Return to site

Sildenafil oral film dissolving agent and preparation method thereof

1. An oral dissolving film agent, characterized in that, the oral dissolving film agent comprises the following components: a pharmaceutical active ingredient, a water-soluble polymer film-forming material, a plasticizer and a flavoring agent, and the pharmaceutical active ingredient is Sildenafil citrate and/or a pharmaceutically acceptable salt thereof, the water-soluble polymer film-forming material is hydroxypropyl cellulose, pullulan, hydroxypropyl methyl cellulose or polyvinylpyrrolidone Any one or a combination of at least two of them.
2. The oral dissolving film agent of claim 1, wherein the water-soluble polymer film-forming material is a combination of hydroxypropyl cellulose and pullulan;
Preferably, the mass ratio of the hydroxypropyl cellulose and pullulan is 3:1 to 1:3, preferably 2:1;
Preferably, the molecular weight of the hydroxypropyl cellulose is 40,000 to 80,000;
Preferably, the molecular weight of the pullulan is 100,000 to 300,000;
Preferably, the weight of the water-soluble polymer film-forming material accounts for 10%-20% of the dry weight of the oral film-dissolving agent.
3. The oral dissolving agent of claim 1 or 2, wherein the sildenafil citrate or its pharmaceutically acceptable
The particle size of the accepted salt is less than 25μm, preferably 1.7-5.7μm;
Preferably, the weight of the sildenafil citrate or a pharmaceutically acceptable salt thereof accounts for the dry weight of the oral film dissolving agent
50% to 70%.
4. The oral dissolving film agent according to any one of claims 1-3, wherein the plasticizer comprises PEG400,
Any one of PEG600, glycerin, propylene glycol, triacetin, triethyl citrate or dibutyl phthalate or
A combination of at least two, preferably glycerin;
Preferably, the weight of the plasticizer accounts for 5% to 10% of the dry weight of the mouth-dissolving film agent.
5. The oral dissolving film according to any one of claims 1 to 4, wherein the corrective agent comprises sucrose, trichloro
Any one of sucrose, aspartame, stevioside, hesperidin, maltodextrin, flavor, sweetness enhancer or sodium chloride or to
A combination of at least two, preferably a combination of sucralose, flavor and sodium chloride;
Preferably, the mass ratio of the sucralose, flavor and sodium chloride is 3-6:2-4:1.5-3, preferably 6:3:2;
Preferably, the weight of the corrective agent accounts for 15%-25% of the dry weight of the mouth-dissolving film agent.
6. A method for preparing an oral dissolving film according to any one of claims 1 to 5, characterized in that it comprises the following steps:
Step:
The flavoring agent, the water-soluble polymer film-forming material and the plasticizer are mixed in a solvent to obtain a mixed solution, which is added
The active ingredient of the medicine is added, dispersed to obtain a medicine solution, and then a film forming process is performed to obtain the oral dissolving film agent.
7. The preparation method of claim 6, wherein the solvent is pure water or a combination of pure water and ethanol
Things.
8. The preparation method of claim 6 or 7, wherein the mixing of the flavoring agent, the water-soluble polymer film-forming material and the plasticizer in a solvent is achieved by the following method:
(1) Add the corrective agent to the solvent and stir to obtain the corrective agent solution;
(2) Add the water-soluble polymer film-forming material to the flavoring agent solution obtained in step (1), and stir to obtain a uniform water-soluble polymer film-forming material solution;
(3) Add a plasticizer to the water-soluble polymer film-forming material solution obtained in step (2), and stir to obtain a mixed solution;
Preferably, the stirring rate in step (3) is 10-30 revolutions per minute;
Preferably, the stirring time in step (3) is 2-5 hours.
9. The preparation method according to any one of claims 6-8, wherein the solid-liquid ratio of the drug solution is 1:1 to 1:4, preferably 1:2 to 1:3;
Preferably, the method of the film forming treatment is: uniformly coating the drug solution on a flat backing material with a film coater, drying, and releasing the film to obtain the oral film dissolving agent;
Preferably, the backing material is a PE film, a PET film or a PP film;
Preferably, the drying temperature is 25-60°C, preferably 40°C.
10. The preparation method according to any one of claims 6-9, characterized by comprising the following steps:
(1) Add the corrective agent to the solvent and stir to obtain the corrective agent solution;
(2) Add the water-soluble polymer film-forming material to the flavoring agent solution obtained in step (1), and stir to obtain a uniform water-soluble polymer film-forming material solution;
(3) Add a plasticizer to the water-soluble polymer film-forming material solution obtained in step (2), and stir for 2-5 hours to obtain a mixed solution;
(4) Add active pharmaceutical ingredients to the mixed solution obtained in step (3), and disperse to obtain a pharmaceutical solution;
(5) The drug solution is evenly coated on the flat backing material with a film coater, dried at 25-60° C., and the film is released to obtain the oral dissolving agent.