CN109350601A - A kind of Nifedipine Tablets and preparation method thereof - Google Patents
A kind of Nifedipine Tablets and preparation method thereof Download PDFInfo
- Publication number
- CN109350601A CN109350601A CN201811305346.7A CN201811305346A CN109350601A CN 109350601 A CN109350601 A CN 109350601A CN 201811305346 A CN201811305346 A CN 201811305346A CN 109350601 A CN109350601 A CN 109350601A
- Authority
- CN
- China
- Prior art keywords
- nifedipine
- tablets
- preparation
- ingredient
- raw material
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to drug field more particularly to a kind of Nifedipine Tablets and preparation method thereof, the preparation method of Nifedipine Tablets includes the following steps: that raw material is micronized, and pulverizes to nifedipine raw material, and nifedipine partial size is not more than 15 μm after micronization；Ingredient prepares, and weighs filler, disintegrating agent, nifedipine, surfactant and colorant by batch inventory；Wet granulation configures binder solution, dry after the ingredient of preparation is mixed with binder solution, then obtains particle after sieve whole grain；Total mix weighs lubricant, by particle and mix lubricant；Tabletting carries out tabletting using formed punch；By being micronized to nifedipine raw material, the partial size for controlling nifedipine is not more than 15 μm, the ingredients such as disintegrating agent, surfactant and colorant are added during the preparation process simultaneously, so that the Nifedipine Tablets finally obtained have better dissolution rate, are effectively improved its result of extraction.
Description
Technical field
The invention belongs to drug fields, and in particular to a kind of Nifedipine Tablets and preparation method thereof.
Background technique
Nifedipine was found in 1969, and went through to use in the U.S. in 1981.It can be used as a kind of general
Drug is present in the essential drugs standard schedule of the World Health Organization, is most important drug needed for basic health department
One of.Nifedipine is dihydropyridine type calcium antagonists, is one of calcium antagonist, and alternative inhibits calcium ion to enter the heart
The transmembrane transport of myocyte and smooth muscle cell, and calcium ion is inhibited to discharge from intracellular library, it is dense without changing blood plasma calcium ion
Degree.Nifedipine can delay the sinus node function and Atrioventricular Conduction of isolated heart；Electrophysiologic study does not find that this product has yet and delays
Atrioventricular Conduction, the effect for extending sinus node recovery time and slowing down sinoatrial node rate, thus be suitable for various types of hypertension and
Angina pectoris caused by angina pectoris, especially variant angina pectoris and coronarospasm.However, existing nifedipine dissolution rate compared with
Low, result of extraction is undesirable.
Summary of the invention
It is an object of the invention to overcome the above-mentioned deficiency of the prior art, a kind of nifedipine is provided, it is intended to solve existing
The problems such as nifedipine dissolution rate is lower, result of extraction is undesirable.
For achieving the above object, The technical solution adopted by the invention is as follows:
One aspect of the present invention provides a kind of Nifedipine Tablets, by the gross mass of the Nifedipine Tablets be 100% in terms of, it is described
Nifedipine Tablets include the ingredient of following mass percentage:
Nifedipine Tablets provided by the invention, by be added during the preparation process filler, disintegrating agent, surfactant with
And the ingredients such as colorant, so that the Nifedipine Tablets finally obtained have better dissolution rate, average dissolution rate is more than 80%, is had
Effect improves its result of extraction.
Another aspect of the present invention provides a kind of preparation method of Nifedipine Tablets, includes the following steps:
Raw material micronization, pulverizes nifedipine raw material, and nifedipine partial size is not more than 15 μm after micronization；
Ingredient prepares, and weighs filler, disintegrating agent, nifedipine, surfactant and colorant by batch inventory；
Wet granulation configures binder solution, dry after the ingredient of preparation is mixed with described adhesive solution, so
By obtaining particle after sieve whole grain；
Total mix weighs lubricant, by the particle and the mix lubricant；
Tabletting carries out tabletting using formed punch.
In the preparation method of Nifedipine Tablets provided by the invention, by being micronized to nifedipine raw material, control
The partial size of nifedipine is not more than 15 μm, while disintegrating agent, surfactant and colorant etc. being added during the preparation process and matches
Material is effectively improved its result of extraction so that the Nifedipine Tablets finally obtained have better dissolution rate.
Specific embodiment
In order to which technical problems, technical solutions and advantageous effects to be solved by the present invention are more clearly understood, below in conjunction with
Embodiment, the present invention will be described in further detail.It should be appreciated that specific embodiment described herein is only used to explain
The present invention is not intended to limit the present invention.
On the one hand, the embodiment of the invention provides a kind of Nifedipine Tablets, with the gross mass of Nifedipine Tablets for 100%
Meter, Nifedipine Tablets include the ingredient of following mass percentage:
Wherein, filler can be used for filling the weight or volume of tablet, consequently facilitating carrying out tabletting.The embodiment of the present invention mentions
The Nifedipine Tablets of confession, by the way that the ingredients such as filler, disintegrating agent, surfactant and colorant are added during the preparation process,
So that the Nifedipine Tablets finally obtained have better dissolution rate, it is effectively improved its result of extraction.
Further, Nifedipine Tablets include the ingredient of following mass percentage:
Nifedipine Tablets under the content have better result of extraction.
In one embodiment, Nifedipine Tablets include the ingredient of following mass percentage:
Dissolution Rate Testing is carried out to the nifedipine tablets under the content.Dissolution Rate Testing condition is as follows: 900ml water being taken to make
For dissolution medium, sampling filtration at 50 turns of paddle method, 30 minutes takes subsequent filtrate to measure, 6 tablet dissolution average values are 89.4%.
In one embodiment, Nifedipine Tablets include the ingredient of following mass percentage:
Dissolution Rate Testing is carried out to the nifedipine tablets under the content.Dissolution Rate Testing condition is as follows: 900ml water being taken to make
For dissolution medium, sampling filtration at 50 turns of paddle method, 30 minutes takes subsequent filtrate to measure, 6 tablet dissolution average values are 85.1%.
Further, filler includes the one or more of lactose monohydrate, cornstarch and microcrystalline cellulose, i.e.,
Filler may include one of lactose monohydrate, cornstarch and microcrystalline cellulose, two or three.
Further, disintegrating agent includes crospovidone, sodium carboxymethyl starch, low substitution carboxy-propyl cellulose and crosslinking
One of sodium carboxymethylcellulose or more than one, it is preferable that disintegrating agent includes croscarmellose sodium, is being matched
When material prepares, weighed according to preset weight ratio.
Surfactant includes anionic surfactant, preferably lauryl sodium sulfate.
Adhesive is povidone, and colorant is preferably sunset yellow.
On the other hand, the embodiment of the invention also provides a kind of preparation method of Nifedipine Tablets, include the following steps:
Step S10: raw material micronization pulverizes nifedipine raw material, and nifedipine partial size is not after micronization
Greater than 15 μm；
Step S20: ingredient prepares, by batch inventory weigh filler, disintegrating agent, nifedipine, surfactant and
Colorant；
Step S30: wet granulation configures binder solution, the ingredient of preparation is mixed with described adhesive solution
After dry, then obtain particle after sieve whole grain；
Step S40: total mix weighs lubricant, by the particle and the mix lubricant；
Step S50: tabletting carries out tabletting using formed punch.
In the preparation method of Nifedipine Tablets provided in this embodiment, by being micronized to nifedipine raw material, control
The partial size of nifedipine processed is not more than 15 μm, while disintegrating agent, surfactant and colorant etc. being added during the preparation process
Ingredient is effectively improved its result of extraction so that the Nifedipine Tablets finally obtained have better dissolution rate.
Further, in step S10, nifedipine raw material is pulverized using airslide disintegrating mill, after micronization
Nifedipine particle size range is 5 μm~15 μm.When the partial size of nifedipine raw material is too small, it is easy to produce electrostatic, subsequent
It is easy to generate agglomerate under the action of electrostatic in pelletization, to influence the quality of the nifedipine tablets finally obtained；And
When the partial size of nifedipine raw material is too big, then can extreme influence nifedipine tablets result of extraction.In the embodiment of the present invention
By the size controlling of nifedipine in 5 μm~15 μ ms, both avoided because of partial size too small the problem of being easy to produce electrostatic,
The result of extraction that avoiding influences tablet because partial size is too big can also have while guaranteeing nifedipine tablets quality
Good dissolution rate.
Further, in step S20, filler include lactose monohydrate, cornstarch and microcrystalline cellulose one kind or
More than one, it is preferable that filler includes lactose monohydrate, cornstarch and three kinds of microcrystalline cellulose, and microcrystalline cellulose is preferred
It is weighed when carrying out ingredient preparation according to preset weight ratio for microcrystalline cellulose SH802.
Disintegrating agent includes that crospovidone, sodium carboxymethyl starch, low substitution carboxy-propyl cellulose and cross-linked carboxymethyl are fine
Tie up one of plain sodium or more than one, it is preferable that disintegrating agent includes croscarmellose sodium, is carrying out ingredient preparation
When, it is weighed according to preset weight ratio.
Surfactant includes anionic surfactant, preferably lauryl sodium sulfate.
Colorant is preferably sunset yellow.
Further, step S30 includes:
Step S301: binder solution is prepared, adhesive is weighed according to quantity, adhesive is dissolved in purified water, adhesive can
For povidone, preferably PVP K30, the concentration of PVP K30 solution is preferably 5%；
Step S302: filler, disintegrating agent, nifedipine, surfactant and colorant are added to wet for premixing
It is mixed in method granulator；
Step S303: binder solution is added in wet granulator and is mixed, to prepare flexible material；
Step S304: it is dry, the flexible material prepared in above-mentioned steps is dried using fluidized bed；
Step S305: whole grain carries out whole grain using sieve.
Further, moisture content is controlled in step S304, in drying process between 4%~6%.
Further, in step S305, in whole grain step, sieve is 16 mesh~20 mesh screens, can be according to required particle
Partial size is selected, such as can be 16 mesh screens, 18 mesh screens, 20 mesh screens, preferably 16 mesh screens.
Further, in step S40, lubricant is magnesium stearate；The particle prepared in step S30 is mixed with magnesium stearate
Conjunction is placed in three-dimensional mixer and is mixed, and incorporation time is no less than 5 minutes.Due to magnesium stearate and tablet and powder incorporation time
It is too long to will lead to dissolution rate and break crisp strength reduction, it is therefore desirable to control the incorporation time of magnesium stearate and tablet and powder.It should
Incorporation time can be 5~10 minutes, preferably 5 minutes, to not only ensure that magnesium stearate was uniformly mixed with tablet and powder, but also guarantee
Nifedipine tablets obtained have good dissolution rate and break crisp intensity.
Further, in step S50, the formed punch is 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and piece is hard
Degree is 50N~80N, effectively ensures that slice weight meets the requirements, while tablet has good intensity.
Further, after step S50 further include:
Step S60: packaging, installation mold, stiff sheet and aluminium foil are packed according to 10 sheet panels, thus with obtaining nitre benzene
Plain film.Wherein stiff sheet can be PET (polyethylene terephthalate) stiff sheet, PVC (polyvinyl chloride) stiff sheet, PS (polystyrene)
Stiff sheet, ABS (engineering plastics), preferably PVC stiff sheet.
That is the preferred steps of the preparation method of the Nifedipine Tablets of the embodiment of the present invention are as follows:
Step S1: raw material micronization pulverizes nifedipine raw material using airslide disintegrating mill, nitre after micronization
Benzene Horizon particle size range is 5 μm~15 μm.
Step S2: ingredient prepares, by batch inventory weigh filler, disintegrating agent, nifedipine, surfactant and
Toner, wherein filler is lactose monohydrate, cornstarch and microcrystalline cellulose SH802, and disintegrating agent is cross-linked carboxymethyl fiber
Plain sodium, surfactant are lauryl sodium sulfate, and colorant is sunset yellow.
Step S3: wet granulation, first preparation PVP K30 solution weigh PVP K30 according to quantity, and PVP K30 is molten
In purified water, the concentration of PVP K30 solution is 5%；
Then by filler, disintegrating agent, nifedipine, surfactant and colorant be added into wet granulator into
Row mixing；
Then PVP K30 solution is added in wet granulator to be mixed, prepares flexible material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate, and particle is placed in three-dimensional mixer with magnesium stearate and is mixed, and mixes
Closing the time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
The present invention successively carried out test of many times, and it is further detailed as reference pair invention progress now to lift A partial experiment result
Thin description, is described in detail combined with specific embodiments below.
Embodiment 1
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 89.5%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 609.6g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 80.6g, croscarmellose sodium 22.4g, lauryl sodium sulfate 16g and sunset yellow
It is spare after 5g.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 82.5%.
Embodiment 2
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 83.9%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 519.8g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 80.6g, croscarmellose sodium 80g, lauryl sodium sulfate 48g and sunset yellow 5g
It is spare afterwards.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 83.5%.
Embodiment 3
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 84.7%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 532.6g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 100g, croscarmellose sodium 80g, lauryl sodium sulfate 16g and sunset yellow 5g
It is spare afterwards.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 82.1%.
Embodiment 4
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 84.2%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 524.6g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 100g, croscarmellose sodium 80g, lauryl sodium sulfate 24g and sunset yellow 5g
It is spare afterwards.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 89.4%.
Embodiment 5
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 83.7%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 516.6g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 100g, croscarmellose sodium 80g, lauryl sodium sulfate 32g and sunset yellow 5g
It is spare afterwards.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 85.1%.
Embodiment 6
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 81.9%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 487.7g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 129g, croscarmellose sodium 80g, lauryl sodium sulfate 32g and sunset yellow 5g
It is spare afterwards.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 84.6%.
Embodiment 7
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, cornstarch and microcrystalline cellulose SH802, total weight
Amount ratio is 80.0%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 538g, cornstarch 457.2g, microcrystalline cellulose by batch inventory
SH802 is 289g, nifedipine 161g, croscarmellose sodium 80g, lauryl sodium sulfate 30.4g and sunset yellow
It is spare after 5g.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by lactose monohydrate, cornstarch, microcrystalline cellulose SH802, nifedipine, croscarmellose sodium,
Lauryl sodium sulfate and sunset yellow are added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 87.8%.
Embodiment 8
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, weight ratio 84.2%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs lactose monohydrate 1351.6g, nifedipine 100g, cross-linked carboxymethyl by batch inventory
It is spare after sodium cellulosate 80g, lauryl sodium sulfate 24g and sunset yellow 5g.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then lactose monohydrate, nifedipine, croscarmellose sodium, lauryl sodium sulfate and sunset yellow are added
Enter and is mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 88.3%.
Embodiment 9
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, weight ratio 84.2%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs cornstarch 1351.6g, nifedipine 100g, cross-linked carboxymethyl by batch inventory
It is spare after sodium cellulosate 80g, lauryl sodium sulfate 24g and sunset yellow 5g.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then cornstarch, nifedipine, croscarmellose sodium, lauryl sodium sulfate and sunset yellow are added
Enter and is mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 89.7%.
Embodiment 10
To prepare in terms of every ten thousand
Nifedipine Tablets include the ingredient of following mass percentage:
In the present embodiment, filler includes lactose monohydrate, weight ratio 84.2%.
Nifedipine Tablets provided in this embodiment the preparation method comprises the following steps:
Step S1: raw material micronization, spare after being pulverized using airslide disintegrating mill to nifedipine raw material, micro mist
Nifedipine particle size range is 5 μm~15 μm after change.
Step S2: ingredient prepares, and weighs microcrystalline cellulose SH8021351.6g by batch inventory, nifedipine 100g, hands over
It is spare after connection sodium carboxymethylcellulose 80g, lauryl sodium sulfate 24g and sunset yellow 5g.
Step S3: wet granulation weighs PVP K30 37.5g first, PVP K30 is dissolved in purified water, povidone
The concentration of K30 solution is 5%；
Then by microcrystalline cellulose SH802, nifedipine, croscarmellose sodium, lauryl sodium sulfate and
Sunset yellow is added to be mixed into wet granulator；
Then the PVP K30 solution that above-mentioned concentration is 5% is added in wet granulator to be mixed, soft material is prepared
Material；
Then the flexible material is dried using fluidized bed, controlled in drying process moisture content 4%~6% it
Between；
Then whole grain is carried out using 16 mesh screens.
Step S4: total mix weighs magnesium stearate 8g, particle is placed in three-dimensional mixer with magnesium stearate and is mixed,
Incorporation time is 5 minutes.
Step S5: tabletting carries out tabletting using 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and sheet hardness is
50N~80N.
Step S6: packaging, installation mold, PVC stiff sheet and aluminium foil are packed according to 10 sheet panels.
Dissolution Rate Testing is carried out to gained nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 84.2%.
Reference preparation
Nifedipine Tablets, 10mg；
Trade name: CASANMIL；
Manufacturer: Quan Xing drug Co., Ltd..
Dissolution Rate Testing is carried out to above-mentioned nifedipine tablets.Dissolution Rate Testing condition is as follows: taking 900ml water as dissolution
Medium, sampling filtration, takes subsequent filtrate to measure at 50 turns of paddle method, 30 minutes, and 6 tablet dissolution average values are 77.9%.
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all in essence of the invention
Made any modifications, equivalent replacements, and improvements etc., should all be included in the protection scope of the present invention within mind and principle.
Claims (10)
1. a kind of Nifedipine Tablets, which is characterized in that by the gross mass of the Nifedipine Tablets be the nitre benzene in terms of 100%
Plain film includes the ingredient of following mass percentage:
2. Nifedipine Tablets as described in claim 1, which is characterized in that the Nifedipine Tablets include that following quality percentage contains
The ingredient of amount:
Preferably, the Nifedipine Tablets include the ingredient of following mass percentage:
3. Nifedipine Tablets as claimed in claim 2, which is characterized in that the preferred Nifedipine Tablets include following quality
The ingredient of percentage composition:
4. Nifedipine Tablets as claimed in any one of claims 1 to 3, which is characterized in that the filler include lactose monohydrate,
The one or more of cornstarch and microcrystalline cellulose；
Preferably, the lubricant is magnesium stearate；And/or
The disintegrating agent is that croscarmellose sodium, crospovidone, sodium carboxymethyl starch and low substitution carboxylic propyl are fine
Tie up one of element or more than one；And/or
Described adhesive is povidone；And/or
The surfactant is lauryl sodium sulfate；And/or
The colorant is sunset yellow.
5. a kind of preparation method of such as described in any item Nifedipine Tablets of Claims 1 to 4, which is characterized in that including as follows
Step:
Raw material micronization, pulverizes nifedipine raw material, and nifedipine partial size is not more than 15 μm after micronization；
Ingredient prepares, and weighs filler, disintegrating agent, nifedipine, surfactant and colorant by batch inventory；
Wet granulation configures binder solution, dry after the ingredient of preparation is mixed with described adhesive solution, then passes through
Particle is obtained after sieve whole grain；
Total mix weighs lubricant, by the particle and the mix lubricant；
Tabletting carries out tabletting using formed punch.
6. the preparation method of Nifedipine Tablets as claimed in claim 5, which is characterized in that in the raw material micronization step,
Nifedipine raw material is pulverized using airslide disintegrating mill, nifedipine particle size range is 5 μm~15 μm after micronization
Preferably, in the ingredient preparation process, the filler includes lactose monohydrate, cornstarch and microcrystalline cellulose
One or more, the disintegrating agent are croscarmellose sodium, and the surfactant is lauryl sodium sulfate,
The colorant is sunset yellow.
7. the preparation method of Nifedipine Tablets as claimed in claim 5, which is characterized in that the wet granulation step includes:
Binder solution is prepared, adhesive is weighed according to quantity, described adhesive is dissolved in purified water；
Premixing, by filler, disintegrating agent, nifedipine, surfactant and colorant be added into wet granulator into
Row mixing；
Described adhesive solution is added in the wet granulator to be mixed；
It is dry, it is dried using fluidized bed；
Whole grain carries out whole grain using sieve.
8. the preparation method of Nifedipine Tablets as claimed in claim 5, which is characterized in that dried in the drying steps
Moisture content is controlled in journey between 4%~6%；
Preferably, in the whole grain step, sieve is 16 mesh~20 mesh screens.
9. the preparation method of Nifedipine Tablets as claimed in claim 5, which is characterized in that in the total mix step, the profit
Lubrication prescription is magnesium stearate；
The particle is mixed to be placed in three-dimensional mixer with the magnesium stearate and is mixed, incorporation time is no less than 5 minutes；
Preferably, in the tableting step, the formed punch is 7.5mm formed punch, and tablet weight variation is not more than ± 3% after tabletting, and piece is hard
Degree is 50N~80N.
10. such as the preparation method of the described in any item Nifedipine Tablets of claim 5-9, which is characterized in that the tableting step
Afterwards further include:
Packaging: installation mold, stiff sheet and aluminium foil are packed according to 10 sheet panels.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811305346.7A CN109350601A (en) | 2018-11-05 | 2018-11-05 | A kind of Nifedipine Tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811305346.7A CN109350601A (en) | 2018-11-05 | 2018-11-05 | A kind of Nifedipine Tablets and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109350601A true CN109350601A (en) | 2019-02-19 |
Family
ID=65344180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811305346.7A Pending CN109350601A (en) | 2018-11-05 | 2018-11-05 | A kind of Nifedipine Tablets and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN109350601A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114533686A (en) * | 2022-02-15 | 2022-05-27 | 湖南普道医药技术有限公司 | Oral solid preparation of dihydropyridine medicine and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104666269A (en) * | 2015-03-17 | 2015-06-03 | 常州康普药业有限公司 | Preparation method of nifedipine tablet |
| CN106265554A (en) * | 2015-05-19 | 2017-01-04 | 上海信谊天平药业有限公司 | A kind of Nifedipine Tablets and preparation method thereof |
| CN107550882A (en) * | 2016-06-30 | 2018-01-09 | 康普药业股份有限公司 | A kind of Nifedipine |
-
2018
- 2018-11-05 CN CN201811305346.7A patent/CN109350601A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104666269A (en) * | 2015-03-17 | 2015-06-03 | 常州康普药业有限公司 | Preparation method of nifedipine tablet |
| CN106265554A (en) * | 2015-05-19 | 2017-01-04 | 上海信谊天平药业有限公司 | A kind of Nifedipine Tablets and preparation method thereof |
| CN107550882A (en) * | 2016-06-30 | 2018-01-09 | 康普药业股份有限公司 | A kind of Nifedipine |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114533686A (en) * | 2022-02-15 | 2022-05-27 | 湖南普道医药技术有限公司 | Oral solid preparation of dihydropyridine medicine and preparation method thereof |
| CN114533686B (en) * | 2022-02-15 | 2023-10-20 | 湖南普道医药技术有限公司 | Oral solid preparation of dihydropyridines medicine and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI453203B (en) | New solid pharmaceutical formulations comprising bibw 2992 | |
| CN101647797B (en) | Pharmaceutical composition containing Amlodipine besilate and valsartan and preparation method thereof | |
| CN105579031B (en) | Stabilizing pharmaceutical composition containing Amlodipine and Valsartan | |
| CN107137370B (en) | Preparation method of telmisartan tablets | |
| CN104042580B (en) | A kind of valsartan dispersible tablet and preparation method thereof | |
| EP4284344A1 (en) | Pharmaceutical composition | |
| CN109350601A (en) | A kind of Nifedipine Tablets and preparation method thereof | |
| US6054145A (en) | Making dosage units using low shear granulation | |
| CN102526748B (en) | Oral tablet containing Valsartan, Hydrochioro and Amlodipine Besylate Tablet | |
| CN104337787B (en) | Pharmaceutical preparation containing razaxaban | |
| Al-Achi | Tablets: a brief overview | |
| CN105769905A (en) | Potassium chloride sustained release tablet and preparation method thereof | |
| CN106983726A (en) | Azilsartan piece and preparation method thereof | |
| CN109953960A (en) | A kind of preparation method of amlodipine besylate tablets | |
| CN106822155B (en) | Piece and preparation method thereof in three Compound Tablet of efavirenz, Lamivudine and tenofovir disoproxil fumarate | |
| CN104546769B (en) | A kind of Amlodipine Besylate Tablet solid oral tablet and preparation method thereof | |
| CN106668016B (en) | Solid preparation of azilsartan and amlodipine besylate composition and preparation method thereof | |
| CN113456639A (en) | Anti-arrhythmia pharmaceutical composition and preparation method thereof | |
| CN109953957A (en) | A kind of amlodipine besylate tablets and preparation method thereof | |
| CN113768889B (en) | Cilostazol-containing pharmaceutical composition and preparation method thereof | |
| Soares Sobrinho et al. | Development and in vitro evaluation of tablets based on the antichagasic benznidazole | |
| CN109953958A (en) | A kind of mixing amlodipine besylate tablets and preparation method thereof | |
| CN108853044A (en) | A kind of Nifedipine sustained release tablets and preparation method thereof | |
| CN112826819B (en) | Preparation method of valsartan amlodipine tablets and valsartan amlodipine tablets | |
| CN109966262A (en) | Lenalidomide pharmaceutical composition |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Pan Haiqun Inventor after: Ge Zhimin Inventor after: Sun Lina Inventor after: Huo Zhiqiang Inventor after: Dai Xinmin Inventor before: Pan Haiqun Inventor before: Ge Zhimin Inventor before: Sun Lina Inventor before: Huo Zhiqiang |