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Pharmacy-Introduction to Solid Preparations (Detailed Edition)
source: 1. Books: He Qin and Zhang Zhirong, editors-in-chief of "Pharmacology" (Third Edition) published by Higher Education Press 2. Chengdu University - Pharmacy Class Notes
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Pharmacy-Introduction to Solid Preparations (Detailed Edition)
- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
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Project management is the process of applying specialized knowledge, skills, tools, and methods to project activities so that the project can achieve or exceed the set needs and expectations within the constraints of limited resources. This diagram provides a comprehensive overview of the 8 components of the project management process and can be used as a generic template for direct application.
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- Outline
Introduction to solid dosage forms Organized by: Ekoko
Overview
Meaning and classification
Definition: Pharmaceutical preparations that exist in solid form are collectively referred to as solid preparations
Classification
1. Classified by preparation form: tablets, capsules, granules, powders, pills, films, etc.
2. Classification by mode of administration: oral solid preparations, oral solid preparations, subcutaneous solid preparations, external solid preparations
Characteristics and preparation process
Features:
1. Good physical, chemical and biological stability
2. Accurate dosing
3. Easy to industrialize production and low production cost
4. Easy to transport and store
5. Easy to take and carry, with good patient compliance
Preparation process: drug (excipient) ð crushing ð sieving ð mixing (to obtain powder) ð granulation (to obtain granules) ð tableting (to obtain tablets)
Behavioral characteristics in the gastrointestinal tract
concept
Disintegration: refers to the process in which oral solid preparations are completely disintegrated, dissolved or broken into granules under specified conditions. Except for insoluble coating materials or broken capsule shells, they should all pass through the screen of the disintegration instrument.
Dispersion: refers to the process in which coarse particles formed after disintegration of the preparation are further broken into fine particles.
Dissolution: refers to the process by which a drug is released from a solid preparation and dissolved in body fluids
Dissolution (release rate in some preparations): refers to the rate and degree of dissolution of the active drug from the preparation under specified conditions.
The dissolution rate constant k1 of the drug after the tablet contacts the gastrointestinal fluid, the dissolution rate constant k2 of the drug after the tablet disintegrates into coarse particles, and the dissolution rate constant k3 of the drug after the coarse particles are further dispersed into fine particles; k3>k2>k1
Measures to improve dissolution rate
(1) Increase the dissolution area of the drug (crushing, disintegration)
(2) Increase the dissolution rate constant
(3) Improving drug solvents (changing crystal forms, making solid dispersants, etc.)
powder science micromeritics
Powder: Powder refers to an aggregate composed of many individual solid particles. It is customary to call powder less than 100μm, and particles larger than 100μm.
Powder science: The science and technology that studies the particle size distribution, shape and other basic characteristics of solid particles and other properties is called powder science
Properties of powder particles
Particle size and particle size distribution
Particle size: an indicator of particle size, one of the most basic physical properties of powder
display method
Geometric diameter: major diameter, width diameter, directional diameter, equivalent diameter
Specific surface area diameter
Effective diameter: also known as Stoke's diameter
The average particle size
Particle size distribution: an important index reflecting the uniformity of particle size, generally described in terms of distribution range and frequency.
test methods:
Microscopy (geometric particle size)
Sieving method (above 45μm)
Laser diffraction particle size analysis method (not suitable for wider particle size distribution)
Coulter counting method (suitable for suspensions, emulsions, liposomes, powdered drugs, etc.)
Sedimentation method (range below 100μm)
Specific surface area method (particle size distribution cannot be obtained, the range is below 100 μm)
Cascade impactor method (aerosol)
Morphology and specific surface area
Particle form
shape index
Sphericity
circularity
Shape factor
Specific surface area
Definition: The surface area of a solid per unit mass or unit volume, represented by Sm and Sv respectively.
Determination method: adsorption method, penetration method
Powder density and void ratio
density density
True density: ρ=m/V∞, the ratio of the mass of the powder to the volume of the particles excluding all voids
Particle density: ρ=m/(V∞ V1), the density calculated by excluding only the measured volume of the gaps between particles
Bulk density: ρ=m/(V∞ V1 V2), the mass of unit volume of powder, its volume includes the total volume of the particles themselves and all the gaps between the particles.
Porosity: the ratio of the total volume of the voids between particles and the particles themselves in the powder to the total volume of the powder, which can be expressed as the intra-particle void (V1) rate, the inter-particle void (V2) rate, and the total void (V1 V2) rate
Liquidity and filling
fluidity
display method
Angle of repose: The angle between the stacking slope and the horizontal plane when the powder is stacked. The smaller the value, the better the liquidity.
Flow rate: The amount of powder flowing out of a small hole container with a certain hole diameter at the bottom per unit time. The greater the outflow rate, the better the fluidity
Compression index: ≤10 powder is very easy to flow, 11~15 is easy to flow, 16~20 is flowable, 21~25 is poor, and the following 5 intervals are poor, very poor, and extremely poor.
Ways to improve liquidity
Increase particle size appropriately
Control the humidity of powder
Add lubricant
Others: changing ion morphology and surface roughness, increasing particle density, improving preparation conditions, etc.
packability packability
Influencing factors:
Particle size, shape and surface properties
glidant
Hygroscopicity and wettability
moisture absorption
Definition: The ability of powder to absorb moisture in the environment during storage is an inherent property of powder.
Critical relative humidity (CRH): Water-soluble drug powder generally does not absorb moisture in an environment with low relative humidity, but when the relative humidity is raised to a certain value, the amount of moisture absorbed can be rapidly increased. The humidity at this time is CRH.
The CRH value of a water-soluble mixture is approximately equal to the product of the CRH values of each substance (CRHAB=CRHA×CRHB), regardless of the proportion of each component
Wetting: The phenomenon that the air adsorbed on the surface of the powder is replaced by liquid is called wetting. The nature of this liquid-gas exchange is called wettability. It is often described by the contact angle θ. θ<90° means easy wetting, 90°~180° means no wetting, and 180° means no wetting at all.
Adhesion and cohesion
Adhesion: The attraction between molecules of different substances that causes particles to adhere to each other.
Cohesion: the property of several particles adhering to each other due to the attraction between molecules of the same substance
(*)Compressibility
Expression form: compressibility, moldability, tabletability
Forms of particle deformation: elastic deformation, plastic deformation, brittle deformation
The mechanism of powder compression molding
After compression, the distance between particles decreases and creates an attractive force.
The plastic deformation contact area increases when particles are under pressure.
After the particles are crushed under pressure, a new surface is produced with a large surface free energy.
When deformed under pressure, they fit together to produce a mechanical bonding force.
Frictional heat generates partial melting of the material, and then solidifies again to form a solid bridge.
Water-soluble ingredients form solid bridges at points of contact
Factors affecting powder compression molding
Unit operations for solid dosage forms
crush crushing
Definition: The process of crushing and grinding large solid materials into small pieces, powder or even ultra-fine powder with the help of mechanical force
Purpose: Adjust the fluidity of drug powder, reduce mechanical irritation, reduce particle size, increase specific surface area, improve bioavailability, etc.
Methods: Dry crushing (commonly used), wet crushing (hard to dissolve in water, use "water flying method"), flow energy crushing, low temperature crushing
sieving seiving
Definition: The process of separating drugs of different particle sizes with the help of screens
Types of medicine sieves: punch sieve, woven sieve. There are nine specifications from No. 1 to No. 9. The larger the sieve number, the smaller the inner diameter of the sieve holes.
mixing mixing
Definition: The process of thoroughly mixing two or more drugs or components of a prescription
Mechanism: convective mixing, shear mixing, diffusion mixing
Method: Stir and mix, grind and mix, sieve and mix
Knead
Instant soft material: Adding a small amount of liquid to solid powder, the liquid evenly wets the inside and surface of the powder particles to prepare a uniform plastic material.
Key: The amount of adhesive added
Requirements: Hold it in your hands and form a ball, then press it lightly and it will fall apart.
granulation granulation
Definition: The operation of processing materials into granules of a certain shape and size
Particle forming principle: adhesion and agglomeration
method
Wet granulation: A method of preparing granules by adding an appropriate amount of liquid binder to the drug and appropriate excipients. Including extrusion granulation, rotational granulation, high-speed stirring granulation, fluidized bed granulation, composite granulation, spray granulation, and liquid phase crystallization granulation.
Dry granulation: A method of using strong pressure to crush uniformly mixed drugs and excipients into large flakes or blocks, and then crush them into particles of a certain size. There are heavy pressing method and rolling method
dry
Mechanism: When the hot air continuously transfers heat energy to the wet material, the moisture in the wet material continues to vaporize, and the moisture inside the material continuously diffuses to the surface of the material in liquid and gaseous states, so that the moisture in the wet material continues to decrease. And dry
Properties of moisture in materials
Equilibrium moisture: The moisture contained when the partial pressure of water vapor generated on the surface of the material is equal to the partial pressure of water vapor in the air. Cannot be removed by drying
Free moisture: The portion of moisture in the material that is more than the equilibrium moisture. Dry and removable
Bound moisture: moisture bound physically and chemically, with a slow drying rate
Unbound moisture: moisture that is mechanically bound and dries quickly
Factors affecting drying rate
constant speed drying
Increase air temperature
Reduce air humidity
Improve heat and mass transfer driving force
Reduced speed drying
Increase material temperature
Improve material dispersion
Promote the diffusion of internal moisture to the surface
Drying methods: convection drying, conductive drying, radiation drying (infrared: consumes electricity, microwave: high cost and affects stability), dielectric heating drying, freeze drying (especially suitable for heat-sensitive materials, but requires large investment and high production costs)
solid dispersion solid dispersion
Overview
Definition: A solid dispersion system made by highly dispersing drugs in an amorphous or microcrystalline molecular state in a suitable carrier material.
Advantages: Improve the oral bioavailability of poorly soluble drugs, can be used to prepare sustained- and controlled-release preparations, improve the chemical stability of drugs, and can be further made into solid dosage forms
Disadvantages: aging phenomenon, small drug loading capacity, difficulty in industrial production
carrier material
water soluble carrier material
Polyethylene glycols PEGs: 4000 and 6000 are the most commonly used
Povidone PVP: available in K15, K30, K90 and other specifications
Surfactants: Poloxamers, Polysorbate 80
Organic acids: citric acid, fumaric acid, tartaric acid
Sugars and alcohols: fructose, mannitol
Water-insoluble carrier material
Ethylcellulose EC
Polyacrylic resin
Lipids: Cholesterol
Enteric carrier material
Cellulose: cellulose acetate CAP, HPMCP, CMEC
Polyacrylic resin: No. II and No. III
type
eutectic mixture
Solid solution (extremely fast dissolution rate)
coprecipitate
Principles of immediate release and sustained release
quick release principle
Highly dispersible drug
The role of the carrier: solubilization, wetting, crystal suppression, and stabilization of the dispersion system
Dissolution rate: molecular state > amorphous state > microcrystalline state
Principle of sustained release: The carrier material can form a network skeleton structure that can accommodate drug molecules. The drug molecules or microcrystals dispersed in the skeleton must slowly diffuse through the network structure and be dissolved.
Preparation method: melting method, solvent evaporation method (co-precipitation method)
Phase identification: scanning electron microscope, dissolution rate determination, infrared spectroscopy, X-ray diffraction, thermal analysis, nuclear magnetic resonance spectroscopy
inclusion complexes
Overview
Definition: An inclusion body formed by a drug molecule being fully or partially embedded in the hole structure of another substance molecule. It is composed of a host molecule and a guest molecule.
Features: Increase the solubility of poorly soluble drugs, increase drug bioavailability, improve drug stability, adjust drug release rate, mask odor, reduce irritation, and reduce drug loss
Inclusion materials: cyclodextrin CD (α, β, γ) and its derivatives, starch, cholic acid, cellulose, protein, nucleic acid
The formation and influencing factors of inclusion compounds: the size and polarity of the host-guest molecular structure, the nature of the CD substituent, the type and amount of inclusion medium, the type and amount of additives, inclusion conditions
Preparation methods: grinding method, saturated aqueous solution method, ultrasonic method, freeze drying method and spray drying method, other methods (microwave treatment and sealed heating, etc.)
Verification: Scanning electron microscopy, solubility and dissolution method, UV spectrophotometry, thin layer chromatography, fluorescence photometry, infrared spectrophotometry, differential thermal analysis and differential scanning calorimetry, X-ray diffraction, nuclear magnetic field resonance spectroscopy
Mesh number: The number of mesh holes in a length of 1 inch (25.4)
No. 1: 10 mesh
No. 2: 24 mesh
No. 3: 50 mesh
No. 4: 65 mesh
No. 5: 80 mesh
No. 6: 100 mesh
No. 7: 120 mesh
No. 8: 150 mesh
No. 9: 200 mesh
The smaller the particle size, the larger the specific surface area