中西医结合治疗重症蝮蛇咬伤26例

目的回顾重症蝮蛇咬伤患者的病历资料,总结重症蝮蛇咬伤的治疗经验。方法对26例重症蝮蛇咬伤患者采用中西医结合疗法进行治疗。西医疗法以局部扩创排毒、注射抗蝮蛇毒血清及对症治疗为主,对危重症患者应用机械通气、血液净化、重症监护等治疗技术;中医疗法以内服院内协定方蛇伤冲剂及采用季德胜蛇药片内服外敷为主。结果治愈22例,好转3例,无效1例,总有效率为96.1%。发生脏器功能损害26例,治疗后恢复25例。住院时间2~16d,平均(7.72±1.35)d。结论中西医结合治疗重症蝮蛇咬伤,治愈率高,脏器功能损害恢复好,住院时间短。     

雪胆素片抗炎镇咳作用的实验研究

目的：对雪胆素片抗炎、镇咳作用进行实验研究。方法：通过观察雪胆素片对小鼠耳廓肿胀、大鼠足趾肿胀的影响研究其抗炎作用;通过小鼠氨水引咳法,观察其镇咳作用。结果：雪胆素片对二甲苯所致的小鼠耳廓肿胀以及角叉菜胶所致的大鼠足趾肿胀有一定的抑制作用;对氨水致咳的小鼠有明显的镇咳作用。结论：雪胆素片具有抗炎、镇咳的作用,为其临床用于治疗支气管炎,急性扁桃体炎等疾患提供了实验依据。     

Effects of long-term estrogen replacement therapy on beta-amyloid precursor protein and mRNA expression in ovariectomized rat hippocampus

BACKGROUND: In vitro cultures of neural stem cells have shown that estrogen can regulate beta-amyloid precursor protein (β-APP) metabolism and reduce amyloid-beta production.OBJECTIVE: To investigate the effects of long-term oral administration of compound nylestriol or low-dose 17beta-estradiol on β-APP and mRNA expression in the hippocampus of ovariectomized (OVX) rats. DESIGN, TIME AND SETTING: This randomized and controlled experiment was performed at the Animal Laboratory and Laboratory of Endocrine and Metabolic Disease, Xiangya Second Hospital of Central South University between April 2003 and May 2004.MATERIALS: According to body mass, 50 six-month-old female Sprague-Dawley rats were randomly divided into five groups (n = 10 per group): normal control, sham operation, OVX model, 17beta-estradiol (Sigma, USA), and compound nylestriol tablet (Laboratory of Endocrine and Metabolic Disease, Xiangya Second Hospital of Central South University) groups.METHODS: Rats in OVX plus 17beta-estradiol and OVX plus compound nylestriol tablet groups underwent ovariectomy. On the second day after surgery, rats were intragastrically given 17beta-estradiol (100 μg/kg), once per day or compound nylestriol tablet (0.5 mg/kg) and levonorgestrel (0.15 mg/kg) every 2 days.MAIN OUTCOME MEASURES: β-APP expression in the hippocampus of OVX rats was determined using immunohistochemistry (SABC method) and β-APP mRNA expression was analyzed by in situ hybridization. The results were quantitatively analyzed using cell counting and average optical density. RESULTS: The number and optical density of β-APP-positive neurons in every subregion of the hippocampus of OVX rats was dramatically increased compared with normal and sham operation groups following 35 weeks of administration (P < 0.05). Levels of β-APP were decreased following oral administration of compound nylestriol or 17beta-estradiol. In situ hybridization showed that long-term estrogen deficiency and oral administration of compound nylestriol or 17beta-estradiol did not alter the number of β-APP mRNA-positive neurons. CONCLUSION: The results show that long-term estrogen deficiency results in an increase of expression of β-APP though no changes in the expression of β-APP mRNA are detected. Replacement of estrogen with low-dose 17 beta-estradiol or compound nylestriol tablet inhibits the expression of β-APP in the hippocampus to the same extent.     

Studies on Formulation and In Vitro Evaluation of Floating Matrix Tablets of Domperidone

Floating matrix tablets of domperidone were developed to prolong gastric residence time and thereby increased drug bioavailability. Domperidone was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by wet granulation technique, using polymers such as hydroxypropylmethylcellulose K4M, carbopol 934P, and sodium alginate, either alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, % friability, floating capacity, weight variation and content uniformity. Further, tablets were evaluated for in vitro release characteristics for 24 h. In vitro release mechanism was evaluated by linear regression analysis. Floating matrix tablets based on combination of three polymers namely; hydroxypropylmethylcellulose K4M, carbopol 934P and sodium alginate exhibited desired floating and prolonged drug release for 24 h. Carbopol loading showed negative effect on floating properties but were found helpful to control the release rate of drug.     

The effect of chemical heterogeneity of HPMC on polymer release from matrix tablets

Polymer release from hydrophilic matrix tablets, composed of hydroxypropyl methylcellulose, was studied for seven different polymer batches. A time difference of more than 80 h between fully dissolved tablets was noticed although the batches were of the same pharmaceutical substituent (USP 2208) and viscosity (100 cps) grade. To find the functionality related parameters for polymer release from hydrophilic matrix tablets the polymer samples were characterised according to size and chemical composition. The size of the polymers was characterised by size-exclusion chromatography with multi-angle light scattering and refractive index detection. The average amount of substituents was measured with nuclear magnetic resonance and the distribution of the substituents along the cellulose chain was determined with high-performance anion-exchange chromatography with pulsed amperometric detection after acid and enzymatic hydrolysis. The results indicated that other types of interactions apart from entanglements were present between the polymer chains, which seemed to affect the polymer release. Most importantly, this study has shown a correlation between the polymer release and the substituent pattern, where the samples with slow release also were more heterogeneously substituted along the polymer chain. From this we can conclude that polymer release is very sensitive to alterations in chemical composition.     

马来酸依那普利片的人体生物等效性研究

目的考察两种马来酸依那普利片的相对生物利用度,评价两者的生物等效性。方法采用双周期自身随机交叉试验设计。20名健康男性志愿者单剂量口服受试制剂或参比制剂,血药浓度采用高效液相色谱-串联质谱测定。结果受试制剂及参比制剂马来酸依那普利实测平均血药峰浓度Cmax分别为（32.74±9.01）、（35.48±11.44）μg.L-1;实测平均达峰时间Tmax分别为（0.76±0.17）、（0.87±0.17）h;受试制剂及参比制剂t1/2分别为（2.52±2.95）、（3.10±5.79）h;AUC（0-48h）平均值分别为（59.22±20.46）、（64.43±23.42）mg·h·L-1;AUC（0-∞）平均值分别为（60.01±20.39）、（65.09±23.43）mg·h·L-1;以AUC计算,受试制剂的相对生物利用度为（97.8±34.1）%。结论受试制剂和参比制剂具有生物等效性。     

5个企业枸橼酸他莫昔芬片的体外溶出度考察

目的对国内5个企业枸橼酸他莫昔芬片进行体外溶出度考察,为临床合理用药提供依据。方法以紫外分光光度法测定含量,浆法测定溶出度。利用Excel软件的VBA编写宏命令,在计算机上快速算出枸橼酸他莫昔芬片的累积溶出百分率和溶出参数,并对各组之间的溶出参数进行方差分析。结果所测产品的体外溶出均达到中国药典规定的30min溶出应大于标示量75%的要求,但各企业枸橼酸他莫昔芬片的溶出参数（m、t50、td、t80）间存在着高度显著性差异（P〈0.01）。结论不同企业枸橼酸他莫昔芬片的溶出参数存在着显著差异,临床用药时应加以注意。     

高效液相色谱法测定排毒清脂片中大黄素、大黄酚的含量

目的：建立高效液相色谱法（HPLC）测定排毒清脂片中的大黄素、大黄酚的含量。方法：色谱柱：UItimate XB－C18柱（250mm×4.6mm,5?滋m）;流动相：甲醇－磷酸溶液（85∶15）;流速：1mL·min-1;检测波长：254nm。结果：大黄素、大黄酚分离良好,进样量分别在0.007984~0.047904?滋g和0.01002~0.06012?滋g范围内与峰面积是良好线性关系,r值分别为0.9991和0.9998,平均回收率分别为99.18%和99.94%,RSD分别为1.19%和1.16%（n=5）。结论：该方法简便、精确、分离效果好、专属性强,可作为排毒清脂片中大黄成分的质量控制方法。     

护肝宁片、葡醛内酯片治疗药源性肝损伤

目的：评价护肝宁片与葡醛内酯片治疗药源性肝损伤的疗效。方法：将77例药源性肝损伤患者随机分成护肝宁组39例，葡醛内酯组38例，分别给予护肝宁片及葡醛酯片治疗8周，观察第4周末及第8周末ALT、GGT。结果：第4周末ALT、GGT两组恢复正常率比较，差异有统计学意义（P〈0.105），第八周末比较，差异无统计学意义（P〉0．05）。结论：护肝宁片、葡醛内酯片治疗药源性肝损害均有效，而护肝宁片起效更快、疗程更短，值得临床上推广应用。     

高效液相色谱法测定犬血浆中人参皂苷Rgl的浓度

目的：建立测定驯服家犬血浆中血塞通分散片的主要成分人参皂苷Rg1的高效液相色谱方法。方法：血浆样品采用蛋白沉淀法，以纯化水-乙腈为流动相，经ZORBAX Edipse XDB-C8色谱柱分离，在203nm波长检测。结果：Rg1质量浓度在2．58～51．6mg·L^-1范围内线性关系良好，最低检测质量浓度为2．58mg·L^-1。低、中、高3个质量浓度的提取回收率大于85％。日内、日间相对标准偏差低于10％。结论：本方法准确、快速，可满足临床药动学研究的要求。