CN108785289A - Molten film of naratriptan hydrochloride mouth and preparation method thereof - Google Patents
Molten film of naratriptan hydrochloride mouth and preparation method thereof Download PDFInfo
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- 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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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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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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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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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
- A61K9/70—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
An embodiment of the present invention provides a kind of molten films of naratriptan hydrochloride mouth and preparation method thereof, belong to field of pharmaceutical preparations, can solve the problems, such as that existing naratriptan hydrochloride pharmaceutical dosage form takes inconvenience.The molten film of naratriptan hydrochloride mouth includes：The corrigent of the naratriptan hydrochloride of 5-25wt%, the water-soluble film forming agent of 20-70wt%, the plasticizer of 1-15wt%, the disintegrant of 10-30wt% and 1-10wt%.The molten film of naratriptan hydrochloride mouth can be used for treating the acute attack of migraine.
Description
Technical field
The present invention relates to field of pharmaceutical preparations more particularly to a kind of molten film of naratriptan hydrochloride mouth and preparation method thereof.
Background technology
It is a kind of drug for treating migraine that, which draws triptan,.Migraine is a kind of common chronic forms vascular
Disease.Naratriptan belongs to selective serotonin 1D/1B receptor stimulating agents, also has slight activation to make 5-HT1A and 5-HT1F
With.Because it inhibits with skull cerebrovascular contraction, the inhibition of peripheral neurons and trigeminal neuralgia-neck complex two level neuronal conduction
Effect, to can inhibit activation nocuity trigeminal neuralgia be passed to effect, play the role of control migraine.That draws bent
Pu Tan has the characteristics that oral administration biaavailability is high, it is good to eliminate long half time, drug tolerance.
Naratriptan hydrochloride is the pharmaceutically acceptable salt of naratriptan, has now been developed a variety of dosage forms, such as tablet
With capsule etc., but these dosage forms all have inconvenience on taking.Such as tablet and taking for capsule need water, and
For the people of old man, neck injury and with very inconvenient for the patient for gulping down medicine obstacle.
Invention content
The embodiment of the present invention provides a kind of molten film of naratriptan hydrochloride mouth and preparation method thereof, provide a kind of hydrochloric acid that
The novel form of naratriptan improves the convenience of medication.
The embodiment of the present invention provides a kind of molten film of naratriptan hydrochloride mouth, and the molten film of mouth includes the salt of 5-25wt%
The disintegrant and 1- of sour naratriptan, the water-soluble film forming agent of 20-70wt%, the plasticizer of 1-15wt%, 10-30wt%
The corrigent of 10wt%.
Optionally, the molten film of the mouth includes the water-soluble, film-forming of the naratriptan hydrochloride of 10-20wt%, 40-60wt%
Agent, 5-8wt% plasticizer 15-25wt% disintegrant and 3-6wt% corrigent.
Optionally, the water-soluble film forming agent be selected from polyvinyl alcohol, hydroxypropyl methyl cellulose, sodium cellulose glycolate,
One or more of hydroxypropyl cellulose, xanthans, pectin, polyoxyethylene, cornstarch.
Preferably, the water-soluble film forming agent is the mixture of polyvinyl alcohol Mowiol4-88 and polyvinyl alcohol 1788.
Optionally, the plasticizer is selected from polyethylene glycol, glycerine, glyceryl triacetate, propylene glycol Chinese holly edge acid esters or tween
One or more of 80.
Preferably, the plasticizer is to account for the PEG4000 of the molten film 2-4wt% of mouth and account for the molten film 1-2wt% of mouth
The polyethylene glycol mixture of PEG400.
Optionally, the disintegrant includes sodium carboxymethyl starch, low-substituted hydroxypropyl methylcellulose, crosslinked polyethylene pyrrolidines
One or more of ketone, croscarmellose sodium, sodium alginate, crospovidone and microcrystalline cellulose.
Optionally, the disintegrant is selected from sodium alginate.
Optionally, the corrigent includes the aromatic of the sweetener and 0.1-2wt% that account for the molten film 4-6wt% of mouth.
The embodiment of the present invention provides a kind of preparation method of the above-mentioned molten film of naratriptan hydrochloride mouth, the preparation method packet
It includes：
It is under stirring that water-soluble film forming agent is soluble in water in 60-80 DEG C at a temperature of, obtain polymer gel；
Disintegrant, plasticizer, corrigent is added into polymer gel under stirring, and stirs evenly；
Naratriptan hydrochloride is added under stirring, and stirs evenly, obtains containing drug solns；
It is de-gassed, is film-made to containing drug solns, and the heat drying at 40-50 DEG C, cut, obtain naratriptan hydrochloride mouth
Molten film.
Molten film of naratriptan hydrochloride mouth provided in an embodiment of the present invention and preparation method thereof selects naratriptan hydrochloride to make
For main ingredient, the dissolubility of main ingredient is improved, solubilizer can further increase the dissolving of main ingredient, and disintegrant enables main ingredient in mouth
It is discharged rapidly in chamber, corrigent can improve the mouthfeel taken medicine when main ingredient discharges in oral cavity.These component phase interworkings
It closes, the molten film film forming of mouth of formation is good, without using water delivery service.Preparation process is not related to organic solvent, to environment and human body
It is friendly.
Specific implementation mode
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
Lower obtained every other embodiment, shall fall within the protection scope of the present invention.
Herein, unless otherwise specified, then wt% refers to weight accounting of each ingredient in the molten film of finished product mouth.
An embodiment of the present invention provides a kind of molten films of naratriptan hydrochloride mouth.
The molten film of mouth is to refer to be put in the film type dissolved in oral cavity.The main ingredient of the molten film of mouth provided in this embodiment is
Naratriptan hydrochloride.Naratriptan hydrochloride is a kind of white to linen powder, is dissolved in water.Compared to naratriptan, hydrochloric acid
The water solubility of naratriptan is more preferable, it is easier to be uniformly dispersed in film forming agent.Accounting of the naratriptan hydrochloride in the molten film of mouth
Can be 5-25wt%, it is preferred that accounting can be 10-20wt%.Such as accounting be 5wt%, 10wt%, 15wt%,
20wt%, 25wt% etc..The molten film film-formation result of the mouth obtained by naratriptan hydrochloride within the scope of 10-20wt% is preferable, greatly
When 25wt%, the molten film of gained mouth has been easy granular sensation.
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.Water-soluble film forming agent can be dissolved in the film forming of water
Agent, to dissolve in the oral cavity.Water-soluble film forming agent for example selected from polyvinyl alcohol (PVA), hydroxypropyl methyl cellulose (HPMC),
In sodium cellulose glycolate (CMC-Na), hydroxypropyl cellulose (HPC), xanthans, pectin, polyoxyethylene (PEO), cornstarch
One or more.Preferably, water-soluble film forming agent is polyvinyl alcohol (PVA).
Accounting of the water-soluble film forming agent in the molten film of mouth can be 20-70wt%, it is preferred that accounting can be 40-
60wt%.Specifically, such as accounting 20wt%, 25wt%, 30wt%, 35wt%, 40wt%, 45wt%, 50wt%,
55wt%, 60wt%, 65wt%, 70wt% etc..For water-soluble film forming agent in 20-70wt% ranges, film forming and stripping result are good
Good, when being less than 20wt%, film is not easily molded, and when being more than 70wt%, film is not easy to be taken off on membrane carrier from holding.
Plasticizer is used for increasing the plasticity of film.Plasticizer is for example selected from polyethylene glycol (PEG), glycerine, triacetic acid glycerine
One or more of ester, propylene glycol Chinese holly edge acid esters or Tween 80.Preferably, plasticizer be selected from polyethylene glycol (PEG), glycerine,
Tween 80.
Accounting of the plasticizer in the molten film of mouth can be 1-15wt%, it is preferred that accounting can be 5-8wt%.Such as
1wt%, 2wt%, 5wt%, 6wt%, 10wt%, 13wt%, 15wt% etc..
Disintegrant can make the molten film of mouth accelerate to split the substance for being broken into fine particle in the oral cavity.The disintegrant for example selects
From sodium carboxymethyl starch, low-substituted hydroxypropyl methylcellulose, crosslinked polyvinylpyrrolidone, croscarmellose sodium, seaweed
One or more of sour sodium, crospovidone and microcrystalline cellulose.
Accounting of the disintegrant in the molten film of mouth can be 10-30wt%, it is preferred that accounting can be 15-25wt%.Tool
Body, such as accounting 10wt%, 15wt%, 20wt%, 25wt%, 30wt% etc..
Corrigent includes sweetener and/or aromatic etc., and addition corrigent, which can improve, takes mouthfeel.Sweetening agents are as selected
From one or more of saccharin, Sucralose, neotame, A Litian, honey element, acesulfame potassium, Aspartame and ammonium glycyrrhizinate.
Sweetener is preferably Sucralose.Aromatic for example selected from petit grain oil, strawberry essence, vanilla flavour concentrate, oil of grapefruit, Mint Essence,
One or more of cinnamyl acetate, citral, citronella oil, Levomenthol and menthol.Aromatic is preferably Mint Essence.
Accounting of the corrigent in the molten film of mouth can be 1-10wt%, can be preferably 3-6wt%.Specifically, example
Such as accounting 1wt%, 3wt%, 5wt%, 6wt%, 7wt%, 10wt%.
It is preferred that the aromatic of the sweetener of accounting 4-6wt% and accounting 0.1-2wt% are collectively as strong in the molten film of mouth
Taste agent.
Can also include colorant in the molten film of mouth to make film that certain appearance be presented.Colorant is for example selected from water
Dissolubility pigment etc..Accounting of the colorant in the molten film of mouth is 0-2wt%, further alternative, 0.001-0.5wt%.
Finally, it will be appreciated that usually also containing the acceptable excess water for not influencing medicine film storage, surplus in film
Accounting of the water in the molten film of mouth is 0.5-7wt%.Moisture is excessive, and film is not easily molded；The too low film of moisture is easy drying
It splits, it is not easy to maintain.Specifically, such as accounting 0.5wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, 6wt%,
7wt% etc..It is further preferred that water content is preferably between 0.5-5wt%.It is furthermore preferred that water content preferably between
Between 1-3wt%.The toughness of the molten film of mouth within the scope of this is preferable.
The molten film of naratriptan hydrochloride mouth provided in an embodiment of the present invention is selected naratriptan hydrochloride as main ingredient, is improved
The dissolubility of main ingredient, solubilizer can further increase the dissolving of main ingredient, and disintegrant enables main ingredient to release rapidly in the oral cavity
It puts, corrigent can improve the mouthfeel taken medicine when main ingredient discharges in oral cavity.These components cooperate, the mouth of formation
Molten film film forming is good, without using water delivery service.Preparation process is not related to organic solvent, friendly to environment and human body.
In another embodiment of the invention, it is 20-400KDa as the molecular weight of the polyvinyl alcohol of water-soluble film forming agent,
Degree of hydrolysis is 85-90%.Specifically, in certain embodiments of the present invention, it may be used that molecular weight is 31KDa, degree of hydrolysis is
The polyvinyl alcohol namely trade name of 68.7-88.8% is the polyvinyl alcohol product of Mowiol4-88.In certain realities of the present invention
It applies in example, the polyvinyl alcohol that the degree of polymerization is 88 for 1700, alcoholysis degree can also be used.In certain embodiments of the present invention, also
Polyvinyl alcohol Mowiol4-88 may be used with the mixture of polyvinyl alcohol 1788 as film forming agent, the ratio of the two is, for example, 2:1-
1:2, medicine film uniform ground is formed by using the polyethylene product of such film forming agent.
In another embodiment of the present invention, the mixture of two kinds of polyethylene glycol can be selected as plasticizer application.Such as
Select molecular weight 3000-6000Da PEG and molecular weight the PEG of 250-1000Da mixture, more specifically,
The mixture of PEG4000 and PEG400.Preferably, plasticizer is to account for the PEG4000 of the molten film 2-4wt% of mouth and account for the molten film of mouth
The mixture of the PEG400 of 1-2wt%, such as account for the PEG4000 of the molten film 3wt% of mouth and account for the molten film 1.5wt%PEG400 of mouth
Mixture.When the mixture of PEG4000 and PEG400 is as plasticizer, the toughness of film is higher.
In another embodiment of the invention, the preferred sodium alginate of disintegrant.Sodium alginate is as disintegrant in application, shape
At the molten membrane surface of mouth it is smooth, without particulate matter.
Corresponding with the molten film of naratriptan hydrochloride mouth provided in an embodiment of the present invention, the embodiment of the present invention additionally provides salt
The preparation method of the sour molten film of naratriptan mouth.This method comprises the following steps.
Step 1：It is under stirring that water-soluble film forming agent is soluble in water in 60-80 DEG C at a temperature of, obtain polymer
Gel.
Preferably, water-soluble film forming agent is dissolved in water at a temperature of 70-75 DEG C.
Step 2：Disintegrant, plasticizer, corrigent is added into polymer gel under stirring, and stirs evenly.
It is understood that the order of addition of disintegrant, plasticizer, corrigent can be according to the specific feelings of the material of selection
Condition is configured.It is preferred that being added according to the sequence for being firstly added disintegrant and then the last corrigent of plasticizer.Disintegrant content is logical
Often it is higher than plasticizer and corrigent, disintegrant is first added and is more advantageous to the uniform of solution.
Step 3：Naratriptan hydrochloride is added under stirring, and stirs evenly, obtains containing drug solns.
It is eventually adding main ingredient ingredient naratriptan hydrochloride so that drug can be evenly distributed in containing in drug solns.
Step 4：It is de-gassed, is film-made to containing drug solns, and the heat drying at 40-50 DEG C, cut, obtaining hydrochloric acid, that draws
The bent smooth molten film of mouth.
Preferably, the heat drying at 40-45 DEG C.Preferably, it is filmed on stainless steel.
The preparation method of the molten film of naratriptan hydrochloride mouth provided in an embodiment of the present invention, preparation process is not related to organic molten
Agent, it is friendly to environment and human body.It selects naratriptan hydrochloride as main ingredient, improves the dissolubility of main ingredient, solubilizer can be into
One step increases the dissolving of main ingredient, and disintegrant enables main ingredient to discharge rapidly in the oral cavity, and corrigent can be in main ingredient in oral cavity
When release, the mouthfeel taken medicine is improved.These components cooperate, and the molten film film forming of mouth of formation is good, without being sent with water
Clothes.
In order to more preferably illustrate molten film of naratriptan hydrochloride mouth provided in an embodiment of the present invention and preparation method thereof, tie below
Specific embodiment is closed to be described.
Embodiment 1
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
| Ingredient | Content |
| Naratriptan hydrochloride | 2.78g |
| Polyvinyl alcohol Mowiol4-88 | 10.19g |
| Polyethylene glycol 400 | 1.11g |
| Sodium alginate | 3.34g |
| Sucralose | 0.74g |
| Purified water | 30mL |
Under stirring, polyvinyl alcohol Mowiol4-88 is dissolved in the purified water of the 30mL under 75 DEG C of water bath conditions
In, obtain polymer gel.Polyethylene glycol 400, sodium alginate, Sucralose are added into gel to stir evenly.In stirring shape
Naratriptan hydrochloride is added under state, stirs evenly, obtains containing drug solns.It is coated on stainless steel plate after drug containing solution left standstill is deaerated
On, and it is dry at 45 DEG C.Finally cut into 1000 medicine films.Weighed, the average weight of every medicine film is 18.53mg.
Embodiment 2
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
Under stirring, in the purified water for the 30mL that polyvinyl alcohol 1788 is dissolved under 70 DEG C of water bath conditions, obtain
Polymer gel.Blend, the Abbas's sweet tea of glycerine, croscarmellose sodium and sodium carboxymethyl starch are added into gel
It stirs evenly.Naratriptan hydrochloride is added under stirring, stirs evenly, obtains containing drug solns.Drug containing solution left standstill is taken off
It is coated on stainless steel plate after gas, and dry at 45 DEG C.Finally cut into 1000 medicine films.It is weighed, every medicine film it is flat
Equal weight is 15.44mg.
Embodiment 3
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
| Ingredient | Content |
| Naratriptan hydrochloride | 2.78g |
| Hydroxypropyl methyl cellulose | 15.29g |
| Macrogol 4000 | 0.83g |
| Polyethylene glycol 400 | 0.56g |
| Sodium carboxymethyl starch | 6.39g |
| Mint Essence | 0.56g |
| Purified water | 30mL |
Under stirring, in the purified water for the 30mL that hydroxypropyl methyl cellulose is dissolved under 65 DEG C of water bath conditions,
Obtain polymer gel.Macrogol 4000, polyethylene glycol 400, sodium carboxymethyl starch and Mint Essence are added into gel to stir
It mixes uniformly.Naratriptan hydrochloride is added under stirring, stirs evenly, obtains containing drug solns.Drug containing solution left standstill is deaerated
After be coated on stainless steel plate, and it is dry at 50 DEG C.Finally cut into 1000 medicine films.Weighed, every medicine film is averaged
Weight is 27.80mg.
Embodiment 4
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
| Ingredient | Content |
| Naratriptan hydrochloride | 2.78g |
| Polyvinyl alcohol Mowiol4-88 | 6.62g |
| Macrogol 4000 | 0.40g |
| Polyethylene glycol 400 | 0.20g |
| Sodium alginate | 2.78g |
| Sucralose | 0.13g |
| Purified water | 30mL |
Under stirring, polyvinyl alcohol Mowiol4-88 is dissolved in the purified water of the 30mL under 65 DEG C of water bath conditions
In, obtain polymer gel.Macrogol 4000, polyethylene glycol 400, sodium alginate, Sucralose stirring are added into gel
Uniformly.Naratriptan hydrochloride is added under stirring, stirs evenly, obtains containing drug solns.After drug solns vacuum outgas will be contained
It is coated on stainless steel plate, and dry at 50 DEG C.Finally cut into 1000 medicine films.It is weighed, the average weight of every medicine film
Amount is 13.24mg.
Embodiment 5
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
Under stirring, polyvinyl alcohol Mowiol4-88 is dissolved in the purified water of the 30mL under 60 DEG C of water bath conditions
In, obtain polymer gel.Polyethylene glycol 400, sodium alginate, Sucralose are added into gel to stir evenly.In stirring shape
Naratriptan hydrochloride is added under state, stirs evenly, obtains containing drug solns.It is coated on stainless steel plate after drug containing solution left standstill is deaerated
On, and it is dry at 40 DEG C.Finally cut into 1000 medicine films.Weighed, the average weight of every medicine film is 13.90mg.
Embodiment 6
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
| Ingredient | Content |
| Naratriptan hydrochloride | 2.78g |
| Polyvinyl alcohol 1788 | 3.71g |
| Polyvinyl alcohol Mowiol4-88 | 4.63g |
| Macrogol 4000 | 0.56g |
| Glycerine | 0.56g |
| Sodium alginate | 4.63g |
| Sucralose | 0.83g |
| Mint Essence | 0.28g |
| Purified water | 30mL |
Under stirring, polyvinyl alcohol 1788 and polyvinyl alcohol Mowiol4-88 are dissolved under 65 DEG C of water bath conditions
In the purified water of 30mL, polymer gel is obtained.Macrogol 4000, glycerine, sodium alginate, Sucralose are added into gel
It is stirred evenly with Mint Essence.Naratriptan hydrochloride is added under stirring, stirs evenly, obtains containing drug solns.By drug containing
It is coated on stainless steel plate after solution left standstill degassing, and dry at 50 DEG C.Finally cut into 1000 medicine films.It is weighed, often
The average weight of piece medicine film is 18.53mg.
Embodiment 7
Formula as below is the amount of 1000 molten films of naratriptan hydrochloride mouth, the made molten film of naratriptan hydrochloride mouth
Naratriptan hydrochloride content specification be 2.78mg, the content specification of corresponding naratriptan is 2.5mg.
| Ingredient | Content |
| Naratriptan hydrochloride | 2.78g |
| Polyvinyl alcohol 1788 | 4.63g |
| Polyvinyl alcohol Mowiol4-88 | 3.09g |
| Macrogol 4000 | 0.46g |
| Polyethylene glycol 400 | 0.39g |
| Sodium alginate | 2.78g |
| Sucralose | 0.69g |
| Mint Essence | 0.15g |
| Purified water | 30mL |
Under stirring, polyvinyl alcohol 1788 and polyvinyl alcohol Mowiol4-88 are dissolved under 60 DEG C of water bath conditions
In the purified water of 30mL, polymer gel is obtained.Into gel be added Macrogol 4000, polyethylene glycol 400, sodium alginate,
Sucralose and Mint Essence stir evenly.Naratriptan hydrochloride is added under stirring, stirs evenly, it is molten to obtain drug containing
Liquid.It is coated on stainless steel plate after drug containing solution left standstill is deaerated, and dry at 43 DEG C.Finally cut into 1000 medicine films.
Weighed, the average weight of every medicine film is 15.44mg.
Performance test
1, basic performance is tested
The basic performance of each molten film of embodiment mouth is tested, it is as follows to obtain parameter area.
| Project | As a result |
| Film thickness | 30μm±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.
| Test event | Average dissolution time |
| Embodiment 1 | 26 seconds |
| Embodiment 2 | 30 seconds |
| Embodiment 3 | 26 seconds |
| Embodiment 4 | 17 seconds |
| Embodiment 5 | 28 seconds |
| Embodiment 6 | 29 seconds |
| Embodiment 7 | 27 seconds |
3, Mechanics Performance Testing
Mechanical property is carried out to the molten film of the mouth of each embodiment using LabthinkXLW (EC) Intelligent electronic tensil testing machines
Test, obtains 250~400kg/cm of elasticity modulus2, 400~200kg/cm of tensile strength2, 200~50kg/cm of tear edge, extension
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
Present invention has been described in detail with reference to the aforementioned embodiments for pipe, it will be understood by those of ordinary skill in the art that：Its according to
So can with technical scheme described in the above embodiments is modified, either to which part or all technical features into
Row equivalent replacement；And these modifications or replacements, 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 molten film of naratriptan hydrochloride mouth, which is characterized in that the molten film of mouth includes that drawing of the hydrochloric acid of 5-25wt%
The water-soluble film forming agent of Qu Tan, 20-70wt%, the plasticizer of 1-15wt%, the disintegrant of 10-30wt% and 1-10wt% are rectified
Taste agent.
2. the molten film of mouth according to claim 1, which is characterized in that the molten film of mouth includes the hydrochloric acid of 10-20wt%
Naratriptan, the water-soluble film forming agent of 40-60wt%, 5-8wt% plasticizer 15-25wt% disintegrant and 3-6wt%
Corrigent.
3. the molten film of mouth according to claim 1 or 2, which is characterized in that the water-soluble film forming agent be selected from polyvinyl alcohol,
In hydroxypropyl methyl cellulose, sodium cellulose glycolate, hydroxypropyl cellulose, xanthans, pectin, polyoxyethylene, cornstarch
One or more.
4. the molten film of mouth according to claim 3, which is characterized in that the water-soluble film forming agent is polyvinyl alcohol
The mixture of Mowiol4-88 and polyvinyl alcohol 1788.
5. the molten film of mouth according to claim 1 or 2, which is characterized in that the plasticizer be selected from polyethylene glycol, glycerine,
One or more of glyceryl triacetate, propylene glycol Chinese holly edge acid esters or Tween 80.
6. the molten film of mouth according to claim 5, which is characterized in that the plasticizer is to account for the molten film 2-4wt% of mouth
The polyethylene glycol mixture of PEG4000 and the PEG400 for accounting for the molten film 1-2wt% of mouth.
7. the molten film of mouth according to claim 1 or 2, which is characterized in that the disintegrant includes sodium carboxymethyl starch, low
Replace hydroxypropyl methylcellulose, crosslinked polyvinylpyrrolidone, croscarmellose sodium, sodium alginate, crospovidone and
One or more of microcrystalline cellulose.
8. the molten film of mouth according to claim 1 or 2, which is characterized in that the disintegrant is selected from sodium alginate.
9. the molten film of mouth according to claim 1 or 2, which is characterized in that the corrigent includes accounting for the molten film 4- of mouth
The sweetener of 6wt% and the aromatic of 0.1-2wt%.
10. a kind of preparation method of such as molten film of claim 1-9 any one of them naratriptan hydrochloride mouths, feature exist
In the preparation method includes：
It is under stirring that water-soluble film forming agent is soluble in water in 60-80 DEG C at a temperature of, obtain polymer gel；
Disintegrant, plasticizer, corrigent is added into polymer gel under stirring, and stirs evenly；
Naratriptan hydrochloride is added under stirring, and stirs evenly, obtains containing drug solns；
It is de-gassed, is film-made to containing drug solns, and the heat drying at 40-50 DEG C, cut, obtain the molten film of naratriptan hydrochloride mouth
Agent.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201811036784.8A CN108785289A (en) | 2018-09-06 | 2018-09-06 | Molten film of naratriptan hydrochloride mouth and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201811036784.8A CN108785289A (en) | 2018-09-06 | 2018-09-06 | Molten film of naratriptan hydrochloride mouth and preparation method thereof |
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| CN108785289A true CN108785289A (en) | 2018-11-13 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| CN201811036784.8A Pending CN108785289A (en) | 2018-09-06 | 2018-09-06 | Molten film of naratriptan hydrochloride mouth and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109966271A (en) * | 2019-04-22 | 2019-07-05 | 上海昊海生物科技股份有限公司 | A kind of moxifloxacin hydrochloride film and preparation method thereof |
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| CN109966271A (en) * | 2019-04-22 | 2019-07-05 | 上海昊海生物科技股份有限公司 | A kind of moxifloxacin hydrochloride film and preparation method thereof |
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Application publication date: 20181113 |