Mesalamine suppositories have been used widely for the treatment of distal ulcerative colitis and considered to be safer than systemic administration for its limited systemic absorption.However,previous studies have s...Mesalamine suppositories have been used widely for the treatment of distal ulcerative colitis and considered to be safer than systemic administration for its limited systemic absorption.However,previous studies have shown that mesalamine suppository occasionally causes severe hypersensitivity reactions including fever,rashes,colitis exacerbation and acute eosinophilic pneumonia.Here we present a 25-year-old woman with ulcerative colitis with bloody diarrhea accompanied by abdominal pain and fever which were aggravated after introduction of mesalamine suppositories.In light of symptom exacerbation of ulcerative colitis,increased inflammatory injury of colon mucosa shown by colonoscopy and elevated peripheral eosinophil count after mesalamine suppositories administration,and the Naranjo algorithm score of 10,the possibility of hypersensitivity reaction to mesalamine suppositories should be considered,warning us to be aware of this potential reaction after administration of mesalamine formulations even if it is the suppositories.展开更多
AIM: To compare the efficacy and safety of recombinant streptokinase(rSK) vs hydrocortisone acetate-based suppositories in acute hemorrhoidal disease.METHODS: A multicenter(11 sites), randomized(1:1:1), open, controll...AIM: To compare the efficacy and safety of recombinant streptokinase(rSK) vs hydrocortisone acetate-based suppositories in acute hemorrhoidal disease.METHODS: A multicenter(11 sites), randomized(1:1:1), open, controlled trial with parallel groups was performed. All participating patients gave their written,informed consent. After inclusion, patients with acute symptoms of hemorrhoids were centrally randomized to receive, as outpatients, by the rectal route, suppositories of rSK 200000 IU of one unit every 8 h(first 3 units)and afterwards every 12 h until 8 administrations were completed(schedule A), one unit every 8 h until 6 units were completed(schedule B), or 25 mg hydrocortisone acetate once every 8 h up to a maximum of 24 administrations. Evaluations were performed at 3, 5,and 10 d post-inclusion. The main end-point was the 5thday response(disappearance of pain and bleeding, and≥ 70% reduction of the lesion size). Time to response and need for thrombectomy were secondary efficacy variables. Adverse events were also evaluated.RESULTS: Groups were homogeneous with regards to demographic and baseline characteristics. Fifth day complete response rates were 156/170(91.8%; 95%CI:87.3-96.2), 155/170(91.2%; 95%CI: 86.6%-95.7%),and 46/170(27.1%; 95%CI: 20.1%-34.0%) with rSK(schedule A and B) and hydrocortisone acetate suppositories, respectively. These 64.6% and 63.9%differences(95%CI: 56.7%-72.2% and 55.7%-72.0%)were highly significant(P < 0.001). This advantage was detected since the early 3rd day evaluation(68.8% and64.1% vs 7.1% for the rSK and active control groups,respectively; P < 0.001) and was maintained even at the late 10 th day assessment(97.1% and 93.5% vs67.1% for rSK and hydrocortisone acetate, respectively;P < 0.001). Time to response was 3 d(95%CI: 2.9-3.1)for both rSK groups and 10 d(95%CI: 9.3-10.7) in the hydrocortisone acetate group. This difference was highly significant(P < 0.001). All subgroup stratified analyses(with or without thrombosis and hemorrhoid classification) showed a statistically significant advantage for the rSK groups. Thrombectomy was necessary in4/251 and 14/133 patients with baseline thrombosis in the rSK and hydrocortisone acetate groups, respectively(P < 0.001). There were no adverse events attributable to the experimental treatment.CONCLUSION: rSK suppositories showed a significant advantage over a widely-used over-the-counter hydrocortisone acetate preparation for the treatment of acute hemorrhoidal illness, as well as having an adequate safety profile.展开更多
Ulcerative colitis is a global health problem,affecting millions of individuals worldwide.As an inflammatory condition localised in the large intestine,rectal delivery of immunosuppressive therapies such as tacrolimus...Ulcerative colitis is a global health problem,affecting millions of individuals worldwide.As an inflammatory condition localised in the large intestine,rectal delivery of immunosuppressive therapies such as tacrolimus is a promising strategy to maximise drug concentration at the site of action whilst minimising systemic side effects.Here,for the first time,self-supporting 3D-printed tacrolimus suppositories were prepared without the aid of moulds using a pharmaceutical semi-solid extrusion(SSE)3D printer.The suppositories were printed vertically in three different sizes using combinations of two lipid pharmaceutical excipients(Gelucire 44/14 or Gelucire 48/16)and coconut oil.Although both suppository formulations had the appropriate viscosity characteristics for printing,the Gel 44 formulation required less energy and force for extrusion compared to the Gel 48 system.The Gel 44 disintegrated more rapidly but released tacrolimus more slowly than the Gel 48 suppositories.Although the tacrolimus release profiles were significantly different,both suppository systems released more than 80% drug within 120 min.DSC and XRD analysis was inconclusive in determining the solid-state properties of the drug in the suppositories.In summary,this article reports on the fabrication of 3D printed selfsupporting suppositories to deliver personalised doses of a narrow therapeutic index drug,with potential benefits for patients with ulcerative colitis.展开更多
Background: Herbal rectal suppositories (RSs) were prescribed not only as a drug delivery system but also as a storing method in Persian medicine. According to the record of ancient references, RSs were clinically adm...Background: Herbal rectal suppositories (RSs) were prescribed not only as a drug delivery system but also as a storing method in Persian medicine. According to the record of ancient references, RSs were clinically administered for diarrhea, constipation, colitis, ascites, dysentery and intestinal parasites, sciatic, lower back pain and joint aches, fever, kidney disease and as an aphrodisiac. Objectives: The aim of this study is to categorize and review different types of RSs, their main herbal components and to find evidence to elucidate their clinical administration. Results: In this study, 7 manuscripts were studied to extract and categorize 11 types of herbal rectal suppositorie (RS) formulations, their ingredients and therapeutic indications. Furthermore, the Persian and scientific names of 43 herbs and their temperaments were mentioned in this study. Hence, ancient therapeutic indications of herbs used in RS formulations as well as their proven effects have been studied, which makes it possible to compare ancient and proven indications of medicinal plants used as ingredients of RSs. Conclusions: In modern medicine, RSs are mostly used for anorectic disorders. However in traditional Persian medicine, they were commonly used not only for anorectic and intestinal diseases, but also as an aphrodisiac, an agent for healing joint, sciatic pain and lumbago, an anti-fever, and an anti-ascites. Other implications of this study could be producing new insights of utilizing herbal RSs in diseases and disorders beyond anorectic and intestinal disorders.展开更多
We examined the stability of amoxicillin trihydrate from the preparation Augmentin in compounded forms of drugs such as vaginal suppositories and ointments. The quantity of the antibiotic in the preparations studied w...We examined the stability of amoxicillin trihydrate from the preparation Augmentin in compounded forms of drugs such as vaginal suppositories and ointments. The quantity of the antibiotic in the preparations studied was determined directly after they had been made and after a lapse of 7 and 14 days. We also carried out comparative examinations of the stability of sodium amoxicillin （Tarommentin） and sodium ampicillin （Ampicillin） in ointments with an addition of a boric acid solution. The examinations confirmed the stability of amoxicillin trihydrate in suppositories and in anhydrous and hydrated ointments. The content of this antibiotic in ointmems with an addition of a boric acid solution decreases slightly. Comparative studies of the stability of sodium amoxicillin and sodium amoxicillin revealed a markedly lower stability of the two antibiotics in comparison to the stability of amoxicillin trihydrate.展开更多
The article is devoted to the study of the immunomodulating activity of rectal suppositories with an extract of licorice root and essential oils of chamomile and tea tree. Taking into account that medicine is intended...The article is devoted to the study of the immunomodulating activity of rectal suppositories with an extract of licorice root and essential oils of chamomile and tea tree. Taking into account that medicine is intended and prescribed for children, all the experiments were performed on immature nonlinear one-month rats with weight of 60.0-80.0 g. As a result, it was found out that rectal insertion of suppositories with an extract of licorice root causes an increase in the phagocytic function of neutrophils and increases the quantity of antibodies in the spleen and titers of hemagglutinins and hemolysins in serum, that indicating on the activation of nonspecific and humoral immunity of immature animals. Moreover, the prospects of possible application of suppositories with an extract of licorice root are showed for prevention and treatment of various immunodependent diseases, viral in particular.展开更多
基金Supported by Heber Biotec,Havana(products,reagents) and the Ministry of Public Health of Cuba(hospital facilities and general medical care of the patients)
文摘AIM: To compare the efficacy and safety of recombinant streptokinase (rSK) and phenylephrine-based suppositories in acute hemorrhoidal disease.
文摘Mesalamine suppositories have been used widely for the treatment of distal ulcerative colitis and considered to be safer than systemic administration for its limited systemic absorption.However,previous studies have shown that mesalamine suppository occasionally causes severe hypersensitivity reactions including fever,rashes,colitis exacerbation and acute eosinophilic pneumonia.Here we present a 25-year-old woman with ulcerative colitis with bloody diarrhea accompanied by abdominal pain and fever which were aggravated after introduction of mesalamine suppositories.In light of symptom exacerbation of ulcerative colitis,increased inflammatory injury of colon mucosa shown by colonoscopy and elevated peripheral eosinophil count after mesalamine suppositories administration,and the Naranjo algorithm score of 10,the possibility of hypersensitivity reaction to mesalamine suppositories should be considered,warning us to be aware of this potential reaction after administration of mesalamine formulations even if it is the suppositories.
基金Supported by Heber Biotec,Havana(for providing products and reagents)and the Ministry of Public Health of Cuba(for hospital facilities and general medical care of patients)
文摘AIM: To compare the efficacy and safety of recombinant streptokinase(rSK) vs hydrocortisone acetate-based suppositories in acute hemorrhoidal disease.METHODS: A multicenter(11 sites), randomized(1:1:1), open, controlled trial with parallel groups was performed. All participating patients gave their written,informed consent. After inclusion, patients with acute symptoms of hemorrhoids were centrally randomized to receive, as outpatients, by the rectal route, suppositories of rSK 200000 IU of one unit every 8 h(first 3 units)and afterwards every 12 h until 8 administrations were completed(schedule A), one unit every 8 h until 6 units were completed(schedule B), or 25 mg hydrocortisone acetate once every 8 h up to a maximum of 24 administrations. Evaluations were performed at 3, 5,and 10 d post-inclusion. The main end-point was the 5thday response(disappearance of pain and bleeding, and≥ 70% reduction of the lesion size). Time to response and need for thrombectomy were secondary efficacy variables. Adverse events were also evaluated.RESULTS: Groups were homogeneous with regards to demographic and baseline characteristics. Fifth day complete response rates were 156/170(91.8%; 95%CI:87.3-96.2), 155/170(91.2%; 95%CI: 86.6%-95.7%),and 46/170(27.1%; 95%CI: 20.1%-34.0%) with rSK(schedule A and B) and hydrocortisone acetate suppositories, respectively. These 64.6% and 63.9%differences(95%CI: 56.7%-72.2% and 55.7%-72.0%)were highly significant(P < 0.001). This advantage was detected since the early 3rd day evaluation(68.8% and64.1% vs 7.1% for the rSK and active control groups,respectively; P < 0.001) and was maintained even at the late 10 th day assessment(97.1% and 93.5% vs67.1% for rSK and hydrocortisone acetate, respectively;P < 0.001). Time to response was 3 d(95%CI: 2.9-3.1)for both rSK groups and 10 d(95%CI: 9.3-10.7) in the hydrocortisone acetate group. This difference was highly significant(P < 0.001). All subgroup stratified analyses(with or without thrombosis and hemorrhoid classification) showed a statistically significant advantage for the rSK groups. Thrombectomy was necessary in4/251 and 14/133 patients with baseline thrombosis in the rSK and hydrocortisone acetate groups, respectively(P < 0.001). There were no adverse events attributable to the experimental treatment.CONCLUSION: rSK suppositories showed a significant advantage over a widely-used over-the-counter hydrocortisone acetate preparation for the treatment of acute hemorrhoidal illness, as well as having an adequate safety profile.
基金funded by Xunta de Galicia grant number GRC2013/015 and GPC2017/015.
文摘Ulcerative colitis is a global health problem,affecting millions of individuals worldwide.As an inflammatory condition localised in the large intestine,rectal delivery of immunosuppressive therapies such as tacrolimus is a promising strategy to maximise drug concentration at the site of action whilst minimising systemic side effects.Here,for the first time,self-supporting 3D-printed tacrolimus suppositories were prepared without the aid of moulds using a pharmaceutical semi-solid extrusion(SSE)3D printer.The suppositories were printed vertically in three different sizes using combinations of two lipid pharmaceutical excipients(Gelucire 44/14 or Gelucire 48/16)and coconut oil.Although both suppository formulations had the appropriate viscosity characteristics for printing,the Gel 44 formulation required less energy and force for extrusion compared to the Gel 48 system.The Gel 44 disintegrated more rapidly but released tacrolimus more slowly than the Gel 48 suppositories.Although the tacrolimus release profiles were significantly different,both suppository systems released more than 80% drug within 120 min.DSC and XRD analysis was inconclusive in determining the solid-state properties of the drug in the suppositories.In summary,this article reports on the fabrication of 3D printed selfsupporting suppositories to deliver personalised doses of a narrow therapeutic index drug,with potential benefits for patients with ulcerative colitis.
文摘Background: Herbal rectal suppositories (RSs) were prescribed not only as a drug delivery system but also as a storing method in Persian medicine. According to the record of ancient references, RSs were clinically administered for diarrhea, constipation, colitis, ascites, dysentery and intestinal parasites, sciatic, lower back pain and joint aches, fever, kidney disease and as an aphrodisiac. Objectives: The aim of this study is to categorize and review different types of RSs, their main herbal components and to find evidence to elucidate their clinical administration. Results: In this study, 7 manuscripts were studied to extract and categorize 11 types of herbal rectal suppositorie (RS) formulations, their ingredients and therapeutic indications. Furthermore, the Persian and scientific names of 43 herbs and their temperaments were mentioned in this study. Hence, ancient therapeutic indications of herbs used in RS formulations as well as their proven effects have been studied, which makes it possible to compare ancient and proven indications of medicinal plants used as ingredients of RSs. Conclusions: In modern medicine, RSs are mostly used for anorectic disorders. However in traditional Persian medicine, they were commonly used not only for anorectic and intestinal diseases, but also as an aphrodisiac, an agent for healing joint, sciatic pain and lumbago, an anti-fever, and an anti-ascites. Other implications of this study could be producing new insights of utilizing herbal RSs in diseases and disorders beyond anorectic and intestinal disorders.
文摘We examined the stability of amoxicillin trihydrate from the preparation Augmentin in compounded forms of drugs such as vaginal suppositories and ointments. The quantity of the antibiotic in the preparations studied was determined directly after they had been made and after a lapse of 7 and 14 days. We also carried out comparative examinations of the stability of sodium amoxicillin （Tarommentin） and sodium ampicillin （Ampicillin） in ointments with an addition of a boric acid solution. The examinations confirmed the stability of amoxicillin trihydrate in suppositories and in anhydrous and hydrated ointments. The content of this antibiotic in ointmems with an addition of a boric acid solution decreases slightly. Comparative studies of the stability of sodium amoxicillin and sodium amoxicillin revealed a markedly lower stability of the two antibiotics in comparison to the stability of amoxicillin trihydrate.
文摘The article is devoted to the study of the immunomodulating activity of rectal suppositories with an extract of licorice root and essential oils of chamomile and tea tree. Taking into account that medicine is intended and prescribed for children, all the experiments were performed on immature nonlinear one-month rats with weight of 60.0-80.0 g. As a result, it was found out that rectal insertion of suppositories with an extract of licorice root causes an increase in the phagocytic function of neutrophils and increases the quantity of antibodies in the spleen and titers of hemagglutinins and hemolysins in serum, that indicating on the activation of nonspecific and humoral immunity of immature animals. Moreover, the prospects of possible application of suppositories with an extract of licorice root are showed for prevention and treatment of various immunodependent diseases, viral in particular.
