UNIT

TITLE

PAGE NO.

I

INTRODUCTION OF BIOPHARMACEUTICS

1-9

• BIOPHARMACEUTICS
• PHARMACOKINETICS
• PHARMACODYNAMICS
• PHASES INVOLVED IN DRUG ADMINISTRATION AND THERAPY
• WHAT ROLE DO BIOPHARMACEUTICS, PHARMACOKINETICS, AND PHARMACOLOGICAL RESPONSES PLAY?

2

3

5

6

7

II

DRUG ABSORPTION & ITS MECHANISM

10-20

• INTRODUCTION
• COMMON ROUTES OF DRUG ADMINISTRATION
• DRUG ABSORPTION MECHANISMS
• INTRACELLULAR/TRANSCELLULAR TRANSPORT
• VESICULAR OR CORPUSCULAR TRANSPORT (ENDOCYTOSIS)

11

12

12

13

III

DRUG DISSOLUTION

21-24

• INTRODUCTION
• DIFFUSION LAYER MODEL/FILM THEORY

22

22

IV

FACTORS INFLUENCING DRUG ABSORPTION

25-35

• INTRODUCTION
• FACTORS INFLUENCING DRUG ABSORPTION FROM DOSAGE FORM
• DOSAGE FORM CHARACTERISTICS AND PHARMACEUTICAL INGREDIENTS
• PATIENT RELATED FACTORS AFFECTING DRUG ABSORPTION

26

26

30

31

V

DRUG DISTRIBUTION

36-47

• INTRODUCTION
• PROCESS OF DRUG DISTRIBUTION
• FACTORS AFFECTING DRUG DISTRIBUTION
• TISSUE PERMEABILITY OF THE DRUG
• PHYSICOCHEMICAL PROPERTIES OF THE DRUG

37

38

39

40

41

VI

DRUG-PROTEIN BINDING

48-59

• INTRODUCTION
• DRUG INTERACTIONS
• PATIENT RELATED FACTORS

49

54

55

VII

BIOTRANSFORMATION

60-71

• INTRODUCTION
• BIOTRANSFORMATION

61

61

VIII

EXCRETION

72-76

• INTRODUCTION
• CONCEPT OF CLEARANCE

73

75

IX

FACTORS INFLUENCING RENAL AND NON-RENAL CLEARANCE

77-85

• RENAL DRUG EXCRETION
• FACTORS INVOLVING RENAL EXCRETION
• NON-RENAL DRUG EXCRETION ROUTES

78

78

81

X

BIOAVAILABILITY & BIOEQUIVALENCE

86-93

• INTRODUCTION
• BIOAVAILABILITY-ABSOLUTE VERSUS RELATIVE
• RELATIVE BIOAVAILABILITY
• URINARY EXCRETION STUDIES
• ACUTE PHARMACOLOGICAL RESPONSE METHOD
• THERAPEUTIC RESPONSE METHOD

87

87

88

91

92

93

XI

IN-VITRO DRUG DISSOLUTION TESTING MODELS

94-99

• INTRODUCTION
• IN VITRO—IN VIVO CORRELATION (IVIVC)
• IN VITRO-IN VIVO CORRELATION LEVELS

95

97

98

XII

BIOEQUIVALENCE STUDIES

100-107

• INTRODUCTION
• BIOEQUIVALENCE STUDIES: NEED AND GOALS
• SOME KEY TERMS CRUCIAL TO THIS TOPIC WILL BE DEFINED.
• TYPES OF STUDIES REQUIRED IN BIOEQUIVALENCE STUDIES
• PHARMACOKINETIC STUDIES: DESIGN AND EXECUTION
• WAIVERS OF IN VIVO BIOEQUIVALENCE STUDIES
• CONCLUSION

101

101

101

102

102

106

107

XIII

METHODS FOR ENHANCEMENT OF BIOAVAILABILITY

108-114

• INTRODUCTION
• BIOAVAILABILITY ENHANCEMENT THROUGH ENHANCEMENT OF DRUG PERMEABILITY ACROSS BIO-MEMBRANE
• BIOAVAILABILITY ENHANCEMENT THROUGH ENHANCEMENT OF DRUG STABILITY
• BIOAVAILABILITY ENHANCEMENT THROUGH GASTROINTESTINAL RETENTION

109

112

114

114

XIV

PHARMACOKINETICS

115-121

• INTRODUCTION
• COMPARTMENTAL VS. NON-COMPARTMENTAL PHARMACOKINETIC ANALYSIS
• COMPARTMENTAL PHARMACOKINETIC ANALYSIS
• NON-COMPARTMENTAL PHARMACOKINETIC ANALYSIS (NCA)
• PLASMA DRUG CONCENTRATION-TIME PROFILE

116

116

117

117

118

XV

PHARMACOKINETIC MODELS

122-132

• INTRODUCTION
• COMPARTMENT MODELS
• MODEL BASED APPROACH FOR PHARMACOKINETIC DATA ANALYSIS
• DISTRIBUTED PARAMETER MODEL

123

123

123

129

XVI

ONE-COMPARTMENT OPEN MODEL (I.V. ADMINISTRATION)

133-141

• INTRODUCTION
• ONE-COMPARTMENT OPEN MODEL, I.V. BOLUS ADMINISTRATION
• ONE-COMPARTMENT OPEN MODEL, INTRAVENOUS INFUSION
• INFUSION PLUS LOADING DOSE IN ONE COMPARTMENT MODEL

134

135

137

140

XVII

ONE-COMPARTMENT OPEN MODEL (E.V. ADMINISTRATION)

142-149

• INTRODUCTION
• ZERO-ORDER ABSORPTION MODEL
• FIRST-ORDER KINETIC ABSORPTION MODEL

143

143

144

XVIII

MULTICOMPARTMENT MODELS

150-159

• INTRODUCTION
• TWO-COMPARTMENT OPEN MODEL AFTER INTRAVENOUS BOLUS
• ASSESSMENT OF Α AND Β BY RESIDUAL METHOD
• ASSESSMENT OF PHARMACOKINETIC PARAMETERS
• AREA UNDER THE PLASMA CONCENTRATION-TIME CURVE:
• KINETICS OF MULTIPLE DOSING
• ACCUMULATION OF DRUGS DURING MULTIPLE DOSES
• INFUSION PLUS LOADING DOSE

151

151

153

154

155

155

157

158

XIX

LINEAR PHARMACOKINETICS

160-165

• LINEAR PHARMACOKINETICS
• NON-LINEAR, MIXED-ORDER, OR CAPACITY-LIMITED PHARMACOKINETICS
• HOW TO DETECT NON-LINEARITY
• CAUSES OF NONLINEARITY

161

163

163

163

XX

MICHAELIS MENTEN EQUATION

166-170

• MICHAELIS CONSTANT
• ESTIMATION OF KM AND VMAX FROM THE PLASMA CONCENTRATION-TIME DATA
• ESTIMATION OF KM AND VMAX FROM STEADY-STATE CONCENTRATION

167

168

168