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Lipid formulation of nolatrexed dihydrochloride and its preparation method

A technology of lolatrexex hydrochloride and liposomes, which is applied in the direction of liposome delivery, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problems of inconvenient clinical application of lolatrexex hydrochloride and improve the therapeutic effect. index effect

Inactive Publication Date: 2007-11-14
BEIJING KONRUNS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This medication regimen brings a lot of inconvenience to the clinical application of lolatrexel hydrochloride

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Capsule formula 1 (each capsule contains 50mg of lolatrexel hydrochloride)

[0047] Lolatrexel Hydrochloride 10g

[0048] Starch 40g

[0049] Carboxymethylcellulose 2.5g

[0050] Magnesium Stearate 250mg

[0051] Preparation

[0052] Add 10 g of lolatrexil hydrochloride and 40 g of starch, pass through a 120-mesh sieve, and mix well. Add 8% starch slurry to make the mixed powder into a soft material, pass through a 20-mesh nylon sieve, granulate, and dry below 60°C. Add 2.5g of carboxymethylcellulose and 250mg of magnesium stearate, pass through a 20-mesh sieve to make the whole grain uniform, and pack into capsules. Each capsule weighs 250mg.

Embodiment 2

[0054] Capsule formula 2 (each capsule contains 200mg of lolatrexel hydrochloride)

[0055] Lolatrexel Hydrochloride 20g

[0056] Starch 20g

[0057] Carboxymethylcellulose 1g

[0058] Magnesium Stearate 100mg

[0059] Preparation

[0060] Add 20 g of lolatrexole hydrochloride and 20 g of starch, pass through a 120-mesh sieve, and mix well. Add 8% starch slurry to make the mixed powder into a soft material, pass through a 20-mesh nylon sieve, granulate, and dry below 60°C. Add 1g of carboxymethyl cellulose and 100mg of magnesium stearate, pass through a 20-mesh sieve to make the whole grain uniform, and pack into capsules. Each capsule weighs 400mg.

Embodiment 3

[0062] Freeze-dried powder formula one

[0063] Lolatrexel Hydrochloride 10g

[0064] Mannitol 0.5g

[0065] Water for injection 200ml

[0066] Preparation

[0067] Add 10 g of lolatrexil hydrochloride and 0.5 g of mannitol into a beaker with 120 ml of water for injection, stir and dissolve, add 0.1% activated carbon for decolorization treatment, add water for injection to constant volume, and then use a 0.22 μm microporous filter membrane to positively remove Bacteria, aliquoted and freeze-dried.

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Abstract

The invention discloses a nolatrexed dihydrochloride liposome composition, which comprises 10-20 weights of nolatrexed dihydrochloride, 20-40 weight parts of soybean lecithin, 2-5 weight parts of dipalmitoyl glycerylphosphatide, and 5-20 weight parts of cholesterol.

Description

technical field [0001] The invention relates to a liposome preparation of nolatrexex hydrochloride and a preparation method thereof. Background technique [0002] Lolatrex is a thymidylate synthase (Thymidylate Synthase, TS) inhibitor. Its chemical name is 2-amino-6-methyl-5-(4-pyridylmercapto)-4(1H)-quinazolinone. The clinical application of lolatrex is its dihydrochloride compound. Lolatrex is an anti-tumor drug with a new structure, which was first designed and developed by Agouron Company of the United States based on the crystal structure of TS and using computer-aided drug design technology. It is mainly used in the treatment of liver cancer, colorectal cancer, lung cancer, prostate cancer, pancreatic cancer and head and neck tumors. Among them, the treatment of liver cancer is in the phase III research stage. [0003] Nolatrexex can be given intravenously or orally. The main adverse reactions in clinical trials were pale complexion at the infusion site, edema, ga...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61K9/127A61K9/48A61K9/19A61P35/00
Inventor 王锡娟
Owner BEIJING KONRUNS PHARM CO LTD
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