亚甲蓝光敏消毒法对人血浆部分成分影响的试验观察

向人血浆中加入亚甲蓝染料浓度为１ μｍｏｌ／Ｌ,再以１０ ０００ ｌｕｘ 强度的溴钨灯光照射１０ ｍｉｎ,血浆中主要成分的生化指标只有胆红素与尿酸两种代谢产物有明显降低,其余均无明显变化,各种酶活性未发生明显改变。血浆蛋白分子量ＳＤＳ－ ＰＡＧＥ与盘状ＰＡＧＥ电泳未见明显异常。微量免疫电泳与免疫交叉电泳也未见血浆成分免疫原性改变。     

HUMAN PLASMA ALPHA 2-MACROGLOBULIN : AN INHIBITOR OF PLASMA KALLIKREIN

Activation of plasma kallikrein arginine esterase activity by kaolin resulted in peak activity at 1 min of incubation and a 50% reduction in activity at 5 min in normal plasma, and 30% reduction in the plasma of patients with hereditary angioneurotic edema who lacked the C1 inactivator. The peak esterolytic activity was inhibited by soybean trypsin inhibitor whereas the 5 min activity was resistant to this inhibitor. Acid treatment of normal and hereditary angioneurotic edema plasma destroyed the factor responsible for the fall in esterase activity at 5 min and the factor which rendered the esterase resistant to soybean trypsin inhibitor. Purified α₂-macroglobulin inhibited approximately 50% of the TAMe esterase activity of purified plasma kallikrein without changing its activity toward basic amino acid esters. The interaction between the α₂-macroglobulin and kallikrein resulted in alterations in the gel filtration chromatographic pattern of the TAMe esterase and biologic activity of kallikrein, indicating that kallikrein was bound to the α₂-macroglobulin. The TAMe esterase activity of this complex, isolated by column chromatography, was resistant to C1 inactivator and SBTI. Studies of incubation mixtures of kallikrein, α₂-macroglobulin and C1 inactivator suggested that these inhibitors compete for the enzyme, and that the α₂-macroglobulin partially protects the esterase activity of kallikrein from C1 inactivator. The α₂-macroglobulin isolated from kaolin-activated plasma possessed 240 times the esterolytic activity of the α₂-macroglobulin purified from plasma treated with inhibitors of kallikrein and of its activation. The α₂-macroglobulin blocked the uterine-containing activity and vascular permeability-inducing effects of plasma kallikrein. These studies suggest that the α₂-macroglobulin is a major plasma inhibitor of kallikrein and provide a new example of an interrelationship between the coagulation, fibrinolytic, and kallikrein enzyme systems.     

EFFECTS OF ORAL PRAZOSIN ON TOTAL PLASMA DIGOXIN LEVELS

Prazosin and digoxin are frequently coadministered in clinical practice. To determine the effects of oral prazosin treatment on steady-state digoxin levels, 20 patients receiving a constant maintenance dose of digoxin, who had normal renal and liver functions and were not receiving any other treatment, were given 5 mg of prazosin for 3 days. Plasma digoxin levels were measured before, on days 1 and 3 of prazosin treatment, and after prazosin had been discontinued. It was found that prazosin significantly increased plasma digoxin levels. On discontinuation of prazosin digoxin levels returned to their previous values.     

泮托拉唑肠溶胶囊的人体生物等效性研究

目的评价2种泮托拉唑肠溶胶囊的生物等效性。方法18名健康男性受试者,随机分组,自身交叉口服泮托拉唑肠溶胶囊实验制剂和参比制剂40 mg,采用高效液相色谱法-质谱法测定用药后不同时间的经时血药浓度,以方差分析方法对主要药动学参数AUC0→13、Cmax进行均数的差别检验,以双单侧t检验进行生物等效性判断;对Tmax以非参数检验(符号秩检验)进行生物等效性判断。结果2种泮托拉唑肠溶胶囊实验制剂和参比制剂的药代动力学参数AUC0→13、AUC0→∞、Tmax、Cmax、t1/2分别为7 670.1±2509.6和7 549.6±2 149.9、7 724.4±2 535.1和7 591.2±2 161.2[ng/(h.mL)]、3.0±0.2和3.0±0.2 h、3 107.2±567.0和3 267.2±717.3(ng/mL)、1.1±0.3和1.0±0.2(h)。实验制剂的相对生物利用度为(100.8±10.3)%。方差分析结果表明两种制剂的主要药动学参数AUC0→13、Cmax之间无明显差异。结论2种制剂为生物等效制剂。     

SAFE DISPOSAL OF SOME COMMONLY USED INJECTABLE ANTINEOPLASTIC DRUGS

The disposal of unrequired, injectable antineoplastic drugs in hospital pharmacy departments has recently become a growing problem. In 1981, the manufacturers of these preparations were asked to provide advice on the disposal of their product(s). This article is a summary of the recommendations received from the manufacturers.     

MIGRATION OF LYMPHOCYTES IN PLASMA CULTURES OF HUMAN LYMPH NODES

1. Lymphocytes were usually the first cells to migrate out into the plasmic clot from explanted pieces of lymph nodes. 2. Their paths of migration were irregular but in general they proceeded away from the explant. 3. The lymphocytes migrated at rates varying from 0.03 to 0.0013 mm. per minute. The rate of any one varied from minute to minute, and they often came to rest for varying lengths of time. 4. The migrating lymphocytes were very much elongated, with the nucleus always near the anterior end. The elongated tail contained the endoplasm with a few granular mitochondria and usually a few granules which took up neutral red. 5. The lymphocytes in cultures made from normal and pathological lymph nodes in auto and homoplasma showed no differences.     

IS MONITORING PLASMA LEVELS OF NETILMICIN NECESSARY IN NEONATES?

Thirty-two neonates were treated with netilmicin 3 mg/kg every 12 h by IV infusion for 30 min for suspected infections, colonization, or proven infections. Pharmacokinetic studies were performed in order to define the situations in which monitoring of plasma levels would be appropriate. Mean plasma levels were within the therapeutic range and did not differ in fullterms and preterms. In the 4 children who had 2 successive pharmacokinetic studies, plasma levels were increased between H1 and H5 at the second evaluation due to netilmicin accumulation. Plasma half-life was longer in proven infections and seemed to decrease in preterms with increased gestational age. These results suggest that the dosage schedule should be left inchanged, but that administration time should be reduced from 30 to 20 min and that peak and trough plasma levels should be measured only in proven infections, in very premature babies (gestational age less than 33 wk), and during netilmicin treatment longer than 5 d.