Levocarnitine liposomes injection

A levocarnitine lipid and injection technology, applied in the field of medicine, can solve the problems of easy deterioration and poor resolubility of powder injections, and achieve the effects of improved stability, stable product quality, and excellent stability

Inactive Publication Date: 2010-02-03
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Aiming at the problem that the current levocarnitine solution is perishable after long-term storage and the powder injection has poor resolubility, the object of the present invention is to provide a levocarnitine liposome injection, which is encapsulated with liposomes by the pH gradient method , so as to solve the above-mentioned problems

Method used

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  • Levocarnitine liposomes injection
  • Levocarnitine liposomes injection
  • Levocarnitine liposomes injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of Levocarnitine Liposome Injection

[0049] Prescription (100 bottles): Levocarnitine 25g

[0050] Soy Lecithin 180g

[0051] Cholesterol 45g

[0052] Vitamin E 6g

[0053] Preparation Process

[0054] (1) Dissolve 180g of soybean lecithin, 45g of cholesterol and 6g of vitamin E in 1500ml of isopropanol, slowly inject 1500ml of 0.1mol / L ammonium sulfate solution under stirring, heat and stir to remove the isopropanol, and put it in an ice bath for 10 minutes of ultrasound , to obtain blank liposomes;

[0055] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in 0.9% sodium chloride solution 3000ml and dialyzes 20 hours, removes the ammonium sulfate in liposome external phase;

[0056] (3) Dissolve 25g of levocarnitine in 800ml of water, keep the dialyzed blank liposome at 60°C, slowly add the aqueous solution of levocarnitine under stirring, continue to keep warm for 20min, add 1000ml of 0.9% sodium chloride s...

Embodiment 2

[0058] Example 2 Preparation of Levocarnitine Liposome Injection

[0059] Prescription (100 bottles): Levocarnitine 50g

[0060] Soy Lecithin 250g

[0061] Cholesterol 40g

[0062] tert-Butyl p-Hydroxyanisole 5g

[0063] Preparation Process

[0064] (1) Dissolve 250g of soybean lecithin, 40g of cholesterol and 5g of tert-butyl p-hydroxyanisole in 2000ml of tert-butanol, slowly inject 2000ml of 0.05mol / L ammonium sulfate solution under stirring, heat and stir to remove tert-butanol, place Sonicate in an ice bath for 20 minutes to obtain blank liposomes;

[0065] (2) blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in 4000ml of 10% glycerol solution and dialyzed for 24 hours, removes the ammonium sulfate in the liposome external phase;

[0066] (3) 50g levocarnitine is dissolved in 2000ml water, and the blank liposome that dialyzes is incubated at 60 ℃, slowly adds the aqueous solution of levocarnitine under stirring, continues to keep...

Embodiment 3

[0068] Example 3 Preparation of Levocarnitine Liposome Injection

[0069] Prescription (100 bottles): L-Carnitine 100g

[0070] Soy Lecithin 900g

[0071] Cholesterol 600g

[0072] Vitamin E 36g

[0073] Preparation Process

[0074] (1) Dissolve 900g of soybean lecithin, 600g of cholesterol and 36g of vitamin E in 10,000ml of ethanol, slowly inject 10,000ml of 0.03mol / L ammonium sulfate solution under stirring, heat and stir to remove ethanol, put it in an ice bath and ultrasonically for 20min, and obtain blank fat plastid;

[0075] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in 5% glucose solution 15000ml and dialyzes 26 hours, removes the ammonium sulfate in liposome external phase;

[0076] (3) Dissolve 100g of levocarnitine in 5000ml of water, heat the dialyzed blank liposome at 60°C, slowly add the aqueous solution of levocarnitine under stirring, continue to keep warm for 20min, add 1000ml of 5% glucose solution and pH Value ...

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Abstract

The invention discloses levocarnitine liposomes injection, which is characterized by comprising the following active ingredients in parts by weight: 1 part of levocarnitine, 3-15 parts of soybean lecithin, 0.4-7.5 parts of cholesterol and 0.02-1 part of antioxidant, and a pharmaceutically acceptable carrier, wherein, the antioxidant is one or more of L-cysteine, thiourea, vitamin E and butylated hydroxyanisole and is most preferably the vitamin E. The invention also discloses a preferable preparation method of the levocarnitine liposomes injection, namely ammonium sulphate pH gradient method.The invention provides levocarnitine liposomes injection which has excellent stability, high entrapment rate and low leakage rate in the process of long-term storage. The acute toxicity tests, unusualtoxicity tests and heat source tests adopting the levocarnitine liposomes injection all conform to the specifications and are applicable to industrialized production.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to levocarnitine liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Levocarnitine, also known as L-carnitine, chemical name: (R)-3-carboxy-2-hydroxy-N,N,N-trimethyl-1-propylammonium hydroxide, internal salt, molecular formula: C 7 h 15 NO 3 , molecular weight: 161.20, structural formula: [0003] [0004] It is a special amino acid that widely exists in human body tissues. It is an essential nutrient for humans and animals. It is a vitamin-like nutrient, which is equivalent to vitamin B family. Studies have found that L-carnitine is a compound related to fatty acid metabolism in animals, and its basic function is to assist long-chain fatty acids to penetrate the mitochondrial inner membrane for β-oxidation. Levocarnitine is an essential nutrient whose function is closely related to the metabolism of living...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/205A61K47/28A61P1/16A61P3/02A61P7/08A61P9/00A61P9/04A61P9/06A61P9/10
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST
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