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PubMed1989

Studies on sustained-release suppositories. II. Evaluation of polymer electrolyte containing acidic groups for prolonged rectal absorption of bacampicillin in rabbits.

Rectal absorption of bacampicillin hydrochloride (BAPC) was found to show the best bioavailability with Witepsol H-15 as suppository base among various Witepsol bases. However, an effective plasma concentration of drug (above 0.5 micrograms/ml) was only maintained for 2 h, so sustained-release suppositories of BAPC were studied. Bacampicillin reacts with acidic polymer electrolytes such as pectic acid (Pc), chondroitin sulfate (Cd) and precipitates as its adduct with the polymer in an aqueous solution. The dissolution rate of BAPC from the adducts in a solution was slower than that of BAPC itself. The absorptions of BAPC from the suppositories containing the adducts were prolonged, but the bioavailabilities were decreased compared to that from the suppository containing BAPC alone. Similar prolonged absorption could be obtained simply by mixing Pc or Cd with BAPC in a base. Further, the absorption rate was found to be controlled by the amount of the polymer addition, and both a high plasma level and excellent bioavailability were obtained. This desirable outcome may be due to the simultaneous occurrence of rapid absorption of BAPC itself and formation of the adducts.

Ampicillin↗

PubMed1991

Cisplatin suppository: preparation, release characteristics and clinical evaluation.

Cisplatin (CDDP) has attracted attention as a chemotherapeutic agent for the treatment of uterine endometrial carcinoma but causes serious side effects, including renal toxicity. CDDP suppositories containing NaCl at different concentrations were prepared to enhance the efficacy and to reduce the side effects of CDDP. The release characteristics, melting point and viscosity of the suppositories were first studied. The rate of CDDP release increased as the NaCl concentration increased: it was 12% 12 h after administration of suppositories containing no NaCl, but 32% with 0.2% NaCl. The melting point was raised by addition of NaCl: 35.5 degrees C without NaCl and 36.5 degrees C with 0.2% NaCl. Addition of 0.2% NaCl doubled the viscosity. Clinically, the suppository containing 0.06% NaCl was given to 3 patients with endometrial carcinoma twice a week for 3 weeks to examine serum CDDP levels and endometrial absorption. Patients with endometrial carcinoma showed different peak plasma platinum (Pt) levels which were as low as 0.12, 0.06 and 0.22 micrograms Pt/ml with similar patterns of change in the level. Radiographic analysis revealed many Pt particles in sections of necrosed endometria after 21d of the treatment. No side effects of CDDP were found in biochemical testing or subjective symptoms.

Aged↗

PubMed2000

Absorption of phenytoin from rectal suppositories formulated with a polyethylene glycol base.

STUDY OBJECTIVE: To compare phenytoin pharmacokinetics following administration of an oral suspension and a rectal suppository formulated with a polyethylene glycol base. DESIGN: Unblinded, single-dose, randomized, crossover trial. SETTING: University-affiliated pharmacokinetics and biopharmaceutics laboratory. SUBJECTS: Six healthy subjects. INTERVENTION: Subjects were given a single 200-mg dose of phenytoin as an oral suspension and a rectal suppository separated by a 1-week washout. MEASUREMENTS AND MAIN RESULTS: Blood for plasma phenytoin concentrations was obtained at baseline and 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours after administration. Plasma was analyzed by high-performance liquid chromatography (coefficient of variation < 6%) for total phenytoin concentration. Phenytoin maximum concentration (Cmax), time to Cmax (Tmax), time to first measurable concentration (Tlag), and area under the curve from time zero to time of last measurable concentration (AUClast) were estimated for oral and rectal administration by WinNonlin (v 1.1) and compared using Wilcoxon's signed rank test (p<0.05 for statistical significance). Two subjects did not have detectable plasma phenytoin concentrations after rectal administration. For the other four subjects, median rectal Cmax was significantly lower than oral Cmax (0.4 vs 1.9 microg/ml, p=0.028), median rectal Tmax did not differ from oral Tmax (11.9 vs 8.0 hrs, p=0.465), and median rectal AUClast, although highly variable, was significantly lower than oral AUClast (5.4 vs 36.2 microg x hr/ml, p=0.046). No Tlag was seen after oral administration, but with rectal administration the median Tlag was 2 hours. The estimated relative bioavailability of rectal phenytoin suppositories based on AUC0-24 was 4.7%, with individual values ranging from 0-58.3%. CONCLUSION: It appears that absorption of phenytoin from polyethylene glycol rectal suppositories in healthy subjects is highly variable and unpredictable. Thus this formulation is not recommended.

Administration, Rectal↗

PubMed1987

Cervical priming and labor induction with vaginal application of 3 mg PGE2 in suppositories in term pregnant women with premature rupture of amniotic membranes and unfavorable cervix.

Sixty-one term pregnant women, 29 nulliparous (Group A) and 32 multiparous (Group B) with unfavorable cervix and premature rupture of the membranes (PROM) were given 3 mg PGE2 in suppository form for cervical ripening and labor induction. Five hours after starting the treatment, 12 women of the 29 in Group A and 21 of the 31 in Group B had a favorable cervix and established labor. The remaining 17 nulliparae and 11 multiparae still had an unfavorable cervix and were then given another PGE2 suppository. Until the next morning, i.e. within 24 h, 19 nulliparous and 22 multiparous women gave birth whereas a further 5 nulliparous women who now had favorable cervix but no uterine contractions were delivered after stimulation with intravenous oxytocin. The remaining undelivered women were given another PGE2 suppository. With or without additional oxytocin stimulation, all but 2 multiparous women could be delivered within a further 12 hours. The total number of instrumental deliveries in Group A was 2 caesarean sections due to disproportion (7%) and 5 ventouses. In Group B, 3 caesarean sections (9%) had to be carried out, one due to fetal distress and 2 due to failed induction. From the results of this study we conclude that vaginal application of 3 mg PGE2 in suppository form can be used to induce labor in patients with PROM and unripe cervix. However, when the results are compared with those obtained in previous studies after application of PGE2 in gel, the latter technique seems preferable.

Cervix Uteri↗

PubMed1991

Availability of mesalazine (5-aminosalicylic acid) from enemas and suppositories during steady-state conditions.

The local and systemic bioavailability of a mesalazine enema (Pentasa, Ferring A/S, Denmark) and a mesalazine suppository (Pentasa, Ferring) was assessed during steady-state conditions. Eleven healthy subjects took 1 g of the enema or the suppository twice daily for 1 week, with a drug-free period of at least 1 week in between. At the end of each treatment period the urine and faeces were collected for 48 h, and the concentrations of mesalazine and the metabolite acetyl-mesalazine were measured. Plasma concentrations of drug and metabolite were measured hourly during a 12-h dose interval. The faecal water concentration of mesalazine was significantly higher after suppository treatment (55.7 mmol/l) compared with enema treatment (31.7 mmol/l) (p less than 0.01). The systemic absorption was low; 15% of daily mesalazine dose was recovered in urine after enema treatment and 10% after suppositores (p less than 0.01). Plasma concentrations were low, and no accumulation of either mesalazine or acetyl-mesalazine occurred. In conclusion, the enema and the suppository can be continuously administered as 1 g of mesalazine twice daily, respectively, giving high faecal water concentrations of mesalazine and a low systemic absorption.

Administration, Rectal↗

PubMed1988

Comparison of packages for suppositories by patients with rheumatoid arthritis.

Ninety-four patients with rheumatoid arthritis were asked via a questionnaire about the convenience of packages containing tablets, capsules, or suppositories for home use. Almost half of the patients stated that they had difficulty in opening packages containing capsules or tablets, and two-thirds had difficulty with the packages used for suppositories. The characteristics of six packages used for suppositories were also compared. Patients were given the packages in random order and were asked to open them and remove a suppository. Many of them were unable to open three of the packages with their hands. The evaluation of the six packages by the patients differed widely.

Activities of Daily Living↗

PubMed1999

Analgesic effects of diclofenac suppository and injection after preoperative administration.

Diclofenac sodium (100 mg) has been introduced in the Caribbean as a suppository formulation. In a randomized single-blind (observer-blind) clinical trial, the postoperative analgesic efficacy of diclofenac administered either as a conventional intramuscular injection (75 mg) or as the available suppository formulation (100 mg) was studied in 44 adult male patients undergoing herniorrhaphy in same day surgery. Diclofenac was administered preoperatively at induction of anesthesia to patients (grades ASA I and II) after they had given informed consent. Evaluation of analgesia on the visual analog scale (VAS) did not differ significantly between the two treated groups at three assessment times: on admission to the recovery room, the postoperative ward and at discharge. The times for requests for additional analgesia and the number of patients requesting further analgesia did not differ. Patients who received the suppository were discharged earlier than those who received the injection (40 min vs. 65 min p = 0.02). This preliminary study of the two marketed formulations of diclofenac demonstrated that both preparations provided equivalent analgesia but patients who received the suppository preparation were discharged earlier.

Adult↗

PubMed2001

Effect of drug solubility on in vitro availability rate from suppositories with polyethylene glycol excipients.

Factors involved in the availability mechanism of different drugs from suppositories with polyethylene glycol (PEG) excipients were studied using an in vitro model of the rectal compartment with a porous membrane simulating the rectal barrier. Different from lipophilic excipients, the drug is released as a consequence of the progressive dissolution of PEG into the intrarectal aqueous phase. Drug concentration in this small intrarectal phase produces the gradient against the large volume of the plasmatic phase, which regulates the diffusion rate through the barrier. As with lipophilic excipients, drug solubility in water was found to be an important factor influencing suppository release rate. Nevertheless, PEG influenced in vitro drug availability considerably, by increasing both drug solubility and dissolution rate. The osmotic effect of PEG in the intrarectal compartment influenced the increase in volume of the aqueous phase. The results, compared with those obtained from suppositories with a lipophilic excipient, show a higher dissolution rate from PEG excipient, but a higher diffusion rate across the barrier did not always correspond. Drugs less soluble in water showed a greater availability from PEG suppositories. On the contrary the more soluble drugs were less available.

Area Under Curve↗

PubMed2000

Effect of drug solubility on the in vitro availability rate from suppositories with lipophilic excipients.

The factors involved in mechanisms of availability of different drugs from suppositories with lipophilic excipients were studied by using an in vitro model of the rectal compartment with a porous membrane simulating the rectal barrier. The solubility in water of drugs was found to be the fundamental factor influencing the release rate from suppositories. In fact, following the melting of the suppository at body temperature the drug particles can migrate to the interface with the small volume of rectal secretion where they dissolve. Drug molecules can so diffuse until they come into contact with the rectal barrier through which the drug is absorbed. Drug concentration in the intrarectal aqueous phase produces the gradient against the large volume of the plasma phase. This gradient regulates the diffusion rate through the barrier. A drug with a low water solubility saturates the intrarectal phase at low concentration hindering the subsequent dissolution of the drug particles remaining in the melted excipient. This fact maintains the viscosity of the melted suppository at a ligh level, which slows the migration of the particles. On the other hand, a drug with high water solubility quickly leaves the excipient, producing a high concentration in the intrarectal phase which supports a high diffusion rate across the barrier. The results obtained indicate that drugs with low solubility in water result in low availability, while drugs with good solubility can give an intense and rapid drug supply for a rapid and intense therapeutic response with the dose administered almost completely utilised.

Administration, Rectal↗

PubMedDate not supplied

Investigation of hypoglycemic properties of rectal suppositories with chlorpropamide.

Rectal suppositories with chlorpropamide and suppositories with chlorpropamide in the dispersion system with urea were prepared. Witepsol H15 and H19 and a polyoxyethyleneglycol mixture were used as bases. Rabbits were tested for blood-glucose level. The animals have been administered with prepared suppositories and commercial tablets. It was found that the suppositories prepared on the basis Witepsol H 15 with the dispersed chlorpropamide caused a much higher decrease of blood-glucose level than commercial tablets.

Administration, Rectal↗

PubMed1998

[Study on the anti-herpes simplex virus activity of a suppository or ointment form of Astragalus membranaceus combined with interferon alpha 2b in human diploid cell culture].

A study on the anti-herpes simplex virus activity of the suppository or ointment form of Astragalus membranaceus(AM) combined with recombinant human interferon alpha 2b(IFN) was carried out in human diploid cell culture. AM is a Chinese herb medicine and have been used in China as a tonic for thousands of years and the IFN was produced from E. coli with 95% purity. Obtained results indicated that the placebo suppository and ointment(without AM and IFN) seemed not to decrease markedly the anti-viral activity of IFN in WISH/VSV assay system. The anti-herpes simplex virus activities of suppository and ointment forms of AM and IFN were shown to be significantly higher than that of IFN alone. It is well known that chronic cervicitis is closely related to papillomavirus, cytomegalovirus as well as herpes virus infections. The AM-IFN suppository is suggested to be used in the treatment of cervicitis and the ointment in the treatment of skin herpes.

Antiviral Agents↗

PubMed1992

[The effect of granulocyte elastase inhibitor (urinastatin) vaginal suppository on patients with imminent premature delivery].

Cervical maturation, dilatation and uterine contraction in imminent premature delivery are closely related to chemical mediators from activated granulocytes which infiltrate into the cervix. It is known that urinastatin (urinary trypsin inhibitor, UTI) inhibits many kinds of chemical mediators from granulocytes and macrophages such as granulocyte elastase (elastase) and interleukin 1. We examined the effect of a UTI suppository on uterine contraction and the elastase level in cervical mucus in cases of imminent premature delivery. We treated 43 cases of imminent premature delivery with tocolysis index 3 or 4 with 4 kinds of therapy: Group A (N = 12): ritodorine drop infusion therapy; Group B (N = 9): daily UTI suppository (1,000U) therapy; Group C (N = 14): daily UTI suppository + ritodorine drop infusion therapy; Group D: daily UTI suppository + ritodorine drop infusion + antibiotics (oral cepharosporine) therapy. The elastase level of cervical mucus before treatment was 0.76 +/- 0.40 micrograms/ml in group A, 0.93 +/- 0.43 micrograms/ml in group B, 0.85 +/- 0.40 micrograms/ml in group C and 0.90 +/- 0.41 micrograms/ml in group D. There was no significant difference between these groups. The elastase level in cervical mucus was 0.75 +/- 0.47 micrograms/ml in group A, 0.27 +/- 0.35 micrograms/ml in group B, 0.27 +/- 0.33 micrograms/ml in group C and 0.30 +/- 0.19 micrograms/ml in group D, respectively. The elastase level was decreased significantly in groups B, C and D. The time taken to depress uterine contraction was 65 +/- 66 min in group A, 375 +/- 336 min in group B, 70 +/- 64 min in group C and 58 +/- 53 min in group D, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Intravaginal↗

PubMedDate not supplied

Feasibility of the Ph.Eur. flow-through cell for dissolution testing of the compounded rectal suppositories containing indomethacin or sodium diclofenac.

Ph.Eur. and BP have introduced a dissolution apparatus for suppositories. Suitability of the apparatus for quality control of indomethacin or sodium diclofenac (100 mg) compounded suppositories was evaluated and the effect of the type of suppository base on dissolution profiles was studied. The fastest and most reproducible release profiles were observed for hydrophilic base (macrogols). More than 80% of the drug was released during 60 min, while after 350 min 18.5-50% of the total amount was released from lipophilic bases (Witepsol and Adeps solidus). The results demonstrate that slow and non-reproducible release occurs when the lipophilic suppository base does not melt. The feasibility of the test for the formulations, which do not melt during the procedure, is questionable.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed1992

Bioavailability of ibuprofen from oral and suppository preparations in rats.

Bioavailability of ibuprofen (15 mgkg-1) from oral and suppository dosage forms was investigated. Three different combinations of PEG 4000 and 1000 and theobroma oil were used as suppository bases. Oral administration gave higher values for mean residence time (MRT) and absolute bioavailability (F) compared to suppository dosage forms. The theobroma oil base was associated with lower maximum plasma concentration (cpmax), area under the concentration time curve (AUC) and F values compared to the other bases but differences were not significant (P greater than 0.05). Ibuprofen appears to be strongly retained by the lipophilic base, thereby limiting its diffusion through the rectal mucosal membrane. The absorption profile was slightly improved for the three PEG combination bases but were inferior to oral dosing. It is suggested that the relatively smaller size of the rectal mucosal membrane compared to the small intestine was primarily responsible for limiting the rate/extent of ibuprofen absorption. The absorption profile from the suppository preparations may be enhanced by the appropriate selection of the bases and their additives.

Administration, Oral↗

PubMed1991

Pharmacokinetic evaluation of ethionamide suppositories.

The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double-blind, double-dummy, crossover design was used. Treatments compared 250-mg ETA tablets and a placebo suppository to a 500-mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high-performance liquid chromatography. The area under the serum concentration-time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.

Administration, Oral↗

PubMed1991

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 2. In vitro membrane diffusion studies].

Rectal suppositories with 0.10 g/2.0 g Papaverine hydrochloride content were made with 12 different vehicles. The membrane diffusion method was used to study the factors influencing the in vitro drug liberation. The Polysorbate 20 and 61 tenside pair, the optimal concentration of which was 5% each, was found to influence diffusion favourably. Neutral oils softening the consistency (Miglyol 812 and Estasan), similarly in 5%, also had a favourable effect on the in vitro diffusion by increasing the spreading properties. As to the lipophil suppository masses with high and low hydroxyl numbers, only the latter could be used favourably. The 6-month-long storage resulted in drug retention in several experimental series. Correlation was found in several cases between the physical parameters of the suppositories and their in vitro drug liberation. Finally, with the help of linear regression calculation and in view of the in vitro relative bioavailability values the optimal vehicle is suggested for the formulation of suppositories containing Papaverine hydrochloride. The triglyceride type Estaram 299 was found to be the most suitable in every respect, either in itself or combined with 5% neutral oil.

Diffusion↗

PubMed1977

Butazolidin suppository medication in rheumatism; a clinical study in general practice.

One hundred and seventeen patients with various rheumatic conditions were admitted by eighteen general practitions to a multicentre open clinical trial of the acceptability, effectiveness and tolerability of Butazolidin Suppositories. Dosage was one or two suppositories (= 250 mg or 500 mg phenylbutazone) per day for up to eight weeks. Of the 117 patients entered onto the register for the study, 10 patients refused suppository medication and 8 had local conditions contra-indicating their use. Of the 99 patients starting the trial proper, half had excellent symptomatic relief and tolerance. Sixteen patients discontinued because of poor response. The remainder (34) whilst having significant improvement as shown by mean symptom scores, discontinued treatment. The majority who discontinued did so because of minor local discomfort or minor gastric symptoms, suggesting that acceptability of medication was at least as important as intolerance. No patient had a serious or persistent adverse effect. Comparison with previous studies suggests that gastro-intestinal tolerance to phenylbutazone is improved when it is administered by suppository.

Arthritis, Rheumatoid↗

PubMed1987

[The effect of tegafur suppository and glutathione in patients with gastric and colonic cancer with special reference to the histopathological anticancer effect].

The purpose of these studies is to evaluate the anticancerous effects of tegafur suppository and Glutathione (GSH) as enhanced drug and compare the difference of the histopathological effects and tissue concentration of 5-FU and FT-207 in gastric and colon cancer. Thirty three patients with gastric cancer and 17 with colon cancer were treated by tegafur suppository at a dose of 1,500 mg/day and GSH, 1,200 mg/day intravenously. These patients were clinically divided into two groups, one of which was treated with tegafur suppository (Group A) and another administered with suppository and GSH (Group B). Five-fluorouracil was measured by GC-MF method and FT-207 was also done by HPLC method. After surgery, relationship between tissue concentration of 5-FU and histopathological effects were investigated. In gastric cancer, 5-FU concentration in cancer tissue was significantly kept high level in cancer tissue in patients treated with tegafur and GSH (Group B). However, there was no same results in colon cancer. These results seemed to be the difference of organ specificity. According to histopathological studies, well differentiated adenocarcinoma including papillary carcinoma were markedly effective compared to poorly differentiated adenocarcinoma in both cancer. This difference of anticancerous effect was supposed to be microangiographically different of microvascular architecture and quantity of anticancerous agents in tumor.

Colonic Neoplasms↗