髂内动脉注入鸦油乳对狗正常膀胱组织影响的研究

目的 为鸦油乳掏膀胱肿瘤生长提供组织学依据。方法 正常狗随机分为：注药组（７只）和对照组（３只）,分别经髂内动脉注入鸦油乳０．１ｍｇ／ｋｇ、美蓝０．１ｍｌ／ｋｇ。１周后,随机活检膀胱各个部位作光镜及电镜观察。结果 注药组光镜可见粘膜上皮细胞脱落、坏死、肌层和浆膜充血、水肿、坏死以及急、慢性炎性细胞浸润;电镜发现在微血管内有鸦油乳微栓形成,并见细胞质膜结构的破坏。而对照组未发现明显变化。结论 鸦油乳     

液相色谱-质谱测定鸦胆子油脂肪乳注射液在癌症患者体内的血药浓度

目的 建立液相色谱-质谱(LC-MS)法测定癌症患者单剂量滴注鸦胆 子油脂肪乳后体内油酸浓度。方法 用自身对照试验设计,7名癌症患者,第3 天不给药,抽取不同时间点空白血浆样品;第5天,单剂量滴注鸦胆子油脂肪乳 注射液100 mL,滴注开始后,抽取不同时间点血浆样品,60 min滴完,用LC- MS法测定血药浓度。结果 线性范围为2．44-156 mg·L-1;日内、日间变异 系数均<14％;7名癌症患者单剂量滴注鸦胆子油脂肪乳注射液100 mL后,主 要药代动力学参数:tmax=(1．08±0．19)h,Cmax(95．20±29．10)mg·L-1, AUC0-7h=(265．67±59．32)mg·h·L-1,t1／2=(12．14±6．42)h。结论 本法 适用临床测定血浆中油酸浓度。     

鸦胆子油微乳的制备及稳定性研究

目的研究鸦胆子油微乳的制备、稳定性及微乳中药物含量的测定方法。方法选用MCT(辛葵酸甘油三脂)为油相,大豆卵磷脂为表面活性剂,乙醇为助表面活性剂,在制备三元相图的基础上,考察微乳的组分对微乳形成的影响。结果大豆卵磷脂为乳化剂形成微乳系统所需表面活性剂的量为20%～30%。结论采用微乳作为药物载体制备口服鸦胆子油微乳是一种很好的药物传递系统。     

Antimalarial and cytotoxic quassinoids from the roots of Brucea javanica

Two new quassinoids, brujavanol A (1) and brujavanol B (2), along with five known quassinoids (3–7), were isolated from the roots of Brucea javanica. Their structures were elucidated by spectroscopic methods. The antimalarial and cytotoxic activities of the isolated compounds were also assessed. Compounds 1 and 2 exhibited significant in vitro cytotoxicity against human oral cavity cancer (KB) cells with IC₅₀ values of 1.30 and 2.36 μg/ml, respectively, whereas compound 3 showed excellent antiplasmodial activity against the Plasmodium falciparum strains, K1 (IC₅₀ = 0.58 μg/ml).     

鸦胆子油乳注射液及配置后静脉输液的室温稳定性研究

目的 考察说明书中贮存条件要求冷藏,且须临用前即配即用的鸦胆子油乳注射液的原液和稀释后的静脉输液在室温(25 ℃)下的稳定性,为该药品的临床管理与使用提供依据。方法 模拟临床给药剂量和给药时间,考察性状、pH、渗透压、颗粒细度和油酸含量在室温下放置不同时间点的变化。结果 在室温下,鸦胆子油乳注射液原液放置72 h质量稳定,配置后静脉输液(30 mL∶250 mL 0.9%生理盐水)在24 h内各项理化指标均无明显变化。结论 鸦胆子油乳注射液在医院内部的短时间药物配送无需严格实施冷链管理;配置后静脉输液室温放置24 h稳定,无需“即配即用”。     

Suppression of human hepatocellular cancer cell proliferation by Brucea javanica oil-loaded liposomes via induction of apoptosis

Introduction

Hepatocellular carcinoma (HCC) is a type of malignancy with high incidence and poor prognosis. Brucea javanica is extracted from Simaroubaceae plants. It is found to have low toxicity but high anti-cancer efficiency. The aim of this study is to determine the effects of Brucea javanica oil-loaded liposomes (BJOL) on human hepatocellular cancer cell line HepG2. The related molecular mechanisms were determined.

Material and methods

Morphologic changes of HepG2 cells were observed by transmission electron microscope after treatment with BJOL in vitro. Cell proliferation was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay after cell treatment with different doses of BJOL. Flow cytometry was performed. Nude mice were divided into 4 groups randomly and treated with different doses of BJOL. The apoptosis hepatocellular carcinoma was detected by TUNEL.

Results

Proliferation of HepG2 was inhibited significantly by BJOL in a dose-dependent manner (2.5 mg/l or 5 mg/l). Compared with the animal models treated with the negative control, the animal models in the BJOL group had higher weight and lower metastasis rates (p < 0.01). The rate of apoptosis in hepatocellular carcinoma tissue of the BJOL groups was increased when compared with the control group (p < 0.05).

Conclusions

Brucea javanica oil-loaded liposomes inhibits proliferation of HepG2. The effect appears to be dose-dependent, possibly by inducing apoptosis of cancer cells.     

鸦胆子油乳注射液联合卡培他滨治疗晚期结肠癌的疗效分析

目的研究鸦胆子油乳注射液联合卡培他滨治疗晚期结肠癌的临床疗效及毒副作用,为延长晚期结肠癌患者的生存时间提供指导。方法将36例晚期结肠癌患者随机分为治疗组和对照组,对照组患者采用卡培他滨(1250mg/m2,bid,口服,共14 d)进行化疗,治疗组在对照组基础上再加用鸦胆子油乳注射液(30mL静脉注射,qd,共7 d)进行联合治疗,3周为一个疗程,共8个疗程。对两组患者进行24个月的随访观察,比较两组的疗效及毒副作用和生存时间。结果治疗组的受益率显著高于对照组(P0.05),但两组总有效率比较差异不显著(P0.05);对两组患者的治疗效果进行24个月随访观察,观察组的DFS(%)为16(66.67%),OFS(%)为11(45.83)均高于对照组的7(58.33%)、5(41.67%),但是差异不具有统计学意义(P0.05);中性粒细胞减少、血小板减少在两组间差异具有统计学意义(P0.05),对照组的发生率明显高于治疗组。其他不良反应在两组间比较差异不具有统计学意义(P0.05);采用寿命表法计算两组中位生存期(治疗组为12个月、对照组9个月),两组比较差异不具有统计学意义(Z=2.688,P=0.1010.05)。结论鸦胆子油联合卡培他滨治疗晚期结肠癌虽然对患者生存时间和疗效上差别不大,但是可以提高总体受益率,并且可以降低患者化疗的不良反应。     

鸦胆子油乳协同周剂量TX方案治疗晚期胃癌的疗效研究

摘 要 目的：评价鸦胆子油乳注射液协同周剂量TX方案治疗晚期胃癌的临床疗效。方法：42例晚期胃癌患者随机分为观察组（给予鸦胆子油乳注射液联合周剂量用剂量TX方案）19例和对照组（给予单纯周剂量TX方案化疗）23例。入组患者均至少接受2个周期以上的化疗。观察比较两组近期疗效、生活质量和生存期。结果：观察组近期有效率为63.2%,显著高于对照组的8.7%(P<0.05);观察组疾病控制率为94.7%,对照组为87.0%,差异无统计学意义( P>0.05)。观察组中位生存时间为741 d,显著高于对照组的359 d( P<0.05)。 结论：鸦胆子油乳注射液联合周剂量TX方案治疗晚期胃癌可明显提高患者化疗的近期疗效,延长患者的生存期。     

鸦胆子油乳联合阿帕替尼及替莫唑胺治疗复发性恶性脑胶质瘤

目的 探讨鸦胆子油乳联合阿帕替尼及替莫唑胺治疗复发性恶性脑胶质瘤患者的临床疗效、免疫功能影响及不良反应.方法 选取2016年6月至2018年12月期间郑州大学第一附属医院复发性恶性脑胶质瘤患者52例,随机分为2组,A组26例应用阿帕替尼及替莫唑胺治疗,B组26例应用鸦胆子油乳联合阿帕替尼及替莫唑胺治疗,比较2组临床疗效...     

腹腔置管引流联合羟基喜树碱、鸦胆子油序贯给药治疗恶性腹腔积液

目的探讨腹腔置管引流联合羟基喜树碱、鸦胆子油序贯给药治疗恶性腹腔积液的疗效和安全性。方法选择72例伴有中、大量恶性腹水的晚期肿瘤患者,采用腹腔置管引流尽量放干腹水后,腹腔内注射药物羟基喜树碱20 mg,地塞米松10 mg,多巴胺60 mg,速尿40mg,夹闭引流管6 h后将鸦胆子油50 mL注入腹腔,1周后重复,共2~4次。结果全组腹水完全缓解率为20%(15/72),部分缓解率为50%(36/72),腹水控制有效率为70%(51/72)。主要毒性反应是白细胞、血小板下降。结论腹腔置管引流联合羟基喜树碱、鸦胆子油序贯给药治疗恶性腹腔积液具有较好的疗效和安全性。