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Solid preparation containing capsaicin and preparation method thereof

A solid preparation, capsaicin technology, applied in the directions of medical preparations containing active ingredients, medical preparations inactive ingredients, pill delivery, etc., can solve the problems of difficult preservation, difficult drying, complicated preparation process of enteric-coated tablets, etc. , to achieve the effect of low energy consumption and high stability

Inactive Publication Date: 2016-12-14
杭州成邦医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as described in another patent CN103027901A, this chitosan-loaded capsaicin microsphere has hygroscopicity and is not easy to preserve; meanwhile, the strong stimulation of capsaicin to the stomach has not yet been well resolved
Therefore, in the patent CN103027901A, the chitosan-loaded capsaicin microsphere modified dosage form is made into an enteric-coated tablet. Although the enteric-coated tablet solves the problem of capsaicin stimulating the stomach, it ignores the fact that capsaicin also has the same effect on the intestinal mucosa. irritant
Moreover, the preparation process of enteric-coated tablets is also complicated. Since the temperature used to prepare chitosan-loaded capsaicin microspheres by spray drying method is as high as 160 ° C, capsaicin has already melted at this temperature, so it is difficult to achieve drying, which is also not conducive to capsaicin. element stability

Method used

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  • Solid preparation containing capsaicin and preparation method thereof
  • Solid preparation containing capsaicin and preparation method thereof
  • Solid preparation containing capsaicin and preparation method thereof

Examples

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preparation example Construction

[0043]The preparation method of dropping pill, capsule and tablet is respectively as follows:

[0044] The preparation method of the tablet is as follows: fully mix the capsaicin and menthol of the prescribed amount, pour it into a hot-melt extruder, preheat the hot-melt extruder to 60-70°C, pour in the materials and heat for 3-5 Minutes later, it is extruded into shape; after crushing, it is mixed with the prescribed amount of auxiliary materials, compressed into micro-tablets or conventional tablets, and coated.

[0045] The preparation method of the dripping pill is as follows: fully mix the prescribed amount of capsaicin and menthol, preheat the heating tank of the dropping pill machine to 60-70°C, pour in the material and heat for 3-5 minutes, and control the temperature of the dripper at 70°C. ℃; then drop the mixture of capsaicin and menthol into the simethicone oil not exceeding 20 ℃, shrink and form, that is.

[0046] The preparation method of the capsule is as follo...

Embodiment 10

[0056] Take 46g of capsaicin and 454g of menthol and mix them thoroughly. Heat the heating tank of the dripping pill machine to 70°C in advance, pour in the material and heat for 5 minutes, control the temperature of the dripper at about 70°C, and place the mixture of capsaicin and menthol In the dropper storage barrel of the dropping pill machine, drop it into the simethicone oil below 20°C through a dropper with a diameter of 2mm, and shrink it to form a dropping pill weighing about 5mg.

[0057] Isolation coat layer: Take 20g of HPMC and prepare a solution with 600mL of distilled water, then add 3g of citric acid, 0.4g of Span 80, 2g of polyethylene glycol and 12g of talc, and stir evenly. Coating was carried out in a fluidized bed, and the weight of the isolation layer was increased by 3%.

[0058] Coating slow-release coating layer: take 70g of ethyl cellulose and dissolve it in an appropriate amount of ethanol, take 30g of hydroxypropyl methylcellulose and dissolve it in...

Embodiment 11

[0060] Take 83g of capsaicin and 417g of menthol and mix them thoroughly. Heat the heating tank of the dripping pill machine to 70°C in advance, pour in the material and heat for 5 minutes, control the temperature of the dripper at about 70°C, and place the mixture of capsaicin and menthol In the dropper storage barrel of the dropping pill machine, drop it into simethicone oil at a temperature below 20°C through a dripper with a diameter of 3mm, shrink and shape, and obtain a droplet weighing about 6mg.

[0061] Isolation coat layer: Take 20g of HPMC and prepare a solution with 600mL of distilled water, then add 3g of citric acid, 0.4g of Span 80, 2g of polyethylene glycol and 12g of talc, and stir evenly. Coating was carried out in a fluidized bed, and the weight of the isolation layer was increased by 3%.

[0062] Slow-release coating layer: Dissolve 80g of cellulose acetate in an appropriate amount of ethanol, dissolve 20g of povidone in an appropriate amount of water, mix ...

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Abstract

The invention provides a solid preparation containing capsaicin.The solid preparation is prepared from capsaicin, menthol, a coating layer and auxiliary materials, wherein the coating layer is a double-layer coating and consists of an isolation coating layer and a slow release coating layer.The auxiliary materials include a filling agent and a lubricant. The solid preparation containing the capsaicin applies the menthol as a carrier for the first time, so that the in-water solubility of the capsaicin in the preparation is improved from 0.011 micro-g / mL to 40 micro-g / mL and is far higher than that ofJapan's commercially availablecapsaicin tablets (2.6micro-g / mL). Therefore, the taking dosage of a final product can be reduced, the irritation of the capsaicin to the gastrointestinal tract is reduced. In addition, double-layer coating design is conducted on the final product, the stability of the product is also ensured while release is controlled. Furthermore,attractive, complete and smooth slow-release coatings having a slow-release effect can be achieved without any plasticizer or anti-sticking agent.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid preparation containing capsaicin and a preparation method thereof. Background technique [0002] Capsaicin (capsaicin) is a class of vanillyl amide alkaloids present in pepper fruit, and is the main spicy component in pepper. It has many pharmacological effects, such as anti-inflammatory and analgesic, antibacterial and antipruritic, cardiovascular protection, anti-cancer and weight loss. [0003] In recent years, people have paid more and more attention to obesity, not only because of the pursuit of beauty, but also because people have realized that obesity can induce a series of diseases. The anti-obesity effect of capsaicin has also been recognized by many scholars, and its anti-obesity mechanism can be classified as follows: [0004] ① Affect appetite: Moderate doses of capsaicin can inhibit gastric acid secretion and weaken gastric motility, t...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/48A61K31/165A61K47/10A61P3/04
CPCA61K31/165A61K9/2013A61K9/2866A61K9/2886A61K9/5042A61K9/5073A61K47/10
Inventor 戈震惠美
Owner 杭州成邦医药科技有限公司
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