Suppositories Research Articles

EXPERIMENTAL STUDY OF ANTIMICROBIAL PROPERTIES AND ACUTE TOXICITY OF THE PEO-BASED COMBINED SUPPOSITORIES

Aim. The research of antimicrobial and toxicological parameters of a promising pharmaceutical composition with indole-3-carbinol and meloxicam in the form of rectal suppositories. Materials and methods. The research of antimicrobial activity was carried out in vitro by diffusion in nutrient agar in the modification of "holes" on the reference strains of common pathogens Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis, Candida albicans. Adult rats were used for the study of acute toxicity. Suppository mass were administrated in the largest possible volume rectally or orally. The animals were periodically monitored according to the experimental plan – the assessment of physiological parameters before administration and after 6, 12, 18, 24 hours, at 3, 7 and 14 days. The animals were removed from experiment and necropsy provided after 1, 3, 7, and 14 days. Results. The sizes of zones of inhibition of the microorganisms growth were most significant (from 19.27±0.61 mm of E. coli to 40.80±0.42 mm of S. aureus) near sample of the combined composition suppository compared with other combination of active substances and excipients. During the observation of animals for 14 days and the study of internal organs after autopsy, deviations in physiological (weight, temperature, activity, respiratory rate) and macroscopic morphological indicators of animals from reference values were not detected. Conclusion. According to the results of microbiological studies, a moderate antimicrobial effect of suppositories of combined composition in relation to all the studied pathogens was revealed. The absence of manifestations of acute toxicity allows us to conclude that the pharmaceutical composition can be classified as practically non-toxic substances. The obtained results allow us to recommend a pharmaceutical composition with indole-3-carbinol and meloxicam on a polyethylene oxide basis in the form of suppositories for further preclinical studies of specific pharmacological effects as a prostate protective agent.

Preparation and Standardization of Jatyadi Ghrita Rectal Suppository

Jatyadi Ghrita is a very well known formulation used for wound healing, anorectal disorders like fissure, fistula or any chronic wound. These wound healing properties of Jatyadi ghrita can be used in modern dosage form like suppository, suppositories are used to improve local effect of Jatyadi ghrita because of its easy application and minimum local discomfort. These suppositories are made by fusion or melt method by using cocoa butter as a base, and melted mixture of both are poured into molds and after cooling suppositories are collected from molds and stored in fridge. Temperatures plays major role in preparation of this fusion or melt method suppositories. An attempt has been made for preparation and standardization of Jatyadi ghrita suppositories. Standard Preparation method and Visual examination, melting point, liquefaction time of suppositories are studied under this project.

Effect of hyoscine–n-butyl bromide (Buscopan) rectal suppository in active phase of labour in primigravida

Introduction: Labour is a physiological process characterized by onset of uterine contractions leading to progressive increase in frequency, intensity and duration of uterine contractions, effacement and dilatation of cervix with descent of foetus through birth canal resulting in delivery of foetus with placenta and membranes. Hyoscine butyl bromide is most commonly used in labour room and has variable results in both primigravida and multigravida. Aim and Objective: 1. To evaluate the efficacy of Hyoscine-n- butyl bromide (buscopan) suppository in the active phase of labour in a primigravida.2. To evaluate the maternal and fetal complications of using the buscopan suppository. Materials and Methodology: Primigravida with gestational age 37 completed weeks - 40 weeks admitted in the labour ward with spontaneous onset of labour or induced labour who-fulfil the inclusion & exclusion criteria were randomly selected in this study after taking informed consent. Study group: 150 pregnant women at the initiation of active phase allowed forlabour with instillation of single dose of Buscopan rectal suppository (10 mg) in active phase for cervical dilatation. Control group: 150 pregnant women at the initiation of active phase allowed forlabour without any drug for cervical dilatation. Study Design: Prospective case control study. Result: The mean duration of active phase of labour in study group is 3 hours 10 minutes & in control 5 hours 44 minutes. The difference between both the groups was statistically significant (‘p’ value < 0.001). No significant difference in maternal and fetal complications between study group and control group. Conclusion: Buscopan suppository was very effective in reducing the duration of active phase of labour by promoting cervical dilatation. There was no significant second or third stage complication with the use of the drug. No untoward side effects were noted in the mother or foetus.

Efficacy of chymotrypsin in the prevention of postendoscopic retrograde cholangiopancreatography pancreatitis

EnBackgroundPancreatitis is common after endoscopic retrograde cholangiopancreatography (ERCP).AimTo assess the pharmacological effect of diclofenac, allopurinol and chymotrypsin in the prevention of postendoscopic retrograde cholangiopancreatography pancreatitis (PEP).Settings and designCalcular obstructive jaundice patients without pancreatitis scheduled for ERCP were randomized into three groups.Materials and methodsThe diclofenac group received 200 mg rectal suppositories immediately after ERCP, allopurinol received oral 300 mg 3 h before ERCP, and chymotrypsin received intramuscular injection immediately after ERCP. Serum amylase and lipase were measured before, 1, 6, and 24 h after ERCP and procedure-related risk factors for post-ERCP pancreatitis were recorded. Pancreatitis was considered when serum amylase or lipase levels elevated more than three times the upper limit of normal with newly developed abdominal pain lasting at least 24 h after ERCP.Statistical analysisAnalysis of variance for continuous variables and χ2 for categorical variables.ResultsOne hundred and fifty patients were included; diclofenac group (58 patients, 29 men, mean age 46.9±13.2 years), allopurinol (38 patients, 20 men, mean age 43.1±14.7 years) and chymotrypsin (54 patients, 28 men, mean age 40.6±17.3 years). Twelve (8%) patients developed PEP: the diclofenac group (n=4; 6.9%), allopurinol (n=6; 15.8%) while chymotrypsin (n=2; 3.7%), but this was not statistically significant (P=0.318). In patients who received chymotrypsin, regression of serum amylase and lipase to normal levels was much better compared with the other groups and was associated with better clinical improvement.ConclusionChymotrypsin and allopurinol are comparable to diclofenac in the prevention of pancreatitis post-ERCP. Beside its prophylactic role, chymotrypsin could be effective in rapid improvement if PEP occurs.

DEVICE-FORM FOR PREPARING RECTAL AND VAGINAL SUPPLEMENTS

Оbjective -аccording to the calculations, the technical drawings and a technologicalmap, to make an experimental device-form for the preparation of rectal and vaginalsuppositories by pouring and pressing using hydrophobic and hydrophilic bases.Materials and methods. Authors had put attantion on positive characteristics andavailability of matherials chosen for the device. The material for the manufacture of partsof the mold-shaped material was tin bronze (10% tin, 90% refined copper) and steelgrade 12ChNZA (chromium-nickel alloy stainless steel of high quality). For thepreparation of suppositories using the device-form, the prescribed medicines are mixedwith the appropriate pre-prepared base, the form is prepared, the prepared and semicooled mass is poured into the working nest of device. After cooling, disassemble thedevice and release the ready-made suppositories.Results. The tin bronze, from which the steady-state form is made, is resistant to theaction of physico-chemical factors of the environment and corrosion, has a high thermalconductivity. Significant ductility of the alloy allows for machining parts of the deviceform to obtain high purity of the working surfaces. Given the shortcomings of the existingmeans of suppository production as an important dosage form and guided by therequirements of the State Pharmacopoeia of Ukraine, an original, structurally simple,reliable in operation, durable in service, productive and hygienic device-form for thepreparation of rectal and vaginal suppositories on the basis of the necessary composition.Conclusions. The presented device-form is simple and reliable in operation; made of analloy that allows the manufacture of suppositories in accordance with the requirements ofthe State Pharmacopoeia of Ukraine and meets the criteria formulated by the authors(relative cheapness of starting materials, corrosion resistance, antifriction, plasticity,high thermal conductivity, sterilization by various methods).

Применение цитомединов при наличии органного компонента хронического простатита по классификации UPOINT

chronic prostatitis is a common disease that significantly influence on the quality of life. Our aim was to assess the prevalence of particular domains of UPOINT classification and determine the efficiency of prostate-selective cytomedins in complex therapy of chronic prostatitis with the predominance of organic component. a total of 96 patients aged from 24 to 48 years were treated in City clinical hospital named after D.D. Pletnev in 2017-2018 yy. with a previously diagnosed chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS). The mean duration of the disease was 18.0+/-6.2 months. The total NIH-CPSI score was 24+/-7.3 (pain score 9+/-4.9, urinary score 7+/-2,7, quality of life 8+/-2.3), Qmax was 16+/-4.2 ml/s, prostate volume - 34+/-12 cc. Leukocyturia in post-massage urine was found in 52 patients (54%). Positive urine culture after prostate massage or positive bacterial semen study were found in 22 patients (23%). Prostate-specific therapy consisted of 20 days of rectal suppositories Vitaprost-forte followed by oral therapy by Vitaprost tablet of the same duration. Follow-up examination of 72 patients (75%) was performed after 3 months of therapy. The total NIH-CSPI score decreased to 15.6+/-5.1 (pain score 6.3+/-3.8, urinary score 4.6+/-2.2, quality of life 4.7+/-2), Qmax was 16+/-3.8 ml/s and mean prostate volume was 24+/-6 cc. The normalization of laboratory parameters was achieved in all cases. using the UPOINT classification allows to optimize the treatment of patients with chronic prostatitis. Use of prostate-specific cytomedins (Vitaprost) is highly effective in case of prostatic involvement according to the UPOINT classification.

New Records of Four Species of Dactylogyrus (Monogenea: Dactylogyridae) from Goldfish, Carassius auratus (Linnaeus, 1758) (Pisces: Cyprinidae), in Cuba

Four species of Dactylogyrus were found on gills of goldfish (Carassius auratus) in Cuba. The collected monogeneans were fixed in ammonium picrate and glycerin solution and mounted in glycerin gelatin. The species were identified based on morphological characteristics and measurements, and the 4 dactylogyrids were identified as D. dulkeiti Bychowsky, 1936; D. baueri Gussev, 1955; D. formosus Kulwiec, 1927; and D. intermedius Weger, 1910, which are new records from goldfish in Cuba.

A comparative study of efficacy of diclofenac sodium and paracetamol as rectal suppositories in post-operative pain relief in children undergoing adenotonsillectomy

Background: Due to less compliance in children to injectables, under treatment of post-operative pain occur in a substantial percentage of children. Such pain in children may pose cardiovascular, respiratory and metabolic disturbances in the immediate post operative period and anxiety, fear, and sleep disturbances in later life. Aim and Objectives: To assess and compare the analgesic efficacy of Diclofenac sodium and Paracetamol, administered as rectal suppositories, during immediate post-operative period in children undergoing adenotonsillectomy. Materials and Methods: A total of 100 ASA grade I / II Children in the age group of 5 – 12 years admitted to undergo elective adenotonsillectomy were included in this study and allocated to two groups of 50 each. Group D patients received Diclofinac 1mg./ Kg 8th hourly and Group P received paractemol 40mg/kg bolus dose, 20mg/kg every 6th hourly suppositories for post-operative pain relief. Postoperative pain assessment was done with Objective pain scale and scoring system every 2 hours for a period of 24 hours. Results: The 4th hourly mean of the pain scores were almost the same in both the groups. Also none of the patients had a pain score of more than 5 and hence none of them received rescue analgesics. Conclusion: Diclofenac sodium and Paracetamol, administered as rectal suppositories, in children undergoing adenotonsillectomy are effective means of pain relief during immediate post-operative period. Both the drugs are equal on their analgesic efficacy.

Inert natural killer/T-cell lymphoma with large cell transformation: report of one case and review of literature

Objective To investigate the clinicopathologic features of inert natural killer/T (NK/T)-cell lymphoma with CD30-positive large cell transformation. Methods The pathological data of one patient diagnosed as inert NK/T-cell lymphoma with CD30-positive large cell transformation in the Third Hospital Affiliated to Soochow University from April 2006 to March 2017 were collected. The histopathological features and immunohistochemical phenotype of the patient were observed and followed up. Results The patient received biopsy twice in April 2006 and March 2017. The first tumorectomy in sacral canal showed that diffuse and small lymphoid cell hyperplasia, irregular nucleus, granular chromatin, unobvious nucleolus, focal necrosis. Immunohistochemistry showed CD20(-), CD3(-), ALK(-), CD30(-), CD43(+), CD2(+), CD56(+), TIA-1(+), GrB(+), CD4(-), CD8(-). Finally, the patient was diagnosed as extranodal NK/T-cell lymphoma, nasal type. The microscopic examinations after the second left cervical lymph node biopsy showed large cells infiltrated into the background of small lymphocytes, plentiful cytoplasm, large nuclei, irregular nucleus, part of nuclear folding, obvious nucleolus, mitotic figures visible, visible intravascular tumor suppository, consistent small lymphocytes. Blood vessel invasion could be seen, as wells as consistent small lymphocytes, regular form, less cytoplasm, rare nuclear fission. Immunohistochemistry showed AE1/AE3(-), CD20(-), CD3(+), ALK(-), CD30(+), CD43(+), CD2(+), EMA(-), Ki-67(70%+), CD56(+), TIA-1(+), GrB(+), CD4(-), CD8(-). Finally, the patient was diagnosed as NK/T-cell lymphoma, nasal, recurrence. In situ hybridization showed EB virus encoded RNA (EBER) was positive for two biopsies. Conclusions Inert extranodal NK/T-cell lymphoma is very rare. The pathogenesis is closely related to EB virus infection. Its diagnosis must rely on histopathology and immunohistochemistry. Key words: Natural killer/T-cell lymphoma, nasal type; Inert; Epstein-Barr virus

Effects of multimodal analgesia on cochlear implantation in children

Objective To investigate the effects of multimodal analgesia on cochlear implantation in children. Methods Eighty four child patients [1-6 years, American Society of Anesthesiologists (ASA) grade Ⅰor Ⅱ] scheduled for unilateral cochlear implantation were enrolled. They were randomly divided into three groups (n=28): a patient controlled intravenous analgesia (PCIA) group (group A), a PCIA and ropivacaine wound infiltration group (group B), and a PCIA, ropivacaine wound infiltration and paracetamol suppository group (group C). Both groups B and C received 0.25% ropivacaine (1 ml/kg) for wound infiltration after anesthesia induction. Meanwhile, group C was treated with 30-40 mg/kg paracetamol suppository 15 min before operation. Patients in all groups were given combined intravenous and inhaled anesthesia. Then, the heart rate, mean arterial pressure (MAP), oxygen saturation (SpO2) and postanesthesia care unit (PACU) stay, and adverse reactions were recorded immediately after waking (T0), 4 h after surgery (T1), 8 h after surgery (T2), 12 h after surgery (T3), 24 h after surgery (T4), 36 h after surgery (T5), and 48 h after surgery (T6). The Face, Legs, Activity, Cry and Consolability Scale (FLACC) scores and Ramsay scores were recorded at each time points above. The Pediatric Anesthesia Emergence Delirium (PAED) score was recorded at T0. Results Markedly decreased heart rate and MAP were found in group C at T0 and T1, in comparison with groups A and B (P 0.05). Compared with group A, groups B and C showed remarkable decreases in FLACC score at T0-T6(P 0.05). Conclusions Multimodal analgesia including ropivacaine wound infiltration, anal plug medication of paracetamol suppository and PCIA can improve the effects of postoperative analgesia and decrease the incidence of emergence agitation. Key words: Cochlear implantation; Multimodal analgesia

Rectal Suppositories in Children: ‘Up’ may be the Way to Go!

Rectal Suppositories in Children: ‘Up’ may be the Way to Go!

The optimal choice of therapy for acute hemorrhoids

The article presents the results of conservative therapy of patients with acute hemorrhoids, with a 10-day follow-up period, the purpose of which is to improve the results of treatment of this category of patients. The patients of Group I received conservative therapy with heparin ointment and Relief Pro® suppositories; Group II received local therapy with heparin ointment without rectal suppositories. Design: a single-center randomized controlled follow-up study. The study showed the efficacy of Relief Pro® suppositories in patients with acute haemorrhoids. The use of suppositories allowed to statistically reliably reduce the level of pain (2.59 ± 0.6 points in Group I versus 3.87 ± 0.7 points in Group II (p &lt; 0.05)) on Day 3 of the therapy, reduce the frequency of blood excretion on Day 2 of the therapy (83% and 32% of patients, respectively (p &lt;0.05)) and eliminate the discomfort in the anus (100% observations in Group I by Day 5 of the therapy and 67% in Group 2 by Day 10 of the therapy (p &lt;0.05)).

Conservative treatment of hemorrhoids: focus on combination tribenoside and lidocaine

Hemorrhoidal disease has been known since ancient times and remains one of the most common human diseases. This review presents the results of tribenoside and lidocaine combinations used in the conservative therapy of hemorrhoids, which give grounds to recommend combination therapy with tribenoside and lidocaine in the form of rectal cream and rectal suppositories as an effective and safe method of local treatment of hemorrhoids and moderate severity in different categories of patients, allowing to achieve rapid clinical improvement.

Development of the composition and research of the equivalence of suppositories with diclofenac sodium by in vitro method using “Dissolution” test for lipophilic solid dosage forms

T he aim : Development of the composition and investigation of the equivalence of suppositories with sodium diclofenac by in vitro method on a device with a flow-through cell in accordance with modern requirements of SPhU. M aterials and methods : The development of the suppository composition was carried out with the use of the substance of diclofenac sodium and the excipient of solid fat of various grades. Studies of the active ingredient release in vitro in comparison with the reference listed drug were carried out on a device with a flow-through cell according to the monograph SPhU 2.9.42. Results : The investigations of the physical-chemical properties of the diclofenac sodium substance (micronisation, solubility) and the basis of the solid fat carrier, which affect the release of the active ingredient from the drug formulation were carried. The particle size figure for 2 samples of the active ingredient was from 100 μm to 400 μm and not more than 15 μm, respectively. The optimal composition of suppositories was developed by the method of 2-factor experiments. The conditions for the Dissolution test were determined: the volume of the medium (720 ml), the dissolution temperature (37.0 ± 0.5) oC, the time taken for sampling (15, 30, 45, 60, 90 min), the dissolution medium – buffered solution with a pH of 7.4. The calculated similarity factor f 2 was 67, which indicates the similarity of the release profiles and the equivalence of the researched drug. C onclusions The pharmaco-technological properties of sodium diclofenac and the solid fat auxiliary substance were studied. A method for the release of sodium diclofenac with the use of a device with a flow-through cell in accordance with the requirements of the SPhU is developed. The level of release of sodium diclofenac in the dissolution medium from rectal suppositories was determined by the experimental method, as the first step in the bioavailability determination. The equivalence of the tested samples of suppositories with the reference listed drug with the help of the method in vitro was established.

Analysis of the efficacy of lactobacillus vaginalis capsule in the treatment of senile vaginitis

Objective To explore the effect of lactobacillus vaginal capsule in the treatment of senile vaginitis. Methods From January 2017 to February 2018, 100 elderly patients with vaginitis in the Second People's Hospital of Haining were selected in the study. They were randomly divided into observation group and control group according to the digital table, with 50 cases in each group. The observation group was treated by lactobacillus vagina capsule, and the control group was treated by compound metronidazole suppository. The clinical effects of the two groups were compared. Results The total effective rate of the observation group (96.00%) was significantly higher than that of the control group(76.00%), the difference was statistically significant(χ2=12.547, P 0.05], and there were statistically significant differences in vaginal pH of the two groups before and after treatment(t=8.204, 5.112, all P<0.05), the vaginal pH of the observation group after treatment was significantly lower than that of the control group, the difference was statistically significant[(4.49±0.11) vs. (5.76±0.37), t=5.024, P<0.05]. In the observation group, only 1 case had recurrence at 2 months after treatment, and no recurrence was observed at 3 months and 6 months after treatment, the recurrence rate was 2.00%. In the control group, there were 2 cases, 4 cases, 6 cases had recurrence at 2 months, 3 months and 6 months after treatment, and the recurrence rate was 24.00%. The recurrence rate of the observation group was significantly lower than that of the control group (χ2=25.634, P<0.05). Conclusion Lactobacillus vaginal capsule in the treatment of senile vaginitis has curative effect is distinct, the recurrence rate is low, also the use process is very simple, has high clinical application value. Key words: Vaginitis; Lactobacillaceae; Capsules; Metronidazole; Suppository; Recurrence; Comparative effectiveness research; Aged

Administering a suppository: types, considerations and procedure.

Administering a suppository: types, considerations and procedure.

Study of excipients influence on the cranberry oil releasing from the rectal suppository

Cranberry oil is a sufficiently perspective compound for using in the semisolid rectal dosage forms because it possesses regenerating, antioxidative, anti-inflammatory actions together with practical toxicity absence. The aim of this work is the study of influence of the excipients, which are used in suppository manufacturing (delivery bases and surfactants) on the biopharmaceutical characteristics of the rectal dosage form with cranberry oil. Materials and methods . Concentration of surfactants in all rests was 2 % from the suppository mass, cranberry oil contain was 0.25 g in each suppository taking into account data of the advance investigations. Study was carried out according to plan of single-factor analysis of variance with repeated observations. Releasing of cranberry oil from the suppositories was chosen as a parameter of optimization for the first step of biopharmaceutical availability study. The study was carried out by equilibrium dialysis method by Kruvchinsky at the temperature 37.0 ± 0.5 oС through the semipermeable film “Kuprofan”. After 30 minutes the antioxidative activity was set on the model of non-fermentative initiation of the free radical oxygenation in all dialysates. Results . According to the presented data factor A (sort of base) and factor B (sort of surfactant) make significant influence on cranberry oil releasing from the suppositories (F exp. >F tabl ). At the same time influence of the surfactants sort is slightly more significant than for the base. Also, interaction between these factors was statistically significant. On the base of obtained data, the range of influence of studied factors on the intensity of releasing of cranberry oil bioactive substances from suppository formulation was arranged: В > А > A x B. Conclusions. Variance analysis of results revealed that formulation with confectionary solid butter and emulsifier №1 provide optimal releasing of cranberry oil from the suppositories.

Prostate-protective action of combined composition suppositories with indole-3-carbinol and meloxicam on model of sulpiride-induced benign prosate hyperplasia

Benign prostatic hyperplasia in rats after chronic administration of sulpiride was corrected by administration (rectal suppositories) containing indole-3-carbinol and meloxicam. Established that suppositories correct the mass coefficients of the sex glands, the degree of androgenization of the organism of male rats, positively effect on concentration of fructose in seminal vesicles, activity of phosphatases and function of urinary system. Suppositories do not have a gonadotoxic effect, contribute to normalization of the hormonal function of testes with improving of spermatogenesis. A significant decrease of pathological changes in the gland at cellular level revealed: normalization of 5α-reductase activity, concentration of sex hormone receptors, as result of the specific activity of active ingredient of suppositories - indol-3-carbinol. The expressive prostate-protective action of the combined composition suppositories exceeds such a reference preparation – suppositories with pumpkin seed oil.

Formulation of Paediatric Paracetamol Suppositories Using Shea Butter and Dika Fat as Suppository Bases

Formulation of Paediatric Paracetamol Suppositories Using Shea Butter and Dika Fat as Suppository Bases

Comparative Assessment of the Analgesic Efficacy of Tramadol and Diclofenac Sodium Rectal Suppository in Subjects Undergoing Laproscopic Tubal Ligation

Background: Several drugs such as NSAID s or opiods can be used orally, intravenously or intramuscularly for treatment of post operative pain. The aim of our study was to compare the analgesic efficacy of tramadol and diclofenac sodium suppository and the secondary aim was to monitor and treat the complications if any. Subjects and Methods: Fifty female patients of ASA I and II in the age group of 24-42 posted for laproscopic tubal ligation were enrolled in the study. Verbal analogue scale (0- no pain to 10- worst possible pain) score reading was explained. In the pre operative room all the patients were randomly allocated in two groups by a computer generated list. Post operatively all the hemodynamic parameters and VAS score were recorded at regular intervals of 1, 2, 4, 6, 8, 10,12hrs. Pain was assessed by a staff trained to VAS score assessment and was blinded to the study group. Side effects of nausea and vomiting were noted. Results: Group 2 had high mean age of the study participants compared to group 1 but the comparison was non-significant.(p≤0.05) Only one patient in group A (tramadol) complained of nausea and vomiting. In group A 69% patients needed 1 rescue analgesic at 8 hrs, 11% at 6hrs, 9% at 4hrs and 11% at 10 hrs whereas in group B 64.1% patients needed 1 rescue analgesic at 8hrs, 16.2% at 10 hrs and 19.7 % at12 hrs. &nbsp;Conclusion: From above findings it was concluded that analgesic efficacy of tramadol and diclofenac sodium suppository is comparable. Rectal administration of tramadol reduces the incidence of nausea and vomiting.