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

Extraction, Characterization and Pharmacological Evaluation of Aegle marmelos Leaves

In the present day, antibiotic drugs are gradually becoming obsolete due to the development of antimicrobial resistance. As a result, the scientific community is in search of new antibiotic drugs which can be safely administered to the patents. Natural products are generally known for their nontoxic nature and many of them are known to produce a variety of pharmacological activities. The aim of this work is to extract the leaves of Aegle marmelos, phytochemical characterization of the extract, identification of phytoconstituents by thin layer chromatography, ATR-FTIR Spectroscopy of extract and evaluation of its antimicrobial activity. Extraction of the leaves of Aegle marmelos has been conducted using a Soxhlet apparatus. About 10.32% yield of extract was obtained. Phytochemical screening of the ethanolic leaf extract by standard methods showed the presence of secondary metabolites such as alkaloids, carbohydrates, phenolic compounds, flavonoids, saponins and triterpenoids which were confirmed by TLC. ATR-FTIR Spectroscopic study was conducted to determine the type of functional groups present in extract. The ethanolic leaf extract also produced antibacterial activity against gram positive bacteria Staphylococcus aureus and gram-negative bacteria Escherichia coli and zone of inhibition was 14 mm and 16 mm respectively when compared to standard antibiotic tetracycline. From this research it can be inferred that ethanolic leaf extract of Aegle marmelos has antimicrobial activity because of the presence of secondary metabolites in it. Further investigation will hereby be conducted in future regarding the route of administration of the extract and the type of dosage form. &nbsp

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

PHYTOCHEMICAL INVESTIGATION AND EVALUATION OF IN VITRO ANTIOXIDANT ACTIVITY OF THE PLANT CYPERUS TEGETUM ROXB

Objective: The objective of the present study is to isolate the lead molecules and the antioxidant activity is also evaluated. Method: Cyperus tegetum Roxb. (Cyperaceae) is found in the tribal area of West Midnapur district of West Bengal, India. It is commonly known as Madur Kathi. Different chromatographic techniques, namely, thin-layer chromatography, column chromatography, and high-performance liquid chromatography (HPLC) were used to isolate and identify the different secondary metabolites. Results: The different spectral studies (nuclear magnetic resonance [NMR], infrared [IR], and ultraviolet [UV]) confirmed the presence of stigmasterol as an isolated compound from the extract of C. tegetum (ECT). HPLC analysis revealed the presence of flavonoids, namely, rutin (retention time [Rt]: 3.00), myricetin (Rt: 3.9), and quercetin (Rt: 5.6) and phenolic acids, namely, gallic acid (Rt: 4.0), caffeic acid (Rt: 5.4), chlorogenic acid (Rt: 7.3), and ferulic acid (Rt: 8.8) in ECT. ECT showed strong reducing power, diphenyl-2-picrylhydrazyl hydrate radical, superoxide anion scavenging, and hydrogen peroxide scavenging activities when compared to standard compounds. Conclusion: From this study, several flavonoid and phenolic compounds were identified by RP-HPLC analysis. Flavonoids are rutin, quercetin, and myricetin and phenolic compounds are gallic acid, ferulic acid, chlorogenic acid, and caffeic acid, respectively. The different spectral studies (NMR, IR, and UV) confirmed the presence of stigmasterol as an isolated compound from ECT