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.     

Efficacy of promethazine suppositories dispensed to outpatient surgical patients.

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

Self-Microemulsifiyng Suppository Formulation of β-Artemether

Parasitic diseases are of immense global significance as around 30% of world’s population experiences parasitic infections. Among these, malaria is the most life-threatening disease. Various routes of administration have been explored for delivering antimalarial actives. The present investigation aims at formulating self-microemulsifying suppositories of β-artemether with faster onset of action and prolonged effect to be administered by rectal route. These were compared with conventional polyethylene glycol suppositories with respect to melting range, rheology, texture analysis, disintegration time, self microemulsification time, particle size, and drug content. In vitro drug release was studied by using USP apparatus II. Further, the suppositories were evaluated in murine model against virulent rodent malaria parasite Plasmodium berghei wherein the developed self-microemulsifying suppositories could sustain the activity (94%) for 20 days post infection. The survival of animals was also better as compared to the conventional formulation.     

Comparison between naproxen tablets and suppositories in primary dysmenorrhea

Naproxen tablets and suppositories were compared, in the treatment of primary dysmenorrhea, in a double-blind cross-over trial. The results on 32 patients treated during 128 menstruations with either tablets and suppositories were analysed. Both naproxen tablets and suppositories produced a significant but similar overall relief of dysmenorrhea, although the tablets had a better effect in relieving spasmodic pain than the suppositories (p < 0.05). Occasions of failure to obtain relief were not related to the occurrence of vomiting or diarrhea during the trial. Vomiting seems not to be responsible for the therapeutic failures of oral treatments with prostaglandin-synthetase inhibitors in primary dysmenorrhea.     

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° F or higher which occurred in 68% of the patients. Temperatures returned to normal levels within 4 to 6 hours after the last administration 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 technique during the midtrimester, however the use of PGE₂ in conjunction with a diaphrgam 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.     

Correction of intestinal dysbacteriosis in elderly patients with the use of bifidobacterin introduced by different routes

The results of the correction of disturbances in intestinal microflora in elderly patients with the use of bifidumbacterin in the form of powder or suppositories are presented. The effectiveness of the rectal administration of bifidumbacterin (by microinjections through an enema or in suppositories) is shown in comparison with the oral administration of the preparation. The administration of bifidumbacterin in suppositories for 15 days resulted in decreased content of hemolytic Escherichia below the threshold of determination in all examined patients.     

Comparison of salicylazosulfapyridine bioavailability following oral and rectal administration in patients with ulcerative colitis]

Salicylazosulfapyridine--a drug commonly used in the ulcerative colitis--is effective following both oral and rectal administration. Pharmacokinetics of the drug given per rectum (in the form of suppositories) has not been investigated so far. The present study aims at comparing bioavailability of salicylazosulfapyridine following oral and rectal administration to patients with the ulcerative colitis and healthy volunteers. It was found, that following rectal administration the drug is not so readily absorbed as in oral dosage form. No sulfapyridine and 5-aminosalicylic acid have been detected in blood serum, when the drug was given in the form of rectal suppositories. Clinical stage of the disease did not affect absorption of both unchanged drug and its metabolites. Due to the fact, that the drug is active locally, rectal suppositories seem a therapeutical alternative in patients only with lesions localized in the rectum.     

Bioavailability and LH-suppressing effect of different testosterone preparations in normal and hypogonadal men.

The therapeutic effectiveness of intramuscularly administered testosterone esters and free testosterone in suppositories was investigated by the measurement of plasma testosterone and LH levels after administration to normal and hypogonadal men. Testosterone levels were elevated above the lower physiological limit for 1 day after 25 mg testosterone one propionate, for 2 days after 50 mg testosterone propionate and for 14 days after 250 mg testosterone oenanthate. LH levels were suppressed for the corresponding periods. Elevated plasma testosterone and suppressed LH levels were maintained by testosterone suppositories (3 x 20 mg for 5 days).     

Preclinical investigation and standardization of metronidazole soft dosage forms]

Comparative acute and subacute toxicity of Dentamet gel and Metrovagin suppositories manufactured by ZAO Altaivitaminy was studied with using analogous drugs, i. e. Metrogil Denta, a gel for the gingivae, manufactured by Unique Pharmaceutical Laboratories (India), and Flagil manufactured by Haupt Farma Livron (France) as the reference drugs. It was shown that the drugs induced no changes in the exterior, hair state, body weight and mobility of the experimental animals vs. the control. The pharmacokinetic study of Metrovagin vaginal suppositories vs. the registered analogous drug Flagil showed that Metrovagin was bioequivalent to Flagil. The relative bioavailability of the new drug vs. the control was 103.13%.     

Vaginal mucosa serves as an inductive site for tolerance

These data demonstrate that tolerance can be induced by vaginal Ag exposure. In these experiments, mice were given vaginal agarose gel suppositories containing either 5 mg OVA or saline for 6 h. Mice were given suppositories either during the estrous (estrogen dominant) or diestrous (progesterone dominant) stage of the estrous cycle. Mice were restrained during the inoculation period to prevent orovaginal transmission of the Ag. After 1 wk, mice were immunized s. c. with OVA in CFA. After 3 wk, mice were tested for delayed-type hypersensitivity responses by measuring footpad swelling and measuring in vitro proliferation of lymphocytes to Ag. Using ELISA, the magnitude of the serum Ab response was also measured. In some mice, FITC conjugated to OVA was used to track the dissemination of the protein into the systemic tissues. The magnitude of footpad swelling was significantly reduced in mice receiving OVA-containing suppositories during estrus compared with mice receiving saline suppositories. Concomitant decreases in the Ag-specific proliferative response were also observed in lymph node lymphocytes and splenocytes. Conversely, mice inoculated during diestrus did not show a decreased response to Ag by either footpad response or in vitro proliferation. Serum Ab titers in the estrus-inoculated mice did not decrease significantly. These data demonstrate that the reproductive tract can be an inductive site for mucosally induced tolerance. However, unlike other mucosal sites such as the lung and gastrointestinal tract, reproductive tract tolerance induction is hormonally regulated.     

Replacement of L-T4 suppository in MMI treated rabbits

L-T4 suppositories containing 50, 100 or 200 micrograms of L-T4 were given to rabbits treated with MMI. The serum T4 gradually increased within 3.5 and 6.5 hours following the use of 100 and 200 micrograms of L-T4 suppositories, respectively, without an acute increase in serum T3. The increase in serum T4 continued up to 48 hours. The area under the curve (AUC) for serum T4 was evidently dose-dependent. It is concluded from these results that the T4 suppository will be useful as a replacement therapy for patients with hypothyroidism.     

Trichomonal vaginitis; the problem of chronic or recurring infection

In general practice and in gynecology, vaginal trichomoniasis is a frequent and troublesome problem. However, the trichomonas vaginalis organism is frequently found in an apparently healthy vagina, indicating that symptoms, recurrences, or exacerbations may depend on local changes in secretions, probably due in part to emotional stress. Therapy must, therefore, include not only the topical use of an effective trichomonacidal drug, but also sympathetic and considerate listening by the physician. The combination of furazolidone and nifuroxime in vaginal suppositories and vaginal insufflation powder was found to be an effective trichomonacidal compound. A total of 56 patients with trichomonal, monilial and nonspecific bacterial vaginitis was treated with this nitrofuran combination with good results. In topical therapy, powders seem more effective, probably because a dry environment is unfavorable to the flagellates. The patient should be instructed to insert two vaginal suppositories daily for the first week, then to decrease the dosage gradually as indicated by the physician after clinical examination and microscopic examination of vaginal secretions each week. Of great importance is the fact that some patients may need long-term maintenance therapy-one or two suppositories weekly-especially if the emotional difficulties appear to be insurmountable.     

Diazepam-Loaded Solid Lipid Nanoparticles: Design and Characterization

The aim of the present study was to investigate the feasibility of the inclusion of a water-insoluble drug (diazepam, DZ) into solid lipid nanoparticles (SLNs), which offer combined advantages of rapid onset and prolonged release of the drug. This work also describes a new approach to prepare suppositories containing DZ-loaded SLN dispersions, as potential drug carrier for the rectal route. Modified high-shear homogenization and ultrasound techniques were employed to prepare SLNs. The effect of incorporation of different concentrations of Compritol® ATO 888 or Imwitor® 900K and Poloxamer 188 or Tween 80 was investigated. Results showed that varying the type or concentration of lipid matrix or surfactant had a noticeable influence on the entrapment efficiencies, particle size, and release profiles of prepared SLNs. Differential scanning calorimetry and X-ray diffraction measurements showed that the majority of SLNs possessed less ordered arrangements of crystals than the corresponding bulk lipids, which was favorable for increasing the drug loading capacity. Transmission electron microscopy and laser diffractometry studies revealed that the prepared nanoparticles were round and homogeneous and 60% of the formulations were less than 500 nm. Additionally, SLN formulations showed significant (P?in vitro release of DZ from the suppositories prepared using DZ-loaded SLN dispersions (equivalent to 2 mg DZ) was significantly (P?相似文献   

Termination of early pregnancy by ONO-802 suppositories (16,16-dimethyl-trans-Δ2-PGE1 methyl ester)

ONO-802 was used in the form of vaginal suppositories for the termination of early pregnancy in 63 healthy volunteers. Fifty-four (86%) of the 63 cases had complete abortions and remaining 9 (14%) had incomplete abortions.One (1.6%) of the 63 cases complained of nausea and vomiting, and 3 (4.8%) complained of headaches. No other side effects were observed.These results suggest that ONO-802 is acceptable in the form of vaginal suppositories for the termination of early pregnancy.     

Evaluation of an acetic acid ester of monoglyceride as a suppository base with unique properties

The objective of this investigation was to evaluate an acetic acid ester of monoglycerides made from edible, fully hydrogenated palm oil (AC-70) as a suppository base and compare it with a commercially available semisynthetic base (Suppocire AI). Benzocaine and miconazole were used as model drugs. Suppositories were prepared by the fusion method. The drug loads in the suppositories were kept at 2% to 5% (wt/wt). In vitro release of drug from the suppositories into Sorensen's phosphate buffer (pH 7.4) was studied using a US Pharmacopeia dissolution apparatus 1 and a spectrophotometer. The melting behavior of the bases and the physical state of the drug in the suppositories were studied using a differential scanning calorimeter (DSC). Powder x-ray diffractometry was used to study any possible polymorphic changes in the AC-70 base during formulation and storage. In vitro release studies revealed that the release of benzocaine from the AC-70 suppository was substantially slower than that of the commercial AI base. At a 2.5% (wt/wt) benzocaine load, the release of drug from the AC-70 suppositories was found to be linear. This slow and linear release was attributed to the physical property of the base, which forms liquid crystalline phases in the aqueous dissolution medium. The lyotropic liquid crystalline phase has the ability to incorporate drug into its structure and can control the release kinetics of the drug from such a system. The apparent pH of the release medium (water) was decreased by 1 to 1.5 pH units when the AC-70 base was used. The DSC studies revealed that the melting range of the AC-70 base is 36 degrees C to 38 degrees C, which is ideal for suppository formulations. The results of these studies support the possibility of using this new base for slow-release suppository formulations. This base may be of particular interest for a drug that requires an acidic environment to maintain its activity.     

Termination of early pregnancy by ONO-802 suppositories (16,16-dimethyl-trans-Δ-PGE1 methyl ester)

ONO-802 was used in the form of vaginal suppositories for the termination of early pregnancy in 63 healthy volunteers. Fifty-four (86%) of the 63 cases had complete abortions and remaining 9 (14%) had incomplete abortions.One (1.6%) of the 63 cases complained of nausea and vomiting, and 3 (4.8%) complained of headaches. No other side effects were observed.These results suggest that ONO-802 is acceptable in the form of vaginal suppositories for the termination of early pregnancy.     

Erythromycin pharmacokinetics in children after rectal and oral administration

Pharmacokinetics of erythromycin base was studied clinically in children not older than 14 years treated with new children dosage forms of the antibiotic i. e. 0.1 and 0.25 g enteric coated tablets and 0.06 and 0.125 g suppositories. It was noted that the new dosage forms were characterized by higher availability which was 2.5-3 times higher than that after using the erythromycin base tablets without the coating. Systematic increasing of erythromycin availability after the use of the rectal suppositories was observed with increasing of the children age. Absolute absorption in newborns, sucklings and children over 1 year amounted to 28, 36 and 54 per cent respectively.     

Essential fatty acid deficiency and platelet fatty acids of normotensive and genetically hypertensive rats

Termination of pregnancy in missed abortion and intra-uterine fetal death was accomplished using vaginal suppositories of 20 mg PGE₂ in 31 cases and the results were compared with oxytocin induction (with or without estrogen pre-treatment) in 17 cases at the doses routinely used in our hospital. The PG suppositories proved much more superior (96.7%) than oxytocin (47.7%), but induced a higher rate of side effects. The latter were not serious and were generally tolerated by the patients. There was a positive correlation between duration of fetal retention in utero and the induction expulsion time. The over all patient acceptance of the method was quite favourable and the approach appears to be a definite advance towards management of these cases.     

Management of missed abortion and fetal death in utero

Termination of pregnancy in missed abortion and intra-uterine fetal death was accomplished using vaginal suppositories of 20 mg PGE₂ in 31 cases and the results were compared with oxytocin induction (with or without estrogen pre-treatment) in 17 cases at the doses routinely used in our hospital. The PG suppositories proved much more superior (96.7%) than oxytocin (47.7%), but induced a higher rate of side effects. The latter were not serious and were generally tolerated by the patients. There was a positive correlation between duration of fetal retention in utero and the induction expulsion time. The over all patient acceptance of the method was quite favourable and the approach appears to be a definite advance towards management of these cases.     

TRICHOMONAL VAGINITIS—The Problem of Chronic or Recurring Infection

In general practice and in gynecology, vaginal trichomoniasis is a frequent and troublesome problem. However, the trichomonas vaginalis organism is frequently found in an apparently healthy vagina, indicating that symptoms, recurrences, or exacerbations may depend on local changes in secretions, probably due in part to emotional stress. Therapy must, therefore, include not only the topical use of an effective trichomonacidal drug, but also sympathetic and considerate listening by the physician.The combination of furazolidone and nifuroxime in vaginal suppositories and vaginal insufflation powder was found to be an effective trichomonacidal compound. A total of 56 patients with trichomonal, monilial and nonspecific bacterial vaginitis was treated with this nitrofuran combination with good results.In topical therapy, powders seem more effective, probably because a dry environment is unfavorable to the flagellates. The patient should be instructed to insert two vaginal suppositories daily for the first week, then to decrease the dosage gradually as indicated by the physician after clinical examination and microscopic examination of vaginal secretions each week. Of great importance is the fact that some patients may need long-term maintenance therapy—one or two suppositories weekly—especially if the emotional difficulties appear to be insurmountable.