CN106214649A - A kind of Azilsartan potassium salt solid dispersion preparation and preparation method thereof - Google Patents
A kind of Azilsartan potassium salt solid dispersion preparation and preparation method thereof Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- 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
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- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
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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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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- 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
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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Abstract
The present invention relates to field of medicine preparations, specifically disclose a kind of Azilsartan potassium salt solid dispersion preparation and preparation method thereof.Azilsartan potassium salt solid dispersion preparation of the present invention includes Azilsartan potassium salt, polyvidone, specific lubricant and specific disintegrating agent and diluent.The result of extraction of invention formulation, bioavailability and stability, the beneficially industrialized production of Azilsartan potassium salt solid dispersion preparation.
Description
Technical field
The present invention relates to field of medicine preparations, be specifically related to a kind of Azilsartan potassium salt solid dispersion preparation and system thereof
Preparation Method.
Background technology
Azilsartan potassium salt (azilsartan medoxomil) is Japan's military field research and development.Before the one of Azilsartan
Medicine, is hydrolyzed to Azilsartan during gastrointestinal absorption.On February 22nd, 2011 lists in FDA approval, trade name: Edarbi,
Specification is 40mg, 80mg.In April, 2012, Azilsartan listed in Japan, trade name: Azilva, specification: 20mg, 40mg.A Qi
Husky smooth ester is a kind of selectivity AT1 subtype angiotensin II receptor antagonist.Azilsartan selective exclusion angiotensin
II be combined with AT1 receptor more than 10000 times of AT2 receptor (Azilsartan the affinity of AT1 receptor is exceeded), thus block
The vasoconstriction that angiotensinⅡ causes, Aldosterone Secretion etc. rises blood pressure effect.Its effect does not relies on angiotensinⅡ
Route of synthesis, therefore avoid the ACEI impact on Kallidin I level.With angiotensin-convertion enzyme inhibitor (ACEI) class blood pressure lowering
Medicine is compared, and medication is respectively provided with steady blood pressure lowering, will not cause the advantage of dry cough alone or in combination, the most persistently hypotensive activity.
Diabetics can also be produced potential by part peroxide activator enzyme body proliferator activated receptor-γ (PPAR-γ)
Protective effect, relevant clinical result of the test show its clinical effectiveness be better than present clinical widely used olmesartan medoxomil and
Valsartan.On March 5th, 2012, Edarbi is by global famous medicine and medical research/consultant firm-Decision
Resources company confirms as the golden standard that depressor is evaluated, and to the year two thousand twenty, does not has medicine may substitute this of Edarbi
One golden standard status.Although currently some emerging depressor has certain potentiality, but himself is in effectiveness, safety
It Edarbi may cannot be replaced with the defect on toleration and/or medication.[intellectual property situation] compound patent
(CN1946717) expire on February 22nd, 2025.
Summary of the invention
It is an object of the invention to provide a kind of Azilsartan potassium salt solid dispersion preparation and preparation method thereof, this
The following technical scheme of bright offer:
A kind of Azilsartan potassium salt solid dispersion particles agent, including Azilsartan potassium salt, polyvidone and lubricant；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more.
In certain embodiments of the present invention, described lubricant can be further selected from Pulvis Talci, magnesium stearate, titanium dioxide
One in silicon, sodium stearyl fumarate, sodium lauryl sulphate, two or three；Further, described lubricant is optional
From:
Sodium lauryl sulphate and magnesium stearate two kinds；
Sodium lauryl sulphate and Pulvis Talci two kinds；
Silicon dioxide and magnesium stearate two kinds；Or sodium lauryl sulphate, silicon dioxide and magnesium stearate three kinds.
Wherein, the ratio between multiple lubricant is not limited, but in certain embodiments of the present invention, 12
Ratio between alkyl sodium sulfate and magnesium stearate, silicon dioxide is 1:1:4, the ratio between sodium lauryl sulphate and Pulvis Talci
Example is 1:2.
In certain embodiments of the present invention, in parts by weight, described all dosage forms include 40-100 part Azilsartan
Ester potassium salt, 80-250 part polyvidone and 2-6 part lubricant；Described weight portion can use the unit of weight of any routine with specifically
Form represents, as microgram, milligram, gram, kilogram, two, jin, kilogram etc., such as, concrete with mg as weight portion of described granule
The form of expression, including 40-100mg Azilsartan potassium salt, 80-250mg polyvidone and 2-6mg lubricant.
In certain embodiments of the present invention, described polyvidone further selected from 30 POVIDONE K 30 BP/USP 25, PVP K30 or
30 POVIDONE K 30 BP/USP 90.
In certain embodiments of the present invention, the composition of described granule further can be as follows:
Granule of the present invention filling capsule shells is capsule preparations, therefore present invention also offers a kind of Azilsartan potassium
Salt solid dispersion capsule, including granule of the present invention and capsule shells.
Present invention also offers the preparation method of described granule, by Azilsartan potassium salt, polyvidone and partial lubrication
Agent mixing prepares solid dispersion by melt extrusion method, then adds rest lubricant and obtains described granule；Or will
Azilsartan potassium salt and polyvidone are dissolved in organic solvent, prepare solid by solvent evaporated method or spray drying method and divide
A prose style free from parallelism, obtains described granule after adding lubricant；
Wherein, when being prepared by melt extrusion method, described partial lubrication agent refers not only to a part for a kind of lubricant, but also
Refer to a certain lubricant during multiple lubricant, preferably prepared by melt extrusion method with silica containing multiple lubricant,
It is described partial lubrication agent with silicon dioxide.
Additionally, the present invention also provides for a kind of Azilsartan potassium salt solid dispersion tablet, including Azilsartan potassium salt,
Polyvidone, lubricant, disintegrating agent and diluent；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more；
Described disintegrating agent is selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, low substituted hydroxy-propyl fiber
One or more in element；
Described diluent in microcrystalline Cellulose, starch, pregelatinized Starch, lactose, mannitol, the dextrin one or both with
On.
In certain embodiments of the present invention, described polyvidone further selected from 30 POVIDONE K 30 BP/USP 25, PVP K30 or
30 POVIDONE K 30 BP/USP 90.
In certain embodiments of the present invention, the composition of described tablet further can be as follows:
Mode one:
| Component | Weight portion |
| Azilsartan potassium salt | 40 |
| PVP K30 | 85 |
| Microcrystalline Cellulose 102 | 50 |
| Cross-linking sodium carboxymethyl cellulose | 20 |
| Sodium lauryl sulphate | 8 |
| Silicon dioxide | 2 |
| Tablet weight | 215 |
Mode two:
| Component | Weight portion |
| Azilsartan potassium salt | 80 |
| PVP K30 | 150 |
| Microcrystalline Cellulose 102 | 90 |
| Cross-linking sodium carboxymethyl cellulose | 20 |
| Sodium lauryl sulphate | 7 |
| Silicon dioxide | 3 |
| Tablet weight | 350 |
Mode three:
| Component | Weight portion |
| Azilsartan potassium salt | 20 |
| PVP K30 | 60 |
| Microcrystalline Cellulose 102 | 30 |
| Cross-linking sodium carboxymethyl cellulose | 10 |
| Sodium lauryl sulphate | 7 |
| Silicon dioxide | 3 |
| Tablet weight | 130 |
Present invention also offers the preparation method of described tablet, Azilsartan potassium salt and polyvidone be dissolved in organic solvent,
And prepare solid dispersion by solvent evaporated method or spray drying method, it is subsequently adding lubricant, disintegrating agent and diluent
Mixed pressuring plate, it is thus achieved that described tablet；Or melt extrusion method is passed through in Azilsartan potassium salt, polyvidone and partial lubrication agent mixing
Prepare solid dispersion, then add disintegrating agent, diluent and rest lubricant mixed pressuring plate, it is thus achieved that described tablet；
Wherein, when being prepared by melt extrusion method, described partial lubrication agent refers not only to a part for a kind of lubricant, but also
Refer to a certain lubricant during multiple lubricant, preferably prepared by melt extrusion method with silica containing multiple lubricant,
It is described partial lubrication agent with silicon dioxide.
Detailed description of the invention
The invention discloses a kind of Azilsartan potassium salt solid dispersion preparation and preparation method thereof, method is as follows:
1, melt extrusion method
Take Azilsartan potassium salt and the polyvidone of recipe quantity, add partial lubrication agent, mixing, put in double screw extruder and extrude
This mixture, in extrusion, applies vacuum to melt through row degassing to extruded tube, through two to turning calender roller, and should
Extrudate calendering, subsequently to cooling before grinding, it is thus achieved that solid dispersion.
2, spray drying method
By the Azilsartan potassium salt of recipe quantity, polyvidone, be dissolved in organic solvent (acetone: methanol v/v=1:1-2), spraying
It is dried, inlet temperature 85-90 DEG C, air quantity 20-25kg/hr, atomizing pressure 0.5-0.75bar, atomization gas flow 1.5-2.0kg/
Hr, for liquid stream 4.5-5.0ml/min, the spray-dried powders obtained is vacuum dried 24 hours at putting 45-60 DEG C, it is thus achieved that solid
Dispersion.
3, solvent evaporated method
By the Azilsartan potassium salt of recipe quantity, polyvidone, it is dissolved in organic solvent (acetone: dehydrated alcohol v/v=2:1, third
Ketone: dichloromethane v/v=3:1, methanol: dichloromethane v/v=4:1 or acetone: methanol v/v=3:1) solvent in, at 55-60
Water-bath at DEG C, vacuum 0.07-0.08MPa, recovered under reduced pressure organic solvent, until in after thick, continue reduced vacuum and is dried 1-
3h, proceeds in vacuum drying oven, crosses 80 mesh sieves and pulverizes, it is thus achieved that solid dispersion after 40-65 DEG C of dry 48h.
Below in conjunction with embodiment, the present invention is expanded on further.
Embodiment 1: Azilsartan potassium salt solid dispersion tablet
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 40 |
| PVP K30 | 85 |
| Microcrystalline Cellulose 102 | 50 |
| Cross-linking sodium carboxymethyl cellulose | 20 |
| Sodium lauryl sulphate | 8 |
| Silicon dioxide | 2 |
| Tablet weight | 215 |
Preparation process: solvent evaporated method
The Azilsartan potassium salt of recipe quantity, PVP K30 will be taken, be dissolved in acetone: in the solvent of methanol (1:3), at 60 DEG C
Decompression volatilization in water-bath, vacuum 0.07-0.08MPa, recovered under reduced pressure organic solvent, until in after thick, continues reduced vacuum
It is dried 1h, proceeds in vacuum drying oven, cross 80 mesh sieves after 40 DEG C of dry 48h and pulverize, obtain solid dispersion.
Prepared solid dispersion is added the microcrystalline Cellulose pH102 of recipe quantity, cross-linking sodium carboxymethyl cellulose, 12
Alkyl sodium sulfate, silicon dioxide, mixing, direct compression.
Embodiment 2: Azilsartan potassium salt solid dispersion tablet
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 80 |
| PVP K30 | 150 |
| Microcrystalline Cellulose 102 | 90 |
| Cross-linking sodium carboxymethyl cellulose | 20 |
| Sodium lauryl sulphate | 7 |
| Pulvis Talci | 3 |
| Tablet weight | 350 |
Preparation process: solvent evaporated method
Take the Azilsartan potassium salt of recipe quantity, PVP K30, be dissolved in methanol: in the solvent of dichloromethane (4:1), at 60 DEG C
Lower water-bath, vacuum 0.07-0.08MPa, recovered under reduced pressure organic solvent, until in after thick, continue reduced vacuum and be dried 1h,
Proceed in vacuum drying oven, cross 80 mesh sieves after 40 DEG C of dry 48h and pulverize, obtain solid dispersion.
Prepared solid dispersion is added the microcrystalline Cellulose pH102 of recipe quantity, polyvinylpolypyrrolidone, lauryl sulphate acid
Sodium, Pulvis Talci, mixing, direct compression.
Embodiment 3: Azilsartan potassium salt solid dispersion tablet
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 20 |
| PVP K30 | 60 |
| Microcrystalline Cellulose 102 | 30 |
| Cross-linking sodium carboxymethyl cellulose | 10 |
| Sodium lauryl sulphate | 7 |
| Silicon dioxide | 3 |
| Tablet weight | 130 |
Preparation process: solvent evaporated method
By the Azilsartan potassium salt of recipe quantity, PVP K30, it is dissolved in acetone: in the solvent of dichloromethane (3:1), at 55 DEG C
Lower water-bath, vacuum 0.07-0.08MPa, recovered under reduced pressure organic solvent, until in after thick, continue reduced vacuum and is dried 3h, turn
Enter in vacuum drying oven, cross 80 mesh sieves after 60 DEG C of dry 48h and pulverize, obtain solid dispersion.
Prepared solid dispersion is added the pregelatinized Starch of recipe quantity, low-substituted hydroxypropyl cellulose, dodecyl
Sodium sulfate, silicon dioxide, mixing, direct compression.
Embodiment 4: Azilsartan potassium salt solid dispersion tablet
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 10 |
| PVP K30 | 50 |
| Lactose | 20 |
| Carboxymethyl starch sodium | 10 |
| Sodium lauryl sulphate | 7 |
| Silicon dioxide | 3 |
| Tablet weight | 100 |
Preparation process: spray drying method
By the Azilsartan potassium salt of recipe quantity, PVP K30, it is dissolved in acetone: in the solvent of methanol (1:1), is spray-dried, enters
Air temperature 85 DEG C, air quantity 25kg/hr, atomizing pressure 0.5bar, atomization gas flow 1.5kg/hr, for flow quantity 4.5ml/min,
To spray-dried powders be placed at 45 DEG C vacuum drying 24 hours, obtain solid dispersion.
The lactose of recipe quantity, carboxymethyl starch sodium, sodium lauryl sulphate, silicon dioxide is added by obtaining solid dispersion,
Mixing, direct compression.
Embodiment 5: Azilsartan potassium salt solid dispersion particles agent
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 5 |
| PVP K30 | 50 |
| Microcrystalline Cellulose 102 | 30 |
| Cross-linking sodium carboxymethyl cellulose | 10 |
| Sodium lauryl sulphate | 8 |
| Silicon dioxide | 2 |
| Weight | 105 |
Preparation method: solvent evaporated method
By the Azilsartan potassium salt of recipe quantity, PVP K30, it is dissolved in acetone: in the solvent of dehydrated alcohol (2:1), add in a subtle way
Crystalline cellulose 102, cross-linking sodium carboxymethyl cellulose dissolve, and water-bath at 60 DEG C, vacuum 0.07-0.08MPa, recovered under reduced pressure has
Machine solvent, until in after thick, continue reduced vacuum and is dried 3h, proceed in vacuum drying oven, cross 80 mesh sieves after 65 DEG C of dry 48h
Pulverize, obtain solid dispersion.
Prepared solid dispersion is added the microcrystalline Cellulose 102 of recipe quantity, cross-linking sodium carboxymethyl cellulose, dodecane
Base sodium sulfate and silicon dioxide, mixing, subpackage, obtain granule.
Embodiment 6: Azilsartan potassium salt solid dispersion capsule
Prescription:
| Component | Weight portion |
| Azilsartan potassium salt | 40 |
| PVP K30 | 85 |
| Sodium lauryl sulphate | 20 |
| Magnesium stearate | 8 |
| Gross weight | 153 |
Preparation method: spray drying method
By the Azilsartan potassium salt of recipe quantity, 30 POVIDONE K 30 BP/USP 90, it is dissolved in acetone: in the solvent of methanol (1:2), is spray-dried, enters
Air temperature 90 DEG C, air quantity 20kg/hr, atomizing pressure 0.75bar, atomization gas flow 2.0kg/hr, for flow quantity 5.0ml/min,
The spray-dried powders obtained is placed at 60 DEG C vacuum drying 24 hours, obtains solid dispersion.
Prepared solid dispersion is added the eicosyl sodium sulfate of recipe quantity, magnesium stearate, mixing, it is thus achieved that granule
Agent, pours into 4# capsule and is capsule preparations.
Claims (10)
1. an Azilsartan potassium salt solid dispersion particles agent, it is characterised in that include Azilsartan potassium salt, polyvidone
And lubricant；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more.
Granule the most according to claim 1, it is characterised in that described lubricant is selected from Pulvis Talci, magnesium stearate, titanium dioxide
One in silicon, sodium stearyl fumarate, sodium lauryl sulphate, two or three.
The most according to claim 1, granule, it is characterised in that in parts by weight, including 40-100 part Azilsartan potassium
Salt, 50-200 part polyvidone and 2-6 part lubricant.
4. the preparation method of granule described in claim 1, it is characterised in that by Azilsartan potassium salt, polyvidone and part
Lubricant mixing prepares solid dispersion by melt extrusion method, then adds rest lubricant and obtains described granule；
Or Azilsartan potassium salt and polyvidone are dissolved in organic solvent, prepared solid by solvent evaporated method or spray drying method
Body dispersion, obtains described granule after adding lubricant；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more.
The most according to claim 4, preparation method, it is characterised in that in parts by weight, each parts by weight of raw materials is 40-100 part
Azilsartan potassium salt, 80-250 part polyvidone and 2-6 part lubricant.
6. an Azilsartan potassium salt solid dispersion capsule, it is characterised in that include described in claim 1-3 any one
Granule and capsule shells.
7. an Azilsartan potassium salt solid dispersion tablet, it is characterised in that include Azilsartan potassium salt, polyvidone,
Lubricant, disintegrating agent and diluent；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more；
Described disintegrating agent is selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, low substituted hydroxy-propyl fiber
One or more in element；
Described diluent in microcrystalline Cellulose, starch, pregelatinized Starch, lactose, mannitol, the dextrin one or both with
On.
Tablet the most according to claim 7, it is characterised in that described lubricant is selected from Pulvis Talci, magnesium stearate, titanium dioxide
One in silicon, sodium stearyl fumarate, sodium lauryl sulphate, two or three.
9. it is characterized in that, in parts by weight, including 40-100 part Azilsartan potassium salt, 80-220 part polyvidone, 2-6 part profit
Lubrication prescription, 5-10 part disintegrating agent and 30-70 part diluent.
10. the preparation method of tablet described in claim 7, it is characterised in that Azilsartan potassium salt and polyvidone are dissolved in and have
In machine solvent, and prepare solid dispersion by solvent evaporated method or spray drying method, be subsequently adding lubricant, disintegrating agent
With diluent mixed pressuring plate, it is thus achieved that described tablet；Or by Azilsartan potassium salt, polyvidone and partial lubrication agent mixing by molten
Body extrusion molding prepares solid dispersion, then adds disintegrating agent, diluent and rest lubricant mixed pressuring plate, it is thus achieved that institute
State tablet；
Described lubricant is selected from Pulvis Talci, magnesium stearate, silicon dioxide, sodium stearyl fumarate, sodium lauryl sulphate
Plant or two or more；
Described disintegrating agent is fine selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium or low substituted hydroxy-propyl
Dimension element；
Described diluent in microcrystalline Cellulose, starch, pregelatinized Starch, lactose, mannitol, the dextrin one or both with
On.
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Application publication date: 20161214 |