CN106692116A - Capsule-type inhalation aerosol powder containing isoforskolin - Google Patents
Capsule-type inhalation aerosol powder containing isoforskolin Download PDFInfo
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- CN106692116A CN106692116A CN201510800281.3A CN201510800281A CN106692116A CN 106692116 A CN106692116 A CN 106692116A CN 201510800281 A CN201510800281 A CN 201510800281A CN 106692116 A CN106692116 A CN 106692116A
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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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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Abstract
本发明属药物制剂领域，涉及一种含异佛司可林的胶囊型吸入粉雾剂。本发明以异佛司可林为有效成分，添加合适的辅料，如载体、抗粘附剂、润滑剂、抗静电剂和氨基酸等，通过适宜制剂工艺制成。本发明针对支气管哮喘吸入给药的用药需求，根据异佛司可林自身的理化性质特点，同时结合我国现有粉雾剂的生产水平而设计，能满足临床用药、患者顺应性、工业化规模生产等各项要求。The invention belongs to the field of pharmaceutical preparations, and relates to a capsule type inhalation powder mist containing isofaskolin. The invention uses isofaskolin as an active ingredient, adds suitable auxiliary materials, such as carrier, anti-adhesive agent, lubricant, antistatic agent and amino acid, etc., and is prepared through a suitable preparation process. The present invention aims at the drug demand of bronchial asthma by inhalation, and is designed according to the physical and chemical properties of isofaskolin itself, combined with the production level of the existing powder aerosol in my country, which can meet the needs of clinical medication, patient compliance, and industrial scale production and other requirements.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be related to a kind of capsule type inhalation aerosol powder containing isoforskolin and its
Preparation method.
Background technology
Isoforskolin (isoforskolin) is labdane diterpenes compound, is primarily present in lip
In section Coleus plant Coleus forskohlii Coleus forskohlii Brig.Coleus forskohlii dries herb
Referred to as coleus forskohlin.Research discloses isoforskolin has a powerful adenyl cyclase activation, can directly,
Quickly, reversibly improve cell and tissue in CAMP concentration, have expansion bronchus, cardiac stimulant, hypotensive,
Reduce intraocular pressure and the physiologically active such as antitumor.Can be used for treat bronchial astehma, injury of lungs, angiocardiopathy,
Essential hypertension, glaucoma, metastases, obesity, male sexual disfunction and skin disease etc..
At present containing isoforskolin listing preparation be coleus forskohlin oral liquid and coleus forskohlin capsule, be all coleus forskohlin and
The compound preparation of the root of purple-flowered peucedanum, Radix Glycyrrhizae composition, for cough-relieving, relievings asthma；Two preparation is with isoforskolin as index
Composition, wherein, coleus forskohlin oral liquid every (10mL) must not be less than 0.4mg containing isoforskolin；Capsule
Content be every 0.15-0.16mg.
Additionally, the formulation relevant with isoforskolin or coleus forskohlin disclosed in Chinese patent and document has：Dripping pill,
Tablet, electuary, granule, powder spray, aerosol, Fat Emulsion, emulsion, ophthalmic suspension etc..Wherein,
Formulation for Treating Bronchial Asthma has：Dripping pill (A of publication number CN 1682840), tablet (publication number CN
103720668 A), electuary (publication number CN 101433580 A, CN 103120740 A, CN 1154861A),
Granule (A of publication number CN 104138441, the Academic Journal of Kunming Medical College, 2009,30 (5)：6-9) and powder
Mist agent (C of Authorization Notice No. CN 100362994).
At present, the first-selected method of administration of asthma medications is respiratory tract inhalation, dense with medicine in air flue
Degree is high, consumption is few, whole body without or the advantages of few adverse reaction.Suitable for inhalation formulation have aerosol,
Spray and powder spray；Powder spray, also known as Foradil Aerolizer formoterol fumarate, is asthma inhalation formulation the most frequently used at present.
Compared with aerosol and spray, powder spray has advantages below：1. patient actively sucks medicinal powder, does not exist
The difficulty of coordinated is administered, compliance is good；2., without propellant, can avoid to the pollution of atmospheric environment and right
The stimulation of respiratory tract；3. drug dose is accurate, is administered without overdose dangerous；4. without preservative and alcohol etc.
Solvent, it is nonirritant to lesion mucous membrane；5. can carry with, it is easy to use.
Chinese patent " preparation for the treatment of allergic rhinitis and asthma " (C of Authorization Notice No. CN 100362994)
In disclose a kind of micro-capsule Foradil Aerolizer formoterol fumarate containing isoforskolin.Disclosed isoforskolin elder generation in the patent
It is made micro-capsule of insoluble polymer ethyl cellulose, then is mixed with the filler such as the lactose or mannitol of fine
Close filling capsule and Foradil Aerolizer formoterol fumarate is obtained, per ml of formulation 0.005mg-0.4mg containing isoforskolin.Practice is aobvious
Show, isoforskolin micro-capsule Foradil Aerolizer formoterol fumarate disclosed in the patent is deposited at the aspect such as production technology and drug safety
In problem, e.g., in production technology, the mobility that micro-capsule mixes gained powder with fine filler is very poor,
Cannot be smoothly filling during production；More importantly in terms of drug safety, the patent uses insoluble auxiliary material ethyl
Cellulose prepares micro-capsule, and is further made Foradil Aerolizer formoterol fumarate, and can by this particulate matter suction lung
Patient health can seriously be damaged.As can be seen here, the isoforskolin micro-capsule Foradil Aerolizer formoterol fumarate cannot industrialized production,
Do not possess the possibility of clinical practice application simultaneously.
Because of the present circumstance, present inventor is directed to the medication demand of bronchial astehma inhalation, with reference to China
The level of production of existing powder spray, while the physicochemical property feature according to isoforskolin itself, intends providing a kind of
For the capsule type inhalation aerosol powder containing isoforskolin of prevention and control of bronchial asthma, wherein using clinical acceptable
Powder spray auxiliary material, can simultaneously meet industrial-scale production and the clinical application requirements such as safely and effectively.
The content of the invention
The present invention is intended to provide a kind of capsule type inhalation aerosol powder containing isoforskolin and preparation method thereof.
The present invention is achieved by the following technical solutions：
A kind of capsule type inhalation aerosol powder containing isoforskolin, it is characterised in that the capsule-type powder spray is by glue
Softgel shell and capsule 's content are constituted；
Above-mentioned capsule 's content is made up of active component isoforskolin and auxiliary material, wherein, isoforskolin account for for
0.4-10% (mass percent), preferably 1-4%；Auxiliary material accounts for 90-99.6%, based on each capsule, wherein
The quality of isoforskolin is 0.1-2.5mg, preferably 0.25-1mg.
In the present invention, isoforskolin is added in the form of compound monomer or Flos Colei esquirolii extract；Wherein, with
When Flos Colei esquirolii extract form is added, the content of isoforskolin should be greater than 50% in extract；The extract system of using
During standby powder spray, should according to the dosage of isoforskolin in the content of isoforskolin in extract and powder spray,
Calculate the addition of extract.
In the present invention, to reduce the density of isoforskolin solid micro-powder, medicine when improving powder spray inhalation
In the dispersion effect of respiratory tract, a small amount of amino acid can be added when isoforskolin micro mist is prepared.Described ammonia
Base acid is selected from leucine, isoleucine and lysine, preferably leucine.The consumption of amino acid accounts for isoforskolin
The 0-30% of quality, preferably 10-20%.If based on capsule 's content total amount, amino acid consumption accounts for content total amount
0-3%, preferably 0.04-2%.
In addition to amino acid, above-mentioned auxiliary material is also comprising the one kind in carrier, antitack agent, lubricant, antistatic additive
Or it is several.
Above-mentioned carrier is selected from the one kind in lactose or mannitol, and the preferably special screening of inhalation powder spray crystallizes a water
Lactose.The average particle size range of carrier is selected from 50-250 μm, preferably 80-150 μm.The consumption of carrier is accounted for entirely
The 80%-99.6% of capsule 's content amount, preferably 82.4%-98.6%.
A small amount of small particle lactose can be added in the present invention, in above-mentioned carrier as antitack agent, to reduce different Buddhist department
Adhesiveness between Kelin micro mist and carrier granular, dispersion of the medicine in respiratory tract when improving powder spray inhalation
Effect.Described small particle lactose is crystallization lactose monohydrate, and average particle size range is selected from 1-20 μm, preferably
5-10μm.The consumption of small particle lactose accounts for the 0%-10% of whole capsule 's content amount, preferably 1%-5%.
A small amount of lubricant can be added in above-mentioned auxiliary material, to improve the lubricity of powder.Described lubricant is hard
Fatty acid magnesium, consumption accounts for the 0-1% of whole capsule 's content amount, preferably 0-0.5%.
A small amount of antistatic additive can be added in above-mentioned auxiliary material, to reduce powder institute static electrification lotus property.Described is anti-quiet
Electric agent is PLURONICS F87, and consumption accounts for the 0-0.5% of whole capsule 's content amount, preferably 0%-0.1%.
Capsule type inhalation aerosol powder containing isoforskolin of the invention is obtained using following preparation technology：
1. isoforskolin micromill process
In capsule type inhalation aerosol powder containing isoforskolin, isoforskolin need to through necessary micronizing so that
Its average grain diameter is less than 5 μm.Two kinds of process routes can be used, one kind is disintegrating process；Another kind is spraying
Drying process；
1.1 disintegrating process：The isoforskolin or Flos Colei esquirolii extract of recipe quantity are taken, is entered with appropriate disintegrating apparatus
Row is crushed, and described disintegrating apparatus includes：Airslide disintegrating mill, ball mill and Universalpulverizer；
1.2 drying process with atomizing：Take the isoforskolin or Flos Colei esquirolii extract of recipe quantity, plus appropriate 50% ethanol
(volume ratio) dissolves, and is spray-dried；In the powder spray of amino acid and/or antistatic additive is added, can
Amino acid and/or antistatic additive are dissolved in 50% ethanol solution containing isoforskolin, spraying are carried out together dry
It is dry；
Above two micromill process preferably spray drying technique；
2. the mixing of material and packing
Weigh recipe quantity isoforskolin micro mist and auxiliary material, by equivalent progressively increase method be well mixed, be sub-packed in No. 3 glue
In capsule.
In the present invention, if contain small particle lactose in prescription, first small particle lactose and carrier fully should be mixed,
Add the mixing of isoforskolin micro mist.
If contain magnesium stearate in prescription in the present invention, should first by isoforskolin micro mist and in addition to magnesium stearate
Other auxiliary materials be well mixed, add magnesium stearate mixing.
In order to make it easy to understand, the following specific embodiment that will pass through is to the glue containing isoforskolin of the present invention
Bladder type inhalation powder spray and its preparation technology are described in detail.It is important to note that instantiation is only
It is to illustrate, it is clear that one of ordinary skill in the art can be according to illustrating, within the scope of the invention herein
Various amendments and change are made to the present invention, these amendments and change are also included in the scope of the present invention.
Specific embodiment
Isoforskolin is added in the form of compound monomer in following examples.Different Buddhist in all embodiments
SCH can directly be substituted for Flos Colei esquirolii extract.When being added with Flos Colei esquirolii extract, different Buddhist in extract
The content of SCH should be greater than 50%.When preparing powder spray with extract, should be according to isoforskolin in extract
Content and powder spray in isoforskolin dosage, calculate extract addition.While carrier in prescription
Consumption should be reduced suitably, to ensure the constant of capsule loading amount.
Carrier auxiliary material in following embodiment is with the special lactose of inhalation powder spray of German Mei Jile companiesAs a example by 120.120 can use the special breast of inhalation powder spray of other models of the said firm
Sugar, such as70、230 are substituted；There can also be similar specification with other companies
Lactose with particle diameter distribution is substituted；Can also be substituted with the mannitol with similar particle diameter distribution.
When using amino acid in following embodiment by taking leucine as an example；Wherein, leucine can directly with different
Leucine and lysine are substituted.
Embodiment 1：
Capsule 's content prescription (100)
Constituent mass quality %
Isoforskolin 10mg 0.4%
The special lactose of inhalation powder spray (120) 2490mg 99.6%
Preparation method：
1) isoforskolin, plus 50% ethanol (volume ratio) dissolving are taken, being configured to isoforskolin concentration is
5% solution, filtration, spray drying.Adjustable spraying drying device spout aperture, and spray velocity,
The instrument parameters such as nozzle temperature, internal pressure, make the average grain of final gained isoforskolin micro mist
Footpath is less than 5 μm；
2) isoforskolin micro mist is taken, is added120, fully mixed by equivalent method of progressively increasing；
3) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.1mg.
Note：Isoforskolin micro mist in embodiment 1 can also be obtained using the disintegrating process under above-mentioned 1.1.
Embodiment 2：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin micro mist is prepared by the scheme of embodiment 1.
2) take small particle lactose (400) and carrier lactose (120), passed by equivalent
Addition is fully mixed.
3) take 1) obtained in isoforskolin micro mist, add 2) obtained in lactose mixed powder, progressively increase method by equivalent
Fully mix.
4) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.1mg.
Embodiment 3：
Capsule 's content prescription (100)
Preparation method：
With embodiment 2.Every capsule 's content loading amount is 25mg, 1mg containing isoforskolin after packing.
Embodiment 4：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin and leucine, plus 50% ethanol (volume ratio) dissolving are taken, being configured to different Buddhist department can
The solution that woods concentration is 5% (w/v), leucine concentration is 1% (w/v), filtration, spraying is dry
It is dry.Adjustable spraying drying device spout aperture, and spray velocity, nozzle temperature, internal pressure etc.
Instrument parameter, makes the average grain diameter of final gained isoforskolin/leucine micro mist be less than 5 μm.
2) isoforskolin/leucine micro mist is taken, is added120, fully mixed by equivalent method of progressively increasing.
3) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.1mg.
Embodiment 5：
Capsule 's content prescription (100)
Preparation method：
With embodiment 4.Every capsule 's content loading amount is 25mg, 0.5mg containing isoforskolin after packing.
Embodiment 6：
Capsule 's content prescription (100)
Preparation method：
With embodiment 4.Every capsule 's content loading amount is 25mg, 1mg containing isoforskolin after packing.
Embodiment 7：
Capsule 's content prescription (100)
Preparation method：
Isoforskolin and leucine, plus 50% ethanol (volume ratio) dissolving are taken, isoforskolin is configured to dense
Spend for 5% (w/v), leucine concentration are the solution of 0.5% (w/v), filtration, spray drying.Remainder step
Suddenly with embodiment 4.Every capsule 's content loading amount is 25mg, 2mg containing isoforskolin after packing.
Embodiment 8：
Capsule 's content prescription (100)
Preparation method：
Isoforskolin and leucine, plus 50% ethanol (volume ratio) dissolving are taken, isoforskolin is configured to dense
Spend for 5% (w/v), leucine concentration are the solution of 1.5% (w/v), filtration, spray drying.Remainder step
Suddenly with embodiment 4.Every capsule 's content loading amount is 25mg, 0.5mg containing isoforskolin after packing.
Embodiment 9：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin and leucine, plus 50% ethanol (volume ratio) dissolving are taken, being configured to different Buddhist department can
Woods concentration is that 5% (w/v) and leucine concentration are the solution of 1% (w/v), and filtration, spraying is dry
It is dry.Adjustable spraying drying device spout aperture, and spray velocity, nozzle temperature, internal pressure etc.
Instrument parameter, makes the average grain diameter of final gained isoforskolin/leucine micro mist be less than 5 μm.
2) take small particle lactose (400) and carrier lactose (120), passed by equivalent
Addition is fully mixed.
3) take 1) obtained in isoforskolin/leucine micro mist, add 2) obtained in lactose mixed powder, by equivalent
Method of progressively increasing fully is mixed.
4) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.5mg.
Embodiment 10：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin, leucine and PLURONICS F87, plus 50% ethanol (volume ratio) dissolving are taken, is matched somebody with somebody
Isoforskolin concentration is made for 5% (w/v), leucine concentration are 1% (w/v) and pool Lip river is husky
The solution of nurse 1880.12% (w/v), filtration, spray drying.Adjustable spraying drying device spout
Aperture, and the instrument parameter such as spray velocity, nozzle temperature, internal pressure, make the final different Buddhist of gained
The average grain diameter of SCH/leucine/PLURONICS F87 micro mist is less than 5 μm.
2) isoforskolin/leucine/PLURONICS F87 micro mist is taken, is added120, progressively increase by equivalent
Method is fully mixed.
3) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.5mg.
Embodiment 11：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin, leucine and PLURONICS F87, plus 50% ethanol (volume ratio) dissolving are taken, is matched somebody with somebody
Isoforskolin concentration is made for 5% (w/v), leucine concentration are 1% (w/v) and pool Lip river is husky
The solution of nurse 1880.12% (w/v), filtration, spray drying.Adjustable spraying drying device spout
Aperture, and the instrument parameter such as spray velocity, nozzle temperature, internal pressure, make the final different Buddhist of gained
The average grain diameter of SCH/leucine/PLURONICS F87 micro mist is less than 5 μm.
2) take small particle lactose (400) and carrier lactose (120), passed by equivalent
Addition is fully mixed.
3) take 1) obtained in isoforskolin/leucine/PLURONICS F87 micro mist, add 2) obtained in lactose mix
Powder is closed, is fully mixed by equivalent method of progressively increasing.
4) above-mentioned mixed powder is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different Buddhist department
Kelin 0.5mg.
Embodiment 12：
Capsule 's content prescription (100)
Preparation method：
1) isoforskolin/leucine/PLURONICS F87 micro mist is prepared by the scheme of embodiment 11.
2) take small particle lactose (400) and carrier lactose (120), passed by equivalent
Addition is fully mixed.
3) take 1) obtained in isoforskolin/leucine/PLURONICS F87 micro mist, add 2) obtained in lactose mix
Powder is closed, is fully mixed by equivalent method of progressively increasing.
4) magnesium stearate is added in mixed powder obtained in 3), be well mixed.
5) mixed powder obtained in 4) is sub-packed in No. 3 capsules.Every capsule 's content loading amount is 25mg, containing different
Forskolin 0.5mg.
Embodiment 13：The aerodynamic size distribution tests of medicine in powder spray
The aerodynamic size of drug powder can directly affect medicine in respiratory tract and the deposition of lung, be influence
The key factor of inhalation powder spray curative effect.The present invention uses medicinal ram (Next generation of new generation
Pharmaceutical impactor, NGI) determine above-described embodiment in isoforskolin aerodynamic size it is big
Small and distribution.
Maneuver：Assembling NGI devices, open vavuum pump, open controller switches, and flowmeter is connected into simulation
Throat, opens flowmeter switch, and air velocity is adjusted into 60L/min.One is put into suction apparatus to treat
Capsule is surveyed, suction apparatus is rotated, capsule is opened, by the rubber adaptation at suction apparatus insertion NGI simulations throat
Device, pressing suction button is measured, and suction apparatus is removed after 10 seconds, is put into capsule shells taking-up with tweezers suitable
Measure dissolving, constant volume in the volumetric flask of size.This operation is repeated, 10 capsules are determined altogether.Respectively with appropriate distillation
Water cleans suction apparatus and adapter, simulation throat, preseparator and 8 catch trays, and washing lotion is collected respectively
Constant volume, isoforskolin in the isoforskolin quality and each parts of NGI of remnants in capsule is determined with HPLC methods
Quality.Inhalable fine fraction (Fine particle are calculated with the quality sum of medicine in the 2nd to the 7th catch tray
Fraction, FPF), FPF=(in 2-7 disks collect isoforskolin total amount)/(different Buddhist in 10 capsules
The total amount of SCH) × 100%.
The measurement result of above-described embodiment 1-12 is as shown in table 1.In addition to embodiment 1, different Buddhist in remaining each embodiment
Left drug amount meets Chinese Pharmacopoeia annex to powder spray quality in the particle diameter distribution result and capsule of SCH
Regulation, i.e., remaining dose≤10% in capsule, and FPF >=10%.
The aerodynamic size measure of spread result of table 1
Claims (11)
1. a kind of capsule type inhalation aerosol powder containing isoforskolin, it is characterised in that the capsule-type sucks dust cloud
Agent is made up of capsule shells and capsule 's content, and wherein capsule 's content includes the component of following mass percent：
2. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Isoforskolin added in the form of compound monomer or Flos Colei esquirolii extract；Wherein, carried with coleus forskohlin
When taking the addition of thing form, the content of isoforskolin should be greater than 50% in extract.
3. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Carrier lactose be the special screening crystallization lactose monohydrate of inhalation powder spray, its average particle size range is
50-250μm。
4. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Carrier lactose be the special screening crystallization lactose monohydrate of inhalation powder spray, its average particle size range is
80-150μm。
5. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Small particle lactose for crystallization lactose monohydrate, average particle size range be 1-20 μm.
6. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Small particle lactose for crystallization lactose monohydrate, average particle size range be 5-10 μm.
7. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that described
Amino acid be the one kind in leucine, isoleucine and lysine, preferably leucine.The use of amino acid
It is 0.04-2% to measure.
8. the capsule type inhalation aerosol powder containing isoforskolin described in claim 1, it is characterised in that described
Amino acid is leucine, and its consumption is 0.04-2%.
9. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that by every
One capsule meter, the wherein quality of isoforskolin are 0.1-2.5mg, preferably 0.25-1mg.
10. the capsule type inhalation aerosol powder containing isoforskolin as described in claim 1, it is characterised in that press
Each capsule meter, the wherein quality of isoforskolin are 0.25-1mg.
A kind of 11. preparation methods of the capsule type inhalation aerosol powder containing isoforskolin as claimed in claim 1,
Characterized in that, it includes step：
A) isoforskolin, amino acid and PLURONICS F87, plus volume ratio are taken for 50% ethanol dissolves, filtration,
Spray drying.Adjustable spraying drying device spout aperture, and spray velocity, nozzle temperature and inside
Pressure parameter, makes the average grain diameter of final gained micro mist be less than 5 μm；
B) small particle lactose and carrier lactose, are fully mixed by equivalent method of progressively increasing；
C) take a) obtained in micro mist, add b) obtained in lactose mixed powder, fully mixed by equivalent method of progressively increasing,
Add magnesium stearate mixing；
D) above-mentioned mixed powder is sub-packed in No. 3 capsules.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510800281.3A CN106692116A (en) | 2015-11-15 | 2015-11-15 | Capsule-type inhalation aerosol powder containing isoforskolin |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510800281.3A CN106692116A (en) | 2015-11-15 | 2015-11-15 | Capsule-type inhalation aerosol powder containing isoforskolin |
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| Publication Number | Publication Date |
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| CN106692116A true CN106692116A (en) | 2017-05-24 |
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| CN201510800281.3A Pending CN106692116A (en) | 2015-11-15 | 2015-11-15 | Capsule-type inhalation aerosol powder containing isoforskolin |
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| CN110302157A (en) * | 2018-03-27 | 2019-10-08 | 天津金耀集团有限公司 | A kind of Ipratropium Bromide aerosol combination and preparation method thereof |
| CN112336703A (en) * | 2020-12-04 | 2021-02-09 | 深圳善康医疗健康产业有限公司 | Isoniazid dry powder inhalant for treating pulmonary tuberculosis |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110302157A (en) * | 2018-03-27 | 2019-10-08 | 天津金耀集团有限公司 | A kind of Ipratropium Bromide aerosol combination and preparation method thereof |
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| CN112336703A (en) * | 2020-12-04 | 2021-02-09 | 深圳善康医疗健康产业有限公司 | Isoniazid dry powder inhalant for treating pulmonary tuberculosis |
| CN112336703B (en) * | 2020-12-04 | 2022-03-11 | 深圳善康医疗健康产业有限公司 | Isoniazid dry powder inhalant for treating pulmonary tuberculosis |
| WO2022116792A1 (en) * | 2020-12-04 | 2022-06-09 | 深圳善康医疗健康产业有限公司 | Isoniazid dry powder inhalant for treating pulmonary tuberculosis |
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