Determination of Dimenhydrinate Nasal Delivery System in the Blood by RP-LC

Dimenhydrinate (DM) is used therapeutically for the prevention of motion sickness associated with nausea and vomiting. The aim of this investigation is the development of a new, rapid, sensitive, simple and fully validated RP-LC procedure for the suitable assay of DM in pharmaceutical formulation applied in blood samples. The method was validated before the amount determination studies in order to confirm linearity, precision, accuracy, selectivity, determination and quantification limit and consistency. High determination coefficient (r ²  = 0.998) of the standard curve drawn in the linearity studies showed that the line equation can be used in the quantification of the DM. Literature was reviewed for the methods based on diphenhydramine (DIP), its metabolite dimenhydrinate, in the in vivo determination of dimenhydrinate amount. The most appropriate method to be used in LC was decided to be the method applied by benefitting from the fluorescence characteristic of DIP. Maximum excitation and emission wavelengths in the developed method were scanned using multiple wavelengths and, maximum excitation and emission wavelengths were found to be 215 and 300 nm, respectively. In the validation study used to prove validity of the method, determination coefficient of the developed standard curve was calculated as 0.998 (RSD %), and line equation was concluded to be appropriate for use in amount determination studies. BBS % (1.06, 1.84 %) values obtained as “<2 %” in the intra-day and inter-day precision studies proved the precision of the method. Selectivity study revealed that other materials used in the formulation did not exhibit absorbance in the same wavelengths. Detection and quantification limit were found as 1 and 5 ng mL^?1, respectively. The determination of DM plasma concentrations using the proposed and fully validated LC assay has allowed us to characterize DMPK in the sheep, as well as determine DM relative bioavailability.     

Synthesis,Characterization, and Biological Evaluation of Some Novel Thiosemicarbazones as Possible Antibacterial and Antioxidant Agents

Abstract

The synthesis and characterization of 18 novel thiosemicarbazones have been investigated as part of a research program on development of compounds with antibacterial and antioxidant activities. Among the tested compounds, 2-(4-hydroxybenzylidene)-N-[4-(trifluoromethoxy)phenyl]hydrazine carbothioamide (3g) and 2-(thiophen-2-ylmethylidene)-N-[4-(morpholin-4-yl)phenyl]hydrazine carbothioamide (4b) showed excellent inhibition potency at low concentration (0.5 μg/mL) against Gram-positive pathogens (Enterococcus faecalis and Staphylococcus aureus). All tested compounds were also found to possess antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation.

[Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental files: Additional text, tables, and figures.]     

Characterization and Comparative Studies on Conventional and Microwave Synthesis of Some Disulfides

Abstract

Some disulfide derivatives have been prepared by microwave assisted synthesis methodology from thiophthalimides(sulfenimides) and thiols in a modified microwave oven under reflux at 600 Watt in ethanol. Elucidation of the structures of the synthesized compounds has been performed by IR, ¹H NMR, and ¹³C NMR spectroscopic methods.

[Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental files: Additional figures]     

Annular, cosh and cos Gaussian beams in strong turbulence

For the strong atmospheric turbulence regime, the asymptotic on-axis scintillation behavior of annular, cosh and cos Gaussian beams is theoretically derived and illustrated with numerical examples. It is observed from the plots that annular Gaussian beams exhibit more scintillations than a Gaussian beam, regardless of the amplitude coefficient and source size settings. For small source sizes, cosh Gaussian beams seem to have an advantage over Gaussian beams in terms of reduced scintillation, but for large source sizes a switchover occurs where cos Gaussian beams assume the advantage. Analysis of the effect of inner scale value shows that scintillations increases for all beams as the inner scale increases.     

Propagation properties of anomalous hollow beams in a turbulent atmosphere

Propagation of circular and elliptical anomalous hollow beams in a turbulent atmosphere is investigated in detail. Based on the extended Huygens–Fresnel integral, analytical formulae for the average irradiance of circular and elliptical anomalous hollow beams propagating in a turbulent atmosphere are derived. The irradiance and spreading properties of circular and elliptical anomalous hollow beams in a turbulent atmosphere and in free space are studied numerically. It is found that circular and elliptical anomalous hollow beams at short propagation distance in turbulent atmosphere have similar propagation properties to those of free space, while at long propagation distance, circular and elliptical anomalous hollow beams eventually become circular Gaussian beams in a turbulent atmosphere, which is much different from their propagation properties in free space. The conversion from an anomalous hollow beam to a circular Gaussian beam becomes quicker and the beam spot spreads more rapidly for a larger structure constant, a shorter wavelength and a smaller waist size of the initial beam.     

Twist phase-induced reduction in scintillation of a partially coherent beam in turbulent atmosphere

The scintillation index of a Gaussian Schell-model beam with twist phase (i.e., twisted GSM beam) in weak turbulent atmosphere is formulated with the help of a tensor method. Variations of the scintillation index of a twisted GSM beam on propagation in turbulent atmosphere are studied in detail. It is interesting to find that the scintillation index of a twisted GSM beam can be smaller than that without twist phase in weak turbulent atmosphere. Thus, modulation of the twist phase of a partially coherent beam provides a new way to reduce turbulence-induced scintillation.     

Biological activities,phenolic profiles and essential oil components of Tanacetum cilicicum (BOISS.) GRIERSON

Tanacetum species are consumed as tea in Turkey. We comparatively evaluated the phytochemical potentials and antioxidant activities of the essential oil and methanolic extracts of Tanacetum cilicicum. The chemical constitutes of T. cilicicum essential oil and antioxidant activity of this species was analysed by gas chromatography–mass spectrometry (GC–MS) method. Bicyclo (3,1,1) hept-2-en-4-ol (21.92%), camphor (15.56%) and 1,8-cineole (13.45%) which are oxygenated monoterpenes were found as the major constituents. Phenolic acids and flavonoids were quantificated by HPLC–UV. Catechin was found as the main component. The essential oils and methanolic extracts were evaluated by antioxidant activities. The leaves exhibited significant metal chelation activity with a value of 20.75 ± 4.63 μg/mL.     

Optimal control of a one-dimensional storage process

We consider the discounted and ergodic optimal control problems related to a one-dimensional storage process. The existence and uniqueness of the corresponding Bellman equation and the regularity of the optimal value is established. Using the Bellman equation an optimal feedback control is constructed. Finally we show that under this optimal control the origin is reachable.This work was supported by the National Science Foundation under Grant No. MCS 8121940.     

Spectroscopic determination of acid dissociation constants of N-substituted-6-acylbenzothiazolone derivatives

The acid dissociation constants of twelve novel drug precursor N-substituted-6-acylbenzothiazolone derivatives were determined by using the UV-vis spectroscopic technique. The protonation and deprotonation behaviors of the investigated molecules were researched from the super basic to super acid regions (i.e., 8 mol·L(-1) KOH to 98% H(2)SO(4)) including the pH region. It is observed that all of the molecules are protonated in the super acidic region. The calculated relative stability values of possible tautomer structures indicate that the keto form of investigated molecules is favored over the enol form. It was predicted that protonation occurs at the amide (oxo) group found in the keto form.