早期十全大补汤联合肠内营养乳剂治疗胃癌术后(气血两虚证)喂养不耐受临床评价

目的探讨早期使用十全大补汤联合肠内营养乳剂(TP)治疗胃癌术后(气血两虚证)发生喂养不耐受(FI)的影响因素及对营养指标、中医证候积分的影响。方法回顾性分析术后早期行十全大补汤联合TP治疗的80例胃癌术后(气血两虚)患者的病历资料,根据是否出现FI分为耐受组(34例)和不耐受组(46例)。FI的相关影响因素进行单因素及多因素分析,并观察FI对患者营养指标、中医证候积分的影响。结果单因素分析显示,患者术后第1天下床活动时间、开始肠内营养(EN)的时间、使用营养泵、早期灌肠与FI的发生密切相关(P <0. 05);多因素Logistic回归分析显示,患者第1天下床活动时间≥2 h[OR=0. 022,P=0. 001,95%CI(0. 002,0. 223)]、使用营养泵[OR=0. 021,P=0. 000,95%CI(0. 003,0. 162)]是FI发生的独立危险因素;术后10 d,耐受组患者白蛋白(ALB)、血红蛋白(Hb)升高水平优于不耐受组(P <0. 05),中医证候积分显著低于不耐受组(P <0. 05)。结论胃癌术后(气血两虚证)患者早期给予十全大补汤联合TP治疗开始后,患者第1天下床活动时间不短于2 h、使用营养泵能有效减少FI的发生,并改善了患者的营养状态,减轻了中医临床症状。     

外源性一氧化氮抗日本血吸虫的实验研究

目的观察外源性一氧化氮(NO)抗日本血吸虫的效果。方法以蜂蜡为NO的吸收剂,在不同条件下用逆转乳化法制备NO乳状液,测定其中NO的含量,选择乳状液中NO含量最大的用于抗日本血吸虫试验。在小鼠感染日本血吸虫尾蚴后22天起灌服,剂量为0.5ml/d,连续灌服5d,心脏灌注法收集虫体计数,研究外源性NO抗日本血吸虫的效果。结果外源性NO中NO的最大含量为536.2μmol/L;对小鼠日本血吸虫有一定的杀虫效果,减虫率达45.0%,减卵率达42.7%。结论外源性NO对日本血吸虫有一定的抗虫作用。     

低分子肝素经大鼠胃肠道吸收的研究

目的考察低分子肝素(LMWH)溶液及乳剂在麻醉大鼠胃肠道的吸收情况以及磷脂对LMWH的促吸收作用.方法在体大鼠胃中给药、小肠及小肠各肠段循环液给药,一定时间后测定血液凝固时间的变化及循环液中药量的变化,以反映药物的吸收情况.结果LMWH在体小肠和十二指肠循环溶液及乳剂循环一定时间后,药量显著减少,血液凝固时间明显延长.结论LMWH在胃中无明显吸收,部分被破坏;在小肠中吸收,十二指肠吸收最好.磷脂乳剂对LMWH有一定的保护和促吸收作用.     

榄香烯乳与高聚金葡素联合治疗恶性胸腔积液

 自1995年1月～1997年6月采用随机分组的方法，比较榄香烯乳加高聚金葡素（治疗组）与单纯高聚金葡素（对照组）治疗78例恶性胸腔积液的临床疗效。结果显示治疗组有效率87.18％，对照组有效率53.84％。两组差异非常显著（P＜0.01）。治疗组主要不良反应为食欲不振、胸痛、发热。     

榄香烯与化疗药物联合作用对癌细胞株生长的影响

 用肾透明细胞癌细胞株KCC和红白血病细胞林K562作为靶细胞研究了中药榄香烯和化疗药物的体外协同应用对癌株生长的影响。单独用药情况下，KCC对榄香烯、阿霉素、5氟脲嘧啶均呈不同程度的抵抗，K562则相对较敏感。榄香烯合用阿霉素或5氟脲嘧啶后，对KCC的抑制率明显增强，其中榄香烯加阿霉素组效果要强于合用5-Fu，联合用药后对K562的抑制率也明显增强。经统计学分析：单独用药与联合用药之间差异显著（P＜0.01），实验结果对临床应用榄香烯治疗实质性肿瘤时选择良好的协同药物具有参考意义。     

碘油乳剂的制作及其对肝脏增强的实验研究

目的将40％碘油乳化成40％碘油乳剂，对其物理性质进行测定和观察，然后探讨其对动物肝脏的增强效应。材料和方法40％碘油10ml、蒸馏水15ml、两种适量的乳化剂及其他物质混合后形成初乳，应用乳均机和超声乳化机将初乳乳化成40％碘油乳剂。11只杂种犬，在不同时期静脉、肝动脉、肠系膜上动脉分别注射稀释为15％碘油乳剂及60％泛影葡胺，然后在不同时期行CT扫描。结果乳剂颗粒平均直径0．63u，95％在1.0u以下，最大不超过5．2u，放置12个月颗粒大小分布不变。静脉乳剂肝脏增强最大平均CT值为75HU，泛影葡胺为21．8HU（P＜0.01）；肝动脉乳剂最大平均CT值为120．5HU，泛影葡胺为50．7HU（P＜0．01）；间接门脉乳剂最大平均CT值为117．8HU，泛影葡胺为41．6HU（P＜0．01）。结论我们制作的碘油乳剂颗粒小、稳定性好、毒性低、显影力强。     

Interfacial Properties as Stability Predictors of Lecithin-Stabilized Perfluorocarbon Emulsions

ABSTRACT

The purpose of this study was to determine whether the addition of small quantities of minor lecithin components (phosphatidylinositol, phosphatidic acid, lysophosphatidylethanolamine, and cholesterol) and Pluronic F68 to lecithin could improve the stability of lecithin-stabilized perfluorocarbon emulsions. Attempts were made to correlate emulsion stability with interfacial properties (tension and charge). Dynamic interfacial tension was determined using a Teflon Wilhelmy plate method [reported previously (1)]. Emulsions were prepared by microfluidization. Microelectrophoresis was used to measure emulsion droplet charge, and photon correlation spectroscopy and Coulter analysis were used to determine emulsion stability as a function of droplet size. Thermal kinetic accelerated stability testing was conducted. Various droplet size parameters were used to compare emulsion stabilities, and an overall stability ranking, based on these parameters, was obtained for each emulsion. Small quantities of additives altered emulsion stability and these data were correlated with interfacial properties and initial droplet diameters. The addition of cholesterol to lecithin resulted in the most stable perfluorocarbon emulsion.     

Engineering of polymer–surfactant nanoparticles of doxycycline hydrochloride for ocular drug delivery

Abstract

Context: Physiologic barriers of the eye, short precorneal drug residence time and poor corneal penetration are the few reasons for reduced ocular bioavailability.

Objective: This study was aimed to develop novel polymer–surfactant nanoparticles of hydrophilic drug doxycycline hydrochloride (DXY) to improve precorneal residence time and drug penetration.

Materials and methods: Nanoparticles were formulated using emulsion cross-linking method and the formulation was optimized using factorial design. The prepared formulation was characterized for particle size, ζ potential, encapsulation efficiency, in vitro drug release and ex vivo drug diffusion studies. The antibacterial activity studies were also carried out against Escherichia coli and Staphylococcus aureus using the cup-plate method. In vivo eye irritation study was carried out by a modified Draize test in rabbits.

Results and discussion: The particle size was found to be in the range of 331–850?nm. About 45–80% of the drug was found to be encapsulated in the nanoparticles. In vitro release demonstrated sustained release profile. Lower flux values in case of nanoparticles as compared to DXY pure drug solution in ex vivo diffusion studies confirmed the sustained release. The nanoparticles were found to be significantly effective (p?<?0.001) than DXY aqueous solution due to sustained release of doxycycline from nanoparticles in both the E. coli and S. aureus strains. The formulation was found to be stable over entire stability period.

Conclusion: The developed formulation is safe and suitable for sustained ocular drug delivery.     

新型硫酸头孢喹肟乳液猪体内药物浓度测定

目的 测定硫酸头孢喹肟乳液在猪体内的血药浓度。方法 以吐温80、斯盘85为乳化剂,通过表面活性剂复配方法制备了新型硫酸头孢喹肟乳液制剂。与市售硫酸头孢喹肟混悬液对比研究硫酸头孢喹肟乳液生物等效性,将实验猪随机分组,并分别肌注硫酸头孢喹肟乳液及混悬液,采用高效液相色谱的方法测定其血药浓度,采用DAS 2.0药动学程序计算药动学参数。试验优化了硫酸头孢喹肟血液样品的处理方法,并考察了方法专属性。结果 硫酸头孢喹肟分析方法在0.10~10.00μg/mL之间呈良好的线性关系,回归方程：y=157.06x+18.347,r2=0.9996 (n=5),日内变异系数低于5.76%,日间变异系数低于8.35%;样品的平均回收率为93.4%~97.7%,完全符合生物样品分析要求;两组药动学行为均符合一级吸收二室模型,其主要药动学参数为：吸收半衰期(T1/2a)分别为(0.842±0.015)h和(0.825±0.021)h;达峰时间(Tmax)分别为(1.357±0.043)h和(1.345±0.051)h;峰浓度(Cmax)分别为(3.386±0.083)μg/mL和(3.526±0.091)μg/mL;消除半衰期(T1/2β)分别为(1.054±0.059)h和(1.025±0.087)h;药时曲线下面积(AUC0~t)达(12.706±0.553)mg·h/L和(12.787±0.394)mg·h/L。对两实验组AUC0~t、Cmax、Tmax进行差异性分析,3种药代参数组间差异均不显著(P＞0.05)。结论 自制硫酸头孢喹肟乳液与市售硫酸头孢喹肟混悬液具有生物等效性。     

The optimization of technological processes,stability and microbiological evaluation of innovative natural ingredients-based multiple emulsion

Abstract

For the last couple of decades, multiple emulsions were prepared either by the re-emulsification of primary emulsion or they were produced by an emulsion inversion and their technological peculiarities were widely investigated. The aim of our study was to investigate and determine the optimal technological parameters of innovative multiple emulsion, prepared directly—by addition of ethanolic rosemary extract in the presence of polymeric emulsifier—and evaluate its stability by experimental surface response design approach. The results revealed that simplified W/O/W emulsification process is stirring time and stirring speed sensitive: the change of stirring time from 5 to 15?min at 600?rpm resulted in increased viscosity (from 1705.6?±?62.2 to 3364.1?±?112.5?mPA/s) and smaller oil droplet size (from 33.09?±?1.51 to 17.81?±?0.78?μm), though the conductivity increased from 800?±?2 to 882?±?2 μS/cm (p?<?.05). The second mixing stage (1000?rpm) had a negative effect on the conductivity of W/O/W emulsion because of the inner aqueous phase encapsulation efficiency. Ethanolic rosemary extract was used as multifunctional agent: not only to form multiple emulsion but also to preserve it; microbiological assay confirmed its effectiveness. A stable W/O/W type drug delivery system was successfully created without additional technological stages, phase inversion or surfactants.