Micro-pill containing tegafur, gimeracil and potassium oxonate, capsule preparation and preparation method for micro-pill

A technology of oteracil potassium and tegafur, which is applied in the field of medicine, can solve the problems of reduced drug efficacy, increased drug side effects, and inability to ensure mixing uniformity, so as to solve the problem of loading difference and content uniformity, and improve stability Effect

Inactive Publication Date: 2015-09-23
JIANGSU YUNYANG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since it is necessary to prepare tegafur, gimeracil and oteracil potassium into drug pellets separately, the complexity of the process is increased, and more importantly, it is impossible to guarantee The uniformity of mixing between the pills and oteracil potassium pellets leads to uneven content among different capsules, especially for drugs for the treatment of gastric cancer such as S-1 compound preparations, dose control is particularly important
[0008] Patent CN101711765 B discloses a method for

Method used

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  • Micro-pill containing tegafur, gimeracil and potassium oxonate, capsule preparation and preparation method for micro-pill
  • Micro-pill containing tegafur, gimeracil and potassium oxonate, capsule preparation and preparation method for micro-pill
  • Micro-pill containing tegafur, gimeracil and potassium oxonate, capsule preparation and preparation method for micro-pill

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of capsule preparations containing tegafur, gimeracil and oteracil potassium:

[0028]1. Prescription (1000 capsules)

[0029] Prescription of Tegafur Prescription Pellets:

[0030]

[0031] Isolation Layer Prescription:

[0032]

[0033] Prescriptions containing tegafur, gimeracil, and oteracil potassium pellets:

[0034]

[0035] Prescription of excipient granules:

[0036]

[0037] Prescription of total mixed granules:

[0038]

[0039] 2. Preparation process:

[0040] (1) Preparation of tegafur drug-coated pellets

[0041] After jet milling tegafur (D 90 ≤20μm), added to 40% ethanol solution (part), homogeneously dispersed; HPMC, sodium bicarbonate and sodium hydroxide were added to a certain amount of water, stirred and dissolved; the above two solutions were mixed evenly to obtain Fluoride solution, pH 9.7; blank sucrose pellet cores are added to the fluidized bed, and the drug layer solution is added through a spray gun...

Embodiment 2-10

[0050] Embodiment 2-10 prescription is as follows table: concrete preparation process is the same as embodiment one

Embodiment 1-3

[0052]

[0053]

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Abstract

The invention discloses a micro-pill containing tegafur, gimeracil and potassium oxonate, a capsule preparation and a preparation method for the micro-pill. The micro-pill comprises a tegafur drug layer-coated pill core, an isolation layer and a coating layer containing gimeracil and potassium oxonate. Tegafur, gimeracil and potassium oxonate are ground by airflow, the micro-pill is directly coated with a drug through an empty pill core, additional auxiliary materials are prepared into granules by a fluidized bed, the micro-pill is uniformly mixed with the additional auxiliary material granules, and a capsule is directly filled with a mixture. The prepared capsule is capable of enabling the drug to be stably and quickly released in bodies, remarkably improves the content uniformity and stability of the drug, has relatively high dissolution rate and bioavailability, reduces adverse drug reactions and can be commercially produced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pellet and capsule preparation containing tegafur, gimeracil and otiracil potassium and a preparation method thereof. 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 prodrug of 5-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) , the latter can inhibit thymidine nucleotide synthetase, thereby interfering with DNA biosynthesis and exerting anti-tumor activity. However, the 5-FU produced by tegafur is extremely unstable in vivo, and is easily degraded (up to 85%) by dihydropyri...

Claims

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Application Information

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IPC IPC(8): A61K31/53A61K9/16A61K9/48A61K47/02A61K47/04A61P35/00A61K31/4412A61K31/513
Inventor 鲍晓芳姜飞李燕
Owner JIANGSU YUNYANG PHARMA GRP
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