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At least 127 records · Page 7Linked to original sources
PubMed1987

Bioavailability of sodium valproate suppositories during repeated administration at steady state in epileptic children.

Oral administration of antiepileptic drugs can temporarily be impossible under certain conditions, such as altered states of consciousness, spike-wave stupour, gastro-intestinal disturbances with nausea and vomiting, prior to or during surgery or certain diagnostic procedures, and because of drug refusal in patients with mental retardation or psychiatric problems. Although rectal administration of sodium valproate (NaVPA) has been shown to be a possible alternative route, little is known about the bioavailability and local effects during repeated administration of NaVPA suppositories. These aspects were investigated in 13 epileptic children and adolescents on chronic NaVPA therapy. Eight patients were treated with the oral solution (Group A; mean age 10.6 years) and five patients with enteric coated tablets (Group B, mean age 16.4 years). In every patient five serum levels of VPA over a 24 h period were measured under steady-state conditions. Thereafter, suppositories were administered for 2-7 days and serum levels were again determined (identical dosing and sampling times). Bioavailability of NaVPA was calculated on the basis of the area under the concentration vs. time curve over 24 h. The average bioavailability for suppositories compared with the oral form was 112.4% in Group A and 99.5% in Group B. Fluctuations of serum VPA levels were very similar with suppositories and oral solution, and more pronounced than with the enteric coated tablets. Stool frequency was not increased by repeated administration of suppositories, except for a three-fold increase in one patient. There was no objective or subjective evidence of local irritation from the suppositories. In conclusion, NaVPA suppositories have the same bioavailability under steady-state conditions as oral preparations and they are well tolerated.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed2004

The role of various surfactants on the release of salbutamol from suppositories.

Salbutamol is a selective beta(2)-adrenoreceptor agonist with different pharmacological effects. In this research because of the simplicity of suppository application in elderly and its higher plasma concentration than tablets as well as its particular indication in premature labour, salbutamol suppositories were prepared. The suppositories were formulated containing 10 mg of the drug and Witepsol H15, the oleaginous soluble base using melting method. To optimize the release rate of drug, different surfactants namely, sodium lauryl sulphate (SLS) as an ionic surfactant and Tween 80 as well as Arlacel 60 as non-ionic surfactants with different HLBs were chosen. The effect of surfactant concentration on the release rate of salbutamol from suppositories were also investigated. All prepared formulations fulfilled the specifications set down in British Pharmacopoeia. The results showed that Tween 80 (2%w/w) and SLS (0.75%w/w) caused an increase in dissolution rate of salbutamol from suppositories. As anionic surfactants, such as SLS, cause greater damage on mucosa than non-ionic surfactant, such as Tween 80, this study recommended that Tween 80 could be added in suppository formulation in order to increase the dissolution rate of salbutamol. It was also shown that the release rate of salbutamol altered linearly with the amount of Tween 80 in suppository formulations.

Adrenergic beta-Agonists↗
PubMed2005

Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats.

To develop a poloxamer-based solid suppository with poloxamer mixtures, the melting point of various formulations composed of poloxamer 124 (P 124) and poloxamer 188 (P 188) were investigated. The dissolution and pharmacokinetic study of diclofenac sodium delivered by the poloxamer-based suppository were performed. Furthermore, the identification test in the rectum and morphology test of rectal tissues were carried out after its rectal administration in rats. The poloxamer mixtures composed of P 124 and P 188 were homogeneous phases. Very small amounts of P 188 affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 124/P 188 (97/3%)] with the melting point of about 32 degrees C was a solid form at room temperature and instantly melted at physiological temperature. Very small amounts of P 188 hardly affected the dissolution rates of diclofenac sodium from the suppository. Dissolution mechanism analysis showed the dissolution of diclofenac sodium was proportional to the time. The poloxamer-based suppository gave significantly higher initial plasma concentrations and faster T(max) of diclofenac sodium than did conventional PEG-based suppository, indicating that the drug from poloxamer-based suppository could be absorbed faster than that from PEG-based one in rats. It retained in the rectum for at least 4 h and could not irritate or damage the rectal tissues of rats. Thus, the poloxamer-based solid suppository with P 124 and P 188 was a mucoadhesive, safe and effective rectal dosage form for diclofenac sodium.

Adhesives↗
PubMed1995

Reduction in bowel program duration with polyethylene glycol based bisacodyl suppositories.

UNLABELLED: The neurogenic bowel caused by spinal cord injury frequently requires a bowel program (BP) with stimulant suppositories for effective defecation. OBJECTIVE: The effectiveness of bowel programs initiated by hydrogenated vegetable oil based bisacodyl (HVB) suppositories was compared with that of polyethylene glycol based bisacodyl suppositories (PGB). DESIGN: Single subject, randomized treatment. SETTING: Outpatient. SUBJECT: Chronic T2 complete spinal cord injury (SCI). INTERVENTION: The suppository for the every third-day BP was randomized to PGB or HVB. The times in minutes of the following BP events were recorded: suppository insertion, first flatus, begin stool flow, end stool flow, and transfer off toilet. OUTCOME MEASURES: BP event times were used to derive BP intervals: suppository insertion to first flatus = Time to Flatus, first flatus until begin stool flow = Flatus to Stool Flow, begin stool flow until end stool flow = Defecation Period, end stool flow until the transfer off the toilet = Wait Until Transfer, and suppository insertion until transfer off the toilet = Total BP Time. The number of digital stimulations required and the amount of stool results were recorded. RESULTS: The data included two groups of BPs: HVB (N = 13) and PGB (N = 13). Wilcoxon's rank sum tests were used to compare mean times for each of the BP intervals: Time to Flatus (HVB 37 minutes, PGB 10 minutes, p < .0001), Flatus to Stool Flow (HVB 6.0 minutes, PGB 5.9 minutes, p = .9578), and the Defecation Period (HVB 31, PGB 21, p = .0043).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1999

Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum.

Mucoadhesive liquid suppositories were prepared by adding mucoadhesive polymers (0.6%) to a formulation of thermally gelling suppositories that contained poloxamer 407 (15%), poloxamer 188 (15%) and propranolol HCl (2%). Hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), carbopol, polycarbophil and sodium alginate were examined as mucoadhesive polymers. The characteristics of the suppositories differed depending on the choice of mucoadhesive polymer. For example, the gelation temperature was between 30 and 36 degrees C, the mucoadhesive force was between 430 and 5800 dyne/cm2, the apparent first-order release rate constant in phosphate buffer, pH 6.8, was between 0.399 and 0.271 h-1, the migration distance of the suppository in the rectum 4 h after administration was between 1 and 5 cm, and the bioavailability of propranolol was between 60.9 and 84.7%. Rectal bioavailability increased as the mucoadhesive force increased (r=0.984, p<0.0005), and the migration distance decreased (r=-0.951, p<0.005). No relationship was found between the bioavailability and the gelation temperature, drug release or irritation of the rectal mucosal membrane by the suppository. Therefore, retaining propranolol at the dosed site in the rectum by the addition of appropriate mucoadhesives to the formulation of liquid suppositories appears to be a very important factor in avoiding first-pass hepatic elimination and thereby increasing the bioavailability of the drug. Among the mucoadhesive polymers examined, sodium alginate and polycarbophil exhibited the largest mucoadhesive force and the smallest intrarectal migration resulting in the largest bioavailability of propranolol (84.7 and 82.3%, respectively). In contrast to other polymers, sodium alginate alone caused no irritation of the rectal mucosal membrane. Thus, poloxamer liquid suppositories containing sodium alginate appears to be a preferred formulation for drugs that are sensitive to extensive first-pass metabolism.

Adhesiveness↗
PubMed1999

Development of a thermo-reversible insulin liquid suppository with bioavailability enhancement.

The purpose of this work is to develop a thermo-reversible insulin liquid suppository, which undergoes a phase transition to bioadhesive gels at body temperature and enhances the bioavailability of insulin. The effects of insulin and sodium salicylate on the physicochemical properties of a liquid suppository composed of poloxamer P 407, P 188 and polycarbophil were investigated. The pharmacodynamic study and quantitative histological assessment of the rectal mucosa of rats were carried out after the dose of insulin-loaded liquid suppositories with different amounts of sodium salicylate into streptozotocin-treated rats. Only thermo-reversible insulin liquid suppository [insulin/P407/P188/polycarbophil/sodium salicylate (100 (IU/g)/15/20/0.2/10%)] showed the optimal physicochemical properties and good safety in rats. It gave significantly lower plasma glucose levels, AUC(0-->4h) (the area below basal glucose level) and C(nadir) (the plasma glucose levels at the nadir) than did the solid and liquid suppositories without sodium salicylate in rats, indicating that the insulin from liquid suppository with sodium salicylate could be well absorbed in rats due to the absorption enhancing effect of sodium salicylate. It is concluded that thermo-reversible insulin liquid suppository [insulin/P 407/P 188/polycarbophil/sodium salicylate (100 (IU/g)/15/20/0.2/10%)], which was easy to administer without any pain during insertion and remained at the administered sites, could have a potential to be developed as a more convenient, safe and effective rectal delivery system of insulin.

Administration, Rectal↗
PubMed1997

Safety, tolerability, and pharmacokinetics of sumatriptan suppositories following single and multiple doses in healthy volunteers.

A suppository formulation of the 5HT1 agonist sumatriptan could prove an important therapeutic option in migraine patients who dislike or poorly tolerate injectable therapy and where oral tablet administration is unsuitable because of severe migraine-related vomiting. Two independent double-blind, randomized clinical studies were conducted to evaluate the safety, tolerability and pharmacokinetics of sumatriptan suppositories following ascending single doses (four different dose levels) and multiple doses. In the four-period, crossover, single-dose study, 24 healthy male subjects were randomized to receive a suppository containing 12.5, 25, 50, or 100 mg on separate occasions 3-14 days apart. The suppositories were generally well tolerated; transient asthenia, drowsiness, and headache were the most frequently reported adverse events, and these were not dose-related. Peak plasma concentrations (Cmax) of sumatriptan were proportional to dose from 25 to 100 mg; area under the plasma concentration-time curve (AUC infinity) values were proportional to dose except at the highest doses, when they were greater than those predicted from lower doses. For all doses, the tmax of sumatriptan occurred within 2.5 h, and the t1/2 was approximately 2 h. In the two-period, placebo-controlled, crossover, repeat-dose study, 12 healthy adult male subjects were randomized to receive either a 50-mg sumatriptan suppository or placebo suppository, administered rectally twice a day, for 11 doses (5 1/2 days). Adverse events were no more frequent with sumatriptan than with placebo, and stool guaiac, rectal examinations, and physical examinations remained normal. No significant differences were noted between Day 1 and Day 6 values in the AUC, Cmax, time of peak serum concentration (tmax), elimination half-life (t 1/2), fraction of the dose excreted in the urine (fe), or renal clearance (Clr) of sumatriptan or its pharmacologically inactive indole acetic acid metabolite. Serum metabolite concentrations were two to three-fold higher than corresponding sumatriptan concentrations. No clinically significant accumulation of sumatriptan or its metabolite occurred. Overall, these studies show that sumatriptan administration via a suppository formulation is well tolerated, allows rapid absorption of sumatriptan, results in sumatriptan Cmax values that are proportional to dose from 25 to 100 mg, and is not associated with accumulation of sumatriptan or its metabolite.

Adolescent↗
PubMedDate not supplied

Thermally reversible in situ gelling carbamazepine liquid suppository.

Carbamazepine (CBZ), indicated for the control of epilepsy, undergoes extensive hepatic first-pass elimination after oral administration. A rectal dosage form of CBZ is not commercially available, although it is of particular interest when oral administration is impossible. Conventional suppositories can cause patient discomfort and may reach the end of the colon; consequently, the drug can undergo the first-pass effect. Mucoadhesive liquid suppositories of CBZ were prepared by adding carbopol to formulation of thermally gelling suppositories that contain 20% poloxamer 407 and either 15% poloxamer 188 or 1% methylcellulose. Gellan gum was also tried instead of 20% poloxamer. All formulations contained 10% CBZ. The characteristics of the suppositories differed depending on the formulation. The formula containing 20% poloxamer 407, 1% methylcellulose, and 0.5% carbopol showed reasonable gelation temperature, gel strength and bioadhesive force. The analysis of release mechanism showed that CBZ released from the suppositories by Fickian diffusion. In vivo evaluation of the same formulation showed higher peak plasma concentration of CBZ compared with the orally administered suspension containing the equivalent amount of drug. However, there was no statistical significant difference (p > 0.05) in extent of bioavailability between the liquid suppository and oral suspension as indicated by the values of AUC(0 - infinity), 17.9 and 18.8 micro g x h/ml, respectively. These results suggested that mucoadhesive in situ gelling liquid suppository could be an effective and convenient delivery system of carbamazepine.

Acrylic Resins↗
PubMed1999

Ketoprofen suppository dosage forms: in vitro release and in vivo absorption studies in rabbits.

In vitro release of ketoprofen from suppository bases and in vivo absorption in rabbits were studied. Suppositories containing 50 mg of ketoprofen were prepared using theobroma oil, esterified (c10-c18) fatty acids, and polyethylene glycol 1000 bases. The displacement values of the drug were determined and found to be of the order of theobroma oil > esterified (c10-c18) fatty acids and polyethylene glycol 1000 bases. The suppository hardness data revealed that the theobroma oil base produced relatively brittle suppositories. Using the USP dissolution method, the release of ketoprofen was observed to be greatest from polyethylene glycol 1000 suppositories. With the dialysis technique, the maximum release of drug was obtained from theobroma oil suppository containing polysorbate 40 at a 6% level. Selected suppository formulations were evaluated for rectal absorption studies in rabbits. The in vivo data showed that the optimum drug absorption took place from the polyethylene glycol 1000 base and theobroma oil formulation containing 6% polysorbate 40.

Absorption↗
PubMed2001

Release property of progesterone from a mixed-base suppository consisting of Witepsol W35 and Witepsol E85.

The mechanism of drug release from progesterone suppositories that consist of two types of hard fat (Witepsol W35 and Witepsol E85) was investigated. The strength, the thermodynamic characteristics, the surface structures, the drug release property, methylene blue penetration into suppositories, and change of surface structure after the dissolution test were employed for detecting characteristics of progesterone suppositories. The formulation with a mixing ratio of Witepsol W35 and Witepsol E85 at a 1:1 ratio showed the maximum strength value. The peak temperature of the suppositories showed a tendency to increase with increases in the ratio of Witepsol E85. The maximum height of the profiles measured with laser microscopy, from 20.8 microm to 29.2 microm, reached a maximum after 3 h of the dissolution test. When the suppositories were immersed in pH 7.4 phosphate buffer containing 0.5% methylene blue at 37 degrees C, the penetrating area increased with time. The weight of the suppositories also increased with time. According to these findings, it was suggested that the release of drug from a mixed type of suppository containing progesterone was via the matrix and pores.

Adjuvants, Pharmaceutic↗
PubMed2004

A rapid micro quantification method of paracetamol in suppositories using differential scanning calorimetry.

This study adopts Differential Scanning Calorimetry (DSC) to analyze the thermal properties of samples (2.5-4.0 mg) from the tip, middle, and base sections of individual paracetamol suppositories, which were sampled carefully using a stainless steel scalpel. The contents of paracetamol present in the samples obtained from these sections were determined from the enthalpies of fusion of paracetamol and expressed as % w/w paracetamol to allow comparison of the amount of paracetamol found in each section. The tip, middle, and base sections contained 10.1+/-0.2%, 10.1+/-0.2%, and 10.3+/-0.2% w/w paracetamol, and are statistically similar (One-way anova; p>0.05). This indicates that the preparation technique adopted produces high quality suppositories in terms of content uniformity. The contents of paracetamol in the 120-mg paracetamol suppositories determined by DSC and UV spectrophotometry were statistically equivalent (Students's t-test; p>0.05), 120.8+/-2.6 mg and 120.8+/-1.5 mg, respectively, making DSC a clear alternative method for the measurement of content of drug in suppositories. The main advantages of the method are that samples of only 2.5-4.0 mg are required and the procedure does not require an extraction process, which allows for the analysis to be completed rapidly. In addition, it is highly sensitive and reproducible, with the lower detection limit at 4.0% w/w paracetamol, which is about 2.5 times lower than the content of paracetamol (10% w/w) present in our 120-mg paracetamol suppositories and commercial paracetamol suppositories, which contained about 125 mg paracetamol. Therefore, this method is particularly suited for determination of content uniformity in individual suppositories in quality control (QC) and in process quality control (PQC).

Acetaminophen↗
PubMed1997

Utility of a rectal suppository containing the antiepileptic drug zonisamide.

A suppository of zonisamide (ZNS) was investigated from the viewpoint of pharmaceutical evaluation, pharmacokinetics and pharmacological effect. Two types of ZNS suppositories were prepared. One used Witepsol (H-15:S-55 = 3:1) as a lipophilic base and the other polyethylene glycol (PEG, 4000:1500 = 4:1) as a hydrophilic base. The in vitro release rate of ZNS from the PEG suppository was significantly rapid compared with that of ZNS from Witepsol. Male Wistar rats were administered ZNS (20 mg/kg) using an intravenous, oral or rectal (PEG or Witepsol) route. The absorption of ZNS from the PEG suppository was more rapid than that of ZNS from the Witepsol suppository or from the oral preparation. The peak plasma concentration (Cmax) after a rectal administration of ZNS with Witepsol or PEG suppository was significantly higher than that after the oral administration of ZNS. However, the bioavailability of the three preparations was approximately 100%. Male ICR mice were administered ZNS (80 mg/kg) using the oral or rectal (PEG or Witepsol) route. A positive correlation was observed between the electroshock seizure (ES) threshold and ZNS concentration in plasma or brain. Further, there was no significant difference in the ES threshold or the ZNS concentration in plasma or brain among the three preparations. These results indicate that a ZNS suppository is a very useful preparation from the viewpoint of both pharmacokinetics and pharmacological action.

Administration, Oral↗
PubMed1989

Enhancing effect of glyceryl-1-monooctanoate on the rectal absorption of gentamicin from hollow-type suppositories in rabbits.

A hollow-type suppository containing gentamicin (GM) in its cavity was prepared using Witepsol H-15 (H-15) mixed with glyceryl-1-monooctanoate (MO) or MO alone in the body of the suppository (type I) and a suppository (type II) containing GM and MO in the cavity was constructed using H-15 in the body of the suppository. Without MO, GM (60 mg) was not absorbed (plasma GM levels less than 1 microgram/ml). However, the absorption of GM from the rectum of rabbits was enhanced by coadministered MO in types I and II. Even when the amount of GM was decreased to 6 mg (1/10), GM was observed in the plasma (Cmax, 3.5 +/- 0.3 micrograms/ml) after administration of the suppository made from MO mixed with H-15. The enhancing effect of MO on the rectal absorption of GM could not be further increased by incorporating an amount of MO larger than approximately 300 mg into the suppository. This study demonstrates that MO can be used in the two types of hollow suppositories as an effective enhancing agent of rectal absorption of poorly absorbed drugs such as GM.

Animals↗
PubMed1991

Enhancement effect of lauric acid on the rectal absorption of propranolol from suppository in rats.

In a previous paper, we have demonstrated that medium chain fatty acids significantly enhance the in vitro rectal absorption of propranolol (PL) and that the enhancement may be partly due to the formation of a complex with a fatty acid at a 1:1 molar ratio. To confirm in vivo the enhancement effect of lauric acid on PL absorption, PL suppositories with lauric acid at various molar ratios were administered to rat rectum. PL absorption from Witepsol and macrogol suppositories with lauric acid at a 1:1 molar ratio was much larger than that after PL alone and the 1:2 or 1:3 molar ratio ones. The bioavailability (BA) after administration of the 1:1 molar ratio suppository (PL, 4 mg/kg) was 1.6- and 2.1-fold for the Witepsol and macrogol formulations respectively, compared with that after PL alone. A similar result was obtained with the PL solid dispersion suppository with lauric acid at a 1:1 molar ratio, showing a 1.7-fold higher BA compared with PL alone. The release of PL from the macrogol suppository was significantly faster at a 1:1 molar ratio than that of other preparations, but not so in the solid dispersion suppository. There was not good agreement between the release rates of PL from the suppositories and the plasma levels after dosing. These results supported the concept that a portion of PL, by forming a 1:1 complex with lauric acid, would penetrate across the rectal mucosa more easily than PL alone.

Administration, Rectal↗
PubMed1993

Methods of evaluation of release of carbon dioxide from effervescent suppositories.

Two different test methods were studied for the evaluation of release profiles of carbon dioxide, CO2, from effervescent suppositories. Three lots of commercial suppositories containing sodium bicarbonate and anhydrous sodium dihydrogen phosphate were used. The volume of CO2 released from these suppositories in normal saline with or without polysorbate 80 as a medium was measured with a gas burette. In the measurement performed using the apparatus without stirring, method 1, only 60% of CO2 was released from the suppositories in the medium without polysorbate 80. In this measurement, a native release profile was detected because the medium was not stirred. In the case with stirring, however, method 2, 100% was released from those suppositories in the medium containing 1% polysorbate 80 with comparatively low standard deviations. These findings indicate that method 1 is most beneficial for a test comparing the effects of various factors such as additives and melting points on the release profiles of CO2 from the effervescent suppositories. However, this method is not practical for quality control of formulations because of the incomplete release of CO2; method 2, in contrast, is useful because of its complete release and low standard deviations. These results suggest that methods 1 and 2 for release tests of CO2 are most applicable to the early and late formulation studies of effervescent suppositories, respectively.

Carbon Dioxide↗
PubMed1993

Effects of bases and additives on release of carbon dioxide from effervescent suppositories.

For the formulation of effervescent containing sodium bicarbonate and anhydrous sodium dihydrogen phosphate, the effects of bases and additives on the release profile of carbon dioxide, CO2, from the suppositories were studied by an in vitro release test using a gas burette. The suppository bases employed were Witepsol H-15, W-35 and E-85, and the additives were Aerosil 200 and soybean lecithin. The melting points and viscosities of the suppositories were also measured to interpret the CO2 release profiles. The rate and amount of CO2 released from suppositories prepared with bases having different melting points and hydroxyl values decreased with increasing melting point and decreasing hydroxyl value. The addition of Aerosil 200 to the suppository bases considerably reduced the rate and amount of CO2 released owing to the increasing viscosity of the melted bases, while the addition of soybean lecithin to those bases increased the rate and amount of CO2 released because of the improved wettability. Thus, the release profiles of CO2 from the effervescent suppositories were considerably influenced by the hydroxyl values related to the contents of mono- and di-glycerides, the melting points of the bases, Aerosil 200 and soybean lecithin. This suggests that the rate and amount of CO2 released from the suppositories can be freely controlled by the combination of these various factors.

Carbon Dioxide↗
PubMed1999

[Effect of temperature on drug release and drug absorption in mixed type diclofenac sodium suppositories].

New types of diclofenac sodium suppositories known to control a drug release function for hospital preparations were developed based on a concept of the drug delivery system. Hard fat (Witepsol) used as a base of the suppository consists of a mixture of triglycerides, diglycerides and monoglycerides, and each Witepsol is characterized by its physicochemical properties. Authors disclosed that the amount of drug release measured in the commercially available diclofenac sodium suppositories decreased at a low temperature (36 degrees C). Mixed types of diclofenac sodium suppositories consisting of Witepsol W35 and Witepsol E85 as a base were also prepared and their drug release functions investigated in vitro and in vivo. The in vitro drug release properties changed with the mixing ratios of the two bases and with the temperature of the fluid tested. The amount of released diclofenac sodium increased with increases of both the ratio of Witepsol W35 in the suppository and the temperature of the test fluid. Moreover, several processes causing these phenomena were evidenced by the image analysis. The in vivo absorption of diclofenac sodium was found to be also influenced by these factors. Consequently, it is predicted that such factors as the ratio of Witepsol W35 in the suppository and the temperature will influence the drug absorption and the pharmacological effect of diclofenac sodium suppositories.

Administration, Rectal↗
PubMedDate not supplied

Practicality of 5-aminosalicylic suppositories for long-term treatment of inactive distal ulcerative colitis.

BACKGROUND/AIMS: Topical 5-aminosalicylic acid (5-ASA) is regarded as an effective form of therapy for distal ulcerative colitis. Unfortunately, experience about acceptability and tolerance of long-term treatment with 5-ASA suppositories is still meager. METHODOLOGY: We have evaluated the performance of 5-ASA suppositories as maintenance treatment in 34 patients with inactive distal colitis. Prior to entering the study, all patients were in clinical remission for 1-12 months. A single 500 mg 5-ASA suppository was administered nightly for 12 months in every patient and all other treatments were discontinued. Clinical evaluation was performed at 3, 6 and 12 months. RESULTS: Four patients withdrew from the study within the first 3 months because of local intolerance to the suppositories. Score of both comfort and tolerance was significantly higher in patients who continued treatment than in those who withdrew. Two patients who stayed in remission withdrew, one at 7 months because of thrombocytopenia and the other at 9 months for personal reasons. Of the 28 remaining patients, 7 relapsed and 21 remained in clinical remission at the end of the 12-month study period. Eleven of the 21 responder patients agreed to a sigmoidoscopic examination, that confirmed remission in all of them. Eight out of the 9 patients who had previously received 5-ASA enemas preferred suppositories to enemas. Apart from the 4 patients who did not tolerate suppositories, 26 patients considered this form of therapy quite comfortable. CONCLUSIONS: 5-ASA suppositories are generally well tolerated and considered comfortable for treatments of at least one year.

Adolescent↗