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Preparation method of d-alpha-tocopheryl succinate monoester biomembrane covering

A technology of phenol succinate monoester and biofilm, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of losing the active molecular structure of cancer cells, d-α- Tocopherol succinate monoester cannot be used in human body to treat cancer patients and other problems, and achieve the effect of inducing the deformation of cancer cells

Inactive Publication Date: 2010-07-28
华东中药工程集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0032] This difficulty prevents d-alpha-tocopheryl succinate from being used in humans to treat cancer patients
[0033] We studied the molecular structure of d-α-tocopheryl succinate, and found that one end is a hydroxyl group, which is a hydrophilic group, and the other end is an ester group, which is a lipophilic group. The whole molecule is a surfactant Therefore, after entering animals and human bodies, it is easily hydrolyzed and reduced to tocopherol by various body fluids, losing its active molecular structure that can kill cancer cells

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1. Dissolve 100 kg of d-α-tocopherol succinate monoester technical powder in 500 kg of diethyl ether isopropyl ether ethanol, add 200 kg of β-cyclodextrin, and stir for 1 hour at 50°C to make d-α-tocopherol Phenol succinate monoester is encapsulated in the biofilm, heated and steamed to remove 200 kg of solvent, and cooled to 10°C to obtain d-α-tocopherol succinate monoester biofilm coating.

[0044] The d-α-tocopheryl succinate monoester biofilm coating is separated by a centrifuge, dried in a vacuum drier, and pulverized to obtain the d-α-tocopheryl succinate biofilm coating powder.

[0045] After mixing the above-mentioned d-alpha-tocopherol succinate monoester biofilm coating powder with the binder cellulose dissolved in ethanol liquid, use a granulator to obtain d-alpha-tocopherol succinate monoester biofilm coating Coated granules.

[0046] The dried d-alpha-tocopheryl succinate monoester biofilm coating granules are filled into hollow capsules to obtain...

Embodiment 2

[0047] Example 2. Dissolve 100 kg of d-α-tocopheryl succinate monoester technical powder in 500 kg of diethyl ether isopropyl ether ethanol, add 200 kg of cellulose, and stir at 50°C for 1 hour to make d-α-tocopheryl succinate The acid monoester is encapsulated in the biofilm, heated and steamed to remove 200 kg of solvent, and cooled to 10°C to obtain the d-α-tocopherol succinate monoester biofilm coating.

[0048] After adding 300 kilograms of corn oil and 20 kilograms of emulsifier (Pingping plus Paregalo) to the above-mentioned d-α-tocopheryl succinate biofilm coating, mix them, and use gelatin as the capsule shell to make d in a capsule machine. - α-tocopheryl succinate monoester biofilm coating soft capsule preparation; or mix with gelatin and use liquid paraffin as a forming agent in a dropping pill machine to prepare d-α-tocopheryl succinate biofilm Film-coated drop pill dosage form.

Embodiment 3

[0049]Example 3. Dissolve 100 kg of d-alpha-tocopherol succinate monoester technical powder in 200 kg of chloroform solvent, add 150 kg of phospholipid liposome membrane material, stir for 2 hours and then stand still for 24 hours to make d-alpha-tocopherol The succinate monoester is encapsulated in the biofilm, and 100 kg of solvent is evaporated by heating to obtain the d-α-tocopherol succinate monoester biofilm coating.

[0050] Add 100 kg of distilled water and 20 kg of additives to the d-alpha-tocopheryl succinate monoester biofilm coating, stir and mix, heat to evaporate the remaining solvent, freeze-dry to obtain powder injection; After being homogenized by a homogenizer, the injections are packaged.

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Abstract

The invention relates to a preparation method of a d-alpha-tocopheryl succinate monoester biomembrane covering, belonging to the technical field of drug preparation. The invention aims to provide a preparation method of a d-alpha-tocopheryl succinate monoester biomembrane covering which enables d-alpha-tocopheryl succinate monoester not to be decomposed by human body fluid so as to obtain cancer-curing effect of restraining cancer cell proliferation and inducing cell apoptosis after the d-alpha-tocopheryl succinate monoester enters a human body. The invention has the technical points of: dissolving the powder of d-alpha-tocopheryl succinate monoester drug into an organic solvent and adding a biomembrane material and then stirring to enable the d-alpha-tocopheryl succinate monoester to be coated into a biomembrane; heating to evaporate and remove the solvent to obtain the d-alpha-tocopheryl succinate monoester biomembrane covering. The d-alpha-tocopheryl succinate monoester biomembrane covering prepared by the method can not be decomposed by the human body fluid after entering the human body and has the effects of controlling cancer cell diffusion transfer, restraining the cancer cell proliferation and inducing the cancer cell deformation and even apoptosis.

Description

technical field [0001] The invention relates to a preparation method of a d-alpha-tocopheryl succinate monoester biofilm coating, which belongs to the technical field of medicine preparation. Background technique [0002] Cancer has become one of the diseases with extremely high morbidity and mortality in the world, and the medical community all over the world is conducting in-depth research on finding effective therapeutic drugs for curing cancer. my country has also placed innovative drugs for the treatment of cancer in an important position in medical research. [0003] The original drug and preparation of d-α-tocopheryl succinate monoester have been included in the USP-23 edition of the United States Pharmacopoeia more than ten years ago, and are classified as vitamin drugs. It is widely used in vitamin nutritional supplements and health food in the United States and Europe. [0004] In recent years, medical research institutions at home and abroad have published a lar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K47/38A61K47/30A61K47/24A61K31/355A61P35/00
Inventor 曹光明倪其骅陶维鉴倪霄良曹伟
Owner 华东中药工程集团有限公司
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