Posted by admin on May 31, 2023 in |
Pyrazolines, among the various 5-membered heterocyclic compound derivatives, have drawn attention towards it because of their various pharmacologic activities. They are nitrogenous heterocyclic compounds containing two nitrogens in the adjacent position, which possess considerable biological activity. The synthesis of pyrazolines was initiated after the pioneering work of Fischer and Knoevenagel in the late 19th century. Later, Claisen-Schmidt condensation, and Aldol-condensation, became the most popular methods for the preparation of pyrazolines nowadays. It has been an exciting area of pharmaceutical chemistry to research the biological evaluation of pyrazoline derivatives. The review provides different methods for the synthesis of pyrazolines by Claisen-Schmidt condensation, Aldol-condensation, 1,3-Dipolar Cycloaddition and its biological activities like anti-inflammatory, anti-tubercular, hypotensive, Cannabinoid CB1 Receptor Antagonist activity, anti-viral, etc. It also gives information regarding different possible docking targets and examples in figures. This review article will help explore novel pyrazoline analogues for challenging pathophysiological...
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Posted by admin on May 31, 2023 in |
The present investigation aimed to provide an approach for the solubility and bioavailability enhancement by Comparative solubility of cyclodextrins with Lornoxicam (LXM) by forming ternary Inclusion complexation (TIC). The phase-solubility and saturation solubility studies were executed in the existence of β-CD, HP-βCD and polymers. The drug/CD complexes were formulated and characterized further to confirm complex formation using DSC and FTIR. The solid dispersions (SDs) were formulated using double hydrophilization and accessed using FT-IR, DSC, and in-vitro testing. The equilibrium phase solubility and saturation solubility study for both binary and TIC showed a more significant solubility enhancement of LXM-HP β-CD- poloxamer-407(PXM 407) than LXM-β-CD. The FT-IR and DSC analysis confirmed the formation of a TIC amongst LXM-HP-βCD-PXM 407. The TIC demonstrated a higher Complexation Efficiency (CE) and stability constant than binary. The drug dissolution rate (DR) profile showed significant drug release from developed TIC and improved DR to a greater extent. From comprehensive study findings, it can be stated that employing the TIC of LXM-HP β-CD with PXM 407 might...
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Posted by admin on May 31, 2023 in |
Aegle marmelos (L) Correa also known as Bale, belongs to family Rutaceae. The plant is used to treat several diseases like bronchitis, asthma, malarial, astringent, laxatives, digestive and febrifuge. Leaves are used as antipyretic, antimicrobial, antidiabetic, antihistaminic, anti-inflammatory, antioxidant, and hyperlipidaemic activity. The plant contains diterpenoids, triterpenoids, and phenolic compounds. The present investigation was carried out to isolate, purify, and characterize active constituents from the Aegle marmelos (L) Correa plant. Powdered material of the whole Aegle marmelos (L) Correa plant was taken to prepare extract using Soxhlet apparatus. Various phytochemical tests were performed for alkaloids, glycosides, phenolic, flavonoids, etc. TLC was done for the isolation of compounds. GC-MS, thin layer chromatography, and Nuclear magnetic resonance further characterized the isolated compounds. The anti-asthmatic was evaluated by using in-vitro models. The Petroleum ether extract of Aegle marmelos (L) Correa significantly inhibited histamine contraction and confirmed the significant anti-asthmatic...
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Posted by admin on May 31, 2023 in |
Simvastatin, a lipid-lowering agent, belongs class-II drug of BCS. It has a short biological half-life (3hr), and high first-pass metabolism. The target of the present study was to prepare the microbeads of Simvastatin to provide control release of the drug with enhanced bioavailability through sustained release. The method adopted to prepare Simvastatin loaded microbeads was by the ionic gelation method using a mixture of natural polymers like sodium alginate and aloe vera (1:1). Different crosslinking agents like BaCl₂, FeCl₃, ZnCl₂ and CaCl₂ formulated microbeads. The microbeads were spherical, free-flowing with uniformity in drug content and high drug encapsulation efficiency. The swelling and drug release behavior correlate with the crosslinking agent used to prepare microbeads. The FTIR analysis of the drug, polymers, and the optimized formulation confirmed the compatibility of the drug with the polymers. The DSC studies indicated no interaction between the drug and polymer in the microbeads. Formulation FB-1 showed the extended drug release of more than 6 hours. The novelty of a recent study assures that the...
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Posted by admin on May 31, 2023 in |
Human memory can store and recall previously learned information to be applied for the routine purpose. Memory disorders caused by diseases can have an impact on an individual’s quality of life as well as their overall cognitive abilities. Memory disorders are associated with the alteration in cholinergic neurotransmission. The herbal extract of Euphorbia prostrata was found to be used traditionally for the maintenance of memory-related disorders, but the active constituent and its mechanism were still unrevealed. Thus, in the current study, a ligand library was prepared with some potential lead molecules from the plant Euphorbia prostrata and was computationally screened to identify the most potent ligand responsible for the memory enhancement effect as establishing the probable mechanism of action involved in it. Ellagitannin was found to be the most potent ingredient of the Euphorbia prostrata plant, which is supposed to have a memory enhancement effect. Ellagitannin is supposed to exert its therapeutic effect via an agonistic effect on the muscarinic receptor, muscarinic acetylcholine G-protein coupled receptor, N-methyl-D-aspartate receptor, as...
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