摘要
热熔压敏胶(hot melt pressure sensitive adhesive,HMPSA)用作贴剂基质能改善传统橡胶膏载药量低、皮肤刺激性强、黏附性差等问题,但中药贴剂中往往含有挥发油成分,会对热熔压敏胶的结构产生较大破坏作用。为提高热熔压敏胶与中药挥发油的相容性,拟通过物理改性方式,采用二壬基环己烷-1,2-二羧酸酯、聚丙烯蜡和液体橡胶的混合物(DPL)制备一种结构稳定性热熔压敏胶。以肉桂挥发油为模型药物,通过黏度、软化点和内聚力等评价指标筛选投药量。通过黏附性、红外(FI-IR)、差示热扫描(DSC)、流变、扫描电镜(SEM)、含药量、体外透皮评价热熔压敏胶与肉桂挥发油的相容性及其透皮能力。结果表明5%肉桂挥发油开始出现对热熔压敏胶结构的破坏作用,黏附性结果表明改性HMPSA的初黏力和持黏力无明显改变,180°剥离强度略微下降,黏附性良好。FI-IR表明DPL与HMPSA骨架材料形成n-π共轭体系,DSC表明玻璃态转变温度无明显变化,说明DPL和HMPSA相容性较好。SEM表明肉桂挥发油对DPL-HMPSA无明显结构破坏作用,流变性评价表明DPL-HMPSA的储能模量、损耗因子比HMPSA高,内聚力更强,说明其稳定性更好。负载5%肉桂挥发油后,DPL-HMPSA含药量比HMPSA高1.14倍,3个月后含药量下降率比HMPSA低16%。DPL-HMPSA经皮渗透速率为HMPSA的2.25倍,渗透性能明显提高。综上所述,DPL-HMPSA有助于提高中药挥发油共混的稳定性,为HMPSA作为中药复方贴剂的应用提供基础。
Hot melt pressure-sensitive adhesive(HMPSA) has broad application potential in the field of traditional Chinese medicine(TCM) plasters due to its high drug loading, weak skin irritation, satisfactory adhesion, etc. compared with rubber plasters.However, the structure of HMPSA is prone to suffer from the damage caused by volatile oils in TCM plasters. In view of this, a kind of HMPSA with a stable structure was prepared by physical blending of DINCH, polypropylene wax and liquid rubber(LIR) in the present study, which is denoted as DPL. The dosage of cinnamon volatile oil(CVO), the model drug, was selected with viscosity, softening point and cohesion as evaluation indexes. The interaction between DPL and HMPSA was investigated by Fourier transform infrared spectroscopy(FT-IR) and differential scanning calorimetry(DSC). The compatibility of HMPSA with CVO and its transdermal ability were studied by in vitro transdermal test, adhesion, scanning electron microscopy( SEM) and rheological evaluation. The results showed that 5% CVO began to damage the structure of HMPSA. The initial adhesion and holding adhesion of DPL-modified HMPSA(DPL-HMPSA) were not significantly changed compared with those of HMPSA, whereas the 180° peel strength was decreased. FI-IR unraveled that DPL formed the n-π conjugated system with styrene-isoprene-styrene block copolymer(SIS), and there was no significant difference in the glass transition temperature according to DSC results, which indicated the good compatibility of DPL with HMPSA. With 5% CVO loaded, the drug content of DPL-HMPSA was 1. 14 times higher than that of HMPSA, and the decrease rate of drug content in DPL-HMPSA was 16% lower than that in HMPSA after 3 months. SEM demonstrated that CVO did not cause obvious structural damage to DPL-HMPSA. Rheological evaluation revealed that the storage modulus and loss factor of DPL-HMPSA were higher than those of HMPSA, and the cohesion was also stronger. The percutaneous penetration rate of cinnamaldehyde in DPL-HMPSA was 2. 25 times that of HMPSA. In conclusion, DPL-HMPSA had more stable structure, better compatibility with CVO, and higher in vitro transdermal efficiency of cinnamaldehyde than before the modification. This study can provide reference for the mitigation of the matrix structure damage caused by volatile oil components in TCM plasters and the enhancement of the content and in vitro transdermal rate of drug.
作者
殷硕
吴坛
卢键滢
刘珍达
郭腾
冯年平
YIN Shuo;WU Tan;LU Jian-ying;LIU Zhen-da;GUO Teng;FENG Nian-ping(School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Henkel(China)Investment Co.,Ltd.,Shanghai 201203,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2021年第21期5650-5657,共8页
China Journal of Chinese Materia Medica
关键词
HMPSA
贴膏剂
物理改性
中药挥发油
稳定性
体外透皮
HMPSA
plaster
physical modification
volatile oil of traditional Chinese medicine
stability
in vitro transdermal property
