精制蛋黄卵磷脂亲水-亲油平衡值测定及其在鸦胆子油乳注射液中的应用

目的以亲水-亲脂平衡值为指标考察精制蛋黄卵磷脂在水中和油中的分散特性并研究其在鸦胆子油乳注射液中的应用。方法采用核磁共振波谱(NMR)法,根据其化学位移值及亲水基团与亲油基团质子数相对比值(R)计算亲水-亲脂平衡值。结果精制蛋黄卵磷脂在水中具有良好的分散性。结论可用精制蛋黄卵磷脂代替豆磷脂作乳化剂制备鸦胆子油乳注射液。     

调脂积冲剂对脂肪肝大鼠胰岛素抵抗的影响

目的——探讨调脂积冲剂防治脂肪肝的有效性、可靠性,及其对胰岛素抵抗的影响。方法——采用酒精合并高脂乳剂建立大鼠脂肪肝模型,以易善复和六味地黄丸为阳性对照,检测TC、TG、HDL-C、LDL-C、ALT、GGT和FBG,采用酶联免疫法测定血清胰岛素含量。胰岛B细胞功能评价采用稳态模式评估法,即胰岛素抵抗指数（HOMA-IR）=（FBG）·FINS／22．5。结果——调脂积冲剂能降低ALT、CGT、TC、TG、LDL-C、FBC和FINS的含量,降低胰岛素抵抗指数。讨论——调脂积冲剂能有效防治脂肪肝,其机制可能与其改善胰岛素抵抗有关。     

Drug distribution in enteric microparticles

The aim of this study was to assess the distribution of three fluorescent drug or drug-like molecules in enteric microparticles. Microparticles were prepared using the pH-responsive methylmethacrylate polymer Eudragit L by an emulsion solvent evaporation process. In the process drug and polymer are dissolved in ethanol, and dispersed in a liquid paraffin external phase using sorbitan sesquioleate as stabiliser. The incorporation and distribution of riboflavin, dipyridamole and acridine orange into these microparticles were investigated using confocal laser scanning microscopy (CLSM). The influence of the physicochemical properties of the molecules (solubility in the inner phase, partition coefficient [ethanol/paraffin]) on the distribution, encapsulation efficiency and pH-responsive dissolution behaviour of the microparticles were examined. The drug that tended to partition in ethanol rather than liquid paraffin (riboflavin) was efficiently encapsulated and evenly distributed. In contrast, compounds which partitioned in favour of the liquid paraffin localised towards the surface of the microparticles and exhibited lower encapsulation efficiency (dipyridamole and acridine orange). All three sets of drug-loaded microparticles showed a limited release in acid (<10% release); drug distribution appeared to have a minimum effect on drug release. This microparticle technology has the potential to provide effective enteric drug release with a wide variety of molecules.     

HIFU联合相变氟碳乳剂损伤兔肝脏的二维超声实时监控

目的探讨二维超声实时监控HIFU（high intensity focused ultrasound）,联合相变氟碳乳剂损伤兔肝脏的可行性。方法使用同一聚焦超声换能器,辐照深度、功率一致条件下,静脉注射等量相变氟碳乳剂（实验组）或生理盐水（对照组）后HIFU辐照兔肝脏,测量辐照靶区的灰度值、回声增强区的大小,解剖测量凝固性坏死灶的大小。结果对照组HIFU辐照兔肝脏所产生的灰度值、回声增强区体积和最大面积小于实验组,凝固性坏死灶的最大截面积、体积也小于实验组,能效因子大于实验组。回声增强区最大面积与凝固性坏死灶最大截面积、体积之间存在定量关系。结论二维超声可实时监控相变氟碳乳剂存在条件下的HIFU损伤,相变氟碳乳剂提高了HIFU的损伤效率。     

脂肪乳剂预处理对大鼠布比卡因、左布比卡因致心脏毒性的影响

目的探讨脂肪乳剂对大鼠布比卡因、左布比卡因致心脏毒性的影响。方法成年健康雄性SD大鼠72只,体重220-250g,随机分为五组（n=8）。A组：生理盐水对照组,B组：布比卡因组,C组：布比卡因＋脂肪乳组,D组：左布比卡因组,E组：左布比卡因＋脂肪乳组。其中B、C、D、E组分为取材组和致死组两个亚组（n=8）。A组以3ml.kg-1.min-1的速率持续静脉泵入生理盐水6min。B、C、D、E组以3ml.kg-1.min-1的速率持续静脉泵注生理盐水或脂肪乳5min,以2mg.kg-1.min-1持续静脉泵局麻药1min。在取材组中,泵注1min局麻药后处死大鼠;致死组中,持续泵注局麻药直到大鼠心跳停止。记录给药前动物的基础血压（HR）、心率（BP）,并记录动物出现心律失常（以QRS延长至90ms）、出现心跳停止时的时间（心电图示心脏停搏后观察1min不再出现心电波形为标准）,同时计算各对应时局麻药的累积剂量。对照组及取材组断头法处死,迅速取出心脏,液氮冷冻待测ATP酶活性。结果致死组任意两组比较差异均有统计学意义（P〈0.05）,各组ATP酶含量比较：A组〉E1〉D1〉C1〉B1,任意两组比较差异均有统计学意义（P〈0.05）。结论左旋布比卡因的毒性低于布比卡因。预先给予脂肪乳注射液可明显减轻布比卡因和左旋布比卡因对大鼠的心脏毒性,其机制可能与增加心肌ATP酶活性有关。     

灯盏花素口服亚微乳剂的制备研究

目的制备灯盏花素口服乳剂。方法过伪三元相图法以乳剂外观作为标准优选复合乳化剂的组成,再经过正交实验确定了最优处方与制备工艺。结果本实验采用机械法制备所得的灯盏花素乳剂为性状稳定的乳白色液体。结论本实验制备的乳剂稳定、粒径符合亚微乳剂的标准。     

Preparation and evaluation of ketoprofen floating oral delivery system

A sustained release system for ketoprofen designed to increase its residence time in the stomach without contact with the mucosa was achieved through the preparation of floating microparticles by the emulsion-solvent diffusion technique. Four different ratios of Eudragit S100 (ES) with Eudragit RL (ERL) were used to form the floating microparticles. The drug retained in the floating microparticles decreased with increase in ERL content. All floating microparticle formulations showed good flow properties and packability. Scanning electron microscopy and particle size analysis revealed differences between the formulations as to their appearance and size distribution. X-ray and DSC examination showed the amorphous nature of the drug. Release rates were generally low in 0.1 N HCl especially in presence of high content of ES while in phosphate buffer pH 6.8, high amounts of ES tended to give a higher release rate. Floating ability in 0.1 N HCl, 0.1 N HCl containing 0.02% Tween 20 and simulated gastric fluid without pepsin was also tested. The formulation containing ES:ERL1:1 (FIII) exhibited high percentage of floating particles in all examined media.     

Minoxidil-containing dosage forms: skin retention and after-rinsing hair-growth promotion

Three kinds of topical dosage forms of minoxidil (MXD), namely vesicles, double emulsions, and an inclusion complex with hydoxypropyl- β-cyclodextrin (HP- β-CD), were prepared. The skin retention of MXD in the preparations was evaluated in vitro using hairless mouse skins. After applying the preparations onto the skin and rinsing it, the amount of the drug left on the skin was determined using HPLC. Retention was the highest when the drug was encapsulated in cationic vesicles. Nonionic vehicle, the double emulsion, and HP- β-CD left no significant amount of the drug after rinsing the skin. Thus, an ionic interaction between the cationic vehicle and negatively charged skin is likely responsible for the relatively high skin retention. In vivo hair growth-promotion effect of each dosage form was investigated, in which the sample application onto the clipped backs of female mice (C57BL6) and the subsequent rinsing of the backs were done once a day for 30 days. Only MXD in the cationic vesicles had hair growth promotion effect, possibly due to significant skin retention.     

超滤萃取法提取抗生素

目的：传统的抗生素提取工艺中，溶剂萃取过程中的乳化现象既影响萃取收率和产品质量，以及动力消耗一直是未能很好解决的难题。方法：本文介绍了一种新的提取方法：超滤／萃取法。结果：该方法萃取过程不发生乳化现象，青霉素G的萃取收率平均比原工艺高2％，且青霉素G钾盐质量有明显提高。结论：该方法可以在实际生产中得到应用。     

榄香烯乳治疗恶性胸腔积液的临床观察

恶性胸腔积液是晚期癌症的一个常见并发症,常引起胸痛及呼吸困难,其发展迅速,甚至可危及生命,因此,有效地控制恶性胸腔积液埘提高患者生存质量,延长生存期有重要的意义.采用榄香烯乳治疗恶性胸腔积液,取得了较好的疗效,现将结果报告如下.