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The aim of the strategy to formulate the pulsatile drug delivery system using terbutaline sulfate by direct compression technique and evaluate the effects of formulation and dissolution medium on the behavior of drug release, and to clarify the drug release mechanism based on acquiring results. Pulsatile release tablets include a drug and disintegrating agent-containing core and swellable external layers for slow down drug release, then rupturing the nearby surrounding outer layer for fast release. Core tablets prepared using disintegrating agent by direct compression method and coated with polymers like HPMC K100M, ethyl cellulose, karaya gum in different quantities. Several physical parameters of the tablets evaluated such as stiffness, thickness, friability, weight variation, disintegration, drug content and dissolution test. Terbutaline sulfate released from bi-layered tablets with pulsatile behaviors. In-vitro drug release rate readings showed that F3 and F6 are best based on the less quantity of drug release during the lag time (11% and 14% in 5 h). So, from the result, the F6 has nominated the best formulation. Thus, by the direct compression method prepared, coated tablets before drug release with an obvious lag time is possibly useful preparation for the medication of osteoarthritis, rheumatoid arthritis, dysmenorrhea, asthma which follows a circadian rhythm. It confirmed that eroding, diffusion, and swelling mechanisms were responsible for drug release. Ultimate pulsatile release activities may be done by modifying polymeric membrane quantities and proportions to meet the condition of pulsatile activities.

Background: Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effective and efficient therapeutic anti-diabetic agents is continuing. Recent studies support the search for coumarins or related compounds with potential blood glucose-lowering properties. Aim: The study aims to design, synthesize and evaluate the hypoglycemic activity of a new class of 7-hydroxy coumarin derivatives. Objective: To explore and establish the in-silico-driven pharmacological role of a new class of 7- hydroxy coumarin derivatives as the therapeutic strategies against type 2 diabetes mellitus. Methods: A new class of 7-hydroxy coumarin derivatives was designed by assessment of their physicochemical properties and molecular docking against the Glucagon-like peptide-1 (GLP-1) receptor. Two novel series of 30 compounds were synthesized. The chemical structures of all the synthesized analogues have been elucidated by spectral studies of IR, 1H-NMR, and mass spectroscopy. After considering the molecular docking score and their physicochemical properties, the compounds were screened out for the evaluation of their hypoglycemic potential. The compounds were investigated for their hypoglycemic activity using a streptozotocin (STZ) induced diabetic model and an oral glucose tolerance test (OGTT) method at different dose levels. Result: The molecular docking studies of synthesized derivatives reveal significant molecular interaction with the various amino acid residues of the GLP-1 receptor. IR spectral analysis revealed a strong band of -NH stretching in the range of 3406.7-3201.61 cm-1 and one strong band for the lactone carbonyl group of the coumarin ring in the range of 1722.0-1703.5 cm-1, confirming the chemical structure of all produced compounds. The synthesized coumarin analogues with the best docking score exhibited remarkable hypoglycemic potential as assessed by the STZ model and the OGTT method. Conclusion: Coumarin derivatives explored a good structure-activity relationship (SAR) and produced significant hypoglycemic potential.

A new series of coumarin analogs (1a – 1g) were designed and synthesized. The chemical structures of all compounds were elucidated by IR, 1H NMR, 13C NMR, and mass spectroscopy techniques. The synthesized compounds were investigated for their anti-diabetic activity against streptozotocin (STZ) induced diabetes in rats. The albino rats were selected to observe the oral glucose tolerance test (OGTT) by oral intake of aqueous glucose solution (4 g/kg body weight) in normal rats and estimate the blood glucose level after administration of compounds 1e – 1f at 50 and 100 mg/kg, and standard drug glibenclamide at 0.6 mg/kg body weight. Antidiabetic activity was studied by estimating the blood glucose level in diabetic rats. The results showed that all the synthesized coumarin analogs 1a – 1g exhibited antidiabetic potential. Compounds 1e – 1f produced eminent antidiabetic effects in STZ induced diabetic rats.

Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study.

Objective: A novel series of substituted 3,3-diphenyl propanamide derivatives (I-VIII) were synthesized by reacting 3,3-diphenyl propanoyl chloride with different amines/amino acids, and all the derivatives were investigated for anthelmintic, antibacterial, and antifungal activity.Methods: All the compounds were characterized by infrared (IR) and1H- nuclear magnetic resonance spectrometry data. The synthesized derivatives were investigated for their anthelmintic activity employing housefly worms method and earthworm species model. The antibacterial and antifungal activity was performed employing cup plate method.Results: The synthesized compounds (VII and VIII) exhibited maximum anthelmintic activity as compared with standard drug albendazole at doses of 50 and 100 mg/mL, due to minimal paralyzing and death time in both housefly and earthworm models. The compounds (IV, VII, and VIII) at 50 μg/mL exhibited maximum activity against Gram-negative bacterial strains, namely, Escherichia coli, Pseudomonas aeruginosa as compared with ciprofloxacin and same compounds exhibited maximum antifungal activity against Candida albicans and Aspergillus niger in comparison with standard drug griseofulvin at 50 μg/mL.Conclusion: The synthesized compounds bearing amino acid moiety in their structure (VII-VIII) exhibited impressive anthelmintic activity in comparison with albendazole. This suggests that amino acid/peptide derivative of diphenyl propanamides can act as great anthelmintic agents. Further, the research can be performed to design potent antimicrobial diphenyl propanamide derivatives.

Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release. Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR). Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h. Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.

This work examines the treatment of hexamethylenetetramine (HMT) bearing effluent from N, N-dinitroso pentamethylene tetra-mine producing industrial plants in India. Chemical treatment using Fenton's reagent and aerobic treatment using batch reactors with co-substrate were investigated. Aerobic batch reactors integrated with advanced oxidation process of Fenton's reagent provides effective treatment of HMT effluents. Influence of Fenton's reagent dose reaction/contact and effect of varying co-substrate with effluent initial concentration was observed. Higher dose 100 mL of Fenton's reagent with higher reaction time 20 h resulted better degradation (34.88%) of wastewater. HMT hydrolyzes in acidic environment to ammonia and formaldehyde. Formaldehyde under normal conditions is toxic for biological treatment processes. When hydrolysis and acidification in the reactors are accompanied by low pH, aerobic batch reactors with use of co-substrates glucose, sucrose, and cow-dung extract separately in different proportion to wastewater ranging from 0.67 to 4.00, degraded wastewater effectively. Higher proportion of co-substrate to wastewater resulted better degradation. The relationships between nitrate, pH, turbidity and COD are discussed.