羟基喜树碱自乳化传递系统的处方筛选和体外评价

筛选和制备羟基喜树碱自乳化传递系统的处方并进行体外评价.以平衡质量浓度方法考察了羟基喜树碱在不同的油相、乳化剂和助乳化剂中的质量浓度,通过三元相图辅助筛选处方的组成,采用星点设计-效应面法优化处方中各组分的比例,筛选和制备了羟基喜树碱自乳化传递系统.考察自乳化制剂的粒径、累积溶出度、自乳化速率、微乳形态及其初步稳定性等.筛选出由m(氢化玉米油)(t) m(辛酸癸酸甘油酯)=1∶1为混合油相,m(聚氧乙烯蓖麻油)(t)m(辛酸葵酸聚乙二醇甘油酯)=2∶1为混合乳化剂,二乙烯基乙二醇单乙醚为助乳化剂和羟基喜树碱组成的自乳化传递系统.所得的优化处方可自发形成均匀球状液滴,微乳平均粒径在30 nm左右且分布窄,自乳化速率在5 min以内,溶出度在60 min内达到90％以上,而且制剂稳定性良好.通过处方研究确定了最优处方,研制了羟基喜树碱自乳化传递系统.     

环保节能型水性环氧树脂涂料的研制

利用相对分子质量低的双酚A型环氧树脂、二乙烯三胺和脂肪族环氧化合物合成自乳化环氧树脂乳液和水性固化剂,介绍了乳化剂和固化剂的设计原理。制备了水性环氧树脂涂料,考察了涂料组成对涂料性能的影响。     

自乳化法制备水性聚氨酯丙烯酸酯核壳复合乳液

通过自乳化法制备了丙烯酸改性的水性聚氨酯复合乳液。FT-IR和TEM测试表征,聚氨酯丙烯酸酯乳液混合均匀,粒子呈核壳结构。研究结果表明：改性后聚氨酯的耐热性有一定程度提高。当n（甲基丙烯酸甲酯）：n（聚氨酯）在1．5附近时,断裂伸长率、硬度及耐水性等综合指标最佳。     

Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol

Carvedilol has been made into a novel osmotic pump tablet which includes Gelucire 44/14, Lutrol F68, Transcutol P, silicon dioxide, mannitol, citric acid, and sodium hydrogen carbonate. The Self-emulsifying osmotic pump tablet (SEOPT) has two outstanding features. It could improve the bioavailability of carvedilol by self-emulsifying drug delivery system (SEDDS), control the release rate and make the plasma concentrations more stable by elementary osmotic pump tablet. The results of transmission electron microscope (TEM) and particle size assessment showed that the shape of the resultant emulsion was round and regular, the average diameter of the particles was 246 nm. Since the solubility of carvedilol was improved by the emulsion, the elementary SEOPT could guarantee a complete release of carvedilol under the osmotic pressure of mannitol. The cumulative release at 12 hr was 85.18%. Therefore the disadvantage that lipophilic drugs can not be released completely when prepared into elementary osmotic pump tablet was resolved. The results of Differential scanning calorimetry (DSC), Infrared spectroscopy (IR) and X-ray diffraction diffraction (XRD) proved that carvedilol was amorphous in the preparation. The relative bioavailability of carvedilol in beagle dogs was 156.78%. The plasma concentrations were more stable compared with that of commercially available tablet (Luode®). And the in vitro and in vivo correlation was good (r = 0.9725). Therefore, the elementary SEOPT developed in this paper might provide a new idea for preparing lipophilic drugs into osmotic pump tablet conveniently.     

Self-emulsifying bifendate pellets: preparation,characterization and oral bioavailability in rats

In this study, a self-emulsifying pellet (SEP) was prepared in order to improve the bioavailability of bifendate (DDB). First, a liquid self-emulsifying drug delivery system (SEDDS) was formulated, and then further developed into the SEP by extrusion/spheronization technology using the reconstituted emulsion as the adhesive. The optimized liquid SEDDS consisted of Miglycol^® 840, a mixture of Cremorphor^® EL and Solutol HS^® 15 (1:2, w/w), and Transcutol HP as the oil phase, the surfactant and the co-surfactant at a weight ratio of 40:45:15 (w/w/w), respectively. The SEP were prepared using a mixture of MCC, lactose, and mannitol (45:45:10, w/w/w) as solid adsorbents. The SEP with 40% (w/w) of the liquid SEDDS was round-shaped with a uniform size (800–1000 µm). There was no difference in droplet size between the emulsions obtained from the liquid SEDDS or the SEP (169.8 ± 6.3 nm and 163.7 ± 3.8 nm). Compared with that of DDB pills (less than 20%), in vitro release of DDB from the SEP (over 80% within 60 min) was significantly enhanced in 0.1N HCl, although slower than that of the liquid SEDDS (over 80% within 5 min). AUC of DDB of the SEP after oral administration in rats exhibited 2.36-fold greater than that of DDB pills and no significant difference compared with that of the liquid SEDDS. In conclusion, our studies illustrated that extrusion/spheronization technique could be a useful method to prepare this SEP and it could be a promising way for enhancing oral bioavailability of poorly water-soluble drugs.     

自乳化聚酯树脂汽车中涂漆的合成及性能研究

用逐步聚合法合成了聚酯树脂,用苯偏三酸酐(TMA)在聚酯分子链末端引入羧基以赋予其自乳化性能。讨论了原料,合成工艺条件,TMA用量对聚酯树脂及其水分散体性能的影响。采用GPC分析了封端前后的聚酯树脂的相对分子质量及其分布,以FTIR检测了聚酯树脂及其固化漆膜的结构与变化。结果表明,氮气保护下,当酯化、缩聚反应温度均为240℃,反应时间均为2h并保持反应体系的压力低于2kPa时,可获得高分子质量低酸值的聚酯树脂,在酸值(KOH)>15mg/g的封端树脂中加入三乙胺中和后可获得水分散性优良、储存稳定性高和表观粘度低的水分散体。用酸值(KOH)在10～20mg/g的封端聚酯树脂与六甲醇醚化的三聚氰胺甲醛树脂配制成水性涂料,其固化漆膜具有优良的综合性能,适于用作汽车中涂漆。     

槟榔油急性毒理试验及其自微乳特性研究

研究槟榔油的毒理安全性及微乳化特性,研制出槟榔油自乳化传递系统,以便提高槟榔油的生物利用度。通过槟榔籽油对SD大鼠灌胃给药急性毒性试验,研究其安全性;通过溶解度试验、浊点测试、三相图的绘制和星点设计-效应面法的优化等试验,以自微乳乳化前后表征、微乳液粒径,Zeta电位为指标,优化筛选出各组分的最佳组合和最适配比。结果表明,进行毒性试验的动物均未见明显的毒性症状,体重未见明显影响,各主要生命器官剖检均未见异常;槟榔油自微乳的最佳配方为:槟榔油(19.56%)、聚氧乙烯氢化蓖麻油(54.31%)、乙二醇单乙基醚(26.13%),平均粒径为54.34 nm,zeta电位为-33.82 mV。槟榔油安全范围大,无毒副作用,制备槟榔油自微乳稳定性好。     

自乳化叶黄素制剂的制备和性质研究

研究以叶黄素为原料,通过单因素实验,分析油溶介质、溶解温度、溶解时间对自乳化叶黄素产品的影响,确定油溶介质和最佳的工艺条件。从产品质量和稳定性入手,通过正交实验对非离子型表面活性剂和助表面活性剂进行筛选,确定透明自乳化叶黄素制剂配方:叶黄素:6%、紫苏油:10%、dl-a生育酚:1.5%、吐温-80:6%、蔗糖酯S-15:2%、司盘-40:1.5%、松香甘油酯:3%、甘油:70%,并对其性质进行研究。      

西罗莫司自乳化缓释微丸的制备及对淋巴细胞的作用研究

采用挤出滚圆法,以羟丙甲基纤维素钠为主要骨架型缓释材料制备出西罗莫司自乳化缓释微丸,考察制备工艺中挤出速度、滚圆速度、滚圆时间对目标速率影响并对淋巴细胞作用的研究。结果表明:西罗莫司自乳化缓释微丸的目标收率为(92.8±2.51)%(n=3),采用挤出速度为挤出速度为65 r·min~(-1);滚圆速度为650 r·min~(-1);滚圆时间为3 min最适宜;西罗莫司缓释微丸能够抑制淋巴细胞的增值的活性,随着时间增长,抑制作用增强。以上表明:采用该方法为西罗莫司缓释微丸研究提供新的方法。