盐酸去氢骆驼蓬碱微球体外释药特性研究

目的：探讨盐酸去氢骆驼蓬碱明胶微球(HM—GMS)的体外释药规律．初步阐明其释药机理。方法：分别考察不同体外释放实验方法、不同释放介质、释放介质的不同流速对HM—GMS释药的影响．并用适当的数学模型表达HM—GMS的释药规律。结果：HM—GMS在蒸馏水中释药最快，在不同pH磷酸盐缓冲液中，HM—GMS的释药速度无明显变化，在生理盐水中释药平稳。释放介质的流速对HM—GMS的释药有影响，流速越快、释药越快。选用流室法，并以生理盐水为释放介质，控制流速为9m1／h的条件测定HM—GMS的累积释药百分率。HM—GMS体外释药规律可用Ritger—peppas方程表示。结论：所制微球具有一定的缓释特性。     

盐酸去氢骆驼蓬碱肝动脉栓塞微球处方工艺研究

目的:从新疆民族药蒺藜科植物骆驼蓬种子中提取的抗肿瘤活性生物碱成分——盐酸去氢骆驼蓬碱(HM) ,制成可供肝动脉栓塞的微球新剂型 ,对其处方设计及制备工艺进行研究。方法:选择具有生物可降解性、无毒、价廉且与盐酸 HM无相互作用的明胶为载体 ,采用乳化分散法制备盐酸去氢骆驼蓬碱明胶微球 ,以外观、粒径、载药量、包封率等为考察指标 ,采用正交设计确定了盐酸去氢骆驼蓬碱微球的制备工艺。结果:含药微球为淡黄色粉末 ,光镜及电镜观察微球球形圆整 ,表面附有少量药物结晶。平均产率为 86 .6 3% ,表面药量平均值为 (2 6 .2 4±0 .30 ) % (g/ g) ;载药量为 (34.4 5± 0 .35 ) % (g/ g) ;包封率为 (8.19± 0 .5 1) % (g/ g)。平均算术径为 6 3.0μm ,平均体积径为 6 9.6μm,粒径分布基本属正态 ,跨度 Span为 0 .76 9。 结论:所研制微球符合肝动脉栓塞微球剂的要求     

骆驼蓬有效成分两种给药途径的毒性比较研究

目的:开展骆驼蓬有效成分骆驼蓬碱、去氢骆驼蓬碱两种给药途径的小鼠急性毒性比较研究。方法:采用Bliss法测定小鼠经口灌胃和静脉注射给药骆驼蓬碱、去氢骆驼蓬碱的LD_(50),同时观察小鼠中毒症状及中毒反应的起止时间。结果:骆驼蓬碱经口灌胃的LD_(50)及其95%可信区间为118.9 mg/kg(105.8~133.9 mg/kg),静脉注射的LD_(50)及其95%可信区间为80.3 mg/kg(60.6~146.1 mg/kg);去氢骆驼蓬碱经口灌胃的LD_(50)及其95%可信区间为250.3 mg/kg(210.0~293.3 mg/kg),静脉注射的LD_(50)及其95%可信区间为74.1 mg/kg(67.2~83.1 mg/kg)。小鼠经口灌胃给药时,骆驼蓬碱小鼠死亡时间早于去氢骆驼蓬碱小鼠死亡时间;小鼠静脉注射给药时,去氢骆驼蓬碱小鼠死亡时间早于骆驼蓬碱小鼠死亡时间。结论:小鼠经口灌胃给药骆驼蓬碱毒性去氢骆驼蓬碱毒性,小鼠静脉注射给药去氢骆驼蓬碱毒性骆驼蓬碱毒性。     

MTT法测定HM与HCPT细胞毒作用的体外研究

目的:通过去氢骆驼蓬碱 (HM)微球与羟基喜树碱 (HCPT)注射液对大鼠正常肝细胞 (BRL )的毒性作用的比较研究 ,为 HM的临床应用提供佐证。方法:采用 MTT法测试一定浓度范围内 HM与 HCPT对大鼠正常肝细胞 (BRL)的细胞毒作用大小。 结果 :在一定浓度范围内 ,HM与 HCPT的细胞毒作用与药物浓度均呈线性关系 ;针对 BRL 细胞 ,在一定的浓度范围内 HM的细胞毒作用较 HCPT注射液的细胞毒作用为小 ,经检验差别有统计学意义 (P <0 .0 1)。结论:MTT法操作简单、快速、敏感 ,是较好的体外实验方法之一。HM微球新剂型对 BRL的毒性作用小于 HCPT注射液 ,体外实验表明其毒副作用小 ,结合其剂型的靶向性、缓释性、栓塞性等特点 ,有潜在的临床应用价值     

骆驼蓬提取物、去氢骆驼蓬碱和骆驼蓬碱抗人低密度脂蛋白氧化的作用

骆驼蓬Peganum harmala L.的主要成分为生物碱。作者研究了该植物种子甲醇提取物及其主要成分去氢骆驼蓬碱和骆驼蓬碱体外对Cu2 诱导的低密度脂蛋白(LDL)氧化变性的抑制作用及对自由基的清除能力。将新鲜的骆驼蓬种子在甲醇-水溶液(40∶60)中浸泡过夜,得到的提取物冻干、浓缩。去氢骆驼蓬碱和骆驼蓬碱从该提取物中分离与精制。收集12位年龄在20~25岁的健康志愿者的血浆,制备LDL。将CuSO4和LDL一起培养育进行Cu2 介导的LDL氧化反应,再分别加入不同质量浓度(0、50、100、200μg/mL)的骆驼蓬提取物及10μmol/L去氢骆驼蓬碱或骆驼蓬碱…     

去氢骆驼蓬碱对小鼠免疫功能的影响

去氢骆驼蓬碱是蒺藜科植物骆驼蓬种子中提出的一种生物碱,我们研究了去氢骆驼蓬碱的免疫药理作用,简报如下。在整体实验中,我们所用去氢骆驼蓬碱的剂量分别为16mg/kg bw、25mg/kg bw,小鼠皮下给药,给药时间7天。研究结果表明:去氢骆驼蓬碱可使小鼠胸腺、脾重量减轻;小鼠免疫特异性玫瑰花形成细胞、空斑形成细胞和溶血素的形成也减少,p<0.01。     

天然产物去氢骆驼蓬碱糖基偶联物的合成及抗肿瘤活性评价

基于本课题组前期工作基础,在天然产物去氢骆驼蓬碱(harmine)的C⁷位氧上引入环己基甲基,并在N⁹位上通过不同长度的烷基链偶联甲基2-氨基-β-D-葡萄糖苷,设计并合成了8个去氢骆驼蓬碱糖基偶联物(14a～14h)。体外抗肿瘤活性筛选和构效关系研究发现,偶联物的抗肿瘤活性随连接臂中烷基链长度的延长而增加。化合物14h对MDA-MB-231乳腺癌细胞的增殖抑制活性显著优于去氢骆驼蓬碱。与去氢骆驼蓬碱相比,糖基的引入改善了化合物14h的水溶性,并通过Warburg效应提高了化合物14h的肿瘤细胞选择性。机制研究发现化合物14h可诱导MDA-MB-231细胞凋亡和G₀/G₁期细胞阻滞,并能通过干扰细胞上皮-间充质转化进程抑制肿瘤细胞迁移。本研究为基于去氢骆驼蓬碱的抗肿瘤药物的开发提供了新思路。     

用差热分析法求固体苯唑青霉素钠热降解动力学参数

本文报道用差热分析法(DTA)、以氮或空气为气氛,研究固体青霉素钠的热降解反应,按Kissinger(1956)法计算该反应的活化能(E=59.7kcal/mol)、反应级数(n=1)及频率因子(A=7.4×10~(25)/s)。用DTA求固体药物热降解动力学参数甚为简便,可在较短时间内取得有价值的资料,而且重复性良好,是研究固体药物稳定性的有效实验手段。     

复方左旋18-甲基炔诺酮微球的研究

左旋18-甲基炔诺酮(LNG)与雌二醇(E_2)按5:2重量比配伍,以天然可生物降解的明胶为材料,用相分离法制备了复方左旋18-甲基炔诺酮微球,平均球径为10～40μm,包封率达65％～75％。制成注射液后,经加速与室温观察具有一定的物理化学稳定性,其热解活化能为134.4KJ/mol,体外溶出试验与不包球的注射液相比,T_(1/2)有极显著性差异(P<0.01),说明制成微球后具有明显的缓释作用。经复方与单方的微球注射液组织学对比观察,复方可减轻小鼠卵巢充血的副作用,提示临床应用复方时,LNG引起不规则出血等副作用有可能得以改善。     

载钯量对轻质烷烃异构化催化剂(Pd/HM)性能的影响

采用MR-GC80型压力微反装置,在空速2h~(-1)、氢油分子比8:1、氢压2MPa、反应温度260℃和280℃反应条件下,考察了钯/氢型丝光沸石(Pd/HM)催化剂的含钯量对正己烷异构化反应活性,选择性,稳定性的影响,并结合脉冲激反装置对反应机理进行了探讨。结果表明:钯含量在0.025—0.25%范围内,活性和选择性均随含钯量的增加而提高;超过0.85%,则呈下降趋势;HM载钯后稳定性有明显的改善。催速失活试验表明:0.25%Pd/HM和0.5% Pd/HM催化剂具有相同的稳定性。在Pd/HM上正己烷异构化反应的机理为酸性和双功能结合的复合机理。     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Dr.Zhang Ren''''s Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

Luo Lingjie''''s Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.     

Acupuncture Treatment of Vomiting

CASE HISTORY A female patient, 46 years old, head of the foreign affairs department of a certain university in Beijing, paid her first visit on October 9, 2006, with the chief complaint of vomiting for one month. She got vomiting after meals in early September. Before that, she had discomfortable sensation in the stomach due to angry with others, but she didn't pay much attention. Later, it developed into vomiting after eating. After the vomiting, the discomfort would be relieved, but with slight hypodynamia. She was once diagnosed as having 'neurogenic vomiting'. Having taken some western and Chinese drugs, the above symptoms were a little bit improved, but she would have nausea upon eating and with regurgitation. Because of the fear for vomiting, she did not dare to have food intake, with body weight reduction of 6 kilos in one month.     

Qiu Baoguo''''s Experience in Treating Consumptive Syndromes after Radio-Chemotherapies

Radiotherapy and chemotherapy are the important modern medical therapies for malignant tumors,yet they can also bring about serious local and systemic toxic side reactions so to decrease the patient;'s life quality,manifested by a series of consumptive symptoms.Having engaged in the combined work of Chinese and western medicine for nearly 50 years,the research fellow Qiu Baoguo in Henan Provincial Academy of TCM has developed his unique views on the TCM study of consumptive syndromes.The author of this essay had once the fortune tO follow Dr.Qiu in clinic,and specially would like to introduce in the following Dr.Qiu's experience in treating consumptive syndromes after radio-chemotherapies for patients with malignant tumor.     

Insomnia Due to Deficiency of Both the Heart and Spleen Treated by Acupuncture-Moxibustion and Chinese Tuina

OBJECTIVE: To observe therapeutic effects of the comprehensive therapy of acupuncture-moxibustion and Chinese Tuina for treatment of insomnia due to deficiency of both the heart and spleen. METHODS: 92 cases were divided randomly into the treatment group (treated by acupuncture-moxibustion and Chinese Tuina) and the control group (treated by acupuncture-moxibustion). RESULTS: The therapeutic effect of the treatment group was obviously superior to that of the control group (the CHI2 test showed P < 0.01). CONCLUSIONS: The comprehensive therapy of acupuncture-moxibustion and Chinese Tuina can give marked therapeutic effects for treatment of insomnia due to deficiency of both the heart and spleen.     

Survey and practice of reporting quality of randomized controlled clinical trials on traditional Chinese medicine

Evidence obtained from randomized controlled trials （RCTs） has been generally accepted as the gold standard in the evaluation of clinical effectiveness. Readers need to understand the trial design, implementation, results, analysis and interpretation, so as to fully Jnderstand the results of RCTs. Thus, the investigators of RCTs have to report these items in a complete, accurate and clear manner. Since 1998, we have conducted several evaluations on the reporting quality of RCTs published in Chinese journals on traditional Chinese medicine （TCM） and results have shown that there is an urgent need for higher quality RCTs on TCM.