利福平、聚维酮碘和重组人表皮细胞生长因子治疗大面积烧伤残余创面的观察

目的探讨应用利福平、聚维酮碘软膏和重组人表皮细胞生长因子（rhEGF），治疗大面积烧伤残余创面的疗效。方法治疗组应用利福平、聚维酮碘软膏和rhEGF治疗大面积烧伤残余创面79个，对照组单用聚维酮碘软膏治疗创面66个，比较两组创面细菌清除率和创面愈合情况。结果治疗组创面的总有效率和创面细菌清除率分别为89．87％和86．10％，对照组分别为47％和130％，差别有显著性意义，创面细菌培养以金黄色葡萄球菌和表皮葡萄球菌为常见，对多种抗生素耐药。结论利福平、聚维酮碘软膏和rhEGF对治疗大面积烧伤残余创面有良好的效果。     

烧伤创面外用重组人表皮生长因子衍生物过敏2例

例 1 :患者男 ,48岁。因火焰烧伤左小腿 4%深 2度 1周入院。既往无药物食物过敏史及特殊病史。查体心肺腹无异常 ,创面基底红白相间 ,疼痛 ,肿胀 ,创缘呈炎性反应。在院予以输注青霉素抗炎治疗 ,局部创面 1‰洗必泰液湿敷 1次 /4日后创面肿胀及炎性反应消退。后创面外用ｒｈＥＧＦ(重组人表皮生长因子衍生物 )喷雾剂喷涂 1次 ,2小时后患者出现左小腿创面外及左大腿正常皮肤散在红斑 ,痒痛 ,患者其间未接触特殊食物及其他药物 ,即考虑药物过敏。停用抗生素 ,口服抗组胺药 ,创面ｒｈＥＧＦ喷涂创面换药。患者症状加重 ,全身红斑融成片 ,剧烈痒…     

重组人表皮生长因子软膏对烧伤患者血清表皮生长因子浓度的影响

目的:观察不同深度、不同面积烧伤创面对局部外用重组人表皮生长因子(rhEGF)软膏的吸收作用以及对血清EGF浓度的影响。方法:选择烧伤患者41例,局部外用rhEGF软膏治疗,每日换药一次。浅Ⅱ°创面患者于用药前和用药第4,7天;深Ⅱ°创面于用药前和用药后第7,14天,分别取患者静脉血清,采用放射免疫分析法测定患者各时间点血清中EGF浓度。结果:rhEGF软膏在试验浓度范围内,无论用药面积大小和用药时间长短其血清EGF水平均无明显变化,各时间点用药前后EGF血药浓度无显著差异(P>0.05);血清EGF浓度与创面深度和用药面积无明显的相关性。结论:rhEGF软膏局部外用,通过创面吸收的量甚微,体内无蓄积现象。     

重组人表皮生长因子外用治疗烧伤创面的多中心研究

目的 :观察重组人表皮生长因子 (rhEGF)治疗烧伤的疗效和安全性。方法 :以rhEGF治疗各类烧伤 30 2例 (男性 2 13例 ,女性 89例 ,年龄 33a±s 11a) ,其中试验组 (双盲自身对照 ) 190例 ,开放组112例 ,在常规治疗 ( 1%磺胺嘧啶银霜 )基础上 ,局部喷涂rhEGF或安慰剂。结果 :rhEGF用于浅Ⅱ度、深Ⅱ度、供皮区、残余创面 ,试验组较对照组愈合时间分别提前 2 ,3,3,6d ,不良反应轻微。结论 :rhEGF对烧伤创面具有明显的促进愈合的作用     

重组人表皮生长因子凝胶剂的研制

目的：研制用于创伤修复的重组人表皮生长因子（recombinant human epidermal growth factor rhEGF)凝胶剂。方法：以卡泊姆为水溶性凝胶基质制备rhEGF的凝胶剂,并以大鼠皮肤急性创伤模型和大鼠皮肤烫伤模型评价了rhEGF凝胶剂在创伤修复中的效果。结果：所得rhEGF凝胶剂制备工艺简单,质量可靠,使用方便,对于大鼠皮肤急性创伤和大鼠皮肤烫伤具有明显的疗效。结论：rhEGF凝胶剂可望应用于临床。     

表皮生长因子对创面修复作用的临床观察

目的：观察表皮生长因子（rhEGF)对创面的修复作用。方法：选择30例各类创面,同时选择同体相似深度,相应部位30个创面作对照,创面清创后将浸透rhEGF的双层纱布敷于创面上,外敷凡士林油纱,无菌纱布包扎。每日或隔日换药,观察至愈合。结果：总显效率70%,可使浅Ⅱ度、深Ⅱ度创面分别提前3d、3.2d愈合,3例慢性创面平均18d愈合。结论：rhEGF对浅Ⅱ度创面有非常明显的促进创面愈合作用,对深Ⅱ度创面、慢性创面也有促进愈合作用。     

重组人表皮生长因子凝胶在烧伤创面中的应用

目的：观察外用重组人表皮生长因子（rhEGF）凝胶对人体烧伤创面的治疗作用和安全性。方法：选择2008年1月-2009年6月收治的烧伤患者60例,基本处理后取重组人表皮生长因子凝胶适量均匀涂于创面,需要包扎时将消毒纱布覆盖于创面,进行包扎。观察创面的愈合时间及瘢痕生成情况。结果：创面全部自行愈合,部分患者有散在的扁平瘢痕,无明显瘢痕增生。结论：外用rhEGF凝胶能加快烧伤创面的愈合速度、缩短愈合时间、提高愈合质量、减少瘢痕的形成,无明显不良反应,安全性好。     

重组人表皮生长因子对各种创面的治疗作用

目的　观察重组人表皮生长因子 (rhEGF)对临床各种常见创面的治疗作用和副作用。方法　选择浅Ⅱ°、深Ⅱ°烧伤创面、慢性溃疡创面和中厚供皮区创面共 43例患者为研究对象 ,所有病例均行自身对照 ,选择自身相应部位、相似深度创面作对照 ,慢性溃疡创面以治疗前的病情作对照。结果　治疗组浅Ⅱ°、深Ⅱ°烧伤创面、中厚供皮区创面愈合速度加快 ,同期愈合率提高 ,愈合时间缩短。对慢性溃疡创面也有疗效。未观察到与使用rhEGF有关的全身系统异常变化和不良反应。结论　重组人表皮生长因子是对临床各种常见创面有效、安全的治疗药物     

表皮生长因子的分离纯化与检测

评述近３０年来，天然来源表皮生长因子（ＥＧＦ）分离纯化的主要方法以及活性检测的各种手段。     

重组人酸性成纤维细胞生长因子皮肤用药的药代动力学

目的研究rhaFGF在健康及破损皮肤用药的药代动力学特征。方法在兔健康及破损皮肤上均匀涂抹¹²⁵I-rhaFGF 180 U·cm^-2后,在不同的时间测血浆及组织中的放射性计数,结合纸层析的方法测定组织和血浆中的¹²⁵I-rhaFGF的含量。结果破损皮肤用药后,血中rhaFGF原型物浓度呈快速上升状态,0.5 h达最大值(73.03 pg·mL^-1),其后迅速下降,3 h后接近0。¹²⁵I-rhaFGF给药后96 h,放射性主要浓集于皮肤,其次是肾,大脑最少。结论rhaFGF不能通过健康皮肤进入体内,可通过破损皮肤进入血循环,但吸收量少,原形物半衰期短,无蓄积作用;吸收后的rhaFGF对皮肤有较大亲和力,可分布于远处皮肤,且含量较高。     

THE EFFECT OF FOOD ON CABERGOLINE PHARMACOKINETICS AND TOLERABILITY IN HEALTHY VOLUNTEERS

The effect of food on the pharmacokinetics and tolerability of cabergoline in man was investigated. For this purpose an open, randomized, single-dose study was conducted in 12 healthy male volunteers who received 1 mg cabergoline as tablets both under fasting conditions and after a breakfast containing a substantial amount of carbohydrates, fat, and proteins, in a crossover fashion. The two treatments were separated by a 4 week washout period. Plasma and urine were collected up to 336 and 168 h respectively after administration and cabergoline concentration was measured in both fluids using a validated radioimmunoassay. Tolerability assessment included haematology, blood chemistry, and urinalysis, blood pressure and heart rate measurements, and ECG. Under both fasting and fed conditions low but persistent cabergoline plasma levels were observed in the present study up to 2 weeks after drug intake, in agreement with the long-lasting prolactin-lowering activity of the drug. In subjects receiving cabergoline under fed or fasting conditions, C_max values averaged 44 and 54 pg mL⁻¹, AUC_{(0–336 h)} averaged 6392 and 5331 pg h mL⁻¹, Ae_{(0–168 h)} averaged 12·7 and 11·9 μg, and t_1/2 averaged 109·7 and 101·3 h, respectively. No statistically significant difference was found when C_max, AUC_{(0–336 h)}, t_1/2, and Ae_{(0–168 h)} from subjects treated under fasting and fed conditions were compared. Median t_max values in subjects treated under fasting or fed conditions were identical (2·5 h). The statistical analysis applied to the parameters chosen to evaluate the variations in the blood pressure profiles observed either supine or standing did not show any significant difference between the fed and fasting conditions. Heart rate values were not significantly modified after cabergoline under either fed or fasting conditions. Laboratory evaluation showed some minor deviations from normal, which were not clinically relevant (only one subject showed an occasional and transient elevation in alkaline phosphatase which disappeared in the subsequent laboratory evaluations) and were considered for the most part not to be drug related. Eleven subjects reported adverse events (one after both treatments, five only after drug intake under fasting conditions, and five only after drug intake with food). Side-effects, typical of the pharmacological class, included headache, somnolence, dizziness, nausea, light-headedness, feeling of faintness, and slowing of thought. They were reported mostly on the day of the first drug administration, were mainly short lasting, and were all mild or moderate in severity. In conclusion, the comparison of the pharmacokinetic and tolerability parameters evaluated in the present study indicates that the pharmacokinetics, as well as the safety, of cabergoline are not modified by food intake.     

奥美拉唑胶囊在健康人体内的药物动力学研究

目的：研究健康志愿受试者单剂量口服20mg不同厂家生产的奥美拉唑胶囊剂后的药物代谢动力学。方法：采用HPLC定量检出健康志愿受试者单剂量口服奥美拉唑胶囊剂后不同时间的奥美拉唑血药浓度情况。结果：经3p87药动学程序处理,奥美拉唑胶囊剂A和B在正常人体内工谢过程符合二室模型。结论：OM体内代谢的个体差异圈在,体内血药浓度维持时间长,其中胶囊剂A具有更好的CmaxTmax和AUC.     

葡萄糖酸锌健康人体内生物利用度研究

采用原子吸收分光光度法测定葡萄糖酸锌(ZG)在人体内的生物利用度,用一定模型分析了ZG片药动学参数,其相对于硫酸锌片的生物利用度为144.2％。     

沙丁胺醇气雾剂在健康受试者体内的药代动力学及生物利用度研究

目的研究沙丁胺醇气雾剂在健康受试者体内的药代动力学及其相对于口服水溶液的生物利用度.方法以10名健康男性志愿者为研究对象,采取随机分组、自身对照、开放实验设计,在吸入或口服沙丁胺醇1.2mg后,定时采血,用HPLC方法测定血浆药物浓度,通过PCNONLIN软件进行房室模型拟合,求算药代动力学参数,用非房室模型计算相对生物利用度.结果沙丁胺醇气雾剂的人体内动力学过程符合二室开放模型.两种给药方式的T_max分别为(0.22±0.07)h和(1.8±0.6)h,C_max分别为(3.4±1.1)ng·mL^-1和(3.9±1.4)ng·mL^-1,T_1/2β分别为(4.5±1.5)h和(4.6±1.1)h.AUC_{0-20 min (inhal)}为AUC_{0-20 min (po)} 的7.94倍.相对生物利用度为57.23%.结论所建立的HPLC方法灵敏、专一、准确、精密.沙丁胺醇气雾剂在人体内的吸收过程与口服水溶液有显著差异.     

MITOGENIC ACTIONS OF ENDOTHELIN-1 AND EPIDERMAL GROWTH FACTOR IN CULTURED AIRWAY SMOOTH MUSCLE

1. Hyperplasia of airway smooth muscle contributes to the increase in bronchomotor responsiveness that characterizes asthma. We have investigated the mitogenic potential of endothelin-1 (ET-1) and epidermal growth factor (EGF) in guinea-pig cultured airway smooth muscle and the relationship of these actions to tyrosine phosphorylation and increases in intracellular calcium (Ca²⁺_i). 2. ET-1 stimulated DNA and protein synthesis and also increased cell number, but these mitogenic actions were small compared with those of EGF. 3. ET-1 and EGF increased the level of tyrosine phophorylation of a range of proteins with apparent molecular weights between 80 and 100 kDa and also increased phosphorylation of a single protein of 33 kDa. 4. Ca²⁺_i levels were increased by both ET-1 and EGF. However, concentrations of EGF three orders of magnitude higher than those having mitogenic actions or increasing protein tyrosine phosphorylation were required. ET-1 was a more potent stimulant of increases in intracellular calcium than of mitogenesis. 5. We conclude that elevation of Ca²⁺_i is unlikely to be an important signal for the mitogenic action of EGF. It is suggested that stimulants at the EGF receptor (EGF and transforming growth factor a) may play a role in the airway smooth muscle hyperplasia in asthma.     

国产依诺沙星在健康人体内的药代动力学和制剂生物利用度研究

本文报道18例健康志愿者口服依诺沙星后的药代动力学参数和制剂的生物利用度。用高效液相色谱仪测定服药后15小时内的血浆药浓,结果表明:该药吸收迅速、分布相短暂,体内过程符合线性动力学。口服原粉(553mg)后主要药代动力学参数为:t_(max)=1.10±0.49h;C_(max)=4.37±0.82mg/L;K_α=2.89±1.10h~(-1);tlag=0.18±0.08h;AUC_(-noit)=31.71±6.84h·mg/L;其中13例为二室模型:K_(12)=0.51±0.36h~(-1);K_(21)=0.46±0.12h_(-1);t_(1/2)α=0.72±0.27h;t_(1/2)β=6.77±1.12h;另5例为一室模型:t_(1/2)Ke=4.98±0.55h。随机交叉口服片剂(600mg)和胶囊剂(1200mg),未发现血药浓度消除呈现剂量依赖性。供试3种片剂和1种胶囊剂与原粉比较,均具有较高的相对生物利用度,其范围为98.3％～101. 6％。