Study on Optimization of Formulation Matrix of Processed Aconitum carmichaelii Hydrogel Patch and Its in vitro Drug Release / 中国药房

ABSTRACT

OBJECTIVE:To optimize formulation matrix of processed Aconitum carmichaelii hydrogel patch,and to investigate its in vitro drug release.METHODS:The ratio of NP700,dihydroxyaluminum aminoacetate,tartaric acid and PVP K90 in processed A.carmichaelii hydrogel patch matrix was optimized by central composite design-response surface method (CCD-RSM) with initial adhesion,peel strength and sensory evaluation as evaluation indexes.The modified Franz diffusion cell method was used for in vitro drug release test processed A.carmichaelii hydrogel patch using accumulative release amount of six ester type alkaloids benzene [benzoyl mesaconine (BM),benzoyl aconitum (BA),benzoylhy paconine (BH),mesaconitine (MT),hypaconitine (HT) and aconitine (AT)] as evaluation indexes.RESULTS:The optimal matrix formulation was NP700-dihydroxyaluminum aminoacetate-tartaric acid-PVP K90 (1.72 ∶ 0.10 ∶ 0.02 ∶ 1.65,m/m/m/m).In validation test,the contents of six ester type alkaloids were 52.77,28.52,28.78,8.81,8.75,8.21 μg/g(RSD＜5％,n=3),comprehensive score was 118.67 ± 1.33 (RSD=4.62％,n=3).The release behavior of BM in vitro conformed to the Higuchi equation.The release behaviors of other 5 alkaloids were consistent with the Higuchi equation.12 h accumulative release amounts of BM,BA,BH,MT,HT and AT were 12.04,2.95,3.55,2.64,2.48,1.97 μg/cm2,respectively.CONCLUSIONS:The processed A.carmichaelii hydrogei patch prepared by matrix prescription is good in appearance,adhesion and in vitro release.The research can provide a basis for the development of new dosage form of processed A.carmichaelii.