A kind of dexamethasone oral fast-dissolving film and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dexamethasone oral instant film preparation using pullulan-vitamin E succinate (PUVS) as a matrix and a preparation method thereof. The oral instant film preparation of the invention is prepared by grafting pullulan polysaccharide and vitamin E succinate as a solubilizer and suspending agent, and uniformly mixing it with drug dexamethasone and film-forming material pullulan polysaccharide A light and thin drug-carrying film with uniform distribution of drugs on the surface of the drug-carrying film. The disintegration time of the oral fast-dissolving film prepared by the present invention is less than 20s, and the dexamethasone exists in an amorphous state in the film, which is beneficial to the dissolution and absorption of the drug. Therefore, the dexamethasone oral fast-dissolving film of the present invention has The invention has the advantages of simple preparation process, fast disintegration speed, convenient portability, no limitation of time and place for taking the medicine, no need to take concomitant medicine and good compliance, and the like.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dexamethasone oral fast-dissolving film preparation based on a pullulan-vitamin E succinate conjugate PUVS and a preparation method thereof. Background technique

[0002] Dexamethasone (DEX) is an adrenal cortical hormone drug with pharmacological effects such as anti-inflammatory, anti-endotoxin, immunosuppression, anti-shock and enhancement of stress response, so it can be widely used in various departments to treat a variety of diseases , such as autoimmune diseases, allergies, inflammations, asthma, dermatological and ophthalmic diseases. Dexamethasone is currently only available in tablet and injection form. Oral instant film is a kind of light and thin drug-loaded film prepared by mixing drugs and suitable water-soluble polymer film-forming materials evenly. It can be absorbed on the surface, and it can also be partially absorbed through the digest...

Examples

Embodiment 1

[0049] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is composed of the following components by mass percentage:

[0050] Dexamethasone 1.95%

[0051] PUVS 9.77%

[0052] Film-forming material Pullulan 78.13%

[0053] Propylene Glycol 6.25%

[0054] Sodium alginate 3.9%.

[0055] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0056] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 100:1, and the reaction was continued to stir at ...

Embodiment 2

[0063] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is made up of the following components by mass percentage:

[0064] Dexamethasone 1%

[0065] PUVS 6.3%

[0066] Film-forming material 90%

[0067] Macrogol 4001.8%

[0068] Croscarmellose sodium 0.9%.

[0069] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0070] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 150:1, and the reaction was continued to stir at room temperature ...

Embodiment 3

[0074] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is made up of the following components by mass percentage:

[0075] Dexamethasone 5%

[0076] PUVS 15%

[0077] Film-forming material 64%

[0078] Glycerin 6.4%

[0079] Sodium Carboxymethyl Starch 9.6%.

[0080] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0081] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 30:1, and the reaction was continued to stir at room temperature...

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dexamethasone oral fast-dissolving film preparation based on a pullulan-vitamin E succinate conjugate PUVS and a preparation method thereof. Background technique

[0002] Dexamethasone (DEX) is an adrenal cortical hormone drug with pharmacological effects such as anti-inflammatory, anti-endotoxin, immunosuppression, anti-shock and enhancement of stress response, so it can be widely used in various departments to treat a variety of diseases , such as autoimmune diseases, allergies, inflammations, asthma, dermatological and ophthalmic diseases. Dexamethasone is currently only available in tablet and injection form. Oral instant film is a kind of light and thin drug-loaded film prepared by mixing drugs and suitable water-soluble polymer film-forming materials evenly. It can be absorbed on the surface, and it can also be partially absorbed through the digest...

Examples

Embodiment 1

[0049] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is composed of the following components by mass percentage:

[0050] Dexamethasone 1.95%

[0051] PUVS 9.77%

[0052] Film-forming material Pullulan 78.13%

[0053] Propylene Glycol 6.25%

[0054] Sodium alginate 3.9%.

[0055] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0056] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 100:1, and the reaction was continued to stir at ...

Embodiment 2

[0063] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is made up of the following components by mass percentage:

[0064] Dexamethasone 1%

[0065] PUVS 6.3%

[0066] Film-forming material 90%

[0067] Macrogol 4001.8%

[0068] Croscarmellose sodium 0.9%.

[0069] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0070] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 150:1, and the reaction was continued to stir at room temperature ...

Embodiment 3

[0074] A dexamethasone oral fast-dissolving film, the oral fast-dissolving film is made up of the following components by mass percentage:

[0075] Dexamethasone 5%

[0076] PUVS 15%

[0077] Film-forming material 64%

[0078] Glycerin 6.4%

[0079] Sodium Carboxymethyl Starch 9.6%.

[0080] The preparation method of the dexamethasone oral instant film of the above-mentioned formula, comprises the following steps:

[0081] (1) Preparation of conjugate PUVS: Dissolving pullulan in DMSO to obtain a pullulan solution for later use, 4-dimethylaminopyridine DMAP, 1-(3-dimethylaminopyridine DMAP, 1-(3-dimethypyridine) in a molar ratio of 1:1.2:1 Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, and then slowly added dropwise to the aforementioned pullulan solution. The molar ratio of pullulan to VES was 30:1, and the reaction was continued to stir at room temperature...

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