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OBJECTIVE@#To observe the therapeutic effect of needling technique (acupuncture for regulating spleen and stomach) on diabetic gastroparesis (DGP), and to explore its possible mechanism.@*METHODS@#A total of 128 patients with DGP were randomized into an observation group (64 cases, 4 cases dropped off) and a control group (64 cases, 4 cases dropped off). On the basis of intervention on controlling blood glucose by western medication, needling technique was adopted at Zhongwan (CV 12), Zusanli (ST 36), Yinlingquan (SP 9), Xuehai (SP 10), Sanyinjiao (SP 6), Diji (SP 8), etc. in the observation group, once a day. Mosapride citrate dispersible tablet 5 mg was given orally 3 times a day in the control group. The treatment was given 6 times a week in the both groups, and totally 4-week treatment was required. Before and after treatment, the DGP symptom score, serum content of transmembrane protein 16A (ANO1) were observed, and the clinical therapeutic effect and the safety were evaluated in the both groups.@*RESULTS@#After treatment, the each subitem score (belching, abdominal distension, inappetence, nausea and vomiting, epigastric pain, abnormal defecation) and the total score of DGP symptom were decreased in both groups (<0.05), the subitem scores of belching, abdominal distension, inappetence, nausea and vomiting and the total score in the observation group were lower than those in the control group (<0.05). After treatment, the serum contents of transmembrane protein 16A were reduced in both groups (<0.05), and that in the observation group was lower than the control group (<0.05). The total effective rate was 86.7% (52/60) in the observation group, which was superior to 70.0% (42/60) in the control group (<0.05). Subcutaneous hematoma occurred in 5 cases in the observation group, which was improved after cold compress without other particular intervention.@*CONCLUSION@#The therapeutic effect of needling technique on improving symptoms in patients with diabetic gastroparesis is superior to mosapride citrate dispersible tablet, its mechanism may be related to alleviating the damage of interstitial cells of Cajal (ICC).
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Objective To compare the short-term curative effects of prucalopride and mosapride respectively combined with low dose polyethylene glycol in treating elderly refractory functional constipation.Methods Ninety patients with elderly refractory functional constipation in the outpatient department of our hospital from May 2014 to February 2016 were retrospectively analyzed and divided into two groups randomly,45 cases in each group.the prucalopride group:Prucalopride Succinate Tablets,2mg,4 times daily;the mosapride group:Mosapride Citrate Capsules,5mg,3 times daily.Polyethylene Glycol Electrolytes Powder(PEG) was also used in the two groups,13.125g,twice daily.The course of treatment was 4 weeks.The first defecating time and defecation difficulty relief time,average weekly spontaneous complete bowel movements (SCBM),defecating difficulty,stool character,adverse reactions and change of life quality were observed in the two groups.Results The treatment effective rate of slow transit constipation(STC) and defecatory disorder had the statistical difference between the two groups (P0.05).Compared with the mosapride group,the first defecating time and defecation difficulty relief time in the prucalopride group were shorter with statistical difference (P0.05).The total effective rate had statistical difference between the two groups(P<0.05).The incidence rate of adverse reactions had no statistical difference between the two groups(17.78% vs.15.56%,P<0.05).The total average score of PAC-QOL after treatment in the two groups were both decreased,moreover the decrease in the prucalopride group was more obvious;the difference between the two groups had statistical significance(P<0.05).Conclusion Prucalopride +PEG take effect faster in the treatment of elderly refractory functional constipation and has the advantages in the aspects of overall curative effect and life quality improvement,which is specially suitable for STC and defecatory disorder type.
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Objective To study the effect of mosapride citrate in the treatment of gastroesophageal reflux disease and its effect on gastrin .Methods 86 patients with gastroesophageal reflux disease admitted in our hospital from August 2013 to August 2016, those patients were divided into observation group and control group according to the order of admission,43 cases in each group.The control group was treated with esomeprazole on the basis of basal therapy, and the observation group was treated with mosapride citrate on the basis of control group.The clinical curative effect and adverse reaction were analyzed,visual analogue scale(VAS), gastrin and motilin were compared before and after treatment between the two groups.Results After treatment, the total effective rate in the observation group was significantly higher than the control group [90.70% (39/43) vs.65.12% (28/43)](P<0.05). The VAS score in the observation group was significantly lower than the control group [(2.43 ±0.25) vs.(4.02 ±0.41)](P<0.05).The levels of gastrin and motilin in the observation group were significantly higher than the control group[ (55.87 ±4.82) pg/mL, (308.43 ±19.31) pg/mL vs. (44.12 ±3.86) pg/mL,(243.12 ±15.76) pg/mL](P<0.05).There was no significant difference in adverse reaction rate between two groups. Conclusion Mosapride citrate tablets can be used in gastroesophageal reflux disease , can effectively improve the patient's gastrin levels and clinical symptoms, clinical efficacy is good, and with low rate of adverse reactions.
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Objective To explore the use of mosapride citrate in treating reflux esophagitis and nursing intervention spitley effect. Methods In 40 cases of reflux esophagitis in patients with routine therapy, and classified as the control group, the other 40 patients in the control group based on the use of mosapride citrate. And classified as the observation group, two groups of patients were in our hospital from June 2015 to January 2017. Results The study in the treatment of the two groups of patients with effective rate of 95.0%, the observation group was significantly higher than the control group 80.0%, between the two groups showed significant differences (P<0.05). The adverse effects of more than two groups found, two groups of patients with adverse reaction incidence was no significant difference, that shows no significant difference. Conclusion Mosapride citrate in reflux esophagitis treatment and intervention effect analysis found that the compared with conventional therapy, can be in At the same time, it can improve the curative effect of the patients, and will not increase the possibility of adverse reactions, so it is worthy of clinical reference.
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OBJECTIVE: To investigate the intestinal absorption characters of mosapride citrate(MC) and its tablets. METHODS: The Caco-2 cell monolayer was cultured and the in situ single-pass intestinal perfusion(SPIP) in rat model was created for studying the drug absorption properties, using phenol red method to revise the perfusate volume, a HPLC method was developed to simultaneously detect the phenol red and MC, the absorptive coefficient of Papp and Peff was calculated. RESULTS: MC was absorbed by the whole intestine segments in rats, mainly at upper small intestine. The tablets showed high permeability and good intestinal absorption in Caco-2 cells and SPIP in rats. CONCLUSION: In the Caco-2 cells and rats SPIP models, the tablets are prepared showed good consistency with the branded drug.
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ABSTRACT: The purpose of the study was to prepare orally disintegrating tablets (ODTs) of mosapride citrate for dogs with fast disintegration and low cost. The ODTs were developed by varying the components and the ratio of excipients. A direct compression method was used. The properties of the ODTs, including hardness, friability, active ingredient content, and in vitro disintegration time, were investigated, and an economic analysis of the formulations was performed. For all formulations, friability was less than 1%, and the hardness varied from 37.69±4.08 to 48.73±5.62 N, which indicated that the tablets had sufficient mechanical integrity to withstand packaging and carrying. Results showed that Formulation (F) 2, containing 5% sodium carboxymethyl starch; F3, containing 5% low-substituted hydroxypropylcellulose; and F5 had not only shorter disintegration times but also lower costs, which were suitable for mosapride citrate ODTs. Although F1, contained 5% croscarmellose sodium, and F4, contained 5% crospovidone, with shorter disintegration times, the costs of F1 and F4 were 25.8% and 22.6% higher than that of F5, respectively. Results also revealed that the disintegration time of F5 was not significantly different from those of F1, F2, F3, and F4 (p>0.05), all of which contained superdisintegrants. Without superdisintegrants, F5, which contained a mixture of microcrystalline cellulose, mannitol, and lactose, was also able to achieve a short disintegration time and to meet the requirements of ODTs for dogs.
RESUMO: O objetivo do estudo foi o de preparar os comprimidos por via oral de desintegração (ODTs) de citrato de mosaprida para cães com desintegração rápida e de baixo custo. Os ODTs foram desenvolvidos através da variação dos componentes e proporção de excipientes. Um método de compressão direta foi utilizado. As propriedades dos ODTs, incluindo dureza, friabilidade, o teor de ingrediente ativo e no tempo de desintegração in vitro foram investigados e, adicionalmente, uma análise econômica das formulações foi realizada. Para todas as formulações, friabilidade foi inferior a 1%, a dureza e variou de 37,69 ± 4,08-48,73 ± 5,62 N, o que indica que os comprimidos tinham integridade mecânica suficiente para suportar a embalagem e transporte. Os resultados mostraram que a formulação (F) 2, contendo 5% de amido de carboximetilo de sódio, F3, contendo 5% de hidroxipropil celulose de baixa substituição, e F5 não só tiveram menores tempos de desintegração mas também preços mais baixos, que foram adequados para ODTs de citrato de mosapride. Embora F1, continha 5% de croscarmelose de sódio, e F4, continha 5% de crospovidona, com tempos de desintegração mais curtos, os custos de F1 e F4 eram 25,8% e 22,6% mais elevado do que a F5, respectivamente.. Os resultados também revelam que o tempo de desintegração de F5 não foi significativamente diferente do de F1, F2, F3, e F4 (P> 0.05), todas as quais contêm superdesintegrantes. Sem superdesintegrantes, F5, que contêm uma mistura de celulose microcristalina, manitol e lactose também foi capaz de conseguir um curto tempo de desintegração e satisfaz os requisitos de ODTs para cães.
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Objective] To observe the clinical efficacy and 5-HT of Shugan Jianpi Tiaoshen acupuncture treatment for senile patients with constipation type of irritable bowel syndrome(IBS-C). [Method] A total of 68 patients with IBS-C were allocated into control group and acupuncture group from June 2015 to June 2014. 34 patients in the control group, who accepted Lactulose oral solution and Citrate Mosapride Citrate, of in 15 males and 19 females, the mean age was 66.8, the average duration of disease was 15.6 months;34 patients in acupuncture group, who accepted acupuncture treatment based on control group, in 17 males and 17 females, the mean age was 65.9, the average duration of disease was 17.1 months. Acupoint selection:Tianshu, Zusanli, Taichong, Xingjian, Qimen, Baihui, Neiguan. Observe constipation symptoms, depressive symptoms, and quality of life and serum 5-HT levels before and after treatment. [Result] The pre-treatment constipation symptoms and depressive symptom scores in two groups were decreased than post-treatment( P0.05), but body pain, vitality, emotional function, mental health, social function, and general health values were higher than that of the control group( P<0.05), which showed acupuncture treatment can reduce physical discomfort and improve the quality of life of patients. After treatment,serum 5-HT in control group was 33.8 pg/ml, in acupuncture group was 27.6 pg/m, which were lower than pre-treatment. 5-HT in acupuncture group was lower than control group( P<0.05), which showed the effect of acupuncture on regulation of 5-HT was more significant. [Conclusion]Shugan Jianpi Tiaoshen acupuncture can modulate 5-HT level of elderly patients with IBS-C, and play its role in modulating gastrointestinal function, improving constipation symptoms, depressive symptoms and quality of life.It is an effective method for the treatment of elderly patients with IBS-C.
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Drug metabolism mostly occurs in the liver. Cytochrome P450 (CYP) is a drug-metabolizing enzyme that is responsible for many important drug metabolism reactions. Recently, the US FDA and EU EMA have suggested that CYP enzyme induction can be measured by both enzymatic activity and mRNA expression. However, these experiments are time-consuming and their inter-assay variability can lead to misinterpretations of the results. To resolve these problems and establish a more powerful method to measure CYP induction, we determined CYP induction by using luminescent assay. Luminescent CYP assays link CYP enzyme activity to firefly luciferase luminescence technology. In this study, we measured the induction of CYP isozymes (1A2, 2B6, 2C9, and 3A4) in cryopreserved human hepatocytes (HMC424, 478, and 493) using a luminometer. We then examined the potential induction abilities (unknown so far) of mesalazine, a drug for colitis, and mosapride citrate, which is used as an antispasmodic drug. The results showed that mesalazine promotes CYP2B6 and 3A4 activities, while mosapride citrate promotes CYP1A2, 2B6, and 3A4 activities. Luminescent CYP assays offer rapid and safe advantages over LC-MS/MS and qRT-PCR methods. Furthermore, luminescent CYP assays decrease the interference between the optical properties of the test compound and the CYP substrates. Therefore, luminescent CYP assays are less labor intensive, rapid, and can be used as robust tools for high-throughput CYP screening during early drug discovery.
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Humans , Citric Acid , Colitis , Cytochrome P-450 CYP1A2 , Cytochrome P-450 Enzyme System , Cytochromes , Drug Discovery , Enzyme Induction , Fireflies , Hepatocytes , Isoenzymes , Liver , Luciferases , Luminescence , Luminescent Measurements , Mass Screening , Mesalamine , Metabolism , RNA, MessengerABSTRACT
OBJECTIVE:To investigate the efficacy of compound azintamide enteric-coated tablet plus mosapride citrate dispersible tablet for abdominal distention in patients with functional dyspepsia(FD).METHODS:A total of 80 patients with the chief complaint of abdominal distention were randomized to treatment group(Group A,n=40) to be treated with mosapride citrate dispersed tablets plus compound azintamide enteric-coated tablet,or control group in which the patients were treated bu mosapride citrate dispersed tablets(Group B,n=20) or compound azintamide enteric-coated tablets(Group C,n=20).Comp-ound azintamide enteric-coated tablets were administered orally tid(2 tablets) immediately after meal while the mosapride citrate dispersed tablets(5mg) were administered orally tid 30min before meal for 2 weeks.The main outcome measures were changes of symptom scores of abdominal distension,the total effective rates in improvement of abdominal distension,and drug side effects before and after treatment.RESULTS:After 1-week and 2-week treatment,the average index scores of abdominal distention in the treatment group(Group A) were significantly lower than in the control groups(Group B and Group C) (P