Film formulation of lumateperone or salt thereof, and preparation method therefor
Patent Information
- Application Number
- PCT/CN2025/139577
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2025-02-18
- Filing Date
- 2025-12-03
- Publication Date
- 2026-08-27
Smart Images
Figure PCTCN2025139577-FTAPPB-I100001 
Figure PCTCN2025139577-FTAPPB-I100002 
Figure PCTCN2025139577-FTAPPB-I100003
Abstract
Description
A film-forming agent of lumepirozol or its salt and its preparation method
[0001] This invention claims priority to Chinese Patent Application No. 202510176111.6, filed on February 18, 2025, entitled “A film-forming agent of lumepirozoline or its salt and a method for preparing the same,” the entire contents of which are incorporated herein by reference. Technical Field
[0002] This invention relates to the field of pharmaceutical technology, specifically to a film-forming agent of lumepone or its salt and its preparation method. Background Technology
[0003] Lumateperone (trade name Caplyta) is a novel atypical antipsychotic drug developed by Intra-Cellular Therapies.
[0004] In December 2019, the U.S. Food and Drug Administration (FDA) approved rumepiride tosylate for the treatment of schizophrenia in adults. In December 2021, the FDA further approved rumepiride tosylate for an expanded indication, allowing it to be used as monotherapy or in combination with lithium / valproate for the treatment of bipolar I or II-related depressive episodes in adults, making it the first and only drug with these indications.
[0005] Its structural formula is shown below:
[0006] Lumepiride tosylate is a 5-hydroxytryptamine subtype 2A (5-HT) 2A D2 receptor antagonists, presynaptic and postsynaptic antagonists of D2 receptors, D1 receptor-dependent glutamate regulators, and serotonin reuptake inhibitors.
[0007] Due to the uncertainty of the onset time of schizophrenia and the poor patient compliance during the onset of the disease, it is necessary to administer medication to patients as soon as possible. Therefore, it is very important to prepare rumepiride into a dosage form that is easy to carry, easy to take, and can take effect quickly. Rumepiride tosylate is available in capsule form on the market, and some companies are also developing orally disintegrating tablets to improve patient compliance.
[0008] For example, Chinese patent CN118557536A specifically relates to a rumepiride orally disintegrating tablet composition, its preparation method, and its application. By weight percentage, the raw materials of the rumepiride orally disintegrating tablet composition include: 16%-20% rumepiride tosylate, 40%-60% hydrophilic diluent, 10%-20% alkaline diluent, 5%-15% disintegrant, 3%-9% flavoring agent, 0.5%-1% flow aid, and 0.2%-2% lubricant.
[0009] While rumepiride tosylate has satisfactory efficacy, tolerability, and safety, with relatively minor effects on weight management, cardiovascular metabolism, and extrapyramidal symptoms, it also faces several challenges. The study "New Antipsychotic Drug: Rumepiride (Sheng Qinrun, Shen Yifeng, Li Huafang)" records that the absolute bioavailability of rumepiride capsules in humans is 4.4%. Due to its low bioavailability and high first-pass metabolism, there are significant differences in drug bioavailability among different patients, leading to uncertainty in efficacy. Furthermore, since increasing the dose does not linearly increase drug exposure, better therapeutic effects cannot be achieved by increasing the dose. Moreover, the occupancy of rumepiride tosylate at the D2 target is much lower than that of conventional antipsychotic drugs, at only 39%. Therefore, achieving high blood exposure through oral rumepiride tosylate capsules is difficult.
[0010] In summary, developing a lumepiride tosylate formulation and innovating its preparation method and administration form to improve its bioavailability and increase its D2 target occupancy rate is a key research focus for researchers in this field. Summary of the Invention
[0011] To address the aforementioned problems, this invention provides a rumeperone tosylate film-forming agent. Its preparation involves adding appropriate amounts of film-forming materials, plasticizers, disintegrants, and stabilizers, and then delivering the drug via the oral mucosa or sublingual route. Using the formulation developed in this invention, this delivery method not only significantly improves drug bioavailability, increases blood drug concentration, and enhances brain drug content and D2 target occupancy, but also effectively enhances therapeutic efficacy, providing patients with a more efficient and convenient treatment experience.
[0012] To achieve the above objectives, the technical solution adopted by the present invention is as follows:
[0013] On one hand, the present invention provides a film-forming agent of lumepone or its salt, comprising, by weight parts: 2-30 parts of lumepone or its pharmaceutically acceptable salt, 40-95 parts of film-forming material, 1-30 parts of plasticizer and 0.1-5 parts of antioxidant;
[0014] The film-forming material is selected from at least one of copovidone, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, povidone, hydroxypropyl methylcellulose, polyvinyl alcohol, polyoxyethylene, polyethylene glycol, hydroxypropyl cellulose, and hydroxyethyl cellulose;
[0015] The plasticizer is selected from at least one of polyethylene glycol, glycerin, propylene glycol, triacetin, triethyl citrate, sorbitol, mannitol, dibutyl phthalate, Span and Tween;
[0016] The antioxidant is selected from at least one of butylated hydroxyanisole, butylated hydroxytoluene, and sodium bisulfite.
[0017] Preferably, the product comprises, by weight parts, the following raw materials: 2-25 parts of lumepirozol or a pharmaceutically acceptable salt thereof, 40-92 parts of film-forming material, 1-20 parts of plasticizer and 0.2-5 parts of antioxidant;
[0018] More preferably, the product comprises, by weight parts: 2-12 parts of lumepone or a pharmaceutically acceptable salt thereof, 45-92 parts of film-forming material, 1-15 parts of plasticizer and 0.2-4 parts of antioxidant;
[0019] Preferably, the film-forming material is selected from at least one of copovidone, polyoxyethylene, and hydroxypropyl methylcellulose; more preferably, the film-forming material is selected from at least one of copovidone and polyoxyethylene; more preferably, the film-forming material is copovidone and polyoxyethylene.
[0020] Preferably, the mass ratio of the copolyvinylpyrrolidone to polyoxyethylene is 2-8:2-8.
[0021] Preferably, the plasticizer is selected from at least one of polyethylene glycol, propylene glycol and polyvinylpyrrolidone; more preferably, the plasticizer is polyethylene glycol.
[0022] Preferably, the antioxidant is sodium bisulfite.
[0023] Preferably, the raw materials of the film agent may also include flavoring agents.
[0024] Preferably, the flavoring agent is selected from at least one of sucralose, flavoring, citric acid, and tartaric acid. More preferably, the flavoring agent is selected from at least one of sucralose and flavoring.
[0025] Preferably, the product comprises, by weight parts, the following ingredients: 2-30 parts of lumepirozol or a pharmaceutically acceptable salt thereof, 40-95 parts of film-forming material, 1-30 parts of plasticizer, 0.1-5 parts of antioxidant, and 0.1-3 parts of flavoring agent.
[0026] Preferably, the film is delivered via the oral mucosa or sublingual route.
[0027] Preferably, the lumepirozon or a pharmaceutically acceptable salt thereof is lumepirozon tosylate.
[0028] On the other hand, the present invention provides a method for preparing the above-mentioned film agent, which is a hot-melt method, comprising the following steps:
[0029] After the raw materials are mixed, they are extruded at a speed of 0.01-100 kg / h and stretched into a film.
[0030] Preferably, the hot-melt method includes the following steps:
[0031] (1) Mixing of raw and auxiliary materials;
[0032] (2) Add the mixture to the hot melt extrusion equipment at a rate of 0.01-100 kg / h. The die temperature of the hot melt extruder is 130-190℃. After extrusion, stretch the mixture into a film. Adjust the rotation speed of the film stretching device to obtain films of different thicknesses and widths.
[0033] (3) The prepared membrane is cut into membranes of different sizes and shapes using a membrane cutting machine.
[0034] Preferably, the screw speed of the hot melt extrusion is 20-800 rpm.
[0035] Preferably, when the preparation method is the hot-melt method, the raw materials of the film agent, by mass parts, include the following components:
[0036] Lumepiride toluene 2-28 parts, copovidone 40-66 parts, polyethylene oxide 40-66 parts, polyethylene glycol 2-10 parts, BHT 0.1-0.5 parts, sucralose 0.1-1.5 parts.
[0037] Furthermore, the present invention provides a method for preparing the above-mentioned film agent, which is a solvent method.
[0038] Preferably, the solvent method includes the following steps:
[0039] Step 1: Mix the film-forming material with the solvent, add the solubilizer and flavoring agent, and stir to obtain the adhesive solution;
[0040] Step 2: Apply the adhesive solution evenly to form a film.
[0041] Preferably, the solvent is selected from water or alcohol.
[0042] Preferably, when the preparation method is a solvent method, the raw materials of the film-forming agent, by mass parts, include the following components:
[0043] 10-30 parts of lumepirozoline toluenesulfonate, 45-65 parts of film-forming material, 5-10 parts of propylene glycol, 5-15 parts of polyvinylpyrrolidone, 1-2 parts of sucralose, and 0.3-0.8 parts of fruit flavoring.
[0044] Preferably, the film-forming material is selected from polyvinyl alcohol or hydroxypropyl methylcellulose.
[0045] Preferably, the film agent has a weight of 25 mg or 50 mg.
[0046] Preferably, the dosage of API in the film is 2 mg or 4 mg (calculated as lumepirozol).
[0047] Compared with the prior art, the present invention has the following beneficial effects:
[0048] 1. This invention introduces an innovative lumepimeron tosylate film formulation, which delivers the drug via the oral mucosa or sublingual route. Using the formulation developed in this invention, this delivery method not only significantly improves drug bioavailability and rapidly increases blood drug concentration, but also enhances brain drug content and D2 target occupancy, ultimately effectively strengthening the therapeutic effect and providing patients with a more efficient and convenient treatment experience.
[0049] 2. The film preparation of the present invention involves adding appropriate amounts of film-forming materials, plasticizers, disintegrants and stabilizers, etc., to prepare a film with a smooth appearance, uniform thickness, rapid disintegration, good mechanical properties, and toluenesulfonate lumepirozoline in amorphous or microcrystalline form. It has good solubility and stability, and its bioavailability is significantly higher than that of the original capsule.
[0050] 3. The toluenesulfonate lumepirozol oral film of the present invention has good solubility, can completely disintegrate within 30 seconds, and is rapidly absorbed by the oral mucosa. Detailed Implementation
[0051] To make the technical means, creative features, achieved objectives, and effects of this invention readily understandable, the invention is further illustrated below with specific embodiments. However, these embodiments are merely preferred embodiments and not all embodiments. Other embodiments obtained by those skilled in the art based on the embodiments described herein without creative effort are all within the scope of protection of this invention. It is worth noting that the raw materials used in this invention are all common commercially available products, and their sources are not specifically limited. The technical and scientific terms used in the embodiments have the meanings commonly understood by those skilled in the art to which this invention pertains.
[0052] Raw material source:
[0053] Lumepiride tosylate was purchased from Wuhan Hanxiang Biotechnology Co., Ltd.
[0054] Copovidone was purchased from BASF, with a molecular weight of 45,000-70,000.
[0055] The polyoxyethylene was purchased from Dow Chemical Company in the United States, with a molecular weight of approximately 200,000.
[0056] Polyethylene glycol was purchased from Jiangxi Alpha High-Tech Pharmaceutical Co., Ltd., with a molecular weight of 5000-7000.
[0057] Example 1
[0058] A film-forming agent of lumepirozol or its salt
[0059] The prescription is as follows:
[0060] Table 1. Prescription for Example 1
[0061] The preparation method is hot-melt method:
[0062] Weighing: Accurately weigh the batch prescription amount of raw and auxiliary materials for later use;
[0063] Mixing: First, take the raw material and copovidone and pass them through a 30-mesh sieve; then add the remaining materials and pass them through a 30-mesh sieve together with the above materials.
[0064] Hot melt extrusion: Experiments were conducted using a hot melt extruder to prepare lumepirozon toluenesulfonic acid film. The extrusion temperatures were set to 80, 100, 125, 145, 145, 145, 145, and 145℃, the film nozzle temperature was set to 145℃, the feed rate was 0.6 kg / h, the screw speed was 50 rpm, and the film stretching speed was 2 rpm. The parameters were subsequently adjusted according to the material state.
[0065] Cutting: The prepared membrane is cut into membranes of different sizes and shapes using a membrane cutting machine.
[0066] Examples 2-4
[0067] A film-forming agent of lumepirozol or its salt
[0068] The prescription is as follows:
[0069] Table 2. Prescriptions for Examples 2-4
[0070] The preparation method is the same as in Example 1.
[0071] Examples 5-6
[0072] A film-forming agent of lumepirozol or its salt
[0073] The prescription is as follows:
[0074] Table 3. Prescriptions for Examples 5-6
[0075] The preparation method is the same as in Example 1.
[0076] Examples 7-8
[0077] A film-forming agent of lumepirozol or its salt
[0078] The prescription is as follows:
[0079] Table 4. Prescriptions for Examples 7-8
[0080] Preparation method, solvent method:
[0081] Accurately weigh the prescribed amount of polyvinyl alcohol and add it to 10 times the amount of purified water, stirring thoroughly to allow it to swell. Then, slowly add the prescribed amounts of propylene glycol, lumepirolen toluenesulfonate, polyvinylpyrrolidone, sucralose, and fruit flavoring sequentially, stirring at 1000 rpm for 1 hour to obtain the adhesive solution. Apply the solution using a coating machine, attaching a backing material. Adjust the coating thickness to approximately 80±5 μm, setting the coating speed to 10 rpm, and evenly coat the adhesive solution onto the backing to form a film. Dry at 40±5℃. After drying, the film is intact, exhibiting good flexibility and mechanical strength.
[0082] Cutting: The prepared membrane is cut into membranes of different sizes and shapes using a membrane cutting machine.
[0083] Examples 9-10
[0084] A film-forming agent of lumepirozol or its salt
[0085] The prescription is as follows:
[0086] Table 5. Prescriptions for Examples 9-10
[0087] Preparation method, solvent method:
[0088] Accurately weigh the prescribed amount of hydroxypropyl methylcellulose and add it to 8 times the volume of a 60% ethanol aqueous solution. Stir thoroughly to allow it to swell. Then, slowly add the prescribed amounts of propylene glycol, lumepirolen toluenesulfonate, polyvinylpyrrolidone, sucralose, and fruit flavoring sequentially. Stir at 1000 rpm for 1 hour to obtain the adhesive solution. Apply the adhesive solution using a coating machine, install a backing material, and adjust the coating thickness to achieve a film thickness of approximately 80±5 μm. Set the coating speed to 10 rpm and evenly coat the adhesive solution onto the backing material to form a film. Dry at 40±5℃. After drying, the film is intact and exhibits good flexibility and mechanical strength.
[0089] Cutting: The prepared membrane is cut into membranes of different sizes and shapes using a membrane cutting machine.
[0090] Examples 11-13
[0091] A film-forming agent of lumepirozol or its salt
[0092] The prescription is as follows:
[0093] Table 6. Prescriptions for Examples 11-13
[0094] The preparation method is as described in Example 1.
[0095] Examples 14-16
[0096] A film-forming agent of lumepirozol or its salt
[0097] The prescription is as follows:
[0098] Table 7. Prescriptions for Examples 14-15
[0099] The preparation method is as described in Example 1.
[0100] Example 16
[0101] A film-forming agent of lumepirozol or its salt
[0102] The prescription is as follows:
[0103] Table 8. Prescription for Example 16
[0104] Preparation method, hot melt method:
[0105] Weighing: Accurately weigh the batch prescription amount of raw and auxiliary materials for later use;
[0106] Mixing: First, take the raw material and copovidone and pass them through a 30-mesh sieve; then add the remaining materials and pass them through a 30-mesh sieve together with the above materials.
[0107] Hot melt extrusion:
[0108] Experiments were conducted using a hot melt extruder to prepare lumepiroben toluenesulfonate film. The temperature, feed speed, and film stretching speed were set as shown in Table 9.
[0109] Table 9. Parameters of Example 16
[0110] Examples 17-20
[0111] A film-forming agent of lumepirozol or its salt
[0112] The prescription is as follows:
[0113] Table 10. Prescriptions for Examples 17-20
[0114] Preparation method, hot melt method: same as in Example 1.
[0115] Comparative Example 1
[0116] A film-forming agent of lumepirozol or its salt
[0117] The prescription is as follows:
[0118] Table 11. Prescription for Comparative Example 1
[0119] The preparation method is as described in Example 1.
[0120] Comparative Example 2
[0121] A film-forming agent of lumepirozol or its salt
[0122] The prescription is as follows:
[0123] Table 12. Prescriptions for Comparative Example 2
[0124] The preparation method is as described in Example 1.
[0125] Comparative Example 3
[0126] A film-forming agent of lumepirozol or its salt
[0127] The prescription is as follows:
[0128] Table 13. Prescriptions for Comparative Example 3
[0129] The preparation method is as described in Example 1.
[0130] Comparative Example 4
[0131] A film-forming agent of lumepirozol or its salt
[0132] The prescription is as follows:
[0133] Table 14. Prescriptions for Comparative Example 4
[0134] The preparation method is as described in Example 1.
[0135] Comparative Example 5
[0136] A film-forming agent of lumepirozol or its salt
[0137] The prescription is the same as in Example 1, only the preparation method has been changed in terms of parameters, specifically:
[0138] The preparation method is hot-melt method:
[0139] Weighing: Accurately weigh the batch prescription amount of raw and auxiliary materials for later use;
[0140] Mixing: First, take the raw material and copovidone and pass them through a 30-mesh sieve; then add the remaining materials and pass them through a 30-mesh sieve together with the above materials.
[0141] Hot melt extrusion: Experiments were conducted using a hot melt extruder to prepare lumepirozoline toluenesulfonic acid film. The extrusion temperatures were set to 80, 100, 115, 125, 125, 125, 125, 125℃, the film nozzle temperature was set to 125℃, the screw speed was 50 rpm, and the film pulling speed was 2 rpm. The parameters were subsequently adjusted according to the material state.
[0142] Cutting: The prepared membrane is cut into membranes of different sizes and shapes using a membrane cutting machine.
[0143] Test Example 1
[0144] Tensile strength and disintegration time test results
[0145] Disintegration time: Determined according to the disintegration time test method in Appendix 0921 of the 2020 edition of the Chinese Pharmacopoeia;
[0146] Tensile strength: Using a medical packaging performance tester, tensile tests were conducted on different batches of film. A 5cm sample was cut from each batch, with a clamp spacing of 20mm and a testing speed of 5mm / min. Three samples were tested per batch, and the average tensile strength was recorded.
[0147] Table 15. Results of Examples 1-10
[0148] Table 16. Results of Examples 11-20
[0149] Table 17. Results of Example 16
[0150] Table 18. Results of Comparative Examples 1-5
[0151] As shown in Tables 15-18, when the ratio of copolyvinylpyrrolidone to polyethylene oxide exceeds the range specified in this patent, neither Comparative Example 2 nor Comparative Example 3 can successfully form a film. Furthermore, when the film-forming temperature deviates from the process parameters specified in this patent, although Comparative Example 5 can form a film, the film surface has a noticeable grainy texture, and its appearance does not meet product standards. While the film morphology of Comparative Example 4 is normal, during the stability test, the related impurities increased too rapidly, failing to meet quality requirements.
[0152] In contrast, the films from Examples 1 to 15 all had normal appearances, and their tensile strength and disintegration time met the product standard requirements. This indicates that, under the condition of strictly following the formulation range and process parameters defined in this patent, the quality and performance of the film can be effectively guaranteed.
[0153] Test Example 2
[0154] The film preparations prepared in Examples 1, 14-15, and Comparative Example 4 were placed in aluminum bags, sealed, and then placed in a stability chamber (55°C, RH 75%). Related substances were detected using high-performance liquid chromatography (HPLC), and the data are as follows:
[0155] Table 19. Stability
[0156] Test Example 3
[0157] Animals: Albino guinea pigs, male, weighing 270-330g, 6 in total.
[0158] Animal administration: After fasting for 12 hours, albino guinea pigs were orally administered 3 mg / kg (calculated as rumeperone) of rumeperone tosylate solution (accurately weigh 6.516 mg of rumeperone tosylate powder and place it in a 15 mL centrifuge tube, add 4.530 mL of pure water, and sonicate until dissolved to obtain rumeperone tosylate solution). They were also administered sublingually 0.3 mg / kg (calculated as rumeperone) of rumeperone tosylate film prepared in Example 1.
[0159] Blood collection method: Blood is collected from the upper canthus vascular plexus.
[0160] The specific administration method is as follows:
[0161] Table 20. Administration Method
[0162] Table 21. Results
[0163] As shown in Tables 20-21, the lumepirozon tosylate film formulation, administered sublingually, exhibits a shorter time to peak concentration (Tmax) and a higher peak concentration (Cmax) compared to gavage administration of lumepirozon tosylate solution. This administration method facilitates the rapid crossing of the blood-brain barrier by lumepirozon tosylate, thereby increasing its occupancy at the D2 target site and significantly enhancing its efficacy. Furthermore, relevant data also indicate that sublingual administration of lumepirozon tosylate film significantly improves the absolute bioavailability of the drug.
[0164] Test Example 4
[0165] Animals: Beagles, male, four, average weight 10kg.
[0166] Animal administration: 10 mg (calculated as rumepiride) of rumepiride tosylate film prepared in Examples 1 and Comparative Examples 1-5 and Example 15 of CN110430879 was administered sublingually.
[0167] Table 22. Results
[0168] As shown in Table 22, the toluenesulfonate lumepirozon film-forming agent prepared in Example 1 of this invention can reach T faster. max Furthermore, its effectiveness is enhanced by increasing the occupancy rate of the D2 target, potentially leading to better therapeutic effects. It can take effect more quickly for acute psychotic symptoms compared to some sudden onset conditions.
[0169] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, and is not intended to limit the scope of protection of the present invention. Simple modifications or equivalent substitutions made by those skilled in the art to the technical solution of the present invention do not depart from the essence and scope of the technical solution of the present invention.
Claims
1. A film formulation of lurasidone or a salt thereof, characterized by, Based on parts by weight, it contains the following raw materials: 2-30 parts of lumepirozol or its pharmaceutically acceptable salt, 40-95 parts of film-forming material, 1-30 parts of plasticizer and 0.1-5 parts of antioxidant; The film-forming material is selected from at least one of copovidone, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, povidone, hydroxypropyl methylcellulose, polyvinyl alcohol, polyoxyethylene, polyethylene glycol, hydroxypropyl cellulose, and hydroxyethyl cellulose; The plasticizer is selected from at least one of polyethylene glycol, glycerin, propylene glycol, triacetin, triethyl citrate, sorbitol, mannitol, dibutyl phthalate, Span and Tween; The antioxidant is selected from at least one of butylated hydroxyanisole, butylated hydroxytoluene, and sodium bisulfite.
2. The film-forming agent according to claim 1, characterized in that, Based on parts by weight, it contains the following raw materials: 2-25 parts of lumepirozol or its pharmaceutically acceptable salt, 40-92 parts of film-forming material, 1-20 parts of plasticizer and 0.2-5 parts of antioxidant.
3. The film-forming agent according to claim 1, characterized in that, Based on parts by weight, it contains the following raw materials: 2-12 parts of lumepone or its pharmaceutically acceptable salt, 45-92 parts of film-forming material, 1-15 parts of plasticizer and 0.2-4 parts of antioxidant.
4. The film-forming agent according to claim 1, characterized in that, The film-forming material is selected from at least one of copovidone, polyoxyethylene, and hydroxypropyl methylcellulose.
5. The film-forming agent according to claim 1, characterized in that, The film-forming material is selected from at least one of copolyvinylpyrrolidone and polyoxyethylene.
6. The film-forming agent according to claim 1, characterized in that, The film-forming material is copolyvinyl ketone and polyoxyethylene; the mass ratio of copolyvinyl ketone to polyoxyethylene is 2-8:2-8.
7. The film-forming agent according to claim 1, characterized in that, The plasticizer is selected from at least one of polyethylene glycol, propylene glycol, and polyvinylpyrrolidone.
8. The film-forming agent according to claim 1, characterized in that, The antioxidant is sodium bisulfite.
9. The film-forming agent according to claim 1, characterized in that, The raw materials of the film agent may also include flavoring agents.
10. The film-forming agent according to claim 9, characterized in that, The flavoring agent is selected from at least one of sucralose, flavoring, citric acid, and tartaric acid.
11. The film-forming agent according to claim 9, characterized in that, Based on parts by weight, it contains the following ingredients: 2-30 parts of lumepone or its pharmaceutically acceptable salt, 40-95 parts of film-forming material, 1-30 parts of plasticizer, 0.1-5 parts of antioxidant, and 0.1-3 parts of flavoring agent.
12. The film-forming agent according to claim 1, characterized in that, The film delivers the drug via the oral mucosa or sublingual route.
13. The film-forming agent according to claim 1, characterized in that, The rumepiride or its pharmaceutically acceptable salt is rumepiride tosylate.
14. A method for preparing the film-forming agent according to any one of claims 1-13, characterized in that, The hot melt method includes the following steps: After the raw materials are mixed, they are extruded at a speed of 0.01-100 kg / h and stretched into a film.
15. The preparation method according to claim 14, characterized in that, The screw speed of the hot melt extrusion is 20-800 rpm.
16. The preparation method according to claim 14, characterized in that, When the preparation method is hot-melt method, the raw materials of the film agent, by mass parts, include the following components: Lumepiride toluene 2-28 parts, copovidone 40-66 parts, polyethylene oxide 40-66 parts, polyethylene glycol 2-10 parts, BHT 0.1-0.5 parts, sucralose 0.1-1.5 parts.
17. A method for preparing the film-forming agent according to any one of claims 1-13, characterized in that, This is a solvent method.