Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery

The goal of the present study is to develop polymeric matrix films loaded with a combination of free diclofenac sodium (DFSfree) and DFS:Ion exchange resin complexes (DFS:IR) for immediate and sustained release profiles, respectively. Effect of ratio of DFS and IR on the DFS:IR complexation efficiency was studied using batch processing. DFS:IR complex, DFSfree, or a combination of DFSfree+DFS:IR loaded matrix films were prepared by melt-cast technology. DFS content was 20% w/w in these matrix films. In vitro transcorneal permeability from the film formulations were compared against DFS solution, using a side-by-side diffusion apparatus, over a 6 h period. Ocular disposition of DFS from the solution, films and corresponding suspensions were evaluated in conscious New Zealand albino rabbits, 4 h and 8 h post-topical administration. All in vivo studies were carried out as per the University of Mississippi IACUC approved protocol. Complexation efficiency of DFS:IR was found to be 99% with a 1:1 ratio of DFS:IR. DFS release from DFS:IR suspension and the film were best-fit to a Higuchi model. In vitro transcorneal flux with the DFSfree+DFS:IR(1:1)(1 + 1) was twice that of only DFS:IR(1:1) film. In vivo, DFS solution and DFS:IR(1:1) suspension formulations were not able to maintain therapeutic DFS levels in the aqueous humor (AH). Both DFSfree and DFSfree+DFS:IR(1:1)(3 + 1) loaded matrix films were able to achieve and maintain high DFS concentrations in the AH, but elimination of DFS from the ocular tissues was much faster with the DFSfree formulation. DFSfree+DFS:IR combination loaded matrix films were able to deliver and maintain therapeutic DFS concentrations in the anterior ocular chamber for up to 8 h. Thus, free drug/IR complex loaded matrix films could be a potential topical ocular delivery platform for achieving immediate and sustained release characteristics

2-(6-Chloro-2,3,4,9-tetra­hydro-1H-carbazol-1-yl­idene)propane­dinitrile

The mol­ecular conformation of the title compound, C15H10ClN3, is stabilized by an intra­molecular N—H⋯N hydrogen bond with an S(7) ring motif. The crystal packing is controlled by N—H⋯N and C—H⋯N inter­molecular inter­actions. One of the methyl­ene groups of the cyclo­hexene ring is disordered over two positions with refined occupancies of 0.457 (12) and 0.543 (12)

6-Bromo-2-(3-phenyl­allyl­idene)-2,3,4,9-tetra­hydro-1H-carbazol-1-one

Mol­ecules of the title compound, C21H16BrNO, are linked through pairs of N—H⋯O inter­molecular hydrogen bonds into centrosymmetric R 2 2(10) dimers. One of the C atoms of the cyclohex-2-enone ring is disordered with refined occupancies of 0.61 (2) and 0.39 (2)

6-Bromo-2-[(E)-thio­phen-2-yl­methyl­idene]-2,3,4,9-tetra­hydro-1H-carbazol-1-one

In the title compound, C17H12BrNOS, the cyclo­hexene ring deviates only slightly from planarity (r.m.s. deviation for non-H atoms = 0.047 Å). In the crystal, the mol­ecules are linked into centro­symmetric R 2 2(10) dimers via pairs of N—H⋯O hydrogen bonds. The thio­phene ring is disordered over two positions rotated by 180° and with a site-occupation factor of 0.843 (4) for the major occupied site

Antimicrobial Constituents from Machaerium Pers.: Inhibitory Activities and Synergism of Machaeriols and Machaeridiols against Methicillin-Resistant Staphylococcus aureus, Vancomycin-Resistant Enterococcus faecium, and Permeabilized Gram-Negative Pathogens

Two new epimeric bibenzylated monoterpenes machaerifurogerol (1a) and 5-epi-machaerifurogerol (1b), and four known isoflavonoids (+)-vestitol (2), 7-O-methylvestitol (3), (+)-medicarpin (4), and 3,8-dihydroxy-9-methoxypterocarpan (5) were isolated from Machaerium Pers. This plant was previously assigned as Machaerium multiflorum Spruce, from which machaeriols A-D (6-9) and machaeridiols A-C (10-12) were reported, and all were then re-isolated, except the minor compound 9, for a comprehensive antimicrobial activity evaluation. Structures of the isolated compounds were determined by full NMR and mass spectroscopic data. Among the isolated compounds, the mixture 10 + 11 was the most active with an MIC value of 1.25 μg/mL against methicillin-resistant Staphylococcus aureus (MRSA) strains BAA 1696, -1708, -1717, -33591, and vancomycin-resistant Enterococcus faecium (VRE 700221) and E. faecalis (VRE 51299) and vancomycin-sensitive E. faecalis (VSE 29212). Compounds 6-8 and 10-12 were found to be more potent against MRSA 1708, and 6, 11, and 12 against VRE 700221, than the drug control ciprofloxacin and vancomycin. A combination study using an in vitro Checkerboard method was carried out for machaeriols (7 or 8) and machaeridiols (11 or 12), which exhibited a strong synergistic activity of 12 + 8 (MIC 0.156 and 0.625 µg/mL), with \u3e32- and \u3e8-fold reduction of MIC\u27s, compared to 12, against MRSA 1708 and -1717, respectively. In the presence of sub-inhibitory concentrations on polymyxin B nonapeptide (PMBN), compounds 10 + 11, 11, 12, and 8 showed activity in the range of 0.5-8 µg/mL for two strains of Acinetobacter baumannii, 2-16 µg/mL against Pseudomonas aeruginosa PAO1, and 2 µg/mL against Escherichia coli NCTC 12923, but were inactive (MIC \u3e 64 µg/mL) against the two isolates of Klebsiella pneumoniae

<span style="font-size:12.0pt;font-family: "Times New Roman";mso-fareast-font-family:"Times New Roman";mso-ansi-language: EN-GB;mso-fareast-language:EN-US;mso-bidi-language:AR-SA" lang="EN-GB">Solvent free microwave assisted synthesis and evaluation of potent antimicrobial activity of 1,11<i style="mso-bidi-font-style:normal">H</i>-pyrimido[4,5-<i style="mso-bidi-font-style:normal">a</i>]carbazol-2-ones, 1,11<i style="mso-bidi-font-style:normal">H</i>-pyrimido [4,5-<i style="mso-bidi-font-style:normal">a</i>]carbazol-2-thiones and pyrazolo[3,4-<i style="mso-bidi-font-style:normal">a</i>]carbazoles</span>

414-421Microwave assisted condensation of urea, thiourea and hydrazine hydrate with 1-chloro-2-formyl carbazoles in the presence of PTSA as catalyst yields 1,11H-pyrimido[4,5-a]carbazol-2-ones, 1,11H-pyrimido[4,5-<i style="mso-bidi-font-style: normal">a]carbazol-2-thiones and pyrazolo[3,4-<i style="mso-bidi-font-style: normal">a]carbazoles, respectively. The structures of the synthesized compounds have been confirmed on the basis of elemental analysis and spectral data. All the synthesized compounds have been evaluated for their antibacterial and antifungal activities. Some of the synthesized compounds 2a-g and <b style="mso-bidi-font-weight: normal">3a-g exhibit significant antibacterial activity against Escherichia coli and Pseudomonas aeruginosa. The compounds 2a-g and <b style="mso-bidi-font-weight: normal">3a-g exhibit good antifungal activity against <i style="mso-bidi-font-style: normal">Candida albicans, Aspergillus flavus. Pyrazolo[3,4-a]carbazoles 4a-g register good antibacterial activity against Escherichia coli and Pseudomonas aeruginosa. The compound 4e indicate maximum activity of 20 and 24 mm at 500 and 1000µg/disc, respectively, against <i style="mso-bidi-font-style: normal">Lipomyces<span style="font-size:8.5pt; mso-bidi-font-weight:bold" lang="EN-GB"> lopofera fungi

Effect of reaction time on the synthesis and electrochemical properties of Mn3O4 nanoparticles by microwave assisted reflux method

Spherical Mn3O4 nanoparticles were synthesized by microwave assisted reflux method at different reaction times (1, 5, 10, 15, and 20 min). The single phase formation of Mn3O4 nanoparticles was identified through XRD analysis. The FT-IR and Raman spectra revealed the presence of functional groups of Mn3O4 and further support the XRD results. The spherical morphology of Mn3O4 was identified via SEM analysis. The cyclic voltammetry analysis implies that 15 min synthesized Mn3O4 (MN-15) shows the higher specific capacitance of 135 F g−1 among all the prepared Mn3O4 electrodes. The EIS spectra of MN-15 substantiate the less charge-transfer resistance (Rct) of 0.553 �, when compared with the other samples. The discharge capacitance of MN-15 was 103 F g−1 at 0.5 mA cm−2 in 1 M NaNO3 solution. The cycling stability curve over 100 cycles implies that the discharge capacitance is increased from 47 to 68 F g−1 at 5 mA cm−2. This capacitance enhancement during cycling is due to the influence of phase or morphological variation of Mn3O4 electrode

A Model Estimating the Goodness of Fit in an Organization through Three Parameter Generalized Rayleigh Distribution

Various researchers have been studied the use of Stochastic modeling in an organization with different grades of employee.This study intended to estimate the goodness of fit of three parameter generalized Rayleigh distribution in different grades of an organization. It focused on the employee stay each grade and expected time of an employee to leave the organization. The parameter values of this distribution have been estimated from the simulation work. This study concluded that the higher the grade, the length of stay by the employee increases.</jats:p