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 compare the therapeutic effect of the herbal medicine Zhishi Xiaopiwan with that of Cisapride in the treatment of functional dyspepsia (FD). METHODS Fifty one FD patients were randomized into Herbal...AIM To compare the therapeutic effect of the herbal medicine Zhishi Xiaopiwan with that of Cisapride in the treatment of functional dyspepsia (FD). METHODS Fifty one FD patients were randomized into Herbal group ( n =27) and Cisapride group ( n =24). Two groups were given a four week treatment of Zhishi Xiaopiwan 100ml , tid, a.c. and Cisapride 5mg , tid, a.c. respectively. Patients′ symptoms were assessed and 39 patients′ (22 of Herbal group and 17 of Cisapride group) gastric liquid emptying times were measured with ultrasonography before and after the treatment. RESULTS The therapeutic effective rates of Herbal group and Cisapride group were 81 49% and 87 50% ( P >0 05). The half gastric emptying time (GET 50 ) and gastric emptying time (GET) of healthy controls and FD patients were 36 12min±10 22min vs 52 95min±13 49min and 87 07min±21 11min vs 120 74min±23 08min ( P <0 001). The GET 50 and GET of Herbal group before and after the treatment were 51 63min±13 15min vs 45 62min±10 82min and 117 34min±23 29min vs 103 26min±22 19min ( P <0 01). The results of Cisapride group were 54 66min±14 14min vs 40 95min±11 29min and 125 12min±24 47min vs 95 49min±22 31min ( P <0 01). The differences in values (median) of GET 50 and GET for Herbal group and Cisapride group before and after treatment were 5 75min vs 17 18min and 13 22min vs 33 54min ( P <0 05). CONCLUSION Delayed gastric emptying is one of the pathogenesis of FD. Both Zhishi Xiaopi pills and Cisapride can effectively alleviate the symptoms of FD and accelerate gastric liquid emptying. The effect of Zhishi Xiaopiwan on enhancing gastric motility is comparable with but less than that of Cisapride .展开更多
Summary: Gastric emptying time of liquid meal was detected by using ultrasonography in 28 gas- tric ulcer patients with continual or recurrent dyspepsia symptoms after the ulcer healing. Sixteen out of 28 patients (5...Summary: Gastric emptying time of liquid meal was detected by using ultrasonography in 28 gas- tric ulcer patients with continual or recurrent dyspepsia symptoms after the ulcer healing. Sixteen out of 28 patients (57. 1 % ) with a delay of gastric emptying time (T1/2) were randomly divided into two groups: 8 cases were treated with cisapride 5 mg three times a day and & cases with cisapride 10 mg three times a day respectively. The results showed that cisapride could relieve the symptoms with the effective rate being 68. 8 % in the two groups. T1/2 in the patients after treatment with cisapride was significantly shorter than before treatment (P<0. 001 ). It was concluded that there is a delay of T1/2 in some patients with gastric ulcer healing. Cisapride could promote gastric empty of liquid meal and relieve the symptoms efficiently. The effect of lower dose of cisapride is similar to that of higher dose.展开更多
Objective: To investigate the therapeutic effect of cisapride on gastric injury following hemorrhagic shock resuscitation. Methods: 108 Wistar rats weighing (200 g±30 g) were randomly divided into a sham shock (S...Objective: To investigate the therapeutic effect of cisapride on gastric injury following hemorrhagic shock resuscitation. Methods: 108 Wistar rats weighing (200 g±30 g) were randomly divided into a sham shock (SS) group (n=36), a hemorrhagic shock resuscitation (HS) group (n=36) and a hemorrhagic shock cisapride treated (HSC) group (n=36). Sampling at 1, 2 and 4 hours after resuscitation was done and 6 samples for each observation item were taken. The gastric blood flow volume was measured by isotope label biological microglobulin. Gastric pHi, gastric emptying, MDA and Na+-K+-ATPase of gastric mucosa were measured. Results: In the HSC group, the relative residual rate of gastric pigment decreased significantly, the gastric blood flow volume elevated; gastric pHi increased significantly at 2 hours; the level of mucosal MDA decreased at 4 hours, the activity of Na+-K+-ATPase increased and the lactic acid level in the portal vein decreased significantly compared to the HS group. Conclusions: After hemorrhagic shock resuscitation, cisapride contained the following functions,1) promoting gastric emptying, 2) increasing the blood flow of gastric blood flow volume and gastric pHi, 3) depressing the lactic acid concentration of the portal vein and improving MDA volume and Na+-K+ -ATPase activity of gastric mucosa. It suggests that after comple menting effective circulating blood volume for hemorrhagic shock resuscitation, early use of cisapride for gastric motility is helpful for an improvement of lasting ischemia and hypoxia in stomach.展开更多
AIM:To study the relative efficacy of cisapride, metoclopramide,domperidone,erythromycin and mosapride on gastric emptying(GE)and small intestinal transit(SIT) in morphine treated mice. METHODS:Phenol red marker meal ...AIM:To study the relative efficacy of cisapride, metoclopramide,domperidone,erythromycin and mosapride on gastric emptying(GE)and small intestinal transit(SIT) in morphine treated mice. METHODS:Phenol red marker meal was employed to estimate GE and SIT in Swiss albino mice of either sex.The groups included were control,morphine 1 mg/kg(s.c.15 rain before test meal)alone or with(45 rain before test meal p.o.)cisapride 10 mg/kg,metoclopramide 20 mg/kg, domperidone 20 mg/kg,erythromycin 6 mg/kg and mosapride 20 mg/kg. RESULTS:Cisapride,metoclopramide and mosapride were effective in enhancing gastric emptying significantly(P<0.001) whereas other prokinetic agents failed to do so in normal mice.Metoclopramide completely reversed morphine induced delay in gastric emptying followed by mosapride. Metoclopramide alone was effective when given to normal mice in increasing the SIT.Cisapride,though it did not show any significant effect on SIT in normal mice,was able to reverse morphine induced delay in SIT significantly(P<0.001) followed by metoclopramide and mosapride. CONCLUSION:Metoclopramide and cisapride are most effective in reversing morphine-induced delay in gastric emptying and small intestinal transit in mice respectively.展开更多
Objective: To observe the damage of mixed reflux to the rat esophageal mucosa, and investigate the preventive effects of cisapride, nabumetone and hydrotalcite on the damaged esophageal mucosa. Methods: Three hundred ...Objective: To observe the damage of mixed reflux to the rat esophageal mucosa, and investigate the preventive effects of cisapride, nabumetone and hydrotalcite on the damaged esophageal mucosa. Methods: Three hundred sixty-eight Sprague-Dawley rats were treated as esophagoduodenostomy and divided into four groups in random. Group Y: operation + saline as positive controls; Group P: operation + cisapride; Group R: operation + nabumetone; Group D: operation + hydrotalcite. Different drugs were perfused in the 1 st week after operation. The lesions of esophageal mucosa were observed in the 5th, 9th, 13th, 17th, 22nd, 28th, 35th and 40th week respectively, and evaluated the preventive effects of these drugs. Results: The lesions of esophageal mucosa in group Y were more severe than other three groups in different time (P ＜ 0.05), and the incidence of Barrett's esophagus(BE), severe atypical hyperplasia and esophageal adenocarcinoma (EAC) in group Y were higher than others. After 22 weeks, the lesions in group P were more severe than group R and D, and there were obvious differences in different time ( P ＜ 0.05); but the incidence of BE, severe atypical hyperplasia and EAC in group P had no significant difference with group R and group D( P ＞ 0.05). Conclusion: BE, severe atypical hyperplasia and EAC could occur because of severe reflux esophagitis for a long term. Cisapride, nabumetone and hydrotalcite could reduce mucosa injury in reflux esophagitis and resist the development of BE, severe atypical hyperplasia and EAC.In addition, the curative effects of nabumetone and hydrotalcite were better than cisapride.展开更多
Functional dyspepsia is a frequently-encountered clinical syndrome, characterized by fullness and pain in the upper abdomen, belching, sour regurgitation, anorexia, nausea, vomiting, without organic pathologic change,...Functional dyspepsia is a frequently-encountered clinical syndrome, characterized by fullness and pain in the upper abdomen, belching, sour regurgitation, anorexia, nausea, vomiting, without organic pathologic change, metabolic or psychic diseases. It is closely related with disturbance of gastric motility. Our previous study has indicated that acupuncture has marked therapeutic effects on disturbance of gastric motility. In the present paper, analysis of time-frequency spectrum of EGG was used as indexes, and the clinical therapeutic effects of acupuncture treatment on functional dyspepsia were assessed objectively. The results are reported in the following.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 compare the therapeutic effect of the herbal medicine Zhishi Xiaopiwan with that of Cisapride in the treatment of functional dyspepsia (FD). METHODS Fifty one FD patients were randomized into Herbal group ( n =27) and Cisapride group ( n =24). Two groups were given a four week treatment of Zhishi Xiaopiwan 100ml , tid, a.c. and Cisapride 5mg , tid, a.c. respectively. Patients′ symptoms were assessed and 39 patients′ (22 of Herbal group and 17 of Cisapride group) gastric liquid emptying times were measured with ultrasonography before and after the treatment. RESULTS The therapeutic effective rates of Herbal group and Cisapride group were 81 49% and 87 50% ( P >0 05). The half gastric emptying time (GET 50 ) and gastric emptying time (GET) of healthy controls and FD patients were 36 12min±10 22min vs 52 95min±13 49min and 87 07min±21 11min vs 120 74min±23 08min ( P <0 001). The GET 50 and GET of Herbal group before and after the treatment were 51 63min±13 15min vs 45 62min±10 82min and 117 34min±23 29min vs 103 26min±22 19min ( P <0 01). The results of Cisapride group were 54 66min±14 14min vs 40 95min±11 29min and 125 12min±24 47min vs 95 49min±22 31min ( P <0 01). The differences in values (median) of GET 50 and GET for Herbal group and Cisapride group before and after treatment were 5 75min vs 17 18min and 13 22min vs 33 54min ( P <0 05). CONCLUSION Delayed gastric emptying is one of the pathogenesis of FD. Both Zhishi Xiaopi pills and Cisapride can effectively alleviate the symptoms of FD and accelerate gastric liquid emptying. The effect of Zhishi Xiaopiwan on enhancing gastric motility is comparable with but less than that of Cisapride .
文摘Summary: Gastric emptying time of liquid meal was detected by using ultrasonography in 28 gas- tric ulcer patients with continual or recurrent dyspepsia symptoms after the ulcer healing. Sixteen out of 28 patients (57. 1 % ) with a delay of gastric emptying time (T1/2) were randomly divided into two groups: 8 cases were treated with cisapride 5 mg three times a day and & cases with cisapride 10 mg three times a day respectively. The results showed that cisapride could relieve the symptoms with the effective rate being 68. 8 % in the two groups. T1/2 in the patients after treatment with cisapride was significantly shorter than before treatment (P<0. 001 ). It was concluded that there is a delay of T1/2 in some patients with gastric ulcer healing. Cisapride could promote gastric empty of liquid meal and relieve the symptoms efficiently. The effect of lower dose of cisapride is similar to that of higher dose.
文摘Objective: To investigate the therapeutic effect of cisapride on gastric injury following hemorrhagic shock resuscitation. Methods: 108 Wistar rats weighing (200 g±30 g) were randomly divided into a sham shock (SS) group (n=36), a hemorrhagic shock resuscitation (HS) group (n=36) and a hemorrhagic shock cisapride treated (HSC) group (n=36). Sampling at 1, 2 and 4 hours after resuscitation was done and 6 samples for each observation item were taken. The gastric blood flow volume was measured by isotope label biological microglobulin. Gastric pHi, gastric emptying, MDA and Na+-K+-ATPase of gastric mucosa were measured. Results: In the HSC group, the relative residual rate of gastric pigment decreased significantly, the gastric blood flow volume elevated; gastric pHi increased significantly at 2 hours; the level of mucosal MDA decreased at 4 hours, the activity of Na+-K+-ATPase increased and the lactic acid level in the portal vein decreased significantly compared to the HS group. Conclusions: After hemorrhagic shock resuscitation, cisapride contained the following functions,1) promoting gastric emptying, 2) increasing the blood flow of gastric blood flow volume and gastric pHi, 3) depressing the lactic acid concentration of the portal vein and improving MDA volume and Na+-K+ -ATPase activity of gastric mucosa. It suggests that after comple menting effective circulating blood volume for hemorrhagic shock resuscitation, early use of cisapride for gastric motility is helpful for an improvement of lasting ischemia and hypoxia in stomach.
文摘AIM:To study the relative efficacy of cisapride, metoclopramide,domperidone,erythromycin and mosapride on gastric emptying(GE)and small intestinal transit(SIT) in morphine treated mice. METHODS:Phenol red marker meal was employed to estimate GE and SIT in Swiss albino mice of either sex.The groups included were control,morphine 1 mg/kg(s.c.15 rain before test meal)alone or with(45 rain before test meal p.o.)cisapride 10 mg/kg,metoclopramide 20 mg/kg, domperidone 20 mg/kg,erythromycin 6 mg/kg and mosapride 20 mg/kg. RESULTS:Cisapride,metoclopramide and mosapride were effective in enhancing gastric emptying significantly(P<0.001) whereas other prokinetic agents failed to do so in normal mice.Metoclopramide completely reversed morphine induced delay in gastric emptying followed by mosapride. Metoclopramide alone was effective when given to normal mice in increasing the SIT.Cisapride,though it did not show any significant effect on SIT in normal mice,was able to reverse morphine induced delay in SIT significantly(P<0.001) followed by metoclopramide and mosapride. CONCLUSION:Metoclopramide and cisapride are most effective in reversing morphine-induced delay in gastric emptying and small intestinal transit in mice respectively.
基金Supported by: Clinical Speciality Foundation of Ministry of Health of the people's Republic of China (No.20012130)
文摘Objective: To observe the damage of mixed reflux to the rat esophageal mucosa, and investigate the preventive effects of cisapride, nabumetone and hydrotalcite on the damaged esophageal mucosa. Methods: Three hundred sixty-eight Sprague-Dawley rats were treated as esophagoduodenostomy and divided into four groups in random. Group Y: operation + saline as positive controls; Group P: operation + cisapride; Group R: operation + nabumetone; Group D: operation + hydrotalcite. Different drugs were perfused in the 1 st week after operation. The lesions of esophageal mucosa were observed in the 5th, 9th, 13th, 17th, 22nd, 28th, 35th and 40th week respectively, and evaluated the preventive effects of these drugs. Results: The lesions of esophageal mucosa in group Y were more severe than other three groups in different time (P ＜ 0.05), and the incidence of Barrett's esophagus(BE), severe atypical hyperplasia and esophageal adenocarcinoma (EAC) in group Y were higher than others. After 22 weeks, the lesions in group P were more severe than group R and D, and there were obvious differences in different time ( P ＜ 0.05); but the incidence of BE, severe atypical hyperplasia and EAC in group P had no significant difference with group R and group D( P ＞ 0.05). Conclusion: BE, severe atypical hyperplasia and EAC could occur because of severe reflux esophagitis for a long term. Cisapride, nabumetone and hydrotalcite could reduce mucosa injury in reflux esophagitis and resist the development of BE, severe atypical hyperplasia and EAC.In addition, the curative effects of nabumetone and hydrotalcite were better than cisapride.
文摘Functional dyspepsia is a frequently-encountered clinical syndrome, characterized by fullness and pain in the upper abdomen, belching, sour regurgitation, anorexia, nausea, vomiting, without organic pathologic change, metabolic or psychic diseases. It is closely related with disturbance of gastric motility. Our previous study has indicated that acupuncture has marked therapeutic effects on disturbance of gastric motility. In the present paper, analysis of time-frequency spectrum of EGG was used as indexes, and the clinical therapeutic effects of acupuncture treatment on functional dyspepsia were assessed objectively. The results are reported in the following.
