波棱瓜子提取物对小鼠抗疲劳耐缺氧作用

目的 研究波棱瓜子提取物对小鼠抗疲劳、耐缺氧的作用.方法 按设定剂量(复方丹参组0.84 g/kg,波棱低、中、高剂量组分别为1、2、4 g/kg)连续灌胃给药7d后,观察小鼠疲劳游泳时间及耐缺氧存活时间,探索波棱瓜子提取物对小鼠抗疲劳耐缺氧的作用.结果 疲劳游泳实验中,复方丹参片组、波棱高、中、低剂量组疲劳游泳时间与...     

黄芩苷纳米晶体微丸的制备及其药代动力学初步研究

目的:该研究制备了黄芩苷纳米晶体(baicalin nanocrystal,BC-NC),并进行了大鼠体内药物动力学研究.方法:采用探头超声结合高压均质法制备黄芩苷纳米混悬剂,然后通过流化干燥工艺将其脱水干燥成固体微丸,考察纳米晶体的形态、粒径分布、Zeta电位.以黄芩苷为指标成分,采用HPLC测定大鼠灌胃给药后的血药浓度,用DAS 2.0药动学软件计算药代动力学参数.结果:黄芩苷纳米晶体在扫描电镜下呈不规则颗粒状,平均粒径(248±6) nm,多分散指数(PI)为(0.181±0.065),Zeta电位为(-32.3±1.8)mV.BC-NC达峰浓度(Cmax)为(16.51±1.73) mg·L-1,0～24h的药时曲线下面积(AUC)增加为(206.96±21.23) mg·L-1·h,与黄芩苷原料药及物理混合物相比均有显湿著性提高(P＜0.0l).结论:通过高压均质及流化干燥工艺制得的黄芩苷纳米晶体能显著提高药物体内生物利用度,有望进一步制成口服固体制剂.     

Herpetrione纳米混悬剂的制备及药动学初步研究

 目的 本实验制备了herpetrione纳米混悬剂(PEDX-NS),并进行了大鼠体内药动学研究。方法 采用高压均质法制备herpetrione纳米混悬剂,考察纳米混悬剂的形态及粒径分布。以herpetrione(PEDX)为指标成分,采用HPLC测定大鼠灌胃给药后的血药浓度,用DAS2.0药动学软件计算药动学参数。结果 制得的纳米混悬剂呈不规则球形,平均粒径为(238.6±1.9) nm,多分散度指数为（0.183±0.017）。herpetrione在大鼠体内动力学行为符合二室模型。herpetrione纳米混悬剂药-时曲线下面积(AUC)为25.19 μg·h·mL^-1,达峰浓度(ρ_max)为11.64 μg·mL^-1,与参比药herpetrione普通混悬剂(PEDX-S)相比,分别提高了2.47倍和2.63倍(P<0.01)。结论 高压均质法制备herpetrione纳米混悬剂工艺简单可行,herpetrione纳米混悬剂能显著提高药物体内生物利用度。     

Changes of Pharmacokinetics of 6,7-Dimethoxycoumarin in A Rat Model of Alpha-Naphthylisothiocyanate-Induced Experimental Hepatic Injury after Yinchenhao Decoction(茵陈蒿汤) Treatment

<正>Objective:To study the changes of pharmacokinetics of 6,7-dimethoxycoumarin in a rat model of alpha-naphthylisothiocyanate(ANIT)-induced experimental hepatic injury after oral administration of Yinchenhao Decoction(茵陈蒿汤,YCHD) using an ultra pressure liquid chromatography(UPLC) method.Methods:Rats were divided into a normal group and a model group,after modeled by 4%ANIT(75 mg/kg) for 48 h,they were orally administrated with YCHD extract at the dose of 0.324 g/kg,and then blood was collected from their orbital sinus after different intervals.Changes in liver function were monitored by the levels of liver enzymes [alanine aminotransferase(ALT),aspartate aminotransferase(AST)]and bilirubins[total bilirubin(TBIL),direct bilirubin(DBIL)],the concentration of 6,7-dimethoxycoumarin in plasma were measured by UPLC,and the pharmaceutical parameters were calculated with DAS2.1.1 software.Results:The concentration-time curve of both normal and modeled rats after oral administration of YCHD was obtained.Their time to maximum plasma concentration(t_(max)) were both 0.25 h,the maximum concentration(C_(max)) were 4.533μg/mL and 6.885μg/mL, and their area under concentration-time curve(AUC)_(0→24h) were 16.272 and 32.981,respectively.There was a 51.88%and 100.46%increase in C_(max) and AUC_(0-t)(P0.05),but there showed a 45.52%and 92.93%reduction in clearance of drug and volum of distribution(P0.05),respectively.Conclusions:Hepatic injury could significantly influence the pharmacokinetics of 6,7-dimethoxycoumarin after oral administration of YCHD,the absorption and distribution process was accelerated in liver injured rats,but the metabolism and elimination process was slowed.And this may lead to a significant accumulation of 6,7-dimethoxycoumarin in the body.     

基于血浆药理学的鳖甲超微粉抗肝纤维化作用研究

目的用血浆药理学方法,体外观察鳖甲超微粉含药血浆抗肝纤维化作用。方法采用体外肝纤维化细胞模型,以大鼠含药血浆对HSC-T6细胞增殖的影响为指标,采用效应动力学方法,确定大鼠给药方案和采血时间,并优选体系中血浆添加量。制备鳖甲超微粉和普通粉含药血浆,MTT法检测含药血浆对HSC-T6细胞增殖的影响,ELISA法测定含药血浆对HSC-T6细胞胶原分泌的影响。结果鳖甲超微粉和普通粉含药血浆对HSC-T6细胞增殖和Ⅰ型胶原合成均有显著抑制作用（P〈0.01）,超微粉组的抑制作用强于普通粉组,且有显著性差异（P〈0.01）。结论鳖甲超微粉碎后可提高其抗肝纤维化疗效。     

星点设计-效应面法优化甘草酸磷脂/胆盐混合胶束处方

目的:制备甘草酸磷脂-胆盐混合胶束,并通过星点设计-效应面法优选其处方.方法:采用薄膜分散法制备甘草酸磷脂-胆盐混合胶束,通过单因素试验考察胆盐对磷脂的增溶作用,测定磷脂在胆盐溶液中溶解度.以胆盐摩尔浓度、缓冲盐溶液pH为考察因素,甘草酸溶解度及混合胶束载药量为指标,采用星点设计试验优化处方,并进行多元线性和二项式非线性方程拟合,利用效应面法确定最佳处方配比.结果:最佳处方为磷脂-胆盐1.19∶1,pH 7.4,胆盐摩尔浓度15 mmol·L-1,甘草酸溶解度21.12 g·L-1,混合胶束载药量53.93％,理论预测值与实测值偏差较小,模型具有良好的预测性.结论:磷脂-胆盐胶束能显著增加甘草酸的溶解度,优选的处方工艺简便、稳定.     

超微粉碎技术的残黄片溶出度研究

目的研究超微粉碎技术对残黄片溶出度的影响。方法采用超微粉碎技术对原料药材进行粉碎,压片,以盐酸溶液（pH 1.0）为溶出介质,采用桨法测定体外溶出度,比较基于超微粉碎技术的残黄片和普通粉碎的残黄片的溶出速率和溶出量。结果基于超微粉碎技术的残黄片的体外累积溶出率相比基于普通粉碎的残黄片有显著提高。结论超微粉碎技术工艺简单易行,可提高残黄片有效成分的溶出。     

波棱甲素纳米混悬剂对D-半乳糖胺诱导的小鼠急性肝损伤的保护作用

 目的 研究波棱甲素纳米混悬液（HNS）对D-半乳糖胺（D-GalN）诱导的小鼠急性肝损伤的保护作用,并与波棱甲素普通混悬剂（HS）进行比较。方法 小鼠每日给药2次,连续给药3.5 d后,一次性腹腔注射D-GalN 800 mg·kg-1造成急性肝损伤模型,20 h后取血清测定丙氨酸基转移酶（ALT）、天冬氨酸氨基转移酶（AST）值。结果 HNS各个剂量组均能显著降低中毒小鼠ALT、AST含量,HS仅高剂量组ALT、AST值显著降低,且同等剂量下,HNS各组均明显优于HS各组;病理检查结果显示,波棱甲素具有明显的保肝作用。结论 HNS对D-GalN诱导的小鼠急性肝损伤具有明显的保护作用,且作用明显优于普通混悬剂。其机制可能在于将其制成纳米混悬剂之后,粒径减小,表面积增大,体内吸收增加,从而使它的药效作用增强。     

Lignans-Rich Extract from Herpetospermum caudigerum Alleviate Physical Fatigue in Mice

Objective

To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum.

Methods

The 80% ethanol extracts of Herpetospermum caudigerum were partitioned with chloroform, ethyl acetate and n-butanol, respectively. Male Kunming mice were divided into 13 groups with 16 mice in each group: a control group fed with water, 9 groups treated with 3 fractions of Herpetospermum caudigerum (chloroform fraction, ethyl acetate fraction and n-butanol fraction) at dose of 80, 160 and 320 mg/kg for the low-dose group, medium-dose group and high-dose group, 3 herpetrione (HPE) treated groups fed with HPE at dose of 15, 30, and 60 mg/kg for the low-dose group, medium-dose group and high-dose group. All animals were treated once per day for 30 days. Anti-fatigue activity was assessed through the forced swimming test and serum biochemical parameters including blood lactic acid (BLA), blood urea nitrogen (BUN), malondialdehyde (MDA), hepatic glycogen (HG), lactic dehydrogenase (LDH), superoxide dismutase (SOD) and glutathione peroxidase (GPx) determined following the recommended procedures provided by the commercial kits.

Results

Compared with the control group, the lignans extract (ethyl acetate fraction) of Herpetospermum caudigerum and HPE could signifificantly prolonged the exhaustive swimming time (P<0.05 or P<0.01), and also increased the HG levels (P<0.05 or P<0.01) and the activities of antioxidant enzymes (SOD, GPx and LDH, P<0.05 or P<0.01); BLA and MDA levels were decreased considerably in lignans extract and HPE treated groups (P<0.05 or P<0.01). HPE also could significantly decrease the BUN contents compared with the control group (P<0.05). The chloroform and n-butanol fraction showed no effect on swimming time and biochemical parameters.

Conclusions

The lignans extract had antifatigue activities and HPE may be partly responsible for the anti-fatigue effects of Herpetospermum caudigerum. The possible mechanisms of anti-fatigue activity were related to the decrease of BUN and BLA, the increase of the HG storage and protecting corpuscular membrane by preventing lipid oxidation via modifying several enzyme activities.

     

全军第二次中医、中西医结合学术会议论文综述

全军第二次中医、中西医结合学术会议于1984年9月21～26日在衡阳召开。会议共收到论文459篇,其中临床研究60％,理论与药物实验研究13.5％,中医基本理论探讨9.9％,四诊研究6.3％,针灸、推拿6.3％,其它4％。下面从科研方法角度加以举要概述。