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At least 307 records · Page 17Linked to original sources
PubMed1986

Studies on improvement of pharmaceutical preparations prescribed in hospitals. V. Nifedipine hollow type suppository.

Nifedipine is a calcium antagonist used for the treatment of hypertension and angina pectoris. However, commercial nifedipine preparations are only available in forms suitable for oral administration, e.g. soft capsules and tablets. Therefore, we developed a suppository form in which the drug was incorporated into a hollow type suppository. The suppository preparation was administered to humans for evaluation of the clinical and commercial usefulness. It was as fast-acting as the soft capsule, but the blood concentration of nifedipine immediately after administration was lower than that seen with the soft capsule. It was considered to be superior to the soft capsule and similar to the tablet in terms of its long-acting effect. Thus, the hollow type suppository form of nifedipine should have useful clinical applications.

Adult↗
PubMed1987

New modes of administration of salmon calcitonin in Paget's disease. Nasal spray and suppository.

In volunteers the activity of various doses of a nasal spray and of a suppository of salmon calcitonin was compared to a placebo and to the parenteral route of administration. Both new modes of administration were found to be active on the kidney (and the suppository was found to affect bone turnover as well). The parenteral route proved more effective, but the nasal and/or rectal routes were devoid of systemic side effects and had minimal local intolerance. The nasal spray was used at 200 units daily in 15 patients with Paget's disease, and at 400 units daily in another nine patients, both trials lasting one year. The two regimens proved active on the parameters of bone turnover and the higher dose was more effective than the lower one. Similarly, a 300 unit suppository was given to another 12 patients. This trial is still being completed at this time. At the third month of therapy, the parameters of bone turnover were significantly depressed. Both new modes of therapy were able to improve the focal bone balance of the osteolytic lesions monitored on sequential roentgenograms. Systemic side effects were absent and local side effects were minimal. Only one patient interrupted the nasal spray therapy, and no one interrupted the suppository therapy.

Administration, Inhalation↗
PubMed1985

[Basic and clinical studies of ceftizoxime suppositories in the pediatric field].

Pharmacokinetic and clinical studies of ceftizoxime suppository (CZX-S) were performed in 10 children with the following results. CZX-S attained a peak serum concentration of 6.85 micrograms/ml 30 minutes after dosing with the drug 5.6 mg/kg (one suppository of CZX-S contains 250 mg of CZX in potency). The mean 6-hour urinary excretion rate in 4 children was 18.9%. The subjects consisted of 8 patients comprising 1 with pharyngitis, 3 with tonsillitis, 1 with gingivitis and 3 with urinary tract infection. The overall effect of CZX-S was "excellent" in 5 patients and "good" in 3, with an effectiveness rate of 100%. No side effects ascribable to CZX-S were encountered in any of the patients. A few patients complained of discomfort after the first or second insertion of the drug. However, the discharge of the suppository was as infrequent as 1.5% of the total 133 insertions. CZX-S is therefore well tolerated for clinical use in children. It is concluded that the unique suppository formulation of CZX-S is useful in the treatment of infections in children with heavy psychophysiologic disorders and in children who cannot take oral drugs because of severe vomiting.

Bacteria↗
PubMed1984

Biopharmaceutical investigations of rectal suppositories. Part 1: Pharmaceutical and biological availability of theophylline.

The influence of suppository base and some tensides on the release and resorption of theophylline from model rectal suppositories was investigated in a preliminary way. It was established that the original Bulgarian suppository base Novosup ensures higher pharmaceutical and biological availability of theophylline in comparison with other investigated lipophilic bases. The preliminary inclusion of Tween 80 in Witepsol H 15 increased the pharmaceutical and biological availability of the drug. A linear relationship between the pharmaceutical and biological availability was observed after administration of model suppositories in rabbits.

Animals↗
PubMed1983

Bioavailability of naproxen tablets and suppositories in steady state.

Serum profiles were obtained from patients with rheumatoid arthritis after treatment with naproxen tablets and suppositories for 10 days to assure steady state conditions. The serum concentrations immediately before dose intake correlated well with the area under the concentration curve (AUC) when 250 mg naproxen tablets were taken 12-hourly (r = 0.85) and when 500 mg naproxen was given as tablets or as suppositories once daily in the evening (r = 0.83). These fixed times for blood samplings should be used in clinical trials with naproxen. Naproxen was measured by mass fragmentography. The mean steady state concentration and the mean half-life, calculated from the 12-hourly dosage schedule, were 45.0 +/- 1.7 mg/l and 15.2 +/- 1.4 hours, respectively. Doubling the dose from 250 mg to 500 mg b.i.d. increased the AUC by 30%. Average serum profiles for tablets and suppositories were very similar and gave a relative bioavailability of suppositories compared to tablets of 103% +/- 4%, suggesting comparable efficacy of the two administration forms.

Adult↗
PubMed1984

Cervical ripening with prostaglandin E2 vaginal suppositories.

A prospective, randomized, double-blind, placebo-controlled study was undertaken to evaluate the safety and efficacy of a 3-mg prostaglandin E2 (PGE2) vaginal suppository for the initiation of cervical ripening before the induction of labor. All patients were required to have an initial Bishop score of 4 or les. The 3-mg PGE2 vaginal suppository was found to be an effective method of both cervical ripening and labor induction. Its use resulted in a highly significant improvement in the mean Bishop score compared with the placebo group (2.67 versus 0.55 points, P less than .00005). Its use also resulted in a significant reduction in the number of failed inductions (5 versus 23%, P less than .0005). Moreover, 68% of the patients treated with PGE2 labored after initial suppository placement, and 42% of these patients never required oxytocin augmentation of labor. However, there were three instances of uterine hyperstimulation/hypertonus following placement of the 3-mg PGE2 suppository, suggesting that perhaps a lower dose of PGE2 would improve its safety as a ripening agent without affecting its efficacy.

Adult↗
PubMed1984

Induction of labor with prostaglandin E2 vaginal suppositories.

A prospective randomized study of 85 parturients was undertaken comparing the safety and efficacy of a 3-mg prostaglandin E2 vaginal suppository with intravenous oxytocin for the induction of labor. All patients were required to have a Bishop's score of 5 or higher. Labor was successfully induced in 98% of the patients in both groups by their respective methods. Sixty-four percent of the patients receiving a 3-mg prostaglandin E2 suppository required no intravenous oxytocin. More specifically, 82% (23/28) of the parous patients but only 29% (5/17) of the nulliparous patients who received a single 3-mg prostaglandin E2 suppository for labor induction did not require oxytocin augmentation (P less than .005). The first and second stages of labor were not significantly different for the two groups, and there was no significant difference in the incidence of cesarean section. A 3-mg prostaglandin E2 vaginal suppository may be a useful alternative to oxytocin for the induction of labor in carefully selected patients.

Adult↗
PubMed1983

[Experimental and clinical evaluation of an ampicillin suppository (KS-R1) in children].

Plasma levels of ampicillin (ABPC) after the single rectal insertion of KS-R1 at doses of 125 and 250 mg in 154 children reached a peak at 11 approximately 15 minutes in children of age less than 1 year old, at 16 approximately 20 minutes in children of 1 approximately 3 years, 4 approximately 6 years and more than 7 years old with the highest levels of 11.50, 8.69, 10.33 and 8.30 micrograms/ml, respectively. Highest plasma levels of ABPC were 6.48, 8.00, 12.32 and 17.83 micrograms/ml by the administration of KS-R1 at doses of less than 10.9 mg/kg, 11.0 approximately 15.9, 16.0 approximately 20.9 mg/kg and more than 21.0 mg/kg, respectively, with dose-dependent response which were observed at 11 approximately 15 minutes or 16 approximately 20 minutes. There was no difference of plasma levels between the administration of 125 and 250 mg of KS-R1. The pain of insertion was observed in 0.6% of total 167 cases, the feeling of defecation in 2.4% and the discharge of suppository or its dissolved material or defecation within 30 minutes after insertion in 12.6%, without the influence of patients ages and dosage level. These figures were almost the same as those after the insertion of other suppositories such as erythromycin suppository or antipyretic suppository. Clinical effectiveness of KS-R1 was examined in 51 childish patients with various infections. KS-R1 was rectally given to them at doses of average 41.6 mg/kg/day divided into 3 to 4 times for 7 days. All cases showed excellent and good effects. Bacteriologically, all pathogens which were isolated from 12 patients were eradicated.

Age Factors↗
PubMed1995

[Synthetic salmon calcitonin suppositories for the short-term treatment of involutive osteoporosis].

Intramuscular and intranasal synthetic salmon calcitonin (sCT) has long been used in the treatment of involutional osteoporosis. A new suppository formulation was developed and many studies demonstrated that rectally administered sCT is efficacious and well tolerated. Thirty postmenopausal women, who had a bone mineral density at the lumbar spine below the mean of age-matched women, were enrolled in this study. Using an open balanced, randomized design, the patients were allocated to two groups of treatment: sCT suppositories at the dose of 100 UI/day or 200 UI every other day for six months. Treatment with sCT suppositories caused a statistically significant decrease of pain in both study groups. Bone mineral density at lumbar spine showed an increase in both study groups with significant difference respect the basal value for the patients treated with sCT on alternate day. Based on the results of this study, we can thus conclude that sCT in suppository formulation is effective in reducing pain sintomatology, bone loss and turnover in involutional osteoporosis.

Aged↗
PubMed1995

[Production technology and in vitro study of rectal suppositories containing chloroquine phosphate].

Chloroquine-phosphate was suspended in various lipophilic and hydrophilic suppository bases in an amount of 250 mg/2.0 g. The authors studied the solidity and the disintegration time of the suppositories as well as the in vitro drug liberation with a membrane diffusion method. The effect of the storage time and the storage circumstances on the stability of the suppositories was observed. Tropics-resistance studies were also carried out at a temperature of 45 degrees C and at a relative humidity content of 75%, thus these suppositories may be used for the treatment of malaria. The Witepsol H 15 base was found to be the best in all respect for use in countries with a continental climate. Finally a function relationship was found between the concentration of the pharmacon and the diffusion time with linear regression analysis.

Antimalarials↗
PubMed1994

[Double-blind placebo-controlled study of the effectiveness and tolerability of 10 and 30 mg ketorolac tromethamine suppositories in post-cholecystectomy pain].

OBJECTIVE: To evaluate the efficacy and tolerability of ketorolac tromethamine 10 mg and 30 mg suppositories in comparison to placebo, after single dose administration in patients suffering from post-operative pain after cholecystectomy. DESIGN: Double-blind, randomized, controlled study. SETTING: Anaesthesia Service. PATIENTS: 99 patients with severe pain following surgery. INTERVENTIONS: Cholecystectomy. MEASUREMENTS AND MAIN RESULTS: The analgesia activity of ketorolac tromethamine 10 mg and 30 mg suppositories were evaluated after single dose administration by assessing pain intensity and pain relief using a 4 point scale (VRS). At the end of the treatment period overall assessment of safety and efficacy were recorded by physician and patient. The results show that in both active groups after 30' and until 4 hours, pain intensity decreased significantly with respect to the baseline. However a statistically significant difference between groups of p < 0.02, p < 0.01 and p < 0.05 was found in favour of the 30 mg dose respectively at 30', 6 and 8 hours after administration. All the patients treated with placebo suppositories required another rescue analgesic drug and withdrew from the trial. Three patients complained adverse events not related to treatment: two on placebo and one on ketorolac 10 mg. The systemic and local tolerability of the drug was good. CONCLUSIONS: This study shows that ketorolac 30 mg suppositories are effective in clinical conditions, such as after surgery, in which pain control must be achieved within the shortest time interval and maintained or improved by means of a single route of administration.

Adult↗
PubMed1994

[Study of administration of buprenorphine suppository for postoperative pain relief following transvaginal hysterectomy].

Buprenorphine suppository (BSP) has been available as an analgesic agent in Japan since 1990. It has gained considerable popularity in various clinical situations; however, its usefulness for postoperative pain relief has been controversial. The present study is addressed to postoperative pain in fifty-seven women who underwent transvaginal hysterectomy under spinal anesthesia with tetracaine and phenylephrine. We examined the analgesic effects of buprenorphine (0.4 mg) suppository. Patients were divided into four groups according to the timing of buprenorphine suppository administration: group A1, preoperative administration of BSP, n = 12; group A2, postoperative administration of BSP, n = 17; group A3, intravenous injection of 0.1 mg of buprenorphine during surgery and postoperative administration of BSP, n = 14; group C, control group, n = 14. All the patients in group C complained of pain within 24 hr. The onset time of pain after surgery was significantly longer in patients in group A1 (372 +/- 220 min) and A3 (481 +/- 161 min) than in control group C (282 +/- 97 min). The percentage of patients who did not complain of pain within 24 hr was the largest in group A3 (36%). However there were no significant differences in age, body weight, effective analgesic time, analgesic level or operation time among the four groups. Nausea and vomiting were observed in all groups: C (36%), A1 (41%), A2 (18%), and A3 (29%). From these results, we conclude that preoperative or intraoperative administration of buprenorphine is useful for control of postoperative pain; the method of administration of buprenorphine suppository needs further study.

Adult↗
PubMed1993

Comparative pharmacokinetic evaluation of compressed naproxen suppositories in humans.

Compressed naproxen (CAS 22204-53-1) suppositories (250 mg) were formulated by dispersing the drug in molten polyethylene glycol 4000 followed by congealing and pulverizing the mass into granules and then compressing into suppositories. Their pharmacokinetic performance was evaluated and compared with that of a standard naproxen tablet in 12 healthy human volunteers. There were no statistically significant (p > 0.05) differences in Cmax, tmax, t1/2, AUC and mean residence time (MRT) observed after oral and rectal administration of tablet and suppository, respectively. The relative rectal bioavailability of naproxen from the compressed suppositories was 96.7 +/- 2.6%. Pharmacokinetics of naproxen after oral and rectal administration was highly comparable.

Adult↗
PubMed1993

[Postoperative pain relief by preanesthetic administration of buprenorphine suppository in elective mastectomy].

Seventy female patients scheduled for elective mastectomy were divided into three groups: Buprenorphine suppository (BPS) 0.4 mg group (n = 29); BPS 0.2 mg (n = 23) group; and control (scopolia extract and tannic acid suppository) group (n = 18). Suppositories were administered rectally to patients of each group one hour before induction of anesthesia. Plasma buprenorphine concentrations, sedation scores at entering the operating room, postoperative pain scores and side effects were evaluated. There were no significant differences in sedation effects of suppository among the three groups. Although there were significant differences in pain scores except at the time when patients left the operating room between BPS 0.2 mg group and the control group, postoperative pain relief in BPS 0.2 mg group was judged not enough. However, postoperative pain relief was more satisfactory in the BPS 0.4 mg group. Plasma concentrations of the BPS 0.4 mg group were higher than those of the BPS 0.2 mg group. Although nausea and vomiting were observed in 5 patients (17.2%) of the BPS 0.4 mg group and 4 patients (17.4%) of the BPS 0.2 mg group, respiratory depression and changes in blood pressure and heart rate were not observed in all groups. In conclusion, preanesthetic administration of the BPS 0.4 mg seemed to be useful for postoperative pain relief after elective mastectomy.

Adolescent↗
PubMedDate not supplied

Sumatriptan suppositories for the acute treatment of migraine. S2B351 Study Group.

A randomised, double-blind, parallel-group, placebo-controlled trial was undertaken to assess the efficacy and tolerability of the sumatriptan suppository in 184 patients with acute migraine. Patients used a sumatriptan suppository (12.5 mg or 25 mg) or placebo at home for the treatment of a moderate or severe migraine attack and those who experienced headache recurrence within 24 hours of dosing had the option to repeat the dose. By 2 hours post-dose, 68% of patients in the sumatriptan 25 mg group and 47% of patients in the sumatriptan 12.5 mg group compared with 25% of placebo patients achieved headache relief. Relief rates 2 hours post-dose for nausea, vomiting, photophobia and phonophobia were similar to those reported 2 hours post-dose for headache. Post hoc review of the recurrence data showed that administration of a second suppository was effective in alleviating recurrent headache in over 80% of the sumatriptan-treated patients experiencing recurrence. No serious or unusual adverse events were reported, and the pattern and incidence of adverse events did not vary as a function of dose. These data demonstrate that the sumatriptan suppository is a well-tolerated, effective treatment for the acute treatment of migraine pain and its associated symptoms.

Administration, Rectal↗
PubMed1998

Pharmacokinetics of tramadol and bioavailability of enteral tramadol formulations. 3rd Communication: suppositories.

The pharmacokinetics and the absolute bioavailability of tramadol hydrochloride (CAS 36282-47-0) after rectal administration of tramadol suppositories (Tramal) were determined in a balanced crossover study in 10 female volunteers in comparison with the intravenous injection. Each fasting volunteer received two single doses of 100 mg tramadol-HCl, one rectally (1 suppository) and one intravenously (2 ml of a solution for injection). The formulations were administered in the morning, the washout period was one week. Serum concentrations of tramadol-HCl were determined by gas chromatography-mass spectrometry and the pharmacokinetic evaluation was carried out model-dependently. Only the extent of bioavailability was calculated model-independently. The extent of the absolute bioavailability (F) of tramadol in the suppositories, based on AUC data, was 77.0% (point estimate; n = 10) with a 95% confidence interval of 70.8-83.6% (ANOVAlog). The areas under the serum concentration curves of tramadol-HCl calculated by curve fitting (AUC), which agreed very well with the model-independently determined areas (AUC), were 2933 +/- 304 h.ng/ml (rectal) and 3775 +/- 446 h.ng/ml (i.v.) [mean +/- SD; n = 10]. Optimal curve fitting of the serum concentration data after rectal administration presupposed the existence of two absorption sites with different absorption rates and lag times. Under this premise the absorption half-lives were t1/2,ka;1 = 1.7 h (median; range: 1.1-3.1 h) and t1/2,ka;2 = 0.98 h (0.35-1.9 h), and the corresponding lag times were t0;1 = 0 h (0-0.37 h) and t0;2 = 0.66 h (0.31-3.5 h). The relative portion of the more rapidly absorbed quantity of tramadol varied between 9.2 and 50% (median: 28%). The maxima of the serum concentration curves were reached 2-6 h after rectal administration; the means of the individual maxima were 294 +/- 50 ng/ml (Cmax) and 3.3 +/- 1.3 h (tmax). There were large differences in the distribution rate between the volunteers. The means of the half-life of the slower distribution (t1/2, alpha) were 1.38 +/- 0.47 h (rectal; n = 10) and 1.78 +/- 0.63 h (i.v.; n = 7). In the terminal phase the biological half-life (t1/2, beta) was 5.7 +/- 1.0 h (rectal) and 5.7 +/- 0.9 h (i.v.), respectively. The values determined after i.v. injection for the total distribution volume and the total clearance were 216 +/- 231 (Vd, beta) and 447 +/- 56 ml/min (Cltot). The results show that after rectal administration of the tramadol suppositories the absorption of the active ingredient is rapid enough for therapeutic purposes and that the extent of the absolute bioavailability is higher than after oral administration of tramadol-HCl, probably due to a reduced first-pass metabolisation after rectal administration.

Adult↗
PubMed1987

Prostaglandin E2 vaginal suppository for induction of labour: an efficient, safe and popular method.

Two different methods for induction of labour were randomly used in 100 women with a favourable cervix. The patients were treated with either prostaglandin vaginal suppositories containing 2.5 mg PGE2 in a base of Witepsol S55 (Dynamit Nobel) or intravenous infusion of oxytocin. The PGE2 vaginal suppository was significantly more efficient than the intravenous infusion of oxytocin in relation to the time interval from the start of induction of labour to delivery. Also the percentage of women who delivered within 48 hours (success rate) was higher in the suppository group. Significantly more women in the suppository group found this induction method recommendable.

Dinoprostone↗
PubMed1994

Formulation and in vitro study of antibacterial vaginal suppositories.

Vaginal suppositories frequently used in gynaecological therapy were studied. Several antibacterial pharmacons are used for the topical treatment of vaginitis of various origins. In view of the fact that the liberation of the given active substance and the subsequent therapeutic effect may be improved or inhibited by the vehicle, our aim was to find the optimal suppository base for vaginal suppositories containing sulfadimidine, chloramphenicol and gentamicin sulfate by means of in vitro experiments. On the basis of breaking hardness, disintegration time and spreading properties the French Suppocire NA product, and compositions of macrogols with lower molecular weight proved to be the best lipophilic and hydrophilic bases, respectively. Among the lipophilic bases the in vitro drug liberation of Suppocire NA was significantly better (P < 0.05) than the other lipophilic bases. This vehicle is recommended for the topical treatment of vaginitis, as these suppositories have the further advantage that they can easily be produced on a magistral, galenical or industrial scale as well.

Anti-Infective Agents, Local↗