卵磷脂脂质体对老龄高脂兔动脉粥样硬化的影响

目的　了解口服卵磷脂脂质体对老龄高脂兔动脉粥样硬化的影响。方法　选择 5 0只新西兰兔 ,按体重、♀♂平均原则分为老龄用药组 (高脂食 +卵磷脂脂质体 ,A组 )、成年用药对照组 (高脂食 +卵磷脂脂质体 ,B组 )、老龄高脂对照组 (C组 )、成年高脂对照组 (D组 )、老龄空白对照组 (E组 )。每组 10只 ,老年兔龄 30mon ,成年兔龄 13mon。喂养15d后 ,A、B组分别隔日经口灌入卵磷脂脂质体溶液 ,C、D、E组灌入等量生理盐水 ,3mon后抽血 ,测定血清总胆固醇、甘油三脂、脂蛋白胆固醇、游离脂肪酸及主动脉条粥样硬化面积。结果　与C、D组比较 ,A、B组兔高密度脂蛋白胆固醇 (HDL C及HDL2 C )浓度明显增加 ;极低密度脂蛋白胆固醇 (VLDL C )、低密度脂蛋白胆固醇 (LDL C)、总胆固醇(TC)、甘油三脂 (TG)、游离脂肪酸 (FFA)浓度明显降低 (P<0 0 5～ 0 0 1) ,主动脉粥样硬化面积显著缩小 (P <0 0 5～0 0 1)。A、B两组间比较差异无显著性 (P >0 0 5 )。结论　口服卵磷脂脂质体能改善老龄高脂兔脂代谢 ,减轻动脉粥样硬化。     

卵磷脂治疗脂肪肝142例效果观察

肝脏是脂肪代谢的重要场所,当肝脏对脂肪合成能力增加和转运人血的能力下降时,脂类物质（主要为三酰甘油）在肝内蓄积,超过肝脏重量的5%或在组织学上50%以上的肝实质脂肪化时,即为脂肪肝.脂肪肝不是一个独立的疾病,而是由多种疾病引起的肝脏脂肪性变.我院2001年3月～2004年5月应用卵磷脂治疗脂肪肝142例,效果较好,现报告如下.     

绝经后妇女性激素变化对脂代谢的影响

流行病学研究表明 ,妇女绝经后冠心病的发生率是绝经前的 3～ 4倍。为探讨性激素的变化对脂代谢的影响 ,我们对 3 2例绝经后妇女性激素与血脂进行了测定 ,现报告如下。1　资料与方法1.1　一般资料　对照组 :3 7例 ,为 1999年 7月至 2 0 0 1年 4月来我院健康体检者 ,年龄 2 4～ 3 2岁 (平均年龄 2 7岁 ) ,月经规律 ,经内、外科检查 ,无其他疾病。绝经组 :3 2例 ,为 1998年 5月～2 0 0 1年 3月来我院就诊者 ,年龄 45～ 61岁 (平均年龄 5 2岁 ) ,均为自然绝经 1年以上者。无心、脑血管疾病 ,半年以上未服用过激素药物。1.2　方法　 ( 1)标本采…     

氢化与非氢化卵磷脂对阿霉素脂质体体内外稳定性的影响

目的研究卵磷脂(EPC)和氢化卵磷脂(HEPC)对阿霉素脂质体的体外泄漏及体内循环时间的影响.方法用透析法考察EPC及HEPC普通脂质体在37℃小牛血清及37℃,20℃和4℃PBS中的药物泄漏情况;用高效液相色谱法研究了EPC和HEPC长循环脂质体在大鼠体内的药物动力学.结果在37℃小牛血清中HEPC脂质体较EPC脂质体泄漏慢,而在PBS中则结果相反;大鼠体内药物动力学研究结果表明,HEPC长循环脂质体在血中的平均驻留时间(MRT)较EPC长循环脂质体长得多(23.3h vs 12.0h).结论HEPC长循环脂质体是靶向血管外部位的更好的药物载体.     

两性霉素B及其卵磷脂-胆固醇脂质体降解动力学研究

目的考察以卵磷脂、胆固醇为膜材制备的两性霉素B脂质体的稳定性及降解动力学。方法应用高效液相色谱法考察光和热对两性霉素B溶液及其脂质体中药物稳定性及降解动力学的影响,并拟合其降解动力学模型,求算降解半衰期。结果两性霉素B溶液及其脂质体光降解分别符合一级和零级动力学过程,降解半衰期分别为2.6和24.7d;热降解过程分别符合零级动力学和Higuchi方程;40℃下半衰期分别为27.8和1532.8d;60℃下半衰期分别为8.2和17.9d。结论脂质体可明显降低两性霉素B的光和热降解,延长药物降解半衰期,显著提高两性霉素B的稳定性。     

卵磷脂治疗脂肪肝142例效果观察

肝脏是脂肪代谢的重要场所,当肝脏对脂肪合成能力增加和转运人血的能力下降时,脂类物质(主要为三酰甘油)在肝内蓄积,超过肝脏重量的5%或在组织学上50%以上的肝实质脂肪化时,即为脂肪肝[1].脂肪肝不是一个独立的疾病,而是由多种疾病引起的肝脏脂肪性变.我院2001年3月～2004年5月应用卵磷脂治疗脂肪肝142例,效果较好,现报告如下.     

脂质体载体材料卵磷脂的制备及质量标准研究

目的：制备脂质体载体材料卵磷脂。方法：以新鲜鸡蛋为原料提取并制备了卵磷脂,并对卵磷脂的纯度,含量,氧化程度以及质量标准进行考察。结果：试验制备的卵磷脂为色谱均一的物质,含量高于98％,其氧化程度低,各项质量指标均符合美国药典规定。结论：结果表明,试验制得的卵磷脂可作为制备脂质体的载体材料。     

卵磷脂脂质体滴眼液治疗眼干燥症的研究

目的研究卵磷脂(PC)脂质体滴眼液治疗兔眼干燥症的疗效,并探讨其流变学性质。方法测定0.1%,0.2%和0.4%PC脂质体滴眼液的流变学性质,并通过建立兔眼干燥症模型,考察3种不同浓度的PC脂质体滴眼液的疗效。结果3种不同浓度的PC脂质体滴眼液均为非牛顿流体,且均可显著改善兔眼干燥症,PC在0.1%和0.2%浓度效果较好。结论PC脂质体滴眼液可有效治疗兔眼干燥症,且与其独特的流变学性质有关。     

蛋黄卵磷脂对高血脂大鼠血脂的影响

高血脂的严格定义应该为血脂紊乱或血脂异常。是指人体内血清脂质的浓度水平超出了正常范围。包括血清总胆固醇(TC)水平升高。血清甘油三脂(TG)水平升高。血清高密度脂脂蛋白胆固醇(HDL-C)水平异减低。是心脑血管疾病的主要危险因素之一,目前对其病因及治疗研究较多。现对此作一综述。高血脂究竟是许多疾病的原因还是结果。至今仍没有直接证据。一般认为,人机体血脂水平是遗传因素和环境因素相互作用的结果。     

复方丹参滴丸对实验性高血脂大鼠血清中TC、TG、LDL的影响

用大鼠建立高血脂症动物模型观察复方丹参滴丸对大鼠血脂各项生化指标的影响。结果表明,两个剂量的复方丹参滴丸(40mg/kg、120mg/kg)在预防给药和治疗给药试验中均可明显降低造型后大鼠血液中胆固醇(TC)、甘油三酯(TG)和低密度脂蛋白(LDL)的含量,升高高密度脂蛋白HDL/LDL的比值。     

Pharmacokinetics of lopromide Liposomes in Rabbits

Purpose. The dose-proportionality of pharmacokinetics of an iodinated contrast medium, iopromide, encapsulated into liposomes was investigated. Methods. Following single intravenous administration of 150 mg iodine/kg (potential diagnostic dose) and a five-fold higher dose in rabbits the pattern of elimination was studied until 7 d and the blood concentrations were monitored up to 72 h after administration. The iodine concentration in the liver was calculated on the basis of the blood concentration and related to the concentration measured in the rabbit liver. Results. The dose-normalized blood concentration-time profiles of the encapsulated iodine were not superimposable. Contrary to the low dose a steady-state concentration of 2.8 mg iodine/mL was observed in blood for 60 min after the high dose administration indicating a saturation of the liposomal liver uptake. For both doses the elimination of iodine occurred predominantly via the kidneys and was complete 7 d after administration. The dose-normalized amounts of iodine excreted with the urine were similar for both dose groups. From the blood data it was calculated that doses up to about 300 mg iodine/kg should result in a dose-proportional increase of liposomal liver uptake before saturation occurs. This was confirmed by the measured iodine liver concentrations after increasing the doses stepwise from 150 to 750 mg iodine/kg. Conclusions. In rabbits for the dose range 150 to 750 mg iodine/kg iopromide liposomes reveal dose-dependent pharmacokinetics due to a saturation in liver uptake which occurs for doses of 300 mg iodine/kg corresponding to 300 mg lipid/kg onwards.     

文蛤水解液降糖及降脂作用的实验研究

研究文蛤水解液的降血糖及降血脂作用。方法：给正常小鼠、四氧嘧啶诱导糖尿病小鼠及食物性高脂血症大鼠,分别口服文蛤水解液 １０ ｇ／（ｋｇ· ｄ）,测定血糖及血脂。结果：文蛤水解液能明显降低正常小鼠及糖尿病小鼠的血糖水平（Ｐ＜０．０５）,显著降低食物性高脂血症大鼠的血清甘油三酯（Ｐ＜０．０１）和血清胆固醇水平（Ｐ＜０．０１）。结论：文蛤水解液具有降糖及降脂作用。     

3种不同溶媒介质脂质体的制备及其初步稳定性考察

摘 要 目的：制备3种不同溶媒介质脂质体,即普通脂质体、乙醇脂质体、丙二醇脂质体,筛选及优化制备工艺,并初步考察其稳定性。方法: 以薄膜分散法制备普通脂质体,注入法制备乙醇脂质体和丙二醇脂质体。在相同的处方组成下,考察水化时间、水浴温度、旋转速度等因素对普通脂质体粒径分布的影响,醇水比例、搅拌速度、过膜方式等因素对乙醇脂质体和丙二醇脂质体粒径分布的影响,在此基础上运用正交设计对制备工艺进行优化。以3种不同溶媒介质脂质体的外观形态及平均粒径的变化为指标,分别于第0,1,15,30天取样评价其稳定性。结果:正交试验结果表明,薄膜分散法制备普通脂质体的最佳工艺条件为：水化时间60 min,水浴温度50℃,旋转速度200 r·min-1。注入法制备乙醇脂质体和丙二醇脂质体的最佳工艺条件为：醇水比例1∶〖KG-*2〗2,搅拌速度1 000 r·min-1,先0.45 μm后0.22 μm微孔滤膜的过膜方式。最佳工艺条件制备得到的3种脂质体均为封闭的单层囊状或多层圆球体,普通脂质体平均粒径(1 016.2±135.6) nm,乙醇脂质体平均粒径(578.7±89.2) nm,丙二醇脂质体平均粒径(351.4±53.8)nm。3种脂质体在30 d的观察期内都不稳定,放置15 d后出现明显的分层现象。结论:优化的最佳工艺制得3种不同溶媒介质脂质体粒径均为微纳米级,但稳定性较差,宜临用前配制。     

克班宁脂质体抗心律失常作用的研究

目的：比较克班宁(Crebanine,Cre)及其脂质体的抗心律失常作用。方法：分别采用氯化钡、乌头碱引起的大鼠心律失常模型,比较克班宁(Crebanine,Cre)及Cre脂质体抗心律失常作用。结果：对氯化钡所致的心律失常,Cre脂质体高、低剂量组(5mg/kg、2.5mg/kg),均能使恢复窦性节律鼠数、维持窦性节律至20min以上鼠数显著高于生理盐水组(P<0.01);Cre脂质体(5mg/kg)能使乌头碱所致大鼠VP、VT、VF、死亡时间显著延迟,与NS相比,差异具有显著性意义(P<0.01);与同剂量Cre溶液相比,Cre脂质体的VF出现的时间明显延长(P<0.01)。结论：克班宁脂质体对氯化钡所致的心律失常有一定治疗作用、对乌头碱引起的心律失常有一定预防作用。     

Protective Effect of Coenzyme Q10-loaded Liposomes on the Myocardium in Rabbits with an Acute Experimental Myocardial Infarction

Purpose We assessed whether the infusion of Coenzyme Q10-loaded liposomes (CoQ10-L) in rabbits with an experimental myocardial infarction can result in increased intracellular delivery of CoQ10 and thus limit the fraction of the irreversibly damaged myocardium. Methods CoQ10-L, empty liposomes (EL), or Krebs–Henseleit (KH) buffer were administered by intracoronary infusion, followed by 30 min of occlusion and 3 h of reperfusion. Unisperse Blue dye was used to demarcate the net size of the occlusion-induced ischemic zone (“area at risk”) while nitroblue tetrazolium staining was used to detect the final fraction of the irreversibly damaged myocardium within the total area at risk. Results The total size of the area at risk in all experimental animals was approx. 20% wt. of the left ventricle (LV). The final irreversible damage in CoQ10-L-treated animals was only ca. 30% of the total area at risk as compared with ca. 60% in the group treated with EL (p < 0.006) and ca. 70% in the KH buffer-treated group (p < 0.001). Conclusions CoQ10-L effectively protected the ischemic heart muscle by enhancing the intracellular delivery of CoQ10 in hypoxic cardiocytes in rabbits with an experimental myocardial infarction as evidenced by a significantly decreased fraction of the irreversibly damaged heart within the total area at risk. CoQ10-L may provide an effective exogenous source of the CoQ10 in vivo to protect ischemic cells     

高血压合并高血脂症患者血清铁含量的变化

目的探讨高血压合并高血脂症患者血清铁穴Fe雪含量变化及其临床意义。方法采用原子吸收光谱法和试剂盒分别检测了44例高血压合并高血脂症患者、42例单纯高血压病患者的血清Fe及胆固醇穴Ch雪、甘油三酯穴TG雪,并与30名正常对照组进行比较分析。结果高血压合并高血脂症患者的血清Fe及Ch、TG均明显高于单纯高血压组和对照组,血清Fe含量与Ch和TG及血压均呈显著正相关。结论Fe含量升高可能与高血压合并高血脂症的发生和发展有一定的关系。     

ATP-Loaded Liposomes Effectively Protect the Myocardium in Rabbits with an Acute Experimental Myocardial Infarction

Purpose We assessed whether the infusion of ATP-loaded liposomes (ATP-L) can limit the fraction of the irreversibly damaged myocardium in rabbits with an experimental myocardial infarction. Methods ATP-L, empty liposomes (EL), or Krebs–Henseleit (KH) buffer were administered by intracoronary infusion, followed by 30 min of occlusion and 3 h of reperfusion. Unisperse Blue dye was used to demarcate the net size of the occlusion-induced ischemic zone (area at risk) and nitroblue tetrazolium staining was used to detect the final fraction of the irreversibly damaged myocardium within the total area at risk. Results The total size of the area at risk in all experimental animals was approx. 20% wt. of the left ventricle. The final irreversible damage in ATP-L-treated animals was only ca. 30% of the total area at risk as compared with ca. 60% in the group treated with EL (p < 0.009) and ca. 70% in the KH buffer-treated group (p < 0.003). Conclusions ATP-L effectively protected the ischemic heart muscle in rabbits with an experimental myocardial infarction as evidenced by a significantly decreased fraction of the irreversibly damaged heart within the total area at risk. ATP-L may provide an effective exogenous source of the ATP in vivo to protect ischemically damaged cells.     

Efficacy and Safety of Phospholipid Liposomes in the Treatment of Neuro-psychological Disorders Associated with the Menopause: A Double-blind,Randomised, Placebo-controlled Study

SUMMARY

A double-blind, randomised, placebo-controlled clinical trial was performed to evaluate the efficacy and safety of phospholipid liposomes (Liposom® Forte) administered parenterally in the treatment of anxiety and depression linked to the menopause.

A total of 64 females aged 40-60 years were randomised to receive the active drug or placebo intramuscularly; 58 patients completed the study. Treatment lasted 60 consecutive days. One IM administration of 2?ml active drug or placebo every other day was carried out.

Efficacy was evaluated by the Hamilton Anxiety Scale (HAMA) and the Climacteric Index. An intention-to-treat analysis was performed, defined as all patients administered with at least one dose of the study medications with at least one return visit.

A highly significant (p?<?0.001) decrease in) HAMA total score in both groups was noted. However, the decline in the HAMA score was significantly greater in patients administered phospholipid liposomes after 40 days (p?=?0.006), 60 days of treatment (p?<?0.001) and at the last follow-up visit (p?<?0.001). Also, there were statistically significant differences between treatment groups after 60 days of therapy for individual items, such as anxious mood (p?=?0.006), tension (p?=?0.024) and fear (p?=?0.009), with significantly less patients experiencing these symptoms in the phospholipid liposomes-treated group.

When the Climacteric Index was evaluated, a highly significant (p?<?0.001) decrease in the total score in both groups was noted. However, the decline was significantly greater in patients administered phospholipid liposomes after 40 days of treatment (p?=?0.017), 60 days of treatment (p?=?0.0013) and at the last follow-up visit (p?=?0.0012). Significant differences between treatment groups were recorded after 60 days in asthenia (p?=?0.05), dizziness (p?=?0.024) and restlessness (p?=?0.019) in favour of the active treatment.

Twelve patients reported at least one adverse event, nine in the phospholipid liposomes group

and three in the placebo group (p?=?0.062). The most commonly reported event was drowsiness with two reports in each group.

These findings further demonstrate that phospholipid liposomes administered intramuscularly are active against mild anxiety and depressive symptoms in menopausal women.     

大豆磷脂对四氯化碳肝损伤大鼠的影响

目的评价益肝灵胶囊中辅料大豆磷脂的治疗作用。方法将实验动物分7组，即正常对照组，模型对照组，益肝灵片对照组，益肝灵胶囊对照组，大豆磷脂小、中、大剂量组。除正常对照组外，大豆磷脂组以大鼠腹腔注射四氯化碳复制实验性肝损伤模型后，给予大豆磷脂治疗，周期10d，并与益肝灵片及益肝灵胶囊进行对照。结果仅大剂量大豆磷脂能降低模型大鼠血清丙氧酸氨基转移酶（ALT），而对天门冬酸氧基转移酶（AST）及肝脏系数则无明显影响。而益肝灵胶囊和益肝灵片均能降低升高的ALT，AST和肝脏系数。结论益肝灵胶囊对肝脏的保护作用不是辅料卵磷脂所致，但一定剂量的卵磷脂可能对降低ALT有所帮助。     

氟伐他汀联合苯扎贝特治疗冠心病合并混合型高脂血症的临床观察

目的：观察氟伐他汀联合苯扎贝特治疗冠心病合并混合型高脂血症的调脂效果及安全性。方法：将我中心332例高脂血症患者随机分为4组,每组83例。A组口服氟伐他汀40mg·d^-1,B组口服苯扎贝特400mg·d^-1,C组口服氟伐他汀20mg·d^-1＋苯扎贝特400mg·d^-1,D组口服氟伐他汀40mg·d^-1＋苯扎贝特400mg·d^-1,4组疗程均为24周。观察患者血脂变化及不良反应等。结果：与治疗前比较,4组低密度脂蛋白胆固醇（LDL-C）均显著降低,高密度脂蛋白胆固醇（HDL-C）显著上升（P〈0．05）,且治疗后A、C、D组LDL-C显著优于B组（P〈0．001）,B、C、D组HDL-C显著优于A组（P〈0．001）。其中,D组各项指标治疗效果最佳。4组患者均具有较好的耐受性,均未见严重不良反应发生。结论：氟伐他汀40mg联合苯扎贝特400mg治疗混合型高脂血症疗效较好,能有效纠正各项临床指标,具有较好的安全性和耐受性。