Study Of Yixintong Oral Disintegrating Tablets

Background and Objective:Tablets are traditional formulations. Because of its stability to carry, itsconvenience to take along and to use, high degree of mechanization, low costand high yield, tablets become one of the most common dosage forms. Butthe tablets also have shortcomings such as the more difficult moldingcompression, slower disintegration, low bioavailability and so on.,Thetablets are more difficult to swallow when administrated to the aged, childrenand the psychotics. To a certain extent, the promoting use of the tablets isrestricted. Therefore, The variety of immediate-release formulations,especially the orally disintegrating tablet, has gradually become a hot spot ofthe new drug development in recent years. May2005Drug EvaluationCenter defines the oral disintegrating tablet (Orally Disintegrating Tablet,ODT) as a preparation that can be quickly disintegrated, dispersed ordissolved in the saliva in the oral cavity. The patients can be smoothly takemedicine without water or only a very small amount of water. Without wateror just a small amount of water, and without chewing, the drug is placed inthe oral cavity in case of saliva rapidly dissolving or disintegrating. Drugmove into the digestive system following independent and involuntarydeglutation. The vivo behavior is basically consistent with the ordinarytablets. Unlike sublingual tablets, its onset does not depend on the oralmucosa absorption. The taste of orally disintegrating tablets are themaximalchallenges to prescription designs, which limits greatly the rapiddevelopment of this new formulations. In this article, we use Yixintong as a model drug, EPO as coating material, fluidized bed spray-coating to mask thetaste. multifunctional the premixing adjuvants and wholly powder directcompression method to prepare the industrialized Yixintong oraldisintegrating tablets. Its quality and initial stability was studied too.Methods and Results:1. The choice of excipients of direct compression technology forYixintong ODT.multifunctional excipients (eg. Co-processed Excipients)were chose apharmaceutical adjuvants. The excipient can optimize fluidity, compressibilityand content uniformity. It can also optimize the formulation and be beneficialto the researchment and market. Co-processed Excipients have a variety ofexcellent performance and make the development prescription simple andeffective without the tedious process of granulation. Co-processed Excipientsare made by two or more excipients through some kinds of operation, such asa common drying, spray drying, rapid drying or common crystallinepre-mixing. It makes excipients in subgrain state reaction and covers up thelack of individual excipient by generating functional synergies. After thistreatment, the fluidity and the compressibility of the particles can besignificantly superior to the simple mixing formulations. And it is beneficial tothe use of the direct tabletting process.2. Yixintong ODT PreparationThe selection of coating material is the one which can not be quicklydissolved in the oral cavity,but can be rapidly dissolvied in the stomach.Wemake Yixintong raw drugs be cohered in particles with certain hardness andthe size by Using fluidized bed bottom spray. Then we use fluidized bedbottom spray to coat. Pellets coating material does not dissolve in the nearneutral environment (pH5-7), but can dissolve in pH5following medium soon.Tertiary amino group has a strongly hydrophilic and a larger swellable in pH5 above medium. So even in the high pH gastric juice it can also be dissolved.We use L9（34） orthogonal experiment to optimize the preparation process ofYixintong ODT.3. Quality control of the Yixintong ODTWith reference to the Chinese Pharmacopoeia2010version andtechnical requirements and principles of drug research guidance, we executeYixintong ODT quality control.According to the nature of the hawthorn leaf extract combined with existingnational Pharmacopoeia2010edition standard determination method, we usethe HPLC method for the determination of this content of hyperin in YixintongODT. The results showed that the content determination method is highprecision, reproducibility and can achieve the requirements of instrumentalanalysis.4.Yixintong ODT sample Preliminary investigation of stabilityAccording to the stability principles of drug research guidance in ChinesePharmacopoeia2010version, we set stability study of high temperature (60℃±2℃), high humidity (RH75±5%and RH90±5%), light (4500±500Lx).We make6months accelerated test and12months long-term stability test. Theresults show that this product can resist to light and temperature, but highhumidity moisture(RH75±5%RH90±5%) affects the disintegrationtime.This product can resist to light and temperature. It must prevent fromhigh moisture.Conclusion:This article makes research and discussion about orally disintegratingtablets critical factors comprehensive. First using a fluidized bed coating tomask taste and adopeing Co-processed Excipients to control the particle sizeand the disintegration of ODT, we balance of the problem about thedisintegration and taste masking. Through quality research and preliminary stability study, it can meet the requirements of clinical use and industrialproduction.