The Study Of A New Oral Preparation Of Tumorous Multidrug-Resistance Inhibit Agent-Pyronaridine Phosphate

Pyronaridine phosphate is a new antimalarial drug, which was developed inour country in 1970s'. Up to now, pyronaridine phosphate has only one oralpreparation—enteric-coated tablets. In recent years, pharmacological study foundthat pyronaridine can effectively inhibit tumorous multidrug-resistance, and thisrequires suitable preparation for clinical use. The development of new oralpreparation of pyronaridine is in imperative need. The purpose of our study is todetermine a clinical acceptable oral preparation of pyronaridine phosphate, whichwill inhibit the tumorous multidrug-resistance and enhance its oral bioavailability.Main task of this project:1. Selection of new oral preparation of pyronaridine phosphate.2. Design of new formulation and processing of the pyronaridine phosphate.3. Test of quality and stability of new preparation.4. Comparision of dissolution and pharmacokinetics between new preparation andenteric-coated tablets.After literature search, we found that pyronaridine phosphate capsule was thesuitable preparation at 100mg pyronaridine base/capsule. The propsed preprationmethod of our study was stable and applicable for industral use. The validation ofthe analytical methods used in the study suggested that they were suitable forquality control of pyronaridine phosphate capsules. We also found the dissolution ofcapsules was much faster than enteric-coated tablets and bioavailability washigher(147%), peak time was shorter (2h vs 12h), peak concentration washigher(1662.4 vs 399μg/ml). So the capsules developed according to the newpharmacological indication of pyronaridine phosphate will significantly enhance itsoral bioavilability and thereafter, increase its clinical therapeutic efficacy intumorous multidrug-resistance.