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Efficacy of promethazine suppositories dispensed to outpatient surgical patients.

Postoperative nausea and vomiting frequently complicate outpatient anesthesia and surgery. The duration of treatment for this complication must occasionally extend beyond discharge from the hospital. In this study, we evaluated the commonly used anti-emetic promethazine for its efficacy in the post-discharge period. Adult outpatient surgical patients who had excessive postoperative nausea and vomiting in the recovery room, or who were at risk for postoperative nausea and vomiting following discharge were given two promethazine suppositories (25 mg) for home use. All patients were contacted by our recovery room nurses on the first business day after their surgery and questioned as to their use of the suppositories and, if used, their efficacy. We found that 55 percent of patients given promethazine suppositories for home use had nausea and vomiting in the post-discharge period. Of the patients given promethazine, 89 percent used the suppositories. All of these patients reported improvement in their symptoms following use of the suppositories. None reported adverse effects from the promethazine suppositories. In conclusion, we found promethazine suppositories to be an inexpensive and efficacious treatment for nausea and vomiting in adult outpatient surgical patients following discharge from the hospital. Side-effects were minimal, and our patients voiced no complaints about this mode of therapy. We recommend this therapy for treatment of nausea and vomiting after hospital discharge following adult outpatient surgery.

Aged↗

PubMed2005

[Treatment and mechanism of compound carraghenates suppository to rat acute rectal mucous injury].

OBJECTIVE: To investigate the treatment and mechanism of compound carraghenates suppository to rat acute rectal mucous injury. METHODS: The model of rat acute rectal mucous injury was established by 3% acetic acid. Two hundred and forty rats were divided equally into control and experimental group. The rats of experimental group were administrated with 20 mg carraghenates suppository via rectum twice a day, but rats of control group were not administrated with carraghenates suppository. Thirty rats in both groups were executed at different time points. The pathologic changes were observed and the rectal mucous injury was scored. Immunohistochemical staining was used to evaluate the effect of carraghenates suppository on expression of VEGF, iNOS, IL-8, MMP9, HIF-1 alpha and PCNA in the two groups. RESULTS: The scores of rectal mucous injury was lower, the pathologic changes such as hyperaemia, edema, destroy of glands were less severe, and tissue repair time was shorter in experimental group compared with those in the control group at 24 h, 78 h and 120 h after administration of carraghenates suppository. No obvious cicatrisation was observed in experimental group. Expression of VEGF and MMP9 was significantly lower in experimental group compared with those in the control group at 24 h after administration. Expression of VEGF, iNOS, IL-8, MMP9, HIF-1alpha and PCNA were statistically decreased in experimental group than those in the control group at 72 h, 120 h after administration. MVD in experimental group was statistically decreased than that in the control group. CONCLUSION: The compound carraghenates suppository can reduce the rectal mucous injury from 3% acetic acid, and accelerate the wound healing without obvious cicatrisation. The compound carraghenates suppository can reduce the expression of MMP9, VEGF, IL-8, PCNA, iNOS and HIF-1 alpha, which may play a role in its protective mechanism.

Animals↗

PubMed1983

[Therapeutic evaluation of an ampicillin suppository (KS-R1) used against acute suppurative otitis media in children: a comparison with an oral preparation].

A comparative well-controlled study was performed to evaluate the efficacy and tolerability of KS-R1 (ampicillin rectal suppository, 125 mg X 4/day) administered to the rectum as compared with those of orally administered ampicillin (ABPC) with same dosage. The results obtained were as follows. The clinical effect of the drug was judged in 100 cases (suppository group in 45 cases, oral group in 55 cases) out of 111 cases. The overall efficacy rates evaluated on standard criteria were 93.3% for the suppository group and 89.1% for the oral group. There was no statistically significant difference between 2 groups. Evaluation by stratification according to the dose, disease type and age also revealed a slightly higher efficacy rate on each parameter in the suppository group, but no significant difference between 2 groups. The bacteriological effects evaluated in 84 cases (suppository group in 38 cases, oral group in 46 cases) were 94.7% and 93.5%, respectively. There was no statistically significant difference between 2 groups. Side effects were evaluated in 101 cases (suppository group in 46 cases, oral group in 55 cases), but the incidence rate showed no significant difference between the 2 groups; 3 cases (each 1 of abdominal pain, periproctal redness and periproctal erosion) were observed in suppository group and 2 cases (each 1 of stomach pain + soft stool and diarrhea) in oral group. The results indicate that KS-R1 is equally effective and tolerable against acute suppurative otitis media compared to oral administration of ABPC, and considered to be useful.

Administration, Oral↗

PubMed1984

Pharmacokinetics and bioavailability of metronidazole after tablets, suppositories and intravenous administration.

The pharmacokinetics of metronidazole were determined in cross-over study on 11 healthy volunteers after 400 mg tablets from two producers. 1000 mg suppositories and 800 mg intravenously (IV). High-pressure liquid chromatography was used to assay both unchanged metronidazole (M) and the hydroxy metronidazole metabolite (OH-M). The peak concentrations were observed 1.2 - 1.3 hrs after the administration of tablets and 4.9 hrs after the suppositories. After the IV dose, the OH-M peak appeared only after 8 hours. The serum half-life was 6.5 hrs after the IV dose, 6.1 - 6.8 hrs after the tablets and 6.8 hrs after the suppositories. After IV dosage, the terminal phase distribution volume was 38.1 lit and the total body clearance 4.09 lit/hr. The bioavailability of the tablets was 80.4 and 84.1 per cent and after the suppositories 53.8 per cent. The rate of elimination OH-M was faster after suppositories than after IV dosage where it was intermediate after the tablets. Accordingly, the serum-half-life was 9.7 hrs after suppositories, 19.2 hrs after IV infusion, and 10.6 and 11.8 hrs. after the tablets. The rates of apparent metabolization was graded in the same relative order, with a faster rate after the suppositories, 0.168 hrs-1 compared to 0.368 hrs-1 after the IV route of administration. The differences pertaining to OH-M is considered probably to be caused by interaction with the metabolic activity of the bacterial flora of the colon.

Absorption↗

PubMed1995

[The efficacy of midazolam-famotidine suppository for premedication in children].

We evaluated the efficacy of midazolam-famotidine suppository (M-F suppository) for premedication in children. After obtaining informed parental consent, we studied children aged 5m-7y, ASA I status, scheduled for minor elective surgery. The suppository group (n = 26) was given suppository of both midazolam 0.5 mg.kg-1 and famotidine 2 mg.kg-1, and the intramuscular injection group (n = 19) was given hydroxyzine 1 mg.kg-1. In the suppository group, gastric pH (3.90 +/- 0.34) was significantly higher, and gastric volume (1.88 +/- 0.54 ml) was significantly less than in the intramuscular injection group (1.82 +/- 0.15, 8.42 +/- 1.76 ml). The M-F suppository may offer similar sedative effect as an intramuscular injection of hydroxyzine. We concluded that the M-F suppository is an effective premedicant for pediatric patients.

Administration, Rectal↗

PubMed1996

[The relative bioavailability of paracetamol in suppositories in comparison to tablets].

Relative Bioavailability Studies on Paracetamol in Suppositories as Compared to Tablets. Relative bioavailabilities of 250 mg paracetamol (CAS 103-90-2) in ben-u-ron 125 mg and ben-u-ron 250 mg suppositories were determined in comparison with that of cut-in-half Benuron tablets 500 mg in an open intraindividual 3-period-changeover-study in 18 healthy volunteers. Plasma concentrations of paracetamol were analyzed by means of a specific and sensitive HPLC-method with UV-detection. For the assessment of the bioavailability AUC, Cmax, tmax and HVD (half value duration) were used as pharmacokinetic characteristics. Relative bioavailability of paracetamol was 102% for 125 mg and 93% for 250 mg suppositories, compared with that of cut-in-half 500 mg tablets. Mean maximum paracetamol plasma concentrations (Cmax) were determined as 2.1 micrograms/ml (CV = 31%; (CV = Coefficient of Variation), 2.0 micrograms/ml (CV = 27%) and 3.5 micrograms/ml (CV = 27%) after administration of 125 mg and 250 mg suppositories and 500 mg cut-in-half tablets, respectively. These maximum concentrations were achieved 2.2 +/- 0.7, 1.8 +/- 0.7 and 0.6 +/- 0.3 h (tmax) after administration of the respective preparations. The corresponding HVD-values were 3.8 +/- 1.0, 3.5 +/- 0.9 and 1.8 +/- 0.8 h, respectively. Extent of bioavailability of paracetamol (dose: 250 mg) following administration of 125 mg as well as 250 mg suppositories in comparison with 500 mg tablets was shown to be equivalent. The results obtained in this study confirm the adequate bioavailability of both suppositories compared with tablets. On the other hand both suppository preparations were assessed as being bioequivalent concerning AUC and Cmax.

Acetaminophen↗

PubMed1998

Second trimester abortion using prostaglandin E2 suppositories with or without intracervical Laminaria japonica: a randomized study.

OBJECTIVE: To compare the abortifacient efficacy of vaginal prostaglandin (PG) E2 suppositories with and without pretreatment with intracervical PGE2 gel and Laminaria japonica. METHODS: One hundred seventy-five women between 16 and 20 weeks' gestation requesting abortion were divided randomly into three groups. Forty-one received PGE2 vaginal suppositories alone to induce abortion, 72 had Laminaria placed 24 hours before vaginal PGE2, and 62 were given intracervical 0.5 mg PGE2 gel plus Laminaria 24 hours before vaginal PGE2. Maternal demographic characteristics, induction to delivery time, number of suppositories required, and complications were analyzed. RESULTS: The mean maternal age, gravidity, parity, race, and gestational age were similar among groups. Ninety-five percent of all women delivered within 24 hours. The induction to delivery time was significantly longer in the PGE2-only women (mean +/- standard deviation 689+/-319 minutes) compared with that of those receiving PGE2 plus Laminaria (487+/-321 minutes) and PGE2 plus Laminaria plus gel (547 +/-374 minutes, P = .01). There was a statistically significant difference in the number of suppositories needed to complete the abortion process. The PGE2-only group required more suppositories (median three, range 1-8) compared with PGE2 plus Laminaria (median 3, range 1-3) and PGE2 plus Laminaria plus gel (median 2.5, range 1-9; P = .001). Patients in the PGE2 plus Laminaria plus gel group reported more pain associated with placement (median pain score 4, range 0-10) compared with PGE2 plus Laminaria (median 2, range 0-9; P = .003). There was a lower incidence of febrile episodes in the PGE2-only group (29%) compared with PGE2 plus Laminaria (68%) and PGE2 plus Laminaria plus gel (54%, P = .002). CONCLUSION: Placement of Laminaria japonica 24 hours before PGE2 vaginal suppository-induced abortion resulted in a significantly shorter induction-to-delivery time, and pretreatment with Laminaria japonica decreased the number of suppositories required to complete abortion. Pretreatment with intracervical PGE2 gel increased pain associated with Laminaria placement and did not improve the efficacy of the procedure.

Abortion, Induced↗

PubMed2001

A comparison of the effect of loperamide in oral or suppository form vs placebo in patients with ileo-anal pouches.

OBJECTIVE: The effect of the anti-diarrhoeal drug, loperamide hydrochloride, on bowel function in patients with an ileo-anal pouch was studied by means of a blinded, three-tailed, case-controlled and randomized crossover trial, using a daily dose of 12 mg in either oral (4 mg t.d.s.) or suppository (6 mg b.d.) form. PATIENTS AND METHODS: Daily stool frequency was recorded in a diary and an objective measure of pouch motor function was obtained at the end of each treatment phase. Ten subjects (seven males, three females) aged 23-50 years (median 38 years) were studied 9-48 months (median 27 months) after ileostomy closure. Eight pouches had been constructed for ulcerative colitis and two for familial adenomatous polyposis (9J, 1W). RESULTS: Mean daily stool frequency during the oral loperamide phase was lower than during both the placebo (P=0.05) and suppository (P < 0.02) phases. Stool frequency did not differ significantly between placebo and suppository phases. There was a strong inverse correlation between mean daily stool frequency and pouch capacity (r=-0.82 after both oral and suppository phases). Large isolated pouch contractions were evident in five of eight subjects studied; suppression was observed in two of the five after oral loperamide and in three of the five after loperamide suppositories. Rhythmic pouch contractions were seen in four subjects and suppression was evident after loperamide suppositories (but not after oral loperamide) in three. A daily oral dose of 12 mg loperamide significantly lowered stool frequency in pouch patients and modified some aspects of pouch contraction. Loperamide suppositories produced more prominent suppression of pouch contractions but did not lower stool frequency. CONCLUSION: This suggests that the beneficial effect of oral loperamide is primarily due to its action on intestine proximal to the pouch itself.

Clinical Trial↗

PubMed1997

Multicenter comparison of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine hydrochloride, and allantoin in the treatment of symptomatic trichomoniasis.

BACKGROUND AND OBJECTIVES: Trichomonas vaginalis is a common vaginal pathogen. Oral metronidazole is the drug of choice for the treatment of trichomoniasis. Oral metronidazole, however, may cause unpleasant side effects and is contraindicated during the first trimester of pregnancy. In vitro studies and preliminary clinical data have suggested that intravaginal clotrimazole may be effective against this pathogen. GOALS: To compare the efficacy of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine, and allantoin (AVC suppositories) in the treatment of women with symptomatic trichomoniasis. STUDY DESIGN: In a multicenter, open-label trial conducted in 1982 and 1983, 168 symptomatic women with microscopically evident vaginal trichomoniasis were randomized to receive any of 2 g of metronidazole as a single oral dose, two 100-mg clotrimazole vaginal tablets once a day for 7 days, or vaginal suppositories containing 1.05 g of sulfanilamide, 14 mg of aminacrine hydrochloride, and 140 mg of allantoin (AVC suppositories) twice a day for 7 days. Wet mounts and cultures were repated at 1 to 2 and 4 to 6 weeks after completion of treatment. RESULTS: The number of patients who had positive cultures after treatment were 40/45 (88.9%) in the clotrimazole group, 35/43 (81.4%) in the AVC suppository group, and 9/45 (20%) in the metronidazole group (P < 0.001). All treatments were associated with a reduction in reported symptoms. Oral metrohidazole was more effective in reducing symptoms than either of the topical preparations. Adverse events, mostly mild or moderate in severity, were reported by 7 (14.6%) of 48 patients who had received oral metronidazole and 4 (7.8%) of 51 women who used AVC suppositories. There were no adverse events reported by the 50 women who used clotrimazole vaginal tablets. CONCLUSIONS: Oral metronidazole was more effective in eradicating T. vaginalis than clotrimazole vaginal tablets or AVC vaginal suppositories. All three regimens reduced symptoms; oral metronidazole was more effective in reducing symptoms than either topical preparation.

Administration, Intravaginal↗

PubMed1990

Influence of the hydrophilicity of suppository bases on rectal absorption of carprofen, a lipophilic nonsteroidal anti-inflammatory drug.

The influence of the hydrophilicity of fatty suppository bases on the rectal absorption of the lipophilic drug carprofen (octanol-buffer, pH 7.4; partition coefficient, 40) was investigated in dogs. Five animals received each of six carprofen formulations in a random sequence: intravenous, oral, and rectal solutions, and three suppository formulations. The suppository vehicles tested were semisynthetic glycerides containing saturated fatty acids mainly in the range of C10 to C18 [Massa Estarinum A (MEA), Massa Estarinum B (MEB), and Massa Estarinum 299 (ME299)]; their hydroxyl values increased from 1 for ME299, through 24 for MEB, to 45 for MEA. Following every drug administration, blood samples were collected over a period of 104 h and carprofen plasma concentrations were measured by a specific HPLC method with UV detection. The rate and extent of carprofen absorption were characterized by evaluation of the maximum plasma concentrations (Cmax), the time of their occurrence (tmax), absolute bioavailabilities, statistical moments, and by deconvolution. Carprofen was rapidly and completely absorbed from the oral solution. The maximum concentrations obtained with oral solutions were significantly higher than those observed with rectal solutions and with the three suppository formulations. Results obtained with the rectal solution exhibited a high degree of intersubject variability. After rectal administration of suppositories, the rate and extent of carprofen absorption increased with the hydroxyl value of the suppository base; the mean absorption times (MAT) and tmax were shorter with MEA (2.15 and 1.7 h, respectively) than with the less hydrophilic vehicles (MEB: 4.09 and 2.1 h, respectively; ME299: 4.22 and 2.4 h, respectively).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1993

Bioavailability of racemic ibuprofen and its lysinate from suppositories in rabbits.

Plasma concentration (C)-time (t) plots of ibuprofen from suppositories in rabbits are characterized by the sum of two exponentials, C = Be-lambda 2t-Ae-lambda 1t. When A exceeds B, there is a lag time (tlag = tc = 0) before the start of absorption. Evidence for dose-dependent area under the curve (AUC) of C versus t values is presented with the implication that elimination rate constants (ke) decrease and the AUC/dose ratio increase with dose. The lack of significant differences between the AUC values from suppository and the intravenous studies with similar doses implies complete absorption of ibuprofen from all the suppositories studied. The absorption rate constants (ka) were estimated on the presumption of complete absorption and dose-dependent elimination. Ibuprofen lysinate was absorbed significantly more readily than the free acid from suppositories. The lysinate suppository with a lipophilic surfactant had a higher absorption rate constant than that with a hydrophilic surfactant. The ka values did not significantly differ for a twofold difference in dose. Equations were developed to calculate true AUC and area under the moment curve (AUMC) values when A exceeds B, and to transform C versus t plots to the origin with A' = A = B. Times of maximum peak heights, mean residence (MRT), and mean absorption times (MAT = 1/ka) of suppositories when A > B are shown to differ by the lag time (tc = 0) from the plots of C versus t transposed to the origin. Although corrected AUC values when A > B are equal to the AUC values of C versus t plots transposed to the origin (A' = A = B), the corrected AUMC values when A > B significantly differ from the AUMC values for the C versus t plots transposed to the origin.

Animals↗

PubMed1990

Comparative bioavailability of a cisapride suppository and tablet formulation in healthy volunteers.

The comparative bioavailability of cisapride as a 30 mg suppository and three 5 mg oral tablets was investigated in 12 non-smoking, healthy male volunteers. The two formulations were administered on two separate occasions following an overnight fast, according to a randomized cross-over design. The plasma concentration of cisapride was measured over 48 h after drug administration. The 30 mg suppository exhibited a mean time to the peak plasma concentration of 3.8 h, while the tablets showed a significantly earlier peak time of 1.5 h. The maximum plasma concentration of cisapride after the 30 mg suppository (50.3 ng.ml-1) was significantly lower than after the tablets (74.3 ng.ml-1). The AUCs following the two treatments did not differ significantly from each other. The comparative bioavailability of the 30 mg cisapride suppository in relation to the three 5 mg oral tablets was 85%, with a 95%-confidence interval of 67% to 102% (not adjusted for dose). Normalizing the mean AUC by dose, the relative bioavailability of the suppository was 43% of that of the tablet. The elimination half-life of cisapride was not significantly different following the administration of the two formulations (9.3 h for the suppository and 9.8 h for the tablet).

Adult↗

PubMed1998

Treatment of detrusor instability with oxybutynin rectal suppositories.

Our aim was to determine whether oxybutynin hydrochloride suppositories can be used as a treatment for detrusor instability in patients who have not been able to tolerate oral pharmacological agents. A retrospective chart review of 25 women diagnosed with detrusor instability and treated with oxybutynin rectal suppositories was conducted. Each suppository contained 5 mg oxybutynin, 15 mg micronized Sila gel, and 1.25 g of a fatty acid base. Patients were started on one suppository twice daily and then dose titrated as tolerated. The range of the total daily dose was 5-20 mg. Nine of 25 women (36%) had greater than a 50% overall subjective improvement and 3 (12%) had some improvement. Seven of the 12 responders (58%) continued to use the suppositories for a prolonged period of time (> 90 days). The most common side effects reported were dry mouth 48% and constipation 14.3%. One patient with polymyositis developed a serious anticholinergic reaction which required hospitalization. It was concluded that patients who are unable to tolerate oral anticholinergic and antispasmodic agents for the treatment of detrusor instability may benefit from oxybutynin rectal suppositories.

Administration, Rectal↗

PubMed1982

Preoperative use of 5-fluorouracil suppository for carcinoma of the rectum.

A total of 50 patients with carcinoma of the rectum were treated with 5-fluorouracil suppository before operation. The suppository, which was made of Witepsol suppository base containing 5-fluorouracil, yielded high drug concentrations in carcinoma, draining blood and regional lymph nodes. As a clinical response to the suppository, a significant decrease in the size of tumor mass was noted in 8 of 50 carcinomas, but in other cases the gross change was unmeasurable. Thirty-three percent of the surgically resected carcinomas were histologically judged to have responded to the suppository. In such cases, histologic changes correlated well with the total dose of 5-fluorouracil. The adverse effects of the suppository were confined to anal pain, tenesmus and anal bleeding, probably due to the topical effect of 5-fluorouracil on the rectal mucosa.

Adult↗

PubMed1975

Midtrimester abortion induced by serial intravaginal administration of prostaglandin E2 suppositories in conjunction with a contraceptive diaphragm.

Midtrimester abortion was successfully induced in 68 of 69 patients with serial intravaginal administration of prostaglandin E2 suppositories behind a contraceptive diaphragm. The mean abortion time for the successful inductions was 13.07 hours; multiparous patients aborted somewhat faster, mean 12.72 hours, as compared to nulliparous patients, mean 14.22 hours. In 36 patients the PGE2 suppositories were placed behind an intact diaphragm and the mean abortion time was 14.89 hours. In 33 patients the PGE2 suppositories were placed behind a diaphragm modified by having an opening incised in the center, the mean time in these patients was 11.96 hours. Of the 68 successful abortions 59% of the patients aborted in 12 hours or less and 88% aborted within 24 hours. The most frequently encountered side effect was temperature elevation of 2 degrees F or higher which occurred in 68% of the patients. Temperatures returned to normal levels within 4 to 6 hours after the last adminstration of PGE2. Gastrointestinal side effects occurred in 45% of patients, but these side effects were well tolerated and did not require termination of drug administration in any of the patients. Intravaginal administration of PGE2 suppositories is a very effective abortifacient technque during the midtrimester, however the use of PGE2 in conjunction with a diaphragm did not appreciabley improve the technique although the amount of drug administered and the incidence of side effects was somewhat lower than when the PGE2 suppositories are used alone. If a diaphragm is to be used, a modified diaphragm is indicated since it simplifies the clinical management of the abortion, eases administration of the suppositories and permits a more accurate estimation of cervical changes, vaginal bleeding and abortion.

Abortion, Induced↗

PubMed2004

Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol.

To prepare an ibuprofen-loaded liquid suppository using eutectic mixture with menthol, the effects of menthol and poloxamer 188 (P 188) on the aqueous solubility of ibuprofen were investigated. The physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of ibuprofen, menthol and P 188 were investigated. Then, the pharmacokinetic study of ibuprofen delivered by the liquid suppositories composed of P 188 and menthol were then performed. In the absence of P 188, the solubility of ibuprofen increased until the ratio of menthol to ibuprofen increased from 0:10 to 4:6 followed by an abrupt decrease in solubility above the ratio of 4:6, indicating that four parts of ibuprofen formed eutectic mixture with six parts of menthol. In the presence of P 188, the solutions with the same ratio showed abrupt increase in the solubility of ibuprofen. Furthermore, the solution with ratio of 4:6 showed more than 2.5- and 6-fold increase in the solubility of ibuprofen compared with that without additives and that without menthol, respectively. The poloxamer gel with menthol/ibuprofen ratio of 1:9 and higher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2mg/ml. Ibuprofen increased the gelation temperature and weakened the gel strength and bioadhesive force of liquid suppositories. However, menthol did the opposite due to forming the eutectic mixture with ibuprofen. The ibuprofen-loaded liquid suppository [P 188/menthol/ibuprofen (15/0.25/2.5%)] with the maximum ibuprofen solubility of 1.2mg/ml was administered easily to the anus and to remain at the administered site without leakage after the dose. Furthermore, it gave significantly higher initial plasma concentrations, Cmax and AUC of ibuprofen than did solid suppository, indicating that the drug from poloxamer gel could be more absorbed than that from solid one in rats. Thus, the liquid suppository system with P 188 and menthol, a more convenient and effective rectal dosage form for ibuprofen will be expected to enhance the rectal bioavailability of ibuprofen.

Animals↗

PubMed2006

Enhanced anti-tumor activity and alleviated hepatotoxicity of clotrimazole-loaded suppository using poloxamer-propylene glycol gel.

To develop a novel clotrimazole-loaded poloxamer-based suppository with enhanced anti-tumor activity and alleviated hepatotoxicity, the melting point of various formulations composed of P 188 and propylene glycol were investigated. The dissolution and anti-tumor activity of clotrimazole delivered by the poloxamer-based suppository was performed. Furthermore, the hepatotoxicity of clotrimazole was carried out after its rectal administration compared to oral administration in mice. The poloxamer mixtures composed of P 188 and propylene glycol were homogeneous phases. P 188 greatly affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 188/propylene glycol (70%/30%)] with the melting point of about 32 degrees C was a solid form at room temperature and instantly melted at physiological temperature. The ratio of P 188/propylene glycol greatly affected the dissolution rates of clotrimazole from poloxamer-based suppository. Dissolution mechanism analysis showed the dissolution rate of clotrimazole from poloxamer-based suppositories was independent of the time. The clotrimazole-loaded suppository with P 188 and propylene glycol could not irritate or damage the rectal tissues of rats and gave the improved anti-tumor activity in a dose-dependent manner at mouse. Furthermore, its rectal administration decreased the hepatotoxicity compared to oral administration. Thus, the poloxamer-based solid suppository system with clotrimazole/P 188/propylene glycol was an effective rectal dosage form for the treatment of tumors with alleviated adverse effects.

Animals↗

PubMed1999

Effect of additives on the physicochemical properties of liquid suppository bases.

To investigate the effects of additives on the physicochemical properties of in situ gelling and mucoadhesive liquid suppository base, gelation temperature, gel strength and bioadhesive force of liquid suppository base, poloxamer 407 (P 407) and poloxamer 188 (P 188) (15/15%) were evaluated in the presence of following additives: solvent (ethanol, propylene glycol, glycerin), ionic strength-controlling agent (sodium chloride) and pH-controlling agent (hydrochloric acid, sodium monohydrogen phosphate, sodium dihydrogen phosphate). Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2-4 degrees C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. Taken together, these findings indicate that the effect of additives on the physicochemical properties of liquid suppository bases depends on their bonding capacities, in that additives such as sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate having strong cross-linking bonds with the components of liquid suppository base increase the strength and bioadhesive force of a gel compared to liquid suppository base alone, while additives such as ethanol, propylene glycol and hydrochloric acid having weaker hydrogen bonding result in a weaker response. Thus, sodium chloride and sodium phosphates appear to be promising additives for in situ gelling and mucoadhesive liquid suppository base, if used in adequate amounts.

Adhesiveness↗