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Compound artemisinin piperaquine pellet and preparation method thereof

A technology of compound artemisinin and piperaquine pellets, which is applied in the field of medicinal chemistry, can solve the problems of poor molding and roundness of antimalarial pellets, difficulties in the production of antimalarial drugs for children, and unstable dissolution time, etc. Solubilization, dissolution rate is not affected, good molding and roundness effect

Active Publication Date: 2012-06-06
KPC PHARM INC
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the actual production process, due to the factors of the proportion of drug components and the production process, the antimalarial pellets have poor shape and roundness, and the dissolution time is unstable. At the same time, the dissolution rate of the drug is also affected. Production of malaria drugs presents certain difficulties

Method used

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  • Compound artemisinin piperaquine pellet and preparation method thereof
  • Compound artemisinin piperaquine pellet and preparation method thereof

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preparation example Construction

[0034] The present invention also provides a preparation method of compound artemisinin-like piperaquine pellets, comprising:

[0035] Step 1. Weigh 20-100 parts by weight of artemisinin compounds, 100-500 parts by weight of piperaquine phosphate, 50-300 parts by weight of lactose, 50-300 parts by weight of microcrystalline cellulose, 10-100 parts by weight of cross-linked polymer Vinylpyrrolidone, 0-50 parts by weight of sodium carboxymethyl starch and 1-20 parts by weight of copovidone are mixed;

[0036] Step 2, dissolving 0.05-5 parts by weight of a solubilizer in water as a wetting agent, and preparing pellets by extrusion spheronization or centrifugal pelletization.

[0037] The preparation method of another kind of compound artemisinin-like piperaquine pellets provided by the present invention comprises:

[0038] Step 1. Weigh 30-60 parts by weight of artemisinin compounds, 250-450 parts by weight of piperaquine phosphate, 100-250 parts by weight of lactose, 80-260 par...

Embodiment 1

[0047] Embodiment 1: Preparation method of the present invention prepares compound artemisinin-like piperaquine pellets

[0048] 1. Prescription

[0049] Dihydroartemisinin 20g

[0050] Piperaquine Phosphate 480g

[0051] Lactose 164g

[0052] Microcrystalline Cellulose 140g

[0053] Cross-linked polyvinylpyrrolidone 10g

[0054] Copovidone 8g

[0055] Sodium Lauryl Sulfate 1g

[0056] Pure water 200g

[0057] Gastric-soluble coating powder 170g

[0058] Aspartame 2% (total weight of coating material)

[0059] 2. Preparation method

[0060] Pass the original and auxiliary materials through a 100-mesh sieve, weigh dihydroartemisinin, piperaquine phosphate, lactose, microcrystalline cellulose, cross-linked polyvinylpyrrolidone and copovidone according to the prescription amount, and then mix them evenly to obtain a mixed powder; Dialkyl sodium sulfate is dissolved in water as a wetting agent; take 15% of the mixed powder, put it in a centrifugal pelletizer, and spray i...

Embodiment 2

[0062] Embodiment 2: Preparation method of the present invention prepares compound artemisinin-like piperaquine pellets

[0063] 1. Prescription

[0064] Artesunate 40g

[0065] Piperaquine Phosphate 400g

[0066] Lactose 300g

[0067] Microcrystalline Cellulose 300g

[0068] Cross-linked polyvinylpyrrolidone 100g

[0069] Sodium carboxymethyl starch 50g

[0070] Copovidone 20g

[0071] Span-40 2g

[0072] Pure water 300g

[0073] Gastric-soluble coating powder 320g

[0074] Aspartame 1% (accounting for the total weight of coating materials)

[0075] 2. Preparation method

[0076] Pass the raw materials and auxiliary materials through a 100-mesh sieve, weigh artesunate, piperaquine phosphate, lactose, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, sodium carboxymethyl starch and copovidone according to the prescription amount and mix them evenly to obtain Mixed powder; use Span-40 dissolved in water as a wetting agent; put the mixed powder in a wet m...

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Abstract

The invention relates to the field of medicinal chemistry and discloses a compound artemisinin piperaquine pellet and a preparation method thereof. The compound artemisinin piperaquine pellet of the invention comprises 20-100 weight parts of artemisinin compound, 100-500 parts of piperaquine phosphate, 50-300 weight parts of lactose, 50-300 weight parts of microcrystalline cellulose, 10-100 weight parts of crosslinking polyvinylpyrrolidone, 0-50 weight parts of sodium carboxymethyl starch, 1-20 weight parts of polyvinylpyrrolidone and 0.05-5 weight parts of solubilizer. The compound artemisinin piperaquine pellet of the invention has regular profile, good moulding and roundness, good fluidity, stable dissolving tine, unacted dissolution and covered bitter taste, and is convenient for administration and especially suitable for children, and has wide application scope.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a compound artemisinin-like piperaquine pellet and a preparation method thereof. Background technique [0002] Malaria is a vector-borne disease caused by infection with Plasmodium parasites through the bite of Anopheles mosquitoes. Clinically, it is characterized by periodic chills, fever, headache, sweating, anemia, and splenomegaly. According to WHO (World Health Organization) report, there are 3.2 billion people living in malaria-endemic areas in 107 countries around the world, and more than 500 million people suffer from acute malaria every year, resulting in more than 3 million deaths. [0003] To effectively treat malaria, antimalarial drugs have been extensively researched by experts in the medical field. Artemisinin is a sesquiterpene lactone with a new structure extracted from the Compositae plant Artemisia annua (Armisia annua Linn) for the first time in 1971 by Ch...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K31/357A61K9/16A61K9/30A61K47/38A61P33/06
CPCY02A50/30
Inventor 廖荣郑双庆邱光升王莹曾涛王子幼李卓然
Owner KPC PHARM INC
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