广藿香酮传递体的制备及质量评价
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摘要
目的:制备广藿香酮传递体并对其质量进行评价。方法:采用薄膜分散法制备广藿香酮传递体;以广藿香酮的累积透过量(Q_n)、累积透过率(PR)为评价指标,筛选处方中表面活性剂种类、表面活性剂用量及广藿香酮用量;以最优处方制备广藿香酮传递体,观察其形态、粒径分布和Zeta电位并测定包封率。结果:广藿香酮传递体的最优处方为表面活性剂为胆酸钠,胆酸钠用量为0.25 g,广藿香酮用量为15 mg。最优处方制备的广藿香酮传递体呈乳白色混悬液,其平均粒径为(115.6±3.65)nm(RSD=3.20%,n=3),多分散系数(PDI)为0.185±0.008(RSD=4.30%,n=3),Zeta电位为(-13.76±0.225)mV(RSD=1.70%,n=3),广藿香酮的包封率为(46.01±0.40)%(RSD=0.87%,n=3),Q_n为(378.76±0.61)μg/cm~2(RSD=0.20%,n=3),PR为(89.02±0.96)%(RSD=1.10%,n=3)。结论:制备的广藿香酮传递体质量符合要求,可为后续广藿香酮新剂型的研究提供参考。
OBJECTIVE:To prepare pogostone transfersomes,and to evaluate its quality. METHODS:Film dispersion method was used to prepare pogostone transfersomes. Using the accumulative penetration volume(Q_n)and accumulative penetration ratio(PR)of pogostone as evaluation indexes,the types of surfactant,formulation were screened in respects of the dosage of surfactant and the dosage of pogostone. The pogostone transfersomes were prepared with optimal formulation;the morphology,particle size distribution and Zeta potential were observed and the entrapment efficiency was measured. RESULTS:The optimal formulation was as follows as the sodium cholate was selected as surfactant;the dosage of sodium cholate was 0.25 g;the dosage of pogostone was15 mg. The optimal pogostone transfersomes were ivory-white suspension;average particle size was(115.6±3.65)nm(RSD=3.20%,n=3);PDI was 0.185±0.008(RSD=4.30%,n=3);Zeta potential was(-13.76±0.225)mV(RSD=1.70%,n=3);entrapment efficiency of pogostone was(46.01±0.40)%(RSD=0.87%,n=3);Q_nwas(378.76±0.61) μg/cm~2(RSD=0.20%,n=3);PR was(89.02±0.96)%(RSD=1.10%,n=3). CONCLUSIONS:Prepared pogostone transfersomes are in line with quality requirements,which can provide reference for the further study of new dosage form of pogostone.
OBJECTIVE:To prepare pogostone transfersomes,and to evaluate its quality. METHODS:Film dispersion method was used to prepare pogostone transfersomes. Using the accumulative penetration volume(Q_n)and accumulative penetration ratio(PR)of pogostone as evaluation indexes,the types of surfactant,formulation were screened in respects of the dosage of surfactant and the dosage of pogostone. The pogostone transfersomes were prepared with optimal formulation;the morphology,particle size distribution and Zeta potential were observed and the entrapment efficiency was measured. RESULTS:The optimal formulation was as follows as the sodium cholate was selected as surfactant;the dosage of sodium cholate was 0.25 g;the dosage of pogostone was15 mg. The optimal pogostone transfersomes were ivory-white suspension;average particle size was(115.6±3.65)nm(RSD=3.20%,n=3);PDI was 0.185±0.008(RSD=4.30%,n=3);Zeta potential was(-13.76±0.225)mV(RSD=1.70%,n=3);entrapment efficiency of pogostone was(46.01±0.40)%(RSD=0.87%,n=3);Q_nwas(378.76±0.61) μg/cm~2(RSD=0.20%,n=3);PR was(89.02±0.96)%(RSD=1.10%,n=3). CONCLUSIONS:Prepared pogostone transfersomes are in line with quality requirements,which can provide reference for the further study of new dosage form of pogostone.
引文
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[15]魏燕,张永生,郑杭生,等.盐酸青藤碱传递体的制备及其对大鼠类风湿性关节炎的药效评价[J].中草药,2017,48(23):4872-4879.
[16]郑俊民.经皮给药新剂型[M].北京:人民卫生出版社,2006:192.
[2]梁海春.广藿香有效成分体内外抗真菌作用研究[D].广州:广州中医药大学,2012.
[3]周容,周莉莉,钟思雨,等.提高脂质体主动靶向性材料的研究进展[J].中国药房,2017,28(16):2265-2269.
[4]毛雨婷,纪宏宇,郑东友,等.新型脂质体在经皮给药系统中的应用[J].中国药师,2015,18(12):2141-2144.
[5]方蓉,郑杭生,陈思思.离体皮肤渗透法测定三七总皂苷传递体经皮吸收特性[J].中草药,2015,46(4):513-519.
[6]常翠,陈思思,杨宏图,等.三七总皂苷传递体的处方优化研究[J].中药材,2015,38(12):2602-2605.
[7]卢耀文,杨升云,龙晓英,等.处方组成对槲皮素传递体透皮作用的影响[J].中国医药工业杂志,2017,48(4):523-528.
[8]AHAD A,ALSALH AA,ALMOHIZEA AM,et al.Formulation and characterization of novel soft nanovesicles for enhanced transdermal delivery of eprosartan mesylate[J].Saudi Pharm J,2017,25(7):1040-1046.
[9]孙珊珊,王慧云,王飞飞,等.阿德福韦酯纳米脂质载体的制备及处方优化[J].中国药房,2017,28(16):2259-2261.
[10]余荧蓝,郑智元,伊宸辰,等.青蒿素长循环脂质体的制备及体外性质评价[J].药学学报,2018,53(6):1002-1008.
[11]庄英华,张中文,韩伟,等.超滤离心法测定连翘酯苷脂质体包封率[J].中国新药杂志,2012,21(18):2209-2211,2216.
[12]吴玉,张会,陈军,等.香豆素-6传递体的变形性与体外透皮性质的相关性研究[J].南京中医药大学学报,2016,32(4):375-378.
[13]韩翠艳,金珊珊,王晓丽,等.盐霉素纳米结构脂质载体的制备及处方优化[J].中国药房,2018,29(3):317-321.
[14]SIMOES SI,TAPADAS JM,MARQUES CM,et al.Permeabilisation and solubilisation of soybean phosphatidylcholine bilayer vesicles,as membrane models,by polysorbate,tween 80[J].Eur J Pharm Sci,2005,26(3/4):307-317.
[15]魏燕,张永生,郑杭生,等.盐酸青藤碱传递体的制备及其对大鼠类风湿性关节炎的药效评价[J].中草药,2017,48(23):4872-4879.
[16]郑俊民.经皮给药新剂型[M].北京:人民卫生出版社,2006:192.