The Research On Improvements Of Bioavaliable With Resina Draconis’ Cinlusion Complex

purposeResina Draconis is a valuable Chinese herbal medicine of traditional Chinese, isliliaceae dracaena flag leaf dracaena Dracaena cochinchinensis (Lour.) s. c. Chenextraction of resin, It has obvious curative effect in the treatment of coronary heartdisease, cerebral infarction, myocardial ischemia, brain damage and so on[1-2],However Resina Draconis’s solubility is low, Lead to the poor absorption, absorptionis the key to the drugs work, So severely limit its clinical application , The companyhas its preparation into clathrate, expected to increase its dissolution, improve theabsorb, thus improve bioavailability , This paper on the basis of preparation research,For the improvement of the availability of Resina Draconis and provide the basis fororal agents.used the method of in vitro dissolution to evaluate the dragon’s blood, theinclusion compound’s dissolution rate and the degree of it. Besides, based on theoverall level of cells, organs this paper do some system research on its oral absorptionmechanism and bioavailability.methods1. In vitro dissolution studyWith the accumulate dissolution as the evaluation index, this paper measured thecontents of Loureirion A by HPLC method and set a distinguishable dissolutionresearch to compare resina draconis’s and its inclusion compound’s dissolution rateand degree.2. Caco - 2 cell membrane studyBuild the model of Caco-2 cells, used HPLC method to measure the contents ofLoureirion A and caculated the apparent permeability coefficient(Papp) andPertechnetate thyroid uptake ratio(Pratio) to evaluate the resina draconis and itsinclusion compound absorption and the absorption mechanism in Caco-2 cells.3. Single pass intestinal perfusion studyBuild the model of Single pass intestinal perfusion, used HPLC method tomeasure the Loureirion A and Loureirion B contents and caculated Ka and Papp toevaluate resina draconis and its inclusion compound’s absorption situation andmechanism.4. rat pharmacokinetics and tissue distribution studyFilled the same dose of Resina Draconis and inclusion compound of blood atdifferent time points to two groups of rats respectively. Evaluated the Loureirion Aand Loureirion B contents by HPLC/MS/MS method, dealt medicine generation databy DAS software. Compared two groups of rats’ Bioavailability by calculating theirmain pharmacokinetic parameters . In the same time, do some preliminary research inResina Draconis and its inclusion compound’s heart, liver, spleen, lung, kidney, andbrain tissue’s distribution at different points.results1. Using this method to do dissolution experiment in Resina Draconis and itsinclusion, the results showed that in 10 min, the accumulated dissolution of ResinaDraconis and its inclusion is 3.78% and 79.13%, in 60 min the accumulateddissolution of Resina Draconis and its inclusion is 30.40% and 92.52%. Thedissolution quantity has increased three times, which suggested that there is aeffectively improve of the dissolution rate and degree of Resina Draconis afterclathrate.2. Caco-2 cell model is established in accordance with requirements, the resultsshowed p H7.4 offered perfect transport enviroment for Resina Draconis and itsinclusion. The Papp of Resina Draconis’s clathrate is 1.2 ~ 2.5 times of ResinaDraconis, which suggested that it is good for the absorption of Resina Draconis inCaco - 2 cells after clathrate; Papp decreased with the concentration increase and Pratio< 1.5. All of these signs indicated that there’s no efflux pump participated in, but somecarrier protein part in , which is facilitated diffusion.3. in rats’ Single pass intestinal perfusion model, according to the results,the ResinaDraconis clathrate’s absorption rate and degree in small intestine were raised. There isno-statistical significance of Ka and Papp in different concentrations Resina Draconis,its inclusion compound is alsoand decreased with the increase of concentration, whichsuggested that absorption mechanism is mainly the passive diffusion, at the same timemay have facilitated diffusion. The absorption study of inclusion compound ofdragon’s blood in different intestinal canal shows it absorbed in all canals, mainly insmall intestine and especially do well in duodenum and ileum.4. Compared with the Resina Draconis, rats were given the inclusion complex ofdragon’s blood,Tmax shortened, Cmax increases, AUC (0, t) increases,All of these signsindicated that there is a effectively improve of the dissolution rate and degree afterinclusion;analysis of compartment model are single compartment model, whichsuggested that inclusion compound not changed its distribution in the body . Thedistribution experiment Experimental results show that the resina draconis and itsinclusion compound in the rat heart, liver, spleen, lung, kidney, and brain tissue weredistributed, and the content of inclusion compound is higher than that of resinadraconis; In addition, in heart and brain tissue, the Loureirion A and Loureirion B ofinclusion compound’s dissolution rate and degree, suggests that increased thepermeability of blood brain barrier and the affinity of the heart.inclusion:This paper used the method of in vitro dissolution to evaluate Resina Draconisand its inclusion compound’ dissolution behavior, Besides, based on the overall levelof cells, organs this paper do some system research on its oral absorption mechanism,The results show that it is effectively to improve the dissolution rate and degree ofdragon’s blood after clathrate, it lead to improve absorbtion and bioavailability , anddid’t change Resina Draconis’s absorption mechanism.