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Compound fluorouracil liposome oral liquid and preparation method thereof

A technology for fluorouracil and oral solution, which is applied in the field of compound fluorouracil liposome oral solution and its preparation, can solve the problems of product stability attenuation, unsatisfactory effect, long process and the like, achieve stable product quality, avoid adverse reactions, and avoid The effect of the recycling process

Active Publication Date: 2012-10-24
NORTH CHINA PHARMA COMPANY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to solve this problem, Zhang Qi, Deng Yingjie, Luo Guoan, etc. introduced a method for preparing 5-fluorouracil liposomes by a uniform design method (Journal of Peking University (Medical Edition) Vol.34 No.1Feb.2002) and a The method (Journal of Shenyang Pharmaceutical University, Volume 17, No. 2) of 5-fluorouracil liposome preparations prepared by reverse-phase evaporation in combination with freeze-thaw method, although these two methods make the encapsulation efficiency of 5-fluorouracil reach 39% and 39% respectively. 45.31%, but its effect is still not ideal
Furthermore, both of the above two preparation methods use chloroform as a solvent, the process is long, and the finished products need to be stored at 0-4°C, and the stability of the finished products decays with the prolongation of storage time

Method used

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  • Compound fluorouracil liposome oral liquid and preparation method thereof
  • Compound fluorouracil liposome oral liquid and preparation method thereof
  • Compound fluorouracil liposome oral liquid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Process prescription: fluorouracil (5-FU) 1000g, ginseng polysaccharide 2000g, distearoylphosphatidylcholine 5000g, Tween-80 3500g, oleic acid 2500g, cholesterol 3000g, povidone K30 (PVP) 2500g, butyl hydroxyl Toluene 250g, glycine 500g, add water for injection to a total volume of 250L, weigh distearoylphosphatidylcholine and 36L water for injection (80-85°C) into the colloid mill together, circulate for 10 minutes, then switch to heating In the reaction kettle, add Tween-80 and melted oleic acid and cholesterol, stir at 80°C for 20 minutes, transfer to the colloid mill, add antioxidant butyl hydroxytoluene and phosphate buffer (pH6.7 -6.8) Circulate for 15 minutes to form solution I, then transfer to the reaction kettle and keep warm at 80°C. Then weigh the PVP and 5-FU of the formula, dissolve PVP in 100L, 80°C water for injection, then add 5-FU, heat to 80°C, and then slowly add it to I under stirring to form solution II , after the dropwise addition, add the prepa...

Embodiment 2

[0022] (a) Process prescription:

[0023] Fluorouracil 0.41g, Ginseng Polysaccharide 0.66g, Distearoyl Phosphatidylcholine 1.65g, Tween-801.115g, Oleic Acid 0.825g, Cholesterol 0.66g, Povidone K300.825g, Butylated Hydroxytoluene 0.0825g, Glycine 0.0825g, water for injection to 100ml.

[0024] (b) Weigh distearoylphosphatidylcholine and 25ml of water for injection with a water temperature of 85°C and add them to the colloid mill. After circulating for 20 minutes, transfer them to the heating reaction kettle and set aside;

[0025] (c) heating and melting oleic acid and cholesterol, and stirring for 20 minutes for subsequent use;

[0026] (d) Add Tween-80 and melted oleic acid and cholesterol into the reaction kettle, stir at 85°C for 20 minutes, and transfer to the colloid mill;

[0027] (e) Add butylated hydroxytoluene to the colloid mill, add a phosphate buffer with a pH value of 8.0, and circulate for 15 minutes to form a solution I, then transfer it to the reaction kettle...

Embodiment 3

[0039] After making product according to above-mentioned embodiment 1,2 and comparative example 1,2, under the same condition, immediately measure the encapsulation efficiency of prepared liposome according to Sephadex method, (assay method and calculation method refer to ( Zhang Qi, Deng Yingjie. Freeze-thaw method to prepare 5-FU liposomes [J]. Shenyang Pharmaceutical University) method described in the literature. The experimental results are shown in Table 1.

[0040] Table 1:

[0041]

[0042] Experimental results show that the product provided by the invention has a better encapsulation effect.

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Abstract

The invention discloses compound fluorouracil liposome oral liquid and a preparation method thereof. The preparation method comprises the following steps: preparing components including fluorouracil, ginseng polysaccharides, distearoyl phosphatidylcholine, cholesterol, water and the like; weighing distearoyl phosphatidylcholine, adding water, filling the mixture in a colloid mill, circulating for10 minutes, and obtaining a milled mixture for later use; heating oleic acid and cholesterol to melt the oleic acid and cholesterol; adding Tween-80 and molten oleic acid and cholesterol into a reaction kettle, and transferring the mixture to the colloid mill; adding butylated hydroxytoluene into the colloid mill, transferring the mixture to the reaction kettle and keeping the temperature at 80 to 85 DEG C; adding polyvidone and fluorouracil to prepare solution II; and adding ginseng polysaccharides and glycocoll, stirring for 1 to 2 hours, cooling to room temperature, and fixing a total volume. The product provided by the invention is stable in quality; the liposome encapsulation rate is high; and the product can be stored at normal temperature.

Description

technical field [0001] The invention relates to medicine for human use and a preparation method thereof, in particular to a compound fluorouracil liposome oral solution for treating various cancers and a preparation method thereof. Background technique [0002] Fluorouracil (molecular formula: C 4 h 3 FN 2 o 2 ), is the most widely used anti-metabolite drug in the body. It is first converted into 5-fluoro-2-deoxyuridine nucleotide in vivo, which inhibits thymidine nucleotide synthetase and blocks the transformation of deoxyuridine nucleotide For thymine nucleotides, thereby inhibiting DNA biosynthesis. In addition, it can penetrate into RNA and inhibit RNA synthesis by preventing the incorporation of uracil and orotic acid into RNA. It is mainly used clinically for the treatment of digestive tract cancer (colon cancer, rectal cancer, gastric cancer), breast cancer, primary liver cancer, etc., and also has certain curative effects on ovarian cancer, cervical cancer, chor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/715A61K47/34A61P35/00A61K31/513A61K47/26
Inventor 梁凤林李晓斌王志良刘英华刘书睿赵霞范永刚杨景华路玉锋
Owner NORTH CHINA PHARMA COMPANY
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