Crystal structure of (E)-N-{2-[2-(4-methylbenzylidene)hydrazin-l-yl]-2-oxoethy1}-p-toluene- sulfonamide

The title acyl­hydrazone derivative, C17H19N3O3S, containing an amino acid moiety and electron-donating substituents attached to both the phenyl rings, crystallized with two independent mol­ecules (A and B) in the asymmetric unit. The mol­ecules are bent at the S atom, with C-SO2-NH-CH2 torsion angles of -67.3 (2) and 67.7 (3)° in mol­ecules A and B, respectively. Further, the dihedral angles between the sulfonyl­glycine segments and the p-toluene­sulfonyl rings are 76.1 (1) and 85.8 (1)° in mol­ecules A and B, respectively. The central hydrazone segments and the toluene rings attached to them are almost co-planar with their mean planes being inclined to one another by 5.2 (2) (mol­ecule A) and 2.9 (2)° (mol­ecule B). The dihedral angles between the benzene rings are 86.83 (12) (mol­ecule A) and 74.00 (14)° (mol­ecule B). In the crystal, the A mol­ecules are linked by a pair of N-H...O hydrogen bonds, forming inversion dimers with an R22(8) ring motif. The dimers are linked via three N-H...O hydrogen bonds involving the B mol­ecules, forming chains along [100] and enclosing R22(12) and R44(16) ring motifs. The chains are linked via C-H...O hydrogen bonds and a C-H...[pi] inter­action, forming sheets parallel to (010). There is a further C-H...[pi] inter­action and a slipped parallel [pi]-[pi] inter­action [inter-centroid distance = 3.8773 (16) Å] between the sheets, leading to the formation of a three-dimensional framework

Diethazine Hydrochloride as a New Redox Indicator in Cerimetric Titration of Fe(II), U(IV), Mo(V), Hydroquinone & Ascorbic Acid

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Crystal structure of (E)-N-{2-[2-(3-chlorobenzyl-idene) hydrazinyl]-2-oxoethyl}-4-methylbenzene-sulfonamide monohydrate

The mol­ecule of the title compound, C16H16ClN3O3S·H2O, is L-shaped being bent at the S atom; the S-N-C-C torsion angle is 132.0 (3)°. The central part of the mol­ecule, C-C-N-N=C, is almost linear, with the C-C-N-N and C-N-N=C torsion angles being -174.1 (2) and 176.0 (2)°, respectively. The dihedral angle between the p-toluene­sulfonyl ring and the S-N-C-C(=O) segment is 67.5 (4)°, while that between the two aromatic rings is 52.17 (11)°. In the crystal, the water H atom is involved in O-H...O hydrogen bonds with a sulfonamide O atom and the carbonyl O atom. The water O atom is itself hydrogen bonded to both NH hydrogen atoms. These four hydrogen bonds lead to the formation of corrugated sheets lying parallel to (100). There are also weak C-H...O contacts present within the sheets

1,8-Bis(3-chloro­anilino)-N,N′-bis­(3-chloro­phen­yl)octane-1,8-diimine

There are two half-mol­ecules in the asymmetric unit of the title compound, C32H30Cl4N4, in both of which the N—H bonds are syn to the meta-chloro substituents in the adjacent benzene ring. The other two Cl atoms of these two mol­ecules are disordered with occunpancy ratios of 0.79 (2):0.21 (2) and 0.68 (1):0.32 (1). Adjacent chloro­phenyl rings make dihedral angles of 74.3 (2) and 63.0 (2)° in the two mol­ecules. In the crystal, inter­molecular N—H⋯N hydrogen bonds link the mol­ecules into infinite chains

ZIPRASIDONE HYDROCHLORIDE LOADED NANOSTRUCTURED LIPID CARRIERS (NLCS) FOR INTRANASAL DELIVERY: OPTIMIZATION AND IN VIVO STUDIES

Objective: The present study was an attempt to systemically deliver the most desirable schizophrenia drug, ziprasidone hydrochloride (ZRS) via the intranasal route using nanostructured lipid carrier (NLC) approach. Methods: The desired ZRS loaded NLCs were developed using central composite statistical design and the developed formulation was monitored for improving ZRS bioavailability and their brain targeting efficacy. Results: Pharmacokinetic studies revealed a 10 fold increase (ZRS blood-brain ratio) for NLCs administered through nasal route (in comparison to intravenous route). Similarly, the concentration of ZRS (in the brain) delivered via nasal route exhibits 4 fold increment at all-time points. Conclusion: Therefore, the obtained results suggest a potential nose to brain transport of loaded ZRS by effective bypassing of the Blood-Brain Barrier (BBB)

Effect of Methyl Parathion on Survival and Development of Tadpoles of Indian Cricket Frog Fejervarya Limnocharis

Amphibian populations are declining due to various causes including pesticide contamination in natural habitat. We evaluated effect of Methyl Parathion (MPT) an organophosphate pesticide on survival and development of common paddy field frog Fejervarya limnocharis in a laboratory condition. Effect of 0 µg MPT/L, 500 µg MPT/L, 1000 µg MPT/L, 1500 µg MPT/L, 2000 µg MPT/L and 3000 µg MPT/L was studied using static toxicity test for a duration of 28 days. MPT reduced the survival of tadpole. The mortality increased with the increased concentration of pesticide. The development decreased with increased MPT concentrations. At higher concentrations, MPT induced slow development and tadpoles failed to metamorphose. It is assumed that slow development could affect the larval life and amphibian population in agro-ecosystem

DEVELOPMENT OF pH-DEPENDENT CHRONOMODULATED DELIVERY SYSTEMS OF 5-FLUOROURACIL AND OXALIPLATIN TO TREAT COLON CANCER

Objective: To develop two different oral formulations such as 5-fluorouracil (5-FU) tablets and oxaliplatin (OX) microspheres which were further filled into capsules and coated with pH-sensitive polymer (eudragit S-100) for the chronotherapeutic treatment of colon cancer (Fluorouracil: Oxaliplatin regimen) to perform as a substitute for intravenous (IV) route based chronomodulated chemotherapy. Methods: The 5-FU tablet formulation was prepared with alginate and guar gum polymers in varied concentrations using wet granulation technique in two varieties such as granules coated and tablet coated formulations using eudragit RSPO as coating material to achieve controlled drug release. Alongside OX microspheres were formulated using the ionotropic gelation methodology in combination with alginate and chitosan polymers in varying concentrations to accomplish a time-controlled drug release. Prepared formulations were evaluated for pre-compression and post-compression parameters, percentage yield, percentage drug entrapment, Fourier transformed infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), In vitro and Ex vivo dissolution studies. Results: Pre-compression and post-compression parameters for 5-FU tablets were satisfied with Indian pharmacopeia specifications. The entrapment efficiency of OX microspheres were increased due to the elevated concentration of polymers up to a certain level as seen in A7M, further greater the concentration of polymer resulted in a decline of entrapment efficiency as seen in A4M and A8M. The optimized formulations A14T and A14M were shown in vitro drug release of 90.36 % by 24 h and 79.63 % by 9 h respectively. Conclusion: The two different oral formulations of 5-FU (Tablets) and OX (Microspheres) were found to be successful in controlled drug release. Therefore they can be efficiently used to control the rate of drug release to the colon in synchronization with the circadian timing system in the belief of improved therapeutic efficacy, tolerability and overall survival rate of cancer patients. Hence it is promised to be a better alternative for intravenous route based chronomodulated chemotherapy

A REVIEW ON THE ROLE OF NANOCRYSTALS AND NANOSUSPENSIONS IN DRUG DELIVERY SYSTEMS

Nearly 40% of drugs coming to the market nowadays are having poor solvency related issues and 70% molecules in discovery pipeline are in effect fundamentally insoluble in water. Nanocrystals is an unmistakable instrument to tackle the issue identified with poor fluid solvency and helps in improving the bioavailability of various drugs as presented in the literature. The particle size reduction came about into temperamental nanocrystalline system and the phenomenon of ostawald ripening happens. These techniques are preparing to the improvement of nanosized objects, which can play out multiple technological tasks. There are a few couples of noteworthy benefits of nanocrystal formulations, for example, upgrade oral bioavailability, improved dose proportionality, reduced food effects, appropriateness for administration by all routes and probability of sterile filtration because of diminished particle size range. One of the most adequate preferences of nanocrystals is their wide scope of utilization, for example, ophthalmic delivery, oral delivery, transdermal delivery, pulmonary delivery, intravenous delivery and targeted delivery, especially for tumour and brain. The increment in commercial value of nanocrystals just as the measure of nanocrystal products in the market is picking up more of attention to be utilized as a strategy so as to get commercial advantages. In this paper a brief and accurate precis of nanosuspension is stated with specific spotlight on nanosuspension preparation methodologies, benefits and few major applications of nanosuspensions

FORMULATION AND EVALUATION OF SOLID SELF MICRO EMULSIFYING DISPERSIBLE TABLET OF PIROXICAM

Objective: The aim of this study was to formulate the solid self-micro emulsifying dispersible tablets for promoting the dissolution of Piroxicam. Methods: Solubility study test was performed to know the solubility of various oil phase, surfactants, cosurfactants. Self-emulsifying grading test was done by visual grading system. Ternary phase diagrams and droplet size analysis test were performed to screen and optimize the Piroxicam-self microemulsifying drug delivery system (SMEDS). Then microcrystalline cellulose (KG802) was added as a suitable adsorbent and dispersible tablet were prepared by wet granulation compression method. Results: The final composition of Piroxicam-SMEDS was oil phase (oleic acid, 23%), surfactant (Cremophor R H-40,61%), co-surfactant (PEG-400,16%) based on the result of solubility test, self-emulsifying grading test, droplet size analysis and ternary phase diagrams. Microcrystalline cellulose (KG802) was selected based on dissolution study (98.35%) and added to liquid Piroxicam-Smeds formulation to form dispersible tablets. The in vitro dissolution study showed 98.02 % of drug release from Piroxicam-SMEDS tablets. Conclusion: Piroxicam–Self microemulsifying dispersible tablets have increased the solubility and bioavailability of the Piroxicam to a greater extent. SMEDS formulation can help the solubility of poorly water-soluble drugs

Forage Potential of Summer Annual Grain Legumes in the Southern Great Plains

Winter wheat (Triticum aestivum L.) and perennial warm-season grasses are the primary forage resources for grazing yearling stocker cattle (Bos taurus) in the US Southern Great Plains (SGP). However, low nutritive value of perennial grasses during mid to late summer limits high rates of growth by stocker cattle. In response, there has been a continued search for plant materials with the potential to provide forage high in crude protein (CP) and digestibility during August through September. A broad range of under-utilized legume species that are grown as grain crops in Africa, India, and South and Central America may have some capacity to serve as high quality pasture or harvested forage in the SGP. However, any crop selection must account for limitations related to unpredictable summer rainfall amounts and patterns, and the frequent occurrence of prolonged drought. Further, any selection should not create water deficits for following winter wheat, the primary forage and grain crop in the region. This article summarizes a small subset of the broad range of underutilized grain legumes (pulses) which exist worldwide and soybean [Glycine max (L.) Merr.] that may have capacity to serve as high quality forage for late-summer grazing. Bringing these crops into forage–stocker production systems could improve the overall system effectiveness, in addition to providing other ecosystem services (e.g., ground cover, grain crops)