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A kind of preparation method of S-1 composition

A composition and tegafur technology, which is applied in the directions of pharmaceutical combinations, active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, etc. problems, to achieve the effects of rapid and complete drug dissolution, simple preparation process and reduced contact degree

Active Publication Date: 2018-12-21
JIANGSU HENGRUI MEDICINE CO LTD
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  • 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

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  • A kind of preparation method of S-1 composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 5

[0034] Preparation process: According to the proportions in Table 1, pass the raw and auxiliary materials through an 80-mesh sieve, mix tegafur, oteracil potassium and fillers evenly, add purified water, use Glatt wet granulator to granulate, and dry at 60°C. 30-mesh sieve to dry the whole grain, add gimeracil and magnesium stearate, mix evenly, fill capsules, and prepare S-1 capsules.

[0035] Table 1

[0036]

Embodiment 1～5 and comparative Embodiment 1～4

[0045] Embodiments 1 to 5 and comparative examples 1 to 4: determination of dissolution rate

[0046]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.

[0047] Table 4

[0048]

[0049]

[0050] 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

[0051] Embodiment 1~5 and comparative example 5~8: preparation stability investigation

[0052] (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:

[0053] table 5

[0054]

[0055] (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:

[0056] Table 6

[0057]

[0058] Influencing factor...

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Abstract

The invention provides a preparation method of a tegafur gimeracil and oteracil potassium composition. Particularly, the tegafur gimeracil and oteracil potassium composition is prepared from tegafur, gimeracil, oteracil potassium, filler, and lubricant. The method provided by the invention is carried out by prilling applies tegafur, oteracil potassium, and filler, and performing external processes on gimeracil and lubricant. On the basis of guaranteeing the rapid dissolution of active components in the preparation, the tegafur gimeracil and oteracil potassium composition prepared by the preparation method reduces the growth rate of impurities during the product storage process and improves the product stability.

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

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/513A61K31/44A61K31/53A61K47/26A61P35/00
CPCA61K31/44A61K31/513A61K31/53A61K47/26A61K2300/00
Inventor 王小岩王聪王晓莉刘凯
Owner JIANGSU HENGRUI MEDICINE CO LTD
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