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PubMed1990

Role of rectal formulations: suppositories.

Mesalazine (5-aminosalicylic acid) suppositories are safe, effective, well tolerated, and well retained in patients with active distal proctitis. The best results are seen in patients with idiopathic ulcerative proctitis. Approximately 85% of these patients are healed within 4 weeks and virtually 100% by 10 weeks, with mucosal healing and complete loss of symptoms. Suppositories cover the last 20 cm of the rectum, as shown by technetium labelling. Maintenance therapy using suppositories alone--in doses varying from 500 mg every second bedtime to 1000 mg per day in divided doses--is at least as effective as oral sulphasalazine. Mesalazine suppositories are also useful in treating patients with Crohn's disease affecting the rectum, although the response rate is slower and healing is incomplete in half the patients treated. In the rare solitary rectal ulcer syndrome, mesalazine suppositories may be as efficacious as mesalazine enemas. Patient compliance and dramatic response even when conventional therapy has failed make an excellent case for mesalazine suppositories being the treatment of choice for distal ulcerative proctocolitis.

Administration, Rectal↗
PubMed2001

Preformulation experiences and in vitro model studies with spironolactone-containing suppositories.

The optimal suppository base for the formulation of rectal suppositories containing diuretic spironolactone was selected experimentally. Model studies were carried out about the effect of solubility-increasing additives on the release of the drug from the suppositories. During the in vitro examinations acceptor phases of different pH values were used, and both diffusion time and the number of samplings were changed. Among the lipophilic and hydrophilic suppository bases studied the hydrophilic Macrogolum 1540 was found to be optimal. The release and diffusion of spironolactone was the most favourable from these suppositories. During storage these suppositories remained stable and the values of release did not decrease significantly (p < 0.05).

Algorithms↗
PubMedDate not supplied

Development and evaluation of matrix and two layered sustained release suppositories of theophylline.

Theophylline loaded conventional suppositories, sustained release matrix suppositories and sustained release two layered suppositories were prepared using polyethylene glycol 4000 and eudragit RS-100 and their characteristics were evaluated both in-vitro and in-vivo. In comparison to conventional suppositories, the release of the drug from sustained release matrix suppositories was gradual and extended over a period of time. On the other hand two layered suppositories produced an initial quick release followed by extended release of the drug. The in-vivo results were found to correlate with the in-vitro results.

Animals↗
PubMed1992

Cervical ripening: a randomized study comparing prostaglandin E2 gel to prostaglandin E2 suppositories.

Prostaglandin (PG) E2 has proven effective in many studies as a pre-induction agent for cervical ripening. The purpose of this study was to compare the efficacy of a 5-mg dose of PGE2 prepared gel with that of a quartered PGE2 20-mg suppository. Previous studies have documented uniform distribution of PGE2 in the suppository. After 90 patients entered the study, there appeared to be an unacceptable rate of hyperstimulation following the induction dose using the suppository. The study was discontinued, and data analysis revealed a 24% hyperstimulation rate with the quartered suppository versus 0% with the gel. The successful vaginal delivery rates were equivalent, at 75% for the gel and 66% for the suppository. The 5-mg quartered suppository appeared to initiate an unacceptable amount of uterine activity, much greater than with the 5-mg gel dose.

Administration, Intravaginal↗
PubMedDate not supplied

[Tocolysis with fenoterol suppositories--a comparison with oral administration of fenoterol tablets].

A new application form of fenoterol (Partusisten) as 15 mg suppositories from Boehringer Ingelheim was tested for its tocolytic effect, tolerance and the main side effects under usual clinical conditions in a prospective study in 50 pregnant patients with premature labour in 24-36th week of gestation. During one week's treatment 25 pregnant women received 3 to 4 15 mg fenoterol suppositories and 25 patients 6 to 8 5 mg fenoterol tablets. Beginning on the second day of treatment until the end of therapy in both groups a reduction of the uterine activity of at least 50 percent was achieved. The uterine relaxant effect was sufficient until 3 to 4 hours after the application of fenoterol tablets and 6 to 8 hours after the application of fenoterol suppositories. Side effects were mainly limited to cardiovascular complaints, restlessness and tremor, and we found no significant difference between tablets and suppositories. The maternal heart rate reached its highest level on the second day of treatment. Fenoterol suppositories can be recommended in all cases, where an oral tocolytic therapy is not possible e.g. in cases of vomiting or before operations. Here the application of fenoterol suppositories can replace in some cases the intravenous infusion of fenoterol.

Administration, Oral↗
PubMed1987

[Comparative, controlled study on an ampicillin suppository (KS-R 1) with an oral form of ampicillin in urinary tract infections].

Subjects were in-patients with bacterial urinary tract infections, ranging in age 4 months to 11 years 4 months. As a rule, daily dose was either four 125 mg (in potency) suppositories or four 125 mg (in potency) oral form given at 6-hour intervals over a period of 5 days. The number of children subjected to this study was 105. These children were divided into 2 groups (suppository 54; oral form 51) with matched pretreatment background factors. Therapeutic effectiveness rates were 70.4% for the suppository and 66.7% for the oral form, and no significant difference was observed between the 2 groups. Rates of efficacy by severity, presence or absence of underlying and/or complication diseases, daily dose and causative microorganisms did not differ significantly between the 2 groups. There was no significant difference in time-courses of improvement of clinical signs and symptoms between the 2 groups. Eradication rates for causative microorganisms were 65.9% for the suppository and 62.5% for the oral form. Most frequently isolated causative microorganisms were Escherichia coli and Proteus mirabilis. No significant differences were recognized in the therapeutic effect and usefulness evaluated by physicians in charge. The frequency of side effects did not differ significantly between the suppository group (6 with diarrhea and 1 with anal pain: 12.1%) and the oral form group (5 with diarrhea, 1 with displeasure and 1 with vomiting: 12.7%). Abnormal laboratory findings appeared in 6 cases (2 with eosinophilia, 2 with increased GOT and 2 with increased GPT) in the suppository group and 7 cases (2 with eosinophilia, 2 with thrombocytosis, 2 with increased GOT and 1 with increased GPT) in the oral form group.

Administration, Oral↗
PubMed1984

[Prevention of postoperative anaerobic infections. Economic significance of metronidazole suppositories].

Metronidazole is widely used in the preventive and curative treatment of post-operative anaerobic infections. As the intravenous form is very expensive, a 1 g suppository has been developed. The pharmacokinetics of metronidazole injection and suppository was studied comparatively in 10 healthy subjects. The serum bioavailability of the rectal form was 80% with a peak serum concentration of 10 mg/l four hours after dosing. From calculated pharmacokinetic values it may be suggested that: (1) in cases of elective surgery treatment could begin with the rectal form alone at the rate of one suppository 12-hourly, starting 48 hours before surgery; (2) in emergency surgery, 0,5g of metronidazole i.v. over 20 minutes and a 1 g suppository should be administered at the time of premedication, treatment being continued with one suppository 12-hourly; (3) in patients at high risk of anaerobic infection, one suppository should be given 8-hourly, starting 24 hours before surgery. The main advantage of the rectal treatment is that it is much cheaper than the intravenous treatment administered during the same period.

Adult↗
PubMed1982

[Clinical studies on 5-fluorouracil suppository for rectal cancer].

Suppository of 5-Fluorouracil (5-FU) was administered preoperatively to 19 patients with rectal cancer. In the bioassay of 5-FU concentration in the rectal specimens, 5-FU was detected in the wall distant more than 20 cm from the anal ring, in the lymph nodes and in the blood of superior rectal vein. Ten of 19 cases were treated with suppository and 5-FU solution by intravenous injection at the same time, and the other 9 cases with suppository only. In the former group, 6 cases improved remarkably, and 3 cases in the latter group. Remarkable anticancer effect of 5-FU suppository was found in 9 of total 19 cases. Accordingly, it was suggested that the combination use of than suppository alone suppository and the systemic administration of 5-FU was more effective in cancer chemotherapy.

Adult↗
PubMedDate not supplied

Relative bioavailability of ondansetron 8-mg oral tablets versus two extemporaneous 16-mg suppositories: formulation and gender differences.

STUDY OBJECTIVE: To compare the relative bioavailability of two 16-mg extemporaneously prepared suppository formulations with that of an 8-mg commercially available oral tablet. DESIGN: Prospective, crossover bioavailability study. SETTING: Inpatient clinical research center. SUBJECTS: Sixteen young, nonsmoking, healthy volunteers. INTERVENTIONS: Blood samples were obtained 24 and 48 hours after administration of an 8-mg oral ondansetron tablet and 16-mg suppository, respectively. Two 16-mg suppository formulations were compounded using commercially available Fattibase and Polybase. MEASUREMENTS AND MAIN RESULTS: Ondansetron was well absorbed by both routes of administration. The following pharmacokinetic parameters (mean+/-SEM) were obtained for the 8-mg tablet, 16-mg Fattibase suppository, and 16-mg Polybase suppository, respectively: area under the curve (AUC) in men 154.2+/-21.77, 253.4+/-72.3, 304.8+/-62.2 ng x hr/ml; AUC in women 353.6+/-32.7, 561.6+/-103.6, and 768.7+/-117.9 ng x hr/ml; maximum concentration (Cmax) in men 45.5+/-7.0, 40.6+/-10.4, and 51.2+/-6.7 ng/ml; Cmax in women 51.4+/-.8, 47.1+/-3.9, and 82.9+/-6.6 ng/ml. Times to Cmax (Tmax; mean+/-SEM) for men were 1.5+/-0.3, 4.4+/-0.5, and 2.9+/-0.3 hours; Tmax for women were 1.8+/-0.3, 4.1+/-0.4, and 4.4+/-0.6 hours for the three formulations, respectively. Women had a consistently higher AUC for all three formulations than men (p<0.05). CONCLUSION: With the exception of the 16-mg Polybase formulation in women, the two suppositories closely approximated the pharmacokinetics of the 8-mg oral tablet. These results suggest that gender may be a significant factor in ondansetron's disposition.

Administration, Oral↗
PubMed2003

Efficacy of a glycyrrhizin suppository for the treatment of chronic hepatitis C: a pilot study.

Intravenous administration of glycyrrhizin has potential efficacy on decreasing serum aminotransferase levels in patients with chronic hepatitis. However, patients receiving this treatment are recommended to attend hospital regularly for several years. To improve the quality of life for these patients, we developed a glycyrrhizin suppository. In this pilot study, we examined the most effective and safe material contents of the suppository and revealed clinical efficacy for patients with biopsy-proven chronic hepatitis C comparing intravenous administration of glycyrrhizin. As content combinations of the suppository, a mixture of 300 mg of glycyrrhizinic ammonium salt and 60 &mgr;g of sodium capric acid, with pH neutralization, was confirmed to be most effective and safe condition, based on analysis of serum glycyrrhizin levels and the grade of rectal irritations in tested patients. The efficacy on decreasing serum alanine aminotransferase levels for 12-week administration of the suppository in 13 patients with chronic hepatitis C was similar to that in another 13 patients intravenously administered glycyrrhizin. Moreover, no serious side effects were observed. In conclusion, the usage of the newly developed suppository of glycyrrhizin can improve the quality of life for chronic hepatitis C patients, especially those who do not respond with viral clearance to interferon therapy. Using this suppository, larger and longer-term studies are needed.

Journal Article↗
PubMed1982

Abortifacient effect and uterine cervix-dilating action of 16, 16-dimethyl trans delta 2 PGE1 methyl ester (ONO 802) in the form of a vaginal suppository (a randomized, double-blind, controlled study in the second trimester of pregnancy).

A newly synthesized 16, 16-dimethyl trans delta 2 PGE1 methyl ester (ONO 802) was clinically applied in the form of a vaginal suppository for therapeutic abortion of second trimester pregnancies. Its effects were studied in a double-blind test comparing it with an inactive placebo suppository. The study was conducted at 12 Japanese university hospitals. The number of patients was 125 in total, i.e. 63 receiving ONO 802 vaginal suppository (containing 1.0 mg ONO 802) and 62 receiving inactive placebo suppository. ONO 802 was more effective than placebo with a success rate of 87% (complete (71%) and incomplete (16%) abortions). The onset of uterine contractions was observed in 154.3+/-18.1 min. and the onset of uterine bleeding in 323.6+/-41.0 min. The expulsion of the fetus and placenta was observed in 955.4+/-97.0 and 961.6+/-97.0 min., respectively. The cervix dilating effect of ONO 802 was observed in 63.5% of the patients at 3 hours after the start of administration. Nausea, vomiting, abdominal cramps, diarrhea and pyrexia were noticed. However, all these side effects were transient and mild, requiring no treatment. No abnormality was observed in the puerperal course, duration of uterine bleeding or onset of subsequent menstruation following the therapeutic abortion. Therefore, the present study demonstrated that ONO 802 vaginal suppository was an effective and valuable drug for therapeutic abortion of second trimester pregnancies.

Abortifacient Agents↗
PubMed1980

The use of 16-16 dimethyl trans delta 2 PGE1 methyl ester (ONO 802) vaginal suppositories for the termination of early pregnancy. A comparative study.

Vaginal suppositories containing the 16-16 dimethyl trans delta 2 PGE1 methyl ester (ONO 802) were used for the induction of abortion in early pregnancy, and this non-surgical technique was compared with suction termination performed under local anaesthesia or general anaesthesia. Ninety patients were recruited to the study and divided equally between the three groups. Complete abortion was induced in 87 per cent of the patients treated with ONO 802 suppositories, which compared favourably with 87 and 100 per cent for the patients who had suction terminations under local anaesthesia and general anaesthesia respectively. The vaginal suppositories induced uterine bleeding in all patients and the mean time of onset of lower abdominal pain was 2 hours 55 minutes. The average numbers of episodes of vomiting and diarrhoea for patients given ONO 802 suppositories were 0.9 and 0.7 respectively. Menstrual blood loss was measured objectively in all groups and no significant differences between the three methods could be found. In selected cases, ONO 802 vaginal suppositories would seem to be safe and reasonably effective for the termination of early pregnancy.

16,16-Dimethylprostaglandin E2↗
PubMedDate not supplied

Pharmacokinetics and bioavailability of theophylline following enema and suppository administration in man.

The pharmacokinetics and bioavailability of theophylline from a commercial oral elixir of theophylline, a rectal suppository of aminophylline, and a rectal enema of theophylline monoethanolamine was compared in six normal subjects. Using a complete crossover design, the fasted subjects received a single dose of each dosage form. Blood and saliva samples were collected at frequent time intervals for 24 h, and the plasma assayed for theophylline by a specific thin-layer chromatography densitometric method. No statistically significant differences existed among the three dosage forms with respect to Cmax and AUC corrected for the elimination rate constant and the dose (mg kg-1). However, tmax was significantly larger for the suppository. While the rate of absorption was significantly slower for the suppository, no differences in the extent of absorption existed among the three dosage forms. A one-compartment open model with apparent first-order absorption adequately described the plasma concentration-time data for the elixir and enema, whereas the suppository data were best fitted by a one-compartment open model with apparent zero-order absorption and a lag time. A rate-limiting, concentration-independent release of drug from the base most likely accounts for the slow absorption of theophylline from the suppository. While the saliva:plasma ratio remained fairly constant for most of the study period, the large variability found during the absorption phase following drug administration limits the usefulness of this parameter as a monitor of theophylline plasma concentrations.

Adult↗
PubMed1987

Bioequivalence and pharmacokinetic profile of promethazine hydrochloride suppositories in humans.

A bioequivalence study of promethazine hydrochloride (10-[2-(dimethylamino)propyl]-phenothiazine monohydrochloride) was conducted in 20 male human subjects with the purpose of comparing, under blind condition, the human serum levels of promethazine in three different formulations. The formulations tested were a 50-mg promethazine hydrochloride polyethylene glycol suppository, a 50-mg promethazine hydrochloride cocoa butter-white wax suppository, and a 50-mg oral dose of promethazine hydrochloride syrup. Each subject received single doses of each of the three formulations on each of three different days on a crossover basis. From the measured serum levels, estimates of the bioavailability parameters (area under the serum concentration versus time curve, time-to-peak serum concentration, and peak serum concentration) were obtained by least-squares digital computer fitting. Also, a one-compartment pharmacokinetic open model with two consecutive first-order input steps is proposed. Statistical analysis of the results was performed by using a linear multiple regression approach for the analysis of variance. No significant differences between the syrup and the polyethylene glycol suppositories were obtained (p greater than 0.05) for the above three bioavailability parameters. However, the polyethylene glycol suppositories provided statistically higher peak serum concentration, shorter time-to-peak serum concentration, and larger area under the serum concentration versus time curve than the cocoa butter-white wax suppositories.

Adult↗
PubMed1995

Pharmacokinetics and clinical efficacy of rectal apomorphine in patients with Parkinson's disease: a study of five different suppositories.

The pharmacokinetics and clinical effects of apomorphine after rectal administration were determined in five patients with idiopathic Parkinson's disease (PD). Three different pharmaceutical formulations were tested: a rectal solution of apomorphine (10 or 15 mg), a gelatin suppository (25 and 50 mg), and a Witepsol-H15 suppository (50 and 100 mg). The pharmacokinetics of apomorphine were determined by measuring plasma concentrations using a sensitive and specific high-performance liquid chromatography method. The mean bioavailability varied between 14.7% and 40.2%, which was the bioavailability until the end of clinical benefit. Also, despite the differences in dose, the values of the Cmax were similar, with average values of 12.7-25.6 ng/ml. Wide differences in Tmax were observed, with values varying between 16 min for the enema and 127.5 min for the Witepsol-H15 100-mg suppository. The time course of the clinical effect was determined by assessing the time needed for walking a 25-m course and by calculating a tremor and dyskinesia score. Onset of effect was similar for each of the preparations, with an average onset time of 14-28 min. Significant differences with respect to the duration of the effect were observed. The duration of effect after administration of the Witepsol-H15 100-mg suppository was 156 +/- 43 min versus 50 +/- 13 min after rectal administration of the apomorphine solution. These results show that rectal administration of apomorphine may present an alternative to subcutaneous administration. The sustained-release properties of the Witepsol-H15 suppositories are especially of interest in the treatment of on-off fluctuations in PD.

Aged↗
PubMed1988

The efficiency of prostaglandin E2 vaginal suppositories versus intracervical prostaglandin gel for induction of labor in patients with unfavorable inducibility prospects.

Two different applications of prostaglandin E2 for induction of labor were randomly used in 113 women with an unripe cervix; 57 women were given prostaglandin suppositories each containing 2.5 mg PGE2 in a basis of Witepsol S55 (Dynamit Nobel), another 56 women were treated with intracervical gel containing 1 mg PGE2 in 5 g hydroxypropylmethyl cellulose. The treatment was repeated after 4 h if the cervix was still unripe, and the procedure was repeated the following day if the cervix was still unfavorable. Cesarean sections was performed within 48 h after the start of induction and before the second stage of labor in 8 women in the suppository group and 7 women in the intracervical gel group. Of the remaining 98 women, 73% (34/48 women) in the suppository group and 36% (18/50 women) in the cervical gel group had delivered within 24 h (p less than 0.01). After 48 h, 88% (42/48 women) in the suppository group and 74% of the women (37/50 women) in the cervical gel group had delivered (p greater than 0.05). The induction-delivery interval in the suppository group was half that found in the cervical gel group. There was no significant difference between the two groups in the use of instrumental vaginal deliveries and cesarean sections nor was there any difference with regard to fetal distress. The post-delivery condition of the newborn was similar in the two groups. No side-effects were reported in either of the two groups.

Administration, Intravaginal↗
PubMed2005

Diclofenac suppository administration in conjunction with lidocaine gel during transrectal ultrasound-guided prostate biopsy: prospective, randomized, placebo-controlled study.

OBJECTIVES: To evaluate the additional analgesic efficacy of the rectal administration of diclofenac suppository compared with placebo in patients undergoing transrectal ultrasound-guided prostate biopsy. METHODS: A total of 40 consecutive men undergoing biopsy were enrolled in this study. Patients were randomized equally into two treatment groups. In group 1, patients received an intrarectal 100-mg diclofenac suppository 1 hour before biopsy. In group 2, patients received a glycerin suppository as a placebo intrarectally 1 hour before biopsy. All patients received 10 mL of 2% lidocaine gel intrarectally 10 minutes before biopsy. A self-administrated visual analog scale was used to measure the pain scores at the end of the biopsy and 2 hours and 1 day after the biopsy. RESULTS: The mean patient age was 63.3 +/- 6.8 years and 61.6 +/- 6.7 years in groups 1 and 2, respectively. The mean pain score in groups 1 and 2 was 3.4 +/- 1.3 versus 5.9 +/- 1.7 (P < 0.0001), respectively, at the end of the biopsy. The mean pain score at 2 hours and 1 day after the procedure was 1.2 +/- 1.0 versus 3.6 +/- 1.4 (P < 0.0001) and 0.5 +/- 0.9 versus 1.4 +/- 1.3 (P = 0.017) in groups 1 and 2, respectively. CONCLUSIONS: Intrarectal diclofenac suppository administration is a simple, safe, and effective procedure to reduce pain and improve patients' tolerance of transrectal ultrasound-guided prostate biopsy. We recommend intrarectal diclofenac suppository administration, together with intrarectally administered lidocaine gel, in men undergoing transrectal ultrasound-guided prostate biopsy.

Analgesia↗
PubMed1995

Danazol concentrations in ovary, uterus, and serum and their effect on the hypothalamic-pituitary-ovarian axis during vaginal administration of a danazol suppository.

OBJECTIVE: To determine danazol concentrations in the ovary, uterus, and serum during daily vaginal administration of a danazol suppository and to examine its effect on the hypothalamic-pituitary-ovarian axis. DESIGN: Sampling of tissues after vaginal or oral administration of danazol and sampling of blood during control and danazol-administration menstrual cycles. SETTING: Outpatient volunteers and inpatients at a public hospital. PARTICIPANTS: Thirty patients who were to undergo hysterectomy and oophorectomy because of uterine leiomyoma and eight regularly menstruating volunteers. INTERVENTIONS: Danazol was administered as a vaginal suppository (100 mg) or orally (400 mg). MAIN OUTCOME MEASURE: Danazol concentrations in the ovary, uterus, and serum, and serum E2 and P levels. RESULTS: Danazol concentrations in the ovary and uterus after daily vaginal administration of a suppository containing 100 mg danazol were comparable to those after daily oral administration of 400 mg danazol, but the serum danazol concentration was much lower. Menstrual cycle patterns of serum E2 and P levels were normal during daily vaginal administration of a danazol suppository. CONCLUSION: Daily administration of a suppository containing 100 mg danazol produces high ovarian and uterine concentrations but low serum concentrations, and no effect was detected on the hypothalamic-pituitary-ovarian axis.

Adult↗