A stability-indicating HPLC method to determine cyproterone acetate in tablet formulations

A simple and accurate liquid chromatographic method was developed to estimate cyproterone acetate (CA) in pharmaceuticals. The drug was chromatographed on a reversed-phase C18 column. Eluents were monitored at a wavelength of 254 nm utilizing a mixture (60:40) of acetonitrile and water. Solution concentrations were measured on a weight basis to avoid the use of an internal standard. The method was statistically validated for linearity, accuracy, precision, and selectivity. Due to its simplicity and accuracy, we believe that the method can be used for routine quality control analysis. No specific sample preparation is required except for the use of a column guard and a suitable prefilter attached to the syringe.     

Structure functional expression and spatial distribution of a cloned cDNA encoding a rat 5-HT1D-like receptor

Using polymerase chain reaction (PCR) a complementary DNA (cDNA) encoding a 5-hydroxytryptamine (5-HT) receptor was isolated from rat forebrain. The amplified cDNA specifies an open reading frame of 374 amino acids comprising seven putative transmembrane regions. Expression of the cloned cDNA in human embryonic kidney cells (HEK 293) was used to establish the pharmacological profile of the encoded receptor polypeptide. Membranes containing the cloned receptor showed high affinity binding of [3H]-5-HT. Competition binding experiments with a variety of serotonin receptor ligands displayed a rank order of affinities corresponding to a 5-HT1D subtype: 5-CT > 5-HT = metergoline > CGS 12066 > methysergide > sumatriptan > mianserin = (-)alpha-Me-5-HT = yohimbine > 8-OH-DPAT > or = rauwolscine > spiperone > DOI > propranolol > or = 2-Me-5-HT > or = ICS 205930. Ketanserin and ritanserin displaced [3H]-5-HT-binding in a biphasic manner. In situ hybridization revealed highest expression of the corresponding mRNA in the pyramidal layer of the olfactory tubercle and the nucleus caudatus and accumbens.     

Endothelin ET(B) receptors counteract venoconstrictor effects of endothelin-1 in anesthetized rats

The inhibitory effects of BQ 788 (3 mg/kg, i.v., ET(B)-receptor antagonist) on endothelin-1 (ET-1)- or IRL 1620 (ET(B)-receptor agonist)-induced changes in mean arterial pressure (MAP), mean circulatory filling pressure (MCFP, driving force of venous return), arterial resistance (RA), venous resistance (RV) and cardiac output (CO) were characterized in 6 groups of pentobarbital-anesthetized rats. ET-1 or IRL 1620 (0.5, 1 and 2 nmol/kg, i.v.) dose-dependently increased MAP, RA, RV and MCFP and decreased CO. Maximum changes in RA, RV and CO elicited by ET-1 were greater than those by IRL 1620. Equimolar doses of ET-1 and IRL 1620 also caused similar initial transient decreases in MAP. BQ 788 alone slightly elevated MCFP, but did not alter other variables. The ET(B)-blocker abolished all changes elicited by IRL 1620, but only partially inhibited its responses on MCFP, showing the presence of BQ 788-insensitive receptors. BQ 788 also abolished ET-1's depressor response, partially inhibited its effect on MCFP, and markedly augmented its effects on RA, RV and CO. Thus, ET(B)-receptors counteract the sustained constrictor effects of ET-1 on arterial and venous resistance vessels Our results indicate a substantial arterial and venous dilator role for ET(B) receptors.     

Histopathology of coronary lesions with early loss of minimal luminal diameter after successful percutaneous transluminal coronary angioplasty: is thrombus a significant contributor?

BACKGROUND: Early loss of minimal luminal diameter of >0.3 mm after successful percutaneous transluminal coronary angioplasty (PTCA) is associated with a higher incidence of restenosis. The underlying mechanism of this early loss is unknown and thrombus may be a contributing factor. METHODS: We performed a prospective study using quantitative computerized planimetry on coronary tissue specimens obtained by directional coronary atherectomy of 24 lesions in which early loss occurred 22+/-9 minutes after successful PTCA. RESULTS: Thrombus was present in 9 (37%) of 24 coronary specimens. Segmental areas (mm2) and percentage of total area were distributed as follows: sclerotic tissue, 4.07+/-0.7 mm2 (63%+/-6%); fibrocellular tissue, 0.97+/-0.27 mm2 (16%+/-4%); hypercellular tissue, 0.99+/-0.29 mm2 (12%+/-3%); atheromatous gruel, 0.18+/-0.07 mm2 (3%+/-0.1%); and thrombus, 0.24+/-0.15 mm2 (6%+/-0.4%). There was no difference in the relative early loss index between lesions with or without thrombus (35%+/-7% vs 26%+/-2%, respectively; P= .87). Multiple stepwise regression analysis did not identify any histologic predictors of relative early loss index. CONCLUSION: Histopathologic analysis of coronary lesions with early loss after successful PTCA suggests that thrombus may not play a significant role in this angiographic phenomenon.     

Albumin-containing sol–gel glasses: Chemical and biological study

Glasses incorporating increasing amounts of bovine serum albumin were prepared by sol-gel techniques from a tetra methoxy silane precursor. The surface of the glass samples was studied by X-ray photoelectron spectroscopy, revealing that the protein is present also in the superficial layer of the silica network. Moreover, the protein is distributed in a dose-dependent way, since the N/Si atomic ratio increases linearly with the albumin concentration in the reaction mixture. Angle-dependent measurements show that the protein distribution occurs homogeneously and is the same at different sampling depths. Protein incorporation in the bulk SiO2 network, with a uniform protein distribution between bulk and surface, is confirmed by infrared spectroscopy measurements, performed both in reflectance and transmittance mode. The reaction with a specific antibody and the adhesivity assay of osteoblastic cells show that embedded albumin present on the glass surface is able to interact with other proteins.     

Robust trend parameters in a multivariate spatial linear model

This article gives a robust estimator of the trend parameters in multivariate spatial linear models. This estimator is presented as an alternative to the classical one which is obtained by using cokriging. The goal focuses on improving predictions of spatial variables when data contain both atypical and high influence observations. The procedure consists of extending robust methods used in linear regression models to the multivariate spatial context. The resulting estimator belongs to the class of GM-estimators and then, it is a bounded influence estimator and it has good robust properties, in particular, a high breakdown point and a high efficiency. An illustrative example is given to show how the proposed estimator works. Research partially supported by Ministerio de Ciencia y Tecnología, Project AGL2000-0978.     

Evaluation of the effect of a maternal rearing system on the odour profile of meat from suckling lamb

The aim was to evaluate the effect of maternal rearing system on the chemical composition and odour profile of meat from suckling lamb. Twenty-four single male suckling lambs raised exclusively on maternal milk came from two rearing systems (extensive and intensive), and from Castellana and Churra breeds. The fatty acid composition of lamb meat from both breeds was affected by the rearing system, and Churra lamb reared under the extensive system had noticeable changes in odour attributes as detected by panellists and an electronic nose. Using partial least squares-discriminant analysis, the electronic nose was able to discriminate accurately between samples of Churra and Castellana meat according to their production system. However, it was not able to correctly classify meat samples from the extensive and intensive systems when both breeds were analysed together. The results suggest a significant effect of the rearing system and breed on suckling lamb meat quality traits.