MindMap Gallery Pharmacy of Traditional Chinese Medicine Chapter 23 Biopharmaceutics and Pharmacokinetics
Summary of key knowledge points in the chapters of Biopharmaceutics and Pharmacokinetics of Traditional Chinese Medicine and Pharmacy, a secret weapon for preparing for the postgraduate entrance examination! A must-have guide for students at the end of the term!
Edited at 2024-03-14 22:05:52El cáncer de pulmón es un tumor maligno que se origina en la mucosa bronquial o las glándulas de los pulmones. Es uno de los tumores malignos con mayor morbilidad y mortalidad y mayor amenaza para la salud y la vida humana.
La diabetes es una enfermedad crónica con hiperglucemia como signo principal. Es causada principalmente por una disminución en la secreción de insulina causada por una disfunción de las células de los islotes pancreáticos, o porque el cuerpo es insensible a la acción de la insulina (es decir, resistencia a la insulina), o ambas cosas. la glucosa en la sangre es ineficaz para ser utilizada y almacenada.
El sistema digestivo es uno de los nueve sistemas principales del cuerpo humano y es el principal responsable de la ingesta, digestión, absorción y excreción de los alimentos. Consta de dos partes principales: el tracto digestivo y las glándulas digestivas.
El cáncer de pulmón es un tumor maligno que se origina en la mucosa bronquial o las glándulas de los pulmones. Es uno de los tumores malignos con mayor morbilidad y mortalidad y mayor amenaza para la salud y la vida humana.
La diabetes es una enfermedad crónica con hiperglucemia como signo principal. Es causada principalmente por una disminución en la secreción de insulina causada por una disfunción de las células de los islotes pancreáticos, o porque el cuerpo es insensible a la acción de la insulina (es decir, resistencia a la insulina), o ambas cosas. la glucosa en la sangre es ineficaz para ser utilizada y almacenada.
El sistema digestivo es uno de los nueve sistemas principales del cuerpo humano y es el principal responsable de la ingesta, digestión, absorción y excreción de los alimentos. Consta de dos partes principales: el tracto digestivo y las glándulas digestivas.
Biopharmaceutics and Pharmacokinetics
meaning
Biopharmaceutics is a science that studies the mechanisms and processes of absorption, distribution, metabolism and excretion of drugs and their preparations in the body, and clarifies the relationship between drug factors, dosage form factors, body biological factors and drug efficacy.
How drugs are transported
passive transport
Lipid diffusion, membrane pore transport
active transport
Vitamin B2
facilitated diffusion
pinocytosis
ion pair transport
The process of drugs in the body
absorb
The process by which drugs enter the systemic circulation from the site of administration
Closely related to drug dosage forms
Gastrointestinal administration and absorption
Drug absorption in the stomach is passive transport
The small intestine is the main site of passive absorption of oral drugs
Absorption from parenteral administration
oral absorption
Sublingual tablets (absorbed by sublingual mucosa)
Oral patch (absorbed by buccal mucosa)
injection
Intraperitoneal injection has first-pass effect in the liver, while injection in other parts of the body directly enters the systemic circulation.
distributed
Influencing factors
Binding of drugs to plasma proteins
The binding of drugs to plasma proteins is reversible, and the bound and free drugs in the blood are in a state of dynamic equilibrium.
Blood circulation and vascular permeability
The distribution of drugs is mainly affected by blood flow in tissues and organs
Organizational integration and accumulation
Blood-brain barrier, blood-fetal barrier transport
Blood-brain barrier: Fat-soluble drugs pass easily, water-soluble and polar drugs have difficulty passing
Blood-fetal barrier: As fetal growth reaches its peak, drug permeability increases
pH of body fluids and physical and chemical properties of drugs
metabolism
Mainly performed in the liver
excretion
The main route of drug excretion is through the kidneys, followed by bile excretion
Renal excretion
Glomerular filtration: unable to filter out plasma proteins and drugs bound to plasma proteins
tubular reabsorption
Renal tubular secretion: The plasma protein binding rate of the drug does not affect the rate of renal tubular secretion
bile excretion
The main route of extrarenal excretion
The transport mechanism is mainly active transport
Factors affecting the efficacy of pharmaceutical preparations
Dosage form factors of drugs (key points)
Physical and chemical properties of drugs
Drug half-life ×
Drug dissociation and lipid solubility
Molecular drugs that are highly fat-soluble and undissociated are more likely to penetrate biological membranes (acidic drugs are better absorbed in a lower pH environment, and alkaline drugs are better absorbed in a higher pH environment)
Drug dissolution rate and solubility
drug particle size
Drug crystal form
Stable
metastable
It will be converted into a stable form, which is a thermally unstable crystal form. However, because its solubility is greater than the stable form, metastable drugs are commonly used to make a variety of solid preparations.
Unstable
Drug prescription composition
Excipients, dosage, and drug interactions
pharmaceutical process
Preparation
Process technology
Dosage form and route of administration
Ranking of different absorption rates for the same drug administration route
Intravenous > Inhaled > Muscular > Subcutaneous > Rectal or sublingual > Oral > Dermal
Drug release rate from injection
Aqueous solution>Aqueous suspension>Oil solution>O/W emulsion>W/O emulsion>Oil suspension
Oral dosage drug absorption rate
Solution>suspension, emulsion>powder>capsule>tablet>pill
biological factors of the body
Hepatic first-pass effect of drugs
Physiological state of the medication site
drug interactions
Bioavailability and bioequivalence
bioavailability
Refers to the speed and degree of availability of active substances at the site of action after they are released from pharmaceutical preparations and absorbed. It is usually evaluated by the blood concentration-time curve.
Extent of Bioavailability (EBA)
Refers to the amount of drug entering the blood circulation, which can be expressed by the area under the blood drug concentration-time curve
When the reference product is intravenously administered, the resulting ratio is called the absolute bioavailability
Rate of Bioavailability (RBA)
It refers to the speed at which a drug enters the systemic circulation. The ratio of blood drug concentration to peak time (tmax) is commonly used to indicate the speed at which a preparation is absorbed.
Absolute oral bioavailability
The ratio of the area under the drug-time curve of the preparation being tested to the area under the drug-time curve of intravenous injection
(AUC after oral administration of the same amount of drug/AUC after intravenous injection of a certain amount of drug)*100%
When conducting bioavailability experiments, the same subject takes the test preparation at different times, usually with a time interval of 1 week.
Indicators of bioavailability - parameters reflecting bioequivalence evaluation
peak concentration
It refers to the highest blood drug concentration that can be achieved in the body after extravascular administration, also known as the peak.
It is a parameter related to the therapeutic effect and toxicity level.
Time to reach peak (tmax)
refers to the time when blood drug concentration reaches its peak
Parameters that reflect the onset of drug action
Area under the plasma concentration-time curve (AUC)
Proportional to the total amount of drug absorption, it is a parameter that represents the degree of drug absorption.
Pharmacokinetics
Drug transport speed process
First level speed process (slow release)
The drug transport rate is proportional to the first power of the drug dose or blood drug concentration
Features
Drug elimination half-life and shelf life are constant regardless of dose or drug concentration
t1/2=0.693/ke
t0.9=0.1054/k
The area under the plasma concentration-time curve of a single dose is proportional to the dose
In the case of a single administration, the amount of drug excreted in urine is proportional to the dose.
Zero-order speed process (controlled release)
Drug transport rate is constant, regardless of drug dose or blood concentration
Features
Half-life increases with dose
Model parameters
speed constant
Kinetic parameters that describe the rate of drug transport (elimination)
apparent volume of distribution
It is a proportional constant in the relationship between the amount of drug in the body and the blood drug concentration. It refers to the volume of body fluid required when the amount of drug in the body is evenly distributed according to the blood drug concentration.
Formula: Vd=X/C
Vd is the apparent distribution volume
X is the amount of drug in the body
C is the blood drug concentration
Features
It has no direct physiological significance and does not reflect the true volume in most cases. Its numerical value can reflect the distribution characteristics of the drug.
The Vd value of most drugs far exceeds the actual capacity
Drugs with high water solubility or high polarity are not easy to enter cells or fat tissue, have high blood drug concentration and small apparent distribution volume.
Lipophilic drugs usually have low plasma concentrations and large apparent volumes of distribution