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目的:采用纳米胶束增溶技术制备同时含有脂溶性挥发油与水溶性成分连翘苷(PN)等的全成分载药液体制剂,并考察连翘挥发油纳米胶束对水溶性成分PN体外透皮、透黏膜吸收的影响。方法:采用双提法提取连翘的挥发油与水溶性成分,并用GC-MS测定挥发油的主要成分;再将挥发油以纳米胶束的形式增溶于水溶性药液中制备全成分载药液体制剂(ACLL),采用透射电镜(TEM)、光子相关光谱仪(PCS)与激光共聚焦显微镜(CLSM)考察挥发油纳米胶束的药剂学性质;用高效液相色谱法测定PN含量,采用水平双室扩散池法考察连翘挥发油纳米胶束对PN体外透皮、透黏膜吸收的影响,并与连翘水溶性药液(HCLL)进行对照。结果:连翘挥发油的主要成分为β-蒎烯(49.01%)、α-蒎烯(15.78%)、β-罗勒烯(13.79%)、芳樟醇(5.91%)、α-侧柏烯(2.07%)、β-香叶烯(1.91%)与异松油烯(1.84%)等萜烯类混合物;挥发油胶束为圆球形,粒径为193.3 nm,Zeta电位为-83.8 m V;连翘药液为澄清透明的棕褐色液体,其中PN含量为0.225 mg/m L。实验表明,ACLL组的PN在整个透皮、透黏膜实验过程中的累积透过量始终高于HCLL;7.0 h时,对于透皮给药实验ACLL组PN累积透过量是HCLL组的2.04倍,透黏膜给药实验ACLL组PN累积透过量是HCLL组的1.16倍。结论:连翘挥发油纳米胶束能够促进水溶性成分PN的透皮、透黏膜吸收,体现了其全成分作用的优势,在一定程度上也阐明了中药全成分发挥协同作用的机理之一。
OBJECTIVE: To prepare a full-component drug-loaded liquid formulation containing both fat-soluble volatile oil and forsythin (PN) by nano-micellar solubilization technology. The effects of volatile oil nano-micelles on the transdermal permeation , The impact of transmucosal absorption. Methods: The volatile oil and water-soluble components of Forsythia suspensa were extracted by double extraction and the main components of volatile oil were determined by GC-MS. The volatile oil was solubilized in water-soluble liquid in the form of nano-micelles to prepare the full-component liquid medicine preparation (ACLL). The pharmacological properties of the volatile oil nanomicelles were investigated by transmission electron microscopy (TEM), photon correlation spectroscopy (PCS) and confocal laser scanning microscopy (CLSM). The content of PN was determined by HPLC. Pool method was used to investigate the effect of Forsythia suspense volatile oil nanomicelles on PN transdermal and transmucosal absorption in vitro and to compare with the Forsythia suspensa aqueous solution (HCLL). Results: The main constituents of the volatile oil of Forsythia suspensa were β-pinene (49.01%), α-pinene (15.78%), β-oculeol (13.79%), linalool (5.91% 2.07%), terpenoids such as β-myeme (1.91%) and terpinolene (1.84%). The volatile oil micelles were spherical with diameter of 193.3 nm and Zeta potential of -83.8 mV. Qiao liquid to clarify the transparent tan liquid, which PN content of 0.225 mg / m L. The experimental results showed that the cumulative permeation rate of PN in ACLL group was always higher than that of HCLL in the whole transdermal and transmucosal experiment. At 7.0 h, the cumulative penetration of PN in ACLL group was 2.04 times that of HCLL group Mucosal administration of ACLL group PN cumulative transmission is 1.16 times the HCLL group. CONCLUSION: Forsythia suspensa oil nanomicelles can promote transdermal and transmucosal absorption of water-soluble component PN, which reflects the advantages of its all-component action. To some extent, it also clarifies that one of the mechanisms of synergistic effect of the whole components of traditional Chinese medicine is synergistic.