CN109106696A - Lun Panai mouthfuls of molten films of pyrrole and preparation method thereof - Google Patents
Lun Panai mouthfuls of molten films of pyrrole and preparation method thereof Download PDFInfo
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- CN109106696A CN109106696A CN201811114936.1A CN201811114936A CN109106696A CN 109106696 A CN109106696 A CN 109106696A CN 201811114936 A CN201811114936 A CN 201811114936A CN 109106696 A CN109106696 A CN 109106696A
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- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
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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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
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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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7007—Drug-containing films, membranes or sheets
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Abstract
The invention discloses a kind of pyrrole Lun Panai mouthfuls of molten films and preparation method thereof, belong to field of pharmaceutical preparations, are able to solve existing pyrrole Lun Panai pharmaceutical dosage form and take inconvenient problem.The pyrrole Lun Panai mouthfuls of molten films include pyrrole Lun Panai particle, film forming agent and disintegrating agent of the partial size (D90) less than 35 μm.The pyrrole Lun Panai mouthfuls of molten films can be used for treating epilepsy.
Description
Technical field
The present invention relates to field of pharmaceutical preparations more particularly to a kind of pyrrole Lun Panai mouthfuls of molten films and preparation method thereof.
Background technique
Epilepsy is the chronic neurodegenerative disease of a kind of recurrent exerbation, protracted course, clinical manifestation is movement, feel,
The symptom of consciousness and vegetative nerve functional disturbance.Epilepsy is one of nervous system common disease, and illness rate is only second to cerebral apoplexy, can
Betide all age group.
Pyrrole Lun Panai is a kind of noncompetitive AMPA receptor antagonist, it is by inhibiting postsynaptic AMPA receptors glutamic acid living
Property, it reduces neuron and is overexcited, to treat epileptic.Pyrrole Lun Panai is soluble in N-Methyl pyrrolidone, be dissolved in acetonitrile and
Acetone is slightly soluble in methanol, ethyl alcohol and ethyl acetate, atomic to be dissolved in octanol and ether, does not dissolve in heptane and water.Pyrrole Lun Panai is current
Can there are thin membrane coated tablet dosage form and oral suspension dosage form with dosage form.Film coating tablet needs are taken by water, and for
For epileptic, tablet and not convenient is swallowed with water.Oral outstanding mixed liquor type is inconvenient to carry, also leads to the compliance of patient
It reduces.
Summary of the invention
The embodiment of the present invention provides a kind of pyrrole Lun Panai mouthfuls of molten films and preparation method thereof, provides a kind of pyrrole Lun Panai's
Novel form improves the convenience of medication.
The present invention provides a kind of pyrrole Lun Panai mouthfuls of molten films, the molten film of mouth includes partial size (D90) at 1-35 μm
Pyrrole Lun Panai particle, film forming agent and disintegrating agent.
Preferably, the molten film of the mouth further includes surfactant pluronic.
Preferably, the partial size (D90) of the pyrrole Lun Panai is at 10-20 μm.
Optionally, the film forming agent includes polyvinyl alcohol.
Optionally, the disintegrating agent includes sodium alginate.
Optionally, the molten film of the mouth further includes plasticizer polyethylene glycol.
Optionally, the molten film of the mouth further includes corrigent.
The present invention also provides a kind of preparation methods of above-mentioned pyrrole Lun Panai mouthfuls of molten films, which comprises
Pyrrole Lun Panai is subjected to micronization processes, obtains pyrrole Lun Panai particle of the partial size (D90) at 1-35 μm；
Pyrrole Lun Panai particle after micronization processes is dissolved in second alcohol and water with surfactant, film forming agent, disintegrating agent
In the mixed solvent, be uniformly mixing to obtain film forming matrix；
The film forming matrix is deaerated, is film-made, is dried to obtain the pyrrole Lun Panai mouthfuls of molten films.
Preferably, described that pyrrole Lun Panai is subjected to micronization processes, partial size (D90) is obtained in pyrrole Lun Panai of 1-35 μm
Son includes:
Pyrrole Lun Panai is subjected to micronization processes, obtains pyrrole Lun Panai particle of the partial size (D90) at 10-20 μm.
Preferably, the weight ratio of the in the mixed solvent, water and ethyl alcohol is 1:2-5.
Pyrrole Lun Panai mouthfuls of molten films provided by the invention and preparation method thereof, using the pyrrole Lun Panai particle of micron level,
Pyrrole Lun Panai is made to the molten film of mouth quickly dissolved in the oral cavity by the dissolubility for improving pyrrole Lun Panai, convenient anhydrous
Under the conditions of take, provide patient medication compliance and convenience.
Specific embodiment
It in order to make the object, technical scheme and advantages of the embodiment of the invention clearer, below will be in the embodiment of the present invention
Technical solution be clearly and completely described, it is clear that described embodiments are some of the embodiments of the present invention, rather than
Whole embodiments.Based on the embodiments of the present invention, those of ordinary skill in the art are not making creative work premise
Under every other embodiment obtained, shall fall within the protection scope of the present invention.
One embodiment of the invention provides a kind of pyrrole Lun Panai mouthfuls of molten films, this mouthful of molten film includes that partial size (D90) is less than
35 μm of pyrrole Lun Panai particle, film forming agent and disintegrating agent.
The pharmaceutical dosage form for the film-like that the molten film of mouth can at least partly dissolve in oral cavity.
The reagent of furtherance film supplemented by film forming agent, i.e., by the evaporation of solvent or carrier to the mixture containing film forming agent or
Solidification to the mixture for being mixed with film forming agent, can form continuous film.Coalescing agents are such as selected from polyvinyl alcohol, hydroxypropyl methyl
One of cellulose, sodium cellulose glycolate, hydroxypropyl cellulose, xanthan gum, pectin, polyoxyethylene and cornstarch are several
Kind.
Main ingredient pyrrole Lun Panai in the embodiment of the present invention is not soluble in water, and solubility in water is only 0.032g/L (25
℃).Lower solubility also results in lower bioavilability simultaneously.In order to solve this problem, the embodiment of the present invention is adopted
With the pyrrole Lun Panai particle of micron level, can be dispersed in the molten film of mouth.The ratio of pyrrole Lun Panai drug granule
Surface area influences whether its dissolved efficiency, and micro mist is thinner, and specific surface area is bigger, and the area contacted with external environment is bigger, drug
It is easy for dissolving, and then also improves bioavilability.The partial size (D90) of pyrrole Lun Panai particle in the embodiment of the present invention is less than
35μm.Partial size (D90) is the equivalent diameter of the largest particles when cumulative distribution is 90% in distribution curve.Such as partial size (D90)
It is 20 μm, i.e. particle of the partial size less than 20 μm accounts for all particles 90%.Micron level can be obtained by kinds of processes means
Drug particle.Such as pyrrole Lun Panai bulk pharmaceutical chemicals can be carried out with micronization processes to obtain the drug particle of micron level.
Disintegrating agent is that the molten film of mouth can be made to accelerate to split the substance for being broken into thin in the oral cavity.Disintegrating agent for example selected from
Sodium carboxymethyl starch, low-substituted hydroxypropyl methylcellulose, crosslinked polyvinylpyrrolidone, croscarmellose sodium, alginic acid
One or more of sodium, crospovidone and microcrystalline cellulose.Disintegrating agent is added in the embodiment of the present invention to help drug
The acceleration of pyrrole Lun Panai is dissolved and is absorbed.
Pyrrole Lun Panai mouthfuls of molten films provided in an embodiment of the present invention improve pyrrole using the pyrrole Lun Panai particle of micron level
Pyrrole Lun Panai is made to the molten film of mouth quickly dissolved in the oral cavity, conveniently in anhydrous conditions by the dissolubility of Lun Panai
It takes, provides the compliance and convenience of patient's medication.
In another embodiment of the present invention, the molten film of mouth further includes surfactant, and surfactant can be further
Increase the solvability of drug in a solvent.Surfactant is for example selected from fatty acid glyceride, sucrose fatty ester, lecithin
One of rouge, polysorbate, sucrose fatty ester, ten polyglyceryl laurates, lauryl sodium sulfate and pluronic
Or it is several.
In one embodiment of the invention, surfactant is pluronic.Pluronic is a kind of novel high score
Sub- nonionic surfactant, is polyoxyethylene poly-oxygen propylene aether block copolymer, and general formula is HO (C2H4O)a(C3H6O)b
(C2H4O)cH, it is 15-67 that wherein a and c, which is 2-130, b, and middle section is hydrophobic chain, and both ends are divided into hydrophilic chain.Pu Langni
Gram there is solubilizing effect for main ingredient, promotes main ingredient dissolution in a solvent.In addition, having compared to lauryl sodium sulfate etc.
For soap is similar to the surfactant of taste, pluronic odorless, tasteless is highly suitable to be applied for the molten film of mouth.In addition, general
Lang Nike without immunogene, dissolve in body fluid, drug can be promoted by blood-brain barrier, and then improve the biological utilisation of pyrrole Lun Panai
Degree.Specifically, in some embodiments of the invention, selecting pluronic F127, molecular formula is as above, wherein 101 a, c, and b is
56.In other embodiment of the invention, Pluronic F68 is selected, molecular formula is as above, a, c 79, b 28.Both classes
The pluronic of type is preferable to the compatibilization effect of main ingredient pyrrole Lun Panai.
For main ingredient pyrrole Lun Panai, although partial size is lower, specific surface area is bigger, is more conducive to dissolution and the medicine of drug
The bioavilability of object, but the problem of consider process costs simultaneously, the granularity of micro mist is also unsuitable too low, with pyrrole Lun Panai particle
Can be dispersed in film forming matrix is advisable.Therefore, in certain embodiments, the partial size (D90) of pyrrole Lun Panai particle is not small
In 1 μm, i.e., between 1-35 μm.Specifically, the partial size (D90) of pyrrole Lun Panai particle can be 1 μm, 5 μm, 10 μm, 15 μm, 20
μm,25μm,30μm,35μm.It is further preferred that in certain embodiments, the partial size of pyrrole Lun Panai particle 10-20 μm it
Between.Pyrrole Lun Panai particle in the range can take into account the cost of excellent in a solvent dispersibility and micromill process.
In some embodiments of the invention, the preferred polyvinyl alcohol of film forming agent.Optionally, as the polyvinyl alcohol of film forming agent
Molecular weight be 20-400KDa, degree of hydrolysis 85-90%.Specifically, in certain embodiments of the present invention, can use and divide
Son amount is 31KDa, the polyvinyl alcohol that degree of hydrolysis is 68.7-88.8% namely polyvinyl alcohol that trade name is Mowiol4-88
Product.In certain embodiments of the present invention, the polyvinyl alcohol that the degree of polymerization is 88 for 1700, alcoholysis degree can also be used.At this
It, can also be using the mixture of polyvinyl alcohol Mowiol4-88 and polyvinyl alcohol 1788 as film forming in some embodiments of invention
Agent, the weight ratio of the two for example 2:1-1:2 are formed by medicine film uniform ground using the polyethylene product of such film forming agent.
In another embodiment of the invention, disintegrating agent is sodium alginate.Sodium alginate is as disintegrating agent in application, being formed
The molten membrane surface of mouth it is smooth, without granular sensation.
In another embodiment of the present invention, in order to increase the plasticity of finished product film, the molten film of mouth further includes plasticizer.Increase
Mould agent for example selected from one of polyethylene glycol (PEG), glycerol, glyceryl triacetate, propylene glycol Chinese holly edge acid esters and Tween 80 or
It is several.Preferably, plasticizer is selected from polyethylene glycol (PEG).It is further preferred that the mixture that two kinds of polyethylene glycol can be selected is made
For plasticizer application.Such as select molecular weight 3000-6000Da PEG and molecular weight the PEG of 250-1000Da mixing
Object, more specifically, the mixture of PEG4000 and PEG400.Preferably, plasticizer is the mixture of PEG4000 and PEG400, and
The weight ratio of PEG4000 and PEG400 is 1-3:1, preferred 2:1.When the mixture of PEG4000 and PEG400 is as plasticizer,
The toughness of film is higher, the not cracky in storing process.
In order to which that improves the molten film of mouth takes mouthfeel, in certain embodiments, the molten film of mouth further includes corrigent.Corrigent
It may include sweetener and/or aromatic.Sweetening agents are such as selected from saccharin, Sucralose, neotame, A Litian, honey element, An Sai
One or more of honey, Aspartame and ammonium glycyrrhizinate.Aromatic is for example selected from petit grain oil, strawberry essence, vanilla flavour concentrate, Portugal
One or more of grape shaddock oil, Mint Essence, cinnamyl acetate, citral, citronella oil, Levomenthol and menthol.It is preferred that
Sucralose and Mint Essence are collectively as corrigent.
In addition, in certain embodiments, the molten film of mouth can also including colorant etc. other auxiliary agents.Colorant for example selected from
Water colo(u)r etc..
In some embodiments of the invention, each component accounts for the weight percentage of the molten film of finished product mouth are as follows: 5-20wt%
The film forming agent of main ingredient pyrrole Lun Panai, 20-60wt%, the plasticizer of 1-20wt%, the disintegrating agent of 10-25%, 1-15wt%
The corrigent of surfactant and 1-10wt%.
More preferably, in some embodiments of the invention, each component accounts for the weight percentage of the molten film of finished product mouth
Are as follows: the disintegration of the film forming agent, the plasticizer, 15-20% of 5-15wt% of main ingredient pyrrole Lun Panai, 40-50wt% of 10-15wt%
Agent, the surfactant of 6-10wt% and 3-6wt% corrigent.
Finally, it will be appreciated that usually also containing the acceptable balance solvent for not influencing medicine film storage, example in film
Such as water or the mixed solvent of water and ethyl alcohol.Accounting of the balance solvent in the molten film of mouth is 0.5-7wt%, specifically, for example
Accounting 0.5wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt% etc..Preferably, 1-3wt%.By solvent
Content controls within this range, and the flexibility of the molten film of gained mouth is preferable.Solvent content is excessive, and film is not easily molded；Solvent content
Too low, film is easy drying and splits, not easy to maintain.
With the molten film of above-mentioned mouth correspondingly, the embodiment of the invention also provides the preparation methods of this mouthful of molten film.This method
Include the following steps.
Step 1: pyrrole Lun Panai being subjected to micronization processes, obtains pyrrole Lun Panai particle of the partial size (D90) less than 35 μm.
In this step, the partial size of pyrrole Lun Panai bulk pharmaceutical chemicals is reduced using micronization processes, such as makes its partial size (D90) be
1 μm, 5 μm, 10 μm, 15 μm, 20 μm, 25 μm, 30 μm or 35 μm etc..
Preferably, step 1 includes: that pyrrole Lun Panai is carried out micronization processes, obtains pyrrole of the partial size (D90) at 10-20 μm
Lun Panai particle.
Step 2: the pyrrole Lun Panai particle after micronization processes is dissolved in second with surfactant, film forming agent, disintegrating agent
The in the mixed solvent of alcohol and water, is uniformly mixing to obtain film forming matrix.
The selection such as description in the molten film embodiment of above-mentioned mouth of surfactant, film forming agent, disintegrating agent, it is no longer superfluous herein
It states.In addition, corresponding with the molten film embodiment of above-mentioned mouth, step 2 can also include that plasticizer, corrigent, colorant etc. is added
The step of auxiliary agent.
In this step, the weight ratio of the in the mixed solvent, water and ethyl alcohol is preferably 1:2-5, it is further preferred that weight
Than being preferably 1:3.The mixed solvent of the ratio is preferable to the solute effect of drug.
The selection of each component and content are for example, see the molten film embodiment of above-mentioned mouth in the molten film of mouth, and details are not described herein again.
Step 3: the film forming matrix being deaerated, is film-made, is dried to obtain the pyrrole Lun Panai mouthfuls of molten films.
The preparation method of pyrrole Lun Panai mouthfuls of molten films provided in an embodiment of the present invention, is first micronized pyrrole Lun Panai
Processing improves the dissolubility of pyrrole Lun Panai, and pyrrole Lun Panai is made to the molten film of mouth quickly dissolved in the oral cavity, is conveniently existed
It is taken under anhydrous condition, provides the compliance and convenience of patient's medication.
In one embodiment of the invention, in order to promote to dissolve, optionally, step 2 further include it is following step by step.
Step 21: by after micronization processes pyrrole Lun Panai particle and surfactant be dissolved in second alcohol and water mixing it is molten
Homogeneous solution is obtained in agent.
Step 22: film forming agent, disintegrating agent being added in the homogeneous solution and stirring makes it be uniformly dispersed, is formed a film
Matrix.
Corresponding with the molten film embodiment of above-mentioned mouth, step 22 can also include that plasticizer, corrigent, colorant etc. is added
The step of auxiliary agent.
The embodiment provided in order to better illustrate the present invention is said below by the mode for enumerating specific embodiment
It is bright.
Embodiment 1
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 15 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 0.67g Pluronic F68 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol and water
Weight ratio be 3:1.Take 6.67g hydroxypropyl methyl cellulose, 2.4g crosslinked polyethylene pyrrole network alkanone, 0.8g glycerol and 0.53g
Sucralose is dissolved in above-mentioned homogeneous solution and is uniformly mixing to obtain film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 45 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 13.33mg, content of dispersion 2mg.
Embodiment 2
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 20 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 1g pluronic F127 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol and water
Weight ratio is 2:1.Take 7.83g polyvinyl alcohol 1788,3.83g crosslinked polyethylene pyrrole network alkanone, 0.83g propylene glycol Chinese holly edge acid esters and
0.83g Aspartame is dissolved in above-mentioned homogeneous solution and is uniformly mixing to obtain film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 50 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 16.67mg, content of dispersion 2mg.
Embodiment 3
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 25 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 2g pluronic F127 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol and water
Weight ratio is 3:1.Take 10g polyvinyl alcohol Mowiol4-88,3g crosslinked polyethylene pyrrole network alkanone, 2g propylene glycol Chinese holly edge acid esters and
0.6g Aspartame is dissolved in above-mentioned homogeneous solution and is uniformly mixing to obtain film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 40 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 20mg, content of dispersion 2mg.
Embodiment 4
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 13 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 1.23g Pluronic F68 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol and water
Weight ratio be 4:1.Take 6.92g polyvinyl alcohol Mowiol4-88,2.92g sodium alginate, 0.77g Macrogol 4000,0.77g
Polyethylene glycol 400 and 0.31g Aspartame are dissolved in above-mentioned homogeneous solution and are uniformly mixing to obtain film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 42 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 15.38mg, content of dispersion 2mg.
Embodiment 5
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 12 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 1.09g Pluronic F68 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol and water
Weight ratio be 2:1.Take 3.64g polyvinyl alcohol 1788,4.55g polyvinyl alcohol Mowiol4-88,2.91g sodium alginate, 1.82g
Macrogol 4000,0.91g glycerol, 0.64g Aspartame and 0.09g Mint Essence are dissolved in above-mentioned homogeneous solution and stir
Uniformly obtain film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 42 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 18.18mg, content of dispersion 2mg.
Embodiment 6
Pyrrole Lun Panai bulk pharmaceutical chemicals are micronized, the pyrrole Lun Panai particle that partial size (D90) is 10 μm is obtained.Take 2g pyrrole Lun Panai
Particle and 1.17g pluronic F127 are dissolved in 40mg ethyl alcohol and the in the mixed solvent of water obtains homogeneous solution, wherein ethyl alcohol with
The weight ratio of water is 2:1.Take 5g polyvinyl alcohol 1788,3.33g polyvinyl alcohol Mowiol4-88,2.67g sodium alginate, the poly- second of 1g
Glycol 4000,0.33g polyethylene glycol 400,0.5g Sucralose and 0.17g Mint Essence are dissolved in above-mentioned homogeneous solution and stir
It mixes and uniformly obtains film forming matrix.
Film forming matrix is deaerated and is coated on stainless steel plate, dry at 42 DEG C, cutting obtains 1000 pyrrole Lun Panai
The molten film of mouth.Every film weight is 16.67mg, content of dispersion 2mg.
Performance test
1, basic performance is tested
The basic performance of each embodiment oral instant membrane is tested, it is as follows to obtain parameter area.
| Project | As a result |
| Film thickness | 35μm±1μm |
| Appearance | Membranous type is smooth, and bubble-free, surface is without particle |
2, dissolution time is tested
6 molten films of mouth are randomly selected to above-mentioned each embodiment and measure its dissolution time, and calculate average dissolution time.
Specifically, the molten film of mouth is dissolved under the conditions of 37 DEG C of water bath with thermostatic control, measure the time all dissolved, and be recorded in following table.
3, Mechanics Performance Testing
Mechanical property is carried out using oral instant membrane of LabthinkXLW (EC) Intelligent electronic tensil testing machine to each embodiment
It can test, obtain 250~400kg/cm of elasticity modulus2, 400~200kg/cm of tensile strength2, 200~50kg/cm of tear edge prolongs
Stretch rate 150~220%.
The above performance test explanation, the molten film of mouth provided in an embodiment of the present invention meet using standard.
Finally, it should be noted that the above embodiments are only used to illustrate the technical solution of the present invention., rather than its limitations；To the greatest extent
Pipe present invention has been described in detail with reference to the aforementioned embodiments, those skilled in the art should understand that: its according to
So be possible to modify the technical solutions described in the foregoing embodiments, or to some or all of the technical features into
Row equivalent replacement；And these are modified or replaceed, various embodiments of the present invention technology that it does not separate the essence of the corresponding technical solution
The range of scheme.
Claims (10)
1. a kind of pyrrole Lun Panai mouthfuls of molten films, which is characterized in that the molten film of mouth includes pyrrole logical sequence pa of the partial size D90 less than 35 μm
How particle, film forming agent and disintegrating agent.
2. pyrrole Lun Panai mouthfuls of molten films according to claim 1, which is characterized in that the molten film of mouth further includes that surface is living
Property agent pluronic.
3. pyrrole Lun Panai mouthfuls of molten films according to claim 1 or 2, which is characterized in that the partial size of the pyrrole Lun Panai
(D90) at 10-20 μm.
4. pyrrole Lun Panai mouthfuls of molten films according to claim 1 or 2, which is characterized in that the film forming agent includes polyethylene
Alcohol.
5. pyrrole Lun Panai mouthfuls of molten films according to claim 1 or 2, which is characterized in that the disintegrating agent includes alginic acid
Sodium.
6. pyrrole Lun Panai mouthfuls of molten films according to claim 1 or 2, which is characterized in that the molten film of mouth further includes increasing
Mould agent polyethylene glycol.
7. pyrrole Lun Panai mouthfuls of molten films according to claim 1 or 2, which is characterized in that the molten film of mouth further includes rectifying
Taste agent.
8. a kind of preparation method of pyrrole Lun Panai mouthfuls of molten films as described in claim 1, which is characterized in that the method packet
It includes:
Pyrrole Lun Panai is subjected to micronization processes, obtains pyrrole Lun Panai particle of the partial size (D90) less than 35 μm；
Pyrrole Lun Panai particle after micronization processes is dissolved in the mixed of second alcohol and water with surfactant, film forming agent, disintegrating agent
In bonding solvent, it is uniformly mixing to obtain film forming matrix；
The film forming matrix is deaerated, is film-made, is dried to obtain the pyrrole Lun Panai mouthfuls of molten films.
9. the preparation method of pyrrole Lun Panai mouthfuls of molten films according to claim 8, which is characterized in that described by pyrrole Lun Panai
Micronization processes are carried out, obtaining pyrrole Lun Panai particle of the partial size (D90) less than 35 μm includes:
Pyrrole Lun Panai is subjected to micronization processes, obtains pyrrole Lun Panai particle of the partial size (D90) at 10-20 μm.
10. the preparation method of pyrrole Lun Panai mouthfuls of molten films according to claim 8, which is characterized in that the mixed solvent
In, the weight ratio of water and ethyl alcohol is 1:2-5.
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| CN114557982A (en) * | 2022-04-07 | 2022-05-31 | 沈阳药科大学 | Perampanel electrospun fiber oral instant film agent and preparation method thereof |
| CN116617193A (en) * | 2023-07-10 | 2023-08-22 | 北京丰科睿泰医药科技有限公司 | Pirenpananel oral film-dissolving agent |
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