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Dihydroartemisinin controlled-release preparation used for treating lupus erythematosus

A technology of dihydroartemisinin and controlled-release preparations, which is applied in the field of pharmacy, can solve the problems of short half-life of dihydroartemisinin and inconvenient medication, and achieve the effects of reduced treatment cost, convenient medication and stable performance

Inactive Publication Date: 2013-07-03
GUILIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life of dihydroartemisinin, it is inconvenient to take it several times a day to maintain the effective blood concentration.
At present, there are no reports about dihydroartemisinin controlled-release preparations for the treatment of lupus erythematosus

Method used

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  • Dihydroartemisinin controlled-release preparation used for treating lupus erythematosus
  • Dihydroartemisinin controlled-release preparation used for treating lupus erythematosus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Immediate-release pellets: 20g of dihydroartemisinin of 10-50μm, 10g of mannitol, 10g of lactose, 26g of microcrystalline cellulose, 6g of crospovidone, 0.2g of butylated hydroxytoluene, 0.1g of citric acid, hydroxypropyl 8 g of cellulose and 20 g of 95% (v / v) ethanol are used as binders to make quick-release pellets.

[0033] Controlled-release pellet core: 80g dihydroartemisinin 10-50μm, 100g sucrose, 147g starch, 60g dextrin, 136g microcrystalline cellulose, 27g povidone, 2g butylated hydroxytoluene, 1g citric acid, hypromellose Cellulose 14g, 70% (v / v) ethanol 350g are wetting agent, make controlled-release ball core.

[0034] Sublayer coated pellets: 540 g of controlled-release ball cores, coated with 5.4 g of zein protein and 270 g of 95% (v / v) ethanol, with a weight gain of about 1%.

[0035] Coated pellets 1: 135g of coated bottom pellets, coated with ethyl cellulose 2g, hypromellose 0.4g, polyethylene glycol-400 0.3g, 95% (v / v) ethanol 70g mixed solution coati...

Embodiment 2

[0040] Dihydroartemisinin solid dispersion: 10 g of povidone is dissolved in 100 g of 95% (v / v) ethanol, 20 g of dihydroartemisinin is added to dissolve it, and the solution is adsorbed on 30 g of crospovidone, Evaporate the solvent to make fine particles.

[0041] Immediate-release pellets: 60g of dihydroartemisinin solid dispersion, 5g of croscarmellose sodium, 5g of lactose, 10g of microcrystalline cellulose, 0.2g of butylated hydroxytoluene, 0.1g of citric acid, and 2.1g of povidone 1. Distilled water 30g is a wetting agent, made into quick-release pellets.

[0042] Controlled-release pill core: micronized dihydroartemisinin 80g, starch 117g, polyethylene glycol-6000 150g, hypromellose 80g, microcrystalline cellulose 110g, butylated hydroxytoluene 2g, citric acid 1g, hypromellose Cellulose 20g, 70% ethanol solution 500g are wetting agent, make controlled-release ball core.

[0043] Sublayer coat pellets: 540 g of controlled-release ball cores, coated with a mixture of No...

Embodiment 3

[0049] Immediate-release pellets: 20g of dihydroartemisinin of 10-50μm, 35g of microcrystalline cellulose, 4g of crospovidone, 0.3g of butylated hydroxytoluene, 0.2g of citric acid, 3g of povidone, 30g of 95% ethanol As a binder, it is made into quick-release pellets.

[0050] Controlled-release pellet core: 60g of dihydroartemisinin with a diameter of 10-50 μm, 120g of sucrose, 300g of microcrystalline cellulose, 27g of povidone, 3g of butylated hydroxytoluene, 30g of hydroxypropyl cellulose and 300g of distilled water as wetting agents. Formed into a controlled-release pellet core.

[0051] Coated pellet 1: 67.5g of controlled-release pellet core, wrapped with 1g of hypromellose, povidone 1, 0.5g of polyethylene glycol-400, 0.5g of glycerin, and 150g of 70% (v / v) ethanol clothing, gaining about 2% in weight.

[0052] Coated pellet 2: 135g of controlled-release pellet core, coated with No. IV acrylic resin 4g, povidone 1g, polyethylene glycol-400 0.2g, glycerin 0.2g, 95% (v...

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Abstract

The invention discloses a dihydroartemisinin controlled-release preparation used for treating lupus erythematosus. The controlled-release preparation shows at least one property of the following: (1) according to an in-vitro release curve, when the preparation is placed for 0.5h according to a standard dissolution test, an accumulative release rate of dihydroartemisinin is 10-25%; and (2) according to a healthy adult single-dose oral administration dihydroartemisinin in-vivo absorption curve, an average time for 40% absorption is longer than approximately 2h, and / or an average time for 70% absorption is longer than approximately 6h. With the preparation, dihydroartemisinin in-vivo release speed can be controlled. The preparation can be taken only once every day, and long-time effective blood concentration can be maintained, such that medication is more convenient. The preparation has stable performance, and low toxic and side effect. Because the preparation only needs to be taken once a day, treatment cost is reduced.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a dihydroartemisinin controlled-release preparation for treating lupus erythematosus. Background technique [0002] Lupus erythematosus, especially systemic lupus erythematosus (SLE), is a complex systemic disease that invades not only the skin, but also connective tissue, blood vessels, and internal organs. It is a refractory autoimmune disease. In recent years, the incidence of SLE has been on the rise. According to the survey, the prevalence of SLE in the world is about 17 / 10-48 / 100,000. In the United States, the prevalence of people over 18 years old is 50.8 / 100,000, the prevalence rate of the Chinese population is 30-70 / 100,000, second only to blacks (100 / 100,000), ranking second in the world. [0003] For the treatment of lupus erythematosus, Western medicine mostly uses high-dose steroid corticosteroids (abbreviated as hormones) and immunosuppressants, which can control the disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/357A61P19/04A61P17/00A61P37/02
Inventor 龚秋燕潘梅
Owner GUILIN PHARMA
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