HPLC法同时测定复方锌布颗粒中马来酸氯苯那敏和布洛芬的含量

目的建立同时测定复方锌布颗粒中马来酸氯苯那敏和布洛芬的含量的方法。方法采用Alltech C18(250 mm×4.6 mm,5μm)色谱柱,以乙腈-醋酸钠缓冲液(醋酸钠6.13 g,加水750 ml使溶解,用冰醋酸调节pH至4.0)-异丙醇(50∶45∶5)为流动相,流速1.0 ml.min-1,检测波长263 nm。结果马来酸氯苯那敏、布洛芬线性范围分别为31.65~84.4、2254.65~6012.4μg.ml-1,平均回收率分别为99.42%和99.06%。结论本方法可快速准确地检测复方锌布颗粒中的马来酸氯苯那敏和布洛芬。     

HPLC法测定复方敏立通片中各组分的含量

采用反相ＨＰＬＣ法，以醋酸氟氢松为内标，在氰基柱上以水—甲醇—乙腈—三乙胺（８０∶２０∶２０∶１．４，用磷酸调整ｐＨ为７．５）为流动相，检测波长为２５４ｎｍ，同时测定复方敏立通片中马来酸氯苯那敏和倍他米松的含量．方法简便，快速准确，各组分与内标有良好线性关系和分离度．平均回收率马来酸氯苯那敏为９９．２％（ＲＳＤ＝０．７％），倍他米松为１００．９％（ＲＳＤ＝０．６％），ｎ＝７．     

A comparative study on the effects of alpha-hexachlorocyclohexane and its metabolite beta-pentachlorocyclohexene on growth and monooxygenase activities in rat liver

The present study adds support to the hypothesis that β-pentachlorocyclohexene (β-PCH) is a primary intermediate in α-hexachlorocyclohexane (α-HCH)4 metabolism in the rat. Degradation of α-HCH to β-PCH was shown to occur in vitro and in vivo, partially by non-enzymic catalysis. β-PCH accumulated in liver and adipose tissue of α-HCH treated rats, which had received the glutathione-lowering agent diethyl maleate. β-PCH disappears from the body much more rapidly than the parent compound α-HCH: about 50 per cent of a single i.p. dose were degraded within 2.5 hr, while half-life of α-HCH is known to be approximately 130 hr. To maintain equimolar liver concentrations, β-PCH must be given in doses 100-fold higher than α-HCH. β-PCH and α-HCH were fed for a period of ten days at various dose levels to give steady-state liver concentrations. It was found that β-PCH has similar hepatic effects to α-HCH: both agents induced liver growth and a phenobarbital-type pattern of monooxygenase activities, as measured by the following substrates: aminopyrine, ethylmorphine, benzphetamine, 4-nitroanisole, aniline, benzo[α]pyrene, ethoxyresorufin and 2,5-diphenyl-oxazole. Threshold doses for these effects were 30–43 μmoles/kg/day for β-PCH and 1.0–1.7 μmoles/kg/day for α-HCH. However, on the basis of molar hepatic concentrations β-PCH was a more potent inducer than α-HCH (2–10 times). Threshold concentrations ranged from 0.4 to 0.6 nmoles β-PCH/g liver and from 0.7 to 1.5 nmoles α-HCH/g liver. β-PCH concentrations in livers of rats treated even with high doses of α-HCH were below the threshold for induction of liver growth and of monooxygenase increases. It is, therefore, highly unlikely that β-PCH is responsible for the effect of α-HCH on rat livers.     

Morphological changes in CNS of rats treated with perhexiline maleate (Pexid)

Summary The basic cellular lesion in CNS of suckling rats treated with Pexid was studied by light and electron microscopy. The most pronounced abnormality, the formation of various intracytoplasmic inclusions, was found in neurons, astrocytes, oligodendrocytes, ependymal cells, endothelial cells and fibroblasts. These abnormal inclusions were generally membrane-bound, although clearly non-membrane-bound inclusions were occasionally found. The several internal patterns of the inclusions were (1) lamellar, both concentric and parallel, (2) reticular and (3) crystalloid. These alterations were completely resersed following withdrawal of the drug.The structural characteristics of the abnormal inclusions in Pexid-treated animals were similar to those found with certain hypocholesterolemic, neuroleptic, anorectic, and antimalarial drugs. This suggests that the inclusions occurring within the cells of animals treated with any of these drugs may develop in a similar manner, and that the formation of such inclusions is likely to be a form of cellular reaction common to certain metabolic disturbances.     

The role of histamine in estradiol-induced conditioned consumption reductions

Conditioned consumption reductions (CCRs) develop toward novel taste stimuli as a consequence of associating those tastes with certain physiological changes. Few studies have focused on the neurochemical basis of this learned behavior. The purpose of these experiments was to reexamine the role of histamine in CCRs elicited by estradiol. Previous studies have suggested that histamine mediates CCRs induced by radiation, centrifugal rotation, and estradiol. However, because the animals were trained in a drug state, but tested in a nondrug state, it is possible that state-dependent learning confounded the results of these studies. The following series of experiments was performed to test this possibility for estradiol-induced CCRs. Implementing our own methodologies in Experiment 1, we demonstrated that an estradiol-induced CCR was blocked by treatment with the histamine 1 receptor blocker, chlorpheniramine maleate, before sucrose consumption during acquisition. In Experiment 2, identical states were maintained during acquisition and extinction by administering chlorpheniramine prior to sucrose exposure during both phases. The results indicated that chlorpheniramine blocked the estradiol-induced CCR. However, circumventing state-dependency in Experiment 3 by administering chlorpheniramine following exposure to sucrose during acquisition augmented the estradiol CCR. Taken together, the results of these experiments suggest that the ability of chlorpheniramine to abolish estradiol-induced CCRs is not due to state-dependency or to the antihistaminergic properties of chlorpheniramine. It is proposed that the results of all of the experiments can be accounted for by the aversive properties of chlorpheniramine.     

Efficacy and pharmacokinetics of fluvoxamine maleate in patients with mild depression undergoing hemodialysis

Seven Japanese patients on maintenance hemodialysis who were comorbid with mild depression were medicated with 50 mg/day fluvoxamine maleate for 28 days. Effectiveness was obtained in four out of seven patients (57%). The plasma fluvoxamine concentrations were examined in three patients. The plasma fuvoxamine concentration decreased by 22% by hemodialysis. There is a tendency for the dialyzed rate of fluvoxamine to become lower if the plasma albumin concentration is higher. The half-life of fluvoxamine was possibly shortened more in the patient with hypoalbuminaemia. The plasma fluvoxamine concentration reached a steady state 8 days after the start of medication and thereafter. The time required to reach steady state was lengthened when compared with the results in normal Japanese volunteers.     

In vitro release studies of chlorpheniramine maleate from gels prepared by different cellulose derivatives

The objective of this study was to evaluate the in vitro and ex vivo percutaneous absorption of chlorpheniramine maleate (CPM) from different hydrogel formulations. Various concentrations of polymers, including hydroxypropylmethylcellulose (HPMC), sodium carboxymethylcellulose (NaCMC) and methyl cellulose (MC) were used in the hydrogel formulations. All experiments were conducted using cellulose dialysis membrane. The passive permeation of CPM was affected by the polymer concentrations. The effect of each polymer on the release rate of CPM was found to be statistically different (P<0.05). The formulation which exhibited maximum drug release through cellulose membrane was then used with other membranes namely polyurethane membrane, rat skin and human skin. The release rate of CPM from different membranes was found to be statistically different (P<0.05). Within the different diffusional barriers rat skin was found to be best alternative to human skin. It seems suitable the use of cellulose derivatives for topical application of CPM to obtain high therapeutic concentration at the application site. The synthetic membranes can be used to assess product performance in quality assurance but give little indication of its performance ex vivo.     

美敏伪麻口服溶液含量测定方法的改进

目的改进关敏伪麻口服溶液含量测定的方法。方法色谱柱为苯基键舍硅胶色谱柱，流动相为水-乙腈-磷酸（60：40：0．1，每1000mL中含4．0g十二烷基硫酸钠），流速为1．0mL／min，检测波长为264nm。结果盐酸麻黄碱、氢溴酸右美沙芬、马来酸氯苯那敏质量浓度分别在10．01—2001．6μg／mL，3．33～665．6μg／mL，0．75—149．2μg／mL范围内与相应峰面积呈良好的线性关系，平均回收率分别为100．59％（RSD=0．32％），100．82％（RSD：0.85％），99．13％（RSD=0．53％）。结论所用方法精密度高、结果准确，能在同一液相系统下对美敏伪麻口服溶液中3种成分进行含量及有关物质的测定。     

马来酸依那普利及其片剂的稳定性研究

稳定性研究结果表明,马来酸依那普利及其片剂须在避光、密封条件下保存,在此条件下贮存期可达3年以上。