To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Met...To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) wereused to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in thecarrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporationmethod. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier,pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion(4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride soliddispersion was measured with water, SGF and simulated intestinal fluid (SIF) . The in vitro drugreleases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride soliddispersion were investigated with water and SGF as media, respectively. Results No diffraction peakswere found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that thedrug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, thesolubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared withHPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. Thein vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitrodrug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improvedowing to the increased drug solubility.展开更多
AIM:To evaluate the efficacy and safety of adjunctive mosapride citrate for bowel preparation before colonoscopy. METHODS:We conducted a randomized,double-blind, placebo-controlled study with mosapride in addition to ...AIM:To evaluate the efficacy and safety of adjunctive mosapride citrate for bowel preparation before colonoscopy. METHODS:We conducted a randomized,double-blind, placebo-controlled study with mosapride in addition to polyethylene glycol(PEG)-electrolyte solution.Of 250 patients undergoing colonoscopy,124 were randomized to receive 2 L PEG plus 15 mg of mosapride citrate (mosapride group),and 126 received 2 L PEG plus placebo(placebo group).Patients completed a questionnaire reporting the acceptability and tolerability of the bowel preparation process.The efficacy of bowel preparation was assessed by colonoscopists using a 5-point scale based on Aronchick's criteria.The primary end point was optimal bowel preparation rates(scores of excellent/good/fair vs poor/inadequate). RESULTS:A total of 249 patients were included in the analysis.In the mosapride group,optimal bowel preparation rates were significantly higher in the left colon compared with the placebo group(78.2%vs 65.6%,P<0.05),but not in the right colon(76.5%vs 66.4%,P=0.08).After excluding patients with severe constipation,there was a significant difference in bowel preparation in both the left and right colon(82.4%vs 66.7%,80.8%vs 67.5%,P<0.05,P<0.01).The incidence of adverse events was similar in both groups. Among the subgroup who had previous colonoscopy experience,a significantly higher number of patients in the mosapride group felt that the current preparation was easier compared with patients in the placebo group(34/72 patients vs 24/74 patients,P<0.05). CONCLUSION:Mosapride citrate may be an effective and safe adjunct to PEG-electrolyte solution that leads to improved quality of bowel preparation,especially in patients without severe constipation.展开更多
AIM:To evaluate the effect of prokinetic drugs on electrogastrography(EGG) parameters according to symptomatic changes in patients with functional dyspepsia(FD).METHODS:Seventy-four patients with FD were prospectively...AIM:To evaluate the effect of prokinetic drugs on electrogastrography(EGG) parameters according to symptomatic changes in patients with functional dyspepsia(FD).METHODS:Seventy-four patients with FD were prospectively enrolled in this study between December 2006 and December 2010.We surveyed the patients using a questionnaire on dyspeptic symptoms before and after an 8-wk course of prokinetic drug treatment.We also measured cutaneous pre-prandial and postprandial EGG recordings including percentage of gastric waves(normogastria,bradygastria,tachygastria),dominant frequency(DF),dominant power(DP),dominant frequency instability coefficient(DFIC),dominant power instability coefficient(DPIC),and the ratio of post-prandial to fasting in DP before and after the 8-wk course of prokinetic drug treatment.RESULTS:Fifty-two patients(70%) achieved symptomatic improvement after prokinetic drug treatment.Patients who had normal gastric slow waves showed symptom improvement group after treatment.Postprandial DF showed a downward trend in the symptom improvement group,especially in the itopride group.Post-prandial DP was increased regardless of symptom improvement,especially in the itopride group and mosapride group.Post-prandial DFIC and DPIC in the symptom improvement group were significantly increased after the treatment.The EGG power ratio was increased after treatment in the symptom improvement group(0.50 ± 0.70 vs 0.93 ± 1.77,P = 0.002),especially in the itopride and levosulpiride groups.CONCLUSION:Prokinetics could improve the symptoms of FD by regulating gastric myoelectrical activity,and EGG could be a useful tool in evaluating the effects of various prokinetics.展开更多
OBJECTIVE: To investigate the therapeutic effect of the herbal medication Xiao Pi-II on the symptoms and gastric motility of patients with functional dysepsia (FD). METHODS: A total of 180 FD patients were divided ran...OBJECTIVE: To investigate the therapeutic effect of the herbal medication Xiao Pi-II on the symptoms and gastric motility of patients with functional dysepsia (FD). METHODS: A total of 180 FD patients were divided randomly and equally into Xiao Pi-II and mosapride groups. The two groups were treated with Xiao Pi-II (100 mL, t.d.s., ante cibum) and mosapride (5 mg, t. d.s., ante cibum) for 2 weeks. Before treatment and 3 days after all medication was stopped, patients responded to a questionnaire evaluating gastrointestinal symptoms and were assessed with abdominal three dimensional ultrasonography (3D-US) for gastric motility. RESULTS: Gastrointestinal symptoms (especially bloating, post-prandial fullness and eructation) were improved significantly in FD patients treated with Xiao Pi-II (P<0.05, P<0.05, and P<0.05), but no significant difference was found in the mosapride group (P>0.05). The effective rates in the Xiao Pi-II and mosapride group were 86.7% and 60.0%, respectively (P<0.05). The gastric liquid emptyingrate (GLER) in the Xiao Pi-II group showed a significant increase (P<0.01) after 2 weeks of treatment but there was no significant change (P>0.05) of GLER in the mosapride group. CONCLUSION: Compared with mosapride, Xiao Pi-II improved symptoms and GLER significantly in FD patients with delayed gastric emptying.展开更多
文摘To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) wereused to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in thecarrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporationmethod. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier,pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion(4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride soliddispersion was measured with water, SGF and simulated intestinal fluid (SIF) . The in vitro drugreleases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride soliddispersion were investigated with water and SGF as media, respectively. Results No diffraction peakswere found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that thedrug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, thesolubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared withHPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. Thein vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitrodrug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improvedowing to the increased drug solubility.
文摘AIM:To evaluate the efficacy and safety of adjunctive mosapride citrate for bowel preparation before colonoscopy. METHODS:We conducted a randomized,double-blind, placebo-controlled study with mosapride in addition to polyethylene glycol(PEG)-electrolyte solution.Of 250 patients undergoing colonoscopy,124 were randomized to receive 2 L PEG plus 15 mg of mosapride citrate (mosapride group),and 126 received 2 L PEG plus placebo(placebo group).Patients completed a questionnaire reporting the acceptability and tolerability of the bowel preparation process.The efficacy of bowel preparation was assessed by colonoscopists using a 5-point scale based on Aronchick's criteria.The primary end point was optimal bowel preparation rates(scores of excellent/good/fair vs poor/inadequate). RESULTS:A total of 249 patients were included in the analysis.In the mosapride group,optimal bowel preparation rates were significantly higher in the left colon compared with the placebo group(78.2%vs 65.6%,P<0.05),but not in the right colon(76.5%vs 66.4%,P=0.08).After excluding patients with severe constipation,there was a significant difference in bowel preparation in both the left and right colon(82.4%vs 66.7%,80.8%vs 67.5%,P<0.05,P<0.01).The incidence of adverse events was similar in both groups. Among the subgroup who had previous colonoscopy experience,a significantly higher number of patients in the mosapride group felt that the current preparation was easier compared with patients in the placebo group(34/72 patients vs 24/74 patients,P<0.05). CONCLUSION:Mosapride citrate may be an effective and safe adjunct to PEG-electrolyte solution that leads to improved quality of bowel preparation,especially in patients without severe constipation.
文摘AIM:To evaluate the effect of prokinetic drugs on electrogastrography(EGG) parameters according to symptomatic changes in patients with functional dyspepsia(FD).METHODS:Seventy-four patients with FD were prospectively enrolled in this study between December 2006 and December 2010.We surveyed the patients using a questionnaire on dyspeptic symptoms before and after an 8-wk course of prokinetic drug treatment.We also measured cutaneous pre-prandial and postprandial EGG recordings including percentage of gastric waves(normogastria,bradygastria,tachygastria),dominant frequency(DF),dominant power(DP),dominant frequency instability coefficient(DFIC),dominant power instability coefficient(DPIC),and the ratio of post-prandial to fasting in DP before and after the 8-wk course of prokinetic drug treatment.RESULTS:Fifty-two patients(70%) achieved symptomatic improvement after prokinetic drug treatment.Patients who had normal gastric slow waves showed symptom improvement group after treatment.Postprandial DF showed a downward trend in the symptom improvement group,especially in the itopride group.Post-prandial DP was increased regardless of symptom improvement,especially in the itopride group and mosapride group.Post-prandial DFIC and DPIC in the symptom improvement group were significantly increased after the treatment.The EGG power ratio was increased after treatment in the symptom improvement group(0.50 ± 0.70 vs 0.93 ± 1.77,P = 0.002),especially in the itopride and levosulpiride groups.CONCLUSION:Prokinetics could improve the symptoms of FD by regulating gastric myoelectrical activity,and EGG could be a useful tool in evaluating the effects of various prokinetics.
文摘OBJECTIVE: To investigate the therapeutic effect of the herbal medication Xiao Pi-II on the symptoms and gastric motility of patients with functional dysepsia (FD). METHODS: A total of 180 FD patients were divided randomly and equally into Xiao Pi-II and mosapride groups. The two groups were treated with Xiao Pi-II (100 mL, t.d.s., ante cibum) and mosapride (5 mg, t. d.s., ante cibum) for 2 weeks. Before treatment and 3 days after all medication was stopped, patients responded to a questionnaire evaluating gastrointestinal symptoms and were assessed with abdominal three dimensional ultrasonography (3D-US) for gastric motility. RESULTS: Gastrointestinal symptoms (especially bloating, post-prandial fullness and eructation) were improved significantly in FD patients treated with Xiao Pi-II (P<0.05, P<0.05, and P<0.05), but no significant difference was found in the mosapride group (P>0.05). The effective rates in the Xiao Pi-II and mosapride group were 86.7% and 60.0%, respectively (P<0.05). The gastric liquid emptyingrate (GLER) in the Xiao Pi-II group showed a significant increase (P<0.01) after 2 weeks of treatment but there was no significant change (P>0.05) of GLER in the mosapride group. CONCLUSION: Compared with mosapride, Xiao Pi-II improved symptoms and GLER significantly in FD patients with delayed gastric emptying.
