Remington: Essentials of pharmaceutics

Cover
Front Matter
	Table of Contents
	Preface
	Contributors
Information Resources in Pharmacy and the Pharmaceutical Sciences
	INTRODUCTION
	LOCATING APPROPRIATE TYPES OF INFORMATION RESOURCES
Analysis of Medicinals
	SPECIFICATIONS
	COMPENDIA
	MONOGRAPHS
	RELEASE AND STABILITY TESTING
	UNIVERSAL TESTS
	METHOD VALIDATION FOR UNIVERSAL TESTS
	TAXONOMY
	DOSAGE FORMS—INJECTABLES
	DOSAGE FORMS—ORAL DRUG PRODUCTS
	ADDITIONAL DOSAGE FORMS
	FUTURE DIRECTION
	NAFCILLIN INJECTION
	NAFCILLIN FOR INJECTION
	CAPECITABINE TABLETS
	PERFORMANCE TESTS
	IMPURITIES
	ADDITIONAL REQUIREMENTS
	NAPROXEN DELAYED-RELEASE TABLETS
	ACETAMINOPHEN EXTENDED-RELEASE TABLETS
Quality Assurance and Control
	QA AND QC: ORGANIZATION/RESPONSIBILITIES
	QUALITY BY DESIGN
	DOCUMENTATION
	QUALITY IN PHARMACEUTICAL BIOTECHNOLOGY
	CONTEMPORARY ISSUES
	FDA MODERNIZATION
	PART 211 CURRENT GOOD MANUFACTURING PRACTICE FOR FINISHED PHARMACEUTICALS
Stability of Pharmaceutical Products
	INTRODUCTION
	REGULATORY REQUIREMENTS
	PRODUCT STABILITY
	PREDICTING SHELF LIFE
	APPROXIMATIONS IN ASSESSING PRODUCT STABILITY
	PHARMACEUTICAL CONTAINERS
	CLOSURES
Bioavailability and Bioequivalence Testing
	INTRODUCTION
	DISSOLUTION
	ABSORPTION FACTORS
	BIOEQUIVALENCE TESTING
	METHODS FOR DETERMINING BIOEQUIVALENCE
	MINIMIZING THE NEED FOR BIOEQUIVALENCE STUDIES
	EVALUATION OF BIOEQUIVALENCE DATA
	BIOEQUIVALENCE ASSESSMENT AND DATA EVALUATION
	CRITERIA FOR BIOEQUIVALENCE
	STUDY DESIGN
	THERAPEUTIC EQUIVALENCE EVALUATIONS
Dissolution
	DEFINITION OF DISSOLUTION AND  THEORETICAL CONCEPTS FOR THE RELEASE OF THE DRUG FROM DOSAGE FORMS
	MATHEMATICS OF DISSOLUTION
	DISSOLUTION PROFILE COMPARISONS
	APPLICATION OF QUALITY BY DESIGN (QbD) PRINCIPLES IN DISSOLUTION TESTING
Modern-Day Drug Discovery and Development
	INTRODUCTION
	EVOLUTION OF 21ST-CENTURY PHARMACEUTICAL RESEARCH
	PHARMACEUTICAL RESEARCH ORGANIZATIONS
	THE SEARCH FOR NEW DRUGS
	NATURAL PRODUCT SOURCES
	FUNCTIONS OF RESEARCH SCIENTISTS
	DRUG DEVELOPMENT
The New Drug Approval Process
	THE FOOD AND DRUG ADMINISTRATION
	OVERVIEW OF THE US DRUG APPROVAL PROCESS
	POST-APPROVAL ACTIVITIES
	SUMMARY
Metrology and Pharmaceutical Calculations
	WEIGHTS AND MEASURES
	WEIGHING AND MEASURING
	DENSITY AND SPECIFIC GRAVITY
	PHARMACEUTICAL CALCULATIONS
	LOGARITHMS
	PHARMACEUTICAL PROBLEMS
	REFERENCES
	ANSWERS TO PROBLEMS
Statistics
	INTRODUCTION
	LOCATION PARAMETERS
	DESIGN OF EXPERIMENTS AND COLLECTION OF DATA
	DESIGN AND CONDUCT OF CLINICAL TRIALS
	THE BINOMIAL AND NORMAL PROBABILITY DISTRIBUTIONS
	ESTIMATION AND STATISTICAL INFERENCE
	DATA TRANSFORMATIONS
	DESIGN AND CONDUCT OF CLINICAL TRIALS
	THE BINOMIAL AND NORMAL PROBABILITY DISTRIBUTIONS
Molecular Structure, Properties, and States of Matter
	MOLECULAR STRUCTURE AND PROPERTIES
	STATES OF MATTER
Thermodynamics
	INTRODUCTION
	THE FIRST LAW
	WORK AND HEAT
	ENTROPY AND THE SECOND LAW
	THE THIRD LAW
	FREE ENERGY
	STANDARD MOLAR GIBBS FREE ENERGY
	NON-IDEALITY
	EQUILIBRIA
	SOLUBILITY
	HEAT OF SOLUTION
	TEMPERATURE DEPENDENCE OF EQUILIBRIUM CONSTANTS
	PARTITIONING BEHAVIOR
	PROTEIN BINDING
Solutions and Phase Equilibria
	SOLUTIONS AND SOLUBILITY
	PHARMACEUTICAL SOLVENTS
	COLLIGATIVE PROPERTIES OF SOLUTIONS
	METHODS TO INCREASE SOLUBILITY OF POORLY SOLUBLE DRUGS
Separation Methods
	FILTRATION
	MATHEMATICS OF FILTRATION
	FILTERING MEDIA
	FILTRATION AIDS
	RAPID FILTRATION APPARATUS
	CENTRIFUGATION
	PRECIPITATION
	SEPARATION OF IMMISCIBLE LIQUIDS
	EXPRESSION
	COUNTERCURRENT DISTRIBUTION
	OTHER SEPARATION TECHNIQUES
Ionic Solutions and Electrolytic Equilibria
	ELECTROLYTES
	CHEMICAL EQUILIBRIA
	PHARMACEUTICAL SIGNIFICANCE
Tonicity, Osmoticity, Osmolality, Osmolarity
	BASIC DEFINITIONS
	THERAPEUTIC CONSIDERATIONS
	OSMOLALITY AND OSMOLARITY
	COMPUTATION OF OSMOLARITY
	OSMOMETRY AND THE CLINICAL LABORATORY
	UNDESIRABLE EFFECTS OF ABNORMAL OSMOTICITY
	OSMOTICITY AND ENTERAL HYPERALIMENTATION
	OSMOLALITY DETERMINATION
	FREEZING-POINT CALCULATIONS
	TONICITY TESTING BY OBSERVING ERYTHROCYTE CHANGES
	METHODS OF ADJUSTING TONICITY
Chemical Kinetics
	CHEMICAL REACTIONS
	REACTION MECHANISM
	REACTION RATE
	FIRST-ORDER REACTIONS
	SECOND-ORDER REACTIONS
	THIRD-ORDER REACTIONS
	PSEUDO-ORDER REACTIONS
	MORE COMPLEX REACTIONS
	EFFECTS ON REACTION RATE
	CATALYSIS
	OTHER EFFECTS
	DRUG STABILIZATION
Complex Formation
	COMPLEX BONDING
	METAL-ION COORDINATION COMPLEXES
	MOLECULAR COMPLEXES
	COMPLEX STABILITY
	CYCLODEXTRINS
	COMPLEXES IN PHARMACY
Interfacial Phenomena
	INTRODUCTION
	INTERFACIAL FORCES AND ENERGETICS
	ADHESIONAL AND COHESIONAL FORCES
	WETTING PHENOMENA
	CAPILLARITY
	PRESSURE DIFFERENCES ACROSS CURVED SURFACES
	ADSORPTION
	SURFACE-ACTIVE AGENTS
Colloidal Dispersions
	DEFINITIONS AND CLASSIFICATIONS
	PROPERTIES OF COLLOIDAL DISPERSIONS
	LYOPHILIC DISPERSIONS
	LYOPHOBIC DISPERSIONS
	ASSOCIATION COLLOIDS
	PHARMACEUTICAL APPLICATIONS OF COLLOIDAL SYSTEMS
Coarse Dispersions
	THE DISPERSION STEP
	INTERFACIAL PROPERTIES
	SUSPENSIONS
	SETTLING AND ITS CONTROL
	FORMULATION OF SUSPENSIONS
	EMULSIONS
	EMULSION TYPE AND MEANS OF DETECTION
	FORMATION AND BREAKDOWN OF DISPERSED LIQUID DROPLETS
	EMULSIFYING AGENT
	PREPARATION OF EMULSIONS
	STABILITY OF EMULSIONS
	BIOAVAILABILITY FROM COARSE DISPERSIONS
Rheology
	INTRODUCTION
	FUNDAMENTALS
	ELASTIC SOLIDS
	NEWTONIAN FLUIDS
	NON-NEWTONIAN FLUIDS
	OTHER EMPIRICAL EQUATIONS AND MODELS
	COMPUTATIONAL RHEOLOGY
	RHEOLOGICAL MEASUREMENTS
	GENERAL VISCOMETER AND RHEOMETER TYPES
	CAPILLARY AND SLIT VISCOMETERS AND RHEOMETERS
	ROTATIONAL VISCOMETERS AND RHEOMETERS
	FALLING BALL AND ROLLING BALL VISCOMETER AND RHEOMETERS
	COMPARISON BETWEEN INSTRUMENTS
	NON-NEWTONIAN CORRECTIONS
Powders
	INTRODUCTION
	PROPERTIES OF POWDERS
	BULK PROPERTIES OF POWDERS
	PRODUCTION METHODS
	PARTICLE SIZE REDUCTION
	POWDER HANDLING
	POWDERS AS A DOSAGE FORM
Solutions, Emulsions, Suspensions, and Extracts
	SOLVENTS FOR LIQUID PHARMACEUTICAL PREPARATIONS
	STABILITY CONSIDERATIONS
	SOLUTIONS
	NONAQUEOUS SOLUTIONS
	EMULSIONS
	SUSPENSIONS
	EXTRACTS
Sterilization Processes and Sterility Assurance
	INTRODUCTION
	MICROBIAL GROWTH AND DEATH
	EQUIPMENT QUALIFICATION
	CONTAINER AND LOAD MAPPING
	BIOLOGICAL INDICATORS
	PHYSICAL MEASUREMENTS
	EQUIVALENCE IN STERILIZATION
	OTHER STERILIZATION METHODS
	PARAMETRIC RELEASE OF STERILIZED MATERIALS
	ASEPTIC PROCESSING
	CONCLUSION
Parenteral Preparations
	OVERVIEW OF UNIQUE CHARACTERISTICS OF PARENTERAL DOSAGE FORMS
	FORMULATION PRINCIPLES
	VEHICLES
	SOLUTES
	ADMINISTRATION
	PARENTERAL COMBINATIONS
	GENERAL CONSIDERATIONS
	GENERAL MANUFACTURING PROCESS
	COMPONENTS
	WATER FOR INJECTION (WFI)
	CONTAINERS AND CLOSURES
	CONTAINER TYPES
	RUBBER CLOSURES
	NEEDLES
	PYROGENS (ENDOTOXINS)
	PRODUCTION FACILITIES
	FUNCTIONAL AREAS
	MAINTENANCE OF CLEAN ROOMS
	PERSONNEL
	ENVIRONMENTAL CONTROL EVALUATION
	PRODUCTION PROCEDURES
	CLEANING CONTAINERS AND EQUIPMENT
	PRODUCT PREPARATION
	FILTRATION
	FILLING
	SEALING
	STERILIZATION
	FREEZE-DRYING (LYOPHILIZATION)
	QUALITY ASSURANCE AND CONTROL
	STERILITY TEST
	PYROGEN TEST
	PARTICULATE MATTER EVALUATION
	CONTAINER/CLOSURE INTEGRITY TEST
	SAFETY TEST
	PACKAGING AND LABELING
Pharmaceutical Compounding – USP <797> Sterile Preparations
	INTRODUCTION
	COMPOUNDING PERSONNEL: RESPONSIBILITIES IN IMPLEMENTING USP <797>
	FACILITIES
	COMPOUNDING STERILE PREPARATIONS
	QUALITY ASSURANCE
	CONCLUSION
Ophthalmic Preparations
	INTRODUCTION
	ANATOMY AND PHYSIOLOGY OF THE EYE
	BIOAVAILABILITY
	TYPES OF OPHTHALMIC DOSAGE FORMS
	DRUG ADMINISTRATION
	METHODS OF USE FOR TOPICAL ADMINISTRATION
	IRRIGATING SOLUTIONS
	INTRAOCULAR INJECTIONS
	INTRAVITREAL INJECTIONS/IMPLANTS
	JUXTASCLERAL INJECTIONS
	INTRACAMERAL INJECTIONS
	IONTOPHORESIS
	SUBCONJUNCTIVAL INJECTIONS
	RETROBULBAR INJECTIONS
	PREPARATION
	PHARMACY COMPOUNDING
	STERILIZATION
	OPHTHALMIC PREPARATION CHARACTERISTICS
	PACKAGING
	ANTIMICROBIAL PRESERVATIVES
	OTC PRODUCTS FOR DRY EYE
	CONTACT LENSES AND THEIR CARE
	GUIDELINES FOR SAFETY AND EFFICACY TESTING
	SUMMARY
Medicated Topicals
	INTRODUCTION
	THE SKIN AND ITS APPENDAGES
	DRUG DELIVERY TO THE SKIN AND ITS APPENDAGES—BASIC PRINCIPLES
	THE FORMULATION OF DOSAGE FORMS AND DELIVERY SYSTEMS FOR TOPICAL DRUG APPLICATION
	CONVENTIONAL TOPICAL DOSAGE FORMS—SEMISOLIDS
	OTHER DOSAGE FORMS FOR APPLICATION TO THE SKIN AND ITS APPENDAGES
	RECTAL, VAGINAL, AND URETHRAL ROUTES OF ADMINISTRATION
Oral Solid Dosage Forms
	TABLETS
	CAPSULES
Coating of Pharmaceutical Dosage Forms
	INTRODUCTION
	EVOLUTION OF THE COATING PROCESS
	PHARMACEUTICAL COATING PROCESSES
	FILM-COATING PROBLEMS
	COATING PROCEDURES AND EQUIPMENT
	QUALITY CONTROL OF COATED TABLETS
	STABILITY TESTING OF COATED PRODUCTS
	RECENT TRENDS IN PHARMACEUTICAL COATING TECHNOLOGY
Oral Modified-Release Drug Delivery Systems
	INTRODUCTION
	RATIONALE AND DEFINITIONS OF ORAL MODIFIED-RELEASE TECHNOLOGIES
	DELAYED-RELEASE SYSTEMS
	EXTENDED-RELEASE SYSTEMS
	ORAL EXTENDED-RELEASE TECHNOLOGIES
	SUMMARY
Aerosols
	INTRODUCTION
	MODE OF OPERATION
	PROPELLANTS
	CONTAINERS
	VALVES
	ACTUATORS
	PACKAGING
	APPLICATIONS
	FORMULATION OF MDIS USING HFCS AS THE PROPELLANT
	NEWER DEVELOPMENTS
Biotechnology and Drugs
	BACKGROUND
	BIOTECHNOLOGY DRUGS
	UNIQUE PHARMACEUTICAL CHALLENGES OF BIOTECHNOLOGY-DERIVED THERAPEUTICS
	PHARMACOGNOSTICAL APPLICATIONS
	PHARMACOLOGICAL APPLICATIONS
	PHARMACEUTICAL MANUFACTURING APPLICATIONS
	ORGANIC SYNTHESIS APPLICATIONS
	MORAL AND ETHICAL QUESTIONS
Pharmaceutical Packaging
	INTRODUCTION
	CONTAINER SELECTION BY DOSAGE FORM
	QUALITY CONTROL
	OVERVIEW OF TEST METHODS
	SUMMARY
Pharmaceutical Excipients
	INTRODUCTION
	MATERIAL SUMMARIES
Basic Pharmacokinetics and Pharmacodynamics
	ANALYTICAL CONSIDERATIONS
	THE CRITICAL NATURE OF THE CONCENTRATION VERSUS EFFECT RELATIONSHIP
	DRUG CONCENTRATION VERSUS TIME PROFILE
	PHARMACOKINETIC MODELS
	RATES AND ORDERS OF REACTIONS
	INSTANTANEOUS INPUT WITH INSTANTANEOUS DISTRIBUTION
	INSTANTANEOUS INPUT WITH NONINSTANTANEOUS DISTRIBUTION
	CONTINUOUS INPUT
	MULTIPLE-DOSE ADMINISTRATION
	NONCOMPARTMENTAL ANALYSIS FOLLOWING INSTANTANEOUS INPUT
	ABSORPTION
	ORGAN-SPECIFIC CLEARANCE
	DOSE-AND TIME-DEPENDENT PHARMACOKINETICS
	STEREOCHEMICAL CONSIDERATIONS
	KINETICS OF PHARMACOLOGIC EFFECT
Drug Action and Effect
	DRUG ACTION AND EFFECT
	DEFINITIONS AND CONCEPTS
	DOSE-EFFECT RELATIONSHIPS
	DRUG RECEPTORS AND RECEPTOR THEORY
	OCCUPATION AND OTHER THEORIES
	MECHANISMS OF DRUG ACTION
	TYPES OF TARGETS FOR DRUG ACTION
	RECEPTOR BINDING
	RECEPTOR STRUCTURE AND FUNCTION
Drug Absorption, Distribution, Metabolism, and Excretion
	INTRODUCTION
	STRUCTURE AND PROPERTIES OF MEMBRANES
	DIFFUSION AND TRANSPORT
	PHYSICOCHEMICAL FACTORS IN PENETRATION
	ABSORPTION OF DRUGS
	ROUTES OF ADMINISTRATION
	FACTORS THAT AFFECT ABSORPTION
	DISTRIBUTION
	BIOTRANSFORMATION
	EXCRETION
Pharmacokinetics/Pharmacodynamics in Drug Development
	PHASE II CLINICAL TRIAL VALIDATION OF DOSE FOR USE IN PHASE II TRIALS
	CREATING A PHARMACODYNAMIC RELATIONSHIP
	PHASE II CLINICAL TRIAL VALIDATION OF DOSE FOR USE IN PHASE III TRIALS
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