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At least 19 recordsLinked to original sources
PubMed1977

Pentazocine suppositories for post-operative pain: intramuscular pentazocine injections versus suppositories in a controlled trial in 588 patients.

A between-patient comparison of the analgesic effect of pentazocine 50 mg by suppository and 30--45 mg by intramuscular injection was made in 558 postoperative patients, 54% within 24 hours of operation. The suppositories proved acceptable overall, even though effectiveness was less at half an hour after administration (particularly in those patients with severe initial pain) and there was greater need for further analgesia at one hour. The cost of treatment with suppositories is less than with injections. After the suppositories there were half as many patients asleep at one hour than after injections, and fewer possible side-effects (7 compared to 24).

Adolescent↗
PubMed1992

Pharmaceutical characterization of corticosteroid suppository treatment for ulcerative colitis.

The dose and method of administration of a corticosteroid given for the treatment of patients with ulcerative colitis are determined according to the range of the diseased area and its severity. In this study, we prepared a hydrophilic suppository consisting of water-soluble prednisolone sodium succinate (PSL-SS) and a hydrophilic base, polyethylene glycol (PEG), and a hydrophobic suppository consisting of water-insoluble prednisolone (PSL) and a hydrophobic base, Witepsol (WT). We determined the spread of the drugs after intrarectal administration and their therapeutic effect. When rats received the hydrophilic suppository, the drug spread farther oral than when they received the hydrophobic suppository. Moreover, more than half of the PSL-SS recovered was observed to have changed into PSL. A therapeutic effect on the colitis induced in rats by acetic acid was noted in the area up to 10 cm from the anus in the case of the hydrophilic suppository, while the effect of the hydrophobic suppository was seen only in the area up to 2.5 cm from the anus. In patients with ulcerative colitis, the hydrophilic suppository showed retrograde spread to a site 34.4 +/- 5.3 cm from the anus, while the hydrophobic suppository spread to a site 19.0 +/- 2.4 cm from the anus. These results suggest that a hydrophobic suppository should be used for patients in whom inflammation is confined to the rectum, and a hydrophilic suppository used for patients in whom inflammation reaches the rectum and the middle part of the sigmoid colon.

Administration, Oral↗
PubMed1992

Prolonged release of morphine alkaloid from a lipophilic suppository base in vitro and in vivo.

The in vitro release characteristics of four suppository formulations of morphine (15 mg) were investigated using the USP rotating basket dissolution apparatus. Morphine hydrochloride in polyethylene glycol (PEG), a hydrophilic suppository base, morphine alkaloid in PEG and morphine hydrochloride in Novata BBC (a lipophilic suppository base) completely released the drug within 25 min whereas, morphine alkaloid in Novata BBC (MAN) released the drug over 10 h. The absorption of the morphine hydrochloride/PEG (MHP) suppository was compared with that of a 15 mg oral solution in eight patients with malignant disease in a crossover design. Time of peak plasma morphine concentration (tmax) was similar for both preparations (1.8 +/- 1.6 h and 1.2 +/- 0.5 h, respectively; p > 0.05), showing that the MHP suppository was rapidly absorbed. The MAN and MHP suppositories were then compared in a further nine patients in a crossover design. Prolonged release of morphine from the MAN suppository was also evident in vivo as tmax (2.5 +/- 1.4 h) was significantly greater than that for the morphine hydrochloride/PEG suppository (0.7 +/- 0.3 h; p < 0.002). There was no significant difference in AUC (0-7 h) (34.5 +/- 19.2 versus 38.9 +/- 16.1 ng.h/ml, respectively; p > 0.05) indicating a similar amount of morphine absorbed. Plasma morphine concentrations were more sustained for 7 h after dosage with the MAN suppository, with lower peak (8.3 +/- 4.9 and 12.3 +/- 6.6 ng/ml, respectively) and higher 6 h plasma morphine concentrations (5.81 +/- 4.85 and 3.30 +/- 1.0 ng/ml, respectively; p < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Rectal↗
PubMed1978

Pentobarbital absorption from capsules and suppositories in humans.

Serum pentobarbital levels following administration of the sodium salt as a 100-mg capsule orally and as two 120-mg suppository formulations (A and B) rectally were measured. From these data and previously determined kinetic constants after intravenous administration, the absorption rates and bioavailability of pentobarbital from each dosage form were determined. All three dosage forms were 100% absorbed. Peak serum pentobarbital levels occurred at 1, 4, and 10 hr for the capsule, Suppository A, and Suppository B, respectively. In vitro studies agreed with the serum data in that Suppository A released drug in an in vitro aqueous pH 1.4 system at a much greater rate that Suppository B. The capsule and Suppository A both appeared to be absorbed by simple first-order processes; however, Suppository B had a complex absorption pattern, which was modeled using sequential zero-order and first-order absorption.

Administration, Oral↗
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↗
PubMed1992

Bioavailability of morphine in rabbits after rectal administration of suppository containing controlled release morphine tablet.

Two kinds of sustained release morphine suppositories have been prepared; one is an oleaginous base suppository (MSC) containing a controlled release morphine tablet (MST: MS Contin), and the other is a hollow-type suppository (MSCH) containing MST and morphine powder packed in its hollow space. In vitro release tests and in vivo rectal absorption experiments in rabbits were performed. The profiles of morphine release from MST and MSC in vitro were similar, and revealed that suppository bases had no effect on the release profile of morphine from the preparation. Morphine release from MSCH was rapid in the early phase, and then enclosed morphine was slowly and continuously released from MST. Phamacokinetics of morphine from the suppository were compared with the orally administered MST, and it was found that there was no difference in the maximum plasma concentration (Cmax) and the peak time (Tmax) between MSC and MST, but the mean residence time (MRT) of MSC was approximately three times longer than that of MST, and the extent of bioavailability (BA) of MSC was significantly larger than that of MST (71.6 +/- 14.2% and 11.9 +/- 4.0%, respectively). Cmax can be altered arbitrarily by changing the morphine content in the hollow space of MSCH. As in the case of MSC, the plasma concentration of morphine from MSCH was maintained. It is concluded from the above results that MSC is a satisfactory sustained release morphine suppository for the treatment of cancer pain, administering it twice a day, and that MSCH is effective due to its fast analgesic effect and sustained release nature not only for cancer pain but also for surgical operations.

Administration, Rectal↗
PubMed1992

Absorption enhancement of polypeptide drugs by cyclodextrins. I. Enhanced rectal absorption of insulin from hollow-type suppositories containing insulin and cyclodextrins in rabbits.

The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and various amounts of each CyD in citric buffer solution at pH 3.0 or powder in its cavity, suppository II containing CyD without insulin, and suppository III containing insulin without CyD. Without CyD, the insulin and glucose levels in plasma were unchanged, whereas a significant increase in the plasma insulin concentration and a marked decrease in the glucose levels were found following simultaneous administration of insulin and CyDs by suppository I. The enhancing effect of CyD on rectal insulin absorption (absorption-enhancing effect) by chemically modified CyDs (heptakis(2,6-di-O-methyl)-beta-CyD (DM-beta-CyD) and 2-hydroxypropyl-beta-CyD (HP-beta-CyD)) was higher than those by natural CyDs (alpha-, beta-, and gamma-CyD). The area under the plasma concentration-time curve (AUC) and Cmax of insulin significantly decreased with the preadministration (administration of CyD 6, 24 and 48 h before rectal insulin administration) of DM-beta-CyD. The absorption-enhancing effect disappeared 24 h after preadministration. These results suggest that CyDs enhance insulin absorption from the rectum, and that attenuation of the membrane transport barrier function in the rectum recovers at a maximum of 24 h after administration of CyDs.

Absorption↗
PubMed1992

In vivo and in vitro release of indomethacin from water-soluble and fatty base suppositories.

The plasma concentration of indomethacin was measured after the rectal administration of water-soluble and fatty base suppositories in rats. The results were compared with the in vitro indomethacin release from suppositories determined by Paddle method using three different types of membranes: cellulose membrane, artificial sausage membrane and natural sausage membrane. The plasma concentrations of indomethacin during the first 4h after the rectal administration were higher in rats that received water-soluble base suppositories than in those that received fatty base types. When either a cellulose membrane or an artificial sausage membrane of cow protein was used in the Paddle method, the amount of indomethacin released from fatty base suppositories was significantly higher than that from water-soluble base ones. However, the results were reversed when a natural sausage membrane of pig colon was used. The discrepancy in the in vitro experiments using water-soluble base suppositories seemed to be due to the difference of pore size of membrane used. Careful consideration should be given to the membrane used in the Paddle method especially when this method is employed to examine the release of poorly soluble drugs like indomethacin in both water-soluble and fatty base suppositories.

Animals↗
PubMed1992

Cervical ripening: a randomized study comparing prostaglandin E2 gel to prostaglandin E2 suppositories.

Prostaglandin (PG) E2 has proven effective in many studies as a pre-induction agent for cervical ripening. The purpose of this study was to compare the efficacy of a 5-mg dose of PGE2 prepared gel with that of a quartered PGE2 20-mg suppository. Previous studies have documented uniform distribution of PGE2 in the suppository. After 90 patients entered the study, there appeared to be an unacceptable rate of hyperstimulation following the induction dose using the suppository. The study was discontinued, and data analysis revealed a 24% hyperstimulation rate with the quartered suppository versus 0% with the gel. The successful vaginal delivery rates were equivalent, at 75% for the gel and 66% for the suppository. The 5-mg quartered suppository appeared to initiate an unacceptable amount of uterine activity, much greater than with the 5-mg gel dose.

Administration, Intravaginal↗
PubMed1992

Allergy to lysozyme/egg white-containing vaginal suppositories.

Seven patients who received a lysozyme, nystatin, and tetracycline containing vaginal suppository because of suspected vaginal infection, developed local or systemic allergic reactions. The coincidence of the symptoms with the repeated use of the suppository as well as skin and lymphocyte transformation tests indicated that the lysozyme in the suppository was responsible for the allergic reactions. This lysozyme preparation contained additional egg proteins, which contributed to the allergic reaction in certain patients: three patients with a previous history of egg allergy and serologic and/or skin test evidence for egg-white sensitization developed the allergic reaction after the first suppository. Four patients had urticaria or anaphylaxis after treatment for at least three days; none of these four patients developed egg allergy. Five of seven individuals had positive skin tests (prick or scratch) to ovomucoid and lysozyme, but none of the patients had lysozyme-specific IgE in the circulation. All seven patients, with or without egg allergy, showed vigorous T cell responses to purified lysozyme and partly to other egg-white proteins in the lymphocyte transformation test, which was absent in controls. Vaginal suppositories that contain lysozyme and other contaminating egg white proteins can either elicit allergic reactions in patients with a preexisting egg white allergy or induce sensitization to lysozyme and other egg white components.

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↗
PubMed1975

Reduction of cervical resistance by prostaglandin suppositories prior to dilatation for induced abortion.

Several recent reports citing increased rates of prematurity among women who have had induced first-trimester abortion suggest that forceful cervical dilatation may result in cervical incompetence in future pregnancy. There appear to be conflicting clinical impressions regarding the effectiveness on cervical softening and the reduction of cervical resistance produced by various prostaglandins. The development of the Electronic Force Monitor which is capable of precise measurement of the forces encountered in overcoming resistance during dilatation provided objective evidence with which to evaluate the effects of vaginally administered prostaglandin E2 and F2alpha suppositories. Suppositories were administered 3 hours prior to cervical dilatation, after which suction curettage was performed. Compared to the nonmedicated control group, patients receiving PGF2alpha suppositories exhibited greatly reduced cervical resistance, in some cases permitting direct introduction of the suction curette without need for any preliminary dilatation. Those patients receiving PGE2 suppositories showed an intermediate degree of cervical softening.

Abortion, Induced↗