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Leflunomide ethosome composition and its preparation method

A technology of leflunomide alcohol and leflunomide, which is applied in the field of leflunomide-containing ethosome composition and its preparation, and can solve the problems of low leflunomide transmittance

Inactive Publication Date: 2014-05-21
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The above prior art does not well solve the problem of low leflunomide penetration rate. The inventor unexpectedly found that leflunomide is made into ethosome transdermal preparation, which can obviously improve the transdermal rate of leflunomide. The flunomide ethosome gel can not only significantly reduce the side effects of leflunomide, but also improve the curative effect. Compared with the prior art, the composition and process are simple, and it is suitable for industrial production

Method used

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  • Leflunomide ethosome composition and its preparation method
  • Leflunomide ethosome composition and its preparation method
  • Leflunomide ethosome composition and its preparation method

Examples

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Embodiment 1

[0081] prescription composition Prescription 1 Prescription 2 Prescription 3 Prescription 4 Leflunomide 0.5g 0.5g 0.5g 0.5g Lecithin 5g 3g 1g 0.5g Absolute ethanol 45g 45g 45g 45g α-tocopherol 0.1g 0.1g 0.1g 0.1g water 49.4g 51.4g 53.4g 53.9g Total 100g 100g 100g 100g

[0082] The preparation method of leflunomide ethosome: take the prescribed amount of lecithin and leflunomide, dissolve them in absolute ethanol to form an alcoholic solution, stir at a mechanical speed of 700rpm in a water bath at 30°C, and mix the above The alcohol solution was slowly added dropwise to the water, and continued to stir for 30 minutes. After taking it out, it was cooled to room temperature, homogenized at a speed of 10,000 rpm for 1 minute, and filtered through a 0.22um filter membrane respectively to obtain the leflunomide ethanol, whose appearance was pale Yellow transparent liquid, the emulsion droplet size of the pre...

Embodiment 2

[0084] prescription composition Prescription 5 Prescription 6 Prescription 7 Prescription 8 Leflunomide 0.5g 0.5g 0.5g 0.5g Lecithin 3g 3g 3g 3g Absolute ethanol 30g 35g 60g 70g α-tocopherol 0.1g 0.1g 0.1g 0.1g water 66.4g 61.4g 36.4g 26.4g Total 100g 100g 100g 100g

[0085] The preparation method is the same as in Example 1. The emulsion droplet diameters of the prepared ethosomes are: prescription 5: 300-400nm; prescription 6: 40-70nm; prescriptions 7 and 8: 20-40nm.

Embodiment 3

[0087] prescription composition Prescription 9 Prescription 10 Prescription 11 Prescription 12 Prescription 13 Leflunomide 0.1g 1g 1.5g 2g 3g Soy lecithin 2g 2g 2g 2g 2g Absolute ethanol 45g 45g 45g 45g 45g α-tocopherol 0.1g 0.1g 0.1g 0.1g 0.1g water 52.8g 51.9g 51.4 50.9g 49.9g Total 100g 100g 100g 100g 100g

[0088] The preparation method is the same as in Example 1. The prepared ethosome emulsion particle diameters are: prescription 9: 500-700nm; prescription 10: 400-500nm; prescription 11-13: 200-400nm.

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Abstract

The invention relates to a leflunomide ethosome composition and a preparation method thereof. The leflunomide ethosome composition mainly consists of leflunomide, phospholipid, short-chain alcohol and water. The ethosome significantly improves the transdermal rate of leflunomide, can significantly reduce side effects of oral administration of leflunomide and improves curative effects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a leflunomide-containing ethosome composition and a preparation method thereof. The leflunomide ethosome composition is mainly composed of leflunomide, phospholipids, short-chain alcohols and water . Background technique [0002] Leflunomide (Leflunomide) is a new drug for the treatment of active rheumatoid arthritis. It is the first drug approved by the US FDA for rheumatoid arthritis and can improve the course of the disease. Its dosage form is tablets, and the specification is 10, 20 and 100 mg / tablet. Although its curative effect is remarkable, the active metabolite reaches the peak plasma level only 6-12 hours after oral administration, and the onset of effect is slow. At the same time, it often causes gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, gastritis and gastroenteritis after oral administration, and It has ce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K31/42A61K47/32A61K47/34A61K47/36A61K47/38A61P19/02A61P29/00
Inventor 张涛丁彦吉邓杰罗静钟晓东
Owner CHONGQING PHARMA RES INST