德国JRS公司药用辅料在制剂中的应用和案例分享

LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA德国德国JRSJRS公司药用辅料公司药用辅料在制剂中的应用和案例分享德国JRS公司Guangzhou2010.5LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAJ.RETTENMAIER&SÖHNE=JRS近130年历史的家族企业LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAJRSJRSExcipientsExcipients微晶纤维素（2%微粉硅胶）LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA维维微纯微纯®®微晶纤维素标准规格特殊规格MicrocrystallineCelluloseMicrocrystallineCelluloseLEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA产品介绍及应用指南微晶纤维素4n-8.1-A型号平均含水量本体应用推荐颗粒尺寸密度(µm)(g/cm³)10525max.5%0,23惰性载体,吸附性好10165max.5%0,30粘合剂,特别适合湿法造粒10365max.3%0,30含水量降低,适合对水敏感活性成分30165max.5%0,40比重增加,适合小剂量的制备102100max.5%0,33较好的流动性,适合直接压片112100max.3%0,33低含水量,适合对水敏感的药物12180max.5%0,36极佳的流动性和较好的粘合性直接压片首选规格含水量降低,适合对水敏感药物制备200250max.5%0,34极佳的流动性,但粘合性比12差14180max.3%0,36维微纯®维微纯®302100max.5%0.43低含水量,适合对水敏感的药物比重增加,适合高速压片,密度较大的药物LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA微晶纤维素质量衡量重要指标结晶度/KIIndex黑点控制LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA技术数据LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAhhrrh/r=h/r=tantanαα流动性/休止角LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC流动性比较6n-9.1-A休止角αα=45°101102α=42°12200α=36°LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAStudyhasbeenmadeincooperationwithFreieUniversitätBerlin,Prof.Dr.R.Bodmeier05010015020025002468101214Hardness[N]CompactionForce[kN]可压性比较TypesVIVAPUR200VIVAPUR12VIVAPUR102Formulation:MCC99,5%Mg-stearate0,5%LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA0501001502002503000246810121416PRESSURE(kN)HARDNESS(N)102-100%12-100%200-100%80%LACTOSE50%LACTOSE比较微晶纤维素与不同比例乳糖混合的可压性:可压性随着乳糖比例的增加片硬度降低.LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC加入比例对硬度的影响0204060801001201401357911152025COMPRESSIONFORCE(kN)HARDNESS(N)7,5%+22,5%withoutMCCFormulation:Activeingredient100mgLactose44mgAerosil200:1.5mgMg-stearate:1.5mgDisintegrant.3.0mg15%LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAVIVAVIVAPURPUR®®1212FORFORDIRECTDIRECTCOMPRESSIONCOMPRESSIONMICROCRYSTALLINEMICROCRYSTALLINECELLULOSECELLULOSELEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA下冲上冲填料避免出现LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC12在直接压片中的优势MCC中最好的流动性LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA10110212200type45°42°36°36°angleofreposeBestMCCflowLEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCCtype101MCCtype102MCCtype12MagnificationMagnification130x130xLEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMALEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC12在直接压片中的优势MCC中最好的流动性显著提高压片后的含量均匀度、减小片重差异LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAPharmaceuticalTechnologyEurope直接压片:微晶纤维素12vs‘常用规格‘102byMasakiHasegawaNovember2001issueLEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMixingBehaviourdependingfromMixingTime012345678910%A25%A50%A10%A25%A50%Acv5min.15min.30min.MCCtype102MCCtype12cv=rel.standarddeviationActive:AcetaminophenLEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA02468100.1%1.0%5.0%10%25%50%Acetaminophencv(%)含量均匀度MCC102MCC12活性成分比例提高至50%时单用MCC102无法直接压片LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC12在直接压片中的优势MCC中最好的流动性显著提高压片后的含量均匀度、减小片重差异混合过程中颗粒结构不会被破坏LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMA高功能性创新药用辅料PROSOLVSMCC在制剂中的应用LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAMCC(98%)CSD(2%)什么是什么是PROSOLVSMCCPROSOLVSMCC®®??增强可压性和流动性很独特!LEADINGTHEWORLDINEXCIPIENTSJRSPHARMALEADINGTHEWORLDINEXCIPIENTSLEADINGTHEWORLDINEXCIPIENTSJRSPHARMAJRSPHARMAPROSOLVSMCC的三个规格PROSOLVSMCC50=微晶纤维素101+CSDPROSOLVSMCC90=微晶纤维素102+CSDPROSOLVSMCCHD90=微晶纤维素302+CSDPROSOLVSMCC50=微晶纤维素101+CSDPROSOLVSMCC90=微晶纤维素102+CSDPROSOLVSMCCHD90=微晶纤维素302+CSDLEADINGTHEWORLDIN