Pharmacokinetic and metabolite profile of orally administered anemoside B4 in rats with an improved exposure in formulations of rectal suppository.

ETHNOPHARMACOLOGICAL RELEVANCE: Pulsatilla chinensis (Bunge) Regel is a traditional Chinese herbal medicine used to treat intestinal amebiasis, malaria, vaginal trichomoniasis, and bacterial infections. Anemoside B4 (AB4), a pentacyclic triterpenoid saponin, is one of the primary bioactive substances in Pulsatilla chinensis (Bunge) Regel, and gavage administration of AB4 to animals has been demonstrated to exhibit anticancer, anti-inflammatory, and antiviral actions. However, AB4 exposure in plasma is very low after oral administration, and the biotransformation of AB4 in vivo after oral administration remains unknown. AIM OF THE STUDY: The reason for conducting this research was to explore at the metabolite profile of AB4 in rats following oral administration. Additionally, we aimed to develop an appropriate extravascular formulation to increase the exposure and duration of AB4 in vivo. MATERIALS AND METHODS: A well-validated HPLC-QQQ-MS/MS method was used for the quantification of AB4 in plasma and was further applied to evaluate and compare the pharmacokinetic properties of AB4 dissolved in a saline solution and AB4 formulations in a rectal suppository or enteric capsule. Reliable UHPLC coupled to Q-Exactive Plus high-resolution MS was used to identify the metabolites in rat plasma, bile, urine, and faeces. RESULTS: AB4 was extensively metabolized, and a total of 29 metabolites were identified. The primary metabolic routes included deglycosylation, oxidation, dehydrogenation, reduction, sulfation, hydration, acetylation, and glucuronidation. The pharmacokinetic comparison showed that both the rectal suppository and enteric capsule increased the exposures of AB4 and one of its active metabolites, 23-hydroxybetulinic acid (23-HA). Notably, rectal suppositories increased systemic AB4 exposure (AUC0-∞) by approximately 49 and 28 times higher than that of the AB4 saline solution and enteric capsules, respectively. The t1/2 of AB4 was extended to approximately 7 h after rectal administration compared to 2 h after oral administration. CONCLUSION: Overall, our study demonstrated that the mismatched exposure-response relationship of AB4 could result from extensive metabolism in the gastrointestinal and circulatory systems. Thus, a rectal suppository could be an alternative formulation of AB4 to obtain both higher and longer exposure.

A randomized trial of safety, acceptability and adherence of three rectal microbicide placebo formulations among young sexual and gender minorities who engage in receptive anal intercourse (MTN-035).

Efforts to develop a range of HIV prevention products that can serve as behaviorally congruent viable alternatives to consistent condom use and oral pre-exposure prophylaxis (PrEP) remain crucial. MTN-035 was a randomized crossover trial seeking to evaluate the safety, acceptability, and adherence to three placebo modalities (insert, suppository, enema) prior to receptive anal intercourse (RAI). If participants had no RAI in a week, they were asked to use their assigned product without sex. We hypothesized that the modalities would be acceptable and safe for use prior to RAI, and that participants would report high adherence given their behavioral congruence with cleansing practices (e.g., douches and/or enemas) and their existing use to deliver medications (e.g., suppositories; fast-dissolving inserts) via the rectum. Participants (N = 217) were sexual and gender minorities enrolled in five different countries (Malawi, Peru, South Africa, Thailand, and the United States of America). Mean age was 24.9 years (range 18-35 years). 204 adverse events were reported by 98 participants (45.2%); 37 (18.1%) were deemed related to the study products. The proportion of participants reporting "high acceptability" was 72% (95%CI: 65% - 78%) for inserts, 66% (95%CI: 59% - 73%) for suppositories, and 73% (95%CI: 66% - 79%) for enemas. The proportion of participants reporting fully adherent per protocol (i.e., at least one use per week) was 75% (95%CI: 69% - 81%) for inserts, 74% (95%CI: 68% - 80%) for suppositories, and 83% (95%CI: 77% - 88%) for enemas. Participants fully adherent per RAI-act was similar among the three products: insert (n = 99; 58.9%), suppository (n = 101; 58.0%) and enema (n = 107; 58.8%). The efficacy and effectiveness of emerging HIV prevention drug depends on safe and acceptable delivery modalities that are easy to use consistently. Our findings demonstrate the safety and acceptability of, and adherence to, enemas, inserts, and suppositories as potential modalities through which to deliver a rectal microbicide.

The efficacy of glycerin suppositories for preterm infants: A meta-analysis of randomized controlled studies.

BACKGROUND: The effect of glycerin suppositories on full enteral feeds remained controversial in preterm infants, and thus we conducted this meta-analysis to identify the influence of glycerin suppositories on full enteral feeds in preterm infants. METHODS: The protocol was registered in PROSPERO (CRD20214283090). We searched PubMed, EMbase, Web of science, EBSCO and Cochrane library databases through February 2020, and included randomized controlled trials assessing the effect of glycerin suppositories on full enteral feeds in preterm infants. This meta-analysis was performed using the random-effect model. RESULTS: Six Randomized controlled trials were included in the meta-analysis. Overall, compared with control group in preterm infants, glycerin suppositories demonstrated no significant effect on days to full enteral feeds (mean difference = -0.26; 95% confidence interval [CI] = -1.16 to 0.65; P = .58), the incidence of necrotizing enterocolitis (odd ratio = 3.62; 95% CI = 0.56-23.32; P = .18) or death (odd ratio = 1.46; 95% CI = 0.40-5.40; P = .57), but may increase the days under phototherapy (mean difference = 0.50; 95% CI = 0.43-0.57; P < .00001). Only low heterogeneity was seen among all outcomes. CONCLUSIONS: Glycerin suppositories may provide no additional benefits to preterm infants.

Efficacy of the Panax Notoginseng Ejiao Suppository in the Treatment of Patients with Ulcerative Proctitis and Its Effect on Inflammatory Response and Immune Function.

Objective: To investigate the efficacy of the Panax notoginseng Ejiao suppository in patients with ulcerative proctitis and its effect on inflammatory response and immune function. Methods: This study recruited 100 patients with ulcerative proctitis who were hospitalized to our hospital's anorectal outpatient department between May 2015 and October 2020. They were randomly separated into either a control or a study group, with 50 cases in each. The control group received the mesalazine suppository, whereas the study group received the Panax notoginseng Ejiao suppository. Outcome measures included clinical effectiveness, inflammatory response, and immunological state of patients. Results: The total efficiency in the study group was significantly higher than that in the control group (P = 0.019). The Mayo score and Baron endoscopic score between the two groups were significantly decreased after treatment, with lower results in the study group (P < 0.05). The inflammatory variables were dramatically reduced following therapy, with the study group doing worse. Following treatment, the number of Th 17 cells declined dramatically in both groups, while the proportion of Treg cells increased significantly, with greater alterations of Th17 cells and Treg cells observed in the study group than those in the control group (P < 0.05). The Panax notoginseng Ejiao suppository resulted in significantly shorter time lapses before symptom alleviation and a lower incidence of recurrence at 6 months after treatment versus mesalazine suppository (P < 0.05). Conclusion: In patients with ulcerative proctitis, the Panax notoginseng Ejiao suppository significantly improves clinical efficacy, reduces the incidence of recurrence, mitigates inflammatory response, and improves immune function.

Glycerin Suppositories and Enemas in Premature Infants: A Meta-analysis.

BACKGROUND AND OBJECTIVES: Premature infants are often given glycerin suppositories or enemas to facilitate meconium evacuation and the transition to enteral feeds. We reviewed the best-available evidence for the use of glycerin suppositories and enemas in premature infants. METHODS: We searched MEDLINE, Embase, and Cochrane Central for randomized controlled trials (RCTs) of premature infants treated with glycerin suppositories or enemas through January 2022. Studies were screened and data extracted independently and in duplicate. We included RCTs of premature infants <32 weeks gestation and/or birth weight <1500 g who were treated with glycerin suppositories or enemas. Meta-analysis was performed using random effects and reported as relative risk or mean difference. RESULTS: We identified 6 single-center, RCTs of 389 premature infants treated with glycerin suppositories (n = 207) or enemas (n = 182). Mortality rates ranged from 0% to 17%, and the meta-analysis revealed no differences between treatment groups (P = .86). Active treatment was associated with earlier meconium evacuation (mean, 1.5 days; 95% confidence interval, 3.0 to 0.01; P = .05) but not a faster time to enteral feeds (mean, 0.5 days; P = .48). We identified 1 ongoing trial with a target recruitment of 220 premature infants. The quality of evidence was very low to moderate because of inadequate statistical power and other methodologic issues. CONCLUSIONS: The use of glycerin suppositories and enemas in premature infants is associated with earlier meconium evacuation, but the clinical significance of this finding is uncertain. Treatment has no definitive effects on mortality, necrotizing enterocolitis, or enteral feeds.

The efficacy and tolerability of pollen extract in combination with hyaluronic acid and vitamins in the management of patients affected by chronic prostatitis/chronic pelvic pain syndrome: a 26 weeks, randomized, controlled, single-blinded, phase III study.

BACKGROUND: Chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) remains a challenging clinical condition to manage. Here, we evaluate the efficacy and tolerability of a new treatment option (suppositories) containing pollen extract in combination with hyaluronic acid and vitamins in the management of patients with CP/CPPS. METHODS: In this prospective, randomized, controlled, single-blinded, phase-III study we enrolled CP/CPPS patients between March and December 2019. Participants were randomized (1:1) to the following treatment groups: 1) pollen extract suppositories 1 daily for 10 days; or 2) ibuprofen 600 mg 1 tablet in the morning for 10 days. At the enrolment time and at the follow-up evaluations (3, 6 months), all patients completed baseline questionnaires ([National Institutes of Health Chronic Prostatitis Symptom Index [NIH-CPSI] and Quality of Well-Being [QoL]) and underwent urological examination and microbiological evaluation. The primary endpoint was the quality-of-life assessment with Patients' Reported Outcomes (PROs). RESULTS: One hundred and eighty-seven patients were screened. Finally, one hundred and twenty-four patients (mean age 34.6±3.9 years) were randomly allocated to the new pollen extract treatment (N.=63) or ibuprofen (N.=61) groups. At the end of follow-up examinations 56/63 group 1 patients (88.8%) showed a significant reduction of the NIH-CPSI total score, compared with 17/61 (27.8%) in group 2 (P<0.0001). Group 1 patients also reported a higher improvement in terms of PROs, when compared with the control group and group 1 patients reported a significant reduction of leucocyte count at the Meares-Stamey Test (-12; -4; P<0.001). Only mild adverse events were reported in the two groups and adverse events were less frequent in the pollen extract suppositories group. CONCLUSIONS: The combination of pollen extract with hyaluronic acid and vitamins is more effective than ibuprofen in improving symptoms and Quality of Life in patients affected with CP/CPPS and has less side effects.

Development and Evaluation of Vaginal Suppository Containing Althaea officinalis L. Polysaccharide Extract

Abstract Intrauterine adhesions cause several gynecological problems. Althaea officinalis L. roots known as marshmallows contain polysaccharides (M.P.) which possess anti-inflammatory and anti-ulcerogenic activities also can form a bio-adhesive layer on damaged epithelial membranes prompting healing processes. Vaginal formulations of herbal origin are commonly applied to relieve cervico-uterine inflammation. Herein, we aim to develop and evaluate vaginal suppositories containing polysaccharides isolated from the A. officinalis root. Six formulations (four P.E.G.-based and two lipid-based suppositories containing 25% and 50% M.P.) met standard requirements, which were then subjected to qualitative and quantitative evaluation. All suppositories exhibited acceptable weights, hardness, content uniformity, melting point, and disintegration time, which fall within the acceptable recommended limits. Higher concentrations of M.P. in PEG-bases moderately increased the hardness (p<0.05). PEG-formulations showed content uniformity>90% of the average content while it was 75-83% for suppocire formulations. All formulations disintegrated in<30minutes. In-vitro release test revealed that M.P. release from 25%-MP formulations was higher than that of 50%-M.P. suppositories. Overall, results revealed the feasibility of preparing P.E.G.-or lipid-based suppositories containing M.P., which met the B.P. quality requirement

Formulation of Suppositories of Alum Produced from Bauxite Waste in Ghana for the Treatment of Hemorrhoid.

The study sought to formulate and evaluate suppositories using a locally produced brand of alum (Aw) obtained from bauxite waste generated at Awaso bauxite mine in the Western-North region of Ghana, for use in the treatment of hemorrhoids. The suppositories were formulated using shea butter modified, respectively, with amounts of beeswax and theobroma oil. In another development, theobroma oil was modified with different concentrations of beeswax. Drug-base interactions were investigated using attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy. The suppositories were prepared using the hot melt and trituration methods. Quality control checks were carried out on the formulations. The evaluated parameters included physical characteristics (texture, presence or absence of entrapped air, and contraction holes), weight uniformity, disintegration time, drug content, and in vitro release profile of the alum from the formulated suppositories. An in vivo analysis was carried out on the most suitable formulation to ascertain its efficacy on inflamed tissues using croton oil-induced rectal inflammation in a rat model. A critical examination of the ATR-FTIR spectra revealed no drug-base interactions. The suppository formulations passed all Pharmacopoeia stated tests. The in vivo study revealed the use of suppositories ameliorated the croton oil-induced hemorrhoid in the rectoanal region of the rats.

Effects of Qing Chang Suppository Powder and its Ingredients on IL-17 Signal Pathway in HT-29 Cells and DSS-induced Mice.

BACKGROUND: Qingchang Suppository, a formula used for more than 30 years in Longhua Hospital, has shown satisfactory clinical effects on Ulcerative Colitis (UC). However, its therapeutic mechanism has not been fully elucidated. PURPOSE: The study aims to investigate the effects of Qingchang Suppository powder (QCSP) and its ingredients by regulating the IL-17A signaling pathway which plays an important role in the development of UC. METHODS: HPLC was used to analyze the main ingredients (Gallic acid, Indigo, Indirubin) in QCSP. HT-29 cells were induced by rhIL-17A and TNF-α, and IL-17A related protein expressions were determined by western blot. BALB/C mice were induced by 4% Dextran Sodium sulfate (DSS). The effects of QCSP and its ingredients were evaluated by measuring weight loss, disease activity index (DAI), colon length, histological analysis. Western blot was used for analysis of IL-17A and MAPK related proteins p-ERK, p-JNK, p-P38. Quantitative reverse transcription polymerase chain reaction (q-PCR) was used to detect the expression of IL-17A, HSP90 and ACT1 in colon tissue. Cytokines such as IL-17A, IL-1ß, IFN-γ and TNF-α were determinated by enzyme-linked immunosorbent assay (ELISA). RESULTS: QCSP had good therapeutic effect on DSS-induced colitis in mice. QCSP significantly relieved weight loss, restored colon length, repaired colon lesions, reduced histological scores and DAI, decreased TNF-α, IL-1ß, IL-17 and IFN-γ contents, significantly suppressed the gene expressions of IL-17A, ACT1 and HSP90, and up-regulated the expressions of tight junction proteins like ZO-1 and Occludin. IL-17A pathway related proteins such as IL-17A, IL-17RA, HSP90, MAPKs, P-iκbα and iNOS were significantly increased in vitro and in vivo. CONCLUSIONS: This paper reveals that QCSP inhibited the IL-17A signaling pathway in HT-29 cells and DSS induced mice, presenting a new mechanism of QCS on treating UC.

Effect of Vitamin D3 in Composition of Original Rectal Suppositories on Parameter of Protein Oxidative Modification in Large Intestine in Experimental Ulcerative Colitis.

The effect of vitamin D3 in the composition of original rectal suppositories on the content of products of oxidative modification of proteins in mucous membrane of the large intestine was studied in rats with experimental ulcerative colitis provoked by a two-stage administration of 3% oxazolone. The rectal suppositories with vitamin D3 (1500 IU) were administered every 12 h during 5 days. Condition of the rats was assessed according to disease activity index (DAI), while the content of oxidative modification products of proteins in the homogenate of the mucous membrane was assayed with extraction-spectrophotometric method in the lesion focus of large intestine. DAI increased during entire observation period of ulcerative colitis, which correlated with the level of products of spontaneous and induced oxidative modification of proteins in mucous membrane of the colon. The study examined the pharmaceutical and technological features of novel rectal suppositories of original composition weighing 300 mg, which are based on polyethylene glycol supplemented with aqueous solution of vitamin D3 (10%). The use of rectal suppositories with vitamin D3 reduced DAI and inhibited the oxidative modification of proteins.

Anti-inflammation effect of Qingchang suppository in ulcerative colitis through JAK2/STAT3 signaling pathway in vitro and in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: Qingchang Suppository (QCS) is a Traditional Chinese Medicine formula (TCM) for Ulcerative Colitis (UC), which has been used for the treatment of UC for more than 30 years with therapeutic effect. This formula is optimized from a classic formula called "Qingdai San". Although some experiments have shown QCS effective for UC, its mechanism on UC is still unclear and needs to be clarified. AIM OF THE STUDY: To investigate the usage of QCS in our hospital, clarify the main compounds in QCS and their anti-inflammation effect both in vivo and in vitro. MATERIALS AND METHODS: Prescription analysis was performed in the clinical department and pharmacology network prediction was predicted for relative signal pathways. 2,4,6-Trinitrobenzenesulfonic acid (TNBS)-induced colitis rats and Lipopolysaccharide (LPS)-induced Caco-2 cell as an inflammatory model were used to evaluate the effect of QCS. RESULTS: QCS and its herbs were associated with inflammatory and immunological diseases. QCS and its ingredients showed little toxicity on Caco-2 cell and could down-regulate the level of Interleukin-6 (IL-6) and expression of signal transducer and activator of transcription 3 (P-STAT3 Tyr705) in LPS-induced Caco-2 cell. In an animal experiment, QCS and its ingredients (indigo and gallic acid) could alleviate the symptoms of TNBS-induced colitis of rats, significantly decrease pro-inflammatory factors and anti-inflammatory factors as well as inhibit the expressions of P-STAT3 and Tyr705. CONCLUSION: QCS and its components could improve UC by anti-inflammation. JAK2/STAT3 pathway might be the possible signaling pathway.

Vaginal suppositories of cumin seeds essential oil for treatment of vaginal candidiasis: Formulation, in vitro, in vivo, and clinical evaluation.

Fungal infections by resistant Candida species continue to be a significant health problem. Novel antifungal agents such as essential oils of cumin seeds (EOCS) are tested against vulvovaginal candidiasis (VVC). The aim of this study was to develop coated polyethylene glycol (PEG) vaginal suppositories containing EOCS for treatment of VVC. PEG suppositories containing EOCS were prepared ppearance, weight variation, drug content, hardness, dissolution time, release, stability and anticandida activity were evaluated. Biocompatibility of selected formulation was tested in female rabbits, followed by clinical evaluation. Coated suppositories showed complete release of the oil after 30 min, in vitro anti-candida activity, enhanced stability and sufficient safety on the vaginal tissues of rabbits. Clinical results showed significant lower rates of vaginal itching, discharge and dyspareunia combined with negative cultures in 70% of patients, revealing efficacy of EOCS-containing vaginal suppositories for treatment of VVC.

The preclinical discovery and development of rectal artesunate for the treatment of malaria in young children: a review of the evidence.

INTRODUCTION: Plasmodium falciparum, the deadliest malaria parasite, kills hundreds of thousands of people per year, mainly young children in Sub-Saharan Africa. Artesunate suppositories are recommended as pre-referral malaria treatment in remote endemic areas for severely ill children to prevent progression of the disease and to provide extra time for patients until the definitive severe malaria treatment can be administered. AREAS COVERED: The authors provide an overview of the discovery of artesunate and its different formulations focusing on rectal administration, summarizing key studies concerning the pharmacokinetic, pharmacodynamic, safety, tolerability and efficacy of rectal artesunate leading to WHO recommendation and market authorization in Africa. In addition, studies on acceptance and adherence to rectal artesunate administration and the post-launch status are also covered. EXPERT OPINION: Efforts by ministries of health in malaria endemic countries together with international health organizations should establish and enforce guidelines to ensure the correct use of artesunate suppositories only as pre-referral medication in presumed severe malaria cases to minimize the risk of abuse as a monotherapy for treatment of uncomplicated malaria. The priority is to not jeopardize the efficacy of artesunate and to prevent resistance development against this valuable drug class in Africa.

Neurogenic bowel treatments and continence outcomes in children and adults with myelomeningocele.

PURPOSE: Neurogenic bowel dysfunction (NBD) is a common comorbidity of myelomeningocele (MMC), the most common and severe form of spina bifida. The National Spina Bifida Patient Registry (NSBPR) is a research collaboration between the CDC and Spina Bifida Clinics. Fecal continence (continence) outcomes for common treatment modalities for NBD have not been described in a large sample of individuals with MMC. NSBPR patients with MMC and NBD were studied to determine variation in continence status and their ability to perform their treatment independently according to treatment modality and individual characteristics. METHODS: Continence was defined as < 1 episode of incontinence per month. Eleven common treatments were evaluated. Inclusion criteria were established diagnoses of both MMC and NBD, as well as age ⩾ 5 years (n= 3670). Chi-square or exact statistical tests were used for bivariate analyses. Logistic regression models were used to estimate the odds of continence outcomes by age, sex, race/ethnicity, level of motor function, and insurance status. RESULTS: At total of 3670 members of the NSBPR met inclusion criteria between November 2013 and December 2017. Overall prevalence of continence was 45%. Prevalence ranged from 40-69% across different treatments. Among continent individuals, 60% achieved continence without surgery. Antegrade enemas were the most commonly used treatment and had the highest associated continence rate. Ability to carry out a treatment independently increased with age. Multivariable logistic regression showed significantly higher odds of continence among individuals aged ⩾ 12 years, female, non-Hispanic white, and with private insurance.

[A multicenter, randomized, open and positive parallel controlled clinical study of clotrimazole vaginal expansion suppository and vaginal tablet in the treatment of mild and moderate vulvovaginal candidiasis].

Objective: Using clotrimazole vaginal tablet as a positive control, to evaluate the results of clotrimazole vaginal expansion suppository in the treatment of mild and moderate vulvovaginal candidiasis in terms of efficacy, patient satisfaction, side effects, and recurrence rate. Methods: This study was jointly conducted by 5 hospitals from August 2017 to October 2018, patients with mild and moderate vulvovaginal candidiasis confirmed by fungal culture and symptoms scores were selected. They were randomized to experimental group and control group as 1∶1 ratio. In the experimental group (n=105), the subjects applied clotrimazole vaginal expansion suppository (150 mg) daily at night for 7 days. In the control group (n=106), the subjects used a single dose of clotrimazole vaginal tablet (500 mg). Follow-ups were performed at (8±3) and (30±5) days after the discontinuation of the drugs, respectively. The difference in clinical symptoms and signs scores was used to evaluate the improvement of clinical symptoms, and the patient's satisfaction and side effects were recorded. Results: At the first follow-up, the experimental group and control group were followed up by fungal culture on the cure rate [66.7% (70/105) versus 63.2% (67/106), P>0.05] and total effective rate [98.1% (103/105) versus 99.1% (105/106), P>0.05], the differences were not statistically significant. At the second follow-up, the recurrence rates of the experimental group and the control group were 5.7% (4/70) and 14.9% (10/67), respectively, with no significant difference (P>0.05). In the evaluation of patient satisfaction, the leakage of the drug in the experimental group was significantly better than that in the control group (P<0.01). The side effects mainly included vaginal stimulation, itching and burning sensation, and there was no statistical difference between the two groups (χ2=1.070, P=0.586). Conclusions: In the treatment of mild and moderate vulvovaginal candidiasis, clotrimazole vaginal expansion suppository is no less effective than clotrimazole vaginal tablet, and there is no significant difference in the recurrence rate between the two. In terms of patient satisfaction, clotrimazole vaginal expansion suppository is superior to clotrimazole vaginal tablet.

Effect of a novel herbal vaginal suppository containing myrtle and oak gall in the treatment of vaginitis: a randomized clinical trial.

BACKGROUND: Uncomplicated infections such as candidiasis, bacterial vaginosis (BV), or trichomoniasis are easy to diagnose and treat. However, about 8% of patients will have a more complicated course with failure to respond to treatment or rapid recurrence of symptoms. There are many suggestions in Traditional Persian Medicine like myrtle (Myrtus communis L.) and oak gall (Quercus infectoria G.Olivier) for treatment of vaginitis. OBJECTIVES: A clinical trial was designed to assess the efficacy of a novel herbal suppository, containing myrtle and oak gall (MOGS) in treatment of vaginitis. METHODS: In a parallel randomized clinical trial, 120 women with vaginitis were randomly assigned to MOGS, metronidazole, or placebo. Formulation was simulated from traditional Persian manuscripts and MGOS was prepared after pharmaceutical optimization processing as well as quantification of gallic acid by HPLC. The study was double-blind for MOGS and placebo and single-blind for metronidazole group. RESULTS: MOGS effectively improved vaginal discharge (p = 0.024 for BV and 0.018 for trichomoniasis) and pH (compared to placebo (p = 0.013) and metronidazole (p = 0.001)). Both MOGS and metronidazole could reverse whiff test. Metronidazole was the best medication for making Nugent score negative (p = 0.005) as well as the best therapy according to laboratory findings to treat BV in comparison with placebo (p = 0.021). While for trichomoniasis, MOGS could improve the disease more successfully (p = 0.001). Both MOGS and metronidazole treated mixed vaginitis (p = 0.002). CONCLUSION: MOGS would be a chance for developing new treatment for trichomoniasis.

Antioxidant Effects of Turmeric Extract in Rectal Suppositories of Original Composition in Experimental Crohn's Disease.

We studied the effect of turmeric extract in the composition of rectal suppositories on the level of LPO products and oxidative modification of proteins in the colon mucosa of Wistar rats with experimental Crohn's disease modeled by rectal administration of trinitrobenzenesulfonic acid. The suppositories containing turmeric extract were administered 12 h after disease induction. On days 3, 5, and 7 of the experiment, clinical parameters of the disease were scored using disease activity scale (DAI) and the concentration of LPO products and intensity of oxidative modification of proteins were measured by the extraction-spectrofluorimetric method. Administration turmeric extract in rectal suppositories reduced the severity of clinical symptoms, the level of LPO products (mostly in the isopropanol phase of the lipid extract), and the total content of products of oxidative modification of proteins. Moreover, correlations between DAI and concentration of LPO products in the colon were found.

Investigating the effect of vitamin D vaginal suppository on sexual function among postmenopausal women: study protocol for a randomized controlled trial.

BACKGROUND: Menopause is associated with changes in sexual function which are partly due to vaginal atrophy in response to estrogen reduction. Estrogen administration temporarily reduces the symptoms of vaginal dryness, but long-term exposure to this drug is likely to be associated with serious complications. Considering the promising results of previous studies concerning the effect of vitamin D on vaginal dryness, the proposed study will investigate the effect of vitamin D vaginal suppository on the sexual function of postmenopausal women. METHODS: In a randomized, controlled clinical trial, 105 postmenopausal women will be randomly assigned to three groups receiving vitamin D vaginal suppository, placebo vaginal suppository, or control (no intervention). Vitamin D vaginal suppositories contain 1000 units of vitamin D3. The timing of the use of vitamin D vaginal suppositories and placebo suppositories will be every night in the first 2 weeks, and every other night in the following 6 weeks (8 weeks in total). The primary outcome will be the sexual function of participants which will be assessed using the Female Sexual Function Index (FSFI) before and immediately after the intervention, and at 1 and 2 months after the end of the intervention. The side effects of these suppositories will be examined as a secondary consequence of the study. Data will be analyzed using SPSS software version 25. In the case of normal distribution of data, the mean score of sexual function will be compared between the groups using a repeated measurements ANOVA. If statistical analysis leads to significant results, the post-hoc test will be used to determine the differences between the groups. Comparison of demographic and fertility characteristics of the women will be carried out using statistical tests such as chi-squares and t-tests. A significance level of p < .05 will be used for statistical analyses. DISCUSSION: If vitamin D vaginal suppositories improve sexual function among premenopausal women with long-term effects and minimum side effects, the suppositories will be considered a safe complementary and alternative choice for alleviating sexual dysfunction among this group. TRIAL REGISTRATION: IRCT20180704040346N1 at 2018-10-13 prospectively registered.

The association of Boswellia resin extract and propolis derived polyphenols can improve quality of life in patients affected by prostatitis-like symptoms.

OBJECTIVES: Chronic prostatitis syndrome is a bothering and poorly understood condition. Many patients report genitourinary pain and Lower Urinary Tract Symptoms as a main complaint. Many different pharmacological or behavioural therapies are prescribed in daily clinical practice, but efficacy data are still lacking. The aim of our study was to test the efficacy and safety of a transrectal delivered association of Boswellia resin extract and propolis derived polyphenols for the relief of prostatitis - like symptoms. MATERIALS AND METHODS: Patients affected by chronic/recurrent prostatitis - like symptoms were prospectively enrolled in our study from December, 2016 to December, 2018. Patients were screened at baseline through clinical examination and validated questionnaires administration: Chronic Prostatitis Symptom Index (CPSI), International Prostate Symptom Score (IPSS), International Index of Erectile Function (IIEF). Inclusion criteria were: age ≥ 18; prostatitis symptoms persisting for at least 3 of the last 6 months; CPSI pain domain score ≥ 5; previous negative Meares-Stamey test. Treatment consisted on the administration of 1 suppository containing Boswellia resin extract and propolis derived polyphenols, once a day for 20 days. The primary endpoint of the study was the improvement of quality of life after treatment, defined by a reduction of ≥ 2 points, or ≥ 25%, of mean CPSI pain domain score, compared to baseline. Secondary endpoints were the improvement of post-treatment CPSI total score and the analysis of treatment - related adverse events. All patients were re-evaluated 1 month after treatment. RESULTS: 40 patients were enrolled in our study. Median age (Inter - Quartile Range IQR) was 51.5 (41.5-63.2) years. Mean baseline CPSI scores were: 22.15 (total score), 9.67 (pain domain), 5.15 (micturition domain) and 7.35 (quality of life domain), respectively. No significant adverse events were reported. At 1 month follow-up, CPSI scores appeared modified as follows: 16.40 (total score, p = 0.001); 6.92 (pain domain; p = 0.001; 4.02 (micturition domain, p = 0.09); 5.45 (quality of life domain, p = 0.002). Mean CPSI pain domain score reduction was -2.75 points (-28.5%). Mean CPSI total score reduction was -5.75 points (-26%). CONCLUSIONS: The association of Boswellia resin extract and propolis derived polyphenols can reduce genitourinary pain and then improve quality of life of men affected by bothersome prostatitis - like symptoms.

Development of an Indigo Naturalis Suppository for Topical Induction Therapy in Patients with Ulcerative Colitis.

BACKGROUND: Indigo naturalis (IN) consists of ligands for the aryl hydrocarbon receptor and exhibits anti-inflammatory effects. Previously, we demonstrated that an 8-week treatment with oral IN is effective in inducing a clinical response in patients with ulcerative colitis (UC). Some UC patients with proctitis are refractory to topical mesalamine or corticosteroids and therefore require an alternative topical treatment. OBJECTIVES: We aimed to prospectively evaluate the safety and efficacy of IN suppositories in UC patients. METHOD: We performed an open-label, single-center, prospective pilot study from February 2018 to October 2018. A total of 10 patients with active UC, who had moderate to severe inflammation from the rectum to the sigmoid colon, were enrolled. The patients received a daily dose of 50 mg IN suppository for 4 weeks. The primary endpoint was safety at week 4. RESULTS: Although 1 patient experienced anal pain, no serious adverse events were observed. At week 4, the rates of clinical remission and mucosal healing were 30 and 40%, respectively. Mayo rectal bleeding subscores significantly improved after treatment (1.80 ± 0.13 vs. 0.90 ± 0.28; p = 0.009). Approximately 80% of the patients with a baseline Mayo endoscopic subscore in the rectum (r-MES) of 2 achieved mucosal healing, but those with a baseline r-MES of 3 did not. CONCLUSIONS: We found that 4 weeks of IN suppository can be tolerated by UC patients, but its efficacy was limited by the severity of the disease. Further investigation will be needed in order to confirm the optimum dose of IN suppository for patients with UC.