Phytochemical screening and in vitro antibacterial activity of Moringa oleifera (Lam.) leaf extract

The aim of the study was to investigate the phytochemical constituents and antibacterial activity of ethanolic extract of Moringa oleifera Lam. belonging to family Moringaceae. Distilled water and ethanol was used to extract the bioactive compounds from the leaves of M. oleifera to detect the phytochemical constituents and to screen its antibacterial activity. The phytochemical constituents were screened by qualitative analysis method. The phytochemical screening indicated the presence of tannins, flavonoids, glycosides, terpenoids, phenols, etc., in leaf extract of M. oleifera. The antibacterial activity of ethanolic leaf extract of M. oleifera was examined against gram positive bacteria (Staphylococcus aureus) and gram negative bacteria (Escherichia coli). Antibacterial assay were done with ethanolic extract of M. oleifera in volumes 50, 100, 150 and 200 μL/well, using agar well diffusion method. The study showed that ethanolic extract of M. oleifera showed potent antibacterial activity against S. Aureus and E. coli

ENDORSEMENT OF SMALL PATIENTS POPULATION STUDY THROUGH DATA MINING CLASSIFICATION: SIGNIFICANCE TO MANIFEST DRUG INTERACTION STUDY OF CARDIOVASCULAR DOSAGE FORMULATION

Objective: A simple, sensitive, precise computational classifiers justifies the positive indication of drug interaction through statistical validation and confirms for further root level investigation. Methods: The blood pressure (BP) & Lipid profile valued data sheet was prepared from 100 patients those were chronically treating with cardiovascular formulation consisting Atorvastatin 10mg + Olmesartan 20mg. The data sheet contains 100 patients with 10 variables and final decision attributes of working & non-working. Then, with the operation of seven different related classifier the details of % of accuracy by class, correct & incorrect classified instance and stratified cross- validation were estimated. Those statistical results of classifiers were compared, correlate and interpreted to bring a fixed conclusion based on it. Results: The % of accuracy for all classifiers results commonly 95.9596 %, 93.9394 % and 96.9697 % and inter-depending class attributes denoting by a = NW & b =W Matrix values are 84│11, 84│9, 87│9 respectively. Thus, the accuracy is excellent covering within the limits of (±15%) as a correct classified instant. Conclusion: Statistical computation on less populated patients through classifiers, evidentially confirms the drug-interaction profile of collected data through data mining process. So that, it can proceeds further upto root level through instrumental bioanalysis. Â&nbsp

Prevalence and predictors of metabolic syndrome with comparison of myoinositol and metformin in PCOS women

Background: The objective is to determine the prevalence of metabolic syndrome (MBS) and the effects of insulin sensitizers to improve the clinical and hormonal milieu for better reproductive outcome in PCOS women.Methods: This prospective cross-sectional study was conducted on 50 PCOS women and 50 age matched control to determine the prevalence of the MBS in two tertiary hospitals over one year. Diagnosis of PCOS was based on at least two of ESHRE/ASRM criteria and diagnosis of MBS was based on at least three of NCEPATPIII criteria. Patients already diagnosed as PCOS were treated with insulin sensitizers myoionositol and metformin which were compared.Results: The study revealed that the prevalence of MBS was 40 % (20/50) nearly 4-fold higher than that of control groups. Among PCOS women, the most prevalent MBS factors were high BMI (52%) and low serum HDL-C (42%). The least prevalent factor was high fasting serum glucose level (16%). The resumption of spontaneous regular menstrual cycle and pregnancy rate in infertile groups of PCOS patients with myoionositol and metformin were 61% vs. 26% and 50% vs.91% respectively. The myoionositol group did not require any extra ovulating agents for pregnancy, while 7 out of 11 patients in metfromin group needed clomiphen citrate for ovulation induction to achieve pregnancy.  With myoinositol there is significant reduction of weight, BMI, LH/FSH ratio and fasting insulin level; whereas metformin shows decrement of weight and BMI only.Conclusions: The prevalence of MBS in PCOS is nearly 4 times in present study and there is significant improvement of symptom profile, weight, BMI and change of hormonal pattern in myoinositol group

Prospective observational study of vancomycin injection in SLED patient of ethnic Indians

As the Vancomycin is itself a nephrotoxic antibiotics, so it is sometime recommended to the Slow-low Efficiency Dialysis (SLED) patients against highly resisted infection. In this case, the dose monitoring is strictly maintained after Intravenous injection. The collected blood was analyzed for its concentration in HPLC for 11 patients and the half life was evaluated to study Therapeutic drug monitoring. The T1/2 of evaluated vancomycin is 39.12+ 6.81 hrs. The mean of the systemic clearance is 16.91+6.99 and mean Vd is 0.57+ 0.147. Comparatively the reported study of Mean + SD of half-life, volume of distribution, and systemic clearance were 43.1 + 21.6 hours, 0.84 L/kg + 0.17 L/kg, and 24.3 mL/min + 8.39 mL/min respectively. Thus the t-test of the means was 0.5828, degree of freedom (df) was 20, standard error of difference was 6.829 and so, the two-tailed P value is 0.5665 i.e. P > 0.5. In ethnic Indian SLED patients, T1/2 of mean + SD of 39.12 + 6.81 hrs was compared to the Caucasian patients i.e, 43.1 + 21.6 hrs. And the t-test and P-value is 0.5828 & 0.5665 respectively. Thus it was concluded that the half-life of ethnic Indian patients is less in compare to Caucasians but this difference is not so significant. The half-life of ethnic 8 patients is less than 40 out of 11 patients.Keywords: Vancomycin assay; Slow-low efficiency dialysis; Pharmacokinetic analysis; Ethnic indian

DETERMINATION OF METFORMIN AND SITAGLIPTIN IN HEALTHY HUMAN VOLUNTEERS' BLOOD PLASMA AND ITS BIOEQUIVALENCE STUDY UNDER FASTING CONDITION

Objective: Metformin hydrochloride and sitagliptin are the oral anti-hyperglycemic medications used to treat type 2 diabetes and are used in combination to treat patients. In this work, we have developed a bioanalytical method for simultaneous estimation of both the drugs form some formulation and subsequently the validation of the developed method metformin and sitagliptin in human plasma. Methods: The stability studies were done as per USFDA and EMA guidelines. The sample extraction approach presented here was a straightforward liquid extraction. The linearity range of metformin was 11.72 ng/ml to 3000 ng/ml, and sitagliptin was 4.68 ng/ml. to 1200 ng/ml. For metformin, the LOD was 1.0 ng/ml, and LLOQ was 11.72 ng/ml. and for sitagliptin, the LOD was 0.75 ng/ml, and LLOQ was 4.68 ng/ml. LC-ESI-MS/MS was used to develop and validate this method using the Phenomenex Kinetex C18 column. Milli-Q water containing 10 mmol Ammonium Acetate (pH =3.6) and Acetonitrile containing 0.1% Formic Acid (pH =2.4) as solvent systems for the estimation of Sitagliptin in a single dose. Metoprolol is used as an Internal Standard. Results: The total chromatographic run time was only 7.0 min, and the elute time of metformin and sitagliptin was 3.94 min and 3.97 min, respectively. Relative Bioavailability was found at 101.14% for Metformin and 96.96% for Sitagliptin. The overall results show that the Cmax, AUC0-t, and AUC0-∞ for metformin and sitagliptin were within the acceptable limit of 80%-125%. Conclusion: This bioanalytical method was successfully applied in the bioequivalence study. The study design was a randomized, open-label, two treatment, two-period, two sequences, single-dose, crossover bioequivalence study under fasting conditions

Bioequivalence study of two formulations containing 400 mg dexibuprofen in healthy Indian subjects

Objective: This study presents the results of two-period, two-treatment crossover investigations on 24 healthy Indian male subjects to assess the bioequivalence of two oral formulations containing 400 mg of dexibuprofen (CAS 51146-56-6). An attempt was also made to study the pharmacokinetics of dexibuprofen in the local population of Indian origin.Method: Both of the formulations were administered orally as a single dose separated by a one-week washout period. The concentration of dexibuprofen in plasma was determined by a validated HPLC method with UV detection using carbamazepine as internal standard. The formulations were compared using the parameters area under the plasma concentration-time curve (AUC0-t), area under the plasma concentration-time curve from zero to infinity (AUC0-∞), peak plasma concentration (Cmax), and time to reach peak plasma concentration (tmax).Results: The results of this investigation indicated that there were no statistically significant differences between the logarithmically transformed AUC0-∞ and Cmax values of the two preparations. The 90 % confidence interval for the ratio of the logarithmically transformed AUC0-t, AUC0-∞ and Cmax were within the bioequivalence limit of 0.8-1.25 and the relative bioavailability of the test formulation was 99.04 % of that of reference formulationjok?.Conclusion: Thus, these findings clearly indicate that the two formulations are bioequivalent in terms of rate and extent of drug absorption. Both preparations were well tolerated with no adverse reactions observed throughout the study

BIOEQUIVALENCE STUDY OF AZELNIDIPINE 16 MG TABLET TO EVALUATE PHARMACOKINETIC PROFILE OF SINGLE DOSE IN HEALTHY, ADULT, HUMAN VOLUNTEERS UNDER FASTING CONDITION

Objective: The present study's objective is to conduct a comparative bioavailability study with a special emphasis on the test product's bioequivalence using a standard reference product as a comparator. Methods: Before initiating the bioequivalence study, the plasma sample analysis method was developed and validated by using LC-MS/MS method. The entire study was conducted as a single-dose crossover randomized bioequivalence study with open-label, two treatment, two-period, and two sequences on 24 healthy volunteers under fasting condition. With proper informed consent process the oral dose of the Reference product (R) or Test product (T) was administered on healthy volunteers at 0 h during each period of the study. After the drug's oral administration, a certain quantity of blood sample was collected, and the plasma sample was separated using a cold centrifuge. The plasma samples were analysed by using the validated LC-MS/MS method. The pharmacokinetic parameters, statistical data and ANOVA of the test and reference product were evaluated. Results: The Cmax, Auc0-t, AUC0-∞ and tmax of the test product were found to be 6.29 ng/ml, 117.0 ng. h/ml, 161.67 ng. h/ml and 3.33 h. respectively. And the Cmax, Auc0-t, AUC0-∞ and tmax of reference product were found 6.59 ng/ml, 123.21 ng. h./ml, 172.20 ng. h/ml and 3.38 h respectively. Relative bioavailability was found 94.96%. The overall results show that the 90% confidence intervals (Log-Transformed and Untransformed) for Cmax, AUC0-t and AUC0-∞ for Azelnidipine were within the acceptable limit of 80%-125%. Conclusion: The entire study's conclusion can be drawn as the test product was bioequivalence with the reference product's comparator

AN LC-MS/MS BASED BIOANALYTICAL APPROACH TO RESOLVE PHARMACOKINETIC INVESTIGATION OF ACOTIAMIDE HYDROCHLORIDE AND ITS APPLICATION TO BIOEQUIVALENCE STUDY

Objective: Acotiamide, a prokinetic drug used to treat Functional Dyspepsia, which acts by modulating gastric motility. However, in this present study, a simple and accurate bioanalytical method was developed for the estimation of Acotiamide in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS) and validated according to US-FDA guideline. Methods: The method was developed in blank human blood plasma; propranolol was used as internal standard (IS). Protein Precipitation technique was followed for the extraction of the drug from the plasma sample. In liquid chromatography, the C18 analytical column (50 x 3 mm, particle size-5 μm) was used; as a mobile phase, 0.1% formic acid in Mili Q water, and ACN with methanol (1:1) used, at 0.50 ml/min flow rate. Detection was done by positive electrospray ionization (ESI) with a run time of 7 min in multiple reaction monitoring (MRM) mode. Eight calibration concentrations were taken, ranging from 1.5625-200 ng/ml for Acotiamide. Different stability studies were performed and obtained results found within the acceptable range. Moreover, a comparative pharmacokinetic analysis was done in 24 healthy human volunteers in a single dose, randomized, crossover study. Results: The precursor to production reaction was; m/z 451.200 → 271.200 for Acotiamide and m/z 260.300 → 116.100 m/z for IS. The obtained calibration curve was linear, with a mean r2value 0.9953. Among the pharmacokinetic parameters, Cmax and Tmax were 25.71±2.31,23.61±2.32 ng/ml; 2.54±0.12, 2.43±0.21 h for reference and test samples, respectively. Conclusion: No major adverse events were noted in the clinical phase, the developed method was accurate and linear; obtained pharmacokinetic parameters hence represented

Assessment of preclinical pharmacokinetics and acute toxicity of pioglitazone and telmisartan combination

The prevalence of hypertension is very common amongst the diabetic patients and is reported as the major cause of mortality in diabetes. Pioglitazone reported to have an ability to alter the blood cholesterol level and cardioprotective efficiency along with its antidiabetic activity. Telmisartan, through activation of PPAR-γ receptor exerts insulin sensitizing property in addition to its primary cardioprotective efficiency. Theoretically, a combination of pioglitazone and telmisartan may be beneficial to effectively control the high blood glucose level and management of coexisting cardiovascular complication in diabetes. The aim of this research was to experimentally evaluate the pharmacokinetic interaction of pioglitazone and telmisartan when are coadministered in rat. Pioglitazone and telmisartan were administered orally as a single dose individually and in combination to the rats. The plasma samples of the pharmacokinetic study were analyzed using a validated LCMS method. The acute toxicity of the combination with a high dose in rats was also evaluated as a part of the determination its safety profile. There was no significant change in pharmacokinetic parameters were resulted due to coadministration of pioglitazone and telmisartan in rat. Absence of major toxicological effect supports the safety of the combination in vivo