Dihydroartemisinin tablet and preparation method thereof

A technology for dihydroartemisinin and tablets, which is applied in the field of medicine, can solve the problems of great influence on solubility, difficulty and limitation of dihydroartemisinin, and achieves the guarantee of safety and effectiveness, low impurity content, and dissolution rate. high effect

Active Publication Date: 2018-05-04
KPC PHARM INC
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the above method, the raw material dihydroartemisinin is ground by grinding, but due to the nature of dihydroartemisinin, it is very difficult to grind finely, and heat and impurities will be generated during the grinding process, which will affect the safety of the product
Dihydroartemisinin is insoluble in water, and its particle size has a great influence on the solubility. The raw material of dihydroartemisinin is simply passed through a 120-mesh sieve, and the processed tablets are not fully dissolved within the specified time. Although they comply with the "Chinese Pharmacopoeia "Regulations, 30 minutes of dissoluti

Method used

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  • Dihydroartemisinin tablet and preparation method thereof
  • Dihydroartemisinin tablet and preparation method thereof
  • Dihydroartemisinin tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
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Example Embodiment

[0039] Example 1: The effect of dry granulation, wet granulation and direct compression of whole powder on the quality of dihydroartemisinin tablets

[0040] 1. Test method

[0041] Weigh the original and auxiliary materials of the prescription to make dihydroartemisinin (D 90 <100μm) contains 10%, lactose (spray dried lactose monohydrate) contains 35%, microcrystalline cellulose (102 or 112) contains 35%, sodium carboxymethyl starch contains 15%, sodium lauryl sulfate contains 1.5% , Polyvinylpyrrolidone contains 3%, magnesium stearate contains 0.5%, and all auxiliary materials pass through an 80-mesh sieve. Weigh 4 parts, and granulate them according to the following methods: the first part is dry-granulated at a pressure of 60kg, and the water outlet on the pressure roller is kept stable under 10℃ during the granulation process; the second part is made with 75% ethanol. The solvent is wet granulated, and the wet granules are dried at 45° C.; the third part is 50% ethanol as the...

Example Embodiment

[0056] Example 2: The effect of the particle size of dihydroartemisinin on the dissolution of tablets

[0057] 1. Test method

[0058] Weigh the original and auxiliary materials of the prescription amount respectively, so that dihydroartemisinin contains 10%, lactose (spray dried lactose monohydrate) contains 35%, microcrystalline cellulose (102 or 112) contains 35%, and sodium carboxymethyl starch contains 15%, sodium lauryl sulfate 1.5%, polyvinylpyrrolidone 3%, and magnesium stearate 0.5%. Weigh a total of 5 parts, and process the raw material dihydroartemisinin according to the following methods: the first raw material is not sieved, and the second raw material is passed through a 120-mesh sieve (D 90 90 90 90 <30μm, all auxiliary materials pass through 80 mesh sieve. After mixing, dry granulation was carried out at a pressure of 60 kg, and then tableting was carried out after granulation. The parameters of granulation and tableting were consistent. Take the compressed dihydr...

Example Embodiment

[0066] Example 3: The influence of lactose and microcrystalline cellulose types on the quality of dihydroartemisinin tablets

[0067] 1. Test method

[0068] Weigh the original and auxiliary materials of the prescription to make dihydroartemisinin (D 90 <100μm) contains 10%, lactose (spray-dried lactose monohydrate, Tablettose 80) contains 35%, microcrystalline cellulose (101, 102 or 112) contains 35%, sodium carboxymethyl starch contains 15%, dodecyl Sodium sulfate contains 1.5%, polyvinylpyrrolidone contains 3%, magnesium stearate contains 0.5%, and all auxiliary materials pass through an 80-mesh sieve. Weigh a total of 5 parts, the first part is directly compressed with spray-dried lactose monohydrate, microcrystalline cellulose 101 and other materials in the formulation; the second part is spray-dried lactose monohydrate, microcrystalline cellulose 102 and the formulation The other materials are mixed and directly pressed into tablets; the third part is spray-dried lactose mon...

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Abstract

The invention belongs to the technical field of medicines, and discloses a dihydroartemisinin tablet and a preparation method thereof. The dihydroartemisinin tablet comprises dihydroartemisinin, spray-dried lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch, sodium lauryl sulfate, polyvinylpyrrolidone and magnesium stearate, wherein the microcrystalline cellulose is microcrystalline cellulose 102 or microcrystalline cellulose 112. The preparation method of the dihydroartemisinin tablet comprises the following steps: mixing the dihydroartemisinin, the spray-dried lactose monohydrate, the microcrystalline cellulose, the sodium carboxymethyl starch, the sodium lauryl sulfate, the polyvinylpyrrolidone and the magnesium stearate, and then directly tableting. Compared with the prior art, the dihydroartemisinin tablet prepared according to the preparation method provided by the invention has the advantages as follows: the dihydroartemisinin tablet is low in impuritycontent, high in dissolution rate and good in stability, and the safety and the effectiveness of the dihydroartemisinin tablet can be better guaranteed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a dihydroartemisinin tablet and a preparation method thereof. Background technique [0002] Dihydroartemisinin is a derivative of artemisinin, an effective antimalarial monomer extracted from Herba Artemisiae Annuae, and its chemical name is (3R, 5aS, 6R, 8aS, 9R, 12S, 12aR )-octahydro-3,6,9-trimethyl-3,12-oxo-12H-pyrano[4,3-j]-1,2-benzodisepin-10(3H)- Alcohol, molecular formula C 15 h 24 o 5 , the molecular weight is 284.35, and the structural formula is as follows. [0003] [0004] With the deepening of research on dihydroartemisinin, it is found that its biological activity presents diversity. Studies have shown that dihydroartemisinin has anti-tumor, anti-inflammation, anti-fibrosis, anti-arrhythmia, anti-fungal, anti-pregnancy, anti-arrhythmia, anti-parasite and radiosensitization effects in addition to its definite antimalarial activity. It can treat ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/366A61K47/26A61K47/38A61P33/06A61P35/00A61P29/00A61P9/06A61P31/10A61P33/00A61P3/10A61P11/00A61P31/06A61P37/02
CPCA61K9/2018A61K9/2054A61K31/366Y02A50/30
Inventor 王洪静黄照昌曾涛方芳文纳张敏李
Owner KPC PHARM INC
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