Dissolution and Absorption of Nipedipine from Nifedipine-Polyvinylpyrrolidone Coprecipitate

Attempt was made to develop the solid dosage form of nifedipina which showed good absorption rate and total bioavailability. Nifedipine is a poorly water-saluble drug, whom bioavailability is low when administered orally in the crystalline form. Solutions of nifedipine were well absorbed from the gastrointestinal tract. The dissolution rate of PVP-nifedipine coprecipitates exhibited rapid dissolution rate. X-ray diffraction data suggested the lack of crystallinity in the coprecipitate. The relation between the dissolution rates and average molecular weights of PVP was studied. Nifedipine in the copretipitate was chemically stable to heat and humidity, but the dissolution rate of nifedipine from the coprecipitate stored at 21° and 75% R.H. markedly decreased. X-ray diffraction data revealed that it might be due to the transformation of amorphous form of nifedipine to crystalline form under higher relative humidity. The gastrointestinal absorption of nifedipine in beagle dogs after oral administration of the coprecipitate was increased than that after oral adniniatration of the physical mixture.     

Insulation characteristics of perfluorocarbon liquid/solid insulation for nonflammable large power transformer

A new type nonflammable large power transformer system is proposed in which the excellent cooling characteristics and insulation properties of nonflammable perfluorocarbon (PFC) liquid is utilized. In the system, transformer windings are put in an insulating cylinder filled with PFC liquid. The core includes cooling panel through the liquid. The space between the insulating cylinder and tank is filled with compressed SF⁶ gas. This paper describes the insulation characteristics of main insulation and inter-winding insulation models which simulate the transformer. It is found that (1) higher withstand voltage is expected by means of insulation barriers in the main insulation model; (2) partial discharge in inter-winding insulation model is beginning to behave in a constant electric field strength on the point of 0.1 mm liquid gap length.     

Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells

Three subtypes of human (h) arginine vasopressin (AVP) receptors, hV1A, hV1B and hV2, were stably expressed in Chinese hamster ovary (CHO) cells and characterized by [3H]-AVP binding studies. In addition, the coupling of the expressed receptor protein to a variety of signal transduction pathways was investigated. Scatchard analysis of saturation isotherms for the specific binding of [3H]-AVP to membranes, prepared from CHO cells transfected with hV1A, hV1B and hV2 receptors, yielded an apparent equilibrium dissociation constant (Kd) of 0.39, 0.25 and 1.21 nM and a maximum receptor density (Bmax) of 1580 fmol mg(-1) protein, 5230 fmol mg(-1) protein and 7020 fmol mg(-1) protein, respectively. Hill coefficients did not differ significantly from unity, suggesting binding to homogenous, non-interacting receptor populations. Pharmacological characterization of the transfected human AVP receptors was undertaken by measuring the relative ability of nonpeptide AVP receptor antagonists, YM087, OPC-21268, OPC-31260, SR 49059 and SR 121463A, to inhibit binding of [3H]-AVP. At hV1A receptors, the relative order of potency was SR49059>YM087>OPC-31260>SR 121463A> >OPC-21268 and at hV2 receptors, YM087=SR 121463A>OPC-31260>SR 49059> >OPC-21268. In contrast, the relative order of potency, at hV1B receptors, was SR 49059> >SR 121463A=YM087=OPC-31260=OPC-21268. In CHO cells expressing either hV1A or hV1B receptors, AVP caused a concentration-dependent increase in intracellular Ca2+ concentration ([Ca2+]i) with an EC50 value of 1.13 nM and 0.90 nM, respectively. In contrast, stimulation of CHO cells expressing hV2 receptors resulted in an accumulation of cyclic AMP with an EC50 value of 2.22 nM. The potency order of antagonists in inhibiting AVP-induced [Ca2+]i or cyclic AMP response was similar to that observed in radioligand binding assays. In conclusion, we have characterized the pharmacology of human cloned V1A, V1B and V2 receptors and used these to determine the affinity, selectivity and potency of nonpeptide AVP receptor antagonists. Thus they may prove to be a valuable tool in further examination of the physiological and pathophysiological roles of AVP.     

Sequential methotrexate/5-fluorouracil therapy with 5'-deoxy-5-fluorouridine against advanced gastric cancer: comparison between bolus injection and drip infusion of 5-fluorouracil administration. Hirosaki Cooperative Study Group for Cancer Chemotherapy

Forty-two patients with gastric cancer were entered in this study. Forty-one of them were eligible and administered sequential methotrexate (MTX)/5-fluorouracil (5-FU) with 5'-deoxy-5-fluorouridine (5'-DFUR). 5-FU was administered intravenously by drip infusion for 2 hours in 22 cases (group A), and was infused by bolus injection in 19 cases (group B). The treatment schedules were as follows: MTX 100 mg/m2 was given intravenously (i.v.) followed by 5-FU 600 mg/m2 i.v. 2 hours later and leucovorin 15 mg/body i.v. 8 and 20 hours later. This cycle was repeated once a week. 5'-DFUR 1,200 mg/body/day was given orally on 5 consecutive days per week. Three of 20 cases (15%) in group A showed PR, while 5 of 15 cases (33%) in group B showed PR. Median survival time was 2.8 months in group A and 3.7 months in group B. There was, however, no statistical difference. Gastrointestinal toxicity was commonly observed. Leukocytopenia was more severe in group B. Alopecia was more frequently observed in group B (p < 0.025). These results suggested bolus injection of 5-FU was a promising way of administration in sequential MTX/5-FU therapy.     

Reactive ion etching of III-V compounds using C2H6/H2

Reactive ion etching of InP, GaInAs and GaAs using a mixture of ethane and hydrogen, C₂H₆/H₂, is demonstrated for the first time. It has been found that by choosing optimum etching parameters one can obtain excellent vertical sidewalls as well as very smooth surfaces, keeping the etching rate at a convenient value of 20-60 nm/min     

Effect of helix-coil transition on association behavior of both-ends hydrophobically-modified water-soluble polypeptide

Dodecyl and dodecanoyl groups (C12) are attached at the chain ends of poly[N⁵-(2-hydroxyethyl) l-glutamine] (PHEG), and association behavior of this both-ends hydrophobically modified water soluble polypeptide (C12-PHEG-C12) has been investigated by means of light scattering measurements. Water/ethylene glycol (EG) mixed solvents were used as selective solvent for PHEG block, and PHEG changed its structure from random-coil state to α-helix with increasing EG content in the mixed solvent (W_EG). When W_EG is less than 0.5, flower-like micelle with C12 associated core and PHEG corona in loop conformation was suggested to be formed. Increase of W_EG from 0.5 to 0.6 induced drastic increase of association number and size of the associate, in which many C12 associated cores may be connected by PHEG in bridge conformation. This structure change of associate is considered to be driven by the increase of helix content of PHEG with W_EG, which enhances the possibility to form bridge conformation because of its rigidity. Solution preparation method, i.e. order of addition of solvent, was found to influence the structure of associate, although its effect on the helix content of PHEG was negligible.     

High-speed digital-signal transmission experiments by optical wavelength-division multiplexing

The letter reports results obtained with laboratory transmission experiments on high-speed digital signals by optical wavelength-division multiplexing, using a newly developed optical multiplexer and demultiplexer, as well as other high-performance optical devices and fibres.     

Ductility and strain-induced transformation in a high-strength transformation-induced plasticity-aided dual-phase steel

The influence of forming temperature and strain rate on the ductility and strain-induced transformation behavior of retained austenite in a ferritic 0.4C-1.5Si-1.5Mn (wt pct) dual-phase steel containing fine retained austenite islands of about 15 vol pct has been investigated. Ex- cellent combinations of total elongations (TELs), about 48 pct, and tensile strength (TS), about 1000 MPa, were obtained at temperatures between 100 °C and 200 °C and at a strain rate of 2.8 X 10_-4/s. Under these optimum forming conditions, the flow curves were characterized by intensive serrations and increased strain-hardening rate over a large strain range. The retained austenite islands were mechanically the most stable at temperatures between 100 °C and 200 °C, and the retained austenite stability appeared to be mainly controlled by strain-induced martensite and bainite transformations (SIMT and SIBT, respectively), with deformation twinning occur- ring in the retained austenite. The enhanced TEL and forming temperature dependence of TEL were primarily connected with both the strain-induced transformation behavior and retained aus- tenite stability.