HPLC法测定泻痢停片中醋酸泼尼松的含量

目的　建立泻痢停片中醋酸泼尼松的高效液相检测法。方法　色谱柱为HypersilODS2 (5 μm ,4.6mm× 2 0 0mm) ,流动相为甲醇 -水 (5 8∶42 ) ,流速 1.0ml min ,检测波长 2 40nm ,氢化可的松为内标物。结果　醋酸泼尼松和内标的保留时间分别为 11.4min和 7.5min。在 80～ 2 40 μg ml浓度范围内 ,醋酸泼尼松与内标峰面积之比和浓度呈良好的线性关系 (r =0 .9998) ,醋酸泼尼松平均回收率为 99.92 % ,RSD为 0 .2 4%。结论　用高效液相色谱法测定醋酸泼尼松的含量 ,有简便、准确、灵敏度高的优点 ,可用于该制剂的质量控制     

甲孕酮联合MVP方案与单纯MVP方案治疗晚期非小细胞肺癌的对比研究

目的　观察患者服用甲孕酮合并 MVP方案与单纯使用 MVP方案化疗治疗初治非小细胞肺癌(non- small cell cancer,NSCL C)的疗效 ,生活质量改善 ,毒性等情况并加以比较。方法　 A组 (2 9例 )接受甲孕酮 MVP方案治疗 ,B组 (2 7例 )接受 MVP方案治疗 ,采用单盲随机分组 ,毒性反应按 WHO标准进行评价。结果　 A、B两组疗效 (CR PR)分别为 2 7.6 %及 2 2 .2 % ,P>0 .0 5。中位生存期 A组 30周 ,B组 2 4周 ,(P<0 .0 1)。白细胞、血红蛋白减少及恶心、呕吐反应 ,B组较 A组明显 ,差异有显著性。两组均未发现其他严重的毒性反应。结论　甲孕酮联合 MVP方案组与单纯 MVP方案治疗组疗效差异无显著性 ,但前者中位生存期长 ,患者生活质量改善 ,毒副反应小     

Hydrolysis kinetics of propylene glycol monomethyl ether acetate in rats in vivo and in rat and human tissues in vitro.

The kinetic equivalency of propylene glycol monomethyl ether (PGME), derived from propylene glycol monomethyl ether acetate (PGMEA), as well as the parent compound (PGME) following intravenous administration to Fischer 344 rats was evaluated. In addition, in vitro hydrolysis rates of PGMEA in blood and liver tissue from rats and humans were determined. The blood kinetics were determined following iv administration to rats of PGME and PGMEA of low [10 and 14.7 mg/kg body weight (bw)] or high (100 and 147 mg/kg) equimolar dosages of PGME and PGMEA, respectively. The blood time courses of PGME elimination for both dosages of both compounds were identical. Half-lives of PGMEA elimination following iv administration of 14.7 or 147 mg PGMEA/kg bw were calculated to be 1.6 and 2.3 min, respectively. Rat and human in vitro hydrolysis rates of PGMEA were determined by incubation of 5 or 50 microg PGMEA/ml in whole blood or liver homogenate. The rate of loss of PGMEA was more rapid in rat blood than in human blood, with hydrolysis half-lives of 36 and 34 min in human blood and 16 and 15 min in rat blood for the 5 and 50 microg/ml concentrations of PGMEA, respectively. In contrast the rate of loss of PGMEA in human and rat liver homogenate incubations was similar, 27-30 min and 34 min, respectively. These data demonstrate the rapid hydrolysis of PGMEA in vivo to its parent glycol ether, PGME and that, once hydrolyzed, the kinetics for PGME derived from PGMEA are identical to that for PGME. This study supports the use of the toxicological database on PGME as a surrogate for PGMEA.     

Enhanced film-forming properties for ethyl cellulose and starch acetate using n-alkenyl succinic anhydrides as novel plasticizers

Purpose: The aim of this study was to investigate the ability of n-alkenyl succinic anhydrides (n-ASAs) to improve the film-forming characteristics of a novel coating polymer, potato starch acetate degree of substitution 2.8 (SA). n-ASAs were also applied to improve the otherwise brittle properties of ethyl cellulose (EC) aqueous dispersion (Aquacoat^®) and EC solvent-based films. Methods: The effectiveness of two n-ASAs, 2-octenyl succinic anhydride (OSA) and 2-dodecen-1-ylsuccinic anhydride were evaluated as plasticizers. Mechanical properties, both water vapor and drug permeabilities, and glass transition temperatures of the cast free films were measured. Triethyl citrate and dibutyl sebacate were used as reference plasticizers. Results: The long hydrocarbon chain of n-ASA, with its accessible carbonyl groups, enabled a strong plasticization effect on the tested polymers. Due to the excellent mechanical properties (i.e., a tough film structure with considerable flexibility) and low permeability of the plasticized films, n-ASAs, and especially OSA proved to be an ideal plasticizer particularly for EC based coatings. Also, the EC aqueous dispersion plasticized with n-ASAs resulted in a markedly enhanced coalescence of the colloidal polymer particles, even at low drying temperatures. Conclusions: In applications where a coating with high flexibility is required, n-ASAs can be used as plasticizers at moderately high concentrations (up to 60–70%, w/w) without losing the high tensile strength, excellent toughness and low permeability of EC and SA films.     

预先咨询对妇女使用醋酸甲孕酮避孕停用率的影响

目的：了解预先咨询对１５０ｍｇ醋酸甲孕酮（ＤＭＰＡ）作为３个月使用１次的长效避孕针的停用率的影响。方法：将４２１例受试者分为两组，２０４例在用药前和用药中对ＤＭＰＡ的激素作用和可能的副反应接受详细的咨询（强化组），２１７例接受一般性咨询（一般组）。每３个月随访１次，持续１年。观察停用率、常见的医疗事件和停用原因。结果：最常见的停用原因是月经改变，虽然强化组月经不规则发生率（３９．７％）较一般组的（２６．３％）高（Ｐ＜０．０１），但其停用率仍显著低于一般组，１年时累积停用率分别为１１．３％（２３／２０４）和４２．４％（９２／２１７）（Ｐ＜０．０００１）。无妊娠和严重的或不期望的医疗事件发生。结论：对预计的副反应作预先咨询，提高了ＤＭＰＡ可接受性。     

Randomised trial of dopamine compared with hydrocortisone for the treatment of hypotensive very low birthweight infants

AIM—To compare the efficacy of hydrocortisone with dopamine for the treatment of hypotensive, very low birthweight (VLBW) infants.METHODS—Forty infants were randomly allocated to receive either hydrocortisone (n=21) or dopamine (n=19).RESULTS—All 19 infants randomised to dopamine responded; 17 of 21 (81%) did so in the hydrocortisone group. Three of the four non-responders in the hydrocortisone group had clinically significant left to right ductal shunting. The incidence of bronchopulmonary dysplasia, retinopathy of prematurity, intraventricular haemorrhage, necrotising enterocolitis, symptomatic patent ductus arteriosus, hyperglycaemia, sepsis (bacterial or fungal) or survival did not differ between groups. The adrenocorticotrophic hormone (ACTH) stimulated plasma cortisol activity, either before or after treatment, did not differ between the two groups of infants. Although a significant difference in efficacy between dopamine and hydrocortisone was not noted (P = 0.108), there were four treatment failures in the hydrocortisone group, compared with none in the dopamine group.CONCLUSION—Both hydrocortisone and dopamine are effective treatments for hypotension in very low birthweight infants.     

HPLC法测定尿素-醋酸曲安萘德软膏中醋酸曲安萘德的含量

目的 采用高效液相色谱法测定尿素醋酸曲安萘德软膏中醋酸曲安萘德的含量。方法 Kromasil C₁₈(150mm×4.6mm,5μm)色谱柱;流动相为甲醇水乙醚(62∶38∶2);流量1.0ml·min^-1;检测波长为240nm。采用炔诺酮作内标物质。结果 醋酸曲安萘德在0.16～0.79μg范围内呈线性关系,r=0.9998(n=5),平均回收率为100.7%(n=5),RSD为0.97%。结论 本法简便、准确,可以控制该制剂的质量。     

地冰凝胶的制备与质量控制

目的 :制备地冰凝胶 ,并建立其质量控制方法。方法 :以0 5%卡波姆940作为凝胶基质 ,采用高效液相色谱法测定制剂中醋酸地塞米松的含量 ,并进行稳定性考察和皮肤刺激性试验。结果 :醋酸地塞米松检测浓度在20～120μg/ml范围内线性关系良好 ,平均回收率为101 1% ,RSD=0 92% ;制剂稳定性良好 ,对皮肤无刺激作用。结论 :该制剂处方合理 ,制备工艺简便 ,质量控制方法简单、准确。     

Dramatic suppression of plasma and urinary prostate specific antigen and human glandular kallikrein by antiandrogens in male-to-female transsexuals

PURPOSE: Prostate specific antigen (PSA) and human glandular kallikrein (hK2) are mainly produced by the prostate and their genes are regulated by androgens through the androgen receptor. We determine whether PSA and hK2 change significantly in plasma and urine after antiandrogen treatment in male-to-female transsexuals. MATERIALS AND METHODS: Plasma and urine PSA and hK2 were measured with highly sensitive immunofluorometric procedures capable of detecting within 1 or 6 ng./l. PSA or hK2, respectively. Study groups consisted of 10 men treated with cyproterone acetate only (group 1), 15 transdermal estradiol plus cyproterone acetate (group 2) and 31 ethinyl estradiol plus cyproterone acetate (group 3). Plasma and urine samples were collected before initiation of treatment as well as after 4 months of hormonal therapy. For a subset of group 3 patients blood and urine samples were also obtained after 12 months of treatment. RESULTS: Cyproterone acetate, a steroidal antiandrogen, alone or with estradiol was able to suppress greater than 90% of plasma and urinary PSA and hK2 concentration after 4 or 12 months of therapy. CONCLUSIONS: Cyproterone acetate therapy causes dramatic suppression of plasma and urinary PSA and hK2 in men without prostate cancer. Since cyproterone acetate is used for prostate cancer treatment, suppression of PSA after hormonal therapy may not accurately reflect therapy success in reducing tumor burden.     

醋酸舍莫瑞林的免疫活性研究

目的　观察醋酸舍莫瑞林对免疫抑制模型小鼠免疫功能的调节作用。方法　通过给小鼠腹腔注射免疫抑制剂环磷酰胺 ,建立免疫功能低下模型 ,腹腔注射醋酸舍莫瑞林进行体内拮抗实验。测定胸腺指数、脾脏指数、巨噬细胞吞噬功能、T淋巴细胞的增殖指数、耳肿胀度、血清IL - 2的含量。结果　醋酸舍莫瑞林 ( 0 18,0 36mg/kg)能显著提高被环磷酰胺抑制的胸腺和脾脏重量 (P <0 0 1) ;使巨噬细胞吞噬功能明显增加 ,并能拮抗环磷酰胺对小鼠脾脏T淋巴细胞增殖、二硝基氯苯 (DNCB)诱导的迟发型超敏反应和IL - 2产生的免疫抑制作用。结论　醋酸舍莫瑞林能拮抗环磷酰胺所引发的免疫抑制作用