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PubMed1990

[Morphine hydrochloride suppositories. II. Bioavailability of morphine hydrochloride suppositories in dogs].

Bioavailabilities of morphine after rectal administration of three different morphine.HCl suppositories were evaluated in dogs, whose rectum was lavaged or non-lavaged. The suppositories were prepared with three fatty bases (Witepsol H-15, Witepsol W-35, Suppocire AT) by the fusion method. The release of morphine from the suppositories was examined after stored for two weeks at 30 degrees C. The plasma concentrations of morphine and its metabolites, morphine-3-glucuronide and morphine-6-glucuronide, were determined by high-performance liquid chromatography. The bioavailabilities of morphine after rectal administration were compared with those after intravenous and oral administration of morphine++.HCl solution. In the case of rectal lavaged dogs, the plasma levels of morphine after rectal administration of morphine.HCl solution were higher than those after oral administration of morphine.HCl solution. The release of morphine from Witepsol H-15 suppository was more rapid than those from other suppositories. Morphine after rectal administration of Witepsol H-15 suppository was rapidly absorbed in the rectum, and the inter-animal variation of its plasma levels was smaller than those of other suppositories. In rectal non-lavaged dogs, the bioavailabilities of morphine after rectal administration of morphine.HCl solution and suppositories decreased more than those of rectal lavaged dogs. Although the bioavailability of morphine after rectal administration of morphine.HCl was decreased by the influence of contents in the rectum, morphine from Witepsol H-15 suppository was more rapidly absorbed in the rectum, and the inter-animal variation of its plasma levels was smaller. These results indicate that, among their suppositories, Witepsol H-15 suppository is available for the terminal care of malignant disease.

Administration, Oral↗

PubMed1990

[Morphine hydrochloride suppositories. I. Bioavailability of morphine hydrochloride suppositories in rats].

Bioavailabilities of morphine after rectal administration of three different morphine-HCl suppositories (5 mg/kg) were evaluated in rats. The suppositories were prepared with three fatty bases (Witepsol H-15, Witepsol W-35, Suppocire AT) by the fusion method. The plasma and brain concentrations of morphine and its metabolites, morphine-3-glucuronide and morphine-6-glucuronide, were determined by high-performance liquid chromatography. The bioavailabilities of morphine after rectal administration were compared with those after intravenous and oral administration of morphine.HCl solution (5 mg/kg). The plasma levels of morphine after rectal administration of morphine.HCl solution were higher than those after oral administration, whereas the plasma levels of metabolite, morphine-3-glucuronide was lower than those after oral administration. Morphine after rectal administration of Witepsol H-15 suppository released more easily than other suppositories. The inter-animal variation in the plasma levels of morphine after rectal administration of Witepsol H-15 suppository was smaller than those of other suppositories. Results obtained in this study indicate that morphine.HCl suppository prepared with Witepsol H-15 is a promising material as preparation of suppositories.

Animals↗

PubMedDate not supplied

Is one paracetamol suppository of 1000 mg bioequivalent with two suppositories of 500 mg.

A common belief is that one tablet or suppository containing, e.g. 100 mg of a drug can be substituted, without any changes in the therapeutic effect, with two units of the same brand containing 50 mg of the drug. In the present study a single dose of paracetamol was administered to healthy volunteers as (a) two tablets of 500 mg, (b) two suppositories of 500 mg, and (c) one suppository of 1000 mg. There were statistically significant differences in all bioavailability parameters (t(max), C(max) and AUC) between the three treatments. The relative bioavailability of the 500 mg suppositories was 77% and that of the 1000 mg suppositories 66%. The absorption rate from suppositories was markedly lower than from the tablets. Especially low absorption rate was obtained with the suppository of 1000 mg. The two strengths, although having the same trade name, were not therefore bioequivalent.

Acetaminophen↗

PubMed2000

Comparative, open, randomized trial of the efficacy and tolerance of slow-release 5-ASA suppositories once daily versus conventional 5-ASA suppositories twice daily in the treatment of active cryptogenic proctitis: French Pentasa Study Group.

OBJECTIVE: The efficacy and tolerance of slow-release 5-ASA suppositories (Pentasa 1 g/day) were compared with those of conventional 5-ASA suppositories (Rowasa 0.5 g b.i.d.). METHODS: Two hundred and fifty-one (251) patients presenting with an exacerbation of cryptogenic proctitis were randomized. Clinical activity and rectal lesions were measured at days 1 and 14 (and at day 21 for patients not in remission at day 14), and each patient had to fill out a daily diary card (checklist). RESULTS: Results are given for slow-release and classical suppositories, respectively. The reduction in symptoms and lesions was identical in both groups. Treatment was continued until day 21 in 36% versus 33% of the patients, and minor or moderate side effects occurred in 5.6% versus 6.3% (NS). The tolerance of the suppositories was rated as satisfactory every day by 77% versus 54% (p = 0.001), and early suppository expulsion occurred in 0.5% versus 3.4% (p = 0.001). CONCLUSIONS: The treatments were equally effective and both were well tolerated. However, the advantages of the slow-release suppositories were that patients exhibited greater tolerance and early expulsion was less frequent.

Adult↗

PubMed1990

[Biopharmaceutical study of aminophenazone-containing suppositories. 1. Experimental materials and methods, determination of physical qualities of the suppositories].

Suppositories containing aminophenazone in quantities of 0.30 g/2 g were prepared by pouring technology. Two kinds of lipophilic suppository masses Witepsol W 35 and Estarinum 299 have been used as vehicles. Both of suppository bases are official in Ph. Hg. VII. As ingredients ten sorts of liquid tensides in concentrations of 5% have been applied. Experimental methods have been described: compression stability, disintegration time, special penetration time and drug release of suppositories by membrane diffusion method. Results of determinations have been discussed in the second part of the publication. On the basis of experimental results it has been established that the physical parameters of Massa Estarinum 299 had proved to be more advantageous. In 5% concentrations tensides softened consistency of suppositories favorably and shortened disintegration time beneficially in the case of both vehicles. The authors think that special penetration time is more suitable for measuring "disintegration" of suppositories of high powder content at 37 degrees C than the classical disintegration time.

Aminopyrine↗

PubMed1986

Pharmaceutical evaluation of hollow type suppositories. V. Preparation of valproic acid suppository and rectal absorption of valproic acid in rabbits.

Seven kinds of suppositories were constructed with oleaginous base materials (Witepsol H-15 (H-15) and E-85 (E-85]: a conventional type suppository containing valproic acid (VPA) mixed with E-85 (I), a conventional type suppository containing sodium salt of VPA (sodium valproate) (S-VPA) mixed with H-15 (II), hollow type suppositories containing VPA in the forms of oily liquid (free acid) (III), macrogol 1000 or 6000 mixture (IV or V), powder (S-VPA) (VI) and aqueous solution (S-VPA was dissolved in 0.9% NaCl solution) (VII) in each cavity. The content of VPA in type I was decreased considerably by volatility and type II was found to be hygroscopic. Therefore conventional type suppositories containing VPA or S-VPA were not of practical use, whereas III and VI prevented volatility of VPA and minimized the hygroscopic property of S-VPA. Plasma concentration of VPA was measured in rabbits after rectal administrations of III, IV, VI and VII. By using VI, the highest values of the mean of the peak plasma VPA concentration (Cmax) (49.8 +/- 2.6 micrograms/ml) and the mean of the area under the plasma concentration-time curve (AUC) (90.0 +/- 3.7 h X micrograms/ml) were obtained. The Cmax and the AUC estimated after administration of VII were not significantly different from those of VI. The Cmax and the AUC were lower with III than with IV, VI or VII but the extent of bioavailability (EBA) of III was about 80%.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1987

Double-blind, placebo-controlled evaluation of 5-ASA suppositories in active distal proctitis and measurement of extent of spread using 99mTc-labeled 5-ASA suppositories.

Patients with active distal proctitis received either 5-aminosalicylic (5-ASA) acid or identical placebo suppositories, 500 mg t.i.d. for 6 weeks. Activity at 3 and 6 wks was assessed using a Disease Activity Index (DAI), derived from four categories: number of daily evacuations more than usual, evacuations containing blood, sigmoidoscopy appearance, and physician's overall assessment. Each category was graded 0-3. There was thus 0-12 points scored ranging from complete remission to severe disease. A minimum score of 3 from two categories was necessary for study entry. Of 27 patients randomized, 14 received active medication and 13 placebo. Of the 14 patients, with initial mean DAI 7.1 +/- 1.8, 11 were in complete remission at 6 wks (78.6%). Whereas, there was no significant change in the placebo group, with initial mean DAI 7.1 +/- 1.8. An additional 6 patients with inflammatory bowel disease and 6 healthy volunteers were given 99mTc-labelled 5-aminosalicylic acid suppositories. The extent of spread was limited to the rectum, and the suppositories were retained for 3 hours. There was no absorbed radioactivity. 5-ASA suppositories are safe, well-tolerated, and effective treatment for active distal proctitis.

Administration, Rectal↗

PubMedDate not supplied

Ondansetron suppository: a randomised, double-blind, double-dummy, parallel-group comparison with oral ondansetron for the prevention of cyclophosphamide-induced emesis and nausea. The Ondansetron Suppository emesis study group.

This multinational, multicentre, randomised, parallel-group study compared the safety, tolerability and efficacy of ondansetron 8 mg orally twice a day with ondansetron suppository 16 mg once daily in patients receiving cyclophosphamide-containing chemotherapy. A total of 406 patients were randomised to receive ondansetron 8 mg p.o. (198 patients) or ondansetron suppository (208 patients) medication in a double-blind, double-dummy trial. The primary efficacy analysis revealed that ondansetron provided good anti-emetic control with 81% of patients in the 8 mg p.o. b.d. group and 73% of patients in the 16 mg ondansetron suppository o.d. group experiencing complete or major control of emesis (< or = 2 emetic episodes) on the worst day of days 1-3. The 90% confidence interval for the difference between the two treatments for complete or major control (1.4, 15.0%) showed that the treatments could be regarded as equivalent. A difference in favour of oral ondansetron treatment was noted for the complete control (0 emetic episodes) rates over days 1-3, but no differences were found on day 1. There were no significant differences in the distribution of nausea grades between the treatment groups on the worst day of days 1-3 or on day 1. The incidence of adverse events was similar for the two treatment groups, the most frequently reported events were headache and constipation. There were no significant laboratory findings in either treatment group. In conclusion this study showed that the ondansetron treatments could be regarded as equivalent for the primary efficacy endpoint and that ondansetron suppository was well tolerated and effective in the prevention of cyclophosphamide-induced emesis.

Administration, Oral↗

PubMed1977

Pentazocine suppositories for post-operative pain: intramuscular pentazocine injections versus suppositories in a controlled trial in 588 patients.

A between-patient comparison of the analgesic effect of pentazocine 50 mg by suppository and 30--45 mg by intramuscular injection was made in 558 postoperative patients, 54% within 24 hours of operation. The suppositories proved acceptable overall, even though effectiveness was less at half an hour after administration (particularly in those patients with severe initial pain) and there was greater need for further analgesia at one hour. The cost of treatment with suppositories is less than with injections. After the suppositories there were half as many patients asleep at one hour than after injections, and fewer possible side-effects (7 compared to 24).

Adolescent↗

PubMed2001

Treatment of nonspecific chronic prostatitis with Qian Lie Xian Yan Suppository suppository in 104 cases.

Qian Lie Xian Yan Suppository ([symbol: see text]) was rectally applied to treat 104 patients with nonspecific chronic prostatitis (damp-heat syndrome with blood stasis) in contrast to 30 patients treated with traditional Chinese drug Ye Ju Hua Shuan ([symbol: see text] Suppository of Flos Chrysanthemi Indici). The results show that chronic prostatitis is markedly improved by using Qian Lie Xian Yan suppository, with a short-term cure rate of 23.1% and a total effective rate of 84.6%, superior to that of the control group. The animal experiment indicates that Qian Lie Xian Yan suppository has better anti-inflammatory and analgesic effects, with an action of promoting blood circulation.

Administration, Rectal↗

PubMed1991

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 1. Choice of the optimal vehicle and determination of the physical parameters of the suppositories].

Suppositories containing 0.10 g papaverine hydrochloride were made with moulding technology to produce spasmolytic effect. The optimal vehicle was tried to be found for these suppositories. During the experiments 12 different suppository masses were used, including lipophil and lipohydrophil vehicles as well as vehicles with low and high hydroxyl numbers. Five different kinds of physical parameters were determined: melting and drop points, disintegration and special penetration times and breaking hardness. The physical parameters of suppositories without active substance and containing papaverine were examined separately. After 6 months of storage the greater part of the masses showed unfavourable changes (after-hardening, increase of the disintegration time, etc.). In the end the Estaram 299 mass, a triglyceride type of mass with a low hydroxyl number was found satisfactory in every respect, either in itself or combined with 5% Estasan neutral oil.

Chemical Phenomena↗

PubMed1997

[Efficacy of rectal diazepam suppository in the prophylaxis of febrile seizures: comparison with rectal chloral hydrate suppository].

We evaluated the efficacy of diazepam and chloral hydrate given rectally for the prophylaxis of recurrence of febrile seizure. The dose were 0.4 mg/kg for diazepam and 250 mg (for children younger than 3 years old) or 500 mg (for over 3 years old) for chloral hydrate. Another dose was given after an interval of 8 hours if body temperature continued to exceed 38.0 degrees C. Among the 452 patients with febrile seizures who visited our hospital from Jan. 1993 to Jun. 1995, 113 were studied who had at least one febrile episode in the follow-up period that extended over 6 months. These patients were divided into two groups: Group D (72 patients given diazepam) and Group C (41 patients given chloral hydrate). In group D and C, the numbers of febrile episodes were 238 and 167, and those of recurrent seizures 8 (3.8%) and 29 (20.4%), respectively. The recurrences rate was significantly higher in the latter group (p < 0.005). There was no statistical difference as to the mean dosage of diazepam or chloral hydrate between the patients with and without recurrence. The numbers of patients with seizure recurrence were 8 (11.1%) in group D and 12 (29.3%) in group C, being significantly larger in the latter (p < 0.005). Diazepam produced more adverse effects than chloral hydrate did. Thus diazepam suppositories for the prevention of recurrence of febrile seizures were more effective than chloral hydrate suppositories.

Child↗

PubMed1984

Pulsed proton NMR and solid-liquid fat ratio determinations in suppository vehicles and aminophylline suppositories.

The physical state, melting behaviour and release rate of aminophylline suppositories were studied during storage. The fraction of non-crystallized fat, assessed by pulse NMR, varies between different vehicles. At room temperature several vehicles do not seem to be completely crystalline. Aging, as observed in prolonged melting time and a reduced release rate, is not expressed in a drastic reduction of the fraction of non-crystallized fat, as observed by NMR. On the contrary the mobility of the protons in the non-crystallized state is likely to offer a more promising tool to monitor aging.

Aminophylline↗

PubMed1987

Biopharmaceutical characteristics of a suppository base containing poly (oxyethylene)-poly (oxypropylene) copolymer, Unilube. I. Effects of a suppository base containing Unilube 70DP-950B on release and rectal absorption of aminopyrine in rabbit.

The rectal absorption of aminopyrine (AP) from a three-component-system suppository base (TCS), which is a mixture of oleaginous base, water-soluble base and the poly-(oxyethylene) poly-(oxypropylene) block copolymer, Unilube, was investigated. Albino rabbits were used as the animal model. The bioavailability of oleaginous base and water-soluble base (polyethylene glycol 4000) were 44.3% and 82.6%, respectively. The time to reach maximum plasma concentration (Tmax) of the oleaginous and the water-soluble bases were 21.0 +/- 8.2 min and 33.0 +/- 16.4 min, respectively. When TCS was used, its Tmax was 30 min and increasing the amount of Unilube in the base from 5% (w/w) to 20% (w/w) decreased the bioavailability from 100.4% to 47.2%. The softening temperature of TCS was 55-57 degrees C. Collectively, TCS containing 5% of Unilube gave significantly higher bioavailability than the other bases without softening until 57 degrees C. Also, the results of the two different release tests were compared with the results of an animal experiment in this paper.

Animals↗

PubMed1989

Double-blind study of tenoxicam suppositories versus piroxicam suppositories in acute non-articular rheumatism.

The effectiveness and tolerability of tenoxicam and piroxicam, administered as a once-daily 20 mg suppository, were assessed in a comparative, randomised, double-blind trial in 48 subjects suffering from acute non-articular rheumatism. Both spontaneous and induced pain improved significantly with each of the treatments. There was no significant difference between the two treatments, whatever criterion of effectiveness was considered, i.e. spontaneous pain, induced pain or overall judgement. The incidence of undesirable side-effects was comparable for both treatments. Thirteen per cent of patients in the tenoxicam group and 16% of the patients in the piroxicam group experienced at least one undesirable side-effect. The majority of reported side-effects were of a digestive nature; however none of these were serious. The risk/benefit ratio of tenoxicam was found to be identical to that of piroxicam in the treatment of acute non-articular rheumatism.

Acute Disease↗

PubMed1985

[Clinical study of ceftizoxime suppositories in acute suppurative otitis media in children and tissue concentration of ceftizoxime in the palatine tonsil after administration of ceftizoxime suppositories].

The newly developed ceftizoxime rectal suppository (CZX-S) contains 125 mg or 250 mg ceftizoxime (CZX) in potency. From the laboratory and clinical studies on CZX-S, the following results were obtained. Concentration of CZX in serum and palatine tonsil when 250 mg of CZX-S was rectally administered reached the peak level rapidly. The serum levels were 9.39 micrograms/ml in 30 minutes, 6.00 micrograms/ml in 45 minutes, 4.55 micrograms/ml in 60 minutes, 3.87 micrograms/ml in 90 minutes and 2.65 micrograms/ml in 120 minutes. The palatine tonsil levels were 2.73 micrograms/g in 30 minutes, 1.83 micrograms/g in 45 minutes, 1.54 micrograms/g in 60 minutes, 0.99 micrograms/g in 90 minutes and 0.74 micrograms/g in 120 minutes. About 30% of serum concentrations were distributed into palatine tonsil. CZX-S was administered at a daily dose of 375 mg or 750 mg divided 3 times for 4 approximately 9 days in 19 cases of acute suppurative otitis media of children. The overall clinical effect was excellent in 7 cases, good in 7 cases, fair in 2 cases and poor in 3 cases. The effectiveness rate was 73.7%. No side effects were observed in any cases.

Bacteria↗

PubMed1980

[The dynamics of drug release from suppositories. Part 6: The effects of lipophil and hydrophilic suppository bases on the release of adeiphenin (author's transl)].

On studying the release of adiphenin from suppositories, the authors found that it is most rapid from hydrophilic bases. The release rate decreased in the following order: PEG 1500 leads to PEG 2000 leads to PEG 4000 (70%) + Glycerol (30%) leads to PEG 1000 (70%) + Peg 4000 (30%) leads to PEG 4000 leads to PEG 6000. The release is considerably slower from the bases Witepsol W35, Witepsol H15 and cacao butter.

Chemical Phenomena↗

PubMed1981

[The dynamics of the drug release from suppositories. Part 5: Liberation of chlorpromazine from suppository bases (author's transl)].

The authors determined the liberation of chlorpromazine hydrochloride from suppositories prepared with the polyethylene glycols PEG 1000, 1500, 2000, 4000, 6000 and their mixtures as well as with the lipophil bases cocoa butter, Witepsol W35 and Witepsol H15. The determinations were made with the apparatus described by Kerckhoffs and Huinziga using a phosphate buffer (pH = 7.4). It was found that the liberation was most rapid from hydrophilic polyethylene glycol bases; and the release rates decreased in the following order: PGE 4000 (75%) + PEG (25%) leads to PEG 4000 (75%) + glycerol (25%) leads to PEG 2000 leads to PEG 1500 (70%( + PEG 6000 (30%) leads to PEG 4000 leads to PEG 6000. The release from lipophil bases was poor.

Chlorpromazine↗