Preparation method of capsule containing tegafur, gimeracil and potassium oxonate

A technology for oteracil potassium and capsules is applied in the field of preparation of capsules, which can solve the problems of gastrointestinal irritation, affect the physiological activity of preparations and the like, and achieve the advantages of reducing irritation, improving bioavailability and simple preparation process. Effect

Inactive Publication Date: 2013-05-22
JIANGSU YUNYANG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Patent CN102302499A discloses a capsule containing tegafur, gimeracil and oteracil potassium. Although the amount of surfactant sodium lauryl sulfate is reduced during the preparation process, there may still be gastrointestinal Irritating, and may affect the physiological activity of the preparation

Method used

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  • Preparation method of capsule containing tegafur, gimeracil and potassium oxonate
  • Preparation method of capsule containing tegafur, gimeracil and potassium oxonate
  • Preparation method of capsule containing tegafur, gimeracil and potassium oxonate

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The composition of the prescription is as follows (based on 1000 capsules):

[0027]

[0028] Preparation Process:

[0029] (1) Tegafur, oteracil potassium, and gimeracil are respectively passed through a 100-mesh sieve, microcrystalline cellulose and pregelatinized starch are respectively passed through a 80-mesh sieve, and magnesium stearate is passed through a 120-mesh sieve for subsequent use;

[0030] (2) The gemeracil and the pregelatinized starch that take prescription quantity are mixed uniformly, carry out air-flow micronization, obtain gemeracil-pregelatinized starch mixture micropowder;

[0031] (3) Weigh Tegafur, Oteracil Potassium, and Microcrystalline Cellulose in the prescribed amount, mix them with the above-mentioned mixture micropowder, and add 2% PVP K30 Soft material made from ethanol solution, granulated with a 26-mesh sieve, dried at 60°C for 3 hours, granulated with a 24-mesh sieve;

[0032] (4) Take the above granules, add the prescribed am...

Embodiment 2

[0034] The composition of the prescription is as follows (based on 1000 capsules):

[0035]

[0036] Preparation Process:

[0037] (1) Tegafur, oteracil potassium, and gimeracil were respectively passed through a 100-mesh sieve, lactose, microcrystalline cellulose, and pregelatinized starch were respectively passed through a 80-mesh sieve, and magnesium stearate was passed through a 120-mesh sieve for subsequent use;

[0038] (2) The gemeracil and lactose of prescription quantity are weighed and mixed homogeneously, put in the ball mill and take out after ball milling for 1h, obtain the gemeracil-lactose mixture micropowder;

[0039] (3) Weigh Tegafur, Oteracil Potassium, Microcrystalline Cellulose, Pregelatinized Starch, mix with the above-mentioned mixture micropowder, add 5% PVP K30 Soft material made from ethanol solution, granulated with a 26-mesh sieve, dried at 60°C for 2 hours, granulated with a 24-mesh sieve;

[0040] (4) Take the above granules, add the prescr...

Embodiment 3

[0042] The composition of the prescription is as follows (based on 1000 capsules):

[0043]

[0044]

[0045] Preparation Process:

[0046] (1) Tegafur, oteracil potassium, and gimeracil were respectively passed through a 100-mesh sieve, microcrystalline cellulose and pregelatinized starch were respectively passed through a 80-mesh sieve, and magnesium stearate was passed through a 120-mesh sieve for subsequent use;

[0047] (2) the gemeracil and 40g pregelatinized starch that take prescription quantity are mixed homogeneously, carry out air-flow micronization, obtain gemeracil-pregelatinized starch mixture micropowder;

[0048] (3) Take tegafur, oteracil potassium, and microcrystalline cellulose of prescription quantity, mix with the above-mentioned mixture micropowder and remaining pregelatinized starch, add 4% hypromellose aqueous solution to make soft material, Granulate with a 26-mesh sieve, dry at 60°C for 3 hours, and granulate with a 24-mesh sieve;

[0049] (4...

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Abstract

The invention relates to a preparation method of a capsule containing tegafur, gimeracil and potassium oxonate. The preparation method is characterized in that gimeracil is added in a form of micronized solid. The preparation method related by the invention overcomes bad water solubility of gimeracil by utilizing a micronized technology, thus the improvement of medicament dissolution is facilitated.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a preparation method of a capsule containing tegafur, gimeracil and oteracil potassium. Background technique [0002] Tegafur is a cell cycle-specific antineoplastic drug, mainly for the treatment of gastrointestinal tumors, such as gastric cancer, colon cancer, rectal cancer and pancreatic cancer, and can also be used for the treatment of breast cancer, bronchial lung cancer and liver cancer. Tegafur is a derivative of fluorouracil (5-FU), which has excellent bioavailability. After oral administration, it is first converted into 5-FU and then into 5-fluorouracil deoxynucleotide (5-FUMP). Inhibit thymidine nucleotide synthetase, thereby interfering with DNA biosynthesis and exerting anti-tumor activity. [0003] However, the 5-FU produced by tegafur is extremely unstable in vivo, and is easily degraded (over 85%) by dihydropyrimidine dehydrogenase (DPD) in normal ti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/53A61K31/513A61K31/4412A61K9/48A61P35/00
Inventor 范铭常瑞雪周红梅
Owner JIANGSU YUNYANG PHARMA GRP
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