盐酸多塞平乳膏与盐酸赛庚啶乳膏对照治疗慢性神经性皮炎75例

目的:评价盐酸多塞平乳膏治疗慢性神经性皮炎的疗效.方法:75例慢性神经性皮炎患者,随机分为治疗组(n=30,用盐酸多塞平乳膏)、阴性对照组(n=30,用凡士林、甘油等制备的基质乳膏)和阳性对照组(n=15,用盐酸赛庚啶乳膏),局部外用,tid,每次使用面积不超过全身的8%,8d为1个疗程.结果:治疗组治疗后瘙痒和皮疹面积总平均下降分多于阳性对照组及阴性对照组,统计学处理差异均有显著性.盐酸多塞平乳膏止痒作用突出,而皮损消退作用则相对缓慢,不良反应小.结论:盐酸多塞平乳膏治疗慢性神经性皮炎安全有效.     

盐酸尼卡地平凝胶家兔在体透皮吸收研究

进行了盐酸尼卡地平凝胶的家兔在体透皮吸收研究，评价月桂氮Chuo酮对其透皮吸收的促进作用。通过测定家兔皮肤给药后不同时间的血药浓度值，得到了血药－时间曲线，经拟合获得了透皮吸收的主要药动学参数，结果表明加入月桂氮Chuo酮后尼卡地平的峰浓（Cmax)，血药浓度曲线下面积（AUC0－24h)和平均滞留时间（MRT）三个参数均显著增加（P＜0．0001），而达峰时间（Tmax)和时滞（Tlag)两个参数无显著性改变（P＞0．05）。     

三黄片中盐酸小檗碱的HPLC测定

建立了测定三黄片中盐酸小檗碱的HPLC方法，对11个厂家26个批号产品的含量测定结果为0.92mg-4.06mg/片，差别很大，为全面控制三黄片质量，应在标准中增加盐酸小檗碱含量指标。HPLC法测定三黄片中盐酸小檗碱，前处理简单方便，测定快速准确，适用于生产质量控制和药品检验。     

盐酸去甲万古霉素纯度控制方法的改进

目的：改进盐酸去甲万古霉素质量控制的方法。方法：在中国药典与美国药典方法的基础上，优化了两种不同的流动相系统(三乙胺-乙腈-四氢呋喃系统和磷酸氢二铵-甲醇系统)，用梯度洗脱对盐酸去甲万古霉素及其有关物质进行分离。结果：与中国药典方法相比，分离效果显著提高，两种方法在2．5～40μg范围内，峰面积与进样量线性关系良好，检测限10ng。结论：改进后的RP-HPLC方法能更加真实的反映去甲万古霉素及其有关物质的含量。     

HPLC 法测定盐酸地尔硫注射液的含量

本文用ＨＰＬＣ法测定了盐酸地尔硫注射液的含量，克服了注射液中辅料的干扰。回收率为１００．２％，ＲＳＤ为０．４７％。     

The attenuating effect of carteolol hydrochloride, a β-adrenoceptor antagonist, on neuroleptic-induced catalepsy in rats

It is known that β-adrenoceptor antagonists are effective in the treatment of akathisia, one of the extrapyramidal side effects that occur during neuroleptic treatment. Neuroleptic-induced catalepsy, a model of neuroleptic-induced extrapyramidal side effects, was considered suitable as a model for predicting neuroleptic-induced akathisia in humans, although neuroleptic-induced catalepsy was not considered a specific test for neuroleptic-induced akathisia. Therefore, the effects of carteolol, a β-adrenoceptor antagonist, on haloperidol-induced catalepsy in rats were behaviorally studied and compared with those of propranolol and biperiden, a muscarinic receptor antagonist. Carteolol, as well as propranolol and biperiden, inhibited the haloperidol-induced catalepsy. The inhibitory effect of carteolol was almost comparable to that of propranolol, but was weaker than that of biperiden. Carteolol did not evoke postsynaptic dopamine receptor-stimulating behavioral signs such as stereotypy and hyperlocomotion in rats. Carteolol did not antagonize the inhibitory effects of haloperidol on apomorphine-induced stereotypy and locomotor activity in rats. In addition, carteolol did not evoke 5-HT_1A receptor-stimulating behavioral signs such as flat body posture and forepaw treading and did not inhibit 5-hydroxytryptophan-induced head twitch in rats. Finally, carteolol did not inhibit physostigmine-induced lethality in rats. These results strongly suggest that carteolol improves haloperidol-induced catalepsy via its β-adrenoceptor antagonistic activity and is expected to be effective in the treatment of akathisia without attenuating neuroleptic-induced antipsychotic effects due to its postsynaptic dopamine receptor antagonistic activity. Received: 7 March 1996/ Final version: 27 November 1996     

Serotonin 5-HT1A and 5-HT2/1C receptors in the midbrain periaqueductal gray differentially modulate defensive rage behavior elicited from the medial hypothalamus of the cat

Recent studies have established that the expression of defensive rage behavior in the cat is mediated over a descending pathway from the medial hypothalamus to the dorsolateral quadrant of the midbrain periaqueductal gray matter (PAG). The present study was designed to determine the roles played by 5-HT_1A and 5-HT_2/1C receptors in this region of PAG in modulating defensive rage behavior elicited from the cat's medial hypothalamus. Monopolar stimulating electrodes were implanted into the medial hypothalamus from which defensive rage behavior could be elicited by electrical stimulation. During the course of the study, the `hissing' component of the defensive rage response was used as a measure of defensive rage behavior. Cannula-electrodes were implanted into sites within the PAG from which defensive rage could also be elicited by electrical stimulation in order that 5-HT compounds could be microinjected into behaviorally identifiable regions of the PAG at a later time. Microinjections of the selective 5-HT_1A agonist, (+)-8-hydroxy-dipropylaminotetralin hydrobromide (8-OHDPAT) (50 pmol, 2.0 and 3.0 nmol), into the PAG suppressed the hissing response in a dose-dependent manner. Administration of the selective 5-HT_1A antagonist, 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-benzamide hydrochloride (p-MPPI) (1.5 and 3.0 nmol), blocked the suppressive effects of 8-OHDPAT upon hissing. In contrast, microinjections of the 5-HT_2/1C receptor agonist (+)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane hydrochloride ((+)-DOI hydrochloride) (0.01, 1.0 and 1.5 nmol) facilitated the occurrence of hissing elicited from the medial hypothalamus in a dose-dependent manner. Immunohistochemical analysis revealed the presence of 5-HT axons and preterminals throughout the PAG, and in particular, in its dorsolateral aspect which receives major inputs from the medial hypothalamus in association with defensive rage behavior. The overall findings of the study provide evidence that activation of 5-HT_1A and 5-HT_2/1C receptors within the midbrain PAG differentially modulate the expression of defensive rage behavior elicited from the medial hypothalamus of the cat.     

Oral vancomycin hydrochloride therapy for postoperative methicillin-cephem-resistantStaphylococcus aureus enteritis

The postoperative development of methicillincephem-resistantStaphylococcus aureus (MRSA) enteritis can be fatal unless it is detected at an early stage and treated with effective antibacterial agents. We report herein a Japanese multicenter collaborative clinical study on the efficacy and safety of oral vancomycin hydrochloride (VCM) in the treatment of MRSA enteritis. A total of 49 patients who had been diagnosed as having, or were strongly suspected of having, MRSA enteritis during the early postoperative period, were given oral VCM as four standard doses of 0.5g per day. The VCM concentrations in the blood, urine, and feces were then measured. No side effects were observed and the clinical efficacy of oral VCM in the 31 evaluable patients was excellent. There was a 100% clinical response rate and a 95.8% bacterial elimination rate in the feces. The clinical complete response (CR) rate to oral VCM differed significantly between patients in whom MRSA was detected only in the feces (100%) and those in whom MRSA was isolated from an additional source (57%) (P<0.01). Although VCM concentrations in the stools were extremely high, the levels in the blood and urine were very low. These results demonstrate that oral VCM should be the treatment of choice for postoperative MRSA enteritis due to its safety and efficacy.