Sildenafil rapidly disintegrating film composition with high drug loading capacity

A technology of sildenafil and high drug loading, which is applied in the direction of drug combination, non-active ingredients of polymer compounds, medical preparations of non-active ingredients, etc., to achieve good taste, high clinical development and use value, and easy access Effect

Active Publication Date: 2015-05-06
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The choice of film-forming materials for this patent is the same as the problem faced by the international patent application WO2012108738, and this application does not propose a solution for how to improve the in vivo bioavailability of sildenafil citrate
This patent uses pullulan as a film-forming material and faces the same problem as the above-mentioned patent, and this application also fails to propose a solution for how to improve the bioavailability of sildenafil citrate in vivo

Method used

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  • Sildenafil rapidly disintegrating film composition with high drug loading capacity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 Preparation of sildenafil citrate oral instant film composition using gelatin as film-forming material

[0040] In this example, gelatin was used as a film-forming material, and glycerin was used as a plasticizer to prepare sildenafil citrate oral instant film compositions with different drug loadings. The specific prescription composition is shown in the table below. Prepare the sildenafil citrate oral instant film composition according to the following process steps: take the prescription amount of gelatin and dissolve it in hot water, add glycerin and stir evenly; take the prescription amount of sildenafil citrate and add it to the gelatin solution Stir evenly; remove the foam and air bubbles in the feed liquid by vacuum stirring to obtain a uniform feed liquid; use a coating machine to coat the feed liquid into a film with a thickness of 200-500um and dry it at a temperature of 40-70°C; cut The thickness is 80-180um, the area is 5-10cm 2 Oral instant ...

Embodiment 2

[0044] Example 2 The effect of plasticizer content on the performance of sildenafil citrate oral instant film composition

[0045] According to the preparation method described in Example 1, use glycerin as the plasticizer according to the formula listed in the following table to prepare the different sildenafil citrate oral instant film compositions of the plasticizer content, and detect the performance of the film Evaluation.

[0046] prescription composition

[0047] The sildenafil citrate oral instant film composition prepared according to the prescription composition listed in the above table is found to have the following characteristics after testing. Prescription 6 does not contain any plasticizer, and as a result, the oral instant film composition prepared has poor physical properties, is easily broken, and is difficult to cut and shape. Prescription 7 is an oral instant film composition containing 20% ​​glycerin as a plasticizer. Although it is relatively ...

Embodiment 3

[0048] Example 3 Effects of different types of plasticizers on the performance of sildenafil citrate oral instant film composition

[0049] According to the preparation process described in Example 1, the sildenafil citrate oral instant film composition containing different types of plasticizers was prepared according to the prescription composition of the following table, and the performance of the film composition was detected and evaluated.

[0050] prescription composition

[0051] The sildenafil citrate oral instant film composition prepared according to the prescription listed in the above table is found to have the following characteristics after testing: when one or more of the different types of plasticizers with a content of 15% are used in combination, the The prepared sildenafil citrate oral instant film composition has substantially consistent physical properties. In terms of product toughness and strength, it can meet the requirements of production, tra...

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Abstract

The invention belongs to the field of pharmaceutical preparation and especially relates to a sildenafil film composition. The invention provides a sildenafil rapidly disintegrating film composition with high drug loading capacity. The sildenafil rapidly disintegrating film composition with high drug loading capacity comprises (a) an active pharmaceutical ingredient which is sildenafil or pharmaceutically acceptable salt, and (b) a film forming material which accounts for 5-50%(w / w) of the composition and comprises gelatin which accounts for 10%-100% of the film forming material, (c) a plasticizer and (d) a taste regulator, wherein the biological availability of the active ingredient sildenafil in the film composition is about 60%. The composition disclosed by the invention takes gelatin as a main film forming material, and the obtained sildenafil film agent has the advantages of high drug loading capacity, good physical performance, perfect stability, nice taste and high biological availability, and is capable of rapidly disintegrating in oral cavity. The composition disclosed by the invention is used for treating male erectile dysfunction disease.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a sildenafil oral fast-dissolving film pharmaceutical composition with high drug loading. Background technique [0002] Sildenafil (Sildenafil) is a phosphodiesterase V (PDE-5) inhibitor used to treat erectile dysfunction. It was first launched in the United States in 1998 under the trade name "Viagra". The active ingredient in the commercially available sildenafil tablets is in the form of citrate. [0003] Erectile dysfunction refers to the state that normal sexual life is hindered due to the influence of ejaculation and orgasm disorders, specifically manifested as inability to achieve or maintain an erection during sexual intercourse, premature ejaculation and steatorrhea. Drugs currently on the market for the treatment of erectile dysfunction include PDE-5 inhibitors such as sildenafil, vardenafil, tadalafil, and avanafil. Among these drugs, sildenafil citrate was...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/519A61K47/42A61K47/04A61P15/10
Inventor 王栋海杨清敏张明会程廷廷
Owner QILU PHARMA CO LTD
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