盐酸青藤碱在微针阵列作用下的透皮给药研究

目的探索盐酸青藤碱在微针阵列作用下的透皮给药规律与微针促进药物透皮吸收的机制。方法高效液相色谱法测定青藤碱的含量,裸鼠皮肤用微针阵列预刺处理,采用水平双室扩散池法研究微针的针尖形状、刺入力、滞留时间以及阵列数对于盐酸青藤碱透皮给药的影响规律。将微针预刺处理的皮肤制备成切片,并用显微镜观察皮肤的变化。结果微针阵列预刺处理与被动扩散比较能显著提高盐酸青藤碱透皮给药的累积渗透量(P<0.01),但平顶微针比尖顶微针更能有效促进药物的透皮吸收;药物的累积渗透量随着微针处理皮肤的刺入力的增加而增加,但当刺入力超过5.0 N时,药物的累积渗透量不再显著增加;随着微针在皮肤中滞留时间的延长药物的累积渗透量不断增大,当滞留时间超过60 s时药物的累积渗透量不再显著增加;尽管药物的累积渗透量随着微针阵列数的增加而增加,但是二者之间无正向线性关系。皮肤切片表明微针刺入皮肤后能够在皮肤上形成跨越角质层的微孔道。结论微针可以在皮肤上形成微孔道而增强皮肤对药物的渗透性,从而为盐酸青藤碱透皮给药系统提供一种新型、高效的透皮给药新技术,具有广泛的应用前景。     

微针对熊果苷皮肤给药的促渗作用研究

目的考察微针对熊果苷皮肤给药的促渗作用,并与化学促渗剂氮酮进行比较。方法采用深反应离子刻蚀技术制备星形硅微针。制备熊果苷水凝胶剂,采用Franz扩散池法,将人体腹部皮肤置于扩散池间,分3组:微针实验组供给室加入熊果苷水凝胶,皮肤采用微针作用;氮酮对照组供给室分别加入含有1%、3%、5%氮酮的熊果苷水凝胶,皮肤无微针作用;空白对照组供给室加入无氮酮熊果苷水凝胶,皮肤无微针作用。分别在1、3、6、12、24、36、48 h等时间点取样,以HPLC法测定接收池、皮肤表皮层和真皮层中的熊果苷含量,液相条件:C18柱(250 mm×4.6 mm,5μm);流动相为甲醇∶1×10-3mol/ml盐酸(5∶95);柱温25℃;流速1 ml/min;检测波长282 nm。求算熊果苷的累积透过量(Qr)、稳态透皮速率(Js)及皮肤累积滞留量(Qs)。结果星形硅微针可以刺穿人体皮肤角质层。HPLC标准曲线方程C=0.000 2A-0.182 9(r=0.999 9),线性范围0.4～50μg/ml、日内精密度和日间精密度分别为2.4%和2.74%,回收率均大于90%。微针作用组的熊果苷累计透过量、稳态透皮速率和表皮累计滞留量均高于5%氮酮组(P<0.01)。结论微针作用皮肤后可显著增加熊果苷皮肤渗透量。     

熊果酸纳米混悬凝胶剂的制备及其体外透皮研究

目的 制备熊果酸纳米混悬凝胶剂(UA-NS-gel),并考察其体外透皮性能.方法 采用反溶剂沉淀联合高压均质法制备UA-NS,再以卡波姆940为基质制成凝胶剂(UA-NS-gel);采用Franz扩散池法进行体外透皮试验,比较UA-NS-gel和熊果酸凝胶剂(UA-gel)的体外经皮渗透量及滞留量.结果 UA-NS-gel 24 h药物经皮渗透量为(104.40±6.48)μg/cm2,明显高于UA-gel的(28.56±2.16)μg/cm2 (P<0.01);UA-NS-gel皮肤滞留量为(138.08±19.39)μg/cm2,高于UA-gel的(70.51±14.77)μg/cm2 (P<0.05).结论 将熊果酸制成纳米混悬凝胶剂,能够有效地增加药物的皮肤渗透性能和皮肤的滞留量.     

天麻素全载药可溶性微针的制备及体外经皮渗透性研究

  目的  制备天麻素全载药可溶性微针, 并考察其理化性质及体外透皮性能。  方法  采用两步离心法制备天麻素全载药可溶性微针, HPLC法测定其载药量, 并进行形态学、机械性能、皮肤穿刺性能和恢复性能考察; 采用Franz扩散池考察其体外透皮性能。  结果  所制微针阵列完整, 柔韧性好, 每片载药量达(5.45±0.14)mg, 机械性能良好, 能成功刺穿大鼠皮肤, 微针处理后皮肤在2 h内即可恢复到原来的状态。离体皮肤渗透结果显示, 12 h后全载药微针中天麻素的累积渗透量可达87%, 而天麻素溶液中天麻素的累积渗透量为12%, 说明可溶性微针对天麻素具有良好的透皮递送促进作用。  结论  制备的天麻素全载药可溶性微针机械强度及柔韧性好, 实现了水溶性药物的透皮递送。      

鬼臼毒素固体脂质纳米粒经皮渗透和皮肤贮留研究

目的研究鬼臼毒素固体脂质纳米粒经皮渗透和皮肤贮留情况。方法采用Franz扩散池测定鬼臼毒素固体脂质纳米粒的经皮渗透速率,扩散池与供给池之间为大鼠或家兔腹部皮肤,扩散池面积为2.92 cm^2。在体外透皮试验完结后,取下皮肤,剪碎匀浆,用50%异丙醇-生理盐水提取,提取液处理后用HPLC测定药物浓度。结果制得的鬼臼毒素固体脂质纳米粒包封率平均为95.28%,RSD为2.53%（n=5）,粒径在50-200 nm之间。固体脂质纳米粒作为载体时,鬼臼毒素经大鼠和家兔离体腹部皮肤的平均渗透速率和累积透过量较市售酊剂明显降低,同时药物贮留量较市售酊剂明显提高。结论鬼臼毒素固体脂质纳米粒具有较强的皮肤靶向性。     

盐酸特比萘芬二元醇质体的制备及体外评价

目的 制备盐酸特比萘芬二元醇质体并进行体外评价.方法 采用乙醇注入-超声法制备二元醇质体;以粒径、Zeta电位和包封率为评价指标,通过正交试验优化处方;采用改良Franz扩散池对不同脂质体进行体外皮肤渗透试验.结果 最优处方为:药物质量分数为0.5‰,药脂比为1∶5(g∶g),二元醇相体积分数为30％,乙醇-丙二醇体积比为7∶3;以优选的处方制备的二元醇质体粒径为(36.2±1.0)nm、Zeta电位为(-23.22±2.02)mV、包封率为(97.61±0.09)％,表皮真皮层滞留量最高为(23.18±2.38) μg/cm2.结论 所选工艺合理可行,可用于制备盐酸特比萘芬二元醇质体,二元醇质体增加盐酸特比萘芬在表皮真皮层滞留量.     

丹皮酚脂质体凝胶的制备及其透皮作用

目的研究丹皮酚(paeonol,PAE)脂质体凝胶制备及其体外透皮扩散。方法采用乙醇注入法制备PAE脂质体凝胶并对其物理特性进行研究;同时,采用Franz扩散池以大鼠皮肤进行体外经皮渗透实验,考察PAE脂质体凝胶的经皮渗透行为及皮内滞留药物量。结果制备的PAE脂质体凝胶包封率为78.62%,平均粒径为337 nm。体外经皮渗透实验表明,与PAE凝胶相比,其脂质体凝胶24 h内的累积渗透量为84.61μg/cm2,根据渗透动力学回归方程PAE脂质体凝胶累积渗透速度18.738μg/(cm2·h),透皮速率较慢;PAE脂质体凝胶、普通凝胶在凝胶内残留溶液浓度分别为2.550μg/ml、5.239μg/ml;PAE脂质体凝胶、普通凝胶在大鼠皮肤内残留溶液浓度分别为37.98μg/ml、17.99μg/ml,皮肤中药物滞留量明显增加。结论 PAE脂质体凝胶释放速率减慢,药物蓄积于皮肤内增多,对于治疗疾病有较多的释药量,达到长效持久抗炎效果,同时有利于避免丹皮酚因全身吸收而引起的副作用,可作为PAE临床应用的新剂型。     

复方盐酸特比萘芬贴剂的制备与体外透皮性能研究

目的 制备复方盐酸特比萘芬压敏胶贴剂,并对其体外透皮性能进行研究。方法 采用改良Franz扩散池,以离体大鼠皮肤为屏障进行经皮渗透试验,高效液相色谱法测定盐酸特比萘芬和酮康唑不同时间点、不同接收液中的体外皮肤透过量,并对药物在不同时间的皮肤局部贮药量进行测定。结果 24 h内盐酸特比萘酚的体外皮肤透过率低于0.05%,酮康唑的皮肤透过率低于2%,盐酸特比萘芬皮肤贮药量24 h为8.763μg/cm2,酮康唑为20.86μg/cm2,且在72 h内皮肤贮药量呈增加趋势。结论 所制得的复方盐酸特比萘芬贴剂可发挥局部长效的治疗作用,有望开发为长效经皮给药制剂。     

布洛芬滴丸剂的研制及体外溶出度

目的 :研究柔性纳米脂质体对环孢素经皮渗透的促进作用。方法 :采用改进的Ｆｒａｎｚ扩散池体外经皮渗透实验技术 ,比较普通纳米脂质体、含有表面活性剂胆酸钠的柔性纳米脂质体以及胆酸钠胶团溶液对环孢素的经皮渗透促进作用。结果 :将脂质体胶体溶液非封闭性应用于离体小鼠皮肤表面 ,柔性纳米脂质体促进药物穿透皮肤 ,8ｈ后皮肤药物的透过量为 1.16 μｇ·ｃｍ-2 ,2 4ｈ后透过量达到 1.88μｇ·ｃｍ-2 ,皮肤中药物残留量为 (1.78± 0 .5 1) μｇ·ｃｍ-2 。普通纳米脂质体阻止药物透过皮肤却滞留药物于皮肤中 ,2 4ｈ后残留量为 (0 .72± 0 …     

携载姜黄素纳米粒和新吲哚菁绿的透明质酸微针能抑制人舌鳞癌细胞增殖

目的：制备并研究携载药物姜黄素纳米粒和光热触发剂新吲哚菁绿（IR820）的透明质酸微针（以下简称微针）给药系统对人舌鳞癌细胞（Cal-27）的抑制作用。方法：通过模板法分别制备对照微针、姜黄素纳米粒微针、IR820微针、姜黄素纳米粒+IR820微针,并分别进行形貌表征、力学强度测试、体外皮肤刺入试验及体外光热效应测试。将各组微针与Cal-27细胞共培养,其中IR820微针组及姜黄素纳米粒+IR820微针组用808?nm近红外光1?W/cm²照射5?min,并通过活死细胞染色结果对各组细胞存活率进行统计。结果：制备的微针针体形貌均一,具有良好的力学强度及皮肤刺入能力,其中搭载IR820的微针具有较好的光热性能。与各组微针共培养后,Cal-27细胞存活率分别为空白对照组100.00%、对照微针组99.92%、姜黄素纳米粒微针组94.08%、IR820微针组0.41%、姜黄素纳米粒+IR820微针组0.04%。其中,姜黄素纳米粒+IR820微针组对肿瘤细胞杀伤效果最好,IR820微针组次之（均P<0.05）。结论：相比单一的药物治疗,姜黄素纳米粒+IR820微针对Cal-27细胞增殖具有更好的抑制作用。     

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.     

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.     

TCM Treatment of Ankylosing Spondylitis by Tonifying the Kidney and Strengthening the Governor Vessel

Ankylosing spondylitis is a chronic and progressive disorder with inflammation mainly involving the central axis joints. It mainly affects the cervical spine and the lumbosacral area, with the pathogenesis closely related to the kidney and the Governor Vessel (GV). TCM holds that the syndrome is deficiency in origin and excess in superficiality, which is due to insufficiency of the kidney, deficiency of GV, and blocking of the channels with the invasion of exogenous evil, leading to poor circulation of qi and blood and malnutrition of the bones, muscles and joints. The TCM method of tonifying the kidney and strengthening GV to regulate circulation of qi and blood and check the arthralgia pain should be adopted, with the Kidney-Tonifying and GV Strengthening Decoction (益肾强督汤) prescribed.     

IMPROVING P-gp EXPRESSION IN HUMAN MONONUCLEAR CELLS IN VITRO TRANSFECTED BY MULTIDRUG RESISTANCE-1 mRNA

CHEMOTHERAPY playsa greatrolein the treat- ment of malignanttumors,especiallyingynecolo- gicalones.But inanticancerchemotherapy,leuko-cytopeniaisfrequentlytheprimarydose-limitingsideeffect factor.Moreover,cancersarefrequentlychemoresistantbe-causeof overexpressionof P-glycoprotein(P-gp), which isencodedby multidrugresistancegene (MDR1 ) and detectableinup to50% ofhuman cancersand renderscellsresistancetoanticancerdrugs.The safetyand potentialtherapeuticbenefitof mdr1 gene transferredto h…