坎地沙坦酯速释及缓释固体分散体的制备研究

目的制备坎地沙坦酯速释和缓释固体分散体,提高坎地沙坦酯生物利用度。方法用固体分散体技术制备坎地沙坦酯速释和缓释固体分散体,并将制备方法对体外释放度的影响进行分析。结果聚乙二醇6000、泊洛沙姆188为混合载体的速释型固体分散体与物理混合物对比,药物的溶出速率和溶出量明显提高。乙基纤维素（EC）的黏度对缓释型固体分散体有较大影响;释放调节剂PEG的使用比例影响缓释效果;药物与载体用量的比例控制在1∶4~1∶6之间缓释效果较好。结论速释和缓释固体分散体均能提高药物的溶出量,以乙基纤维素为载体的固体分散体缓释效果明显。     

表面活性剂对葛根素固体分散体体外溶出的影响

目的:应用固体分散技术,以提高葛根素的体外溶出速率.方法:采用溶剂法制备了含有和不含有表面活性剂吐温-80的葛根素的PVP-3800固体分散体,进行体外的溶出实验,并用DSC鉴别不同固体分散体中药物的分散状态.结果:葛根素的固体分散体明显地促进了葛根素的溶出,并且含有吐温-80的固体分散体溶出速率比不含吐温-80溶出速率快.DSC的结果表明,葛根素、PVP与吐温120的比例在1∶5∶2和1∶8∶2 形成无定型的共沉淀物,而1∶2∶0,1∶5∶0,1∶8∶0的葛根素以微晶形式存在于固体分散体中.结论:表面活性剂可以提高葛根素固体分散体的溶出速率.     

雷公藤红素胶体二氧化硅缓释固体分散体研究

目的 制备雷公藤红素（tripterine）缓释固体分散体,使药物释放度提高,同时缓慢释放药物,以降低其毒副作用。方法 以胶体二氧化硅为载体,采用溶剂蒸发法制备雷公藤红素固体分散体,对其体外溶出和物相特征进行研究。结果 雷公藤红素和胶体二氧化硅按1∶12制备的固体分散体中,药物缓慢释放,8 h时药物的体外释放度达到90%以上。经差示扫描量热、X衍射和电镜分析,固体分散体中药物以非晶形式存在于载体中。结论 雷公藤红素胶体二氧化硅固体分散体制备工艺简单,药物缓慢释放且释放较完全,具有实际应用价值。     

热熔挤出技术制备小檗红碱固体分散体及其体外评价

[目的]采用热熔挤出技术制备微溶性药物小檗红碱的固体分散体,以提高其溶解度,延缓其体外释放行为。[方法]以Soluplus^® 为载体,采用同螺杆热熔挤出机制备小檗红碱固体分散体,通过差示扫描量热（DSC）分析、粉末X射线衍射（XRD）分析、扫描电子显微镜（SEM）观察和傅里叶变换红外光谱（FT-IR）分析对制备的固体分散体进行表征,并考察挤出物在不同介质中的溶解度和体外溶出度。[结果]DSC和XRD分析结果显示,固体分散体中小檗红碱的主要特征峰减弱甚至部分消失,SEM结果表明固体分散体为无规则形态。FT-IR结果表明小檗红碱与Soluplus^®之间可能存在氢键作用。所制备的小檗红碱固体分散体在pH 6.8的磷酸盐缓冲液中溶解度为原料药的2.59倍。体外溶出度结果显示,小檗红碱固体分散体具有明显缓释作用。[结论]成功制备了小檗红碱固体分散体,且能显著提高其溶解度,并延缓其体外释放行为。     

多烯紫杉醇固体分散体的制备和体内外研究

目的 优选多烯紫杉醇固体分散体的制备工艺,提高多烯紫杉醇的体外溶出度和绝对生物利用度.方法 采用溶剂法制备不同载体,不同溶剂和不同药物载体比例的多烯紫杉醇固体分散体,并进行了体外溶出实验和大鼠体内生物利用度研究;同时采用XRD,DSC,ESEM法鉴别药物在固体分散体中的存在状态.结果 泊洛沙姆188固体分散体对多烯紫杉醇增溶的效果优于PVPk30和单硬脂酸甘油酯;且溶出实验2 h时,泊洛沙姆188固体分散体(10:90)的累计溶出百分率接近于原料药的4倍;XRD,DSC、ESEM显示多烯紫杉醇在固体分散体中以无定型态或分子状态存在;高、低剂量大鼠口服给药的绝对生物利用度分别为10.1%和35.1%.结论 固体分散体能明显提高多烯紫杉醇的体外溶出度和口服生物利用度.     

固体分散体技术改善长春西汀溶出特性的研究

目的 采用固体分散体技术改善长春西汀(VIN)的体外溶出特性.方法 分别以PEG6000、PVPK30为载体,用熔融法、溶剂法制备长春西汀固体分散体,差热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态,并进行了稳定性试验和体外溶出度试验,考察载体的用量、载体中加入表面活性剂的用量和溶出介质对药物溶出特性的影响.结果 VIN-PEG6000固体分散体中药物部分以分子状态分散,部分以微晶分散;VIN-PVPK30固体分散体中药物以无定形状态存在;VIN-PVPK30的药物溶出好于VIN-PEG6000,但稳定性不如VIN-PEG6000;载体的用量、表面活性剂的用量和溶出介质对药物溶出有一定影响.结论 长春西汀固体分散体VIN-PEG6000-十二烷基硫酸钠(1∶6∶0.8)能显著提高药物的溶出速度和程度.     

活性氯酚3-氯-3’,4’-二羟基二苯甲酮固体分散体的制备及体外溶出研究

目的制备活性氯酚3-氯-3’,4’-二羟基二苯甲酮(HP46)的固体分散体(solid dispersion,SD),以提高HP46的体外溶解度和溶出度。方法以聚乙烯吡咯烷酮(PVPK30)为载体,吐温(Tween80)为表面活性剂,采用溶剂法制备HP46的固体分散体,优化固体分散体组成,并进行体外溶出研究。运用粉末X-射线衍射(XRD)和差示热量扫描(DSC)分析固体分散体中药物的分散状态。结果 HP46固体分散体组成的最优质量比为HP46-PVPK30-Tween80 1∶3∶1,XRD和DSC结果表明HP46以无定型或分子状态存在于载体中,体外溶解度和溶出速率显著提高,溶解度为1 319.4μg/ml,在20 min内累积溶出率为77.23%,溶解度和溶出度较原料药分别提高约30倍和8倍。结论以PVPK30为载体,加入表面活性剂Tween80,可有效提高HP46的溶解度和溶出度,固体分散体最优质量比为HP46-PVPK30-Tween80 1∶3∶1。     

川芎嗪自乳化缓释固体分散体释放度测定方法研究

目的:建立川芎嗪自乳化缓释固体分散体释放度测定方法。方法:采用HPLC法测定川芎嗪自乳化缓释固体分散体中TMP的含量,考察相关因素对其体外释药的影响。结果:以转篮法为溶出度测定方法,释放介质为脱气纯水,转速为50r/min。结论:建立了良好的川芎嗪自乳化缓释固体分散体释放度测定方法,为评价和控制该药的质量提供依据。     

葛根素固体分散体的分散状态及其体外评价

目的制备葛根素缓释固体分散体,考察其分散状态。方法以乙基纤维素为载体,制备葛根素缓释固体分散体,利用X射线衍射试验、差示扫描量热法对葛根素在其中的分散状态进行研究。并对该胶囊进行体外溶出度研究。结果X射线衍射图表明葛根素在固体分散体中有一部分葛根是以分子状态分散,而另一部分可能以微晶体状态分散。差示扫描量热法试验结果表明,所制备的缓释固体分散体中不存在药物结晶。溶出度试验结果表明,该缓释胶囊具有良好的缓释效果。结论采用固体分散技术制备的葛根素缓释固体分散体完全可以使药物达到高度分散状态,制备的葛根素缓释固体分散体具有较好的缓释效果。     

氯诺昔康固体分散体的热焓变化及溶出度改善特性

目的：制备非甾体抗炎药氯诺昔康的固体分散体以提高难溶性氯诺昔康体外溶出速率。研究载体类型及药物-载体混合比例对固体分散体体外溶出速率的影响，并根据：DSC测定结果考察各种混合物中氯诺蕾康热焓变化的特性。方法：分别以Poloxamer188、PVPK30和Gelucire 44／14为载体，采用溶剂蒸发法制备氯诺昔康固体分散体。采用浆法进行体外溶出度试验。根据DSC实测数据考察热焓变化特征。结果：固体分散体体外溶出速率的先后顺序为PXM，PVP，GLC，物体混合物顺序为PXM，GLC，PVP，随着载体比例的增加，PVP和泊洛沙姆固体分散体溶出速率常数增加。DSC圈谱表明，随着载体比例的增加，氯诺昔康放热峰的起始温度和△H降低，当氯诺昔康的泊洛沙姆比例为1：10时，药物以无定形状态存在于结晶性的泊洛沙姆中，从而使其在体外具有最快的溶出速率。结论：载体类型及药物-载体比例影响氯谱诺昔康固体分散体的体外溶出特性及热焓变化。     

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…     

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.     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

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.     

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.     

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.     

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.     

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.