Selective detection of azelnidipine in pharmaceuticals via carbon dot mediated spectrofluorimetric method: A green approach.

A spectrofluorimetric method using fluorescent carbon dots (CDs) was developed for the selective detection of azelnidipine (AZEL) pharmaceutical in the presence of other drugs. In this study, N-doped CDs (N-CDs) were synthesized through a single-step hydrothermal process, using citric acid and urea as precursor materials. The prepared N-CDs showed a highly intense blue fluorescence emission at 447 nm, with a photoluminescence quantum yield of ~21.15% and a fluorescence lifetime of 0.47 ns. The N-CDs showed selective fluorescence quenching in the presence of all three antihypertensive drugs, which was used as a successful detection platform for the analysis of AZEL. The photophysical properties, UV-vis light absorbance, fluorescence emission, and lifetime measurements support the interaction between N-CDs and AZEL, leading to fluorescence quenching of N-CDs as a result of ground-state complex formation followed by a static fluorescence quenching phenomenon. The detection platform showed linearity in the range 10-200 µg/ml (R2 = 0.9837). The developed method was effectively utilized for the quantitative analysis of AZEL in commercially available pharmaceutical tablets, yielding results that closely align with those obtained from the standard method (UV spectroscopy). With a score of 0.76 on the 'Analytical GREEnness (AGREE)' scale, the developed analytical method, incorporating 12 distinct green analytical chemistry components, stands out as an important technique for estimating AZEL.

Development and Validation of Stability-indicating RP-HPLC Method for Estimation of Pranlukast Hydrate in its Laboratory Mixture.

Pranlukast hydrate is an anti-asthmatic drug and used in the treatment of acute asthma. Stability-indicating RP-HPLC method for pranlukast hydrate has been developed and validated. The reverse phase high performance liquid chromatographic method was developed using Shimadzu Column: Kromosil 100 C18 (150 mm × 4.6 mm × 5 µm) and mobile phase Acetonitrile: 0.1% Glacial acetic acid (85: 15% v/v). Eluent was monitored with UV-detector at 262 nm with a flow rate of 0.5 mL/min, temperature maintained at 30°C. Stress testing was carried out in acidic, alkaline, oxidative, photolytic and dry heat degradation conditions. The method was validated as per the International Conference for Harmonization guidelines and includes specificity, accuracy, precision, linearity and limit of quantitation and detection parameters. A relative standard deviation <2% indicates the developed method was precise. The accuracy of the method was represented by recovery studies ranging between 99.41 and 99.72%. In acid, alkaline, oxidative stress conditions, pranlukast hydrate degrades significantly and in photolytic, dry heat, hydrolytic conditions remain stable. This proposed method is suitable for the analysis of pranlukast hydrate in its laboratory mixture.

Repurposing of Iloperidone: Antihypertensive and ocular hypotensive activity in animals.

PURPOSE: Iloperidone, second generation antipsychotic drug, reported in clinical trial to produce orthostatic hypotension as side effect. It was claimed to be antagonistic at alpha adrenergic receptor in central nervous system. We evaluated effect of Iloperidone on peripheral alpha 1 adrenoreceptor by in silico and in vitro methods while in vivo hypotensive, antihypertensive and ocular hypotensive activity was evaluated in animals. METHODS: Pharmacological activity prediction of Iloperidone was done using PASSOnline and SwissTargetPrediction softwares and molecular docking with Alpha 1A adrenoreceptor using AutoDock Vina. Hypotensive activity in normotensive and antihypertensive activity against DOCA-salt induced hypertension in rats were evaluated at doses 0.03 mg/Kg and 0.1 mg/Kg, i.p of Iloperidone. Blood pressure was measured by invasive blood pressure measurement technique using PowerLab 4/30 and intraocular pressure was measured using digital tonometer. RESULTS: Iloperidone (0.1 mg/Kg) showed significant decrease in blood pressure (38.96 ± 1.1%) in normotensive rats, while in DOCA salt induced hypertensive rats, systolic blood pressure was found to be decreased by 29.04 ± 1.45% and 31.43 ± 1.21% in 0.03 mg/Kg and 0.1 mg/Kg treated rats respectively. Iloperidone prevented rise in systolic BP with adrenaline. Intraocular pressure was found to be decreased by 36.66 ± 3.15% in rabbits after 1 h of instillation of 0.1% Iloperidone. CONCLUSION: Iloperidone exerted hypotensive and/or anti-hypertensive activity in rats and ocular hypotensive activity in rabbits.

Assessment of the antidiabetic potential of Cassia grandis using an in vivo model.

The aqueous and ethanolic extracts of C. grandis (Family: Leguminosae) were evaluated for antidiabetic activity by a glucose tolerance test, in normal rats and alloxan-induced diabetic rats. The aqueous and ethanolic extracts showed that they significantly lowered the blood glucose levels to normal in the glucose tolerance test. In alloxan-induced diabetic rats the maximum reduction in blood glucose was observed after three hours, at a dose level of 150 mg/kg of body weight. The percentage of protection given by the aqueous and ethanolic extracts was 32.72 and 46.42%, respectively. In the long-term treatment of alloxan-induced diabetic rats, the degree of protection was determined by measuring the blood glucose, cholesterol, and triglycerides on the tenth day. Both the extracts showed a significant antidiabetic activity comparable to that of glibenclamide. These results showed that the Cassia grandis possessed significant antidiabetic activity.