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Tadalafil containing orally-dissolved film agent and preparation method thereof

A technology of tadalafil and oral dissolving film, applied in the directions of pharmaceutical formulations, sexually transmitted diseases, sheet conveying, etc., can solve the problems such as affecting the health of production personnel, high requirements for workshop ventilation and explosion-proof, and increased production costs. Improve the therapeutic effect, novel dosage form, convenient medication effect

Inactive Publication Date: 2016-12-07
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it uses ethanol aqueous solution as a dispersing solvent, and the film will generate a large amount of ethanol vapor during the heating and drying process, which has high requirements for the ventilation and explosion protection of the workshop, and the production cost will increase. More importantly, it will affect the production personnel in the workshop. good health

Method used

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  • Tadalafil containing orally-dissolved film agent and preparation method thereof
  • Tadalafil containing orally-dissolved film agent and preparation method thereof
  • Tadalafil containing orally-dissolved film agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: the impact of bulk drug particle size on product quality

[0053]

[0054] Note: *: used in prescription but removed in final product.

[0055] The film prepared from the above components is dark yellow, has good flatness and foldability, plasticity and toughness, and the breaking force is within 12-16N, meeting the requirements of cutting, packaging, transportation and clinical use. The melting time is within 20 to 25 seconds, and there is no significant difference. The actual melting time in the mouth is about 10 to 15 seconds. There is no sticky feeling and the taste is good.

[0056] The above results show that: the particle size of tadalafil API D90 in the range of 10 to 25 μm has no significant impact on the physical properties and melting time of the product.

Embodiment 2

[0057] Embodiment 2: the impact of bulk drug, film-forming agent, plasticizer consumption on product quality

[0058]

[0059] Note: *: used in prescription but removed in final product.

[0060] The film prepared from the above-mentioned components has good flatness, foldability, plasticity and toughness, and the breaking force is within 11-19N, meeting the requirements of cutting, packaging, transportation and clinical use. The melting time is within 20 to 30 seconds, without significant difference, and the melting time in the mouth is about 10 to 20 seconds, with no sticky feeling and good taste.

[0061] The above results show that when the proportion of the raw material is in the range of 20-50%, the proportion of the film-forming agent is in the range of 30-60%, and the proportion of the plasticizer is in the range of 10-20%, the product has good characteristics in terms of plasticity, toughness and melting time limit.

Embodiment 3

[0062] The influence of embodiment 3 solubilizing agent and transdermal absorption accelerator on product quality

[0063]

[0064] Note: *: used in prescription but removed in final product.

[0065] The film prepared from the above components has good flatness, foldability, plasticity and toughness, and the breaking force is within 13-17N, meeting the requirements of cutting, packaging, transportation and clinical use. The melting time is within 20 to 30 seconds, without significant difference, and the melting time in the mouth is about 10 to 20 seconds, with no sticky feeling and good taste.

[0066] The above results show that when the proportion of the solubilizer is 2-10%, and the proportion of the transdermal absorption accelerator is within the range of 0.5-5%, the physical properties and melting time of the product meet the requirements.

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Abstract

The invention relates to a tadalafil containing orally-dissolved film agent and a preparation method thereof. The tadalafil containing orally-dissolved film agent starts to be absorbed in the oral cavity, takes effect quickly and is good in treatment effect and convenient to take, and water drinking is not needed. The tadalafil containing orally-dissolved film agent comprises the active ingredient tadalafil, a high-polymer film-forming material, a skin penetration enhancer and pharmaceutically-acceptable other auxiliary materials, wherein the weight percentage of tadalafil in the orally-dissolved film agent is 10-50%, preferably 20-50%; the D90 partical size of tadalafil is smaller than or equal to 25 microns, preferably smaller than or equal to 20 microns and more preferably smaller than or equal to 15 microns. The skin penetration enhancer is added into the prescription, meanwhile, the particle size of the bulk pharmaceutical chemical is controlled, tadalafil is micronized, it is ensured that the medicine is partially absorbed at the oral mucosa, the active ingredient is absorbed in the oral cavity more rapidly, and the film agent takes effect faster than tablets and other common film agents.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an orally dissolving film whose active ingredient is tadalafil, and a preparation method of the preparation. Background technique [0002] Studies have shown that about half of men over the age of 40 suffer from erectile dysfunction (ED), which seriously affects their quality of life. At present, significant research achievements have been made on the pathogenesis of ED, especially at the level of signal transduction pathways, and it has been confirmed that the nitric oxide-cyclic guanosine monophosphate (NO-cGMP) signaling pathway is the key pathway for the pathogenesis of ED. Clinical application, such as the marketing of phosphodiesterase type 5 (PDE-5) inhibitors such as sildenafil, vardenafil, and tadalafil, has achieved remarkable clinical effects. [0003] Tadalafil, its chemical name is: (6R,12aR)-2,3,6,7,12,12a-hexahydro-2-methyl-6-(1,3-benzodioxane- 5-yl)-pyra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4985A61K47/38A61K47/20A61K47/22A61K47/34A61K47/10A61P15/10
CPCA61K9/006A61K9/7015A61K31/4985A61K47/10A61K47/20A61K47/22A61K47/38
Inventor 周志超杨清敏王栋海张明会
Owner QILU PHARMA
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