维A酸维生素C棕榈酸酯泡囊的体外释放、经皮渗透和皮肤贮留研究

目的 研究维生素C棕榈酸酯泡囊作为维A酸载体时,主药的体外释放、经皮渗透和皮肤贮留情况。方法 采用Franz扩散池测定维A酸从载体中的释放速度,扩散池与供给池之间为纤维素膜(截留分子量8 000~14 000),扩散池面积为2.92 cm²。体外透皮试验用小鼠、大鼠或兔子背部皮肤替代半透膜。在体外透皮试验完结后,取下皮肤,剪碎匀浆,用50%异丙醇-生理盐水提取,提取液处理后用HPLC测定药物浓度。结果 结果表明维A酸释放速率和累积经皮渗透量大于市售乳膏,同时具有较高的皮肤贮留量。结论 维生素C棕榈酸酯泡囊作为维A酸载体有助于增加局部药物浓度。     

维A酸维生素C棕榈酸酯泡囊的体外释放、经皮渗透和皮肤贮留研究

目的研究维生素C棕榈酸酯泡囊作为维A酸载体时,主药的体外释放、经皮渗透和皮肤贮留情况。方法采用Franz扩散池测定维A酸从载体中的释放速度,扩散池与供给池之间为纤维素膜（截留分子量8000～14000）,扩散池面积为2.92cm^2。体外透皮试验用小鼠、大鼠或兔子背部皮肤替代半透膜。在体外透皮试验完结后,取下皮肤,剪碎匀浆,用50%异丙醇-生理盐水提取,提取液处理后用HPLC测定药物浓度。结果结果表明维A酸释放速率和累积经皮渗透量大于市售乳膏,同时具有较高的皮肤贮留量。结论维生素C棕榈酸酯泡囊作为维A酸载体有助于增加局部药物浓度。     

维生素C棕榈酸酯再肿瘤治疗中的研究进展

近年来,维生素C的抗肿瘤作用已引起了人们的广泛关注,但维生素C需较高剂量才可达到抗肿瘤作用,且化学性质不稳定,使其临床应用受到了限制.为了解决上述问题,研究者一直致力于维生素C衍生物的合成.维生素C棕榈酸酯作为维生素C的脂溶性衍生物,在理化性质、抗肿瘤活性等方面具有较多的优势.本文从维生素C棕榈酸酯的理化特征、抗肿瘤活性、机制和应用等方面对其在肿瘤治疗中的研究情况进行综述,为其在临床肿瘤防治中的研究提供依据.     

HPLC法测定复合维生素制剂中全反式维生素A棕榈酸酯的含量

摘 要 目的：建立复合维生素制剂中全反式维生素A棕榈酸酯的含量测定方法。方法: 采用HPLC法,色谱柱：Apollo Silica (250 mm×4.6 mm,5 μm);流动相：正己烷 异丙醇（999.5∶0.5）;流速：1.0 ml·min^-1;柱温：30 ℃;检测波长：325 nm;进样量：100 μl。结果: 全反式维生素A棕榈酸酯的线性范围为0.2260～0.6780IU·ml^-1（相当于0.1243～0.3729 μg·ml^-1,r=0.999 9）,平均回收率为99.86%,RSD为0.64%（n=9）。结论: 本法简便、准确、灵敏度高、重复性好、通用性强,可用于复合维生素制剂中全反式维生素A棕榈酸酯的含量测定。     

RP-HPLC法同时测定维生素AD微珠中维生素A棕榈酸酯和维生素D2的含量

目的： 建立同时测定维生素AD微珠中维生素A棕榈酸酯和维生素D2含量的反相高效液相色谱法。方法：采用Phenomenex C18色谱柱,甲醇为流动相,流速1.0 mL ? min-1,柱温35 ℃,检测波长265 nm,进样量10 μL,按内标法计算维生素A棕榈酸酯和维生素D2的含量。结果：维生素A棕榈酸酯和维生素D2线性范围分别为522.3 IU?mL-1～2089.4 IU?mL-1 (r =0.9999)和51.88 IU?mL-1～207.5 IU?mL-1(r =0.9999),平均回收率分别为100.3 %和103.4 %,定量限分别为1.979 IU ?mL-1和3.179 IU ?mL-1。结论：本方法操作简单、快速、准确,可同时测定维生素AD微珠中维生素A棕榈酸酯和维生素D2的含量。     

维生素A棕榈酸酯原料细菌内毒素检查方法研究

目的：建立检查维生素A棕榈酸酯进行细菌内毒素检查法。方法：维生素A棕榈酸酯以无水乙醇为溶剂溶解,再用细菌内毒素检查用水稀释制成乳浊液,依照《中国药典》2020年版(四部)1143细菌内毒素检查法,对维生素A棕榈酸酯细菌内毒素检查法进行干扰试验预试验和干扰试验,同时增加细菌内毒素回收干扰试验预试验和干扰试验。结果：维生素A棕榈酸酯在实验过程中出现的复析、乳浊现象对细菌内毒素检查无影响,维生素A棕榈酸酯在0.015625mg.ml-1^浓度下对细菌内毒素检查无干扰作用。结论：本法可用于维生素A棕榈酸酯细菌内毒素的质量控制。     

HPLC法测定维生素AD微丸中维生素A棕榈酸酯的有关物质

目的:建立两个高效液相色谱法测定维生素AD微丸中维生素A棕榈酸酯的有关物质.方法:采用Phenomenex Luna NH2色谱柱(4.6 mm×250 mm,3μm),以正己烷为流动相,检测波长325 nm,以主成分外标法测定维生素A棕榈酸酯顺式异构体;采用Waters SunFire(4.6 mm×250 mm,5...     

维生素A棕榈酸酯眼用凝胶治疗干眼症的疗效观察

目的观察对干眼症用维生素A棕榈酸酯眼用凝胶治疗与玻璃酸钠滴眼液治疗的临床疗效对比。方法选择2013年1月至2013年7月门诊60例(60眼)干眼症的患者,按随机的原则分治疗组(维生素A棕榈酸酯眼用凝胶治疗)、对照组(玻璃酸钠滴眼液治疗)各30例,分析临床疗效。所有患者在治疗前、治疗后2~4周采用裂隙灯下观察泪膜破裂时间(BUT)、虎红试验分数情况评价治疗效果。结果两组的显效、有效与总有效率均有显著性差异(χ2 0.01(1)=8.89,P<0.01),治疗组的效果明显优于对照组。结论维生素A棕榈酸酯眼用凝胶对干眼症的患者有明显的临床疗效。     

高效液相色谱法测定兔眼房水中维生素A棕榈酸酯的含量

摘 要 目的:比较不同萃取剂及提取方式对房水中维生素A棕榈酸酯（VAP）提取率的影响,并用HPLC法测定兔眼房水中VAP浓度,提供其药动学实验基础。方法: 分别比较二氯甲烷、氯仿、正己烷及乙醚萃取兔房水中VAP的提取率及不同处理提取方式对提取率的影响。以甲醇沉淀兔眼房水中的蛋白质后进行HPLC测定,流动相为甲醇,检测波长为327nm,流速l ml·min^-1 ,柱温35℃。结果:二氯甲烷、氯仿萃取法对VAP提取率较低;而乙醚与标准应用液及房水互溶达不到萃取目的;正己烷萃取法制备的房水样品VAP提取率较高。兔眼房水中VAP浓度在0.047～4.080μg·ml^-1 范围内呈良好的线性关系,方法学回收率99.0%,绝对回收率96.1%,日内和日间RSD小于10％。结论:本方法具有灵敏、准确、快速等特点,可应用于眼房水VAP的药动学研究。     

维A酸隐形泡囊的制备及其体外性质的研究

目的 制备维A酸隐形泡囊并考察其理化、体外生物学性质.方法 考察隐形泡囊的形态和粒径分布,经凝胶色谱分离,再用分光光度法测定维A酸的含量,计算包封率,测定冻干品的载药量;以普通泡囊的结果作为对照,考察巨噬细胞摄取率和癌细胞生长抑制率.结果 维A酸泡囊和隐形泡囊的平均粒径分别为33、41 μm,包封率分别为91.4%、93.10%,载药量分别为3.15%、2.82%.隐形泡囊规避巨噬细胞的吞噬能力提高26%以上;隐形泡囊与原药对癌细胞的生长抑制率相同.结论 所制维A酸隐形泡囊的包封率高、操作方法简便;隐形泡囊既可保持较高抗癌活性,又能规避吞噬.     

Ascorbyl palmitate-incorporated paclitaxel-loaded composite nanoparticles for synergistic anti-tumoral therapy

A co-loaded drug delivery system based on ascorbyl palmitate that can transport various functional drugs to their targets within a tumor represents an attractive strategy for increasing the efficiency of anticancer treatment. In this study, we developed a dual drug delivery system to encapsulate ascorbyl palmitate (AP) and paclitaxel (PTX) for synergistic cancer therapy. AP, which is a vitamin C derivative, and PTX were incorporated into solid lipid nanoparticles (AP/PTX-SLNs), which were used to treat murine B16F10 melanoma that had metastasized to the lungs of mice. These nanoparticles were spherical with an average size of 223?nm as measured by transmission electron microscope and dynamic light scattering. In vitro cytotoxicity assays indicated that the AP/PTX-SLNs with an AP/PTX mass ratio of 2/1 provided the optimal synergistic anticancer efficacy. In vivo, AP/PTX-SLNs were revealed to be much more effective in suppressing tumor growth in B16F10-bearing mice and in eliminating cancer cells in the lungs than single drug (AP or PTX)-loaded SLNs via a synergistic effect through reducing the Bcl-2/Bax ratio. Furthermore, no marked side effects were observed during the treatment with the AP/PTX-SLNs, indicating that the co-delivery system with ascorbyl palmitate holds promising clinical potential in cancer therapy.     

建立检测祛痘类化妆品中违禁添加维A酸的液相分析法

目的建立检测祛痘类化妆品中非法添加违禁成分维A酸的方法,为化妆品的监管提供技术支撑。方法色谱柱采用Agilent Poroshell 120EC—C18（3．0mm×100mm,2．7μm）,甲醇-0．5％冰醋酸（90：10）为流动相,检测波长350nm,流速1．0mL·min^-1。结果维A酸进样量在1.012～20．24μg范围内与峰面积呈良好线性关系,相关系数r=0．9997,加样回收率为99．8％,RSD=0．4％（n=9）,检测限（S／N=3）为0．002μg·mL^-1。结论本文建立的液相分析法经方法学验证可用于化妆品违禁添加维A酸的快速检测。     

Pectin Micro- and Nano-capsules of Retinyl Palmitate as Cosmeceutical Carriers for Stabilized Skin Transport

Retinyl palmitate (RP)-loaded pectinate micro- and nano-particles (PMP and PNP) were designed for stabilization of RP that is widely used as an anti-wrinkle agent in anti-aging cosmeceuticals. PMP/PNP were prepared with an ionotropic gelation method, and anti-oxidative activity of the particles was measured with a DPPH assay. The stability of RP in the particles along with pectin gel and ethanolic solution was then evaluated. In vitro release and skin permeation studies were performed using Franz diffusion cells. Distribution of RP in each skin tissue (stratum corneum, epidermis, and dermis) was also determined. PMP and PNP could be prepared with mean particle size diameters of 593~843 μm (PMP) and 530 nm (i.e., 0.53 μm, PNP). Anti-oxidative activity of PNP was greater than PMP due largely to larger surface area available for PNP. The stability of RP in PMP and PNP was similar but much greater than RP in pectin bulk gels and ethanolic solution. PMP and PNP showed the abilities to constantly release RP and it could be permeated across the model artificial membrane and rat whole skin. RP was serially deposited throughout the skin layers. This study implies RP loaded PMP and PNP are expected to be advantageous for improved anti-wrinkle effects.     

地塞米松棕榈酸酯脂肪乳注射液的制备

摘 要 目的：制备地塞米松棕榈酸酯脂肪乳注射液,并评价其理化性质。方法: 采用热熔乳化 高压均质法制备地塞米松棕榈酸酯脂肪乳注射液,并对脂肪乳的粒径分布、PdI、Zeta电位和微观形态进行评价;初步考察地塞米松棕榈酸酯脂肪乳注射液的稳定性。结果: 制备的地塞米松棕榈酸酯脂肪乳注射液的平均粒径为（215.1±38.2）nm,PdI 为0.218,Zeta电位为（-18.1±2.3）mV;经透射电镜观察显示,地塞米松棕榈酸酯脂肪乳呈球形,大小分布较为均匀;长期稳定性试验结果表明,地塞米松棕榈酸酯脂肪乳注射液在6个月内稳定性良好。结论:采用热熔乳化 高压均质法制备地塞米松棕榈酸酯脂肪乳注射液工艺简单易行,有望应用于工业化生产之中。     

维甲酸自乳化给药系统的体外溶出及比格犬药物动力学研究

目的评价维甲酸(RA)自乳化释药系统的体外溶出及在比格犬体内的药动学.方法采用HPLC法测定比格犬血浆药物浓度.用四条比格犬交叉实验考察RA自乳化制剂与市售胶囊体内药动学.结果实验表明与市售胶囊剂相比:以水为溶出介质,维甲酸RA自乳化制剂15 min可以溶出80%以上; 而市售胶囊只溶出不到5%.比格犬体内药动学研究结果表明:与市售胶囊剂相比,自乳化制剂达峰时间提前,tmax=1.25 h 而市售胶囊 tmax=2 h;最大血药浓度达到市售胶囊剂的近两倍, AUC(0～∞)提高了67%.结论自乳化制剂可以显著提高RA的体外溶出及体内吸收.     

HPLC测定纳米纤维眼用膜剂中地塞米松棕榈酸酯的含量

目的 建立测定纳米纤维眼用膜剂中地塞米松棕榈酸酯含量的高效液相色谱法。方法 采用岛津LC-20A型高效液相色谱仪,色谱柱为Diamosil C₁₈(150 mm×4.6 mm,5 μm),柱温40 ℃,流速：1 mL·min^-1,流动相为100%甲醇,检测波长239 nm,进样量20 μL。结果 地塞米松棕榈酸酯浓度在0.1~5 mg·mL^-1内线性关系良好(r=0.999 5),日内精密度和日间精密度RSD均<2%(n=5),平均绝对回收率99.89%,RSD为1.15%(n=15)。结论 本方法简便易行,重复性好,灵敏度高,结果准确可靠,适用于纳米纤维眼用膜剂中地塞米松棕榈酸酯含量测定。     

多西环素非离子表面活性剂泡囊处方研究

目的 通过制备多西环素非离子表面活性剂泡囊以提高多西环素的稳定性.方法 采用溶剂注入法制备多西环素非离子表面活性剂泡囊,并用正交设计和单因素考察法优化处方,并对其进行稳定性考察.结果 根据优化后的处方制得的多西环素非离子表面活性剂泡囊样品在(25±2)℃条件下,密闭遮光保存6 m,其含量和包封率无明显下降.结论 非离子表面活性剂泡囊作为药物载体,可提高多西环素的稳定性.     

Niosomes and Polymeric Chitosan Based Vesicles Bearing Transferrin and Glucose Ligands for Drug Targeting

Purpose. To prepare polymeric vesicles and niosomes bearing glucose or transferrin ligands for drug targeting. Methods. A glucose-palmitoyl glycol chitosan (PGC) conjugate was synthesised and glucose-PGC polymeric vesicles prepared by sonication of glucose-PGC/ cholesterol. N-palmitoylglucosamine (NPG) was synthesised and NPG niosomes also prepared by sonication of NPG/ sorbitan monostearate/ cholesterol/ cholesteryl poly-24-oxyethylene ether. These 2 glucose vesicles were incubated with colloidal concanavalin A gold (Con-A gold), washed and visualised by transmission electron microscopy (TEM). Transferrin was also conjugated to the surface of PGC vesicles and the uptake of these vesicles investigated in the A431 cell line (over expressing the transferrin receptor) by fluorescent activated cell sorter analysis. Results. TEM imaging confirmed the presence of glucose units on the surface of PGC polymeric vesicles and NPG niosomes. Transferrin was coupled to PGC vesicles at a level of 0.60 ± 0.18 g of transferrin per g polymer. The proportion of FITC-dextran positive A431 cells was 42% (FITC-dextran solution), 74% (plain vesicles) and 90% (transferrin vesicles). Conclusions. Glucose and transferrin bearing chitosan based vesicles and glucose niosomes have been prepared. Glucose bearing vesicles bind Con-A to their surface. Chitosan based vesicles are taken up by A431 cells and transferrin enhances this uptake.