Journal of Pharmaceutical and Medicinal Chemistry

Globally, an estimated 422 million adults are living with diabetes mellitus, according to the latest 2016 data from the World Health Organization. Diabetes is a group of disorder characterized by high blood glucose level. Constant high level of blood glucose may lead to many life-threatening complications viz, cardiovascular disease, stroke, chronic kidney disease, foot ulcers, and damage to the eyes. The treatment strategy is mainly targeted to lower blood glucose level by one or other means. This can be achieved by either slowing down the rate by which glucose enters into the bloodstream (Biguanides: Metformin; α-Glucosidase inhibitor: Acarbose etc) or by stimulating body’s ability to utilize the glucose present in the blood by the cells (Sulfonylureas: Chlorpropamide; Thiazolidinediones: Pioglitazone; GLP-1 analogue; DPP 4 inhibitors; Exenatide). This review focuses on conventional antidiabetics currently used and drawbacks associated with it and newer oral hypoglycemic agents with their advantages over the conventional ones.

A simple, economic, rapid, accurate and stability indicating RP-HPLC method was developed for the estimation of amount of of Dalfampridine in pure and tablet dosage form. The method was performed on Phenomenex C18 (125 X 4.6 mm, 5 µm) using the mobile phase composed of buffer (0.01M sodium acetate pH 4.5): methanol in the ratio of 60:40 v/v. Th flow rate was maintained at 0.8 mL/min. The retention time for Dalfampridine was found to be 1.713 min. The method was found to be linear in the range of 5-25 µg/mL and the regression equation was found to be y=14691x-12844. For intra- and inter-day precision the %RSD for Dalfampridine was found to be 0.218 and 0.622%. Percentage mean recovery was found to be 98.36%. LOD and LOQ values obtained for Dalfampridine were found to be 0.107 µg/mL and 0.323 µg/mL respectively. Acid, alkali, oxidative, thermal and neutral degradation studies were performed. The results are analysed statistically and are found to be satisfactory. Hence this method can be routinely applicable for analysis of Dalfampridine in pure and tablet dosage form. Keywords: Dalfampridine, RP-HPLC, Recovery, Dosage form.

Pyrazolopyrimidines are the fused heterocyclic ring systems which structurally resemble with purines, and exhibit important biological actions. Pyrazolopyrimidines derivatives have great importance in the field of chemical synthesis, agriculture and pharmaceutical industries due to their wide range of applications. Over the past few decades, researchers have focused their research on the synthesis of novel pyrazolopyrimidine derivatives. The pyrazolopyrimidines heterocyclic ring is an integral part of various synthetic compounds with wide range of therapeutic and pharmacological potentials like anti-inflammatory, antibacterial, anticancer, antifungal, antiviral, anticonvulsant, anti-tubercular, etc Many marketed drugs are pyrazolopyrimidine derivatives like antiviral drugs which include acyclovir, ganciclovir, didanosine, abacavir and adefovir. Due to the wide scope of pharmacological potentials of pyrazolopyrimidine derivatives, research community has shown great interest to discover new pyrazolopyrimidines having potent bioactivities with no or lesser side effects. This review summarizes the recent developments on the synthetic approaches, mechanism of action and anticancer activity of pyrazolopyrimidines.

Keywords: Pyrazolopyrimidines, Anticancer

Background: This research focused on HPTLC method for the simultaneous estimation of natural antioxidant markers namely rutin, gallic acid and quercetin from the plant extract of Cucumis melo var agrestis (CME). Aims and Objectives: The main aim of this research is to extract and simultaneously quantitate the three antioxidant markers-rutin, gallic acid and quercetin from CME by using normal phase HPTLC. Materials and Methods: Separation of compounds was performed on TLC aluminium plates precoated with silica 60 F254 after that detection of rutin, gallic acid and quercetin. Camag TLC scanner 3 prepared with win CATS software was used for densitrometric scanning at 254 nm. This method was additional validated in terms of linearity, precision, accuracy and sensitivity as per the ICH guidelines. Results: A good linear relationship was obtained for the calibration plots with R2 = 0.9957, 0.9909, and 0.9920 for rutin, gallic acid and quercetin respectively. Accuracy was checked by recovery study performed at three different stages with the average recovery between 95% and 98% for all the three markers. Conclusion: This developed method of HPTLC can be used for the detection of antioxidant markers in botanicals and herbal formulations.

Keywords: Bioflavonoids; Rutin; Gallic acid; Quercetin; Antioxidant and Developed method of HPTLC.

The proposed work was accurate and precise stability indicating RP-HPLC method has been developed and validation of Sofosbuvir, in tablet dosage form. The separation was achieved on a Kromasil C18 (4.6×250 mm, 5µ) column using a mixture of Methanol: water (60: 40% v/v) as the mobile phase at a flow rate of 1.0 mL/min and detected 247 nm. The retention time of sofosbuvir 3.475 minutes. The linear responses in the concentration range of 10-60 µg/mL of Sofosbuvir. The method precision for the determination of assay was less than 2.0% RSD. The method is useful in the quality control of bulk and pharmaceutical formulations.

Keywords: Sofosbuvir; RP-HPLC; Validation; Tablet dosage forms.

A novel, rapid, precise and accurate high performance liquid chromatographic method was developed and validated for the simultaneous determination of Sitagliptin phosphate and Simvastatin in bulk drug and pharmaceutical formulation. The components were separated on Ymc Cyano (150 mm × 4.6 mm I.D., 5 μm particle size) with a mobile phase composed of 20 mM ammonium formate and acetonitrile in the ratio of 50:50 v/v (Adjust the pH to 3.5 with 0.1% formic acid) at a flow rate of 1.2 mL/min. The response was measured at 218 nm. The peaks were detected at 5.33 minutes and 4.19 minutes for Sitagliptin phosphate and Simvastatin respectively. Calibration curves were found to be linear (r2=0.999 for both Sitagliptin phosphate and Simvastatin respectively) over the concentration range of 2.5-200 µg/mL for Sitagliptin phosphate and 1-80 µg/mL for Simvastatin. The method was validated for linearity, precision, accuracy, ruggedness and robustness. The proposed method can be applicable for simultaneous quantitation of Sitagliptin phosphate and Simvastatin in tablet dosage form. Validation results assured that the recommended method was specific, rapid, reliable and reproducible. Good percent recoveries and low % RSD reveals the suitability of the present method for analysis of Sitagliptin phosphate and Simvastatin in quality control laboratories.

Keywords: Sitagliptin; Simvastatin; RP-HPLC; Estimation.