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PubMed1990

[Analgesic activity of morphine suppository in rats].

Analgesic activity of morphine administered rectally as a suppository was investigated in rats in order to ascertain analgesic activity of morphine suppository. Morphine hydrochloride given rectally as a suppository produced analgesic activity in a dose-related manner in the tail pressure and acetic acid-induced writhing tests, and its potency (ED50 = about 17 and 0.689 mg/kg, respectively) was approximately twice that of morphine hydrochloride administered orally as an aqueous solution. The analgesic action was as durable as that of oral morphine, but its onset was faster. The plasma and brain levels of morphine reached peak until 30 min after rectal administration of morphine suppository, and these time-courses approximately corresponded with that of the analgesic action. These results suggest that morphine given rectally to rats as a suppository produces analgesic action equivalent or superior to orally administered morphine after absorption from the rectum.

Analgesics↗

PubMed1987

[A cylindrical thermistor probe for experiments on suppositories in rabbits].

A cylindrical thermistor probe with a rubber disk stopper, which is beneficial for inserting a suppository into the rectum of rabbits without removal of the probe from the rectum, was developed. It is possible to measure body temperature continuously by using this probe in an experiment to assess the effects of a suppository on the body temperature of rabbits. After insertion of a suppository, leakage of the melted suppository from the rectum was not observed. No differences between this thermistor probe and an ordinary thermistor probe in the ability of the probe to detect the febrile response of rabbits injected with a bacterial pyrogen were observed. From these results, it could be concluded that this newly improved cylindrical thermistor probe is suitable for studying the effect of suppositories on the body temperature of rabbits.

Animals↗

PubMedDate not supplied

The effectiveness of rectal administration of insulin suppository on normal and diabetic subjects.

The effectiveness of insulin administration by rectal suppository was examined in normal and non-insulin-dependent nonobese diabetic subjects. A 100-U insulin suppository (mean 1.8 U/kg) given to the diabetic subjects caused four times as great a fall in plasma glucose compared with the normal subjects given the same dose (mean 1.6 U/kg). The insulin response after suppository administration demonstrated a significantly positive correlation (r = 0.83, P less than 0.01) with the plasma glucose level before administration. Diabetic subjects given a 100-U insulin suppository (mean 1.7 U/kg) 15 min after meals three times daily showed a significant (P less than 0.05) improvement in postprandial hyperglycemia accompanied by a restoration of the normal circadian profile of plasma IRI and a reduction of urinary glucose from 26 +/- 5.9 to 2.0 +/- 1.0 g/day. No untoward reactions were observed. These data strongly imply a unique characteristic of the insulin suppository in spite of low bioavailability.

Adult↗

PubMed1998

In vitro release of amoxycillin from lipophilic suppositories.

The in vitro release characteristics of amoxycillin from different lipophilic suppository bases were investigated using the USP rotating basket method. Suppositories containing 250 mg amoxycillin were prepared in theobroma oil and in the semi-synthetic bases Witepsol W35, Suppocire A32, Novata BD, and Novata 299. Both freshly prepared and 1-month-old suppositories were tested. Analysis of amoxycillin was performed using a validated high-performance liquid chromatographic (HPLC) technique. Release profiles differed significantly between bases, with the greatest amount of amoxycillin being released from both newly made and 1-month-old Novata BD bases (87.57 +/- 8.18 and 99.66 +/- 6.63%, respectively), and the lowest amount released from the newly manufactured theobroma suppositories (8.82 +/- 0.75%) and the 1-month-old Suppocire A32 suppositories (7.78 +/- 0.27%).

Amoxicillin↗

PubMed1997

A comparative clinical trial of sequential treatments of severe malaria with artesunate suppository followed by mefloquine in Thailand.

Sixty-three patients with severe falciparum malaria were randomly administered one of the two regimens of a sequential combination of artesunate suppository followed by an oral mefloquine tablet. Thirty-two patients received artesunate suppositories (200 mg/capsule) given rectally at 0, 4, 8, 12, 24, 36, 48, and 60 hr (total = 1,600 mg: Group I). Thirty-one patients received the same artesunate suppositories given rectally at 0, 12, 24, 36, 48, and 60 hr (total = 1,200 mg: Group II). Both regimens were followed by two doses of oral mefloquine, 750 mg given at 72 hr and 500 mg at 84 hr. Patient baseline characteristics were comparable in the two groups. All patients were admitted for 28 days to the Bangkok Hospital for Tropical Diseases to assess efficacy, tolerability, and delayed neuropsychiatric effects. The mean [SD] parasite clearance time was significantly shorter in Group I than Group II (47.3 [12.4] hr versus 55.3 [17.4] hr; P = 0.05) and the rate of parasite reduction was significantly faster in Group I (P = 0.05, by log-rank test). Mean [SD] fever clearance times were similar in the two Groups (71.1 [41.2] hr and 76.9 [47.9] hr, respectively). Twenty-two patients with unrousable coma on admission (median Glasgow Coma Score = 9) regained consciousness after 1-4 days. No deaths occurred. Sixty of sixty-three patients were parasitologically and clinically cured within 3-4 days of treatment. Three patients (5%) with deteriorating conditions required rescue treatment (one patient in Group I was administered intravenous artesunate, and two patients in Group II required two extra doses of suppository). No patients had major adverse drug effects. The cure rates at 28 days of follow-up in Group I were 96% (26 of 27 patients) and 89% (24 of 27 patients) in Group II. Artesunate suppository followed by mefloquine was well tolerated and effective. In severe malaria, the sequential treatment is a suitable alternative treatment to parenteral drugs. Further studies in a larger number of patients under field conditions are required.

Administration, Oral↗

PubMed1998

Comparative clinical trial of artesunate suppositories and oral artesunate in combination with mefloquine in the treatment of children with acute falciparum malaria.

A randomized pilot study to compare the safety and efficacy of artesunate suppositories (15 mg/kg/day for three days) versus oral artesunate (6 mg/kg/day for three days), both in combination with mefloquine (25 mg/kg), was conducted in 52 Thai children with uncomplicated multidrug-resistant falciparum malaria. Forty-five patients (87%) had a full 28-day follow-up in the hospital to assess efficacy and exclude reinfection. Mean [range] times to fever clearance of the two groups were similar (42 hr [15-104] versus 42 hr [6-119]). Artesunate suppositories resulted in significantly longer times to achieve 50% and 90% reductions of the initial parasite counts (17 and 26 hr versus 9 and 15 hr; P < 0.05 and P < 0.001). Time [range] to parasite clearance was longer in the artesunate suppositories group (42 hr [14-93] versus 35 hr [16-69]), but the difference was not significant. The cure rates by days 28 were not significantly different, 92% for artesunate suppository-treated patients and 100% for oral artesunate-treated patients. Both drug regimens are safe and effective. Further studies are needed to characterize the pharmacokinetic properties and the optimum regimen of artesunate suppositories for the treatment of severe malaria.

Administration, Oral↗

PubMed2000

[Evaluation of the efficacity and speed of action of sertaconazole nitrate suppository and cream combined treatment for vulvovaginal candidiasis].

OBJECTIVE: To assess efficacy and speed of action of a monodose sertaconazole vaginal suppository administered as a single treatment or combined with sertaconazole cream applied to the vulvar area. METHODS: This prospective, multicentric, randomised open study was conducted on 77 women with vulvovaginal candidiasis confirmed by mycological examination. They were either treated with one sertaconazole monodose vaginal suppository only (group O) or treated with the suppository combined with sertaconazole cream applied to the vulvar area for 7 days (group OC). The patients who were not clinically cured at D7 received a second phase of treatment. RESULTS: Clinical cure rates were higher in group OC than in group O at D7 (76% versus 68%), and D14 (100% versus 80%). The efficacy on symptoms was faster in group OC, with 78% of the patients relieved of pruritus as early as D2 versus 61% in group O, although these differences were not significant. Clinical local tolerance was very good, with 95% of patients not experiencing any local side effects. CONCLUSION: When candidiasis is both vulvar and vaginal, the combination of sertaconazole cream with a monodose sertaconazole vaginal suppository tends to improve clinical cure at D7 and D14 and to relieve more patients as early as D2 than the vaginal suppository used as a single treatment.

Administration, Intravaginal↗

PubMed2001

[Clindamycin soluble suppository-production and its efficacy in treating bacterial vaginosis].

OBJECTIVE: To make the soluble suppository of clindamycin which is an effective drug for treatment of Bacterial vaginosis and to treat patients in clinical trials. METHODS: Outpatients who had vaginal infections from Sept. 1998 to Jan. 1999 were investigated. The diagnoses of bacterial vaginosis were made according to Amsel's criteria and 80 patients were included in this study. They were divided into two groups to be treated respectively by metronidanole suppository and clindamycin suppository which were made by our hospital pharmacy. RESULTS: The cure rate of metronidanole was 87.5% and that of clindamycin 90.3%; No significant difference was noted between the two groups(P > 0.05). The new clindamycin suppository was not irritant and it was easy to dissolve in vagina. There was no discontinued treatment because of side-effect. CONCLUSION: The clindamycin suppository does not irritate the mucosa of vagina, it is an efficacious remedy for bacterial vaginosis.

Administration, Intravaginal↗

PubMed1992

Allergy to lysozyme/egg white-containing vaginal suppositories.

Seven patients who received a lysozyme, nystatin, and tetracycline containing vaginal suppository because of suspected vaginal infection, developed local or systemic allergic reactions. The coincidence of the symptoms with the repeated use of the suppository as well as skin and lymphocyte transformation tests indicated that the lysozyme in the suppository was responsible for the allergic reactions. This lysozyme preparation contained additional egg proteins, which contributed to the allergic reaction in certain patients: three patients with a previous history of egg allergy and serologic and/or skin test evidence for egg-white sensitization developed the allergic reaction after the first suppository. Four patients had urticaria or anaphylaxis after treatment for at least three days; none of these four patients developed egg allergy. Five of seven individuals had positive skin tests (prick or scratch) to ovomucoid and lysozyme, but none of the patients had lysozyme-specific IgE in the circulation. All seven patients, with or without egg allergy, showed vigorous T cell responses to purified lysozyme and partly to other egg-white proteins in the lymphocyte transformation test, which was absent in controls. Vaginal suppositories that contain lysozyme and other contaminating egg white proteins can either elicit allergic reactions in patients with a preexisting egg white allergy or induce sensitization to lysozyme and other egg white components.

Adult↗

PubMed2003

[Contraceptive efficacy of bioadhesive nonoxynol-9 Gel: comparison with nonoxynol-9 suppository].

OBJECTIVE: To compare the contraceptive efficacy of a new spermicide, bioadhesive nonoxynol (N-9) gel, with a traditional N-9 suppository. METHODS: A total of 240 child-bearing aged woman volunteers were randomly divided into two groups: 120 cases using the gel for contraception, and another 120 using the suppository. Using lifetable method and log rank test, we compared the pregnancy rates and other discontinuation rates after follow-up for 6 months in two groups. RESULTS: No abnormal findings of cervical smears were detected before and after this clinical trial in all 240 women. The follow-up rates at 6 months were 100.0% and 97.5% in the gel group and the suppository group, respectively. The 6-month gross cumulative pregnancy rates of typical use were 6.39 and 2.95 per 100 women (P > 0.05), respectively. If we eliminated the 5 pregnancy women (3 in the gel group, and 2 in the suppository one), who did not consistently use the spermisides for every intercourse, the cumulative pregnancy rates at 6 month in perfect use would be 3.71 and 2.03 (P > 0.05). And the discontinuation rates due to allergy or other side effects at 6 months in typical use were 3.45 and 4.57 (P > 0.05), respectively. All of the results observed between two groups in this study were not statistically significant. CONCLUSION: The contraceptive efficacy of bioadhesive N-9 gel is as same as that of the N-9 suppository, and its clinical use is quite safe.

Contraceptive Agents, Female↗

PubMed1990

Efficacy of indomethacin suppository in primary dysmenorrhoea.

The efficacy of indomethacin suppositories (100 mg 1-3 times a day) in the treatment of primary dysmenorrhoea was investigated in a double-blind, crossover study involving 40 patients, in comparison to placebo. The patients were treated for four menstrual periods-two periods with placebo and two periods with indomethacin suppositories. A dysmenorrhoeic score based on subjective estimations of nine symptoms was used, the symptoms including pelvic pain, backache, headache, dizziness, nausea, vomiting, diarrhoea, nervousness and incapacitation. As compared to placebo, indomethacin suppositories led to a insignificant decrease in the frequency and severity of the associated symptoms, as evaluated by subjective rating (P less than 0.05). Indomethacin suppositories were well tolerated and there was no drop-out. No side effects were reported except for a mild burning sensation in the rectal region experienced by 3 patients on indomethacin suppositories.

Administration, Rectal↗

PubMed1989

Rectal absorption enhancement of gentamicin in rabbits from hollow type suppositories by sodium salicylate or sodium caprylate.

The absorption of gentamicin (GM) from the rectum of rabbits after coadministration of GM (60 mg) and sodium salicylate (SA) or sodium caprylate (CA) as absorption-enhancing agents was investigated. Two types of hollow type suppositories were used--a conventional type (Type I) and a release-restricted type (Type II). Without SA or CA, GM was not absorbed. However, GM absorption was marked when 90 mg of solid SA or CA was added (the bioavailability of GM was 58% with SA, and 59% with CA). The enhancing effect of SA or CA (30 mg) in solid or aqueous solution form on GM absorption was evaluated using the Type I suppository. In the case of SA, the highest plasma GM level (Cmax 15.3 +/- 1.7 micrograms/ml, AUC0-4 27.3 +/- 3.9 h.micrograms/ml) was obtained following coadministration of powdered GM and SA; the plasma GM level (Cmax 1.5 +/- 0.6 micrograms/ml, AUC0-4 3.0 +/- 1.3 h.micrograms/ml) following the administration of a solution of GM and SA was significantly decreased as compared with the results using the powdered form. In the case of CA, the plasma GM level (Cmax 14.8 +/- 4.5 micrograms/ml, AUC0-4 25.4 +/- 8.7 h.micrograms/ml) following administration of the solution form was not significantly decreased in comparison with the results obtained using the powdered form. A marked increase in the enhancing effect of SA on the rectal GM absorption was found following use of Type II suppositories when GM and SA were coadministered in solution form. However, the GM absorption after coadministration of GM and CA using Type II suppositories was not significantly different from the absorption resulting from use of Type I suppositories. Our results suggest that the form and concentration of drug should not be ignored in evaluating the enhancing effects of SA or CA on the rectal absorption of poorly absorbed drugs such as GM.

Administration, Rectal↗

PubMed1989

[Effect of vaginal antibiotics suppository on retroperitoneal-space infection after hysterectomy and lymphadenectomy for uterine cancer].

Effects of vaginal antibiotics suppository on the retroperitoneal-space infection were studied in 42 patients who had hysterectomy and lymphadenectomy with diagnosis of uterine cancer stage I or II. All patients received intravenous administration of 1 g LMOX (3 times/day) for 7 days after operation. One group of patients (21 cases) received 0.5 g of ABPC vaginal suppository (twice/day) for 10 days immediately after operation. Another group of 21 patients did not received vaginal suppository. The LMOX concentrations in the exudate decreased rapidly from the 3rd day to the 7th day. The frequencies of bacterial appearance in the retroperitoneal-space in the vaginal suppository group were 33% on 5th day, 33% on 7th day and 20% on 9th day, while those in the control group were 100%, 100% and 76%, respectively. It was concluded that the administration of vaginal antibiotics suppository was easy to handle and effective for preventing the retroperitoneal-space infection after hysterectomy and lymphadenectomy.

Ampicillin↗

PubMed1989

[Comparative study of artemisinin suppositories and piperaquine phosphate in the treatment of falciparum malaria].

Artemisinin, developed by Chinese scientists, is a new type of anti-malarial drug with quick effect and low toxicity. Since its solubility in water or oil is very low, it cannot be made into a clear injection to be given intramuscularly or intravenously for emergency use. The artemisinin suppositories used in the study was provided by the institute of Chinese Materia Medica in 1982. Phase I and Phase II clinical trials of the drug were made by Guangzhou College of TCM. The results showed that the therapeutic effect of Artemisinin suppositories was satisfactory with no apparent side effects. The total dosage recommended was 2800-3200 mg. In 1986, fifty-six adults with falciparum malaria were treated with a total dose of 2800 mg Artemisinin suppositories for 3 days and randomly compared with a control group of Piperaquine phosphate in the Dongfang Town Hospital, Dongfang ( ) County of Hainan Island. The parasite clearance time in Artemisinin suppositories group (71.8 +/- 16.0 hrs) was significantly faster than that of Piperaquine phosphate group (100.3 +/- 20.3hrs), but recrudescence rate by 28 days (48.2%) was much higher than that of Piperaquine phosphate (17.0%). Artemisinin suppositories is simple to administrate and therefore it could be applied in endemic area of remote countryside and to the patients of incapable of oral dosing.

Adolescent↗

PubMed1985

[Prevention of postoperative anaerobic bacterial infections in abdominal surgery with metronidazole suppositories].

Metronidazole is widely used for the prevention and treatment of post-operative anaerobic infections. In this study, the prophylactic effectiveness of metronidazole suppositories was tested in patients undergoing abdominal surgery. The suppositories had previously been tested in healthy subjects for drug absorption and tolerance. Patients were divided into three treatment groups: one group received the drug intravenously, another as suppositories and the third one by both routes. Clinical effectiveness was evaluated and plasma metronidazole levels were measured. On the basis of the results obtained, we suggest that a 1 g suppository should be administered 8-hourly over the 20 hours preceding surgery, then 12-hourly if preparation of the digestive tract can be inserted between two administrations. In emergency surgery, 1 suppository must be given at least 1 hour before induction, the 12-hourly, and a 500 mg intravenous infusion at the time of induction.

Abdomen↗

PubMed1988

Effect of surfactant incorporation techniques on sulphamethoxazole suppository formulations.

In vitro release, stability as well as bioavailability of sulphamethoxazole (SMZ) suppositories were investigated using solid dispersion techniques for surfactant incorporation. Tween 20, Tween 80 and Myrj 53 were the surfactants utilized in this investigation. Suppositories were prepared by fusion method using Witepsol H15 as a base. It was found that SMZ-surfactant physical mixture showed the highest drug release from suppositories. This indicated that the technique of surfactant incorporation has a great role in enhancing the drug release from suppositories. Stability study revealed that the technique of surfactant incorporation did not affect the drug stability. Bioavailability investigation has proved surfactant incorporation in suppository formulations of SMZ in fatty bases.

Adult↗

PubMed1986

Piroxicam capsules versus suppositories: a pharmacokinetic and clinical trial.

15 patients with rheumatoid arthritis or osteoarthritis received a single dose (20 mg) piroxicam (Felden) as suppository. Serum piroxicam concentrations were assayed by fluorometry 1, 2, 4, and 8 h after the installation of the suppository, the mean values being 1.3, 1.9, 1.8, and 1.8 mg/l, respectively. Then the patients continued on oral piroxicam 20 mg daily for maximum 3 weeks, and serum piroxicam levels (mean 6.3 mg/l) were checked at the end of this period. Nine patients then continued on piroxicam suppositories 20 mg daily for one week, and serum piroxicam levels (mean 4.5 mg/l) were again assayed at the end of this maintenance. Pain at rest, pain on motion, and joint movement restriction were scored on day 1, after oral maintenance, and after rectal maintenance. Reduced scores were found with time, but the only statistically significant effect was in the overall subjective pain relief measured after oral maintenance. Rectal irritation was recorded in one patient. It is concluded that a) absorption of piroxicam from suppository was adequate, b) it was possible to maintain adequate serum piroxicam levels by repeated administration of suppository for one week, and c) the gastrointestinal toleration was acceptable in these patients selected for showing poor tolerance towards other nonsteroidal antiinflammatories.

Aged↗

PubMedDate not supplied

Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories: interlaboratory study.

A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by 8 laboratories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbance of the minima at about 389 and 412 nm. Each collaborator received 4 creams (0.2%), 1 jel (0.2%), 1 molded suppository (6 mg/3.198 g), and 2 gelatin-encapsulated suppository samples (12 mg/6.661 g and 14 mg/6.863 g). The cream samples included blind duplicates prepared to contain 0.212% aminacrine hydrochloride, 15% sulfanilamide, and 2% allantoin. Mean recovery for the authentic cream was 104.7% with a coefficient of variation (CV) of 9.22%. The commercial products contained these respective amounts (CVs): creams, 100.0% (2.48%) and 101.5% (2.16%); jel, 118.0% (9.58%); molded suppository, 102.7% (1.88%); and gelatin encapsulated suppositories, 93.1% (1.0%) and 94.3% (1.60%). Standard aminacrine hydrochloride provided for the study was 99.6% pure by nonaqueous titration. Thin layer chromatographic identification of aminacrine hydrochloride was also tested collaboratively. The method was not adopted by AOAC.

Aminacrine↗