Dexamethasone oral instant film agent with pullulan-vitamin E succinate as matrix and preparation method of dexamethasone oral instant film agent

Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a dexamethasone oral instant film agent with pullulan-vitamin E succinate (PUVS) as a matrix and a preparation method of the dexamethasone oral instant film agent. The oral instant film agent is a light and thin medicine carrying film prepared by grafting pullulan and vitamin E succinate as a solubilizerand a suspending agent and uniformly mixing a film forming material, namely the pullulan with a medicine, namely dexamethasone, and the medicine is uniformly distributed on the surface of the medicine carrying film. The disintegration time of the oral instant film agent prepared by the invention is less than 20s, and the dexamethasone exists in the film agent in an amorphous state, so that dissolution and absorption of the medicine are facilitated; and therefore, the dexamethasone oral instant film agent has the advantages of being simple in preparation process, high in disintegration speed,convenient to carry, free of limitation of time and place in medicine taking, free of a concomitant taking agent for concomitant taking, good in 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 instant film with a pullulan-vitamin E succinate conjugate PUVS as a matrix and a preparation method thereof. Background technique

[0002] Dexamethasone (DEX) is an adrenocortical hormone drug that has pharmacological effects such as anti-inflammation, anti-endotoxin, immune suppression, anti-shock and enhancement of stress response, so it can be widely used in various departments to treat various diseases , such as autoimmune diseases, allergies, inflammation, asthma, dermatology and eye diseases. The dosage forms of dexamethasone on the market are currently only tablets and injections. Oral instant film is a light and thin drug-loaded film prepared by mixing the drug with a suitable water-soluble polymer film-forming material. After the dosage form is placed on the tongue of the human oral cavity, the drug contained in it can directl...

Examples

Embodiment 1

[0049] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of 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 cavity instant film of above-mentioned formula comprises the following steps:

[0056] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 100:1, continue to stir and react at room temperature for 48 hours; add the reaction solution dropwise to...

Embodiment 2

[0063] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of mass percentage:

[0064] Dexamethasone 1%

[0065] PUVS 6.3%

[0066] Film-forming material 90%

[0067] Polyethylene glycol 400 1.8%

[0068] Croscarmellose Sodium 0.9%.

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

[0070] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 150:1, continue to stir and react at room temperature for 48 hours; add the reaction solution dropwise to abs...

Embodiment 3

[0074] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of mass percentage:

[0075] Dexamethasone 5%

[0076] PUVs 15%

[0077] Film-forming material 64%

[0078] Glycerin 6.4%

[0079] Sodium Starch Carboxymethyl 9.6%.

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

[0081] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 30:1, continue to stir and react at room temperature for 48h; add the reaction solution dropwise to absolute ethanol to...

technical field

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

[0002] Dexamethasone (DEX) is an adrenocortical hormone drug that has pharmacological effects such as anti-inflammation, anti-endotoxin, immune suppression, anti-shock and enhancement of stress response, so it can be widely used in various departments to treat various diseases , such as autoimmune diseases, allergies, inflammation, asthma, dermatology and eye diseases. The dosage forms of dexamethasone on the market are currently only tablets and injections. Oral instant film is a light and thin drug-loaded film prepared by mixing the drug with a suitable water-soluble polymer film-forming material. After the dosage form is placed on the tongue of the human oral cavity, the drug contained in it can directl...

Examples

Embodiment 1

[0049] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of 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 cavity instant film of above-mentioned formula comprises the following steps:

[0056] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 100:1, continue to stir and react at room temperature for 48 hours; add the reaction solution dropwise to...

Embodiment 2

[0063] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of mass percentage:

[0064] Dexamethasone 1%

[0065] PUVS 6.3%

[0066] Film-forming material 90%

[0067] Polyethylene glycol 400 1.8%

[0068] Croscarmellose Sodium 0.9%.

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

[0070] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 150:1, continue to stir and react at room temperature for 48 hours; add the reaction solution dropwise to abs...

Embodiment 3

[0074] A kind of dexamethasone oral cavity instant film, described oral cavity instant film is made up of the following components of mass percentage:

[0075] Dexamethasone 5%

[0076] PUVs 15%

[0077] Film-forming material 64%

[0078] Glycerin 6.4%

[0079] Sodium Starch Carboxymethyl 9.6%.

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

[0081] (1) Preparation of conjugate PUVS: Dissolve pullulan in DMSO to obtain a pullulan solution for use, mix 4-dimethylaminopyridine DMAP, 1-(3-di Methylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC and vitamin E succinate VES were dissolved in DMSO and stirred and activated at room temperature for 1 h, then slowly added dropwise to the aforementioned pullulan solution, the resulting The molar ratio of pullulan and VES is 30:1, continue to stir and react at room temperature for 48h; add the reaction solution dropwise to absolute ethanol to...

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