Studies Of Preparation Of Compounds R Includion Complex

The guest molecule is partialiy or completely incorporated into the cavity of thehost molecule,formed complex,called clathrates(inclusion complex).In general,thisparticular complex is mainly composed of the host molecules and guest moleculescomponents.This inclusion compound can be divided into three types,including a pipeshape,cage and layered. The drug is prepared in the form of inclusion compound haswide application in pharmaceutics.Such as,increasing the solubility of the drug toprepare various pharmaceutical preparations;increasing the drug dissolution rate(dissolution rate) to improve the bioavailability of the drug formulation to reduce thefrequency of administration and dose to the patients; making the liquid drug powder,thereby preventing evaporation of the active ingredients of drugs;masking the specialodor of drugs and reduce irritation to stomach,etc.,then improve the compliance ofpatients;improving the chemical stability of the drugs (such as hydrolysis,oxidation,photolysis and dehydration).The experiment used a model drug compounds R,according to BiopharmaceuticsClassification System is classified as Class â…¡ active substances,namely highpermeability, low solubility. Accordingly, the solubility is a key factor in limitingtheir bioavailability.The active compounds conform to the requirements that the guestmolecules is made to inclusion complexs.Therefore,the active compounds is preparedinto inclusion complex to improve its solubility and to increase its dissolutionrate,then improvng its bioavailability.In this study,grinding method is employed toprepare clathrate,and then direct compression is adopted to prepare inclusion complextablets.Otherwise,the solubility of inclusion complex and dissolution rate of thetablets was studied.This research has laid certain foundation for insoluble drugsprepared into inclusion complex and inclusion compound prepared preparation.In this study,conducted before prescribing research on compound solubility andstability in different media were investigated,at the same time established the contentdetermination and a dissolution test method.Following the adoption of pre-experiment,the grinding and preparation process for preparing complexs and theinclusion rate determination process and the main factors affecting the prescriptionare investigated and researched.The inclusion rate as main index,the influencingfactors of inclusion compound prepared is investigated by single factor.These factorsare grinding time,wetting agent types,API/CD and the amount of wetting agent.Themost important factors and the level of each influence factor are confirmed by usingsingle factor test,and then Box-Behnken Design conducted.The main trend that eachfactor impact on inclusion rate obtained by the Box-Behnken experiment.Finally,different inclusion rate of prescription is prepared into the inclusion complextablets.The inclusion compound tablets dissolution were studied.The cumulativedissolution rate of three different prescriptions of inclusion complex are much higherthan the cumulative dissolution of ordinary prescription tablets.Fully illustrated,theclathrate of compound R prepared by grinding can improve the dissolution of poorlysoluble drugs.Poorly soluble active ingredients severely limit its clinical application.A largepart of the active ingredient due to its low solubility,it is eliminated by thepharmaceutical industry.Methods for improving drug solubility could save countlessapplications of the active ingredient.This research mainly discusses on improvinginsoluble drug solubility and dissolution rate by inclusion technology. Preparation ofpoorly soluble drug inclusion complex and preparations lay a theoretical foundation.