Targeting of mitomycin C to the liver by the use of asialofetuin as a carrier.

Desialylated fetuin (asialofetuin) was adopted as a carrier for introducing drugs in parenchymal liver cells. Mitomycin C, as a model guest-compound, was covalently attached to asialofetuin through a spacer of the succinyl group. The asialofetuin-mitomycin C conjugate contained 4.4 w/w% of mitomycin C and liberated it gradually at physiological conditions (t1/2 = 37 h). The survival time of the conjugate in rat blood circulation was significantly smaller than that of the non-desialylated fetuin conjugate; the elimination half-life was 7.3 min after intravenous injection. At 30 min after injection of the conjugate in rats, 40% of the dose was present in the liver. Parenchymal cells in the liver selectively took up the conjugate, which was highly distributed to the lysosomal fraction in the cell. The greater uptake of the conjugate by hepatocytes reflected the increased excretion in the bile; totally 10.4% of the dose was recovered.     

Screening of psychotropic drugs in human hair based on high-performance thin-layer chromatography and microliquid extraction

The monitoring of the physiological and functional state of personnel from dangerous industries is very important for the ensuring of ecological security. Usually, this involves testing for the consumption of alcohol and drugs of abuse. During the last several years the use of legal psychotropic drugs has increased and the control over these drugs has became an actual problem. As is well known, the long-term history of drugs present in the body is accessible through hair analysis. This is why the aim of our research is to create a screening procedure based on coupling high-performance thin-layer chromatography with microliquid extraction as a psychotropic drug testing method for hair. Some widely distributed antidepressants, neuroleptics, and sedative drugs are chosen for research. The optimal experimental conditions for all of the consequent steps for the screening detection of the model samples are determined. The visual and densitometric detection limits allow for the employment of the proposed technique for a fast and cost-effective analysis of the drugs of abuse.     

Sandwich structures at oil-water interfaces under alkaline conditions

Equilibrium liquid crystal (LC) layer on an interface between crude oils and water was observed at high pH. This layer is composed mainly of sodium naphthenates produced in situ at the water/oil interface. Transient LC layer was also evolved at the interface of aqueous phase of sodium hydroxide solutions and oleic phase of naphthenic acid (NA) solutions as result of a chemical reaction between NaOH and NA. This chemical reaction causes transport process resulting in a disturbance of the interface. Optical observation of this interface disturbance reviled that the interface covered with LC shows considerably lower flexibility as compared to LC free interface. The LC layer eventually dissolves in the water phase at low oil-to-water ratio, while at high oil-to-water ratio it can form an equilibrium phase, which spreads spontaneously at the oil-water interface.     

Determination of carvedilol in human cardiac tissue by high-performance liquid chromatography

A new high-performance liquid chromatographic method has been developed for the determination of the beta-receptor blocker carvedilol in human cardiac tissue. After homogenizing tissue samples in a microdismembrator, carvedilol and the internal standard naftopidil are extracted with acetone. The extract is evaporated to dryness and reconstituted in a potassium acetate buffer of pH 3.5. Samples are cleaned up with solid-phase extraction columns. Carvedilol and the internal standard show recoveries of 69.8 +/- 12.2% and 63.9 +/- 9.34%, respectively. The linearity range for carvedilol is 0.01-0.35 ng/mg (parts per billion) tissue (wet weight), and the limit of quantitation is 0.01 ng/mg. The percentage coefficient of variation of the intra-assay varies between 1.45 and 5.38% and the interassay between 4.25 and 6.96%. To use as an application of the assay, the cardiac carvedilol tissue level in a patient on oral carvedilol therapy for congestive heart failure is reported.     

Formation of furan derivatives in the course of the Stevens rearrangement of ammonium salts containing 4-allyloxy(phenoxy)-2-butynyl group

Ammonium salts containing phenacyl group in combination with 4-allyloxy(phehoxy)-2-butynyl group, when treated with a suspension of potassium hydroxide in benzene, undergo the 3,2-Stevens rearrangement with the formation of allenic amino ketones which under the reaction conditions give the furan derivatives.     

Parameter-free structure-property correlation via progressive reaction posets for substituted benzenes

Progressive reaction networks as frequently arise in chemistry are naturally identifiable as "partially ordered sets" (or posets). Here the direction of the reaction identifies the partial ordering of the set of molecular species. The possibility that different properties are similarly ordered is a further natural consideration and is here investigated for a suite of over 30 properties for (methyl and chloro) substituted benzenes. Such a posetic correlation is favorably demonstrated for these substituted benzenes, and it is illustrated how suitable properties may be simply predicted in an interpolative parameter-free (albeit not model-free) fashion through the use of the reaction poset. Some numerical model-quality indicators are identified, and the simple approach is deemed quite reasonable.     

HPLC Determination of some antibilharzial antimonials by extraction of antimony

The antimonial drug (antimony potassium tartrate, antimony piperazine tartrate or antimony lithium thiomaleate) in aqueous solution or biological fluid is treated with sodium diethyldithiocarbamate in the presence of a suitable masking reagent, the pH is adjusted to 9 +/- 0.5. and the antimony complex extracted with n-hexane and determined by reversed-phase HPLC with an ODS column and detection at 254 nm. The limits of detection are 20 ng (for antimony potassium tartrate and antimony lithium thiomaleate) and 16 ng (for antimony piperazine tartrate).     

Doppler-free laserspectroscopic investigations of hyperfine structure in the atomic cobalt spectrum

Performing Doppler-free laserspectroscopic investigations in the red wavelength region (640–670 nm) we were able to determine 10A-factors and 9B-factors of atomic cobalt levels. Now precise values of 18A-factors and 16B-factors of levels belonging to the configurations (3d+4s)⁹ are known. Fitting of the one-electron radial parameters to introduce agreement between experimental and theoretical hfs constants allows the prediction of hfs constants of not yet investigated fine structure levels. Values of the electric quadrupole moment of the Co⁵⁹ nucleus are determined in two electron configurations. The resulting mean value of the spectroscopic quadrupole moment isQ=0.35(3) barn.     

Spectrophotometric determination of acrivastine in urine and capsules

Three sensitive and accurate spectrophotometric methods are presented for the determination of the antihistaminic acrivastine (ACR) in capsules and urine. The first method utilizes the reaction of 2-nitrophenylhydrazine hydrochloride in presence of dicyclohexylcarbodiimide and pyridine. The violet colour of the resulting acid hydrazide is measured at 550 nm. The second method is based on alkaline oxidation of the drug with potassium permanganate and subsequent measurement of the formed manganate ion at 608 nm. The third method uses derivative spectrophotometry for the determination of ACR. The last method is extended to the in vitro determination of the drug in urine. All methods gave a relative standard deviation of less than 2%.     

Polymethine dyes — Indolo[3,2-d]thiazole derivatives

New polymethine dyes with an indolo[3,2-d]thiazole residue are described, and their spectral properties are discussed. Replacement of the vinylene group in the naphtho[1,2-d]thiazole residue by an NH group leads to a considerably greater bathochromic shift of the absorption maximum of carbo- and merocyanines as compared with replacement by a sulfur atom. The basicity of the indolo[3,2-d]thiazole residue is higher than the basicity of the naphtho[1,2-d]-thiazole and thionaphtheno[3,2-d]thiazole residues.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1606–1610, December, 1972.