Application of nonlinear fitting and selection of the most fitted equation by AIC in stability test of pharmaceutical ingredients

We proposed a method for objectively selecting the most fitted rate equation among candidate rate equations based on chemical kinetics by both nonlinear regression analysis and Akaike's information criterion (AIC), to express the decrease of pharmaceutical ingredient as an appropriate equation. Pseudo-zero, first, and second-order rate equations were prepared as candidates beforehand, and AIC was introduced for selecting the most fitted rate equation among the candidates. We compared the proposed method to the Weibull method that expressed any decrease patterns as a single equation.

We quantified the contents of thiamine nitrate (VB1) and taurine after storage for one, three, and six months under 40°C-75% relative humidity by high-pressure liquid chromatography. Decrease patterns of each sample were most fitted to one of the candidate rate equations, that is, pseudo-zero, first, and second-order rate equations, respectively, and the degree of fit in the most fitted equation was superior to that of the Weibull method, except for the pseudo-first-order rate equation.

Moreover, we confirmed that the proposed method was considerably precise for estimating the stability of pharmaceuticals by comparing estimated residual rates and confidence intervals to experimental data.     

The metabolism and distribution of docosapentaenoic acid (n−6) in rats and rat hepatocytes

In this study, a new marine oil that contains 45% docosahexaenoic acid (DHA, 22∶6n−3) and 13% docosapentaenoic acid (DPA, 22∶5n−6) was administered to rats. The metabolism and distribution of DPA in rats was investigated. In experiment 1, the effects of DHA and n−6 fatty acids (linoleic acid, I A; arachidonic acid, AA; and DPA) on AA contents were investigated in vivo. LA group: LA 25%, DHA 30%; LA-DPA group: LA 15%, DPA 10%, DHA 35%; LA-AA-DPA group: LA 10%, AA 5%, DPA 10%, DHA 35% were administered to rats for 4 wk. In the liver, the AA content in the LA-DPA and LA-AA-DPA groups was significantly higher than in the LA group. The decreased AA contents in the LA group might be caused by DHA administration. Although DHA also was administered in the LA-DPA and LA-AA-DPA groups, the AA contents in these two groups did not decrease. These results suggested that DPA retroconverted to AA, blunting the decrease in AA content caused by DHA administration. To conduct a detailed investigation on DPA metabolism and its relation with AA and DHA, rat hepatocytes were cultured with pruified DPA and DHA for 24 h. We discovered the retroconversion of DPA to AA occurred only when AA content was decreased by a high DHA administration; it did not occur when AA content was maintained at a normal level.     

Long-term cure of a malignant lymphoma of the pleural cavity treated by irradiation

Malignant lymphomas arise in the pleura in association with a long-standing chronic tuberculous pyothorax. We report a case of a non-Hodgkin's lymphoma of the pleural cavity, inoperable because of local invasion into thoracic wall, who has survived more than 6 years without recurrence. This patient represents the longest reported survival after radiation therapy alone. Radiotherapy holds an important role in the treatment of locally advanced lymphoma of the pleural cavity.     

Responses of maxillary sensilla styloconica inBombyx mori to glucosides fromOsmunda japonica,a nonhost plant

We isolated glucosides from the royal fern,Osmunda japonica, which elicit a deterrent response in larvae ofBombyx mori. These compounds were absent in taro (Colocasia antiquorum) and castor-oil plant (Ricinus communis) leaves and did not evoke responses of sensory cells in the lateral and medial sensilla styloconica ofSpodoptera litura. This glucoside extract of the royal fern leaves stimulates receptors generally associated with deterrent. It is also possible that this compound may act as a behavioral deterrent, and from actual feeding tests, it is suggested that this compound may prevent feeding in some monophagous insects, such asBombyx mori. The deterrent glucoside possesses a noncyclic aglycon.     

New modifications of poly(vinyl alcohol)s and their applications

Poly(vinyl alcohol) (PV-OH), prepared from poly(viny) acetate), is used widely in many industries. Various grades have been produced, with different degree of polymerization and degree of hydrolysis. Recently, novel modified (PV-OH)s with anion, cation, silanol or hydrophobic groups have been studied and developed. They have new properties in addition to those of ordinary PV-OH and have new applications. The methods of modification and the characteristics and some applications of the modified polymers are described.     

Expression, structure and chromosomal localization of the human cGMP-binding cGMP-specific phosphodiesterase PDE5A gene

1. Nicotinylalanine, an inhibitor of kynurenine metabolism, has been shown to elevate brain levels of endogenous kynurenic acid, an excitatory amino acid receptor antagonist. This study examined the potential of nicotinylalanine to influence excitotoxic damage to striatal NADPH diaphorase (NADPH-d) and gamma-aminobutyric acid (GABA)ergic neurones that are selectively lost in Huntington's disease. 2. A unilateral injection of the N-methyl-D-aspartate (NMDA) receptor agonist, quinolinic acid, into the rat striatum produced an 88% depletion of NADPH-d neurones. Intrastriatal infusion of quinolinic acid also produced a dose-dependent reduction in striatal GABA content. 3. Nicotinylalanine (2.3, 3.2, 4.6, 6.4 nmol 5 microl(-1), i.c.v.) administered with L-kynurenine (450 mg kg(-1)), a precursor of kynurenic acid, and probenecid (200 mg kg(-1)), an inhibitor of organic acid transport, 3 h before the injection of quinolinic acid (15 nmol) produced a dose-related attenuation of the quinolinic acid-induced loss of NADPH-d neurones. Nicotinylalanine (5.6 nmol 5 microl(-1)) in combination with L-kynurenine and probenecid also attenuated quinolinic acid-induced reductions in striatal GABA content. 4. Nicotinylalanine (4.6 nmol, i.c.v.), L-kynurenine alone or L-kynurenine administered with probenecid did not attenuate quinolinic acid-induced depletion of striatal NADPH-d neurones. However, combined administration of kynurenine and probenecid did prevent quinolinic acid-induced reductions in ipsilateral striatal GABA content. 5. Injection of nicotinylalanine, at doses (4.6 nmol and 5.6 nmol i.c.v.) which attenuated quinolinic acid-induced striatal neurotoxicity, when combined with L-kynurenine and probenecid produced increases in both whole brain and striatal kynurenic acid levels. Administration of L-kynurenine and probenecid without nicotinylalanine also elevated kynurenic acid, but to a lesser extent. 6. The results of this study demonstrate that nicotinylalanine has the potential to attenuate quinolinic acid-induced striatal neurotoxicity. It is suggested that nicotinylalanine exerts its effect by increasing levels of endogenous kynurenic acid in the brain. The results of this study suggest that agents which influence levels of endogenous excitatory amino acid antagonists such as kynurenic acid may be useful in preventing excitotoxic damage to neurones in the CNS.     

A cause of the motion of arcs in the presence of a magnetic field

A cause of the retrograde motion of arcs in the magnetic field is explained by the gyromotion of ions which are produced in the arc column. It is shown that the mechanism is consistent with fundamental aspects of the retrograde motion.     

Finite-time settling adaptive observer for linear discrete-time systems

This paper deals with a design method for an adaptive scheme which would identify the parameters and observe the state of any unknown single-input single-output linear discrete-time systems using only input-output data. Kreisselmeier's parametrized system [5] is used instead of the original system. Then the parameter identification process and the state observation process are well separated. To accelerate the convergence rate of the estimates, a finite-time settling scheme is proposed. It is shown that the estimates obtained converges to true values at k = 3n ?1, where k is the discrete time and n is the order of system. A numerical example is given to indicate acceptable performance of the proposed scheme.     

Input/output facilities in LISP 1.9

LISP1.9 provides new input/output facilities, the conceptual channel and the current channel, which make program writing easier and execution faster. The channel attributes-column-setting, line number option, prompt-string, user-buffer, eol-handler, eof-handler and access rights-are useful for program writing; the channel interaction attributes-input-memo, output-memo and file I/O verification-are useful for system development. Random file I/O, array I/O, record handling, array-string conversion and Japanese character output are also provided.