Abstract

Troxipide is a novel gastro protective agent with antiulcer, anti-inflammatory and mucus secreting properties. This bioequivalence study was carried out to determine the pharmacokinetic profile of troxipide in plasma in an open label, comparative, randomized, two way cross over design involving two treatments and two periods with one week washout period in 28 healthy male subjects.

Blood samples were collected at intervals up to 28 hours, as per the approved protocol. Plasma concentrations of troxipide were analyzed by high performance liquid chromatography (HPLC) and noncompartmental method was used for pharmacokinetic analysis. The mean (±S.D.) values of the pharmacokinetic parameters (test vs. reference) were Cmax (1052.47±254.41 vs. 1039.10±301.54 ng ml-1), AUC(0-t) (8737.48±1545.24 vs. 8850.04±1892.63 ng h ml- 1 ), AUC(0-∞) (9622.12±1692.57 vs. 9695.02±2133.95 ng h ml-1), and t1⁄2 (7.44±1.85 vs. 7.24±2.10 h). There were no statistically significant differences between Cmax , AUC(0-t) and AUC(0-∞) and their log transformed data (p>0.05) for the test and reference formulations. The 90% of confidence intervals (C.I.s) for the test/reference ratio of mean Cmax , AUC(0-t), and AUC(0-∞) were within the acceptable range of 80.00 to 125.00. The mean (±S.D.) times to maximal plasma concentration (tmax ) of troxipide were 3.04±0.93 vs. 3.07±1.39 h for the test and the reference formulations respectively. Both the formulations were well tolerated.

In conclusion, the two formulations were bioequivalent and may be used interchangeably.

ABSTRACT

Introduction: The use of low dose combination antihypertensive agents is a good contemporary strategy for the treatment of patients with hypertension, a multifactorial disease.

Aim: To assess the clinical efficacy and safety of the fixed low dose combination of S(-)Amlodipine and Atenolol (ESLO-AT) in patients with hypertension, angina pectoris, or both.

Materials & Methods: 48 practicing physicians throughout India collaborated in the recruitment of 154 hypertensive patients, over a period of nine months. These patients were administered fixed low dose combination of 2.5mg S(-)Amlodipine and 50mg Atenolol (ESLO-AT). They were observed for changes in their blood pressure & heart rate over a period of 4 weeks.

Results: Significant decrease in systolic blood pressure, diastolic blood pressure and heart rate by a mean of 32 mmHg (± 2.09 CI 95%), 18 mmHg (± 1.41 CI 95%) and 15 beats/min (± 1.56 CI 95%) respectively were observed after treatment with the fixed low dose combination of S(-)Amlodipine and atenolol (ESLO-AT) for 4 weeks. The JNC VII recommended target blood pressure goal of < 140/90 mmHg was achieved in 77.27% of the patients while 87.33% of them achieved the target heart rate goal of < 83 beats/min at the end of 4 weeks. The combination also reduced incidences of anginal attacks in patients with concomitant angina. The therapy was found to be well tolerated by the study population.

Conclusion: These findings provide further evidence of the role of fixed low dose combination therapy with S(-)Amlodipine and atenolol (ESLO-AT) in the management of hypertension.

Abstract

AIM: To assess the relative bioavailability and pharma- cokinetic properties of two formulations (test and refer- ence) of Lafutidine 10 mg.

METHODS: The study was performed as an open label, randomized, two-way, two-period, two-treatment, single dose cross-over bioequivalence study, under non-fed condition to compare the pharmacokinetic profiles of the lafutidine formulation manufactured by Emcure Pharma- ceuticals Ltd., India using an indigenously developed ac- tive pharmaceutical ingredient (API) and the commercial- ly available Stogra® formulation, of UCB Japan Co., Ltd., Japan. The two treatments were separated by a wash- out period of 5 d. After an overnight fasting period of 10 h, the subjects were administered either the test or the reference medication as per the randomization schedule. Blood samples were collected at intervals up to 24 h, as per the approved protocol. Concentrations of lafutidine in plasma were analyzed by a validated liquid chromatog- raphy/tandem mass spectrometry (LC/MS/MS) method, and a non-compartmental model was used for pharma- cokinetic analysis. The pharmacokinetic parameters were subjected to a 4-way ANOVA accounting for sequence, subjects, period and treatment. Statistical significance was evaluated at 95% confidence level (P ≥ 0.05).

RESULTS: The mean (± SD) values of the pharmacoki- netic parameters (test vs reference) were Cmax (265.15 ± 49.84 ng/mL vs 246.79 ± 29.30 ng/mL, P < 0.05), Area under the curve (AUC)(0-t) (1033.13 ± 298.74 ng.h/mL vs 952.93 ± 244.07 ng.h/mL, P < 0.05), AUC(0-∞) (1047.61 ± 301.22 ng.h/mL vs 964.21 ± 246.45 ng.h/mL, P < 0.05), and t1⁄2(1.92 ± 0.94 h vs 2.05 ± 1.01 h, P < 0.05). The 90% confidence intervals (CI) for the test/reference ratio of mean Cmax, AUC(0-t), and AUC(0-∞) were within the acceptable range of 80.00 to 125.00. The mean times (± SD) to attain maximal plasma concentration (tmax) of lafutidine were 0.95 ± 0.24 h vs 1.01 ± 0.29 h (P < 0.05) for the test and the reference formulations respectively. Both the formulations were well tolerated.

CONCLUSION: In summary, this study has demon- strated the bioequivalence of the two formulations of lafutidine 10 mg. Hence it can be concluded that the two formulations can be used interchangeably in clinical set- tings.

ABSTRACT

Introduction: Hypertension, being a multi factorial disease, is well managed by using fixed dose combination of antihypertensive agents.

Aim: To assess the safety and clinical efficacy of the fixed dose combination of S(-)Amlodipine and Hydrochlorothiazide (ESLO-D) in patients with hypertension.

Materials & Methods: Seventy four practicing physi.zians throughout India collaborated in the recruitment of 145 hypertensive patients, over a period of eight months. These patients were administered fixed dose combination of 2.5mg S(-)Amlodipine and 12.5mg Hydrochlorothiazide (ESLO-D). They were observed for adverse events and changes in their blood pressure and heart rate over a period of four weeks.

Results: Significant decrease in systolic blood pressure, diastolic blood pressure and heart rate by a mean of 22.95 ± 11.77 mmHg, 12.57 ± 8.62 mmHg and 5.84 ± 6.69 beats/min respectively were observed after treatment with the fixed dose combination of S(-) Amlodipine and hydrochlorothiazide (ESLO-D) for 4 weeks. The JNC VII recommended target blood pressure goal of < 140/90 mmHg was achieved in 80% of the patients while 67.74% of them achieved the target heart rate goal of < 83 beats/min at the end of 4 weeks. The combination also decreased systolic blood pressure by 18% among patients with isolated systolic hypertension. The therapy was found to be well tolerated by the study population.

Conclusion: These findings provide further evidence of the role of fixed dose combination therapy with S(-)Amlodipine and hydrochlorothiazide (ESLO-D) in the management of hypertension, including isolated systolic hypertension.

Key words: Hypertension, S(-)Amlodipine, Hydrochlorothiazide, fixed dose combination, blood pressure

ABSTRACT

Background and Objective: Tolperisone hydrochloride is a centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm. The present observational study was undertaken to assess the safety and efficacy of Tolperisone (Myotop-150) in Indian patients.

Settings and Design: An observational study involving 92 physicians across the various states of India, who prescribed Tolperisone (Myotop-150) to their patients.

Methods and Material: The demographic exposure and outcome data of the patients who were prescribed Myotop-150 (Tolperisone hydrochloride) were obtained from the completed case record forms which were received from the physicians. Adverse events which were observed during the therapy were recorded. Symptom severity was given a scoring on a 7-point Likert scale before and after the therapy.

Results: Data was collected for 165 patients, with a mean age of 43.88 ± (SD) 11.27 years [Range: 15 to 72 years]. At the baseline, the mean ± SD of the score on the 7-point Likert scale was 4.96 ± 1.01. After treatment with tolperisone, the mean score was 1.87 ± 0.91, with a significant reduction of 3.08 ± 1.14; p < 0.0001. After therapy, 42.04% of the patients reported “no problem”. In 88.02% of the patients who were treated, the physicians rated the treatment with tolperisone as excellent, very good or good. Side-effects were observed in 7.88% of the patients.

Conclusions: The present observational study demonstrates that the therapy with tolperisone is an effective and well- tolerated strategy in patients with diseases or conditions which are associated with spasticity or muscle spasm.

Abstract

Aim: To compare the efficacy and safety of ferrous ascorbate and colloidal iron in children with iron deficiency anemia.

Study Design: An open, randomized, comparative, parallel-group study

Place and Duration of Study: Department of Pediatric Medicine of ‘Nilratan Sircar Medical College and Hospital’, Kolkata, India, between January 2009 and February 2010.

Methodology: Children between the age group of 6 months to 12 years were included if they had anemia defined as hemoglobin <10 gm%. Children received treatment with either ferrous ascorbate or colloidal iron for 12 weeks. Each child received elemental iron 3 mg/kg body weight/day. Follow-up assessments were performed at the end of week 4, week 8 and week 12.

Results: Out of the 137 children screened, 80 were included in the analysis. The mean rise in hemoglobin at the end of the 12 weeks was significantly higher in ferrous ascorbate group than colloidal iron group [3.24 ± 1.66 gm% vs. 1.42 ± 2.04 gm%; p <0.01]. Responder rate (hemoglobin ≥11.5 gm%) after 12 weeks of therapy was 53.57% in ferrous ascorbate group versus 10.34% in colloidal iron group; p<0.01.

Conclusion: The study provides evidence for the role of ferrous ascorbate as an efficient oral iron supplement in the treatment of iron deficiency anemia in children.

Abstract

Objective The present study was undertaken to assess the impact of intravenous iron sucrose (Feronia IV) in the treatment of iron deficiency anemia observed in gynecological and obstetrical practice. Methods Seventy-seven practicing gynecologists and obstetricians throughout India collaborated in the recruitment of 145 women over a period of 1 year, of which 143 were analyzable cases. Results The overall mean rise in hemoglobin level was observed to be 2.43 gm % at the end of 4 weeks. The dose of iron sucrose administered ranged from 100 to 1,050 mg. In women who received 200 mg of the drug, and the mean Hb rise was found to be 2.21 ± 1.06 gm %. The highest observable rise in hemoglobin level was 5.5 gm % with 800 mg of iron sucrose. No serious adverse reactions were reported during the observation period. Conclusion Intravenous Iron sucrose is a safe and effective treatment for the rapid reversal of iron deficiency anemia, in obstetric and gynecological settings.

Keywords

Anemia Iron sucrose Hemoglobin Pregnancy

Aims: To evaluate the symptomatic efficacy and safety of Lafaxid™ (lafutidine 10 mg) in Indian patients with Acid Peptic disorder (APD).

Study Design: An observational, prospective, uncontrolled, open-label multi-centric study.

Place and Duration of Study: Patients were recruited from 12 cities across India by 61 investigators, between October 2010 and December 2011.

Methodology: We included 1500 patients (973 men, 527 women; age range 15-85 years) with Acid Peptic disorder. Lafutidine (10 mg tablets) was prescribed by the physicians as once daily dose (OD) for 28 days. The efficacy was analysed based on the change in the symptom baseline score on the 100 point Visual Analogue Scale (VAS) for individual symptoms, and the safety was determined based on adverse events reported during the study with the prescribed usage of lafutidine on day 14 and day 28 after start of the treatment.

Results: Lafutidine monotherapy was given to 1378 patients. A very high reduction in the mean VAS score was observed from baseline for individual symptoms, viz. nausea, vomiting, belching, heart burn, epigastric pain, acid regurgitation, abdominal bloating & loss of appetite at the end of the study. The global mean VAS score (a sum of individual symptom VAS score) of these patients decreased from 120.34 ± 67.58 to 14.18 ± 26.97 at the end of the study (P < .001). There were 124 APD patients, previously treated but uncontrolled, with acid inhibitors like PPIs, H2RAs etc., also showed a significant reduction (157.42 ± 83.88 to 26.47 ± 46.34) in the VAS score on day 28 (P<.001). During the entire study, adverse events of mild and moderate nature were observed in 0.4% (6 patients) of the total patient population.

Conclusion: The present study demonstrates that therapy with Lafaxid™ is symptomatically effective and well tolerated in patients with APDs.

Abstract

Aims: To assess the efficacy of lafutidine therapy versus rabeprazole in Indian patients with endoscopically and histologicaJly proven gastritis and peptic ulcer

Study Design: A double blind, double dummy, randomized, comparative study

Plate and Duration of Study: Global Liver and Gastroenterology Centre, Bhopal, India, between March 2010 and October 2010.

Methodology: A total of 100 patients were enrolled, including 50 with endoscopically and histologically proven gastritis and other 50 with peptic ulcer (over 5 mm in diameter). Each group was randomized to receive either lafutidine or rabeprazole tablet and their corresponding competitor placebo dummy tablet, for a period of 4 weeks. Cure rate was confirmed endoscopically at the end of week 4 as compared to the baseline evaluation. Symptom response and Helicobacter pylori (H. Pylori) eradication were also compared among the two drugs at the end of the treatment period.

Results: Complete cure of gastritis was observed in all the patients (100%) treated with lafutidine and 95.24% [20/21; 95% Cl: 76.18 to 99.88%] patients treated with rabeprazole. Complete cure of ulcer was observed in 72.0 (18/25, 95% Cl = 50.61 to 87.93%) and 79.16% (19/24, 95% Cl = 57.85 to 92.87%) patients treated with lafutidine and rabeprazole respectively. There was no significant difference in gastritis/ulcer cure rate and symptom response rate between the two treatment groups at the end of the study. H pylori eradication rates was 82.61% (19/23) in lafutidine group vs 47.37% (9 /19) in rabeprazole group (L\=35.2%, 95% Cl = 3.2 to 67.3%; P= .023). Both, lafutidine and rabeprazole were well tolerated during the entire study.

Conclusion: Endoscopically proven cure rate in patients suffering from gastritis and peptic ulcers is found to be comparable after 4 weeks treatment with Lafutidine and rabeprazole, but lafutidine showed better H. pylori eradication rate as compared to rabeprazole.

Abstract

Objective To compare the efficacy of ferrous ascorbate and colloidal iron in the treatment of iron deficiency anemia in children.

Methods Eighty one children, aged 6 mo to 12 y, were screened for iron deficiency anemia (IDA) and those diagnosed with IDA were randomized to receive ferrous ascorbate or colloidal iron for a period of 12 wk, such that each child received elemental iron 3 mg/kg body weight/d. Increase in hemoglobin (Hb) level was the primary outcome measure. Assessment was performed at baseline, wk 4, wk 8 and wk 12.

Results Of 81 children screened, 73 were included in the study. The mean rise in Hb at the end of the 12 wk was significantly higher in ferrous ascorbate group than the colloidal iron group [3.59±1.67 g/dl vs. 2.43± 1.73 g/dl; P<0.01]. Significantly higher proportion of children receiving ferrous ascorbate (64.86 % vs. 31.03 %; P<0.01) became non-anemic in comparison to colloidal iron.

Conclusions Ferrous ascorbate provides a significantly higher rise in hemoglobin levels in comparison to colloidal iron. The study supports the use of ferrous ascorbate in the pediatric age group, providing evidence for its role as an efficient oral iron supplement in the treatment of iron deficiency anemia.