CN112618518A - Lurasidone hydrochloride oral instant membrane preparation and preparation method thereof - Google Patents
Lurasidone hydrochloride oral instant membrane preparation and preparation method thereof Download PDFInfo
- Publication number
- CN112618518A CN112618518A CN202110062769.6A CN202110062769A CN112618518A CN 112618518 A CN112618518 A CN 112618518A CN 202110062769 A CN202110062769 A CN 202110062769A CN 112618518 A CN112618518 A CN 112618518A
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- CN
- China
- Prior art keywords
- lurasidone hydrochloride
- oral instant
- preparation
- lurasidone
- film
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- Pending
Links
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Images
Classifications
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- A—HUMAN NECESSITIES
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
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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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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Psychiatry (AREA)
- Inorganic Chemistry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Hospice & Palliative Care (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides a lurasidone hydrochloride oral instant membrane preparation and a preparation method thereof. Each dosage unit of the oral instant membrane comprises the following components in percentage by mass: 20.0-60.0 w/w% of active drug lurasidone hydrochloride, 20.0-60.0 w/w% of water-soluble film forming material, 3.0-30.0 w/w% of plasticizer, 0.05-0.5 w/w% of surfactant and proper amount of stabilizer, flavoring agent and opacifier. The preparation method comprises the steps of sequentially adding the plasticizer, the flavoring agent, the opacifier, the surfactant and the lurasidone hydrochloride into a prepared film forming material aqueous solution in advance, uniformly stirring, ultrasonically defoaming, adding into a continuous coating machine for continuous film coating, drying and cutting to obtain the oral instant film preparation. The oral instant film preparation can be quickly dissolved on the oral cavity and tongue, can be taken without water, solves the problems of poor medicine taking compliance of patients and medicament storing and spitting phenomena in the current lurasidone hydrochloride clinical use process, and can improve the effectiveness of the medicaments and the compliance of the patients.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to an oral instant membrane preparation containing lurasidone hydrochloride and a preparation method thereof. The prepared lurasidone hydrochloride oral instant film preparation can be quickly dissolved on the oral tongue and can be taken without water, the problems of poor medicine taking compliance of patients and medicament storage and spitting phenomena in the current lurasidone hydrochloride clinical use process are solved, the effectiveness of the medicaments and the compliance of the patients can be improved, and the lurasidone hydrochloride oral instant film preparation is particularly suitable for children with dysmnesia and behavioral dysfunction and old patients.
Background
The active ingredient of the invention is lurasidone hydrochloride (lurasidone hydrochloride), which is a novel atypical antipsychotic drug developed by Wutian pharmacy and Sumitomo pharmacy in combination for treating schizophrenia. The structure is as follows:
lurasidone hydrochloride is approved to be marketed in European Union earlier than 3-22 months in 2014, and then approved by FDA and pMDA in 2010 and 2020 respectively to be marketed in USA and Japan, and the trade names are both
24 days in the year of 2019, 1 month,
is approved by NMPA and imported into China under the trade name of
The lurasidone hydrochloride can simultaneously act on 5-HT2a, a receptor and a dopamine D2 receptor, obviously improve positive and negative symptoms of a schizophrenia patient, and relieve catalepsy caused by conditioned fear stress.
The lurasidone hydrochloride is a common tablet at present in clinical dosage form, but the common tablet is difficult to swallow, so that the lurasidone hydrochloride is not suitable for children and old patients to take the dosage form, and cannot be taken conveniently by the patients under the condition of no water.
In the acute stage of schizophrenia patients, the conditions of refusing to take medicines, storing medicines in the oral cavity and spitting medicines often occur, and the problem of medication compliance of the schizophrenia patients generally exists. Therefore, the dosage form of tablet and capsule is often ineffective for patients, and easy-to-use dosage forms should be considered for patients with schizophrenia. In view of the above, there is a need to provide a new preparation with convenient use, good compliance and stable quality to solve the above problems.
The oral instant pellicle is prepared by loading effective components of chemicals or Chinese medicinal extracts with certain dosage into a pellicle material, making into thin film, placing on tongue, and rapidly dissolving and releasing the medicine without drinking water; the medicine can be quickly dissolved on the tongue, so that the patient does not need to worry about choking or inhaling, and does not need to worry about medicine storage or spitting, the medication compliance and the convenience of the patient are greatly improved, the medicine is particularly suitable for children and old patients, and the clinical nursing cost is reduced. The invention adopts solvent casting to prepare the lurasidone hydrochloride into the oral instant film agent, which can improve the medication compliance of patients.
Disclosure of Invention
The invention aims to provide an oral instant film preparation of lurasidone hydrochloride, which has the advantages of good taste, no need of drinking water, quick dissolution in oral cavity, high bioavailability and convenient use, and overcomes the inconvenience of clinical medication of the existing dosage form of lurasidone hydrochloride; the preparation process of the oral instant membrane preparation is simple, convenient and feasible, the cost is low, and the related pharmaceutic adjuvants are easy to purchase, so that the oral instant membrane preparation has good social benefit and economic benefit.
In order to achieve the aim, the invention provides a lurasidone hydrochloride oral instant film preparation which comprises lurasidone hydrochloride, a high-water-solubility film forming material, a plasticizer, a surfactant, a stabilizer, a flavoring agent and an opacifier, wherein the sum of the ingredients is 100%.
Further, the active drug lurasidone hydrochloride accounts for 20.0-60.0 w/w%, the high-water-solubility film-forming material accounts for 20.0-60.0 w/w%, the plasticizer accounts for 3.0-30.0 w/w%, and the surfactant accounts for 0.05-0.5 w/w%.
Further, the mass percent of the components is 30.0-50.0 w/w% of active drug lurasidone hydrochloride, 40.0-55.0 w/w% of high water-soluble film forming material, 4.0-13.0 w/w% of plasticizer, 0.05-0.2 w/w% of surfactant, 2.0 w/w% of flavoring agent, 0.9 w/w% of stabilizer and 0.05 w/w% of opacifier, and the sum of the components is 100%.
Further, the dosage of the active drug lurasidone hydrochloride in the lurasidone hydrochloride oral instant membrane preparation with a single dosage unit is 20-120 mg, and the average particle size of the lurasidone hydrochloride is smaller than 100 mu m.
Further, the high water-solubility film-forming material comprises at least one of polyvinyl alcohol, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, sodium alginate, CMC-Na, polyoxyethylene, bletilla hyacinthine gum, maltodextrin, corn starch or carrageenan, and is preferably hydroxypropyl methyl cellulose.
Further, the plasticizer comprises at least one of sorbitol, polysorbate, xylitol, maltitol, glycerin, polyethylene glycol, propylene glycol, glycerate, and fatty acid, preferably glycerin.
Further, the surfactant includes at least one of polysorbate, fatty acid glyceride, sorbitan fatty acid, amino acid type, betaine type, quaternary ammonium, stearic acid, sodium lauryl sulfate and poloxamer, preferably poloxamer.
Further, the stabilizer comprises at least one of edetic acid and derivatives or salts thereof, 2, 6-di-tert-butyl-4-methylphenol, tea polyphenol, tocopherol and butyl hydroxy anisole, and preferably disodium edetate; or the correctant is one or more of sucralose, sucrose, saccharin sodium, stevioside, aspartame, menthol, cherry essence, strawberry essence, milk essence, chocolate essence, grape essence, sweet orange essence and mixed pulp essence.
Further, the opacifier is titanium dioxide.
In order to achieve the above object, the present invention further provides a preparation method of the lurasidone hydrochloride oral instant film preparation, which is used for preparing the lurasidone hydrochloride oral instant film preparation according to any one of the above technical schemes, and comprises the following steps:
s1, crushing lurasidone hydrochloride by adopting a grinding, sieving or airflow crushing method, wherein the average particle size is controlled below 100 mu m for later use;
s2, dispersing the high-water-solubility film-forming material in the prescription amount into purified water at the temperature of 70-90 ℃, stirring and dissolving to obtain a colorless transparent solution, and then cooling to room temperature for later use;
s3, adding lurasidone hydrochloride, a plasticizer, a surfactant, a stabilizer, a flavoring agent and an opacifier in a formula amount into the high-water-solubility film-forming material solution, and stirring for 3-8 min; homogenizing with a high speed shearing machine at 5000-; finally obtaining a light yellow milky solution;
and S4, ultrasonically defoaming the light yellow emulsion solution obtained in the step S3, adding the light yellow emulsion solution into a continuous coating machine for continuous coating, drying and cutting to obtain the lurasidone hydrochloride oral instant membrane preparation.
The lurasidone hydrochloride belongs to a BCS II class medicine in the biological pharmacy, namely a low-solubility and high-permeability medicine, and the medicine is slowly dissolved out in the gastrointestinal tract due to low solubility, so that the absorption of the medicine is limited, the dissolution is the rate-limiting process of the absorption, and the oral absorption of the medicine can be effectively improved by accelerating the dissolution of the medicine. The in vitro dissolution of the medicine is an important index for inspecting the quality of the preparation, and the dissolution method and the limit can reflect the quality difference and are key indexes of prescription screening and preparation methods.
The invention has the beneficial effects that:
(1) the oral instant film preparation of lurasidone hydrochloride provided by the invention has disintegration time of less than 30 seconds, is fast to dissolve, is completely dissolved in four dissolution media of water, dilute hydrochloric acid solution (containing 0.2% of lauryl sodium sulfate) with pH value of 1.2, acetate buffer solution with pH value of 4.0 and phosphate buffer solution (containing 0.2% of lauryl sodium sulfate) with pH value of 6.8 within 15 minutes, and has shorter disintegration time and faster dissolution rate compared with the lurasidone hydrochloride ordinary tablets prepared by the prior art; i.e., it is rapidly dissolvable in the oral cavity; and because the medicine can be quickly dissolved on the tongue, the patient does not need to worry about choking or inhaling, and does not need to worry about medicine storage or spitting, so that the medicine taking compliance and the convenience of the patient are greatly improved, the medicine is particularly suitable for children and old patients, and the clinical nursing cost is reduced.
(2) The preparation method of the lurasidone hydrochloride oral instant membrane preparation provided by the invention is convenient to operate, good in reproducibility, strong in controllability and low in cost, and related pharmaceutic adjuvants are easy to purchase, so that the preparation method has good social benefit and economic benefit.
Drawings
FIG. 1 is a commercially available
The dissolution curve of the oral instant film preparation of lurasidone hydrochloride prepared in example 3 in a dilute hydrochloric acid solution (containing 0.2% of sodium dodecyl sulfate) at pH1.2 was measured.
FIG. 2 is a commercial product
The results were determined from the dissolution profile of the lurasidone hydrochloride oral fast dissolving film formulation prepared in example 3 in acetate buffer solution at ph 4.0.
FIG. 3 is a commercially available
The results were determined from the dissolution profile of the lurasidone hydrochloride oral instant film formulation prepared in example 3 in a phosphate buffer solution (containing 0.2% sodium lauryl sulfate) at ph 6.8.
FIG. 4 is a commercial product
The results were measured on the dissolution curve of the lurasidone hydrochloride oral instant film preparation prepared in example 3 in water.
Detailed Description
For better understanding, a plurality of preferred embodiments of the present invention will be described in detail, and the technical solutions of the embodiments of the present invention will be clearly and completely described below. All other embodiments, which can be derived by a person skilled in the art from the embodiments of the present invention without any inventive step, are within the scope of the present invention.
The oral instant film agent of lurasidone hydrochloride has the characteristics of short disintegration time limit and fast dissolution compared with the common preparation medicament, and is convenient to take, and performance evaluation methods all adopt non-standard methods.
The specific method for evaluating the performance is as follows:
mechanical properties: taking 1 finished film agent, clamping two ends of the film agent by a clamp for 0.5cm respectively, enabling a chest expander to stretch at a constant speed in a vertical state until the film agent is broken, recording the peak value reached by the tensile force in the process as the maximum load, measuring the distance between the two clamps when the film agent is broken, and calculating the elongation of the film agent according to the following formula:
Disintegration time limit: wetting filter paper with purified water, spreading the filter paper in a clean culture dish, placing 1 finished film on the surface of the wetted filter paper, and observing and recording the time required for the finished film to be completely disintegrated and melted. The results are shown in Table 1.
Dissolution curve: the samples prepared by the invention and the commercial samples are respectively carried out by adopting the second method (pulp method) of the 2015 version of Chinese pharmacopoeia 0931
The oral cavity instant film preparation of the lurasidone hydrochloride and the lurasidone hydrochloride tablet sold in the market are determined by measuring dissolution curves in dissolution media of water, pH1.2 dilute hydrochloric acid (containing 0.2 percent of lauryl sodium sulfate), pH4.0 acetate buffer solution and pH6.8 phosphate buffer solution (containing 0.2 percent of lauryl sodium sulfate), wherein the volume of the media is 900mL, the temperature of the media is 37 +/-0.5 ℃, the rotating speed is 50rpm, and the sampling time points are 5min, 10min, 15min, 20min, 30min, 45min and 60min
Carrying out comparative study on dissolution curve by using similarity factor f and adopting a model-independent mathematical method2As an index, a self-made sample and a commercially available sample were quantitatively evaluated
Difference in dissolution curves, f2The calculation formula of (2) is as follows:
wherein n is the number of sampling points, RtAnd TtEach commercially available at time t
And the average cumulative dissolution percentage of the self-made lurasidone hydrochloride oral instant membrane preparation. If commercially available
The average cumulative dissolution percentage of the oral instant film preparation of the lurasidone hydrochloride in 15min is more than 85 percent, and the two are similar without calculating f2(ii) a If the average cumulative dissolution percentage of either preparation at 15min is less than 85%, f is calculated according to the above formula2Value of (a), (b), f)2In the range of 0 to 100, f2Greater than 50 they are similar, f2Less than 50 the two are not similar.
The invention provides a preparation method of a lurasidone hydrochloride oral instant membrane preparation, which comprises the following steps:
s1, crushing lurasidone hydrochloride by adopting grinding, sieving or airflow crushing and other methods, and controlling the average particle size to be below 100 mu m for later use;
s2, dispersing the high-water-solubility film-forming material in the prescription amount into purified water at the temperature of 70-90 ℃, stirring and dissolving to obtain a colorless transparent solution, and then cooling to room temperature for later use;
s3, adding the plasticizer, the surfactant, the stabilizer, the flavoring agent and the opacifier in the formula amount into the high-water-solubility film-forming material solution, and stirring for 3-8 min; homogenizing with a high speed shearing machine at 5000-; finally obtaining a light yellow milky solution;
and S4, ultrasonically defoaming the light yellow emulsion solution obtained in the step S3, adding the light yellow emulsion solution into a continuous coating machine for continuous coating, drying and cutting to obtain the lurasidone hydrochloride oral instant membrane preparation.
The preparation steps of the preparation methods of the examples 1 to 6 are basically the same, and the main difference is that the formulas are different, and the preparation methods are as follows:
example 1
Recipe for example 1:
| name (R) | Dosage (mg) | Ratio (%) |
| Lurasidone |
40 | 40 |
| Hydroxypropyl methylcellulose | 53 | 53 |
| Glycerol | 4 | 4 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Formulation of example 2:
| name (R) | Dosage (mg) | Ratio (%) |
| Lurasidone |
40 | 40 |
| Hydroxypropyl methylcellulose | 52 | 52 |
| Glycerol | 5 | 5 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Formulation of example 3:
| name (R) | Dosage (mg) | Ratio (%) |
| Lurasidone |
40 | 40 |
| |
50 | 50 |
| Glycerol | 7 | 7 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Formulation of example 4:
| name (R) | Dosage (mg) | Ratio (%) |
| |
40 | 40 |
| Hydroxypropyl methylcellulose | 48 | 48 |
| Glycerol | 9 | 9 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Formulation of example 5:
| name (R) | Dosage (mg) | Ratio (%) |
| |
40 | 40 |
| Hydroxypropyl methylcellulose | 46 | 46 |
| Glycerol | 11 | 11 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Formulation of example 6:
| name (R) | Dosage (mg) | Ratio (%) |
| |
40 | 40 |
| Hydroxypropyl methylcellulose | 44 | 44 |
| Glycerol | 13 | 13 |
| Sucralose | 2 | 2 |
| Edetate disodium | 0.9 | 0.9 |
| Poloxamers | 0.05 | 0.05 |
| Titanium dioxide | 0.05 | 0.05 |
| Purified water | Proper amount of | / |
Example 7 Performance test experiments
According to the recipes of examples 1 to 6, the preparation method of the invention was used to prepare a lurasidone hydrochloride oral instant film preparation (hereinafter, referred to as "home-made lurasidone hydrochloride oral instant film preparation"), and the appearance and mechanical properties of the lurasidone hydrochloride oral instant film preparation prepared in examples 1 to 6 were measured and compared with those of commercially available oral instant film preparations
The disintegration time of (c). The results are shown in Table 1.
TABLE 1 Lurasidone hydrochloride oral fast dissolving film formulations prepared in examples 1-6 and commercially available
The results of measurement of the main physical and chemical properties of (1).
As is clear from the results in Table 1, the oral instant film preparations of lurasidone hydrochloride prepared in examples 1 to 6 were excellent in appearance, tensile strength and elongation, and the oral instant film preparations of lurasidone hydrochloride prepared in each example were completely disintegrated within 30 seconds, whereas the commercially available oral instant film preparations of lurasidone hydrochloride
Complete disintegration in about 7 min.
EXAMPLE 8 dissolution test
Testing home-made lurasidone hydrochloride oral instant film formulations and commercially available
In four media: dissolution rates in water, dilute hydrochloric acid (containing 0.2% sodium lauryl sulfate) at ph1.2, acetate buffer solution at ph4.0, and phosphate buffer solution (containing 0.2% sodium lauryl sulfate) at ph6.8 were plotted, and the measurement results are shown in fig. 1 to 4.
As can be seen from the graphs 1 to 4, the dissolution rate of the self-made lurasidone hydrochloride oral instant film preparation in the four dissolution media in the first 15min is obviously superior to that of the commercially available lurasidone hydrochloride oral instant film preparation
Self-made lurasidone hydrochloride oral instant membrane preparation and commercially available oral instant membrane preparation
The evaluation results of the similarity factors are shown in Table 2.
Table 2 lurasidone hydrochloride oral fast dissolving film preparation prepared in example 3 and commercially available
The evaluation results of the similarity factor of (2).
As can be seen from the results in Table 2, the in vitro dissolution behavior of the oral fast dissolving film preparation of lurasidone hydrochloride prepared in example 3 was comparable to that of the commercially available oral fast dissolving film preparation
Similarly, the lurasidone hydrochloride oral instant membrane preparation prepared by the invention is shown to improve the clinical medication compliance of patients, reduce the clinical nursing cost and simultaneously keep the same effectiveness as the lurasidone hydrochloride tablet sold in the market.
It should be noted that, as will be understood by those skilled in the art, the highly water-soluble film-forming material in the present invention may be one or more of hydroxypropyl methylcellulose, polyvinyl alcohol, hydroxypropyl cellulose, polyvinyl pyrrolidone, sodium alginate, CMC-Na, polyoxyethylene, bletilla gum, maltodextrin, corn starch or carrageenan, and is not limited to hydroxypropyl methylcellulose.
The plasticizer can be one or more of sorbitol, polysorbate, xylitol, maltitol, glycerol, polyethylene glycol, propylene glycol, glycerate and fatty acid, and is not limited to glycerol.
The surfactant may be at least one or more of polysorbate, fatty acid glyceride, sorbitan fatty acid, amino acid type, betaine type, quaternary ammonium, stearic acid, sodium lauryl sulfate and poloxamer, and is not limited to poloxamer.
The stabilizer can be one or more of edetic acid and derivatives or salts thereof, 2, 6-di-tert-butyl-4-methylphenol, tea polyphenol, tocopherol and butyl hydroxy anisole, and is not limited to disodium edetate; the correctant can be any one or combination of more of sucralose, sucrose, saccharin sodium, stevioside, aspartame, menthol, cherry essence, strawberry essence, milk essence, chocolate essence, grape essence, sweet orange essence and mixed fruit essence, and is not limited to sucralose.
Although the present invention has been described in detail with reference to the preferred embodiments, it will be understood by those skilled in the art that various changes may be made and equivalents may be substituted for elements thereof without departing from the spirit and scope of the present invention.
Claims (10)
1. The lurasidone hydrochloride oral instant membrane preparation is characterized in that: the lurasidone hydrochloride/water-soluble film-forming agent comprises lurasidone hydrochloride, a high-water-solubility film-forming material, a plasticizer, a surfactant, a stabilizer, a flavoring agent and an opacifier, wherein the sum of the components is 100%.
2. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: according to the mass percentage, the active drug lurasidone hydrochloride comprises 20.0-60.0 w/w%, 20.0-60.0 w/w% of high water-solubility film-forming material, 3.0-30.0 w/w% of plasticizer and 0.05-0.5 w/w% of surfactant.
3. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: according to the mass percentage, the active drug lurasidone hydrochloride is 30.0-50.0 w/w%, the high water-solubility film-forming material is 40.0-55.0 w/w%, the plasticizer is 4.0-13.0 w/w%, the surfactant is 0.05-0.2 w/w%, the flavoring agent is 2.0 w/w%, the stabilizer is 0.9 w/w% and the opacifier is 0.05 w/w%, and the sum of the components is 100%.
4. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the dosage of the active drug lurasidone hydrochloride in the lurasidone hydrochloride oral instant membrane preparation with a single dosage unit is 20-120 mg, and the average particle size of the lurasidone hydrochloride is less than 100 mu m.
5. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the high-water-solubility film-forming material comprises at least one of polyvinyl alcohol, hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, sodium alginate, CMC-Na, polyoxyethylene, bletilla hyacinthine gum, maltodextrin, corn starch or carrageenan, and preferably hydroxypropyl methylcellulose.
6. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the plasticizer comprises at least one of sorbitol, polysorbate, xylitol, maltitol, glycerol, polyethylene glycol, propylene glycol, glycerate and fatty acid, and preferably glycerol.
7. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the surfactant comprises at least one of polysorbate, fatty acid glyceride, sorbitan fatty acid, amino acid type, betaine type, quaternary ammonium compound, stearic acid, sodium dodecyl sulfate and poloxamer, preferably poloxamer.
8. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the stabilizer comprises at least one of edetic acid and derivatives or salts thereof, 2, 6-di-tert-butyl-4-methylphenol, tea polyphenol, tocopherol and butyl hydroxy anisole, and preferably disodium edetate; or the correctant is one or more of sucralose, sucrose, saccharin sodium, stevioside, aspartame, menthol, cherry essence, strawberry essence, milk essence, chocolate essence, grape essence, sweet orange essence and mixed pulp essence.
9. The lurasidone hydrochloride oral instant film formulation of claim 1, wherein: the opacifier is titanium dioxide.
10. A preparation method of a lurasidone hydrochloride oral instant film preparation, which is used for preparing the lurasidone hydrochloride oral instant film preparation of any one of claims 1 to 9, and is characterized in that: comprises the following steps:
s1, crushing lurasidone hydrochloride by adopting a grinding, sieving or airflow crushing method, wherein the average particle size is controlled below 100 mu m for later use;
s2, dispersing the high-water-solubility film-forming material in the prescription amount into purified water at the temperature of 70-90 ℃, stirring and dissolving to obtain a colorless transparent solution, and then cooling to room temperature for later use;
s3, adding lurasidone hydrochloride, a plasticizer, a surfactant, a stabilizer, a flavoring agent and an opacifier in a formula amount into the high-water-solubility film-forming material solution, and stirring for 3-8 min; homogenizing with a high speed shearing machine at 5000-; finally obtaining a light yellow milky solution;
and S4, ultrasonically defoaming the light yellow emulsion solution obtained in the step S3, adding the light yellow emulsion solution into a continuous coating machine for continuous coating, drying and cutting to obtain the lurasidone hydrochloride oral instant membrane preparation.
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