CN113133985A - Preparation method of amoxicillin capsule - Google Patents
Preparation method of amoxicillin capsule Download PDFInfo
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- CN113133985A CN113133985A CN202110409535.4A CN202110409535A CN113133985A CN 113133985 A CN113133985 A CN 113133985A CN 202110409535 A CN202110409535 A CN 202110409535A CN 113133985 A CN113133985 A CN 113133985A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Abstract
The invention discloses an amoxicillin capsule preparation method, which comprises the steps of mixing an amoxicillin raw material with purified water, adding the mixture into a wet granulation machine to prepare amoxicillin granules, drying and screening the amoxicillin granules to obtain amoxicillin heavy powder granules, mixing a lubricant and carboxymethylcellulose sodium on the amoxicillin heavy powder granules to be ground into powder, and filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule. The prepared amoxicillin capsule has obviously improved dissolution rate, smooth dissolution rate, less added auxiliary material component and no overlarge capsule volume.
Description
Technical Field
The invention relates to the technical field of amoxicillin capsule preparation, and in particular relates to a preparation method of amoxicillin capsule.
Background
Amoxicillin, also known as amoxicillin or amoxicillin, is one of the most commonly used broad-spectrum beta-lactam antibiotics of the semi-synthetic penicillins, as a white powder with a half-life of about 61.3 minutes. Is stable under acidic condition, and the gastrointestinal absorption rate is up to 90%. The amoxicillin has strong bactericidal effect and strong ability of penetrating cell membranes. The oral semi-synthetic penicillin is one of the oral semi-synthetic penicillins which are widely applied at present, the preparation of the oral semi-synthetic penicillin comprises capsules, tablets, granules, dispersible tablets and the like, and the oral semi-synthetic penicillin is often combined with clavulanic acid to prepare the dispersible tablets at present. Wherein the amoxicillin capsule accounts for more than 70 percent of the total weight of the amoxicillin capsule.
Dissolution rate refers to the rate and extent of dissolution of a drug from a solid preparation such as a tablet in a predetermined solvent. Most oral solid preparations must enter blood circulation after being taken, and can be effective after reaching a certain blood concentration, so that the premise that the drug is released from the preparation and dissolved in body fluid is absorbed is that the process is called dissolution in biopharmaceuticals, and the dissolution speed and degree are called dissolution, and from the viewpoint of drug inspection, the dissolution refers to the speed and degree of dissolution of the drug from solid preparations such as tablets or capsules in a specified solvent. The existing amoxicillin capsules have the problem of low dissolution rate, and the use of a disintegrating agent for promoting dissolution causes the overlarge volume of the capsules due to a large amount of the disintegrating agent, and the impurity control aspect is not obviously improved.
Disclosure of Invention
The invention aims to provide a preparation method of an amoxicillin capsule aiming at the defects of the prior art, and solves the problems of low dissolution rate and excessive use of disintegrating agents of the amoxicillin capsule.
In order to achieve the aim, the invention provides a preparation method of amoxicillin capsules, which comprises the following steps: s1, granulating, namely mixing the amoxicillin raw material with purified water, and then adding the mixture into a wet granulating machine to prepare amoxicillin granules; s2, drying, namely drying the amoxicillin granules by using a boiling dryer, wherein the drying time is 50-60 minutes, and the temperature at the beginning of drying is at least 10 ℃ higher than that at the end of drying; s3, screening, namely screening the dried amoxicillin particles through a rotary vibration screen to obtain amoxicillin heavy powder particles; s4, preparing auxiliary materials, namely respectively grinding the lubricant and the carboxymethyl cellulose sodium into powder, and then screening by a vibrating screen; s5, mixing, namely weighing amoxicillin heavy powder particles, the screened lubricant and sodium carboxymethylcellulose in proportion, adding the weighed amoxicillin heavy powder particles, the screened lubricant and the sodium carboxymethylcellulose into a mixer, and mixing, wherein the weighed amoxicillin heavy powder particles, the weighed lubricant and the sodium carboxymethylcellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 20-60 minutes; and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Optionally, in step S3, the step of sieving the dried amoxicillin granules through a rotary vibrating sieve includes that the dried amoxicillin granules are sieved through a 20-mesh sieve to remove coarse granules, and then the amoxicillin granules with different particle sizes are sieved through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence.
Optionally, in step S3, the particle size distribution of the screened amoxicillin heavy powder particles is: 20-40 meshes: 5-10 parts, 40-60 meshes: 35-45 parts of, 60-80 meshes: 35-45 parts, less than 80 meshes: 5-10 parts.
Optionally, in step S3, the particle size distribution of the screened amoxicillin heavy powder particles is: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts.
Optionally, the lubricant is magnesium stearate.
Optionally, in step S1, the mass ratio of amoxicillin raw material to purified water is 30: 1.
Alternatively, in step S2, the drying time is 50 minutes, the first 30 minutes drying temperature is 50 ℃ to 60 ℃, and the last 20 minutes drying temperature is 30 ℃ to 40 ℃.
Alternatively, in step S2, the drying time is 60 minutes, the first 30 minutes drying temperature is 50 ℃, the starting temperature of the last 20 minutes drying temperature is 40 ℃, and the drying temperature decreases linearly as the drying time increases, discharging when the temperature is 30 ℃.
Optionally, in step S6, the amoxicillin heavy powder granules, the sieved lubricant and the sodium carboxymethylcellulose are weighed and added into a mixer for mixing for 20-40 minutes.
Alternatively, in step S6, the amoxicillin heavy powder granules, the sieved lubricant and the sodium carboxymethylcellulose are weighed and added to the mixer for mixing for 30 minutes.
Compared with the prior art, the invention has the beneficial effects that:
the preparation method of the amoxicillin capsule comprises the steps of mixing an amoxicillin raw material with purified water, adding the mixture into a wet granulation machine to prepare amoxicillin granules, drying and screening the amoxicillin granules to obtain amoxicillin heavy powder granules, mixing a lubricant and carboxymethylcellulose sodium on the amoxicillin heavy powder granules, grinding the mixture into powder, and filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule. The carboxymethyl cellulose sodium can improve the dissolubility of the hydrophobic amoxicillin granules in water, the dissolution rate of the prepared amoxicillin capsule is obviously improved, the dissolution rate is smooth, the proportion of the added auxiliary materials is small, and the overlarge volume of the capsule cannot be caused. In addition, the dissolution effect is further improved by controlling the temperature parameter and the time parameter during drying, and the dissolution performance is good.
Detailed Description
In order to make the technical solutions in the embodiments of the present application better understood, the technical solutions in the embodiments of the present application are clearly and completely described below, and it is obvious that the described embodiments are only a part of the embodiments of the present application, and not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present application.
Example 1
A preparation method of amoxicillin capsules comprises the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, preparing auxiliary materials, namely grinding magnesium stearate and sodium carboxymethyl cellulose into powder respectively, and then screening the powder by a vibrating screen, wherein the particle size range of the magnesium stearate and sodium carboxymethyl cellulose powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 30 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Example 2
A preparation method of amoxicillin capsules comprises the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, preparing auxiliary materials, namely grinding magnesium stearate and sodium carboxymethyl cellulose into powder respectively, and then screening the powder by a vibrating screen, wherein the particle size range of the magnesium stearate and sodium carboxymethyl cellulose powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 20 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Example 3
A preparation method of amoxicillin capsules comprises the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, preparing auxiliary materials, namely grinding magnesium stearate and sodium carboxymethyl cellulose into powder respectively, and then screening the powder by a vibrating screen, wherein the particle size range of the magnesium stearate and sodium carboxymethyl cellulose powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 40 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Example 4
A preparation method of amoxicillin capsules comprises the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 60 minutes, wherein the drying temperature in the first 30 minutes is 50 ℃, the initial drying temperature in the last 20 minutes is 40 ℃, the drying temperature is linearly reduced along with the extension of the drying time, and the amoxicillin granules are discharged when the temperature is 30 ℃;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, preparing auxiliary materials, namely grinding magnesium stearate and sodium carboxymethyl cellulose into powder respectively, and then screening the powder by a vibrating screen, wherein the particle size range of the magnesium stearate and sodium carboxymethyl cellulose powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 30 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Example 5
A preparation method of amoxicillin capsules comprises the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 5 parts, 40-60 meshes: 35 parts, 60-80 meshes: 45 parts, less than 80 meshes: 10 parts of (A);
s4, preparing auxiliary materials, namely grinding magnesium stearate and sodium carboxymethyl cellulose into powder respectively, and then screening the powder by a vibrating screen, wherein the particle size range of the magnesium stearate and sodium carboxymethyl cellulose powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 30 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Comparative example 1
The amoxicillin capsule is prepared according to the following steps.
S1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, preparing auxiliary materials, grinding magnesium stearate into powder respectively, and screening the powder through a vibrating screen, wherein the particle size range of magnesium stearate powder particles is 60-120 meshes;
s5, mixing, namely weighing amoxicillin heavy powder particles according to a proportion, adding the sieved magnesium stearate and sodium carboxymethyl cellulose into a mixer for mixing, wherein the weighed amoxicillin heavy powder particles, the lubricant and the sodium carboxymethyl cellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles and 2-4 parts of lubricant;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
Comparative example 2
The amoxicillin capsule is prepared according to the following steps.
S1, granulating, namely mixing the amoxicillin raw material with purified water according to a certain amount, and adding the mixture into a wet granulating machine to prepare amoxicillin granules, wherein the ratio of the amoxicillin raw material to the purified water is 30: 1;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer for 50 minutes, and controlling the time to ensure that the drying temperature is 50 ℃ in the first 30 minutes and 30 ℃ in the last 20 minutes;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration sieve, removing coarse particles of the dried amoxicillin particles through a 20-mesh sieve, and then screening the amoxicillin particles with different particle sizes through a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve in sequence to obtain amoxicillin heavy powder particles, wherein the particle size distribution of the screened amoxicillin heavy powder particles is as follows: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts;
s4, mixing, namely adding the amoxicillin granules, the carboxymethyl starch sodium, the talcum powder and the magnesium stearate into a mixer for mixing, wherein the amoxicillin granules, the carboxymethyl starch sodium, the talcum powder and the magnesium stearate comprise the following components in parts by weight: 100 parts of amoxicillin granules, 3 parts of carboxymethyl starch sodium, 2 parts of talcum powder and 2 parts of magnesium stearate;
and S5, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
The amoxicillin capsules prepared in example 1, example 2, example 3, example 4, example 5, example 6, comparative example 1 and comparative example 2 were respectively subjected to dissolution grouping test according to amoxicillin capsule dissolution test method, and each group of test specimens was 500 parts. The specific determination method comprises the following steps: 900ml of degassed distilled water is taken as a dissolution medium, the temperature is kept constant at 37 +/-0.5 ℃, and the rotating speed is 100 r/min. Sampling at 10 min, 15 min, 20 min, 30 min and 45min, filtering at 6ml per month, precisely absorbing the filtrate at 5ml, and diluting with water to 10 ml; and the contents under the condition of different filling amounts are taken and mixed uniformly, a proper amount (equivalent to the average amount of 0.55 amoxicillin capsules) is precisely weighed, water is added for dissolution and is diluted to 10ml, the absorbance is respectively measured at the wavelength of 272nm by a spectrophotometry, and the dissolution rate is calculated according to the ratio of the absorbance of the two. The data obtained from the experiments are shown in the following table.
The table of the dissolution experiment data of the amoxicillin capsule comprises:
and (3) analyzing experimental data:
according to the experimental data of the embodiment 1, the comparative example 1 and the comparative example 2, the fact that the dissolution of the amoxicillin particles with hydrophobicity in water can be greatly improved by adding the excipient of the sodium carboxymethyl cellulose is shown, and meanwhile, the adding proportion of the sodium carboxymethyl cellulose is small, so that the size of the capsule is not influenced. Moreover, the dissolution speed performance of the disintegrating agent is totally superior to that of the existing preparation process of the disintegrating agent, and the disintegrating agent has good effect.
According to the experimental data of the example 1, the example 2 and the example 3, the dissolution rate is influenced by the mixing time of the amoxicillin heavy powder particles, the lubricant and the carboxymethyl cellulose, the dissolution rate is better when the mixing time is about 30 minutes, and the dissolution rate is influenced by too much or too short mixing time.
Comparing the experimental data of example 1 and example 4, it is demonstrated that when drying, the drying temperature is 50 ℃ in the first 30 minutes, the starting temperature of the drying temperature is 40 ℃ in the last 20 minutes, and the drying temperature is linearly decreased with the extension of the drying time, and when discharging is carried out at 30 ℃, the temperature of the drying process is smoother, the dissolution rate of the product is improved, and especially the dissolution rate at the beginning is more obvious.
The experimental data of the comparative example 1 and the example 5 show that when the specific gravity of the amoxicillin heavy powder particles with smaller particle size is increased, the dissolution rate of the product is also increased.
According to the amoxicillin capsule preparation method, amoxicillin raw materials are mixed with purified water, and then the mixture is added into a wet granulation machine to prepare amoxicillin granules, and the amoxicillin granules are dried and screened to obtain amoxicillin heavy powder granules, on the basis, the lubricant and the sodium carboxymethyl cellulose are mixed and ground into powder, and the mixed medicinal powder is filled into a capsule shell by a full-automatic capsule filling machine to prepare the amoxicillin capsule. The prepared amoxicillin capsule has obviously improved dissolution rate, smooth dissolution rate, less added auxiliary material component and no overlarge capsule volume.
Meanwhile, the dissolution speed is further improved and the dissolution effect is greatly improved by controlling the mixing time of the main drug and the auxiliary materials, the temperature parameter in the drying process and the particle size and the specific gravity of the amoxicillin heavy powder particles.
Although the present invention has been described with reference to the preferred embodiments, it is not intended to limit the scope of the present invention, and those skilled in the art can make various changes and modifications to the embodiments without departing from the spirit and scope of the present invention.
Claims (10)
1. The preparation method of the amoxicillin capsule is characterized by comprising the following steps:
s1, granulating, namely mixing the amoxicillin raw material with purified water, and then adding the mixture into a wet granulating machine to prepare amoxicillin granules;
s2, drying, namely drying the amoxicillin granules by using a boiling dryer, wherein the drying time is 50-60 minutes, and the temperature at the beginning of drying is at least 10 ℃ higher than that at the end of drying;
s3, screening, namely screening the dried amoxicillin particles through a rotary vibration screen to obtain amoxicillin heavy powder particles;
s4, preparing auxiliary materials, namely respectively grinding the lubricant and the carboxymethyl cellulose sodium into powder, and then screening by a vibrating screen;
s5, mixing, namely weighing amoxicillin heavy powder particles, the screened lubricant and sodium carboxymethylcellulose in proportion, adding the weighed amoxicillin heavy powder particles, the screened lubricant and the sodium carboxymethylcellulose into a mixer, and mixing, wherein the weighed amoxicillin heavy powder particles, the weighed lubricant and the sodium carboxymethylcellulose are as follows in parts by weight: 100 parts of amoxicillin heavy powder particles, 1-3 parts of lubricant and 2-4 parts of sodium carboxymethylcellulose, wherein the mixing time is 20-60 minutes;
and S6, filling the mixed medicinal powder into a capsule shell by using a full-automatic capsule filling machine to prepare the amoxicillin capsule.
2. The amoxicillin capsule preparation method of claim 1, wherein in step S3, the step of subjecting the dried amoxicillin granules to a rotary vibrating sieve comprises subjecting the dried amoxicillin granules to a 20-mesh sieve to remove coarse granules, and then sequentially subjecting the amoxicillin granules to a 40-mesh sieve, a 60-mesh sieve and an 80-mesh sieve to sieving to obtain amoxicillin granules with different particle sizes.
3. The amoxicillin capsule preparation method according to claim 2, wherein in step S3, the particle size distribution of the screened amoxicillin heavy powder particles is: 20-40 meshes: 5-10 parts, 40-60 meshes: 35-45 parts of, 60-80 meshes: 35-45 parts, less than 80 meshes: 5-10 parts.
4. The amoxicillin capsule preparation method according to claim 2, wherein in step S3, the particle size distribution of the screened amoxicillin heavy powder particles is: 20-40 meshes: 7 parts, 40-60 meshes: 40 parts, 60-80 meshes: 40 parts, less than 80 meshes: 7 parts.
5. The method for preparing amoxicillin capsules according to claim 1, characterized in that the lubricant is magnesium stearate.
6. The amoxicillin capsule preparation method according to claim 1, wherein in step S1, the mass ratio of amoxicillin raw material to purified water is 30: 1.
7. The method for preparing amoxicillin capsules according to claim 1, characterized in that in step S2, the drying time is 50 minutes, the first 30 minutes drying temperature is 50 ℃ -60 ℃, and the last 20 minutes drying temperature is 30 ℃ -40 ℃.
8. The method for preparing amoxicillin capsules according to claim 1, characterized in that in step S2, the drying time is 60 minutes, the drying temperature for the first 30 minutes is 50 ℃, the starting temperature for the drying temperature for the last 20 minutes is 40 ℃, the drying temperature decreases linearly with the increase of the drying time, and the discharging is performed when the temperature is 30 ℃.
9. The amoxicillin capsule preparation method according to claim 1, wherein in step S6, the amoxicillin heavy powder particles, the sieved lubricant and sodium carboxymethylcellulose are weighed and added to a mixer for mixing for 20-40 minutes.
10. The amoxicillin capsule preparation method according to claim 9, wherein in step S6, the amoxicillin heavy powder particles, the sieved lubricant and sodium carboxymethylcellulose are weighed and added to a mixer for mixing for 30 minutes.
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| CN114869884A (en) * | 2021-07-30 | 2022-08-09 | 江苏恒丰强生物技术有限公司 | Compound amoxicillin powder for porcine respiratory diseases and preparation method thereof |
Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4925674A (en) * | 1988-08-25 | 1990-05-15 | Himedics, Inc. | Amoxicillin microencapsulated granules |
| CN1679558A (en) * | 2005-02-03 | 2005-10-12 | 南京先宇科技有限公司 | Composite medicine containing flucloxacillin magnesium and amoxicillin sodium |
| US20070160673A1 (en) * | 2004-02-24 | 2007-07-12 | Achwarz Franz X | Amoxicilline instant granulate |
| US20080207583A1 (en) * | 2005-01-07 | 2008-08-28 | Sandoz Ag | Process For Preparing Granulates Comprising Amoxicillin |
| CN104856972A (en) * | 2015-03-27 | 2015-08-26 | 华北制药股份有限公司 | Amoxicillin capsules and preparation method thereof |
| US20160199301A1 (en) * | 2013-09-03 | 2016-07-14 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Micronized amoxicillin |
| CN107875136A (en) * | 2017-12-27 | 2018-04-06 | 广州白云山医药集团股份有限公司白云山制药总厂 | A kind of Amoxicillin pharmaceutical preparation and preparation method thereof |
| CN108210475A (en) * | 2016-12-13 | 2018-06-29 | 河南后羿实业集团有限公司 | A kind of amoxil capsule and preparation method thereof |
| CN109953971A (en) * | 2019-05-14 | 2019-07-02 | 吉林市吴太感康药业有限公司 | A kind of preparation method of amoxil capsule |
| CN112156082A (en) * | 2020-11-16 | 2021-01-01 | 海南海力制药有限公司 | Amoxicillin capsule preparation method and amoxicillin capsule |
-
2021
- 2021-04-16 CN CN202110409535.4A patent/CN113133985A/en active Pending
Patent Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4925674A (en) * | 1988-08-25 | 1990-05-15 | Himedics, Inc. | Amoxicillin microencapsulated granules |
| US20070160673A1 (en) * | 2004-02-24 | 2007-07-12 | Achwarz Franz X | Amoxicilline instant granulate |
| US20080207583A1 (en) * | 2005-01-07 | 2008-08-28 | Sandoz Ag | Process For Preparing Granulates Comprising Amoxicillin |
| CN1679558A (en) * | 2005-02-03 | 2005-10-12 | 南京先宇科技有限公司 | Composite medicine containing flucloxacillin magnesium and amoxicillin sodium |
| US20160199301A1 (en) * | 2013-09-03 | 2016-07-14 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Micronized amoxicillin |
| CN104856972A (en) * | 2015-03-27 | 2015-08-26 | 华北制药股份有限公司 | Amoxicillin capsules and preparation method thereof |
| CN108210475A (en) * | 2016-12-13 | 2018-06-29 | 河南后羿实业集团有限公司 | A kind of amoxil capsule and preparation method thereof |
| CN107875136A (en) * | 2017-12-27 | 2018-04-06 | 广州白云山医药集团股份有限公司白云山制药总厂 | A kind of Amoxicillin pharmaceutical preparation and preparation method thereof |
| CN109953971A (en) * | 2019-05-14 | 2019-07-02 | 吉林市吴太感康药业有限公司 | A kind of preparation method of amoxil capsule |
| CN112156082A (en) * | 2020-11-16 | 2021-01-01 | 海南海力制药有限公司 | Amoxicillin capsule preparation method and amoxicillin capsule |
Non-Patent Citations (1)
| Title |
|---|
| 于佳等: "国产头孢氨苄甲氧苄啶胶囊溶出度质量评价", 《中国抗生素杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114869884A (en) * | 2021-07-30 | 2022-08-09 | 江苏恒丰强生物技术有限公司 | Compound amoxicillin powder for porcine respiratory diseases and preparation method thereof |
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