| Houshuning tablet is comprised of Hedyotic diffusa Willd., Herba Andrographitis, H elicteresang ustifolia L inn.. It has the effect to deprive the evil wetness, anti-inflammatory and pyretolysis,and used to treat chronic pharyngitis and acute pharyngitis.After systematic study on the procedure of production three batches' of middle-sizedexperimental production were carried on. The result indicated that the preparation procedure of theproduction is reasonable and feasible. Based on the quality study of the product, quality controlstandard was set up, and also the preliminary study on the stability of this product indicated that thepreparation is stable and the quality is controllable. Also, the pharmacokinetics of P-coumaricacid in rabbits was studied to provide reference for clinical study. It should be helpful for acquiringa deep development and annlication as well as rationalizing the future drug design..1. Preparation process researchThe orthogonal testing method is used to study the optimum water extraction process in theextract preparation. The extraction amount of p-coumaric acid was choosen as the assessmentindex in the Houshuning Tablets. Methods Independent variables were ratio of material tosolvent, soak time, times of extraction,, extracting time. The optimal technology for extraction iscomposed of two times of extracting with the added water value being 8 and 6 times that ofmateriamedica,3 hours of soaking period and 1.5 hour of extracting time for each extraction respectively.the effect of different excipients on taste, hygroscopicity and stability was investigated; thedifferent wetting agents on formability was studied.2. Quality standard researchA new TLC method was set up for examination of andrographolide anddehydroandrographolide in Houshuning Tablets. A HPLC method for testing the total content ofandrographolide and dehydroandrographolide and the content of p-coumaric acid in this preparationwas produced, and the lower limit the total content of andrographolide and dehydroandrographolideand the content of p-coumaric acid in the preparation was given according to several batches'oftesting result. These also showed that the analytical method is reasonable and practical, the qualityis controllable, and the quality of the end product is stable. According to three batches ofexperimental results, the Houshuning Tablets'draft quality control standard was formulated. 3. Investigation on stability of Houshuning TabletsAccording to "New Medicine Examination and approval Means" the stability test of thepreparation has been carried on with high temperature, a high humidity condition, which was called"acceleration test" by inspection of the character, the distinction, and the content examination and soon. At the same time; a long time normal condition stability test was also carried on. During theinspection time, the physics and chemistry characters of Houshuning Tablets were inspected and thecontent of active ingredient confine to the draft quality control standard. These indicated thatHoushuning Tablets is stable, the preparation procedure and the draft quality control standard isreasonable and feasible.4. Pharmacokinetic study onp-coumarie acid in rabbit plasmaA simple and sensitive HPLC-UV method was established to determine p-coumaric acid inrabbit plasma., the separation was performed on a C18 reversed-phase column with detectionwavelength set at 300nm. The calibration curve was linear over the range of 0.05～80μg·mL-1.within-day precisions and between-day precisions were lower than 6.1％. The accuracyexpressed by RE were 92.1-96.6％. This method was successfully applied to investigate thepharmaceutical of p-coumaric acid in rabbits. The concentration of p-coumaric acid in rabbit plasmais determined after injection of three different doses of p-coumaric acid into a rabbit's verge veinof ear. Pharmacokinetic parameters were assessed with non-compartment model and compartmentmodel method.Following three different doses(2 mg.kg-1, 4 mg-kg-1, 10 mg.kg-1) intravenous injection ofp-coumaric acid, t1/2 of p-comaic acid were 44.0±8.5, 36.7±14.3 and 38.2±6.8min,respectively, which showed a rapid elimination of it in rabbits. No significance was observed amongdoses. AUC proportionatly increase with doses. Those indicate the linear pharmacokinetic behaviorof p-coumaric acid in rabbits. |
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