头孢氨苄缓释片在健康人体内的生物利用度和药物动力学

目的:比较头孢氨苄缓释片和普通胶囊的生物利用度和药物动力学。方法：10例健康志愿者分别单剂量口服500mg头孢氨苄缓释片和普通胶囊，血药浓度测定方法为HPLC法。结果：两种剂型体内过程均符合一室开放模型，缓释片的达峰时间（Tmax）为（2．58±0．59）h，峰浓度（Cmax）为（10．08±1．68）μg／ml．吸收速率常数（Ka）为（0．90±0．53）／h，消除速率常数（Ke）为（0.26±0.02）／g，半衰期（T1／2）为（2.67±0.23）h，清除率（Cl）为（6.93±1.71）L／h，分布容积（Vd）为（26.66±6.72）L，药一时曲线下面积（AUC）为（48.31±9.32）μg·h／ml。两种剂型T一C一Ka、Ke、T1／2和Cl均存在显著性差异（P＜0．01），Vd、AUC无显著性差异（P＞0．05）；缓释片的相对生物利用度为（104．90±8．35）％。结论：缓释片的吸收减慢，Tmax推迟，T1／2延长，可减少服药次数，提高药物治疗的顺应性。     

吡哌酸片的电荷转移反应分光光度测定

研究了吡哌酸与四氯苯醌间的荷移反应．两者在硼砂缓冲溶液中形成１∶１的络合物，其λ_（ｍａｘ）为３３０．８ｎｍ，摩尔吸光系数ε＝１．６６×１０~４，ＲＳＤ为２．２％。用于测定制剂含量，结果与药典方法一致。     

Improved Static Compression Behaviors and Tablettabilities of Spherically Agglomerated Crystals Produced by the Spherical Crystallization Technique with a Two-Solvent System

Purpose. Poorly compressible crystals of acebutolol hydrochloride were agglomerated by the spherical crystallization technique with a two-solvent system to improve the compressibility for direct tabletting. The mechanism of improvements in static compression behaviors and tablettabilities of the spherically agglomerated crystals were investigated. Methods. The improvement of static compression behaviors of the agglomerated crystals was determined by measuring the stress relaxations and elastic recoveries of compressed powder of original and agglomerated crystals. The improved tablettability of agglomerated crystals was evaluated by the pressure transmission ratio upon compression, the ejection pressure for releasing the tablet from the die and the tablet strength, i.e., tensile strength required for breaking. Results. The higher relaxation pressure and the lower elastic recovery of the agglomerated crystals than of the original crystals were found. The pressure transmission ratio data showed that the friction pressures of the two crystals were similar during the compression period. The ejection pressure of the agglomerated crystals was lower than that of the original crystals. The tensile strength of the tablet of agglomerated crystals was greater than that of the original crystals. Conclusions. The compressibility and tablettability of the spherically agglomerated crystals prepared by the spherical crystallization technique were much improved due to their increased plastic property and reduced adhesive property compared to the original crystals.     

火把花根片对哮喘豚鼠气道炎症抑制作用的实验研究

目的 研究火把花根片对哮喘豚鼠气道炎症的作用。方法 建立哮喘豚鼠动物模型。豚鼠17只随机分为2组，即对照组(8只)和火把花根组(9只)。测定支气管肺泡灌洗液(BAIF)细胞总数、嗜酸性粒细胞、淋巴细胞、中性粒细胞数量及蛋白浓度，图像分析软件测定气道壁厚度及腺体厚度。结果 火把花根组BAIF细胞总数、嗜酸性较细胞为主的炎性细胞数量及蛋白浓度均低于对照组(P＜0．01)，图像分析表明火把花根组气道壁厚度及腺体厚度均较对照组减低(P＜0．01)。结论 火把花根片可抑制哮喘豚鼠的气道慢性炎症，对支气管哮喘有治疗作用。     

苏云金芽孢杆菌以色列变种发泡块剂灭白纹伊蚊幼虫的效果研究

目的：比较苏云金芽孢杆菌Bti－951发泡块剂（由本所研制）和Bti－Ft发泡块剂（德国提供）灭白纹伊蚊效果。方法：模拟现场试验和现场试验。结果：室内生物测定，Bti－951发泡块剂LD50为0.2365μg／ml；Bti－Ft发泡块剂LD50为0．0903μg／ml。在3．4～3．7m2现场水池中，两种发泡块剂使用剂量为0．5、1．0、1．5g／m2，制剂24小时灭蚊效果均达100％；当剂量为1．5g／m2时，Bti-951发泡块剂持效15天，Bti－Ft可达20天。结论：该剂型运用于小型水体，便于贮存、携带和使用，比乳剂、粉剂持效更长。     

米非司酮配伍米索前列醇终止早孕118例临床观察

就米非司酮配伍采米前列醇序贯用药终止７周内早孕１１８例进行临床观察，发现完全流产率９２．３７％，不全流产率５．９３％，持续妊娠率１．６９％。临床证明该方法方便、安全有效、副作用极小，但个别孕妇产生不全流产，引起出血过多及出血时间延长。不全流产率有随孕妇年龄、孕龄、孕次增加而增加的趋势。     

Pharmacokinetics of Controlled Release and Immediate Release Morphine Sulphate Tablets after a Single Dose and Multiple Doses in Chinese Volunteers

健康志愿者１０名，随机交叉口服硫酸吗啡控释片（ＣＲＭＳ）３０ｍｇ（３０ｍｇ×１）和硫酸吗啡普通片（ＩＲＭＳ）２０ｍｇ（１０ｍｇ×２），分别于服药前后各时点取静脉血，用ＧＣＭＳ测定血浆中吗啡含量。以药代软件程序处理，分别求得ＣＲＭＳ和ＩＲＭＳ的Ｃｍａｘ为１９．３８±３．８０和２１．２７±６．２１ｎｇ／ｍｌ；ｔｍａｘ为２．３６±０．３７ｈ和０．５５±０．１６ｈ；ｔ１／２β为３．５３±０．８７ｈ和３．０３±０．７４ｈ，曲线下面积ＡＵＣ为１４５．１５±１７．６５和９３．０８±１６．６５ｎｇ·ｈ／ｍｌ。癌症病人多次口服硫酸吗啡至稳态，ＣＲＭＳ和ＩＲＭＳ的峰浓度分别为２７．４３±０．３３ｎｇ／ｍｌ，２２．６８±０．１６ｎｇ／ｍｌ；谷浓度分别为１９．４５±１．４４ｎｇ／ｍｌ；１８．１４±０．４９ｎｇ／ｍｌ。     

A prospective randomized,double-blinded,placebo-controlled trial comparing mifepristone and vaginal misoprostol to vaginal misoprostol alone for elective termination of early pregnancy

BACKGROUND: Vaginal misoprostol has been shown to be an effective single agent for medical abortion. This randomized, double-blinded, placebo-controlled trial compared a regimen of mifepristone and misoprostol with misoprostol alone for termination of early pregnancy. METHODS: 250 women with gestations < or = 56 days were randomized by a random number table to receive either 200 mg mifepristone orally or placebo followed 48 h later by 800 microg vaginal misoprostol. Administration of misoprostol was repeated every 24 h up to three doses if abortion failed to occur. Abortion success was defined as complete abortion without the use of surgical aspiration. RESULTS: Successful medical abortions occurred in 114 out of 119 subjects (95.7%) after mifepristone followed by vaginal misoprostol. In all, 110 out of 125 subjects (88.0%) successfully aborted after placebo and vaginal misoprostol. The higher success rate of complete abortion with the mifepristone and misoprostol regimen was statistically significant compared with the placebo and misoprostol regimen (P < 0.05). CONCLUSIONS: A regimen of mifepristone and misoprostol was significantly more effective for termination of pregnancies < or = 56 days than misoprostol alone. The 88% efficacy obtained with vaginal misoprostol alone may be clinically acceptable when mifepristone is not available.     

白松片对慢性应激抑郁模型大鼠行为学及血浆CORT、ACTH的影响

目的：观察白松片对慢性应激抑郁大鼠模型行为学和血浆CORT、ACTH含量的影响。方法：SD雄性大鼠28只随机分为空白对照组、模型对照组、氟西汀对照组及白松片试验组，选用慢性轻度不可预见性应激加孤养造模，观察各组大鼠敞箱实验和液体消耗等行为学指标变化，采用放射免疫方法检测大鼠血浆皮质醇(CORT)和促肾上腺皮质激素(ACTH)含量。结果：慢性应激抑郁大鼠体重增加缓慢，敞箱实验中的水平运动、垂直运动得分、清洁动作次数显著减少，中央格停留时间显著延长；糖水消耗明显下降，纯水消耗显著增多，而且其血浆皮质醇和促肾上腺皮质激素含量增加。氟西汀和白松片均显著改善慢性应激抑郁大鼠模型的行为学和神经内分泌变化。结论：慢性轻度不可预见性应激可使大鼠行为及神经内分泌发生异常改变，引起抑郁状态，白松片对此具有一定拮抗作用。     

芪丹通脉片对缺血/再灌注犬心肌微血管功能的影响

目的评价中药复方芪丹通脉片对急性缺血再灌注致心肌微血管功能的影响。方法应用12只健康犬,随机分为对照组(control)和芪丹通脉片治疗组(QDTMT treatment group),对照组经十二指肠给予生理盐水(1.5ml/kg),给药后30min分离冠状动脉左前降支,放置电磁流量计探头测定血流量,在其下缘左前降支1/2处结扎90min,松开后再灌注180min观察,分别于灌胃前、缺血90min和再灌注180min静脉快速均匀推入微泡声学造影剂SONOVUE,FLASH模式进行静脉声学造影,实时连续记录心肌声学造影前后的图像采用,采用Echopac图象工作站软件包进行分析心肌声学造影的图像视频密度,根据时间-视频密度曲线计算曲线下面积(area under curve,AUC)以评价心肌微血管的血流灌注状态,根据图像分析缺血心肌范围的影响。芪丹通脉片组则经十二指肠给予芪丹通脉片浸膏混悬液(1g/ml,1.5ml/kg),其余实验过程同对照组。并在不同时间点从冠状静脉窦采血,检测血清中NO和血浆中ET-1的含量。结果在基础状态、缺血前和缺血90min,对照组和芪丹通脉片干预组的时间-视频密度曲线计算曲线下面积(AUC)以及缺血后出现的灌注缺损所占左心室的百分比没有显著差异。然而再灌注180min两组的AUC存在显著差异(14.09±2.31 vs 11.47±1.55,P<0.05),左心室心肌灌流均没有完全恢复,但芪丹通脉片能够显著促进再灌注后心肌微循环灌流的恢复(92.10±2.2)%,与对照组(87.49±4.12)%比较,存在显著差异(P<0.05)。在缺血90min和再灌注180min,芪丹通脉片处理组血清中NO和血浆中ET-1分别为(68.98±10.01)μmol/L、(67.55±9.81)μmol/L和(114.73±11.89)μg/L,(139.97±12.36)μg/L,与对照组存在显著差异(56.38±8.27)μmol/L,(53.55±6.03)μmol/L和(137.40±13.48)μg/L,(161.90±19.14)μg/L,(P<0.05)。结论芪丹通脉片能够促进心肌缺血/再灌注后微循环血流的恢复,调节循环血中的NO和ET含量,改善微循环功能,抑制缺血/再灌注所致的心肌损伤。