The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were...The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were observed in the solution. The aims of the present study were to assess the degradation rates of FLT in other alkaline solutions and clarify the chemical structures of the four degradation products in order to obtain basic data for designing an enema for inflammatory bowel disease. The apparent degradation rate constants in 0.05 M NaOH and 0.1 M NaOH:CH_3CN=1:1 were 0.472 ± 0.013 h^(-1) and 0.154 ± 0.000 h^(-1)(n=3), respectively. The chemical structures of products 1–4 in 0.1 M NaOH:methanol=1:1 were revealed by nuclear magnetic resonance(NMR)and mass spectrometry data. The chemical structure of products 2 was that the 17-position of the thioester moiety of FLT was substituted by a carboxylic acid. The degradation product in 0.1 M NaOH:CH_3CN=1:1 was found to be product 2 based on ~1H NMR data. The degradation product in 0.05 M NaOH was considered to be product 2 based on the retention time of HPLC. These results are useful for detecting the degradation products of FLT by enzymes of the intestinal bacterial flora in the large intestine after dosing FLT as an enema.展开更多
Lichen planus is a fairly common chronic idiopathic disorder of the skin,nails and mucosal surfaces.Esophageal involvement of this disease on the other hand is rare and only about 50 cases have been reported in litera...Lichen planus is a fairly common chronic idiopathic disorder of the skin,nails and mucosal surfaces.Esophageal involvement of this disease on the other hand is rare and only about 50 cases have been reported in literature.Given its rarity,it can be difficult to diagnose and may be easily misdiagnosed as reflux esophagitis.Currently,there are no clear recommendations on the optimal management of this disease and little is known about the best treatment approach.Systemic steroids are usually the first line treatment and offer a favorable response.In this report,we would like to present a novel approach in the management of esophageal lichen planus in a middle-aged woman treated successfully with swallowed fluticasone propionate 220 mcg twice a day for 6 wk,as evidenced by objective clinical findings.Based on our review of related literature and experience in this patient,we feel that a trial of swallowed fluticasone may be a prudent approach in the management of these patients since it has a more favorable side effect profile than systemic treatment.展开更多
文摘The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were observed in the solution. The aims of the present study were to assess the degradation rates of FLT in other alkaline solutions and clarify the chemical structures of the four degradation products in order to obtain basic data for designing an enema for inflammatory bowel disease. The apparent degradation rate constants in 0.05 M NaOH and 0.1 M NaOH:CH_3CN=1:1 were 0.472 ± 0.013 h^(-1) and 0.154 ± 0.000 h^(-1)(n=3), respectively. The chemical structures of products 1–4 in 0.1 M NaOH:methanol=1:1 were revealed by nuclear magnetic resonance(NMR)and mass spectrometry data. The chemical structure of products 2 was that the 17-position of the thioester moiety of FLT was substituted by a carboxylic acid. The degradation product in 0.1 M NaOH:CH_3CN=1:1 was found to be product 2 based on ~1H NMR data. The degradation product in 0.05 M NaOH was considered to be product 2 based on the retention time of HPLC. These results are useful for detecting the degradation products of FLT by enzymes of the intestinal bacterial flora in the large intestine after dosing FLT as an enema.
文摘Lichen planus is a fairly common chronic idiopathic disorder of the skin,nails and mucosal surfaces.Esophageal involvement of this disease on the other hand is rare and only about 50 cases have been reported in literature.Given its rarity,it can be difficult to diagnose and may be easily misdiagnosed as reflux esophagitis.Currently,there are no clear recommendations on the optimal management of this disease and little is known about the best treatment approach.Systemic steroids are usually the first line treatment and offer a favorable response.In this report,we would like to present a novel approach in the management of esophageal lichen planus in a middle-aged woman treated successfully with swallowed fluticasone propionate 220 mcg twice a day for 6 wk,as evidenced by objective clinical findings.Based on our review of related literature and experience in this patient,we feel that a trial of swallowed fluticasone may be a prudent approach in the management of these patients since it has a more favorable side effect profile than systemic treatment.
