Oral soluble film composition containing vardenafil and application thereof

Abstract

The invention discloses an oral soluble film composition containing vardenafil and application of the oral soluble film composition. The oral soluble film composition comprises the following components in percentage by weight: 20.5%-25% of an active substance, 28.3%-32% of microcrystalline cellulose, 2.6%-3.3% of vitamin E, 1.5%-2.1% of a separant, 0.8%-1.1% of a lubricant, 35.6%-41.5% of a film forming material, 1.2%-1.8% of a plasticizer, 0.08%-0.12% of a pH regulator and 2.7%-3.5% of a flavoring agent, the active substance is vardenafil or vardenafil hydrochloride, the concentration of the active substance is 35-45 mg / ml, and the oral soluble film composition is applied to improving the erectile function, prolonging the sexual life time, improving the microenvironment of local spermatogenesis and improving the sperm vitality. The pH regulator is matched, so that the dissolution speed of the medicine can be increased; 40-60 hydroxypropyl methyl cellulose and polyvinyl alcohol are blended to form a film material, so that the film coating effect can be ensured, and the properties of the film can be improved; vitamin E is added in the formula, so that the microenvironment of local spermatogenesis can be improved, the sperm motility is improved, and the medicinal value of the composition is improved.

Description

Technical Field

[0001] The present invention relates to the field of medical technology, in particular to an orodispersible film composition containing vardenafil and application thereof. Background Art

[0002] Premature ejaculation and erectile dysfunction are the two most common sexual dysfunction diseases in clinical practice. Due to the mutual relationship between their etiology and pathogenesis, the two often occur together. PE is the most common sexual dysfunction in clinical practice. Its pathogenic factors may include genetic tendency, poor overall health and obesity, prostatitis, thyroid hormone imbalance, emotional problems and stress, and traumatic sexual experiences. PE can be divided into primary premature ejaculation, secondary premature ejaculation, natural variant premature ejaculation, and premature ejaculation-like ejaculatory dysfunction. Drugs commonly used in clinical treatment of PE include serotonin reuptake inhibitors, local anesthetics, psychological / behavioral therapy, α receptor antagonists, etc., but their overall efficacy is poor.

[0003] Vardenafil is an effective and highly selective phosphodiesterase 5 inhibitor with rapid onset of action. It is the second drug approved for the treatment of male erectile dysfunction after Viagra and is internationally recognized as one of the first-line oral drugs for the treatment of male erectile dysfunction. Currently, solid particles of vardenafil have a bad taste when used and a slow dissolution effect, and also do not have the effect of improving sperm. Therefore, the present application proposes an orodispersible film composition containing vardenafil. Summary of the invention

[0004] The object of the present invention is to provide an orally dissolving film composition containing vardenafil and its application, so as to solve the problems raised in the above background technology.

[0005] To achieve the above object, the present invention provides the following technical solution: an orally dissolving film composition containing vardenafil, wherein the components include the following substances by weight: the components include the following substances by weight: 20.5%-25% of active substance, 28.3%-32% of microcrystalline cellulose, 2.6%-3.3% of vitamin E, 1.5%-2.1% of release agent, 0.8%-1.1% of lubricant, 35.6%-41.5% of film-forming material, 1.2%-1.8% of plasticizer, 0.08%-0.12% of pH regulator and 2.7%-3.5% of flavoring agent;

[0006] The active substance is vardenafil or vardenafil hydrochloride, and the concentration of the active substance is 35-45 mg / ml.

[0007] Preferably, the plasticizer is one or more of glycerol, polyethylene glycol 400, propylene glycol or triethyl citrate.

[0008] Preferably, the concentration of the plasticizer is 33.5-43.8 mg / ml.

[0009] Preferably, the flavoring agent is one or more of sucralose, fructose, essence, xylitol, aspartame, saccharin sodium, cyclamate, inulin glycoside and acesulfame potassium.

[0010] Preferably, the release agent is one or more copolymers of ethylene, methacrylic acid and acrylate.

[0011] Preferably, the lubricant is one or more of magnesium stearate, magnesium lauryl sulfate, sodium stearyl fumarate, micro powder silica gel, talc and colloidal silicon dioxide.

[0012] Preferably, the film-forming material is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol, and the model of the hydroxypropyl methylcellulose is any one of SHE40, SHE50 and SHE60.

[0013] Preferably, the orally dissolving film composition containing vardenafil is used to improve erectile function, prolong the duration of sexual life, improve the local microenvironment of spermatogenesis, and improve the motility of sperm.

[0014] Compared with the prior art, the present invention has the following beneficial effects:

[0015] 1. By adding flavoring agents, the original taste of the vardenafil pharmaceutical composition can be improved, the use effect can be improved, and the dissolution rate of the drug can be increased by combining with a pH regulator;

[0016] 2. Use 40-60 hydroxypropyl methylcellulose and polyvinyl alcohol to blend the film-forming material, which can ensure the coating effect and improve the properties of the film;

[0017] 3. Adding vitamin E to the formula can improve the local microenvironment of spermatogenesis, improve sperm motility, and enhance the medicinal value of the composition. DETAILED DESCRIPTION

[0018] The present invention is described in detail below, and the technical solutions in the embodiments of the present invention are clearly and completely described. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0019] The present invention provides a technical solution: an orally dissolving film composition containing vardenafil, wherein each component comprises the following substances by weight: each component comprises the following substances by weight: 20.5%-25% of active substance, 28.3%-32% of microcrystalline cellulose, 2.6%-3.3% of vitamin E, 1.5%-2.1% of separating agent, 0.8%-1.1% of lubricant, 35.6%-41.5% of film-forming material, 1.2%-1.8% of plasticizer, 0.08%-0.12% of pH regulator and 2.7%-3.5% of flavoring agent;

[0020] The active substance is vardenafil or vardenafil hydrochloride, and the concentration of the active substance is 35-45 mg / ml.

[0021] Wherein, the plasticizer is one or more of glycerol, polyethylene glycol 400, propylene glycol or triethyl citrate.

[0022] Among them, the concentration of plasticizer is 33.5-43.8 mg / ml.

[0023] Among them, the flavoring agent is one or more of sucralose, fructose, flavor, xylitol, aspartame, saccharin sodium, cyclamate, inulin glycoside and acesulfame potassium.

[0024] Wherein, the release agent is one or more copolymers of ethylene, methacrylic acid and acrylate.

[0025] Wherein, the lubricant is one or more of magnesium stearate, magnesium lauryl sulfate, sodium stearyl fumarate, micro powder silica gel, talc and colloidal silicon dioxide.

[0026] The film-forming material is a mixture of hydroxypropylmethylcellulose and polyvinyl alcohol, and the model of the hydroxypropylmethylcellulose is any one of SHE40, SHE50 and SHE60.

[0027] Among them, the orodispersible film composition containing vardenafil is used to improve erectile function, prolong the duration of sexual life, improve the local microenvironment of spermatogenesis, and improve the vitality of sperm.

[0028] Embodiment 1:

[0029] The components of the orally dissolving film composition are calculated by weight as follows: 20.5% of vardenafil, 29% of microcrystalline cellulose, 2.6% of vitamin E, 1.5% of a release agent, 0.8% of a lubricant, 41.4% of a film-forming material, 1.4% of a plasticizer, 0.1% of a pH regulator, and 2.7% of a flavoring agent;

[0030] Weigh the above-mentioned drug raw materials according to the formula, and crush them for later use, mix the raw materials and film-forming materials evenly, disperse the plasticizer and the pH adjuster in purified water and stir evenly to obtain a solution, place the raw materials and the film-forming material in the solution, heat and disperse them homogeneously, cool after dispersion, add microcrystalline cellulose, isolation agent, vitamin E, lubricant and flavoring agent and stir evenly, let the above-mentioned drugs stand to defoam, then apply and dry, and then cut into slices and package after drying.

[0031] Embodiment 2:

[0032] The components of the orally dissolving film composition are calculated by weight as follows: 22% of vardenafil, 30% of microcrystalline cellulose, 3% of vitamin E, 1.8% of a release agent, 1% of a lubricant, 37.5% of a film-forming material, 1.6% of a plasticizer, 0.1% of a pH regulator, and 3% of a flavoring agent;

[0033] Weigh the above-mentioned drug raw materials according to the formula, and crush them for later use, mix the raw materials and film-forming materials evenly, disperse the plasticizer and the pH adjuster in purified water and stir evenly to obtain a solution, place the raw materials and the film-forming material in the solution, heat and disperse them homogeneously, cool after dispersion, add microcrystalline cellulose, isolation agent, vitamin E, lubricant and flavoring agent and stir evenly, let the above-mentioned drugs stand to defoam, then apply and dry, and then cut into slices and package after drying.

[0034] Embodiment 3:

[0035] The components of the orodispersible film composition are as follows by weight: 25% of vardenafil, 29.5% of microcrystalline cellulose, 3% of vitamin E, 1.5% of a release agent, 1% of a lubricant, 35.6% of a film-forming material, 1.3% of a plasticizer, 0.1% of a pH regulator and 3% of a flavoring agent;

[0036] Weigh the above-mentioned drug raw materials according to the formula, and crush them for later use, mix the raw materials and film-forming materials evenly, disperse the plasticizer and the pH adjuster in purified water and stir evenly to obtain a solution, place the raw materials and the film-forming material in the solution, heat and disperse them homogeneously, cool after dispersion, add microcrystalline cellulose, isolation agent, vitamin E, lubricant and flavoring agent and stir evenly, let the above-mentioned drugs stand to defoam, then apply and dry, and then cut into slices and package after drying.

[0037] Composition clinical trials:

[0038] 100 patients with primary premature ejaculation and 100 patients with erectile dysfunction were selected, with an age range of 20-45 years, with an average age of 28.5 years;

[0039] 100 patients with primary premature ejaculation were recruited, 12 of whom were lost to follow-up or dropped out, and 88 patients finally completed the trial. After 2 weeks of treatment, the IELT of premature ejaculation patients increased significantly from (2.4±0.5)min to (5.5±1.8)min.

[0040] A total of 100 patients with erectile dysfunction were recruited, 8 of whom were lost to follow-up or dropped out, and 92 patients finally completed the trial. After 2 weeks of treatment, the IELT of patients with erectile dysfunction was significantly improved from (11±2) min to (20±3) min.

[0041] Safety observation: No abnormalities were found in the liver and kidney function and blood and urine routine tests of the two groups of patients before and after treatment;

[0042] It can be concluded that the Chinese medicine composition of the present invention is used for treating phlegm-dampness type premature ejaculation and erectile dysfunction, and has the characteristics of good efficacy, no side effects, portability, and convenient administration.

[0043] The above description enables those skilled in the art to implement or use the present invention. Various modifications to these embodiments will be apparent to those skilled in the art, and the general principles defined herein may be implemented in other embodiments without departing from the spirit or scope of the present invention. Therefore, the present invention will not be limited to the embodiments shown herein, but will conform to the widest scope consistent with the principles and novel features disclosed herein.

Claims

1. An orally dissolving film composition containing vardenafil, characterized in that: The components include the following substances by weight: Active substance 20.5%-25%, microcrystalline cellulose 28.3%-32%, vitamin E 2.6%-3.3%, release agent 1.5%-2.1%, lubricant 0.8%-1.1%, film-forming material 35.6%-41.5%, plasticizer 1.2%-1.8%, pH regulator 0.08%-0.12% and flavoring agent 2.7%-3.5%; The active substance is vardenafil or vardenafil hydrochloride, and the concentration of the active substance is 35-45 mg / ml.

2. The orodispersible film composition containing vardenafil according to claim 1, characterized in that: The plasticizer is one or more of glycerol, polyethylene glycol 400, propylene glycol or triethyl citrate.

3. The orodispersible film composition containing vardenafil according to claim 2, characterized in that: The concentration of the plasticizer is 33.5-43.8 mg / ml.

4. The orodispersible film composition containing vardenafil according to claim 1, characterized in that: The flavoring agent is one or more of sucralose, fructose, essence, xylitol, aspartame, saccharin sodium, cyclamate, inulin glycoside and acesulfame potassium.

5. The orodispersible film composition containing vardenafil according to claim 1, characterized in that: The release agent is one or more copolymers of ethylene, methacrylic acid and acrylate.

6. The orodispersible film composition containing vardenafil according to claim 1, characterized in that: The lubricant is one or more of magnesium stearate, magnesium lauryl sulfate, sodium stearyl fumarate, micro powder silica gel, talc and colloidal silicon dioxide.

7. The orodispersible film composition containing vardenafil according to claim 1, characterized in that: The film-forming material is a mixture of hydroxypropylmethylcellulose and polyvinyl alcohol, and the model of the hydroxypropylmethylcellulose is any one of SHE40, SHE50 and SHE60.

8. Use of the orally dissolving film composition containing vardenafil according to any one of claims 1 to 7, characterized in that: It is used to improve erectile function, prolong the duration of sexual life, improve the local microenvironment of spermatogenesis, and improve sperm motility.