低分子肝素前体脂质体制剂的研究

目的：探讨用前体脂质体法制备LMWH脂质体制剂的影响因素及质量评定。方法：以包封率为指标,用正交设计试验法研究由前体脂质成含药脂质体过程中的影响因素,并以包封率、形态、粒度、分布评估了制剂的质量,以动物试验考察了制剂的缓释性。结果：影响因素作用的大小顺序为：甘露醇用量＞类酯配比＞药物浓度＞十八胺用量,最佳工艺制剂包封率为37．3％,在电镜下为圆形或椭圆形,90％颗粒粒径小于1．2μm,动物试验表明,该制剂体内可维持8h的药物作用。结论：前体脂质体法制脂质体制剂有较高的包封率、良好的粒度分布及一定的缓释性。     

正交试验优选黄芩素长循环脂质体制备工艺研究

目的:研究黄芩素长循环脂质体的处方和制备工艺.方法:采用逆相蒸发法制备脂质体.以HPLC法测定脂质体中黄芩素的含量,计算包封率和载药量,采用单因素和正交试验法优化黄芩素长循环的处方和制备工艺.结果:优化后的黄芩素长循环脂质体平均包封率为81.42％,平均载药量32.25％,粒度分布均匀.结论:脂质体制备工艺合理,HPLC法测定脂质体包封率准确性高,重现性好,制剂学性质稳定.     

肉苁蓉总苷前体脂质体的研制

目的探讨肉苁蓉总苷前体脂质体的各项理化性质及水溶性天然药物提取物制成前体脂质体的可行性。方法采用新型前体脂质体制备技术,将水溶性药物肉苁蓉总苷制成肉苁蓉总苷前体脂质体;采用透射电镜观察形成的脂质体形态;采用粒径测定仪测定脂质体粒径;采用葡聚糖凝胶柱洗脱法测定脂质体包封率。结果电镜下脂质体呈球形,外层隐约可见有多层。脂质体粒径小,粒度分布均匀,脂质体稀释倍数越大,粒径越小,ξ电位在-21.05mV,包封率值为(24.98±0.76)%。结论新型前体脂质体制备技术可将水溶性天然药物提取物肉苁蓉总苷包封在脂质体内,初步说明前体脂质体制备具有可行性。     

葛根素前体脂质体的制备及体外性质研究

目的 制备葛根素前体脂质体,并对其体外性质进行研究.方法 采用载体沉积法制备葛根素前体脂质体,单因素考察和正交实验优选处方;透射电镜观察形态;马尔文激光粒度仪测定粒径、Zeta电位;透析法结合高效液相色谱法测定包封率;动态透析法考察体外释药性质.结果 制得的脂质体形态多为圆形或椭圆形,平均粒径为278 nm,Zeta电位为-17.5 mV,包封率为(43.53±1.33)%,体外释药符合一级动力学方程.结论 葛根素前体脂质体包封率较高,具有一定的缓释效果.     

四种前体脂质体制剂的包封率比较及小肠吸收研究

目的:采用一种新型前体脂质体制备方法将4种不同极性的药物分别制成前体脂质体,考察此种制备方法对不同药物的适用性。方法:比较齐墩果酸、水飞蓟素、替加氟、肉苁蓉总苷4种前体脂质体制剂水合后所形成脂质体的包封率,选用齐墩果酸前体脂质体、水飞蓟素前体脂质体水合后进行离体小肠吸收实验,以考察所形成脂质体的吸收情况,从而对体内吸收情况进行预测。结果:4种前体脂质体制剂中,包封率为齐墩果酸>水飞蓟素>替加氟>肉苁蓉总苷;离体小肠吸收实验结果显示:齐墩果酸脂质体、水飞蓟素脂质体与其对照溶液相比,药时曲线下面积增大。结论:前体脂质体制备方法尤其适用于弱极性药物如齐墩果酸,制成的脂质体制剂与对照相比,明显促进了药物的吸收。     

双氯芬酸钾脂质体制剂的制备及大鼠体外透皮研究

目的　研究双氯芬酸钾 (DP)脂质体制剂的制备及体外的经皮吸收特点。方法　采用改良均质法制备DP钾脂质体制剂 ;采用改良Franz扩散池 ,研究DP脂质体制剂与上市凝胶制剂大鼠皮肤的体外透皮吸收差异。结果　改良均质法制备的DP脂质体 ,平均粒径为 3 45nm ,粒径分布比较均匀 ,包封率为 87 3 %。体外透皮实验中 ,DP脂质体制剂较凝胶制剂的透皮能力高 (P <0 0 5 )。结论　脂质体包封的双氯芬酸钾制剂质地均一 ,稳定 ,能有效地渗透过皮肤     

维生素A前体脂质体的研制及其特性考察

目的：研究维生素A前体脂质体，提高维生素A的稳定性。方法：采用冷冻干燥法，选择甘露醇做冻干剂制备维生素A前体脂质体，并考察维生素A脂质体的形态、粒径分布、包封率和稳定性。结果：维生素A前体脂质体经水合后呈单室脂质体，脂质体粒径分布均匀，平均粒径0．615μm，药物包封率为98．5％。在40℃贮存3个月，脂质体形成、粒径及包封率无明显变化。结论：前体脂质体能明显提高维生素A稳定性。     

对氧磷酶长循环脂质体的制备及评价

 目的研制对氧磷酶长循环脂质体。方法采用薄膜分散法制备对氧磷酶长循环脂质体,采用凝胶柱法测定包封率,以包封率为指标,分别考察药脂比、胆固醇用量、聚乙二醇-胆固醇用量、离子强度等对脂质体的影响,在此基础上用正交设计对处方进行优化。结果经薄膜分散法制得的脂质体包封率为(87.66±3.46)%,平均粒径为126nm左右,粒度分布均匀,呈单峰分布,电镜结果显示外形圆整,分散性较好。4℃放置15d包封率无明显变化,酶活性基本稳定。结论聚乙二醇修饰的对氧磷酶长循环脂质体制备工艺简单可行,对氧磷酶长循环脂质体制剂学、酶学性质稳定。     

采用溶剂分散和挤压器联动装置制备阿霉素脂质体的稳定性研究

目的:考察溶剂分散和挤压器联动装置制备阿霉素脂质体制剂的稳定性.方法:使用联动装置制备空白脂质体,联动装置将阿霉素采用pH梯度法载药于空白脂质体中,评价其在体外不同影响因素下的制剂稳定性.测定了阿霉素脂质体理化性质,用透析法检测阿霉素脂质体的药物包封率,用HPLC考察阿霉素脂质体在大鼠体内药代动力学行为.结果:该联动装置可使脂质体的制备工艺简化,投料成品一步完成,同时可在线监控粒径,采用此装置制备的脂质体阿霉素的粒径为(98±9 nm),药物包封率为98.3%.结论:溶剂分散和挤压器联动装置可用于工业化生产阿霉素脂质体制剂,设备实用性强,产品质量可控性好.     

均匀设计法制备5-氟尿嘧啶脂质体及其稳定性

目的:寻找制备5-氟尿嘧啶(5-FU)脂质体最佳处方.减少试验次数,降低试验成本.方法:将数学中的均匀设计法应用到5-FU脂质体制剂的处方筛选中.结果:根据均匀设计法优化处方制得的5-FU脂质体包封率可达39.21%,脂质体的粒径均匀,外观好,所包封的药物5-FU稳定性好,膜材磷脂的酸值和过氧化值的变化小,脂质体的稳定性得到了提高.结论:均匀设计法简便、试验次数少、适用范围广,适合于制剂的处方筛选.     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

The comparative studies of the influences of Urapidil and Nicardipine on sino-atrial node function, atrio-ventricular node function and hemodynamics

Objective:To investigate the influences of urapidil and nicardipine on rabbit sinus function,atrio-ventricular node function and hemodynamics.Methods:Thirty-two Angora's rabbits were selected and randomly divided into four groups.U1 group:urapidil 0.25 mg/kg;U2 group:urapidil 0.5 mg/kg;N1 group:nicardipine 10 μg/kg;N2 group:nicardipine 20 μg/kg.All these medicine were administrated within 30 seconds.Measurements were taken before and after the administration of urapidil or nicardipine for the following data:mean blood pressure(MAP),heart rate(HR),sino-atrial conduction time(SACT),maximal sinoatrial recovery time(SNRTmax)corrected sinus node recovery time(CSNRT),index of sinus node recovery time(SNRTI),Wenckebach A-V conduction frequency (WB),and P-R interval.Results:Significant MAP and HR changes were identified in all of the four groups before and after administration of both urapidil and nicardipine.No significant changes could be found in the rest of the parameters.Intergroup analysis showed that SACT and CSNRT of N1 and N2 groups were shorter than those of the U2 group(P＜0.01);the MAP decreased(P＜0.01)and the HR increased drastically(P＜0.01).Conclusions:Neither urapidil(0.25 mg/kg,0.5 mg/kg)nor nicardipine(10μg/kg,20μg/kg)has any significant influence on rabbit sinus function or rabbit atrio-ventricular node function.Nicardipine could be a better choice than urapidil for parafunctional sinus node patients.     

Expression of OPGmRNA and ODFmRNA in the patients of hip fracture due to osteoporosis

Objective：To investigate the gene expression of osteoprotegerin（OPG） and osteoclast differentiation factor（ODF） in the bone tissue of patients with hip fracture due to osteoporosis. Methods：OPGmRNA and ODFmRNA in the bone tissue in 50 cases of osteoporosis sufferers（over 50 years old） with hip fracture（Observer Group） and 30 cases of hip facture sufferers with no osteoporosis（Control group） were analyzed with the Semi-Quantitative RT-PCR method. Results：The mRNA expressed of ODF, OPG were both high in the patients with hip fracture. In the control group, the expression of OPG mRNA was observed, while the expression of ODF mRNA was very slight. Conclusion：Aged patients contained all signals including OPG, ODF that are essential for inducing osteoclastogenesis and promoting bone resorption.     

The clinicopathological and immuohistochemical analysis of solid-pseudopapillary tumor of the pancreas： report of 9 cases

Objective：To investigate the clinical features, pathological characteristics and immunophenotype of solid-pseudopapillary tumor of the pancreas（SPTP）. Methods：Nine surgically treated cases of SPTP were retrospectively reviewed. Hematoxylin and Eosin（HE） staining and immunohistochemical staining were used to analyze all cases, and the general clinical data was collected. Results：Six patients were asymptomatic except for a palpable mass. Two patients complained of vague-epigastric pain. One patient appeared jaundice. The tumor was encapsulated and solid tissues alternately with cystic tissues. Histologically, the histological structure of solid portion was pseudopapillary with a fibrovascular core. Tumor cells were uniform and medium-sized which were arranged in sheets ets or nests or pseudopapillary patterns. Immunohistochemical studies demonstrated that SPTP proved positive in vimentin（9/9 cases）, AAT（9/9 cases）, NSE（9/9 cases）, ACT（7/9 cases）, CK20（2/9 cases）, CgA（1/9 cases）, S-100（3/gcases）, PR（4/gcases）, Syn（3/9 cases） and CD56（5/9cases）, negative in CEA and ER. Conclusion：SPTP is a tumor predominantly occurring in young women frequently without special symptoms. This tumor has various characteristical histological patterns with different immunophenotype.     

Electro-Acupuncture Combined with the Trigger Point Needle-Embedding for Treatment of Primary Trigeminal Neuralgia in 31 Cases

In recent years, the author of this essay has applied electro-acupuncture combined with the trigger point needle-embedding for treatment of primary trigeminal neuralgia in 31 cases, yielding satis- factory results as reported in the following.     

Investigation of Matrix Metalloproteinase -1, 2 and tissue inhibitor of matrix metalloproteinases-1 in Endometriosis

Objective： To explore the role of matrix metalloproteinase-1,2 （MMP-1, MMP-2） and tissue inhibitor of matrix metalloproteinases-1 （TIMP-1） in endometriosis. Methods： The eutopic and ectopic endometria from 40 subjects suffering from endometriosis and regular.endometria from 40 subjects （excluding endometriosis） were collected and examined by in situ hybridization technology and western blot assay. Results： Both expressions of MMP-1 and -2 were stronger in ectopic endometrium and eutopic endometrium than in normal endometrium. On the contrary, the expression of TIMP-1 in ectopic endometrium and eutopic endometrium was lower. The differences were significant （P 〈 0.01 ）. Moreover, there was no relationship among the expressions of MMP-1, 2 and TIMP-1 in ectopic endometrium. Conclusion： The expressions of MMP-1, 2 and TIMP-1 lose balance and lack of periodic changes in ectopic endometrium , which explains the biological invasive behavior of endometriosis. It was suggested-that regulating the balance between the MMPs and TIMP-1 should be an ideal therapeutic target to endometriosis.     

Shi Da-zhuo (史大卓) —An outstanding cardiologist of integrative medicine

Prof. SHI Da-zhuo, Ph.D., male, was born on March 20, 1960. Prof. SHI entered the Ph.D. program in 1990 at the China Academy of Chinese Medical Sciences under the supervision of Prof. CHEN Ke-ji, majoring in the treatment of cardiovascular diseases. After receiving his Ph.D. degree in 1993, Prof. SHI started working at the Cardiovascular Center in Xiyuan Hospital affiliated to China Academy of Chinese Medical sciences.     

Persist in and Carry Forward the Integrative Medical Research——Speech at the 6th National General Congress of Chinese Association of Integrative Medicine by Academician CHEN Zhu,Minister of Ministry of Health

The 6th National General Congress of Chinese Association of Integrative Medicine （CALM） was convened at 19-20, April 2008 in Beijing. Academician CHEN Zhu, the minister of Ministry of Health indicated at the congress that the integration of Chinese and Western medicine is very well in keeping with the situation of our country and the general rule of development in medical science; and as a good integration of Chinese medicine and Western medicine, it is mutually beneficial and advantageous to both of them. Seeing the creativity shown in integrative medical investigation in theoretic and methodological sides, we should and must persist in and develop it.