Research Andrographis Effective Parts Dispersible Preparation And Quality Evaluation

Andrographis effective parts (AEP)mainly contains terpene lactones Andrographis (A), dehydroandrographolide (DDA),14-deoxy andrographolide (DA) and neoandrographolide (NA), etc., in vivo experiments show that it has anti-inflammatory, anti-viral, anti-tumor immunomodulatory effects; but within two terpene lactones ingredient is water insoluble, so its poor absorption in the body, blood lower concentration, leading to low bioavailability; while tablet with simple preparation, easy to take rapid disintegration, fast absorption and bioavailability characteristics. Therefore, the research team expects to AEP tablet prepared to promote its absorption in the body, increasing its plasma concentration; and evaluate the quality of dispersible tablets.This study using wet granulation tabletting prepared Andrographis effective part tablet, and its active ingredient dispersed (A, DDA, DA, NA) cumulative dissolution in30min as the main evaluation through single factor test determining fillers, disintegrants, type and amount of dissolution medium; binding single factor test results, microcrystalline cellulose (MCC) as a filler, Low-substituted hydroxy-propylcellulose (L-HPC) as disintegrant, Determination of the active ingredient (A, DDA, DA, NA) Cumulative dissolution in30min in a1000ml0.3%sodium dodecyl sulfate (SDS) using the paddle method dissolution medium, In the evaluation of dissolution, the amount of L-HPC to disintegrants, binders povidone (PVP) and the amount of disintegrant add a method for the three factors were selected in three different levels, orthogonal design optimization filter out the best prescription. Hardness, weight variation, uniformity,identification and determination of qualitative research and evaluation performed best prescription tablet preparation.Through single factor test to determine prescription fillers as MCC, disintegrating agent L-HPC, dissolution medium of0.3%sodium dodecyl sulfate (SDS) solution; disintegration time of less than3min,"Chinese Pharmacopoeia"2010edition the second part of the appendix tablet "dispersed" requirement I A. By orthogonal experiment shows that the best prescription tablet for AEP100mg, MCC247mg, L-HPC40mg, PVP4mg, silica powder8mg, thiourea0.8mg, piece weight of400mg, within addition of the disintegrating agents, were prepared by wet granulation tabletting method. According to the best prescription tablet prepared a "slurry method" in1000ml0.3%SDS dissolution medium cumulative dissolution within30min to reach more than90%. Quality evaluation study shows that the tablet hardness, uniform dispersion, weight differences are in line with the preparation requirements, identification experiments show tablet contains terpene lactones within two ingredients. The mobile phase systems of method for the determination were acetonitrile:water, detection wavelength205nm, The retention time of A, NA, DA, DDA was27.97,34.46,38.76,39.48min, respectively; Methodological study, The linear range of A, NA, DA, DDA were9.775-97.75μg/ml、0.85-8.5μg/ml、1.4-14μg/ml、2.765-27.65μg/ml, respectively;Day precision RSD values≦0.89%, day RSD values≦1.21%, sample stability of48h RSD values≦1.51%; Recovery experiments RSD values A, NA, DA, DDA, respectively, were less than3.42%,3.52%,3.45%,1.62%. Assay experiments showed that the active ingredient tablet A, NA, DA, DDA percentages were10.53%,0.70%,2.20%,3.55%.Using wet granulation tableting method with L-HPC, MCC, PVP etc. materials and AEP prepared AEP dispersible tablet was yellow round tablet, diameter10mm, sided glossy round, obtained dispersion uniformity, higher accumulation within30min of dissolution, compared with the raw material medicine increased3times; The tablet was quality and stability, high drug content, good disintegration properties, and high dissolution. To promote drug absorption and improved bioavailability further study provides a theoretical basis.