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Oral preparation containing tegafur, gimeracil and oteracil potassium

An oral preparation, the technology of tegafur, which is applied in the field of pharmaceutical preparations, can solve the problems of inconvenient industrial production, complex production process, and large gastrointestinal irritation, and achieve the goals of improving medication compliance, simple preparation process, and reducing irritation. Effect

Active Publication Date: 2012-08-01
QILU PHARMA HAINAN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN101574326A discloses a capsule preparation of S-1 and its preparation method. This invention improves the stability of S-1, but the dissolution rate of the drug has not been improved. In order to ensure rapid dissolution, a large amount of surfactant has been added. The minimum dosage reaches 10mg / capsule, which is more irritating to the gastrointestinal tract. At the same time, the pellet coating technology is adopted, and the production process in the workshop is complicated.
[0007] CN1660105A discloses a prescription and preparation process of S-1 orally disintegrating tablets, which can cover up the bad bitter taste of the medicine, but the water solubility of the medicine has not been improved
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

Method used

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  • Oral preparation containing tegafur, gimeracil and oteracil potassium
  • Oral preparation containing tegafur, gimeracil and oteracil potassium
  • Oral preparation containing tegafur, gimeracil and oteracil potassium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-21

[0035] The particle sizes of the active ingredients are: 80μm≤tegafur≤180μm, 50μm≤gimeracil≤150μm, 50μm≤octeracil potassium≤150μm, and the raw material composition of the oral preparation is shown in Table 1-3.

[0036] Table 1. Examples 1-7 Oral solid preparations of tegafur, gimeracil, and oteracil potassium

[0037] Element

Example 1

Example 2

Example 3

Example 4

Example 5

Example 6

Example 7

Tegafur

15g

20g

25g

40g

50g

50g

50g

Gimeracil

4.35g

5.8g

7.25g

11.6g

14.5g

14.5g

14.5g

Oteracil Potassium

14.7g

19.6g

24.5g

39.2g

49g

49g

49g

lactose

8g

10.7g

13.4g

21.4g

26.8g

53.6g

134g

Mannitol

12g

16g

20g

32g

40g

80g

200g

Crospovidone

1.5g

2g

2.5g

4g

5g

10g

...

Embodiment 22-42

[0065] The particle sizes of the active ingredients are: 20μm≤tegafur≤80μm, 3μm≤gimeracil≤50μm, 3μm≤octeracil potassium≤50μm, and the composition of raw materials for oral preparations is shown in Table 4-6.

[0066] Table 4. Preparation of oral solid preparations of tegafur, gimeracil, and oteracil potassium

[0067]

[0068] Preparation Process

[0069] 1) Ingredients: Weigh lactose, tegafur, gimeracil, oteracil potassium, crospovidone, mannitol, povidone, and magnesium stearate according to the prescription. The povidone is made into 10wt% aqueous solution or water-ethanol (1:1) mixed solution for later use.

[0070] 2) Premixing: add lactose, tegafur, gimeracil, oteracil potassium, crospovidone, and mannitol to the HLSH2-6A wet granulator in sequence. The premixing process parameters are the same as in Examples 1-7.

[0071] 3) Making soft material: the process parameters are the same as those in Examples 1-7, turn on the equipment, and add 10 wt% povidone aqueous so...

Embodiment 43-63

[0091] Preparation of oral preparations with particle sizes of active ingredients of tegafur ≤ 20 μm, gimeracil ≤ 3 μm, and oteracil potassium ≤ 3 μm

[0092] Table 7. Oral solid preparations of tegafur, gimeracil, and oteracil potassium in Examples 43-49

[0093]

[0094] The preparation process is as follows:

[0095] 1) Ingredients: Weigh lactose, tegafur, gimeracil, oteracil potassium, crospovidone, mannitol, povidone, and magnesium stearate according to the prescription.

[0096] 2) Premixing: add lactose, tegafur, gimeracil, oteracil potassium, crospovidone, povidone, and mannitol to the HLSH2-6A wet granulator in sequence. The premixing process parameters are the same as in Examples 1-7.

[0097] 3) Making soft material: Set the process parameters as in Example 1-7, turn on the equipment, add water or a water-ethanol (1:1) mixed solution in a stirring state to make a suitable soft material.

[0098] 4) ~ 8) wet granulation, drying, dry granulation, total blending,...

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Abstract

The invention relates to an oral preparation containing tegafur, gimeracil and oteracil potassium. The oral preparation comprises the following active ingredients: tegafur with granularity of less than or equal to 180 microns, gimeracil with granularity of less than or equal to 150 microns and oteracil potassium with granularity of less than or equal to150 microns. The oral preparation reduces the irritation of the active ingredients on the gastrointestinal tract of a human body and improves pharmaceutical compliance of patients on the premise of guaranteeing that the active ingredients are dissolved out quickly.

Description

technical field [0001] The invention relates to an oral preparation containing tegafur, gimeracil and oteracil potassium (S-1, TS-1) and belongs to the technical field of pharmaceutical preparations. Background technique [0002] Tegafur (FT, FT207) is one of the pyrimidine anticancer drugs. It is the prodrug of 5-fluorouracil (5-FU), and has inhibitory effect on most solid tumors. In the body, it can interfere and block the biosynthesis of DNA, RNA and protein, thereby producing its anticancer effect. Basic medical research and clinical observation have proved that tegafur has less toxic and side effects, higher chemotherapy index, less impact on immunosuppression and related immune organs, and is a safe drug that can be used continuously in clinical practice. This product is absorbed through the gastrointestinal tract after oral administration, and the concentration in the blood reaches its peak within 1-3 hours. The duration is longer than that of intravenous administra...

Claims

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Application Information

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IPC IPC(8): A61K31/53A61K31/513A61K31/44A61K9/20A61K9/48A61K9/16A61P35/00
Inventor 王晶翼于艳玲杨清敏张明会
Owner QILU PHARMA HAINAN
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