Cosolvency of Dimethyl Isosorbide for Steroid Solubility

Dimethyl isosorbide (DMI), which is currently under investigation for its potential use as a pharmaceutical vehicle and drug permeation enhancer, is a water-miscible liquid with relatively low viscosity. The solubilization behavior of DMI as a cosolvent for nonpolar drugs was characterized via dielectric constant measurements of binary solvent systems containing DMI and either water, propylene glycol (PG), or polyethylene glycol (PEG). Evidence from the dielectric constant profiles and NMR studies suggest that DMI undergoes complexation with water and PG, but not with PEG, through hydrogen bonding interactions. The solvent complexation exhibited a major effect on the solubilities of prednisone, dexamethasone, and prednisolone in the mixed solvent systems. Maximum solubility of each drug was found to occur near a DMI/water or DMI/PG concentration ratio of 1:2. In the DMI–PEG mixed system, while there is no apparent interaction between DMI and PEG molecules, the solubility of prednisone was found to increase with decreasing dielectric constant.     

UPLC-MS/PDA检测中药制剂中醋酸泼尼松和醋酸地塞米松的研究

 目的建立快速、准确、高灵敏度的测定中药平喘制剂中醋酸泼尼松和醋酸地塞米松检测的方法。方法采用UPLC-MS/PDA法,以甲醇-0.01mol·L^-1醋酸铵(0.1%甲酸)缓冲溶液梯度洗脱,流速0.2mL·min^-1,离子源为ESI源,正离子检测,对中药制剂中非法添加醋酸泼尼松和醋酸地塞米松进行定性定量分析,并对其裂解途径进行解析。结果6批受试制剂中有2批分别检测到有醋酸泼尼松和醋酸地塞米松。结论此方法选择性强、灵敏度高,可作为分析中药制剂中醋酸泼尼松和醋酸地塞米松的有效检测方法。     

维药无花果叶对抗大鼠泼尼松性骨质疏松的作用研究

目的：研究维药无花果叶醇提物对泼尼松致大鼠骨质疏松的对抗作用。方法：将50只大鼠随机分成正常对照组、泼尼松模型组和维药无花果叶醇提物高、中、低（10mg/kg、20mg/kg、30mg/kg）剂量组，每组10只。分别灌胃相应药物，每日1次，连续8周后取血清检测生化指标，对骨进行组织切片检查，长度、宽度以及骨质的测量。结果：泼尼松模型组大鼠股骨重量、尺骨羟脯氨酸和骨钙含量比正常对照组明显降低，胫骨骨髓腔中脂肪组织增多（P〈0．01），血浆胆固醇（TG）含量上升、碱性磷酸酶（ALP）和高密度脂蛋白（吼）含量下降（P〈0．01）。维药无花果叶醇提组能有效提高骨的重量和骨质的含量（P〈0．01），减少骨髓腔中脂肪的含量，升高碱性磷酸酶和高密度脂蛋白含量（P〈0．01）。结论：泼尼松可抑制大鼠的，肾生长及引起骨丢失，而维药无花果叶醇提物可有良好的对抗作用。     

自制苏芪合剂联合治疗Ⅲ～Ⅳ级IgA肾病的临床疗效观察

目的 探讨自制苏芪合剂对Ⅲ～Ⅳ级IgA肾病患者的疗效及患者T细胞功能的改善.方法 28例Ⅲ～Ⅳ级IgA肾病患者随机分为两组,对照组:醋酸泼尼松-日1mg,kg,隔日晨起顿服,盐酸苯那普利-日10mg;治疗组:在上述用药的基础上加用自制苏芪合剂.8周后,观察患者缓解率、T细胞功能及不良反应.结果 治疗组患者在缓解率、T细胞功能改善等方面优于对照组,且因糖皮质激素的使用而出现的不良反应少于对照组.结论 苏芪合剂联合治疗Ⅲ～Ⅳ级IgA肾病疗效显著并能有效改善T细胞功能.     

重症肌无力患者泼尼松治疗前后免疫学指标的变化

探讨泼尼松治疗重症肌无力（MG）免疫学机制。对382例MG患者在漏尼松中剂量冲击，小剂量维持疗法治疗前后，检测酰胆碱受体抗炎（AchRab)，突触前膜抗体（PsMab)，单个核细胞亚群（PBMC），肿瘤坏死因子（TNF），可溶性白介素－2受体（SIL－2R），β2－微球蛋白（β2－m)，以及红细胞免疫功能的变化。结果表明：MG患者在泼尼松治疗前后多项免疫指标有显著性的变化。为泼尼松治疗MG提供了评定疗效的免疫学指标，进一步阐明了MG发病的免疫学机制。     

流动注射分析法测定醋酸泼尼松片含量均匀度的研究

根据蓝四氮唑与泼尼松生成蓝色产物,并于525nm 波长处测定吸光度。测定条件为:反应管长度为3.8m(0.5mm id);流速为1.6ml/min;反应温度为55±0.5℃;注射样品溶液为100μl;本测定系统的测定速度可达100次/h;线性范围可达0.09mg/ml;检测限量为1.54μg/ml;测定结果的变异系数小于1%。     

Pharmacokinetic interaction of contraceptive steroids with prednisone and prednisolone

Summary The oestrogenic component of oral contraceptives affects the activity of liver enzymes and the concentrations of plasma proteins implicated in steroid metabolism and transport. The present study was designed to determine these effects on the kinetics of prednisone and prednisolone. After an oral dose of prednisone, women on oral contraceptive steroids (n=10) had higher mean (±SD) area under the plasma concentration versus time curves of total (428±67 µg/ml/min vs 188±28 µg/ml/min, p<0.001) and unbound prednisolone (64±10 µg/ml/min vs 41±10 µg/ml/min, p<0.001) than women not taking oral contraceptive steroids (n=10). The differences were attributable to a lower non-renal clearance of prednisolone and to a higher apparent systemic availability of the drug in contraceptive users than in the controls. The affinity of albumin and transcortin for prednisolone was lower in women on oral contraceptives than in controls (p<0.001). Thus, altered kinetics and protein binding may account for the known increase in glucocorticoid efficacy by oestrogens.     

Early splenectomy and polychemotherapy versus polychemotherapy alone in chronic myeloid leukemia

The effect of early splenectomy and of polychemotherapy with hydroxyurea, busulfan, and alternate bimonthly courses of arabinosyl cytosine and vincristine plus prednisone, was evaluated in 139 previously untreated patients with chronic myeloid leukemia (CML), consecutively admitted to 18 hospitals from March 1973 to October 1974. Fifty-six patients were splenectomized and 83 patients were not splenectomized. Splenectomy did not influence the duration of chronic and blastic phase, and did not prolong survival. The prognosis of high risk patients was not improved. During the chronic phase, high platelet counts were more frequent in splenectomy group, and five patients developed thrombotic or thromboembolic complications, 5 to 19 months after the operation. The median survival of the whole group was 50 months, with 32 of 139 patients (actuarial proportion 30%) remaining alive 72 months after diagnosis, but the slope of the survival curve was similar to that of historical controls. The results of this trial suggests that new strategies should be developed for the therapy of CML.     

Plasma protein binding of prednisolone in normal volunteers and arthritic patients

Summary The plasma binding of prednisolone was studied in twenty normal volunteers and twenty rheumatoid arthritis patients. An in vitro assessment of the binding following the addition of prednisolone, prednisone, and hydrocortisone to the plasmas obtained from the subjects showed significant differences in the percentage of prednisolone bound. However, the differences observed were regarded as clinically insignificant. The plasma protein binding was determined by an in vitro equilibrium dialysis of the individual plasma samples at 37° C. Prednisolone levels on both sides of the dialysis membrane were determined using radioactivity and HPLC analytical methodologies. The percentages of prednisolone bound calculated from the analytical results of either the radiochemical or HPLC method were not significantly different. The change in the percentage of prednisolone bound to plasma proteins was studied as a function of the total prednisolone plasma concentration in a normal volunteer and in a systemic lupus erythematosis patient. As a result of prednisolone binding to both transcortin and albumin, the binding of prednisolone changes as a function of prednisolone concentration. The binding data were fitted using nonlinear least squares regression, and the affinity constants for the binding of prednisolone to transcortin and albumin were estimated.     

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