Administration Of Suppositories Research Articles

Diclofenac suppository administration in conjunction with lidocaine gel during transrectal ultrasound-guided prostate biopsy: Prospective, randomized, placebo-controlled study

Objectives To evaluate the additional analgesic efficacy of the rectal administration of diclofenac suppository compared with placebo in patients undergoing transrectal ultrasound-guided prostate biopsy. Methods A total of 40 consecutive men undergoing biopsy were enrolled in this study. Patients were randomized equally into two treatment groups. In group 1, patients received an intrarectal 100-mg diclofenac suppository 1 hour before biopsy. In group 2, patients received a glycerin suppository as a placebo intrarectally 1 hour before biopsy. All patients received 10 mL of 2% lidocaine gel intrarectally 10 minutes before biopsy. A self-administrated visual analog scale was used to measure the pain scores at the end of the biopsy and 2 hours and 1 day after the biopsy. Results The mean patient age was 63.3 ± 6.8 years and 61.6 ± 6.7 years in groups 1 and 2, respectively. The mean pain score in groups 1 and 2 was 3.4 ± 1.3 versus 5.9 ± 1.7 ( P <0.0001), respectively, at the end of the biopsy. The mean pain score at 2 hours and 1 day after the procedure was 1.2 ± 1.0 versus 3.6 ± 1.4 ( P <0.0001) and 0.5 ± 0.9 versus 1.4 ± 1.3 ( P = 0.017) in groups 1 and 2, respectively. Conclusions Intrarectal diclofenac suppository administration is a simple, safe, and effective procedure to reduce pain and improve patients’ tolerance of transrectal ultrasound-guided prostate biopsy. We recommend intrarectal diclofenac suppository administration, together with intrarectally administered lidocaine gel, in men undergoing transrectal ultrasound-guided prostate biopsy.

Famotidine prevents canine gastric blood flow reduction by NSAIDs

To investigate the effect of famotidine on gastric blood flow reduction induced by diclofenac sodium, a common non-steroidal anti-inflammatory drug in Japan, using laser Doppler flowmetry in the canine stomach. The gastric mucosal blood flow was measured by laser Doppler flowmetry in 15 healthy male beagles before and 60 min after the administration of diclofenac suppository (1.0 mg/kg) into the rectum. The examination was done in a crossover, single-blinded fashion. All dogs underwent both famotidine (0.5 mg/kg) and placebo (saline) injection simultaneously with the administration of diclofenac. In addition, the tissue concentration of prostaglandin E2 was measured. The blood flow decreased by 18.3 +/- 9.1% in the gastric body, by 26.3 +/- 8.1% in the antrum in the placebo group after the administration of diclofenac sodium, while the decreases seen were significantly smaller in the famotidine group: 3.2 +/- 12.6% in the gastric body and 7.9 +/- 16.5% in the antrum (P = 0.001 for the gastric body, P = 0.0034 for the antrum). Conversely, the percentage of mucosal prostaglandin E2 concentration decrease in each group did not show a significant difference. Famotidine alleviates the reduction of gastric blood flow induced by diclofenac sodium. Further, not only mucosal prostaglandins but also gastric acid may play an important role in non-steroidal anti-inflammatory drugs-induced gastric microcirculatory disturbance.

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

To investigate the treatment and mechanism of compound carraghenates suppository to rat acute rectal mucous injury. 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. 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. 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.

437Diclofenac suppository administration during transrectal ultrasound guided prostate biopsy: A randomized, placebo-controlled study

437Diclofenac suppository administration during transrectal ultrasound guided prostate biopsy: A randomized, placebo-controlled study

Time and economic cost of constipation care in nursing homes.

Chronic constipation is a common disorder among residents in long-term care; yet the cost to the nursing home of constipation-related care is not known. The objective of this study was to quantify the nursing staff and supply-related cost of constipation care to nursing homes from the perspective of the nursing home. Prospective, observational time-and-motion design. Two United States nursing homes. A total of 59 nursing home residents with chronic constipation and nursing staff providing constipation care to them. Actual time to complete constipation care-related tasks was measured via stopwatch by trained observers, and the number and professional level (eg, staff nurse, CNA) of staff performing each task was recorded. Frequency of constipation care task data was obtained through 60-day retrospective medical chart review for each subject. Nurse wage rate data was obtained from the Nursing Home Salary and Benefits Report, a US-based national source. Resident and nursing home descriptive information was also collected. The average cost per task occurrence ranged from 0.72 US dollars for enema administration to 1.74 US dollars for oral medication administration. Average nursing staff costs per subject per year were 1577 US dollars for oral medication administration, 215 US dollars for dietary supplement administration, 39 US dollars for constipation assessment, 17 US dollars for suppository administration, and 6 US dollars for enema administration. Based on estimates of frequency of occurrence, the total annual labor and supply cost per long-term care resident with constipation was 2253 US dollars. Nursing staff performance of constipation care-related tasks is time consuming and costly in the long-term care setting.

Cannabinoids for Therapeutic Use

The two main modes of cannabinoid administration, oral ingestion of tetrahydrocannabinol (THC) and smoking of dry cannabis plant material, both have specific advantages and disadvantages. Disadvantages of oral ingestion include slow and erratic absorption, delayed onset of action and low systemic bioavailability, whereas disadvantages of smoking include mucosal damage and short duration of effect. In recent years several new modes of cannabinoid delivery have been tested. Alternative routes of systemic pulmonary administration include inhalation with a vaporizer and the use of cannabinoids in aerosol form. They avoid or reduce the formation of carcinogenic combustion products found in cannabis smoke. Sublingual (buccal) administration of liquid cannabis extracts has been tested in clinical trials in the UK. This mode is easy to administer and might enable easier dose titration than oral capsules. Transdermal delivery achieves a sustained and steadier action than inhalation or oral administration of THC, and is being investigated in preclinical studies by groups in the US and Israel. Use of ethosomal carriers has been shown to enhance skin permeation by the lipophilic cannabinoids. Rectal administration of THC-hemisuccinate suppositories has been tested in some patients; systemic bioavailability is twice as high as with oral administration because of the reduced first-pass effect. Water-soluble agonists to the cannabinoid receptor that allow intravenous administration have been developed. Dexanabinol, a non-psychotropic neuroprotective cannabinoid derivative, was given intravenously in clinical studies to decrease the consequences of severe closed head injuries. Increasing water solubility, for example by the use of cyclodextrin technology, also improved the possibilities of topical cannabinoid administration to the eye for glaucoma treatment. Several of these new approaches to cannabinoid delivery now under preclinical and clinical investigation may find their way into clinical practice within a few years.

Effects of Qianlie’an suppository in patients with chronic prostatitis syndrome: A randomized open-labelled prospective and controlled trial

Objective: To evaluate the clinical efficacy of Qianlie’an (QLA) suppository via anal route administration in treating chronic prostatitis syndrome.Methods: A randomized open-labelled prospective controlled trial was carried out. The total of 120 patients with chronic prostatitis syndrome were randomly divided into 2 groups: 60 patients in the treated group who were treated with QLA suppository combined with ofloxacin, and the other 60 patients in the control group who were given ofloxacin alone. The efficacy was evaluated by WBC count in the expressed prostatic secretion (EPS) and the Chronic Prostatitis Symptom Index (CPSI) made by the National Institute of Health (NIH). The clinical effects were also observed in a 4-week follow-up.Results: All but six cases completed the trial and the follow-up. It showed that in the treated group recovery rate was 17. 2%, markedly effective rate 34. 5%, effective rate 32. 8%, total markedly effective rate 51. 7%, and total effective rate 84. 5%, all of which were superior to those in the control group (total markedly effective rate 32.1% and total effective rate 66.1%, respectively),P < 0.01.Conclusion: Administration of QLA suppository via anal route combined with oral antibiotics is an effective therapy for chronic prostatitis syndrome. It can relieve the symptoms of chronic prostatitis syndrome markedly and rapidly. It is a new choice for treatment of the disease.

Time and Economic Cost of Constipation Care in Nursing Homes

Chronic constipation is a common disorder among residents in long-term care; yet the cost to the nursing home of constipation-related care is not known. The objective of this study was to quantify the nursing staff and supply-related cost of constipation care to nursing homes from the perspective of the nursing home.Prospective, observational time-and-motion design.Two United States nursing homes.A total of 59 nursing home residents with chronic constipation and nursing staff providing constipation care to them.Actual time to complete constipation care-related tasks was measured via stopwatch by trained observers, and the number and professional level (eg, staff nurse, CNA) of staff performing each task was recorded. Frequency of constipation care task data was obtained through 60-day retrospective medical chart review for each subject. Nurse wage rate data was obtained from the Nursing Home Salary and Benefits Report, a US-based national source. Resident and nursing home descriptive information was also collected.The average cost per task occurrence ranged from 0.72 US dollars for enema administration to 1.74 US dollars for oral medication administration. Average nursing staff costs per subject per year were 1577 US dollars for oral medication administration, 215 US dollars for dietary supplement administration, 39 US dollars for constipation assessment, 17 US dollars for suppository administration, and 6 US dollars for enema administration. Based on estimates of frequency of occurrence, the total annual labor and supply cost per long-term care resident with constipation was 2253 US dollars.Nursing staff performance of constipation care-related tasks is time consuming and costly in the long-term care setting.

Time and Economic Cost of Constipation Care in Nursing Homes

Objective Chronic constipation is a common disorder among residents in long-term care; yet the cost to the nursing home of constipation-related care is not known. The objective of this study was to quantify the nursing staff and supply-related cost of constipation care to nursing homes from the perspective of the nursing home. Design Prospective, observational time-and-motion design. Setting Two United States nursing homes. Participants A total of 59 nursing home residents with chronic constipation and nursing staff providing constipation care to them. Measurements Actual time to complete constipation care-related tasks was measured via stopwatch by trained observers, and the number and professional level (eg, staff nurse, CNA) of staff performing each task was recorded. Frequency of constipation care task data was obtained through 60-day retrospective medical chart review for each subject. Nurse wage rate data was obtained from the Nursing Home Salary and Benefits Report, a US-based national source. Resident and nursing home descriptive information was also collected. Results The average cost per task occurrence ranged from $0.72 for enema administration to $1.74 for oral medication administration. Average nursing staff costs per subject per year were $1577 for oral medication administration, $215 for dietary supplement administration, $39 for constipation assessment, $17 for suppository administration, and $6 for enema administration. Based on estimates of frequency of occurrence, the total annual labor and supply cost per long-term care resident with constipation was $2253. Conclusion Nursing staff performance of constipation care-related tasks is time consuming and costly in the long-term care setting. Chronic constipation is a common disorder among residents in long-term care; yet the cost to the nursing home of constipation-related care is not known. The objective of this study was to quantify the nursing staff and supply-related cost of constipation care to nursing homes from the perspective of the nursing home. Prospective, observational time-and-motion design. Two United States nursing homes. A total of 59 nursing home residents with chronic constipation and nursing staff providing constipation care to them. Actual time to complete constipation care-related tasks was measured via stopwatch by trained observers, and the number and professional level (eg, staff nurse, CNA) of staff performing each task was recorded. Frequency of constipation care task data was obtained through 60-day retrospective medical chart review for each subject. Nurse wage rate data was obtained from the Nursing Home Salary and Benefits Report, a US-based national source. Resident and nursing home descriptive information was also collected. The average cost per task occurrence ranged from $0.72 for enema administration to $1.74 for oral medication administration. Average nursing staff costs per subject per year were $1577 for oral medication administration, $215 for dietary supplement administration, $39 for constipation assessment, $17 for suppository administration, and $6 for enema administration. Based on estimates of frequency of occurrence, the total annual labor and supply cost per long-term care resident with constipation was $2253. Nursing staff performance of constipation care-related tasks is time consuming and costly in the long-term care setting.

Serum paracetamol concentrations in adult volunteers following rectal administration

Paracetamol is usually given in adults at a dose of 10-20 mg kg(-1) orally or rectally. Work in children suggests that doses of 40 mg kg(-1) are needed to provide therapeutic concentrations when this drug is used by the rectal route. We have investigated the dose of rectal paracetamol needed to achieve serum concentrations within the accepted therapeutic range of 10-20 microg ml(-1) in adults. Ten healthy adult volunteers received increasing doses of rectal paracetamol (15, 25, 35, and 45 mg kg(-1)). Following suppository administration, serum paracetamol concentrations were measured half hourly to 4 h then hourly to 8 h. Sustained concentrations within our therapeutic range were achieved with 35 and 45 mg kg(-1). Maximum measured concentrations were 12.5 (10-16), 16.5 (14-20), and 20 (17.5-23) microg ml(-1), median (inter-quartile range) after 25, 35, and 45 mg kg(-1), respectively. We conclude that doses of 35-45 mg kg(-1) of rectal paracetamol are needed to achieve sustained therapeutic plasma concentrations in healthy adult volunteers.

Pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories and oral syrup to healthy subjects

The pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories at three dosage strengths and oral syrup were studied. The study had an open-label, randomized, crossover design. At intervals of five to nine days, healthy volunteers were given two 12.5-mg promethazine rectal suppositories, one 25-mg suppository, one 50-mg suppository, or 50 mg (10 mL) of promethazine oral syrup. Blood samples were collected before each dose and at intervals from 0.5 to 48 hours afterward. Promethazine concentration was determined by high-performance liquid chromatography, and pharmacokinetic values were calculated with noncompartmental methods. Thirty-six subjects (18 men and 18 women) completed the study. Absorption was highly variable for all the formulations. On average, absorption was more rapid and the maximum plasma concentration (Cmax) higher for the syrup than for the suppositories. Cmax was significantly lower for the 50-mg suppository (mean, 9.04 ng/mL) than for the syrup (19.3 ng/mL). The time to Cmax (tmax) was significantly shorter for the syrup (mean, 4.4 hours) than for the suppositories (6.7-8.6 hours). There were no significant differences in dose-normalized Cmax among the three suppository treatments. Area under the concentration-versus-time curve (AUC) was comparable between the syrup and the 50-mg suppository and between the treatments with two 12.5-mg suppositories and the 25-mg suppository. Elimination profiles were similar among all treatments (mean half-life [t1/2], 16-19 hours). There were no significant differences in pharmacokinetics on the basis of sex or race. The mean relative bioavailability for the three suppository treatments ranged from 70% to 97%. Individual relative bioavailabilities ranged from 4% to 343%. The pharmacokinetics of promethazine administered in oral syrup and rectal suppositories were highly variable, but, in general, the suppositories produced a lower Cmax and later tmax than the syrup. All formulations were comparable in terms of dose-normalized AUC and t1/2, and the three suppository treatments were comparable in terms of dose-normalized Cmax.

Stereoselective pharmacokinetics of ibuprofen and its lysinate from suppositories in rabbits

Studies were performed on the effect of ibuprofen racemate ionisation extent on the pharmacokinetics of its enantiomers following administration in suppositories to rabbits. The suppositories, containing 146.3 mg ibuprofen in acidic form (IBP) or 250 mg ibuprofen lysinate (IBPL), equivalent to the above IBP dose, were prepared using lipophilic Witepsol H-15 as a base and administered to rabbits in a crossover design. Compared with IBP, administration of IBPL was followed by faster absorption and elimination of R and S enantiomers. However, significant differences at α=0.05 were observed only at the stage of elimination. AUC was markedly higher following administration of suppositories containing IBP than following suppositories with IBPL and this pertained to both R and S enantiomers. Evident inversion of R into S form was noted 30 min following IBPL administration and 1 h after IBP administration. Ionisation extent only insignificantly affected the scope of chiral inversion of ibuprofen R into S form (AUC S-IBP /AUC R-IBP =1.66, AUC S-IBPL /AUC R-IBPL =1.57). No presystemic inversion of R into S was observed in rabbits following administration of IBP or IBPL in suppositories. IBP enantiomers were isolated from 0.5 ml serum using solid phase extraction in C 18 columns and were quantified by HPLC using the chiral Whelk O1 column and UV detector ( λ=264 nm).

Improvement of availability of allopurinol from pharmaceutical dosage forms I - suppositories

Solid dispersion and crystallization of a very slightly water-soluble drug, allopurinol, were prepared using urea, sodium salicylate and β-cyclodextrin ( β-CD) as carriers. The spectroscopic infra-red (IR), differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) data indicate a role of these carriers in decreasing the crystallinity of allopurinol and complexing abilities. Solid dispersion and crystallization of the drug with these carriers were used in suppository formulations to investigate their role in enhancement of drug release through the membrane barrier. The bases used included Suppocire AM and the mixture of polyethylene glycols (PEGs). The release rates of allopurinol from lipophilic and hydrophilic suppository bases were examined and compared with those obtained for their inclusion compounds incorporated in the same bases. The prepared suppositories were evaluated for in-vitro drug release, when fresh and on storage. The release of pure allopurinol from the lipophilic base was remarkably higher than that from the hydrophilic one. The release of allopurinol from lipophilic as well as hydrophilic bases was significantly enhanced by crystallization of the drug from 5% w/v of sodium salicylate. Allopurinol crystallized from sodium salicylate, showed enhanced release reaching about 100% in 1 h from the Suppocire AM base. The obtained data from these experiments proved the superiority of the PEG formulations containing coevaporates of the drug to sodium salicylate, ratio 1:1, or of the drug to β-CD, ratio 1:2; T 90%,12 and 36 min, respectively. A significant decrease of uric acid excretion in rabbits was observed after rectal administration of suppositories containing allopurinol crystallized from sodium salicylate.

Sustained Release of Diclofenac from Polymer-Containing Suppository and the Mechanism Involved

Sustained release of diclofenac sodium (DcNa) from suppositories composed of triglycerides and polymer was investigated by dissolution testing through an artificial membrane. DcNa was slowly released from a suppository containing carboxyvinyl polymer (CVP), and the extent of the release decreased with the amount of CVP added. Little effect was noted with the addition of other water-soluble polymers, such as hydroxyethylcellulose (HEC), xanthan gum, and polyvinylalcohol (PVA). When sodium benzoate was used instead of DcNa, a similar result was obtained with the addition of CVP. The result of release rate analysis together with the viscosity and pH in these cases showed that the reduction of solubility and diffusion due to sodium exchange between DcNa and CVP played an important role in the sustained release from the suppository. Also, in comparison with the results when CVP was not used, the plasma concentration profile of diclofenac after the administration of CVP suppository displayed a twofold longer half-life time.

Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol ®

Suppositories are the preferable dosage form for patients at home or experiencing nausea. Serotonin (5-HT 3)-receptor antagonists are used to treat vomiting in intravenous or oral administration but not suppository form. Ramosetron hydrochloride (RAM) is a new 5-HT 3 antagonist which effectively inhibits vomiting, and we prepared RAM suppositories using Witepsol ® H-15 (H-15) containing Carbopol ® 934P (CP). The viscosity of suppository base and RAM release properties from suppositories were examined. Plasma RAM concentrations after administration of suppositories to rabbits were estimated and irritation of rectal tissues were observed. Antiemetic effects of suppositories were studied using ferrets. The base viscosity increased with addition of CP. Suppositories containing CP exhibited better absorption in rabbits compared to H-15 suppositories, correlated with release behavior. Suppositories containing 2% CP had 2.5 times larger AUC 0–24 h than H-15 suppositories, and the MRT was prolonged by 5.8 h compared with i.v. administration. 10% CP suppositories administered to rabbits for 5 days did not irritate the tissues. Antiemetic studies indicated that 2% CP suppository of RAM might have the same effect as i.v. administration. These results suggest that RAM suppositories containing CP are safe and useful in once-a-day dosage form for treatment of chemotherapy-induced nausea.

Preparation and evaluation of double-phased mucoadhesive suppositories of lidocaine utilizing Carbopol® and white beeswax

In an attempt to restrict drug absorption from suppositories to only the lower rectum, mucoadhesive lidocaine (LID) suppositories were prepared using Witepsol® H-15 as a base, and Carbopol® 934P (CP) and white beeswax (WAX) as additives. CP has a mucoadhesive property and WAX gives the suppositories stiffness. The suppositories containing 10% CP and 20% WAX stayed in the lower recta of rats for at least 2 h. Double-phased suppositories consisting of a front layer containing 10% CP and 20% WAX and a terminal layer containing LID and various amounts of CP were prepared. In vitro release profiles of LID from double-phased suppositories were similar to conventional single-phased suppositories containing CP alone. Values of AUC0–6 h and MRT of LID after administration of double-phased suppositories to rabbits were larger than those for single-phased suppositories with or without CP. On the other hand, the initial plasma metabolites concentrations after administration of double-phased suppositories were significantly lower and tended to exhibit delayed Tmax compared to single-phased suppositories. These results suggest that the double-phased mucoadhesive suppositories suppress initial metabolism of LID, and may be useful for improving bioavailabilities of drugs, like LID, which accept first-pass effect considerably.

Plasma levels of artesunate and dihydroartemisinin in children with Plasmodium falciparum malaria in Gabon after administration of 50-milligram artesunate suppositories.

A thermostable suppository of artesunate (artesunic acid) has been developed. In Gabon, 12 children with Plasmodium falciparum malaria received two administrations of this suppository in a 4-hr interval. Parasitemia and fever were then measured and the plasma levels of artesunate and its active metabolite, dihydroartemisinin, were determined by means of a reversed phase high-pressure liquid chromatography method using reductive electrochemical detection. Substantial parasite clearance (97-100%) was noted 24 hr after the beginning of the treatment and body temperature had returned to normal. Absorption, metabolism, and elimination of artesunate were rapid. Mean values of maximum plasma levels (Cmax) and maximum concentration peak times (tmax) were evaluated. The Cmax of dihydroartemisinin (0.18 +/- 0.10 microg/ml [mean +/- SE]) was higher than the Cmax of artesunate (0.09 +/- 0.04 microg/ml) and the tmax of dihydroartemisinin (1.13 +/- 0.58 hr) was higher than the tmax of artesunate (0.58 +/- 0.19 hr). Plasma levels 30 min after the second suppository administration were not consistently higher than those found 30 min after the first administration.

Studies of drug delivery systems for a therapeutic agent used in osteoporosis. I. Pharmacodynamics (hypocalcemic effect) of elcatonin in rabbits following rectal administration of hollow-type suppositories containing elcatonin.

In this study, we developed a new hollow-type suppository containing elcatonin ((Asu1,7)-eel calcitonin, ECT), a synthetic derivative of eel calcitonin, which produces hypocalcemia, as a pharmaceutical preparation for self administration, to be used instead of parenteral injections for patients with osteoporosis. The absorption of ECT from the rectal mucous membrane was evaluated by observation of the decrease in serum calcium (Ca) concentrations following rectal administration in rabbits. ECT was efficiently absorbed from the rectum and effectively decreased serum Ca concentrations. The data of the area under the percent decrease in serum Ca concentration (deltaCa%)-time curve (deltaCa%-AUC), assumed to be an index of the pharmacodynamics (pharmacological effect) of ECT, indicated that similar hypocalcemic effects were obtained following rectal and intravenous administrations of ECT. In regard to the effect of coadministration of other compounds on rectal absorption of ECT, no significant difference in the deltaCa%-AUC between rectal ECT administration with or without nafamostat mesilate (a protease inhibitor) was observed. However, the coadministration of ECT with cytochalasin B or monensin (endocytosis inhibitors) significantly decreased the deltaCa%-AUC, indicating that rectal ECT absorption is probably inhibited by endocytosis inhibitors. On the other hand, it was found that sodium decanoate, a medium-chain fatty acid (sodium salt), significantly enhanced the rectal absorption of ECT. We conclude that this ECT hollow-type suppository offers promise as a new method for the administration of ECT.

Preparation and utility of glibenclamide suppository for hospital use

Glibenclamide (GC) is widely used as an oral hypoglycemic drug in the treatment of non-insulin dependent diabetes mellitus (NIDDM). Since GC is usually taken for a long period, side effects and noncompliance are among the problems. In order to solve those problems, we prepared GC suppositories and examined their usefulness. Suppositories containing 4, 20, and 40 mg of GC were prepared and examined for drug release, drug absorption and blood glucose levels after the rectal administration of suppositories in rabbits. In the release test, GC suppositories released the drug continuously for 6 hours. The areas under the drug release time curve (ADT) of 20 and 40 mg GC suppositories were 3.5 and 6.2 times of 4 mg GC suppositories respectively. The plasma concentrations after administration of 4 and 20 mg GC suppositories showed about the same profiles for 6 hours. After administration of 40 mg GC suppositories, the maximum plasma concentration (Cmax) was observed at 2 hours. All the GC suppositories showed lower blood glucose levels compared with the control. The remainder of the area under the blood glucose concentration time curve between the control (RAUC) in the case of 40 mg GC suppository was 1.3 times larger than that of the 4 mg GC suppository. The GC suppositories sufficiently lowered the blood glucose levels. These results suggest that the GC suppositories should be useful in the hospital preparation for the treatment of NIDDM patients.

Patient attitudes to perioperative suppository administration for postoperative analgesia.

Four hundred surgical patients were questioned preoperatively to ascertain their attitudes to suppository analgesia. Given a choice, 82 per cent of patients expressed a preference for intramuscular administration of diclofenac, with 18 per cent choosing a suppository. Males were more likely than females to choose an intramuscular injection. Males choosing a suppository were more likely to belong to a higher socio-economic group while females choosing a suppository were more likely to be married. Twenty-three per cent of patients who initially opted for intramuscular administration changed to suppository administration when the possibility of pain or discomfort at the injection site was explained. Females who changed to suppository administration were more likely to belong to a higher socio-economic group and to be married. Twenty-seven per cent of patients choosing an intramuscular injection expressed concern if a suppository were to be inserted without consent. Eleven per cent of patients choosing a suppository expressed similar concern. There is an overall reluctance, particularly within the male population to accept suppository analgesia. Patients from higher socio-economic groups may be more willing to accept what they perceive to be less traditional forms of treatment.