复方盐酸右旋麻黄碱缓释片生物利用度的研究

应用反相ＨＰＬＣ法研究了复方盐酸右旋麻黄碱缓释片在兔体内动力学变化过程，并以自制普通片为对照，实验数据按单室模型采用非线性最小二乘法模型嵌合程序进行迭代处理。结果表明缓释片维持体内有效血药浓度时间长，其相对生物利用度为１２２．４８％，理论值与实测值基本相符（Ｐ＞０．０５）。     

Optimization of a formulation for direct compression using a simplex lattice design

In this paper it is demonstrated how the optimum composition of a mixture for direct compression consisting of -lactose monohydrate, roller-dried -lactose and microcrystalline cellulose can be found using a systematic optimization technique. The experiments were chosen according to a simplex lattice design. The results of these experiments were used to fit a mathematical model, which then can predict the properties of all possible mixture compositions and enables a graphic representation of these properties in the form of contour plots. At a level of 4% the effect of three disintegrants (sodium starch glycolate, croscarmellose sodium and crospovidone) on the properties of the tablets compressed from these filler-binders, was evaluated by superimposing the contour plots of the different tablet responses. It was found that all the disintegrants used were effective in this combination of filler-binders. In order to evaluate drug dissolution rate an extra experiment with crospovidone as the disintegrant was performed, in which oxazepam was used as a test drug.     

Studies on tableting properties of lactose

The consolidation and compaction behaviour of sieve fractions of crystalline -lactose monohydrate were studied. From mercury porosimetry measurements tablet pore surface areas were derived. At a certain compaction load it appeared that tablets compressed from small particles were generally stronger and showed a larger surface area than compacts prepared from coarse sieve fractions. By plotting compact strength against pore surface area, a unique linear relationship was obtained. From these results it can be concluded that the actual tablet surface area, being a function of both the initial particle size and applied compaction pressure, is responsible for the compact strength.     

5-氨基水杨酸缓释骨架片的研制

目的 :制备 5_氨基水杨酸缓释骨架片。方法 :采用羟丙基甲基纤维素作为骨架材料 ,湿法制粒压片制备 ,并考察体外释药情况。结果 :5_氨基水杨酸缓释骨架片体外释药符合Higuchi方程。结论 :5_氨基水杨酸缓释骨架片具有显著的缓释效果。     

指纹图谱结合一测多评在中成药丹参片质量控制中的应用

目的:采用指纹图谱结合一测多评法(QAMS)评价中成药丹参片的质量。方法:以丹参酮ⅡA为参照物建立丹参片醌类成分的高效液相色谱法(HPLC)指纹图谱。同时,测定丹参酮ⅡA与隐丹参酮、丹参酮Ⅰ的相对校正因子,以QAMS测定丹参片中丹参酮Ⅱ_A、隐丹参酮、丹参酮Ⅰ的含量。结果:建立了丹参片HPLC指纹图谱,并指认了全部5个共有峰,12批丹参片的相似度均大于0.99;QAMS测定了丹参片中3个醌类成分的含量,样品间存在一定波动性。结论:指纹图谱与QAMS结合的质量控制模式准确可靠,可为全面合理评价丹参片的质量提供参考。     

Preparation and evaluation of sodium diclofenac controlled-release tablets

The dissolution behaviour of a direct compression compact prepared with sodium diclofenac and dibasic calcium phosphate (DCP) in different weight ratios with or without Biosoluble polymer^® (acrylic-based resin) was investigated in distilled water and in a medium with changing pH. The results indicate that the amount of sodium diclofenac released from the compact was dependent on the amount of drug and DCP used in the compact, and was also controlled by the amount of Biosoluble polymer^® added. A chemical reaction forming diclofenac acid might occur on the surface of the sodium diclofenac compact during exposure to the acidic medium, which was confirmed by diffuse-reflectance spectroscopy. The tablet with a 12 weight ratio of sodium diclofenac to DCP exhibited a sustained-release behaviour, similar to commercial sustained-release products (Voltaren SR-100^® and Grofenac Retard^®), but a lower release rate was found as compared to the commercial products. The dissolution behaviour of the study tablet and the commercial products was found to be dependent on the dissolution medium and the rotating speeds. Glass beads were added to the dissolution assembly to simulate the influence of food, and the enhanced friction between tablet and glass beads might result in a higher dissolution rate of the tablet and the commercial products.     

Administration of obidoxime tablets to man

Twenty-four male volunteers were given obidoxime tablets in quantities ranging from 1.84–3.58 g in a single dose, or 7.36 g divided into 4 equal doses. With the lowest dose, average peak plasma level of the drug was 1.9 g/ml and after the highest single dose it was 5.6 g/ml, both attained 1.5 h after administration. In the multiple-dosed individuals, plasma levels of the oxime increased gradually following each additional dose, reaching a peak of 3.5 g/ml after the last dose.Thirteen individuals complained of one or more of the following side effects: pallor, nausea, pyrosis, headache, generalized weakness, sore throat, and paresthesia of the face muscles.Activities of blood cholinesterase, glutamic oxalacetic transaminase, glutamic pyruvic transaminase, as well as hematocrit values, heart rate, and blood pressure were not affected.It is postulated that due to the undesirable side effects, the general use of obidoxime tablets should not be recommended. However, prophylactic oral treatment with obidoxime could be considered for persons at high risk of organophosphate poisoning or when parenteral administration might not be feasible.     

清火解毒片的药效学研究

目的：考察清火解毒片的药理作用。方法：采用体内外抑菌法、毛细血管通透性法、鼠耳肿胀法、发热反应法、氨雾致咳法、醋酸刺激扭体法。结果：该药对常见的呼吸道感染小鼠有保护作用趋势；对醋酸所致小鼠腹腔毛细血管通透性亢进有明显抑制作用，但对巴豆油所致的小鼠耳肿胀的抑制作用不明显；对2，4-二硝基苯酚致热大鼠的解热作用也不明显；能明显延长氨雾诱发小鼠咳嗽反应潜伏期、减少咳嗽次数；还能明显抑制醋酸所致小鼠的扭体反应。结论：该药具有一定的抗菌、抗炎、镇咳、镇痛作用。     

藏药晶珠虫草含片质量标准研究

目的：建立晶珠虫草含片（冬虫夏草，红景天、黄芪、青果、人参、麦冬等）的质量标准。方法：采用TLC法对处方中人参、麦冬进行鉴别；用薄层描法测定黄芪甲苷的含量。结果：在TLC色薄中检出人参、麦冬；黄芪甲苷在0．5－2．5uL范围内呈良好的线性关系，r=0.9999,平均回收率98％。RSD为1．35。结论：所建立的方法简单可行，重现性好，为晶珠虫草含片质量控制提供了方法。     

养阴降糖片质量标准研究

目的：建立养阴降糖片(黄芪，牡丹皮，虎杖，葛根等)的质量标准。方法：用TLC法对黄芪、牡丹皮、虎杖、葛根进行了鉴别；用HPLC法测定葛根素的含量。结果：在TLC色谱中检出黄芪、牡丹皮、虎杖、葛根。葛根素在10．0--60．0μg范围内呈良好的线性关系；r=0．9996，平均回收率99．6％，RSD为1．52％。结论：所建立的方法简便可行，重现性好，为养阴降糖片质量控制提供了方法。