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At least 235 records · Page 13Linked to original sources
PubMed1985

[Clinical studies of ceftizoxime suppositories in respiratory tract infections and urinary tract infections in children].

A fundamental and clinical study of ceftizoxime (CZX) suppositories was performed in pre-school and school-age children. The average time courses of CZX serum and urinary concentrations after administration of CZX suppository 250 mg (i.e. per kg body weight doses of 8.3-10.9 mg) to 4 school-age children were as follows. Serum concentrations: 6.1 micrograms/ml at 15 minutes, 6.3 micrograms/ml at 30 minutes, 3.8 micrograms/ml at 1 hour, 1.7 microgram/ml at 2 hours, 0.5 microgram/ml at 4 hours and 0.2 microgram/ml at 6 hours with a biological half-life of 1.43 hours. Urinary concentrations: 885 micrograms/ml for 0-2 hours, 209 micrograms/ml for 2-4 hours and 112 micrograms/ml for 4-6 hours with an average 6-hour urinary recovery rate of 25.6%. The clinical and biological effectiveness and adverse reactions were studied in 11 infants and school-age children afflicted with various infections (acute purulent tonsillitis, 1; acute bronchitis, 3; acute pneumonia, 4; and UTI, 3). The clinical responsiveness was "excellent" in 8, "good" in 2, and "failure" was recorded in 1, with an overall efficacy of 90.9% inclusive of "excellent" and "good". The microbiological effectiveness of CZX suppositories on presumed pathogenic organisms comprising 4 strains of H. influenzae, 1 strain of H. parainfluenzae, and 3 strains of E. coli was satisfactory, as evidenced by the substantially high eradication rate of 87.5%. The only organism that survived CZX suppository treatment was 1 strain of H. influenzae which however was greatly decreased. The only side effect was diarrhea in 1 patient, which however did not necessitate withdrawal of the drug. The only laboratory test abnormality was GOT and GPT elevation in 1 patient which was normalized within 8 days. In conclusion, CZX suppositories were found to be efficacious and safe for treatment of bacterial infections in children.

Bacteria↗
PubMed1984

[Results of combined therapy of irradiation and bleomycin suppository for advanced uterine cervical cancer].

Efficacy, survival rats and adverse effects of the combined therapy of irradiation with intravaginal bleomycin suppositories were analyzed and discussed in 49 patients with uterine cervical cancer. The results were as follows: Histological examination of biopsy specimens from the uterine cervix taken just after the completion of this treatment showed favorable control over the primary lesions. However, the efficacy of the bleomycin suppositories was too mild to form a basis for treatment without intracavitary irradiation. Because of the low concentration of bleomycin in serum after suppository administration, it is thought that bleomycin would have little effect on distant metastases. Survival rates in stage III patients were 83% at 12 months, 77% at 24 months and 70% at 36 months. These were superior to those for irradiation alone. The major adverse effect of bleomycin suppositories was fever, reduction of the bleomycin dose in each suppository but controlled this to some extent Lung fibrosis or severe damage to the liver, kidney and bone marrow were not found.

Adult↗
PubMed1984

In vitro release of meclozine hydrochloride from lipophilic suppository bases with or without tensides.

Meclozine hydrochloride suppositories were prepared with lipophilic bases, and the release rate of the drug from molten suppositories was investigated in vitro. Among various suppository bases, the highest rate was obtained when Witepsol H 15 was used. The release rates were affected if nonionic tensides (Tween 20 and 80) were incorporated. In comparison to the tensides-free suppositories, the rates obtained with suppositories containing 5, 20 and 30% of tensides were higher, approximately the same, and lower (respectively). The results were interpreted in terms of the micellar solubilization of the drug with nonionic tensides.

Animals↗
PubMed1984

Clinical pharmacokinetic comparison of two indometacin containing suppositories with different vehicula.

A single dose each of two brands of indometacin (INN; in some pharmacopoeias called indomethacin) containing suppositories, made with different vehicula , was administered rectally - in a cross over design - to ten healthy volunteers. Product A ( Dolcidium ) was made of a new waxy excipient which emulsifies at body temperature; product B was a leading brand of indometacin containing suppository, made of a hydrophilic polyethyleneglycol basis, which dissolves in body fluid. Plasma indometacin concentrations were measured frequently during a period of 9 h after dosing. Both products showed rather consistent absorption profiles. The maximum plasma indometacin concentration after administration of the product A 50 mg suppository was found after 62 +/- 18 min (mean +/- S.D.), and measured 2.0 +/- 0.5 mg X l-1. After dosing with the reference product those values were 66 +/- 21 min and 1.8 +/- 0.4 mg X l-1, respectively. The area under the plasma indometacin concentration-time curve was found to be 384 +/- 130 mg X l-1 X min for product A 50 mg suppositories and 372 +/- 62 mg X l-1 X min for the reference product. This results in a relative bioavailability of the product A 50 mg suppositories of 1.02, after correction for actual amount of indometacin in each dosage form. None of the above mentioned pharmacokinetic parameters were statistically significantly different (p greater than 0.05), indicating bioequivalence of the two products.

Adult↗
PubMedDate not supplied

Plasma concentrations following single doses of morphine sulfate in oral solution and rectal suppository.

Plasma concentrations of morphine and morphine-3-glucuronide (morphine's major metabolite) were determined following single 10-mg doses of morphine sulfate in oral solution and rectal suppository. Ten patients with pain secondary to cancer were given a single 10-mg dose of oral morphine sulfate in an oral solution or rectal suppository on sequential days. Blood samples were collected at time zero and periodically for 4.5 hours after administration. Plasma concentrations of morphine and morphine-3-glucuronide were determined using liquid chromatography with electrochemical detection. Higher mean concentrations of morphine were achieved with the rectal suppository than with the oral solution at all time points, and the overall mean plasma morphine concentration for the entire 4.5-hour period was significantly higher for the rectal suppository than for the oral solution. There were no significant differences between dosage forms in mean morphine-3-glucuronide concentrations at individual time points or over the entire period. A single dose of morphine sulfate in a rectal suppository was better absorbed than in an oral solution. Further studies are needed to compare the clinical efficacy of these dosage forms under steady-state conditions.

Administration, Oral↗
PubMed1982

[Evaluation of pre-operative chemotherapy using FT-207 suppositories combined with glutathione--with special reference to histopathological antitumor effect].

Thirty patients with gastric cancer were clinically studied by rectal administration of FT-207 suppository at a dose of 1500mg per day as a preoperative adjuvant chemotherapy. Eighteen of thirty patients were divided into two groups, 13 patients of which were only administrated with tegafur (FT-207) suppository (Group A) and 5 patients were administrated with glutathione (GSH) at a dose of 1200mg daily with FT-207 suppository (Group B): The tissue concentration of FT-207 and 5-FU in normal and cancer tissues was measured following the resection of the stomach. In addition, we studied anticancer effect of FT-207 suppository on the basis of our original pathological criteria. Experimental results revealed that 5-FU concentration in serum was reached to maximum at 3 to 4 hours following administration in both groups. The serum concentration in most cases of the former group was decreased to the lower level of the effective concentration for 8 hours, however the latter could be kept the effective concentration for more than 10 hours. The correlation between the tissue concentration and total dose was analyzed. 5-FU concentration, which was active substance of FT-207, in cancer tissue was higher than in normal one, especially in Borrmann II type cancer, but the difference of concentration was not found between group A and B. The correlation between total dose and anticancer effect was also analyzed. Histopathological effect in group A showed a mild change, such as necrosis of cancer nest. On the other hand, group B revealed a markedly effective change like scarring formation. As the result, administration of FT-207 suppository with GSH was clinically and histopathologically effective procedure as preoperative adjuvant chemotherapy.

Antineoplastic Agents↗
PubMed1982

Evaluation of aminophylline suppositories prepared in a hospital pharmacy.

Physical and chemical stability of suppositories containing aminophylline and various bases prepared in our hospital pharmacy was investigated. Ethylenediamine in aminophylline decreased, the melting points of the suppositories rose, and the disintegration and liquefaction times were prolonged in suppositories with Witepsol base when stored at room temperature. Thin-layer chromatography produced evidence supporting the assumption that ethylenediamine may react with Witepsol constituents to form an acid amide linkage. However, the suppositories were stable at lower temperatures. Suppositories prepared with PEG base were found to be satisfactorily stable at room temperature.

Aminophylline↗
PubMed1994

[Relative bioavailability of paracetamol in suppositories preparations in comparison to tablets].

Relative Bioavailability of Paracetamol as Suppositories Compared to Tablets. The relative bioavailability of paracetamol (CAS 103-90-2) in ben-u-ron 500 mg and ben-u-ron 1000 mg suppositories (test formulations) was compared with that of Benuron tablets 500 mg (reference product) in an open, intraindividual, 3-period-changeover-study in 18 healthy subjects. Plasma concentrations of paracetamol were determined using a specific and sensitive HPLC method with UV detection. For the assessment of bioavailability AUC, Cmax, tmax and HVD were used as pharmacokinetic characteristics. Bioequivalence of the rectal formulations was tested by calculating 90% confidence intervals using the Two-one-sided-t-tests-procedure and log-transformed data of AUC and Cmax. For AUC the confidence intervals were required to be in the 80 and 125% range, for Cmax between 70 and 143% (inclusion rule). Data from 17 subjects could be evaluated. Bioavailability of paracetamol was 89 and 90% for the 500 and 1000 mg suppositories, respectively compared with that of the 500 mg reference tablets. Mean maximum paracetamol plasma concentrations (Cmax) were 3.55 and 6.02 or 7.16 mg/l after administration of the 500 and 1000 mg suppositories or the 500 mg tablets, respectively. These maximum concentrations were achieved 2.0, 2.7 and 0.6 h (tmax) after administration of the respective preparations. The corresponding HVD values were 4.3, 5.2 and 2.0 h, respectively. After dose adjustment of the results for the 1000 mg suppositories relative bioavailabilities of paracetamol from both rectal formulations exceeded 80% of that from the tablets.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗
PubMed1994

[Acetaminophen-containing suppositories in vitro and in vivo].

Rectal suppositories with a paracetamol content of 300 mg were prepared and the optimal vehicle was searched for experimentally. 9 different kinds of lipophilic, lipohydrophilic and hydrophilic vehicles were used for this purpose. Research was focused on determining the factors influencing in vitro drug liberation. The suppository compositions which proved to be the best by the membrane diffusion method were tested by in vivo animal experiments with respect to their antipyretic effect. The in vitro and in vivo results were evaluated statistically and some of the suppository bases showed significant differences. In the authors' opinion the optimal vehicle for the preparation of paracetamol-containing suppositories is the Witepsol H 15 suppository base containing 10% Miglyol 812 (neutral oil).

Acetaminophen↗
PubMed2000

Topical treatment of vaginal candidosis with sertaconazole and econazole sustained-release suppositories.

OBJECTIVE: To compare the efficacy and safety of sertaconazole and econazole sustained-release suppositories in the treatment of vulvovaginal candidosis. STUDY DESIGN: 369 women with symptoms and signs of vulvovaginitis were enrolled in this multicenter, randomized, double-blind study. After clinical examination and vaginal sampling, 183 women were treated with a 300-mg sertaconazole suppository and the other 186 with a 150-mg econazole suppository. They were evaluated 1 week after treatment and those who were clinically uncured received a second suppository and were re-assessed 1 week later. All women were evaluated 1 month after the last administration. At each follow-up visit, clinical efficacy was assessed and a vaginal sampling was performed for microscopic examination and culture. RESULTS: Of the 369 women included, only the 310 who had a positive culture for a strain of Candida were taken into account for efficacy analysis: 150 in the sertaconazole group and 160 in the econazole group. One hundred and five women (49 in the sertaconazole group and 56 in the econazole group) were not clinically cured after 1 week and received a second suppository. There were no differences between the two groups for the rates of clinical recovery (disappearance of signs and symptoms) and mycological recovery (negative culture), 1 week after the first application (62.1 and 67.7%, respectively), 1 week after the second application for women treated twice (72.3 and 80.6%, respectively) and for all patients 1 month after the last application (65.3 and 62.0%, respectively). Among the patients cured 1 week after the last application, the mycological recurrence rate after 1 month was significantly higher in the econazole group (32.7 vs. 19.8%, P=0.035). There was a trend towards better efficacy of sertaconazole after the first application, whereas the two treatments had similar efficacy in women treated twice. There were no serious adverse events and only local irritation was reported, without any statistically significant difference between the two groups. CONCLUSION: Single topical administration of sertaconazole and econazole had similar efficacy and safety but the former is associated with a lower rate of mycological recurrence one month after achieving a negative culture.

Administration, Intravaginal↗
PubMed1994

Effect of suppository bases on the release properties of a potent antimicrobial agent (C31G).

C31G is a specific formulation which contains equal molar concentrations of alkyl N-betaine and alkyl N,N-dimethylamine oxide. Vaginal suppositories containing 500 mg of C31G, this potent antimicrobial substance, were prepared by the fusion method in a variety of Suppocire and Witepsol bases with different melting points and hydroxyl values. In vitro release and diffusion characteristics of C31G from different suppository bases were investigated using two different systems. The release from suppositories was determined by using a system without a membrane and the diffusion rate of the released agent was determined through a semipermeable dialyzing tubing. Diffusion kinetics from suppositories were evaluated in terms of the apparent dialytic rate constants using the equation developed by Davis et al. From the results of in vitro studies, Witepsol H15 and Suppocire CM bases were selected as the most suitable ones for the formulations of C31G vaginal suppositories, since it is imperative for topical formulations to release the active substance in high proportions which are not absorbable by the mucosal membranes.

Alkalies↗
PubMed1983

Methods to determine success of attempts to terminate early gestation pregnancies with prostaglandin vaginal suppositories.

One-hundred subjects received vaginal suppositories containing prostaglandin analogues in order to terminate their pregnancies of 49 days gestation or less. This non-surgical method was successful in 61 subjects, failed in 35 subjects and four subjects were lost to follow-up. Success of prostaglandin therapy cannot be predicted using pretreatment clinical parameters, pretreatment serum beta-hCG levels, or the passage of tissue from the vagina based upon history obtained from the subject. The passage of tissue histologically identified as of fetal origin is a definitive way to determine the success of pregnancy termination but the passage of tissue obtained by history is not. Of the 61 subjects in whom the prostaglandin suppositories were a success, 56 (92%) had a beta-hCG level day 7 +/- 2 following treatment which was 15% or less than the pretreatment value and 5 had beta-hCG levels which were more than 15% of the pretreatment value. All subjects with beta-hCG levels 5 to 9 days after the abortion that were less than 15% of the pretreatment concentrations had a successful termination. Of 35 subjects in whom the prostaglandin suppositories were unsuccessful, 26 had a beta-hCC level 7 +/- 2 days following treatment which was greater than the pretreatment level and 9 had beta-hCG levels less than the pretreatment value. The results of this study indicate that when prostaglandin vaginal suppositories are used to terminate early gestations, if there is no decline in beta-hCG levels 7 +/- 2 days following treatment, the pregnancy should be terminated by another method.

Abortion, Induced↗
PubMedDate not supplied

Pharmacokinetic characteristics of ketoprofen suppositories.

The pharmacokinetic profile of ketoprofen suppositories following single and chronic (32 doses) administration to 12 healthy adult male volunteers was established. Each subject received a single rectal dose of 100 mg of ketoprofen on day 1, followed by one suppository of 100 mg b.i.d. for days 8--22, and finally one suppository on day 23. Plasma samples were analysed by gas-liquid chromatography. Following single doses, the mean maximum observed concentrations of ketoprofen in plasma (6.56 microgram ml-1) were achieved at 1.1 h; the mean elimination half-life was 1.78 h. The results indicate that ketoprofen is rapidly and reproducibly absorbed and eliminated from the suppository dose form.

Adult↗
PubMedDate not supplied

A comparison of the effectiveness of Therevac SB and bisacodyl suppositories in SCI patients' bowel programs.

The evaluation described in this article compared the Therevac SB "mini-enema" with bisacodyl suppositories in the bowel management programs of patients with spinal cord injury (SCI). Of particular interest were (a) determining whether the additional costs of Therevac SB could be justified and (b) identifying the degree of bowel program improvement possible. Fourteen SCI patients were selected from the SCI inpatient unit and the clinic of a Department of Veterans Affairs facility. All patients experienced a delay of at least 45 minutes between insertion of a suppository and the beginning of stool evacuation. Each patient used bisacodyl suppositories for five bowel programs, then Therevac SB for five programs, finally repeating the bisacodyl suppositories for five more programs. Each patient maintained a bowel program log. Ten patients completed the evaluation. Using a MANOVA, the authors found a significant difference between bisacodyl and Therevac SB mean evacuation times for this group. An analysis of direct and indirect costs related to bowel care with the two regimens is also presented.

Adult↗
PubMed1979

Antipyretic effect of acetaminophen suppositories in rats.

An animal model used yeast-fevered rats to measure the relative antipyretic effects of different commercially available acetaminophen-containing suppositories. A laboratory-prepared acetaminophen-containing suppository and placebo suppositories also were investigated. Release from the suppositories was measured in vitro. All acetaminophen products containing 600 mg of drug elicited significant decreases in the rectal temperature of fever-induced rats.

Acetaminophen↗
PubMed1980

Decomposition of aminophylline in suppository formulations.

An aminophylline suppository product, when stored at room temperature, was found to be deficient in ethylenediamine content by the USP XIX assay and by a specific method for primary amines. The product also had a melting point that was considerably higher than body temperature. An accelerated decomposition experiment, conducted on normal suppositories of identical original composition, yielded a product refractory at steam bath temperatures and containing no ethylenediamine measurable by the USP assay. The suppositories from both the original sample and the decomposition experiment contained considerable amounts of a white material, which melted at similar to or approximately 150 degrees and which consisted of the diamide products formed by the reaction of ethylenediamine and the fatty acids present in coconut and palm kernel oils. The results, which confirmed the work of Cieszynski, showed that the ethylenediamine constituent of aminophylline can react with suppository base materials to produce insoluble amide decomposition products.

Amides↗
PubMed1982

Medicament release from suppository bases I: Physicochemical characteristics and bioavailability of indomethacin in rabbits.

This investigation was designed to determine the in vitro release of indomethacin from suppository bases and the in vivo bioavailability in rabbits. Suppositories containing 25 mg of indomethacin were made by the fusion method with theobroma oil, esterified fatty acids (C10-C18), and polyethylene glycol 1000. To produce an exact dosage form, a formula for the determination of the displacement value was derived, and it was found that theobroma oil greater than esterified fatty acids (C10-C18) greater than polyethylene glycol 1000. The suppository hardness was determined by using appropriate apparatus and it was found that the esterified fatty acids (C10-C18) allowed the formation of more brittle suppositories. The release rates were determined with the USP dissolution apparatus, with or without cellophane membrane, and it was found that polyethylene glycol 1000 greater than esterified fatty acids (C10-C18) greater than theobroma oil. The bioavailability of indomethacin after rectal administration was greater with polyethylene glycol base. Significant correlation was obtained during the first 45 min between the in vitro release (dialyzing tubing) and the in vivo bioavailability.

Animals↗
PubMed1981

Serum theophylline levels after use of an anhydrous crystalline theophylline suppository.

The absorption of theophylline from a suppository not containing ethylenediamine was tested in 9 healthy volunteers. AUC after rectal administration of anhydrous crystalline theophylline 250 mg (AUCrectal) was compared with the AUC after oral administration of microcrystalline theophylline 250 mg (Nuelin; AUCoral) in a randomized, cross-over study. The ratio AUCrectal/AUCoral was 0.75 at 10h, and the ratio AUCrectal x beta rectal/AUCoral x beta oral extrapolated to infinite time was 0.83. A mean concentration of 5.7 micrograms/ml was reached 3.7 h after a single rectal dose. The absorption studied were performed with suppositories stored for 15 weeks at 22 degrees C. No effect on the in vitro release rate of theophylline from the suppository was observed during storage at room temperature from 3 to 31 weeks after production. Since aminophylline suppositories are known to decompose upon storage, the results suggest that a formulation without ethylenediamine is preferable for the rectal administration of theophylline.

Administration, Oral↗