理伤手法结合中药治疗腰部术后痛疗效观察

目的:探讨理伤手法结合舒筋活血汤加减治疗腰部术后痛的治疗作用.方法:将113例腰部术后痛患者,采用随机对照的方法,分为治疗组(62例)和对照组(51例),治疗组采用理伤手法结合口服舒筋活血汤加减治疗,对照组采用口服舒筋活血汤加减治疗.1周为1个疗程,共观察4个疗程.结果:1个疗程后,两组无明显好转,4个疗程后,治疗组优...     

非布司他在健康受试者体内的尿药排泄特征

 目的 建立人尿样中非布司他浓度的液相色谱-质谱联用（LC-MS）测定法,并研究健康中国受试者口服非布司他片后非布司他的尿药排泄特征。方法 尿液样品酸化后用乙酸乙酯提取,进行LC-MS分析。色谱柱为Hedera ODS-2,流动相为甲醇-10 mmol·L-1的醋酸铵水溶液（含0.05%甲酸）(70∶30)。12 名健康受试者分别单次口服非布司他片80 mg（规格：80 mg）后,测定尿药浓度,计算尿药排泄参数,并进行统计分析。结果 12 名健康受试者口服80 mg非布司他后,48 h内的尿药累积排泄量为(2.684±0.838) mg,累积排泄率为(3.4±1.0)%。男性与女性受试者间的累积排泄量和最大排泄速率无显著性差异。结论 非布司他在健康中国受试者体内的尿药排泄参数与已有文献报道的结果基本一致,且不存在性别差异。     

Bioavailability assessment: Methods to estimate total area (AUC 0-∞) and total amount excreted (A e ∞ ) and importance of blood and urine sampling scheme with application to digoxin

Five methods are compared to estimate the total area under the digoxin plasma or serum concentrationtime curve (AUC0-) after a single dose of drug. To obtain accurate estimates of AUC0-, data required are concentrations at a sufficient number of sampling times to define adequately the concentration-time curve prior to the log-linear phase, and at least three, but preferably four or more equally spaced points in the terminal loglinear phase. One method (designated Method I) requires a digital computer; another (Method III) is the classical method (these two methods do not require equally spaced points in the loglinear phase). Method IIA is the accelerated convergence method of Amidon et al.; Methods IIB and IIC are modifications of this method, but incorporate usual and orthogonal least squares, respectively, which make them more accurate with real (noisy) data. Methods I and IICgave very comparable estimates of AUC0-. Results indicate that digoxin administered orally in aqueous solution was completely (100%) absorbed when bioavailability estimates were based on oral and intravenous AUC0- estimates and the actual doses, whereas formerly only about 80% absorption was reported, based on areas, under plasma concentration curves which were truncated at 96 hr. It is shown that the sampling scheme of blood can produce biased apparent bioavailability estimates when areas under truncated curves are employed, but an appropriate sampling scheme and application of method IIyield accurate bioavailability estimates. This is important particularly in those bioavailability studies where one is attempting to determine the appropriate label dose for a new fastrelease digoxin preparation relative to the label dose and bioavailability of currently marketed tablets. It is shown that the magnitudes and variability of apparent elimination rate constants and halflives of digoxin, estimated from urinary excretion data by the ^– method, depend on which value of A _e is used. The formerly reported greater interindividual variability of AUC data compared to At data for digoxin is explained in that the AUCs, but not the A_e,'s, involve the renal clearance, which exhibits considerable inter- and intraindividual variation.     

南京地区34家医院2012-2015年止吐药物利用分析

目的：评价南京地区34家医院2012—2015年止吐药物的使用情况。方法对2012—2015年南京地区34家医院止吐药物采用销售金额、用药频度和日用药金额等进行排序分析。结果止吐药物使用金额和用药频度呈逐年上升趋势,以5-羟色胺受体拮抗剂为首。结论5-羟色胺受体拮抗剂用量快速增长,在南京地区占主导地位。     

荧光素钠注射液的设备冲洗液的检测方法研究

目的建立荧光素钠注射液的设备冲洗液的检测方法，控制冲洗液中荧光素钠的残留量。方法紫外一可见分光光度法，检测波长234nm。结果荧光素钠在4．955～54．505μg·mL^-1范围内线性关系良好（线性系数r=0．99997），检测限0．03125ppm，定量限0．1ppm，平均回收率99．9％。结论本法简单，快捷，准确，适合控制冲洗液中荧光素钠的残留量。     

色空间法结合化学计量学研究麦麸含水量、粒径及其用量对麸炒山药外观颜色的影响

目的 以色空间法结合化学计量学研究麦麸对麸炒山药外观颜色的影响,为中药炮制辅料麦麸质量标准的制定和麸炒炮制工艺的优选提供依据。方法 以不同含水量（ω）、不同粒径（Φ）的麦麸为辅料以及加入不同用量（n）的麦麸,分别制备麸炒山药。采用色差仪测定麸炒山药外观色度值L^*、a^*、b^*及总色度值E_ab^*［L^*为亮度,a^*为红绿色度值,b^*为黄蓝色度值,E_ab^*=（L^*2＋a^*2＋b^*2）^1/2］,采用SIMCA 14.1和SPSS statistics 26对麸炒山药外观色度值进行数据分析。结果 麦麸含水量主要影响麸炒山药外观色度值a^*,含水量越大,a^*值越小;麦麸粒径主要影响麸炒山药外观色度值L^*,粒径越细,L^*值越分散;麦麸用量则主要影响麸炒山药外观色度值a^*、b^*,每100 g山药用麦麸5～20 g,麦麸用量越大,a^*、b^*值越大。合适规格麦麸炮制的麸炒山药外观色度值及总色度值范围分别为81.09≤E_ab^*<90.12。基于色度值的麦麸规格参数非标准化典则判别函数式分别为ω=0.688 L^*＋1.264 a^*－0.872 b^*－18.113,Φ=0.058 L^*＋0.049 a^*－3.696,n=0.346 L^*＋0.867 a^*－24.666。结论 麦麸含水量<25%,粒径10～50目,每100 g山药饮片用麦麸10～15 g,炮制出的麸炒山药饮片符合《中国药典》2020年版性状要求。过于潮湿、粒径过细及麦麸用量过大或过小均难以满足麸炒山药的外观颜色要求。     

滚压载荷下成年和幼年软骨的棘轮行为

文题释义： 非接触数字相关技术：非接触式测量方法以前主要有光学式和气动式两种,实验采用光学式图像采集系统。图像测量技术作为一种新兴的非接触测量方法有着独特的优越性,它通过把被测对象的图像作为检测和传递信息的手段,从图像中提取有用信息进而获得待测参数,研究通过图像采集点的坐标变化从而计算出受载前后软骨的应变。 棘轮效应：材料受到拉伸或压缩时,如果力大于材料的屈服强度,那么材料就会发生塑性变形。在非对称应力控制循环加载下,材料反向变形大小就会小于初始变形,进而产生了残余应变,如此反复而产生的沿应力方向上塑性变形累积的现象,这种现象即称为棘轮效应。 背景：国内外学者对关节软骨在不同力学环境及循环压缩载荷下的受力情况做了不少研究,但均集中在循环压缩载荷对软骨的作用,有关软骨年龄因素对软骨力学特性影响的研究和软骨在复杂受力环境下的特性研究不深入。                                                      目的：研究不同滚压载荷条件对成年和幼年关节软骨棘轮行为的影响。 方法：以成年猪股骨软骨和幼年猪股骨软骨为实验对象,在不同实验条件下(压缩量：10%,20%,30%;滚压速率：1.66,3.44,6.68 mm/s;缺损宽度：1,2,4 mm)采用滚压加载装置施加载荷,同时使用非接触数字相关技术对加载过程中的试样进行图像采集,通过分析处理图像,研究循环滚压载荷作用下成年及幼年关节软骨的棘轮行为。 结果与结论：①在滚压载荷下,随着滚压循环载荷的进行,成年软骨和幼年软骨的棘轮应变都呈现先快速增加后缓慢增加的趋势;②随着压缩量的增加,成年软骨和幼年软骨的棘轮应变都增加;在相同压缩量下,幼年软骨的棘轮应变大于成年软骨,并且他们的棘轮应变沿着软骨深度从表层到深层逐渐降低;③随着滚压速率的增加,成年软骨和幼年软骨的棘轮应变减小;④1 mm微型缺损关节软骨的棘轮应变数值和趋势与完整无缺损软骨大致相同。在2,4 mm缺损状态下,缺损软骨的棘轮应变值均比同样条件下完整软骨的棘轮应变值要高。 ORCID: 0000-0003-3586-1073(李凯);0000-0002-7288-6686(高丽兰) 中国组织工程研究杂志出版内容重点：组织构建;骨细胞;软骨细胞;细胞培养;成纤维细胞;血管内皮细胞;骨质疏松;组织工程     

P-glycoprotein and cytochrome P450 3A4 involvement in risperidone transport using an in vitro Caco-2/TC7 model and an in vivo model

The possible involvement of P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A4 in risperidone transport was investigated using in vitro and in vivo models. Firstly, uptake studies were performed on a Caco-2/TC7 cell monolayer; the effects of 1 microg ml(-1) risperidone on apparent permeability were determined for secretory and absorptive directions, in the presence or absence of various P-gp and CYP3A4 inhibitors (verapamil, ketoconazole, erythromycin), and of an associated multidrug-resistant protein inhibitor (indomethacin). Secondly, on a conscious rat model, risperidone pharmacokinetic parameters, notably absorption parameters, were determined using compartmental and deconvolution methods. Three groups of seven rats received respectively an IV risperidone dose, an oral risperidone dose (PO group) and the same oral risperidone dose after verapamil administration (POV group). No formation of 9-hydroxyrisperidone was observed on Caco-2 cells after risperidone administration; there was no evidence that intestinal CYP3A4 is involved in risperidone metabolising. Risperidone secretory permeation was higher than absorptive permeation. Verapamil increased risperidone absorption permeation and decreased its secretory permeation. Indomethacin did not modify these permeation values. In rats, verapamil led to an increase in both risperidone and 9-hydroxyrisperidone plasmatic concentrations. The fraction absorbed in the verapamil group was 3.18 times higher than in the oral group (65.9% and 20.7% for POV group and PO group). The absorption rate constant was lower in the verapamil group. Our results indicate that P-gp decreases the intestinal absorption of risperidone and that intestinal CYP3A4 is not involved in risperidone metabolism.     

Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release

Abstract

Amoitone B, a novel compound chemically synthesized as the analogue of cytosporone B, has been proved to own superior affinity with Nur77 than its parent compound and exhibit notable anticancer activity. However, its application is seriously restricted due to the water-insolubility and short biological half-time. The aim of this study was to construct an effective delivery system for Amoitone B to realize sustained release, thus prolong drug circulation time in body and improve the bioavailability. Nanostructured lipid carriers (NLC) act as a new type of colloidal drug delivery system, which offer the advantages of improved drug loading and sustained release. Amoitone B-loaded NLC (AmB-NLC) containing glyceryl monostearate (GMS) and various amounts of medium chain triglycerides (MCT) were successfully prepared by emulsion-evaporation and low temperature-solidification technology with a particle size of about 200?nm and a zeta potential value of about ?20?mV. The results of X-ray diffraction and DSC analysis showed amorphous crystalline state of Amoitone B in NLC. Furthermore, the drug entrapment efficacy (EE) was improved compared with solid lipid nanoparticles (SLN). The EE range was from 71.1% to 84.7%, enhanced with the increase of liquid lipid. In vitro drug release studies revealed biphasic drug release patterns with burst release initially and prolonged release afterwards and the release was accelerated with augment of liquid lipid. These results demonstrated that AmB-NLC could be a promising delivery system to control drug release and improve loading capacity, thus prolong drug action time in body and enhance the bioavailability.     

复方丹参片溶出速率的研究

对不同厂家生产的复方丹参片用转蓝法进行了溶出速率的测定,经方差分析表明不同厂家生产的样品间相对累积释放量有显著性差异(P<0.01)。其中T_(50)最快与最慢相差10倍。结果还提示,崩解时限与T_(50)无显著相关性。表明各地的生产工艺、原料、辅料的来源不同是影响溶出速率的主要原因。