A kind of preparation method of S-1 composition

A composition and technology of tegafur, applied in the direction of drug combination, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve complex cyclodextrin inclusion process, complicated production process, and strengthen drug side effects and other problems, to achieve the effects of rapid and complete drug dissolution, reduced contact degree, and simple preparation process

Active Publication Date: 2019-03-12
JIANGSU HENGRUI MEDICINE CO LTD
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the in vitro dissolution problem has been solved, sodium lauryl sulfate may promote the in vivo absorption of tegafur and gimeracil, which may enhance the toxic and side effects of the drug
[0006] CN101843621A discloses a kind of tigio granule, which is solved by making the active ingredient of the drug into a cyclodextrin inclusion compound to improve the dissolution rate and bioavailability of the drug. However, the cyclodextrin inclusion process is relatively complicated, and the workshop industry Chemical production has many inconveniences
[0007] CN101711765A discloses a S-1 dispersible tablet, gimeracil and oteracil potassium can be released in the stomach before tegafur, and can make oteracil potassium better protect the gastrointestinal tract. Pyrimidine plays a better role in synergizing with tegafur, which improves patient compliance, but the process adopts pellet coating technology, and the production process in the workshop is complicated
However, this process increases the contact degree of raw materials and excipients, which is not conducive to the stability of the preparation
[0011] CN104147012A discloses a method for preparing S-1 orally disintegrating preparations by wet granulation, but the described orally disintegrating preparations contain disintegrants and further contain binders, which is unfavorable for preparation stability

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of preparation method of S-1 composition
  • A kind of preparation method of S-1 composition
  • A kind of preparation method of S-1 composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 5

[0036] Preparation process: According to the ratio in Table 1, pass the raw and auxiliary materials through a 80-mesh sieve, mix the three raw materials evenly, add purified water, use a Glatt wet granulator to granulate, dry at 60°C, sieve through a 30-mesh sieve, and add filling agent and magnesium stearate, mixed uniformly, and filled into capsules to prepare S-1 capsules.

[0037] Table 1

[0038]

Embodiment 1～5 and comparative Embodiment 1～4

[0047] Embodiments 1 to 5 and comparative examples 1 to 4: determination of dissolution rate

[0048]Adopt dissolution measurement method (Chinese Pharmacopoeia 2015 edition general rule 0931 second method), get the capsule in embodiment 1~5 and comparative example 1~4, take purified aqueous solution as dissolution medium, rotating speed is 50 rpm, temperature is 37±0.5°C, operate according to the law, at 15 minutes, take 10ml of the eluate, filter the eluate with a 0.45μm filter membrane, and use high performance liquid chromatography to determine tegafur, gimeracil and oteracil in S-1 capsules The dissolution rate of potassium is limited to 85% of the labeled amount, and the dissolution results are shown in Table 4.

[0049] Table 4

[0050]

[0051]

[0052] The results of the dissolution test show that the dissolution rate of the active ingredients in Examples 1 to 5 (the filler is lactose or sugar alcohols) is greater than 85% in 15 minutes, and the dissolution rat...

Embodiment 1～5 and comparative Embodiment 5～8

[0053] Embodiment 1~5 and comparative example 5~8: preparation stability investigation

[0054] (1) Influencing factor test: get an appropriate amount of Sigion Capsules in Examples 1 to 5 and Comparative Examples 5 to 8, place them under strong light irradiation (4500lx ± 500lx), high temperature (60°C, high humidity 90%) Placed under the same conditions, samples were taken to check the relevant substances on the 5th and 10th days respectively, and the results are shown in Table 5:

[0055] table 5

[0056]

[0057] (2) Accelerated test: get the Tigio capsules in Examples 1 to 5 and Comparative Examples 5 to 8, place 40°C of temperature under commercially available packaging, and place 6 capsules in a constant temperature and humidity box with a relative humidity of 75%. month, and at the end of the 1st, 2nd, 3rd, and 6th months, the relevant substances were sampled and inspected. The results are shown in Table 6:

[0058] Table 6

[0059]

[0060] Influencing factor...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention provides a preparation method of a tegafur gimeracil oteracil potassium composition. Particularly, the tegafur gimeracil oteracil potassium composition comprises tegafur, gimeracil, oteracil potassium, a filler and a lubricant. The method comprises the steps that tegafur, gimeracil and oteracil potassium are used as raw materials and mixed for wet granulation, and then the filler and the lubricant are additionally added to obtain the tegafur gimeracil oteracil potassium composition. By means of the preparation method, on the premise that rapidly dissolving-out of active ingredients in preparations is ensured, the prepared tegafur gimeracil oteracil potassium composition reduces the increasing rate of impurities in the product during storage and improves the stability of the product.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of a composition containing tegafur, gimeracil and oteracil potassium. Background technique [0002] S-1 is a fluorouracil derivative oral anticancer agent, which includes tegafur (FT) and the following two types of regulators: gimeracil (CDHP) and oteracil (Oxo). The functions of its three components are as follows: FT is a prodrug of 5-Fu, which has excellent oral bioavailability and can be converted into 5-Fu in vivo. CDHP can inhibit the catabolism of 5-Fu released from FT under the action of dihydropyrimidine dehydrogenase. Note similar effects. Oxo can block the phosphorylation of 5-Fu. After oral administration, Oxo has a high distribution concentration in the gastrointestinal tissue, thereby affecting the distribution of 5-Fu in the gastrointestinal tract, thereby reducing the toxicity of 5-Fu. Compared with 5-Fu, S-1 has the ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/53A61K9/48A61P35/00A61K31/4412A61K31/513
CPCA61K9/4858A61K31/4412A61K31/513A61K31/53A61K2300/00
Inventor 王小岩王聪王晓莉刘凯
Owner JIANGSU HENGRUI MEDICINE CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap