The Preparation And Related Researches Of SPRIDA

SPRIDA,also called Oxysophoridine,belongs to Quinolizidine alkaloids,and which structure is a double piperidine ring fused by two trivalent nitrogen atoms.It can be purified from Sophora flavescens Air,alopecuuroides,vleiifolia Hance,moorcroftiana.Remarkable progress has been made in the research of Oxysophoridine in recent years,our previous investigation have also explored its versatile pharmacology activity.Studies show that Oxysophoridine has anti-tumor,central nerve system inhibition,antipyretic,antisepsis,anti-inflammatory and heart function enhancement activity,etc.On account of smaller amounts in plants,high cost of extraction,complicated extraction process,we synthesized Oxysophoridine using sophoridine as raw material to satisfy the need of mass production.And Aosaibosi is the by-product in the semisynthesis reaction.And initiatory antitumor study in vitro suggested that it played a certain role in inhabiting tumor cells.Due to Sprida’s easily deliquesced,easily degenerated in the preparation of tablet and water injection and the safety hard to guarantee,Furthermore,injections don’t go through gastrointestinal drug dilivery system and escape the first pass effect of liver and the destruction of gastrointestinal tract,and offers many advantages as rapid action-profile,high bioavailability aa well as small dosage.It has become a necessity to develope a formulation of high and firm effect.For this reason,this subject makes a deep-going study for Oxysophoridine and Aosaibosi,to be specific,that is magnifying the synthesis process of Oxysophoridine,investigating the preparation technology of Oxysophoridine and Aosaibosi powder needle.This thesis summarized the research work of Oxysophoridine and Aosaibosi from the following parts primarily:The chapter Ⅰ is an introduction.It briefly introduced the research progress of Oxysophoridine,Aosaibosi and powder needle.The chapter Ⅱ is about magnifying the synthesis procss of Oxysophoridine.For he longer cycle with larger amount of reactants in the original synthesis technology,hence the cycle is largely shortened after we substituted water for anhydrous alcohol as reaction solvent in our study,which was up to our expection.The main content of chapter Ⅲ is the development of Oxysophoridine powder needle.The more scientific orthogonal test method is employed in this study to optimize the prescription and technological parameter.By doing this,not only the fewer times of experiments and lower cost is brought about,but also the conclusions obtained are more reliable.The chapter Ⅳ is mainly the quality control studies.The identification and tests of every part is conducted according to Chinese Pharmacopoeia 2000 edition.Moreover the study of its stability has also been investigated.The chapter Ⅴ is about the pharmacology activity research of SPRIDA and Aosaibosi.Specially,which involves the study of repressing the sour activity of ammonia and TPA induced ear swelling.