Dissolution curves,in vitro anticoagulant activities and gastrointestinal stabilities of three traditional Chi-nese medicines containing medicinal leech
OBJECTIVE To evaluate the in vitro dissolution profiles,anticoagulant activities and gastrointestinal stabilities of three traditional Chinese medicines containing medicinal leech,i.e..Naoxuekang Dropping Pill(NDP),Huoxuetongmai Cap-sules(HC)and Maixuekang Capsules(MC).METHODS Four physiological pH dissolution media and paddle method were employed for dissolution measurement.At different timepoints,the amount of leech peptides was determined by Lowry method for calculating the dissolution curves.Similarity factor f2 was utilized for assessing dissolution similarity.High performance liquid chromatography(HPLC)was employed for determining the generation amount of p-nitroaniline(pNA)and evaluating the inhibi-tory activities of NDP/HC/MC on thrombin.The changes in thrombin inhibitory activities of NDP/HC/MC were recorded after incubating with gastric protease.And the improvements of lower anticoagulant activity were observed after adding subtilin,casein and sodium deoxycholate.RESULTS In water medium,dissolution behaviors of NDP and HC were similar(f2=56.1)while dis-solution curves of NDP/HC/MC in other dissolution media differed.NDP exhibited the fastest dissolution rate and the highest cumulative amount within the specified testing time.At a leech peptide concentration of 10 mg·mL-1,average inhibition rates of thrombin by NDP/HC/MC were 97.9％,85.5％and 59.4％respectively.After 30-min incubation with gastric protease,aver-age retention rates of thrombin inhibition were 64.2％,33.0％and 10.7％for NDP/MC/HC respectively.Subtilin,casein and sodium deoxycholate could arrest the inhibition of gastric protease on HC/MC.After co-incubation with sodium deoxycholate,gastric protease and MC,anticoagulant activity spiked 4.0 folds as compared with no sodium deoxycholate.Similarly,co-incubations with subtilin,gastric protease and HC resulted in a 2.4-fold rise in anticoagulant activity.CONCLUSION Dissolu-tion profiles,anticoagulant activity and gastrointestinal stability in vitro of NDP/HC/MC have been profiled.It provided refer ences for in-depth studies of their in vivo pharmacological activities.
traditional Chinese medicine containing medicinal leechdissolution curveanticoagulant activitygastric protease degradation
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