BACKGROUND/AIMS: In capsule endoscopy (CE), the capsule does not always reach the cecum within its battery life, which may reduce its diagnostic yield. We evaluated the effect of mosapride citrate, a 5-hydroxytryptamine-4 agonist that increases gastrointestinal motility, on CE completion. METHODS: In a retrospective study, we performed univariate and multivariate analyses for 232 CE procedures performed at our hospital. To identify factors that affect CE completion, the following data were systematically collected: gender, age, gastric transit time (GTT), nonsteroidal anti-inflammatory drug administration, previous abdominal surgery, hospitalization, use of a polyethylene glycol solution, use of mosapride citrate (10 mg), body mass index (BMI), and total recording time. RESULTS: The univariate analysis showed that oral mosapride citrate, GTT, and BMI were associated with improved CE completion. Multivariate analyses showed that oral mosapride citrate (odds ratio [OR], 1.99; 95% confidence interval [CI], 1.01 to 3.91) and GTT (OR, 2.34; 95% CI, 1.13 to 4.87) were significant factors for improving the CE completion. Oral mosapride citrate significantly shortened the GTT and small bowel transit time (SBTT). CONCLUSIONS: Oral mosapride citrate reduced the GTT and SBTT during CE and improved the CE completion rate.
Administration, Oral ; Benzamides ; Body Mass Index ; Capsule Endoscopy ; Cecum ; Citric Acid ; Gastrointestinal Motility ; Hospitalization ; Morpholines ; Multivariate Analysis ; Polyethylene Glycols ; Retrospective Studies

Due to its serious comorbidities and high prevalence, obesity is one of the heaviest burdens for public health. Although diet, exercise and behavioral modification are the first-line treatment for obesity, their outcomes are not satisfactory. The goal of this article is to review currently available anti-obesity drugs so that physicians may apply the principle of pharmacologic treatment for obesity to obese patients in the real clinical situation. Orlistat, phentermine, diethylpropion, mazindol, and phendimetrazine have been approved as anti-obesity drugs by Korea food and drug administration and administered to patients in Korea. Besides, several non-approved drugs, including fluoxetine, bupropion, topiramate and zonisamide, are being used for weight reduction. Among these drugs, orlistat has been studied most and is the only approved drug for long-term weight management. On the other hand, the rest of the approved drugs lack the evidence of safety issues on the long-term administration. Considering that the non-approved drugs have only a small body of clinical trial results for their efficacy and safety as anti-obesity drugs, it is not appropriate to use them as a first-line therapy in obesity. Because several new medicines and combination therapies are under investigations, more drug therapy options seem to be available in this field in coming years. Although the properly executed pharmacologic treatment is a good option for weight reduction, physicians should recognize that diet, exercise, and behavioral modification are essential to all obese patient and that pharmacologic treatment has several limitations until now.
Anti-Obesity Agents ; Bupropion ; Comorbidity ; Diet ; Diethylpropion ; Fluoxetine ; Fructose ; Hand ; Humans ; Isoxazoles ; Korea ; Lactones ; Mazindol ; Morpholines ; Obesity ; Phentermine ; Prevalence ; Public Health ; United States Food and Drug Administration ; Weight Loss

BACKGROUNDNonanesthetic colonoscopy is popular in clinical practice in China. However, intestinal spasms often result in a prolonged examination time, increased operating difficulties, decreased polyp detection rate, and failure to complete the procedure clinically. Therefore, exploring alternative approaches that can reduce the pain in patients during colonoscopy is of utmost importance, and finding the optimal preoperative administration to improve the quality of nonanesthetic colonoscopy is also necessary. This study aimed to investigate the effects of the prophylactic administration of pinaverium bromide before colonoscopy and the effects of pinaverium bromide alone at different time points or combined with scopolamine butylbromide.

METHODSA randomized controlled trial was performed on a cohort of 1000 patients who underwent colonoscopy in outpatient clinic of Wuhan Union Hospital. The patients were randomly assigned to the following groups: Group A, given oral pinaverium bromide (100 mg, three times a day) one day before examination combined with intramuscular injection of scopolamine butylbromide (20 mg) 10 min before colonoscopy; Group B0, given pinaverium bromide alone on the day of colonoscopy (100 mg, three times a day); Group B1, given pinaverium bromide alone (100 mg, three times a day) one day before colonoscopy; Group B2, given pinaverium bromide alone (100 mg, three times a day) two days before colonoscopy; and Group C, given scopolamine butylbromide alone (20 mg) before colonoscopy. The successful rate of colonoscopy, procedure time, degree of abdominal pain, and polyp detection rate were recorded and compared among all groups.

RESULTSThe successful rate of colonoscopy in Group B1(82.0%) and Group B2(83.0%) was significantly higher than that in Group B0(62.0%, all P < 0.01). The time to reach the ileocecal region in Group B1and Group B2were lower than those in Group B0(all P < 0.05). However, no significant differences were observed in polyp detection rate between Group B1(24.0%) or Group B2(26.0%), and Group B0(22.4%, all P > 0.05). Furthermore, there were no significant differences in the various parameters examined between Group B1and Group B2(P > 0.05). The successful rate of colonoscopy in Group A (92.0%) was significantly higher than that in Group B1(82.0%) and Group C (80.0%; both P < 0.05). Moreover, the time for the colonoscope to reach the ileocecal region in Group A were markedly shorter as compared to those in Group B1 and Group C (P < 0.05). The polyp detection rate in Group A was 32.0%, significantly higher than that in Group B1(24.0%, P < 0.05) and Group C (24.2%, P < 0.05).

CONCLUSIONAdministration of pinaverium bromide alone one day before examination was beneficial to relieve symptoms of abdominal pain during nonanesthetic colonoscopy. In addition, therapeutic effects were improved when pinaverium bromide administration was combined with intramuscular injection of scopolamine butylbromide. Therefore, the combined use of pinaverium bromide with scopolamine butylbromide might have great application value to improve the quality of nonanesthetic colonoscopy in the preoperative preparation.

Abdominal Pain ; prevention & control ; Adult ; Colonoscopy ; methods ; Double-Blind Method ; Female ; Humans ; Male ; Middle Aged ; Morpholines ; administration & dosage ; therapeutic use ; Preoperative Period

OBJECTIVE: There is no research regarding the appropriate antiemetic agents for female patients, especially those receiving moderately emetogenic chemotherapy (MEC). We evaluated the antiemetic efficacy of a combination of 5-HT3 receptor with/without aprepitant in patients with gynecological cancer treated with the TC (paclitaxel and carboplatin) regimen of MEC. METHODS: We enrolled 38 patients diagnosed with gynecologic cancer and scheduled to receive the TC regimen. The patients were randomly assigned to receive a 5-HT3 receptor antagonist, either palonosetron in the first cycle followed by granisetron in the second cycle or vice versa. In the third cycle, all patients received a combination of the 5-HT3 receptor and dexamethasone with/without aprepitant. RESULTS: When three drugs were administered, palonosetron consistently produced an equivalent complete response (CR) rate to granisetron in the acute phase (89.5% vs. 86.8%, p=0.87) and delayed phase (60.5% vs. 65.8%, p=0.79). With regard to the change in dietary intake, palonosetron exhibited similar efficacy to granisetron in the acute phase (92.1% vs. 89.4%, p=0.19) and delayed phase (65.7% vs. 68.4%, p=0.14). However, in the delayed phase, the addition of aprepitant therapy with a 5-HT3 receptor antagonist and dexamethasone produced a higher CR rate than a 5-HT3 receptor antagonist with dexamethasone (93.3% vs. 47.8%, p<0.001) and allowed the patients to maintain a higher level of dietary intake (93.3% vs. 56.5%, p<0.001). CONCLUSION: The addition of aprepitant therapy was more effective than the control therapy of a 5-HT3 receptor antagonist, and dexamethasone in gynecological cancer patients treated with the TC regimen.
Adult ; Aged ; Antiemetics/*administration & dosage ; Antineoplastic Combined Chemotherapy Protocols/adverse effects ; Carboplatin/administration & dosage/adverse effects ; Cross-Over Studies ; Diet ; Drug Administration Schedule ; Female ; Genital Neoplasms, Female/*drug therapy ; Granisetron/administration & dosage ; Humans ; Isoquinolines/administration & dosage ; Middle Aged ; Morpholines/administration & dosage ; Nausea/chemically induced/*prevention & control ; Paclitaxel/administration & dosage/adverse effects ; Quinuclidines/administration & dosage ; Serotonin 5-HT3 Receptor Antagonists ; Vomiting/chemically induced/*prevention & control

AIMTo evaluate the effects of an array of additives on drug release from double-layered poly(lactic-co-glycolic acid) (PLGA) matrices.

METHODSAdditives differing in molecular size, hydrophilicity and steric configuration were selected for this study. An anti-proliferative 2-aminochromone, U-86983 (U-86, Pharmacia and Upjohn), was used as a model agent because of our interest in investigating local drug delivery systems for the inhibition of restenosis.

RESULTSIn vitro release of U-86 PLGA matrices without additive showed a typical biphasic release kinetics, i.e. a slow diffusion release (Phase I) followed by a fast erosion-mediated release (Phase II). The water-soluble additives in PLGA matrices changed the biphasic release pattern to a near monophasic profile by increasing the release of the Phase I. Increasing the ratio of additives to PLGA in matrices caused a significant increase in U-86 release rates. A high molecular weight water-soluble additive, Pluronic F127, resulted in a matrix showing perfect zero-order release kinetics. The morphologic evaluation of matrices using scanning electron microscopy indicated that the water-soluble additives were leachable and thus generated a highly porous structure in the matrices. Conclusion Water-solubility, molecular size and steric configuration of additives are the important determinants in generating various types of pore structures in polymer matrix which in turn affect the release mechanism and release kinetics.

Biocompatible Materials ; chemistry ; Chromones ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Drug Carriers ; Drug Delivery Systems ; Excipients ; chemistry ; Lactic Acid ; chemistry ; Molecular Weight ; Morpholines ; administration & dosage ; chemistry ; Pharmacokinetics ; Poloxamer ; chemistry ; Polyglycolic Acid ; chemistry ; Polymers ; chemistry ; Tartrates ; chemistry

OBJECTIVETo compare the therapeutic effects of transcutaneous electrical point stimulation and medication on functional dyspepsia.

METHODSTwo hundred and fifty cases were randomly divided into an observation group and a control group, 125 cases in each group. The observation group was treated with transcutaneous electrical acupoint stimulation and oral administration of placebo, transcutaneous electrical stimulated at Zusanli (ST 36), Liangmen (ST 21), Taichong (LR 3) etc. The control group was treated with oral administration of Mosapride citrate dispersible tablets, Domperidone and Omeprazole and the placebo treatment of transcutaneous electrical acupoint stimulation, the stimulated position was 3-4 cm to the selected points of the observation group, the amount of the stimulation did not reach the treatment amount. The symptom score, the plasma motilin (MTL) concentration and the somatostatin (SS) concentration were observed before and after treatment of 3 courses.

RESULTSAll symptom scores after treatment were lower than that before treatment in the two groups, the scores of the upper abdominal pain, acid regurgitation, belching and abdominal distention in the observation group were significantly lower than that in the control group (P < 0.05, P < 0.01); the treatments of both two groups can increase the plasma MTL concentration and decrease the SS concentration (both P < 0.001), and the plasma MTL concentration in the observation group was significantly higher than that in the control group (P < 0.01), and the SS concentration was significantly lower than that in the control group (P < 0.05).

CONCLUSIONTranscutaneous electrical point stimulation can more reduce the symptoms of upper abdominal pain, acid regurgitation, belching and abdominal distention, etc. in the functional dyspepsia patients than medication treatment, and can increase the concentration of the plasma MTL and decrease the SS concentration, thus to improve the gastrointestinal motility.

Acupuncture Points ; Adult ; Aged ; Benzamides ; administration & dosage ; therapeutic use ; Domperidone ; administration & dosage ; therapeutic use ; Dyspepsia ; blood ; physiopathology ; therapy ; Female ; Gastrointestinal Agents ; administration & dosage ; therapeutic use ; Humans ; Male ; Middle Aged ; Morpholines ; administration & dosage ; therapeutic use ; Motilin ; blood ; Omeprazole ; administration & dosage ; therapeutic use ; Somatostatin ; blood ; Transcutaneous Electric Nerve Stimulation ; methods ; Treatment Outcome

Phosphatidylinositide 3-kinase (PI3K)/protein kinase B (PKB, Akt) pathway plays a major role in proliferation and survival of many types of cells. The inhibitory effect of LY294002, widely applied as an inhibitor of PI3K, in combination with gemcitabine on proliferation of PANC-1 cells was investigated. The expression of PI3K, phosphorylated Akt (p-Akt) and multidrug-resistance like protein (MRP) in normal pancreas tissues, chronic pancreatitis tissues and pancreatic carcinoma tissues was detected. The effects of LY294002 combined with gemcitabine on proliferation of PANC-1 cells and protein levels of p-Akt and MRP were detected. The results showed that the positive expression rate of PI3K, p-Akt and MRP in pancreatic carcinoma tissues was significantly higher than that in normal pancreas tissues and chronic pancreatitis tissues (P<0.01 and P<0.05 respectively). LY294002 could effectively enhance the inhibitory effect of gemcitabine on proliferation of PANC-1 cells. Furthermore, Western blotting revealed that LY294002 combined with gemcitabine reduced the protein levels of p-Akt and MRP, which contributed to the inhibition of proliferation. It is concluded that LY294002 in combination with gemcitabine may represent an alternative therapy for pancreatic carcinoma.
Adult ; Antimetabolites, Antineoplastic ; administration & dosage ; Cell Proliferation ; drug effects ; Chromones ; administration & dosage ; Deoxycytidine ; administration & dosage ; analogs & derivatives ; Dose-Response Relationship, Drug ; Drug Synergism ; Drug Therapy, Combination ; methods ; Enzyme Inhibitors ; administration & dosage ; Female ; Humans ; Male ; Middle Aged ; Morpholines ; administration & dosage ; Pancreatic Neoplasms ; drug therapy ; pathology ; Phosphatidylinositol 3-Kinases ; antagonists & inhibitors ; Treatment Outcome ; Tumor Cells, Cultured

To develop a sensitive and specific high performance liquid chromatography-tandem mass spectrometric (HPLC-MS/MS) method for the determination of mosapride in human plasma, mosapride and internal standard tamsulosin were extracted from plasma with liquid-liquid extraction, then separated on a Waters ACQUITY UPLC BEH C18 column (50 mm x 2.1 mm, 1.7 microm ID) with gradient elution at flow-rate of 0.25 mL x min(-1). The mobile phase was water (containing 0.3% formic acid) and acetonitrile under gradient conditions. Electrospray ionization (ESI) source was applied and operated in the positive ion mode. Multiple reaction monitoring (MRM) mode with the transitions of m/z 422 --> m/z 198 and m/z 409 --> m/z 228 were used to quantify mosapride and the internal standard, respectively. The linear calibration curve was obtained in the concentration range of 0.17 - 68.00 ng x mL(-1). The lower limit of quantification was 0.17 ng x mL(-1). The inter- and intra-day precision (RSD) was less than 13%, and the accuracy (RE) was within +/- 6.3% calculated from QC samples. The method was used to determine the concentration of mosapride in plasma after a single oral dose of 5 mg mosapride citrate to 20 healthy male Chinese volunteers. The method has been proved to be selective, sensitive, rapid and suitable for pharmacokinetic study of mosapride.
Administration, Oral ; Area Under Curve ; Benzamides ; administration & dosage ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Gastrointestinal Agents ; administration & dosage ; blood ; pharmacokinetics ; Humans ; Male ; Morpholines ; administration & dosage ; blood ; pharmacokinetics ; Sensitivity and Specificity ; Serotonin Receptor Agonists ; administration & dosage ; blood ; pharmacokinetics ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry ; methods

OBJECTIVETo explore clinical short and long-term effect of combining dalitong granule (DG) and electroacupuncture group (EA) in the treatment of functional dyspepsia.

METHODSTotally 640 patients with confirmed functional dyspepsia were randomly divided into 4 groups using a randomized digital table: the DG group, the EA group, the combined group and the control group, 160 cases in each group. The DG group was treated with 6 g DG 3 times daily; the EA group was treated with puncture of points Zusanli (ST36), Zhongwan (CV12), Neiguan (PC6), Taichong (LR3) and Gongsun (SP4) twice daily; the combined group with above-mentioned DG and EA; and the control group with 5 mg mosapride 3 times, 20 mg pantoprazole and 25 mg amitriptylines twice daily. The treatment course was 4 weeks for all groups. The symptom score, quality of life score by Short Form 36 Health Survey Questionnaires (SF-36), plasma motilin by radioimmunoassay, electrogastrographic frequencies by electrogastrogram (EGG) and gastric emptying by B-sonography were examined, and adverse reactions were observed before, at the end of treatment and 60 weeks post-treatment.

RESULTSIn the DG group 1 case dropped out for not taking medicine strictly and 1 case was lost to follow-up, while 1 case in the EA group and 2 cases in the combined therapy group were lost to follow-up. Compared with pre-treatment, quality of life score, plasma motilin, electrogastrographic frequencies and gastric emptying were all increased significantly, while symptom score was decreased significantly at the end of treatment in each group (P<0.01); in the combined group quality of life score, plasma motilin, electrogastrographic frequencies and gastric emptying were all significantly higher than those in the other groups, while symptom score was significantly lower than in the other groups (P<0.05). Compared with at the end of treatment, these indices changed insignificantly in the combined group and the EA group 60 weeks post-treatment (P>0.05), but the 4 increased indices were all decreased significantly, and symptom score was increased significantly in the DG and the control groups (P>0.05). The short and long-term total effective rates in the combined group were all significantly higher than those in the other treatment groups (P<0.05 or P<0.01). No serious adverse reaction occurred in the four groups.

CONCLUSIONCombined treatment of DG and EA could increase both plasma motilin and electrogastrographic frequencies, promote gastric emptying, alleviate the symptom of dyspepsia so as to increase quality of life, with better safety and long-term effect.

Adult ; Amitriptyline ; administration & dosage ; Benzamides ; administration & dosage ; Combined Modality Therapy ; Drugs, Chinese Herbal ; administration & dosage ; therapeutic use ; Dyspepsia ; therapy ; Electroacupuncture ; Electrophysiology ; Female ; Gastric Emptying ; drug effects ; Gastrointestinal Agents ; administration & dosage ; Humans ; Male ; Morpholines ; administration & dosage ; Motilin ; blood ; Quality of Life ; Radioimmunoassay ; Sound Spectrography ; Stomach ; diagnostic imaging ; Ultrasonography

Obesity is associated with a reduction in life expectancy and an increase in mortality from cardiovascular diseases, cancer, and other causes. The U.S. Preventive Service Task Force (USPSTF) recommends screening all adults for obesity. Clinicians should offer or refer patients with a body mass index of 30 kg/m2 or higher to intensive, multicomponent behavioral interventions. Behavioral interventions can lead to a moderate weight loss and improvement in blood sugar and other risk factors for cardiovascular disease. Behavioral interventions decreased the incidence of diabetes diagnosis by about 50% over 2 to 3 years. Orlistat, phentermine, diethylpropion, phendimetrazine, mazindol have been approved as anti-obesity drugs by Korea Food and Drug Administration. The U.S. Food and Drug Administration approved lorcaserin and phentermine plus topiramate combination for treatment of obesity in 2012.
Adult ; Advisory Committees ; Anti-Obesity Agents ; Benzazepines ; Blood Glucose ; Body Mass Index ; Cardiovascular Diseases ; Diethylpropion ; Fructose ; Humans ; Incidence ; Korea ; Lactones ; Life Expectancy ; Mass Screening ; Mazindol ; Morpholines ; Obesity ; Phentermine ; Risk Factors ; United States Food and Drug Administration ; Weight Loss