藥劑學(xué)課件：第一章 概述

Biopharmaceutics

(Biopharmacy)

Chapter1Introduction

Branchesofpharmaceutics

PhysicalpharmaceuticsIndustrypharmaceuticsBiopharmaceuticsClinicalpharmaceuticsI.Concept

Studyontheprocessofabsorption,distribution,

metabolism

andexcretionofdruganditsdosageforminvivo.tostatearelationshipbetweenthefactorofbiologyanddosageformandthepharmacologiceffectofdrugtoprovidescientificbasisforevaluationofqualityofthedrugpreparationanddesignanduseofdrugproductsrationally1.Factorsofdosageform

TypeofdrugPhysicalandchemicalpropertiesofdrugDosageformandadministrationofdrugThenatureofexcipientsandadditivesandthedoseofdrugThetechnologicalprocessandoperationconditionsofpreparation

Incompatibilityandinteractionbetweendrugs

Typeofdrugi.e.ester,salt,complex,derivativeandsoone.g.Thesolubilityofsodiumtolbutamide(甲磺丁脲鈉)isbetterthanthatoftolbutamide.Thepharmacologiceffectiseither.

Physicalandchemicalproperties

ofdrug

i.e.diameterofparticle,crystalform,solubility,dissolutionrateandsoonDissolutionistheprocessbywhichachemicalordrugbecomesdissolvedinasolventLotsoffactshaveprovedthatthedissolutionrateoftabletsinfluencestheabsorptionandclinicaltherapeuticeffect.Atthepresent,thepharmacopeiaofChinaandmanyothercountriesallhaverequirementofdissolutionrateforsolidpreparationssuchastabletsorcapsules.e.g.

conventiontabletsmicronizedtabletssoliddispersion(pills)Griseofulvin(灰黃霉素)

Dosageformandadministration

ofdrug

i.e.tablets,capsules,injections,transdermaltherapeuticsystem(TTS)andsoon.e.g.thetherapeuticeffectofinjectionsisfasterthanthatoftablets.Becausetheformerwasabsorbedrapidlytothebloodsystemiccirculation.

Thenatureofexcipientsandadditivesandthedoseofdrug

e.g.Thefillersofphenytoinsodium(苯妥英鈉)capsules,calciumsulphateorlactose

Thetechnologicalprocessandoperationconditionsofpreparation

e.g.Preparationforchloramphenicol

palmitate,heatingiseffectiveandformulatingincoldsolventisineffective.

Incompatibilityandinteractionbetweendrugs

e.g.SMZ+TMP:antibacterialeffectisenhanced

Warfarin+butazolidn:bleeding(sideeffect)2.Biologicalfactor

Differencesinrace,sexandageDifferencesinphysiologicandpathologicalconditions3.Pharmacologiceffectofdrug

TherapeuticeffectSideeffectandToxicityII.DifferencesfromrelativesubjectsPharmacology

Studyonthemodeofactionandmechanismofdrugsinvivo.BiochemistryStudyonthebiochemicalprocessofdrugsinvivo.III.HistoryofbiopharmaceuticsthemainactionofadrugdependsonitschemicalstructurepharmacologiceffectofadrugrelatednotonlytoitschemicalstructurebutalsotodosageformandbiologicfactorsDissolutionrateisaqualityindexinvitroBioavailabilityisaqualityindexinvivoThefounderinforeigncountryKruger–Thiemer,E.Nelson,J.G.Wagner,J.Levy,M.Gibaldi,T.L.Loo,內(nèi)藤俊一,村田敏郎,野上壽,褂見(jiàn)喜一等。

Inourcountry,ChinaPharmaceuticalUniversityconductedatrainingclassofbiopharmaceuticsin1978.IV.Experimentdesignofbiopharmaceutics

TheorybasisExperimentalprocessExperimentAnimalTheorybasis

——Pharmacokineticsstudyonthetransportlawofdruginvivoby

meansofthefundamentalsofkineticsandmathematicsExperimentalprocess

Analyze

bloodconcentrationurineconcentrationmetaboliteconcentrationconcentrationintissue,organandfluidDeterminationofbioavailability

Analysismethods

Ultravioletspectrometry(UV)

Fluoro

spectrophotometryNuclearmagneticresonancespectroscopyFlamephotometerThin-layerchromatography(TLC)Isotopelabelmethod…………ExperimentAnimal

Mammilla(哺乳動(dòng)物)includesrat(mice),rabbit,dog,pig,row,monkeyandsoonHumanbodyV.ResearchWorkDissolutionrateandBioavailabilityofsoliddosageDesignsustained-releaseandcontrolled-releasepreparationsdependenceofphysiological