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Preparation Of New Technologies To Improve The Solubility Of Puerarin

Posted on:2008-11-13Degree:MasterType:Thesis
Country:ChinaCandidate:Z WangFull Text:PDF
GTID:2191360212488980Subject:Chinese medicine preparations
Abstract/Summary:PDF Full Text Request
Objective: Puerarin is mainly used clinically for treatment of cardiovascularsystem diseases. It is widely attentioned for its abundant source and goodpharmacological action. With the widely use of puerarin injection, more and moreadverse drug reactions (ADRs) of it were reported,which are harmful to the healthof the patients. To explore the oral medication of puerarin perhaps is the effectivemethod to lower or avoid its ADRs, and the difficulty of the oral medication ishow to improve the solubility of puerarin in water and the bioavailability. So theinclusion complexes of puerarin with Hydroxypropyl-β-cyclodextrin (HP-β-CD)and the solid dispersions of puerarin with Polyethylene glycol 6000(PEG6000)were prepared in order to improve its poor solubility.Method:(1)Study on the preparation conditions of the inclusion complex ofpuerarin with HP-β-CD: The single factors experiment was adopted to optimizethe preparation conditions. The complexing behavior of HP-β-CD with puerarin inaqueous solution at various pH and concentrations were studied by phasesolubility diagram. Furthermore, the phase solubility curves were drew and theequilibrium contents(K) of the inclusion complexes were calculated.(2)Study onthe preparation conditions of the solid dispersions of puerarin with polyethyleneglycol 6000(PEG6000): The solid dispersions were prepared by the fusion method,and the orthogonal design experiment was adopted to optimize the preparationconditions.(3)Study on the absorption in rat small intestine: The experiments ofthe absorption of puerarin, the inclusion complex, the solid dispersions werecarried on in rat small intestine respectively, and compared the absorption rate ofpuerarin at 3 hour.Result: (1) The best preparation conditions for the inclusion complex of puerarinwith HP-β-CD is: water solvent;the concentration of HP-β-CD: 0.3384 mol/mL;time: 4 hours ; and the temperature: 37.5℃. The solubility of puerarinsignificantly increased as the HP-β-CD concentrations were increased, showing anAL-type phase solubility diagram which revealed that the molar ration of drug toHP-β-CD was 1:1.The solubility of puerarin in the inclusion complexes withHP-β-CD prepared by the optimized preparing process were improved 33timescompared with pure Puerarin in water. (2) The best preparation conditions forthe solid dispersions of puerarin with PEG6000 were: the weight ratio of puerarinto PEG6000,1:9; heating temperature,90℃;and cooling time,40 min. The rate ofdissolution at 5 min and the solubility of puerarin in the solid dispersions prepared by the optimized preparing process were improved 3times and 17timesrespectively as compared with pure puerarin. (3) The absorption rate of puerarinat 3 hour of puerarin , the inclusion complex, the solid dispersions were2.79%,3.87%, 2.41% respectively, and the inclusion complex is the biggest one.Conclusion: By the ways of preparing the inclusion complex of puerarin withHP-β-CD and the solid dispersions of puerarin with PEG6000, the solubility ofpuerarin in water can be increased significantly.
Keywords/Search Tags:puerarin, solubility, HP-β-CD, PEG6000, inclusion complex, solid dispersions
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