Sildenafil oral membrane pharmaceutical composition and preparation method thereof

A technology for sildenafil citrate and medicine, which is applied in the field of urology and can solve the problems of poor absorption, low bioavailability, and reduced

Inactive Publication Date: 2020-11-20
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to achieve the purpose of the present invention, the inventors have developed and prepared a combination of sildenafil citrate, humectant, and stabilizer synergistically, starting from the study of sildenafil citrate combined medication and dosage form improvement. The oral film composition of sildenafil citrate combined with aspirin, after testing, it was surprisingly found that the oral film composition greatly reduces the risk of myocardial infarction in the single administration of sildenafil citrate, and at the same time solves the Poor absorption, low bioavailability and problems with enterohepatic effects

Method used

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  • Sildenafil oral membrane pharmaceutical composition and preparation method thereof
  • Sildenafil oral membrane pharmaceutical composition and preparation method thereof
  • Sildenafil oral membrane pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Embodiment one: the preparation of compound sildenafil alipirin sublingual film

[0089] 1. Prescription

[0090]

[0091] 2. Preparation steps

[0092] (1) Take the above-mentioned components by prescription quantity;

[0093] (1): Weigh 40g of hypromellose and dissolve it in 400g of purified water, heat in a water bath at 60°C, and stir for 30min.

[0094] (2) Add hypromellose (HPMC), propylene glycol, mannitol, croscarmellose sodium, sodium sulfite and sodium bisulfite in sequence, stir and dissolve, then add sildenafil citrate and aspirin, mix well.

[0095] (3) Place the above-mentioned solution in a vacuum drying oven to degas for 20 minutes for later use.

[0096] (4) Apply the liquid medicine evenly on the glass plate, and dry at 40°C until the water content is 2%.

[0097] (5): Measure the content, remove the film, cut according to the content, and the specification of sildenafil citrate is 25mg / tablet.

[0098] Content detection method:

[0099](1) S...

Embodiment 2

[0106] The preparation of embodiment two compound recipe sildenafil Alipirin sublingual film

[0107] 1. Prescription

[0108]

[0109] 2. The preparation steps of compound sildenafil alipirin sublingual film

[0110] (1) Take the components of the above prescription amount;

[0111] (2) Hypromellose was dissolved in 400g of purified water, heated in a water bath at 60°C, and stirred for 30 minutes until dissolved.

[0112] (3) Add HPMC, propylene glycol, mannitol, croscarmellose sodium, sodium sulfite and sodium bisulfite in sequence, stir to dissolve, add sildenafil citrate and aspirin, and mix well.

[0113] (4) The above solution was degassed in a vacuum oven for 20 minutes for later use.

[0114] (5): Apply the liquid medicine evenly on the glass plate, and dry at 40°C until the water content is 6%.

[0115] (6): measure content, stripping, cut according to content, the specification of sildenafil 25mg / sheet.

[0116] The assay method is the same as in Example 1....

Embodiment 3

[0117] Preparation of embodiment three compound sildenafil alipirin sublingual film

[0118] 1. Prescription

[0119]

[0120]

[0121] 2. Preparation steps:

[0122] (1) Dissolve 20g of hypromellose in 200g of purified water in a water bath, heat at 60°C, and stir for 30min until dissolved.

[0123] (2) Add HPMC, propylene glycol, mannitol, croscarmellose sodium, sodium sulfite and sodium bisulfite in sequence, stir to dissolve, add sildenafil citrate and aspirin, and mix well.

[0124] (3) The above solution was degassed in a vacuum drying oven for 20 minutes for later use.

[0125] (4) Apply the liquid medicine evenly on the glass plate, and dry at 40°C until the water content is 4%.

[0126] (5) Measure the content of sildenafil, remove the film, cut according to the content, the specification of sildenafil is 25mg / sheet.

[0127] The assay method is the same as in Example 1.

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Abstract

The invention belongs to the technical field of urinary science, and particularly relates to a compound preparation for treating erectile dysfunction, a compound preparation for treating erectile dysfunction and a solvent coating method for preparing the compound preparation. The effective medicine component of the compound preparation are a compound preparation sublingual membrane of sildenafil citrate and aspirin, and the compound preparation further comprises a disintegrating agent, a humectant, a stabilizer, a film forming material and a plasticizer, wherein the mass ratio of the sildenafil citrate to the aspirin is 1:(0.1-0.9). The sildenafil citrate in the compound preparation sublingual membrane is quick to disintegrate and high in bioavailability, gastrointestinal tract damage andliver first-pass effect can be avoided, toxic and side effects are reduced, sudden death caused by coronary heart disease and the like after sildenafil is taken is prevented, the side effects are greatly reduced, and a synergistic interaction effect is achieved. The compound preparation not only can improve the clinical use compliance of existing marketed dosage forms, but also can improve the clinical curative effect, and has particularly high clinical development and use values.

Description

technical field [0001] The invention relates to the technical field of urology, in particular to a compound preparation for treating erectile dysfunction. Background technique [0002] Impotence (ED) is one of the common diseases that endanger the physical and mental health of adult men. Its physiological essence is that the penis cannot achieve and / or maintain enough erection to obtain a satisfactory sexual life for more than 3 months. Erectile dysfunction in men. Sildenafil is the most widely used oral treatment for ED. Sildenafil, a selective circulating GMP-specific phosphodiesterase type 5 inhibitor (PDE5), treats erectile dysfunction by enhancing the downstream effects of nitric oxide (NO)-mediated vasodilation. PDE5 is found in pulmonary vascular smooth muscle and corpus cavernosum, as well as in tissues such as vascular and visceral smooth muscle and platelets. PDE5 can hydrolyze cGMP into GMP and block the NO-cGMP pathway that causes penile erection. Sildenafil ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/616A61K9/70A61K47/38A61K47/10A61K47/26A61P15/10A61P15/00
CPCA61K9/006A61K9/7007A61K31/519A61K31/616A61K47/10A61K47/26A61K47/38A61P15/00A61P15/10A61K2300/00
Inventor 陈用芳胡延贵刘行鹏郑勇张映财杨绪凤
Owner CHONGQING CONQUER PHARML
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