心脑通胶囊联合低分子肝素钙针治疗急性脑梗死60例

目的观察血滞通胶囊联合低分子肝素钙针治疗急性脑梗死的临床疗效。方法 120例患者随机分为对照组和治疗组各30例,治疗组:血滞通胶囊2粒,日三次口服,低分子肝素钙针5000Iu皮下注射,12h一次,连用7d,对照组:低分子肝钙针5000Iu皮下注射,12h一次,连用7d。两组均给予急性脑梗死常规治疗。结果治疗组总显效率80%,对照组75%,P<0.05,两组有显著差异。结论血滞通胶囊联合低分子肝素钙治疗急性脑梗死疗效显著。     

中等剂量尿激酶联合低分子肝素钙治疗深静脉血栓形成观察

目的观察中等剂量尿激酶联合低分子肝素钙治疗深静脉血栓形成的疗效。方法尿激酶30万U+0.9%N.S 100mL从患肢于2h静脉滴入,日1次,共7d。同时给予低分子肝素钙针5000U每12h皮下注射1次,共10d。结果尿激酶联合低分子肝素钙治疗深静脉血栓形成,患肢肿胀疼痛,缓解快,总有效率达92.8%,且无1例出血。结论中等剂量尿激酶联合低分子肝素钙治疗深静脉血栓形成,疗效可靠且症状缓解快而安全。     

肝素钙注射液治疗不稳定型心绞痛36例临床分析

目的观察不稳定型心绞痛在常规治疗基础上加用肝素钙注射液的疗效。方法腹部皮下注射低分子量肝素钙注射液（天津红日药业股份公司生产的博璞青）6150u,1次/12h,连用7日为1个疗程。结果心绞痛缓解率达88.9%,心电图改善率达86.1%,无心肌梗死及猝死发生。2例在腹壁注射部位出现淤斑。结论不稳定型心绞痛在常规治疗基础上,加用肝素钙可提高疗效,改善预后。     

肠溶阿司匹林和肝素联合抗凝治疗中出现腹膜后血肿

1例69岁冠心病、高血压女性患者服用卡托普利、阿替洛尔、硝酸异山梨酯及硝苯地平治疗2年余.入院后,患者因不稳定心绞痛加用肠溶阿司匹林0.1 g,1次/d和低分子肝素钙5 000 U,1次/12 h 皮下注射.第2天,肠溶阿司匹林增加至0.3 g,1次/d;低分子肝素钙改为肝素钠800～1 500 U/h,静脉泵入.48 h后再次改为低分子肝素钙6 000 U,1次/12 h皮下注射.第5天,患者出现腹膜后血肿,出血量约1 000～1 200 ml.停用肠溶阿司匹林和低分子肝素钙,给予悬浮红细胞、巴曲酶及扩容治疗.入院第28天,CT检查示患者血肿有所吸收,2 d后出院.出院2个月CT复查示出血肿大部分吸收.     

奥沙利铂联合亚叶酸钙和氟尿嘧啶治疗晚期大肠癌的临床观察

目的评价奥沙利铂联合亚叶酸钙和大剂量氟尿嘧啶（5-FU）持续48 h静脉滴注治疗晚期大肠癌的疗效和安全性。方法32例大肠癌患者采用静脉滴注奥沙利铂100 mg/m^2,亚叶酸钙200 mg/m^2,亚叶酸钙滴注之后用5-FU 0．5 g静注,接着用5-FU 3．0 g/m^2持续静脉滴注48h,每2周1次,2次为1个周期。结果32例病例中,平均疗程数为4个周期,其中完全缓解（CR）1例,部分缓解（PR）15例,稳定（SD）12例,进展（PD）4例,总有效率（CR＋PR）为50%。不良反应为恶心、呕吐和骨髓抑制,但多为Ⅰ～Ⅱ度,一过性感觉异常。结论奥沙利铂联合亚叶酸钙和氟尿嘧啶治疗晚期大肠癌疗效较高,不良反应轻而且安全,患者容易耐受,值得推广使用。     

乙酸阴道热敏凝胶剂在家兔阴道内的药动学

目的研究乙酸阴道热敏凝胶剂经阴道给药后药物在家兔阴道内的药代动力学特征,探索适合阴道用药的新剂型。方法 3 ml含乙酸36.23 mg的乙酸阴道热敏凝胶剂推入家兔阴道内,给药后0.25,0.5,1,1.5,2,4,8,12,16,20和24 h,对家兔阴道进行灌洗并测定灌洗液中乙酸的含量、用微电极插入阴道测定阴道pH值、取阴道组织匀浆后测定组织中乙酸含量。采用非线性最小二乘法进行计算机拟合获得药动学参数。结果乙酸阴道热敏凝胶剂置入家兔阴道后,阴道pH值由给药前中性(pH 6.67)转变为酸性(pH 3.56),阴道pH 3.5～4.0可保持约6 h;pH 3.5～4.5可保持约12 h;pH 3.5～5.0可保持19 h;给药后24 h,pH值为5.32±0.24,乙酸含量为(0.38±0.15)g.L-1,为给药量的11%。阴道组织中乙酸浓度峰值为600μg.g-1,达峰时间为2 h,平均保留时间为7.73 h,药物动力学参数符合二室模型。结论乙酸阴道热敏凝胶剂符合阴道用药的要求。     

乙酸钙-鲍氏不动杆菌临床分离率与耐药率5年监测

目的了解2005至2009年乙酸钙-鲍氏不动杆菌在临床标本中的分离情况及其耐药趋势,为临床感染的预防和治疗提供参考资料。方法回顾分析2005至2009年间所有标本中乙酸钙-鲍氏不动杆菌的分离率,菌株在标本与病区的分布及对14种抗菌药物的耐药率。结果乙酸钙-鲍氏不动杆菌的分离率有逐年升高的趋势,从2005年的0.44增至2009年的1.48;其在呼吸道标本的分离率最高(72.34%),其次是尿液(8.42%)、血液(4.40%);病区分布以重症监护室(ICU)最高(47.80%);乙酸钙-鲍氏不动杆菌对14种抗菌药物的耐药率在2005年仅有4种>50%,而到2009年仅头孢哌酮/舒巴坦的耐药率<50%,其他13种耐药率均>50%;其耐药率均呈递增的趋势,耐药性增幅列前3位的分别是环丙沙星31.7%～75.2%、妥布霉素36.9%～75.2%、庆大霉素40.5%～78.3%。结论乙酸钙-鲍氏不动杆菌的临床分离率在逐年增加,其对多数抗菌药物有较高的耐药性,且耐药率呈逐年上升趋势,尤其是对亚胺培南耐药率的快速增长,应引起临床抗感染治疗的高度重视。     

那屈肝素钙治疗急性脑梗死的前瞻性对照研究

目的 :评价那屈肝素钙治疗急性脑梗死的疗效和安全性。方法 :急性脑梗死 2 0 4例 ,用“add on”法随机分为 2组 ,那屈肝素钙组 10 2例予右旋糖酐 4 0 ,50 0mL ,iv ,gtt ,qd ;那屈肝素钙 4 10 0IUAXa ,sc ,bid ,一个疗程 10d。对照组 10 2例仅用右旋糖酐 4 0。结果 :那屈肝素钙组的总有效率为83.3% ,对照组为 70 .6 % ;起病后在 2 4h内开始治疗的有效率为 94 % ,对照组为 76 % ,差异均有显著意义 (P <0 .0 5)。起病后在 2 4～ 4 8h和 >2～ 7d开始治疗的有效率为 81% ,57% ,对照组 70 % ,58% ,差异均无显著意义 (P >0 .0 5)。未发现出血倾向。结论 :早期使用那屈肝素钙治疗急性脑梗死是有效的 ,安全的。     

巴曲酶与低分子肝素钙联合治疗进展型脑卒中的疗效观察

目的探讨巴曲酶与低分子肝素钙联合治疗进展型脑卒中的疗效。方法将进展型脑卒中病例随机分为治疗组(巴曲酶与低分子肝素钙组)与对照组A(巴曲酶组)、对照组B(低分子肝素钙组)。治疗组给予巴曲酶分别10、5、5kU,1次/d静脉滴注,共用3次,第4天开始氯吡格雷片75mg/d,顿服,以及低分子肝素钙5000U皮下注射,1次/12h,连用7d;对照组A应用巴曲酶分别10、5、5kU,隔日一次静脉滴注,共用3次,第6天开始氯吡格雷片75mg/d,顿服;对照组B第1天即开始氯吡格雷片75mg/d,顿服,以及低分子肝素钙5000U皮下注射,1次/12h,连用7d。结果总有效率比较治疗组为94%,对照组A为65.63%,对照组B为86.1%,治疗组明显优于对照组A、B两组。结论巴曲酶与低分子肝素钙联合应用治疗进展型脑卒中安全有效。     

注射用卡络磺钠和二乙酰氨乙酸乙二胺与木糖醇注射液配伍稳定性研究

目的考察注射用卡络磺钠和注射用二乙酰氨乙酸乙二胺分别与木糖醇注射液的配伍稳定性。方法采用HPLC,测定25℃和35℃条件下静置10h内注射用卡络磺钠和注射用二乙酰氨乙酸乙二胺与5%木糖醇注射液配伍后的含量变化,比较配伍前后外观、pH的变化。结果在25℃和35℃下配伍10h内卡络磺钠含量>97.8%、二乙酰氨乙酸乙二胺含量>98.1%,外观和配伍液pH值无明显变化。结论注射用卡络磺钠、注射用二乙酰氨乙酸乙二胺与5%木糖醇注射液10h内配伍稳定。     

Formation of alginate microspheres produced using emulsification technique

This study investigated the formative process of alginate microspheres produced using an emulsification technique. The alginate microspheres were produced by cross-linking alginate globules dispersed in a continuous organic phase using various calcium salts: calcium chloride, calcium acetate, calcium lactate and calcium gluconate. The size, shape, drug content and Ca²⁺ content of the microspheres were evaluated. The tack, viscosity and pH of the calcium salt solution and percentage of Ca²⁺ partitioned into the organic phase were determined. Microscopic examination of the test emulsion at various stages of the emulsification process was also carried out. The propensity of cross-linking reaction was found to be dependent on successful collision between alginate and calcium salt globules. Examination of the characteristics of microspheres indicated that the formed microsphere was a resultant product of alginate globule clustering. The growth propensity of microspheres was promoted by the higher rate and extent of cross-linkage which was governed by the pH, tack and/or Ca²⁺ content of the cross-linking solution, as well as the dissociation constant and diffusivity of the calcium salt. Overall, the amount of free Ca²⁺ cross-linked with alginate in the formed microspheres was in the following order: calcium acetate > calcium chloride + calcium acetate > calcium chloride + calcium gluconate; calcium chloride + calcium lactate > calcium chloride. In microencapsulation by emulsification, the mean size of the microspheres produced can be modified by varying the tack, pH and Ca²⁺ content of the cross-linking solution and through the use of a combination of calcium salts. The shape of the microspheres produced was, nonetheless, unaffected by the physicochemical properties of the cross-linking solution.     

阿托伐他汀钙片溶出度研究

目的：建立阿托伐他汀钙片溶出度研究方法。方法色谱柱：AgilentTC-C18（4.6×250mm,5μm）;以乙腈：四氢呋喃：0.05M柠檬酸铵缓冲液（pH4.0）=27：20：53为流动相;检测波长：244nm;流速：1.5mL·min-1;以阿托伐他汀钙与阿托伐他汀钙杂质H峰面积之和计算累积溶出量（%）;结果阿托伐他汀钙在pH1.0盐酸溶液、醋酸-醋酸铵缓冲液（pH4.5）中不稳定,降解生成阿托伐他汀钙杂质H,阿托伐他汀钙片在pH1.0盐酸溶液中溶出速率最慢;结论阿托伐他汀钙在pH1.0盐酸溶液中溶出曲线可作为处方筛选的依据。     

HPLC法测定匹伐他汀钙中6种有关物质

目的建立了高效液相色谱梯度洗脱法测定匹伐他汀钙中有关物质的方法。方法采用C18（4.6mm×250mm,5μm）色谱柱,以醋酸盐缓冲液（取醋酸钠0.15g,冰醋酸0.5mL,加水稀释至1000mL）为流动相A,乙腈为流动相B,梯度洗脱条件：0～20min,A为56%;20～40min,A为56%→30%;40～60min,A为30%;以1.0mL.min-1的流速进行梯度洗脱;检测波长为245nm。结果匹伐他汀钙与各有关物质的分离度良好,匹伐他汀钙及杂质Ⅰ、Ⅱ、Ⅲ、Ⅴ、Ⅵ的检测限均为0.04μg.mL-1。结论所建立的方法简便、灵敏、准确,可用于匹伐他汀钙有关物质的测定。     

醋酸钙与肾结石研究初探

目的　通过给动物补充适量的醋酸钙以及在乙二醇引起体内草酸代谢异常的情况下补充同等剂量的醋酸钙 ,对以醋酸钙作为补钙剂与肾结石之间的关系进行研究探讨。方法　采用 6 0只Wistar大鼠作为受试动物 ,分别给予醋酸钙或碳酸钙以及用乙二醇诱发肾结石的同时给予醋酸钙或碳酸钙 ,饲养 8wk后处死动物 ,分别对其肾脏发生结石的情况加以观察。结果　本实验条件下补充适量的钙剂 ,在生理情况正常的动物中没有发现肾结石 ;而在人为造成草酸代谢异常的情况下 ,补钙使结石数量有所增加。结论　正常补充钙制剂不会引起肾结石 ;但是在服用补钙剂的同时应少食含有草酸类物质的食品     

HPLC法同时测定阿托伐他汀钙片与普罗布考片中2主分含量

目的:建立同时测定阿托伐他汀钙片与普罗布考片中2主分含量的方法。方法:采用高效液相色谱法。色谱柱为Di-阿am托on伐sil他C汀18;钙流和动普相罗为布甲考醇检-醋测酸浓铵度缓线冲性液范(围pH分4别.0)为=59.50～∶55,0流.0(速r为=01..909m9L9.)、m1i0n.-01～;检10测0.波0μ长g.为mL24-(61nr=m;0选.99用9丹9)皮,平酚均为加内样标回。收结率果分:别为100.5%(RSD=1.05%,n=9)、99.6%(RSD=0.63%,n=9)。结论:此法简便、准确、重复性好,可以为同时测定二者在制剂中的含量或受试体中的血药浓度提供方法依据。     

DAILY VARIATION IN INFLUENCE OF LITHIUM ON SERUM CALCIUM CONCENTRATION: A PRELIMINARY REPORT

1. One millilitre of 5% glucose (vehicle, n = 10) or 1 mL solution of lithium chloride (LiCl) (0.5 or 2.0 mmol/kg per day, n = 10 for each) was injected intraperitoneally in Wistar rats at 10:00 or 22:00 h for 6 days. Blood samples for ionized and total calcium were taken on day 7. 2. Mild elevations in ionized, but not non-ionized (total-ionized) calcium were observed following LiCl treatment in both administration times. 3. The increment in ionized calcium was greater when LiCl was injected at 22:00 h than when it was given at 10:00 h. 4. These data indicate that: (1) the influence of lithium on calcium metabolism varies with its administration time; and (2) mild hypercalcaemia induced by the agent mainly depends on the elevation in the ionized fraction of calcium.     

HPLC法同时测定阿托伐他汀钙、阿司匹林、缬沙坦和苯磺酸氨氯地平制剂的含量

目的:建立同时测定阿托伐他汀钙、阿司匹林、缬沙坦和苯磺酸氨氯地平制剂含量的方法。方法:采用高效液相色谱法,内标为阿普唑仑。色谱柱为Hypersil ODS2-C18柱,流动相为甲醇-0.025 mol/L乙酸铵缓冲溶液(pH4.0,65∶35,V/V),流速为1.0ml/min,检测波长为245 nm,进样量为10μl,柱温为30℃。结果:阿托伐他汀钙、阿司匹林、缬沙坦和苯磺酸氨氯地平检测质量浓度均在5.0⁴0.0μg/ml范围内与各自峰面积积分值呈良好的线性关系(r分别为0.999 4、0.999 4、0.999 2、0.999 8);精密度、稳定性、重复性试验的RSD≤2.67%;平均加样回收率分别为97.28%、99.09%、97.53%、97.53%,RSD分别为1.14%、1.98%、0.95%、1.58%(n=9)。结论:该方法简便、快速、准确,可用于同时测定阿托伐他汀钙、阿司匹林、缬沙坦和苯磺酸氨氯地平制剂的含量。     

瑞舒伐他汀钙片溶出度研究

目的建立瑞舒伐他汀钙片溶出度研究方法。方法HPLC法,色谱柱：AgilentExtendC18（4．6×250mm,5μm）;流动相：以乙腈为流动相A,以0．02％三氟乙酸溶液为流动相B,0～13min,A：37％,13—27min,A：37％--90％;检测波长：242nm;流速：1．0mL·min-1;发生降解行为的溶出度样品经碱中和前处理后以瑞舒伐他汀钙与瑞舒伐他汀非对映异构体峰面积之和计算累积溶出量（％）。结果瑞舒伐他汀钙在pH1．0盐酸溶液不稳定,降解生成瑞舒伐他汀非对映异构体,瑞舒伐他汀-5S-内酯和瑞舒伐他汀-5R-内酯,后两者经碱中和处理后重新生成瑞舒伐他汀及瑞舒伐他汀非对映异构体,且瑞舒伐他汀钙片在pH1．0盐酸溶液中溶出速率最慢。结论瑞舒伐他汀钙在pH1．0盐酸溶液中溶出曲线可作为处方筛选的依据。     

Pharmacokinetics and relative bioavailability of cyclobarbital calcium in man after oral administration

Summary The pharmacokinetics and relative bioavailability of cyclobarbital calcium have been studied after oral administration of Phanodorm, of tablets according to the Formularium Nederlandse Apothekers (1968; FNA), and an aqueous solution. Six healthy volunteers participated in the investigation on three occasions and each received the three preparations. The dose administered was 300 mg cyclobarbital calcium. Plasma concentrations of cyclobarbital were determined at regular intervals. Absorption from the three preparations was rapid and was faster from the solution. Peak concentrations were usually attained within 1 h. The elimination of cyclobarbital could be described by a single first-order process with an average half-life of 11.6 h (range 8 – 17 h). There was little intra-subject variation of the half-life. Relative bioavailability for each volunteer was estimated by comparing the areas under the plasma concentration curves. The FNA-tablets and Phanodorm exhibited similar bioavailability, whereas the average bioavailability of the solution was 78% of that of FNA-tablets; the reason for this unexpected finding is unknown. It was concluded that cyclobarbital cannot be regarded as a uniformly suitable drug for the treatment of insomnia. The long half-life that was apparent in some of the volunteers (15 – 17 h) creates a substantial risk of residual effects on the following morning. In principle, however, the calcium salt of cyclobarbital may be used for induction of sleep, because of its rapid absorption.     

阿托伐他汀钙纳米粒的制备与质量评价

目的:制备阿托伐他汀钙纳米粒新剂型,对其性质进行研究,优选最佳工艺条件。方法:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒溶液,通过对处方优化,以载体材料用量(X₁)、有机溶剂用量(X₂)、表面活性剂用量(X₃)为自变量,利用Box Behnken设计响应面法以纳米粒粒径(Y)为响应值,优化了阿托伐他汀钙纳米粒的处方。用Malvern激光粒度分析仪测定了粒径分布和纳米粒的Zeta电位,扫描电镜分析了其形态,用高速冷冻离心法和紫外分光光度法测定了包封率和载药量。结果:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒溶液是适合的。响应面优化最优值为阿托伐他汀钙20 mg、卵磷脂178 mg、乙酸乙酯15 mL、聚山梨酯80774 mg,所制备的阿托伐他汀钙纳米粒呈类球形,其平均粒径(71.99±13.62) nm,Zeta电位为(-31.48±2.46) mV,包封率为(91.27±1.7)%,载药量(9.58±0.22)%。结论:采用乳化-溶剂挥发法制备阿托伐他汀钙纳米粒处方及工艺适合,相关性质检测方法可行。