories were made from two 200-microg tablets (Cytotec, Searle Pharmaceuticals, Skokie, IL), whereas the placebo was made from cocoa butter. A 12-point radiation proctitis symptom score was obtained from each patient at 4, 8, 12, and 36 wk after radiation therapy. RESULTS: A total of 16 patients were enrolled. Seven patients received placebo, and nine patients received misoprostol. Mean radiation proctitis symptom scores in the placebo group were 4.86, 5.86, 5.71, and 3.83 at 4, 8, 12, and 36 wk, respectively. The mean scores in the misoprostol group were 0.78, 0.67, 0.33, and 0.37 at 4, 8, 12, and 36 wk, respectively. The difference between the two groups was statistically significant (p < 0.05) at 4, 8, 12, and 36 wk. CONCLUSION: Misoprostol rectal suppositories significantly reduce acute and chronic radiation proctitis symptoms in patients receiving radiation therapy for prostate cancer.

Acute Disease↗
PubMed1981

Pharmacokinetics of diazepam administered rectally in geriatric patients: comparison of suppositories with rectal tubes in a cross-over study.

The pharmacokinetics of diazepam administered as suppositories or as a solution in rectal tubes were compared in six geriatric hospital patients. A single dose of 10 mg was administered in a cross-over study with a one week interval. There was no statistically significant difference in the bioavailability, the mean maximum serum concentration or the time of achievement of the maximum with these preparations. However, the peak serum concentration was somewhat higher with suppositories but the absorption was somewhat faster via rectal tubes. The serum N-desmethyldiazepam concentration increased during the whole 24 hour observation period, there was no difference between the preparations. Our results are in good agreement with most studies of the pharmacokinetics of diazepam. The basal substance of the suppository is of the utmost importance to the absorption of diazepam. The rectal tube for administration of diazepam did not have any advantage over the optimally formulated (a mixture of macrogols) suppository in geriatric patients. In fact, the use of rectal tubes is more expensive, the tube may not be completely emptied, and the solution may not be completely retained in the rectum.

Aged↗
PubMed1980

Pharmacokinetics of metronidazole in healthy adult volunteers after tablets and suppositories.

A cross-over study on metronidazole was carried out with 10 healthy adult volunteers who received tablets (250, 500 and 1,000 mg) and suppositories (500, 1,000 and 2,000 mg). The bioavailability of the suppositories was approximately 90% of the corresponding tablet dose as judged by area under the serum curves and amounts excreted in urine. The absorption was faster after the tablets. The mean curve peaks of unchanged metronidazole after the tablets occurred within 1 h and were 3.7 microgram/ml after 250 mg, 9.8 microgram/ml after 500 mg, and 11.8 microgram/ml after 1,000 mg. The suppositories rendered peaks of 5.5, 9,5 and 14.0 microgram/ml 4 h after doses of 500, 1,000 and 2,000 mg, respectively. In the dosage range 250-1,000 mg, the relationship between the dose and the total area under serum curves was similar for tablets and suppositories. Parts of the drug in serum and urine were antibacterially active metabolites. The mean recovery in urine within 36 h was 7-14% of the dose. The serum half-life of unchanged metronidazole (chemical assay) was 8.8-10.5 h. The terminal phase half-life of the total biologically active compound (microbiological assay) was 7.8-15.1 h.

Adolescent↗
PubMed1994

Pharmacokinetics of RK-28 (a new radiosensitizer) and pharmaceutical design of a suppository form using rats.

The pharmacokinetics of RK-28, a new hypoxic cell radiosensitizer, was studied in rats following its intravenous, intraportal, oral, and rectal administration. The pharmaceutical design of an RK-28 suppository form was also examined. After intravenous injection, RK-28 was rapidly removed from the plasma (biological half-life of 17 min) and its area under the curve (AUC) was proportional to the amount of RK-28 administered. The absolute bioavailability of RK-28 was 59.7% for intraportal administration and 36.9% for oral administration. Following oral administration of RK-28, it seems likely that specific acid-catalyzed decomposition of RK-28 takes place in the stomach and then the absorbed RK-28 undergoes first-pass metabolism in the liver. When "solidified RK-28 suppository," made by solidifying molten RK-28, was inserted into the rectum, hepatic first-pass metabolism could be avoided substantially. The resulting absolute bioavailability of RK-28 increased to 75%. Furthermore, "RK-28 emulsion suppository," prepared by emulsifying RK-28 with 1-hexadecanol and hydrogenated castor oil (HCO 60) at 80 degrees C, showed a plasma concentration-time curve very suitable for radiation therapy; the maximum plasma concentration was attained 30 min after rectal administration and then decreased within a short period. Administration of "RK-28 emulsion suppository," resulted in an absolute bioavailability of 76%.

Administration, Oral↗
PubMed1995

Pharmaceutical evaluation of carbamazepine suppositories in rats.

The absorption of carbamazepine (CBZ) after rectal administration in the form of a suppository was studied in rats. CBZ suppositories were prepared with Witepsol H-15 (H-15), Witepsol S-55 (S-55) or polyethylene glycol 6000 (PEG) bases by moulding procedure. An in vitro investigation was undertaken using a dissolution apparatus. The in vitro dissolution rate of CBZ showed marked differences among the bases in the order PEG > H-15 > S-55. An in vivo study demonstrated marked differences in the time required to reach peak plasma concentration (Tmax) of CBZ after rectal and oral administration: the absorption of CBZ from PEG base was the most prolonged among these bases (in the order PEG > H-15 > S-55 > ORAL). Comparison of the area under the plasma concentration-time curve (AUC) of CBZ after rectal administration of the three different suppositories with those after intravenous and oral administration showed no significant differences in the AUC among the five preparations. These results suggest the possibility that CBZ suppositories can replace oral treatment for epilepsy.

Animals↗