1新释药系统研究进展新释药系统研究进展AdvancesindAdvancesindrugdeliverysystemsrugdeliverysystems张强张强北京大学药学院北京大学药学院Topicalepicutaneous(applicationontotheskin),e.g.allergytesting,typicallocalanesthesiainhalational,e.g.asthmamedicationsenema,e.g.contrastmediaforimagingoftheboweleyedrops(ontotheconjunctiva),e.g.antibioticsforconjunctivitiseardrops-suchasantibioticsandcorticosteroidsforotitisexternaintranasalroute(intothenose),e.g.decongestantnasalsprays.Nasaladministrationcanalsobeusedforsystemiceffect.vaginal,e.g.topicalestrogens,antibacterialsEnteralEnteralisanyformofadministrationthatinvolvesanypartofthegastrointestinaltract:bymouth(orally),manydrugsastablets,capsules,ordropsbygastricfeedingtube,duodenalfeedingtube,orgastrostomy,manydrugsandenteralnutritionrectally,variousdrugsinsuppositoryorenemaformParenteralbyinjectionorinfusionintravenous(intoavein),e.g.manydrugs,totalparenteralnutritionintraarterial(intoanartery),e.g.vasodilatordrugsinthetreatmentofvasospasmandthrombolyticdrugsfortreatmentofembolismintramuscular(intoamuscle),e.g.manyvaccines,antibiotics,andlong-termpsychoactiveagentsintracardiac(intotheheart),e.g.adrenalineduringcardiopulmonaryresuscitation(nolongercommonlyperformed)subcutaneous(undertheskin),e.g.insulinintraosseousinfusion(intothebonemarrow)is,ineffect,anindirectintravenousaccessbecausethebonemarrowdrainsdirectlyintothevenoussystem.Thisrouteisoccasionallyusedfordrugsandfluidsinemergencymedicineandpaediatricswhenintravenousaccessisdifficult.intradermal,(intotheskinitself)isusedforsomeallergens,andalsofortattoosintrathecal(intothespinalcanal)ismostcommonlyusedforspinalanesthesiaandchemotherapyintraperitoneal,(infusionorinjectionintotheperitoneum)e.g.peritonealdialysisIntravesicalinfusionisinfusionintotheurinarybladder.Otherparenteraltransdermal(diffusionthroughtheintactskin),e.g.transdermalfentanylpatchesinpaintherapy,nicotinepatchesfortreatmentofaddictiontransmucosal(diffusionthroughamucousmembrane),e.g.insufflation(snorting)ofcocaine,sublingual,i.e.underthetongue,nitroglycerine,buccal(absorbedthroughcheekneargumline),vaginalsuppositoriesinhalational,e.g.inhalationalanestheticsOtherepidural(synonym:peridural)(injectionorinfusionintotheepiduralspace),e.g.epiduralanesthesiaintravitrealRuteofadministration3肿瘤化疗:科学问题与解决方案Whydrugdelivery?传统制剂给药后:药物全身分布,毒性增加,药效下降4新释药系统研究进展新释药系统1口服速释制剂2口服缓控释制剂3吸入剂4注射剂5透皮给药系统6大分子药物给药系统7载体给药系统8增加吸收制剂9前体药5口服速释制剂口服速释制剂速溶片速溶片口溶片口溶片速崩片速崩片口崩片口崩片快速液化咀嚼片快速液化咀嚼片分散片分散片入口即溶入口即溶//崩,服用方便(老崩,服用方便(老人、病人、儿童)人、病人、儿童)吸收快,起效快,适于急救吸收快,起效快,适于急救生物利用度高生物利用度高部分药物可通过粘膜吸收,避部分药物可通过粘膜吸收,避免首过作用免首过作用注意:味觉注意:味觉6主要技术主要技术冷冻干燥技术(Zydis)闪释技术/微粒载体技术(FlashDose)预处理技术(OraSolv)分散片技术其它技术(不同压片、制粒、干燥技术)主要辅料主要辅料水溶性稀释剂、溶胀性纤维素、高效崩解剂、复合崩解剂等;常用辅料:MCC,甘露醇、山梨醇、赤藓醇、乳糖、交联羧甲基纤维素纳、交联PVP等口服速释制剂口服速释制剂7重要提示重要提示我们缺少自己的专有技术我们缺少自己的专有技术我...