CN106074542A - A kind of preparation method of Azilsartan potassium salt soft capsule - Google Patents
A kind of preparation method of Azilsartan potassium salt soft capsule Download PDFInfo
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- CN106074542A CN106074542A CN201610759552.XA CN201610759552A CN106074542A CN 106074542 A CN106074542 A CN 106074542A CN 201610759552 A CN201610759552 A CN 201610759552A CN 106074542 A CN106074542 A CN 106074542A
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- potassium salt
- soft capsule
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- utricule
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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
- A61K31/4245—Oxadiazoles
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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
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
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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
- A61K9/4858—Organic compounds
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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
- A61K9/4875—Compounds of unknown constitution, e.g. material from plants or animals
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Abstract
The present invention relates to the preparation method of a kind of Azilsartan potassium salt soft capsule.Step: with gelatin, stearic acid, soybean protein, glycerol and pure water for utricule raw material, makes and obtains utricule；The content being uniformly mixed according to prescription；By content and utricule through pelleting, shape, wash ball, be dried, pick ball and subpackage step, prepare soft capsule.The drug regimen of the treatment hypertension of the present invention, reasonable mixture ratio, with rapid delivery of pharmaceuticals, described disease can be produced good curative effect.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to the preparation method of a kind of Azilsartan potassium salt soft capsule.
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 is special
Profit expires (CN1946717) on February 22nd, 2025.
Summary of the invention
It is an object of the invention to: provide the preparation method of the Azilsartan potassium salt soft capsule of a kind of good stability, mainly
It is to realize above-mentioned purpose by addition stability component.
Technical scheme is:
The preparation method of a kind of Azilsartan potassium salt soft capsule, comprises the steps:
1st step, makes utricule: by weight, with gelatin 15～25 parts, stearic acid 3～6 parts, soybean protein 2～3 parts, glycerol
10～25 parts is utricule raw material with pure water 10～15 parts, injects in glue pot by glycerol and pure water, and heated and stirred adds bright
Glue, stearic acid and soybean protein, continue the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: preparation content: by weight, by soybean oil 30～90 parts, unsaturated fatty acid 4～9 parts, Azilsartan
Ester potassium salt 20～50 parts and glycerol 5～20 parts mix, and cross colloid mill, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
In the 1st described step, the temperature of agitating heating is 60～70 DEG C.
In the 2nd described step, unsaturated fatty acid is selected from docosahexenoic acid, eicosapentaenoic acid, fish oil, Semen Lini
Oil, borage oil, alpha-linolenic acid, gamma-Linolenic acid, conjugated linoleic acid or Saw Palmetto P.E.
In the 2nd described step, the temperature 50 during mixing～70 DEG C, incorporation time 20～40min, the number of times crossing colloid mill is
1～3 time.
The Azilsartan potassium salt soft capsule that the present invention prepares has good stability, the advantage that character is stable.
Detailed description of the invention:
The content of the soft capsule of the present invention, in addition to the above-mentioned components, according to actual application needs, it is also possible to comprise it
Its additive component, described additive component can comprise other components of one or more applicable foods.These include
Antioxidant, emulsifying agent, preservative, sweeting agent, essence, pH adjusting agent etc..Additive component is mixed with compositions mixed
Weight percentage ranges shared by compound can be maximum 89wt%, such as 10～89wt%, more preferably 20～75wt%.
Antioxidant can use tocopherols such as alpha-tocopherol, alpha-tocopherol cetylate, alpha-tocopherol acetate,
Tert-butyl hydroxy toluene, butylhydroxy anisole, ascorbic acid, its salt and ester, such as sodium ascorbate, calcium ascorbate,
Vitamin C acyl phosphate ester, the fatty acid ester such as Vitamin C acyl stearate of ascorbic acid and Vitamin C acyl cetylate and ethoxy
Base quinoline.
The fatty acid ester such as Vitamin C acyl Petiolus Trachycarpi of the example of emulsifying agent especially lipophile dispersant, e.g. ascorbic acid
Acid esters, polyglyceryl fatty acid ester such as polyglycereol-3-polyricinoleate, fatty acid esters of sorbitan, especially anhydrosorbitol
Alcohol C10～C28 fatty acid ester.
As pH adjusting agent, can be included in the preparation compositions of the present invention to improve or reduce the preparation group of the present invention
The pH of compound.The pH of described preparation compositions can be lowered or improve, the effect perceived for sense organ, or is used for improving physics and chemistry
Characteristic, such as, increase the dissolubility of the compound of dissolving.PH adjusting agent may refer to acidulant or basifier.Such as, lactic acid, lemon
Lemon acid, malic acid, potassium hydroxide, calcium hydroxide and magnesium hydroxide.
Preservative, the non-limiting example that can be optionally included in the preservative in the preparation compositions of the present invention includes:
Acetic acid, citric acid, benzoic acid, sorbic acid, sulfur dioxide, Potassium Benzoate, potassium sorbate.
As essence, oils and fats essence and the powdered flavors such as one kind or two or more natural essence, compound essence are preferably used, but
It is not particularly limited.Such as, wintergreen oil, Oleum Cinnamomi, menthol oil, oleum menthae viridis, lime oil, Oleum lavandula angustifolia, Fructus Fragariae Ananssae oil, chinese cymbidium
Ketone.
As sweeting agent, preferably commonly use sweeting agent, such as, select at least from maltose alcohol, sucrose, glucose, glucosan
1 kind.
Embodiment 1
The preparation method of Azilsartan potassium salt soft capsule, step:
1st step, makes utricule: by weight, with 15 parts of gelatin, stearic acid 3 parts, soybean protein 2 parts, glycerol 10 parts and pure water
10 parts is utricule raw material, injects in glue pot by glycerol and pure water, and 60 DEG C of heated and stirred add gelatin, stearic acid and Semen sojae atricolor
Albumen, continues the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: preparation content: by weight, by soybean oil 85 parts, gamma-Linolenic acid 4 parts, Azilsartan potassium salt 20 parts,
And glycerol 20 parts mixes at 50 DEG C, incorporation time 20min, cross colloid mill 3 times, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
Embodiment 2
The preparation method of Azilsartan potassium salt soft capsule, step:
1st step, makes utricule: by weight, with 25 parts of gelatin, stearic acid 6 parts, soybean protein 3 parts, glycerol 25 parts and pure water
15 parts is utricule raw material, injects in glue pot by glycerol and pure water, and 70 DEG C of heated and stirred add gelatin, stearic acid and Semen sojae atricolor
Albumen, continues the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: preparation content: by weight, by soybean oil 85 parts, gamma-Linolenic acid 4 parts, Azilsartan potassium salt 40 parts,
And glycerol 20 parts mixes at 50 DEG C, incorporation time 20min, cross colloid mill 3 times, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
Embodiment 3
The preparation method of Azilsartan potassium salt soft capsule, step:
1st step, makes utricule: by weight, with 20 parts of gelatin, stearic acid 5 parts, soybean protein 3 parts, glycerol 20 parts and pure water
12 parts is utricule raw material, injects in glue pot by glycerol and pure water, and 65 DEG C of heated and stirred add gelatin, stearic acid and Semen sojae atricolor
Albumen, continues the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: preparation content: by weight, by soybean oil 90 parts, gamma-Linolenic acid 4 parts, Azilsartan potassium salt 80 parts,
And glycerol 15 parts mixes at 50 DEG C, incorporation time 20min, cross colloid mill 3 times, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
Embodiment 4
The preparation method of Azilsartan potassium salt soft capsule, step:
1st step, makes utricule: by weight, with 20 parts of gelatin, stearic acid 5 parts, soybean protein 3 parts, glycerol 20 parts and pure water
12 parts is utricule raw material, injects in glue pot by glycerol and pure water, and 65 DEG C of heated and stirred add gelatin, stearic acid and Semen sojae atricolor
Albumen, continues the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: preparation content: by weight, by soybean oil 90 parts, gamma-Linolenic acid 4 parts, Azilsartan potassium salt 60 parts,
And glycerol 15 parts mixes at 50 DEG C, incorporation time 20min, cross colloid mill 3 times, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
Claims (4)
1. the preparation method of an Azilsartan potassium salt soft capsule, it is characterised in that comprise the steps:
1st step, makes utricule: by weight, with gelatin 15～25 parts, stearic acid 0～6 parts, soybean protein 0～3 parts, glycerol
10～25 parts is utricule raw material with pure water 10～15 parts, injects in glue pot by glycerol and pure water, and heated and stirred adds bright
Glue, stearic acid and soybean protein, continue the final vacuum deaeration that stirs, and makes and obtains utricule；
2nd step: by weight, by soybean oil 30～90 parts, unsaturated fatty acid 4～9 parts, Azilsartan potassium salt 20～50
Part and glycerol 5～20 parts mix, cross colloid mill, the content being uniformly mixed；
3rd step: the content that the 2nd step is obtained and the 1st step obtain utricule through pelleting, shape, wash ball, be dried, pick ball and point
Dress step, prepares Azilsartan potassium salt soft capsule.
The preparation method of Azilsartan potassium salt soft capsule the most according to claim 1, it is characterised in that: described the 1st
In step, the temperature of agitating heating is 60～70 DEG C.
The preparation method of Azilsartan potassium salt soft capsule the most according to claim 1, it is characterised in that: described the 2nd
In step, unsaturated fatty acid is selected from docosahexenoic acid, eicosapentaenoic acid, fish oil, Semen Lini oil, borage oil, α-Asia
Fiber crops acid, gamma-Linolenic acid, conjugated linoleic acid or Saw Palmetto P.E.
The preparation method of Azilsartan potassium salt soft capsule the most according to claim 1, it is characterised in that: described the 2nd
In step, the temperature 50 during mixing～70 DEG C, incorporation time 20～40min, the number of times crossing colloid mill is 1～3 time.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610759552.XA CN106074542A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt soft capsule |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610759552.XA CN106074542A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt soft capsule |
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| CN106074542A true CN106074542A (en) | 2016-11-09 |
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| CN201610759552.XA Pending CN106074542A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt soft capsule |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102342944A (en) * | 2011-07-14 | 2012-02-08 | 丁尧 | Medicament composition for treating hypertension |
| CN102711735A (en) * | 2009-11-20 | 2012-10-03 | Gp制药股份公司 | Capsules of active pharmaceutical ingredients and polyunsaturated fatty acid esters for the treatment of cardiovascular diseases |
| CN105476011A (en) * | 2015-12-27 | 2016-04-13 | 刘家容 | Preparing method of lycopene soft capsule |
-
2016
- 2016-08-30 CN CN201610759552.XA patent/CN106074542A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102711735A (en) * | 2009-11-20 | 2012-10-03 | Gp制药股份公司 | Capsules of active pharmaceutical ingredients and polyunsaturated fatty acid esters for the treatment of cardiovascular diseases |
| CN102342944A (en) * | 2011-07-14 | 2012-02-08 | 丁尧 | Medicament composition for treating hypertension |
| CN105476011A (en) * | 2015-12-27 | 2016-04-13 | 刘家容 | Preparing method of lycopene soft capsule |
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Application publication date: 20161109 |
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