Formulation, In-Vitro Evaluation and Comparative Study Ofitopride Hydrochloride Loaded Sustained Release Matrix Tablet Using Okra Mucilage as a Natural Binder

Natural polymers are abundantly available in plants with their wider pharmaceutical applications and are preferred more than some synthetic polymers because of their biodegradable, biocompatible and non-toxic properties. The study aims to formulate Itopride Hydrochloride loaded Sustained Release (SR) matrix tablet from the mucilage extracted from okra plant (Abelmoschus esculantus) and carry out the comparative study on the release retardant effect of synthetic binders like HPMC K100M and sodium carboxymethyl cellulose and their combinations. The extraction of the mucilage was carried by the maceration process. The formulation of Itopride loaded SR matrix tablet was carried by moist granulation technique. The micrometric, physiochemical studies and purity tests confirms the suitability of mucilage as an excipient. Pre-compression study suggests good flow property of the powders. The minimum angle of repose was observed in F7 with 29.03±0.6º and F2 exhibited maximum angle of repose with 34.30±0.5º. Carr's index and Hausner's ratio was lower in F1 with 11.56±0.4 and 1.11±0.3 respectively. Drug-excipient interaction study performed using FTIR spectrophotometry suggested no interaction between the drug and excipients. The in-vitro drug release of Itopride Hydrochloride loaded SR tablet up to 12 hours in 0.1 N HCl was conducted and observed to be maximum in F3 with 87.34±5.33% and minimum in F6 with 77±5.65 %. Drug release from the formulations were significant compared to the marketed product of Itopride Hydrochloride (p<0.05). The data were analyzed by Tukey post hoc multiple comparison test.

Multitarget therapy in patients with GERD and obesity

The article presents the results of a clinical study involving 59 overweight or obese patients with gastroesophageal reflux disease. Non-erosive reflux disease was diagnosed in 30 (51%), erosive esophagitis A (Los Angeles endoscopic classification) in 29 (49%) patients. The severity of the main symptoms of GERD was assessed, physical examination, esophagogastroduodenoscopy, daily pH impedance monitoring of the upper gastrointestinal tract, psychometric testing were performed. The body mass index correlated with age (0.35); the presence of a diaphragmatic hernia (0.32); cough (0.35); pH in the stomach (0.30); the number of slightly alkaline gastroesophageal refluxes (0.32); slightly alkaline time in the esophagus in minutes (0.30) and percent (0.32); reactive anxiety (0.30), number of points of FF scale (–0.26) and MH scale of the SF-36 questionnaire (–0.25). Waist circumference correlated with the presence of erosive esophagitis (0.25); male sex (0.32); diaphragm hernia of (0.40); duodenogastric reflux (0.42); DeMeester index (0.31), the duration of the longest acid gastroesophageal reflux (0.25). Patients with erosive esophagitis compared with patients with non-erosive reflux disease more often consumed alcohol; had higher BMI; more often had epigastric pain and oral bitterness, longer bolus time in the esophagus and poorer quality of life according to the MH scale of the SF-36 questionnaire. Taking into account the revealed features of pathogenesis, the drugs of choice in the treatment of GERD in overweight and obese patients may be multitarget molecules of itopride hydrochloride (Itomed®), ursodeoxycholic acid (Ursosan®) and rebamipid (Rebagit®).

COMPARATIVE EVALUATION OF THE EFFICACY AND TOLERABILITY OF ITOPRIDE HYDROCHLORIDE AND DOMPERIDONE IN PATIENTS WITH NONULCER DYSPEPSIAAT JLNMC, BHAGALPUR, BIHAR

Background :Prokinetic drugs are widely used for treatment of non-ulcer dyspepsia (NUD). Aims and Objectives : To assess the efficacy and tolerability of a new prokinetic agent, itopride hydrochloride in patients of NUD and compare it with domperidone. Methods : Fifty-six patients who fulfilled the inclusion and exclusion criteria were enrolled in the study. Patients underwent upper gastrointestinal endoscopy to rule out organic pathology as a cause for their symptoms. The patient’s symptoms were graded on a 4-point scale (0 to 3) at the beginning of treatment and at the end of Week-one and Week-two Patients were randomly allocated to receive either one tablet of itopride hydrochloride 50mg three times daily or one tablet of domperidone 10mg three times daily for two weeks. Pre-treatment and post-treatment hemogram, liver function and renal function tests, prolactin level and ECG were done in all patients. The response to therapy was evaluated by assessing the relief of symptoms at the end of two weeks on a 5 -point scale. Statistical analysis was done using two-tailed paired t-test; Wilcoxon matched pairs ranks sum test, Mann-Whitney-U test and chi-square test as applicable. Results : Of the fifty-five patients enrolled in the study (age range of 18-60 yrs, median age of 35yrs), 26 were males and twenty nine were females. They had a median duration of symptoms for 4 weeks. Twenty-seven patients received itopride and 28 received domperidone. One patient did not follow up in the domperidone group, thus 54 patients were evaluable for analysis. Moderate to complete symptomatic relief was observed in 22 (81%) patients in the itopride group and 19 patients (70%) in the domperidone group (p > 0.05, NS). Both the drugs were well tolerated and neither caused prolongation of QT interval nor any abnormality in any serum biochemistry values. Conclusion : Therapy with itopride resulted in good symptomatic relief, was safe, well tolerated and comparable in efficacy to domperidone in relieving the symptoms of NUD. By virtue of its efficacy and tolerability, it could be an ideal choice for providing symptomatic relief to patients suffering from non-ulcer dyspepsia.

Efficacy of Prokinetic Itopride in Type 2 Diabetes Mellitus

The constant increase in the incidence of diabetes in the world and the high frequency of lesions of the upper gastrointestinal tract with impaired motor function in this category of patients, on the one hand, worsen the clinical picture, and on the other, reduce the effectiveness of sugar-lowering therapy. Currently, specialists have at their disposal a number of prokinetics that contribute to the restoration of the motor-evacuation function of the stomach, but many of them have many undesirable effects. The aim of our study was to evaluate the effectiveness of itopride hydrochloride in the treatment of patients with chronic gastritis associated with Helicobacter pylori and type 2 diabetes. During the study, both general clinical and more specific research methods were used, in particular, esophagogastroduodenoscopy. According to the results of the study, the use of prokinetics in the treatment of patients with type 2 diabetes mellitus reduces the manifestations of impaired motor-evacuation function of the upper gastrointestinal tract. The results obtained indicate to verify the manifestations of chronic gastritis in patients with type 2 diabetes mellitus and the identification of motor dysfunction and the need for prokinetic therapy.

Treatment of patients with a duodenal ulcer with disorders of the motor evacuator function of the stomach and duodenal

Aim. The study of disorders of the motor-evacuation function of the stomach and duodenum (duodenum) in patients with duodenal ulcer and their use in choosing effective therapy.Materials and methods. The study included 107 patients with ulcerous duodenal ulcer with the presence of motor-evacuation disorders of the gastroduodenal zone — group I and 99 patients with ulcerous duodenal ulcer without a violation of motor-evacuation function of the stomach and duodenum — group II. Anamnestic and physical data, results of X-ray and endoscopic examinations were used in verification of the ulcer. Assessment of the motor function of the stomach and duodenum was carried out using the gastroenteromonitor GEM-01 “Gastroskan-GEM”. Depending on the treatment method, patients with ulcerous duodenal ulcer of group I were divided into 2 groups: observation group — 52 patients with ulcerous duodenal ulcer of the duodenal ulcer received 50 mg 3 times a day prokinetic itopride hydrochloride as a part of complex anti-ulcer therapy and a comparison group — 55 patients with ulcerous duodenal ulcer underwent standard antiulcer therapy.Results. In the observation group after treatment, pain disappeared in 90.0% of patients, decreased in 10.0%. In the comparison group, pain completely disappeared in 18.8% of patients, decreased in 76.6%, remained unchanged in 4.7%. Against the background of treatment in patients of the observation group, the frequency and amplitude of the stomach and duodenum corresponded to the normokinetic type of curve. When using itopride hydrochloride in the treatment of patients of the observation group, restoration of the closure function of the pylorus was revealed. After the treatment, the ulcer healed in the observation group in 97.8% of patients (in 88.2% of cases at the stage of a high-quality “white” scar); in the comparison group, ulcer healing occurred in 94.5% of cases, of which in 67.1% — in the stage of poor-quality “red” scar).Conclusion. The use of the prokinetics of itopride hydrochloride as part of complex therapy increases the effectiveness of the treatment of ulcerative duodenal ulcer by restoring the motor-evacuation function of the stomach and duodenum.

Comparative evaluation of efficacy of Pinaverium monotherapy and combination therapy of Pinaverium with itopride hydrochloride in patients with cross irritable bowel syndrome with constipation and postpradial distress syndrome

Forty-seven patients with overlap between irritable bowel syndrome with constipation and (IBS-C) and postpradial distress syndrome (PDS) complying with Rome III criteria were treated with pinaverium in combination with itopride and 58 patients with IBS-C-PDS overlap were treated with pinaverium for 4 weeks. Clinical symptoms and quality of life by SF-36 were estimated at baseline and after 4 weeks of treatment. Pinaverium and Itopride combination therapy significantly improved both IBS-C and PDS-like symptoms, and SF-36 scores when compared to Pinaverium monotherapy over a 4-week period.

The comparative effects of Itopride and Levosulpiride orally used in patients suffering from Non-ulcer dyspepsia

Background: Itopride and Levosulpiride both comes under the group of Prokinetic drugs. These drugs are used for the treatment of non-ulcer dyspepsia, heart burn, nausea and vomiting. Both drugs act on dopaminergic D2 receptor as antagonist and increases the concentration of acetylcholine so that gastric peristalsis will be increase and that time pressure at lower oesophageal sphincter will be increase thus gastric motility increases and there will be good gastro-duodenal co-ordination.Method: This study has to conduct on patients with complains of non-ulcer dyspepsia attended Medical outdoor and department of pharmacology of SKMCH Muzaffarpur, Bihar, India. The total 60 patients have to include in the study, which have to randomly divide in two groups. Group A (itopride) comprising of 30 patients and Group B (Levosulpiride) comprising of 30 patients. Patients have to randomly allocate to receive one tablet of itopride hydrochloride, 50 mg three times daily before meal and one tablet Levosulpiride of 75 mg three times daily before meal. Authors have to enroll the patients at the interval of two weeks and continue it upto 3 months.Results: Study did not found any remarkable change in biochemistry profile. Only QT prolongation changes were found in two patients, but no serious cardiac toxicity was observed with patient receiving Levosulpiride. Neither QT prolongation nor serious cardiac toxicity was observed with itopride hydrochloride therapy.Conclusions: In present study, efficacy of Itopride was comparable to Levosulpiride in relieving the symptoms of non-ulcer dyspepsia. Both the drugs were clinically and biochemically well tolerated. QT prolongation changes were found in two patients, but no serious cardiac toxicity was observed with patient receiving Levosulpiride. Itopride does not show cardiac toxicity and any changes in ECG.