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Thymalfasin liposome preparation for injecting

A new technology of liposome preparation and thymus method, which is applied in the field of medicine, can solve the problems of unspecified mannitol stabilizer scheme and test data, cumbersome preparation process of thymosin injection, and unsuitability for industrial production, etc., so as to improve bioavailability Degree, improve the quality of preparation products, increase the effect of retention time

Inactive Publication Date: 2012-07-18
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The literature does not indicate the protocol and test data of mannitol in combination with other polyols as a stabilizer
At the same time, literature data show that, in the 30-day stability study using the protocol described in the literature, the content of thymofasin (thymosin α1) decreased greatly (related substances increased), and the validity period of thymofaxin preparations is generally 2 years. It is foreseeable that within the period of validity, the scheme of this document may not meet the indicators under the relevant substances and contents newly stipulated in the 2010 version of the Thymus Law
[0005] Patent CN1840177A discloses a Thymusfasin Injection and its preparation method, which contains Thymusfasin, pharmaceutical excipients and water for injection, with a pH value of 5.0-7.0, but the injection made by the conventional method is unstable and can be sterilized at high temperature It is also easy to inactivate the drug
CN1398636A discloses a new combination medicine preparation of thymus method and its preparation method, which is made of the following raw materials in weight ratio: thymosin 1-10, reduced glutathione 2-120, and other pharmaceutically acceptable excipients , including sodium sulfite, sodium chloride and water for injection, the preparations made by this method have deviations in stability and low bioavailability
CN101934068A discloses a preparation method of thymosin injection. The preparation process of this method is too cumbersome and the biological activity is poor
CN102247319A discloses a new medicinal composition containing thymus and its preparation method, which has deviation in stability and low bioavailability
CN101766807A discloses a thymus method new microsphere injection packaging preparation, which consists of thymus method new PLGA slow-release microspheres and injection solvent and thickener, protective agent, pH regulator, isotonic and isotonic regulator, solubilizer, Composed of antioxidants, local pain relievers, and water for injection, the preparation process of this method is too cumbersome and the cost is too high, so it is not suitable for industrial production
These preparations all have the above-mentioned defects, such as insufficient stability

Method used

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  • Thymalfasin liposome preparation for injecting
  • Thymalfasin liposome preparation for injecting
  • Thymalfasin liposome preparation for injecting

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preparation example Construction

[0068] On the other hand, the present invention also provides a preparation method of thymus method new liposome preparation for injection, specifically comprising the following preparation steps:

[0069] (1) Put cholesterol, egg yolk lecithin, phosphatidylinositol and sucrose ester in a pear-shaped bottle, add an organic solvent, heat and stir to dissolve, then remove the organic solvent under reduced pressure on a rotary evaporator, and form on the bottle wall Uniform and transparent phospholipid film;

[0070] (2) Under the protection of nitrogen, add thymofaxin aqueous solution into the bottle and stir to elute the phospholipid membrane and fully swell and hydrate it. After the hydration is complete, do gradient homogenization at 100bar to 600bar for 4 to 6 times, 0.22μm The new liposome of the thymus method is obtained by filtering through a pore filter membrane;

[0071] (3) Under sterile conditions, dissolve the prescribed amount of trehalose and mannitol in water for...

Embodiment 1

[0078] The preparation of embodiment 1 injection thymus method new liposome preparation

[0079] The components and weights of the raw and auxiliary materials used are as follows:

[0080]

[0081]

[0082] The new liposome preparation of thymus method for injection is prepared by preparation process:

[0083] (1) 60g cholesterol, 180g egg yolk lecithin, 30g phosphatidylinositol and 20g sucrose ester S15 are placed in a pear-shaped bottle, added to 10000ml chloroform, heated and stirred to make it dissolve, and then the chloroform is removed under reduced pressure on a rotary evaporator, Form a uniform and transparent phospholipid film on the bottle wall;

[0084] (2) Under the protection of nitrogen, add 1.6g of thymus fasin dissolved in 500ml of water for injection into the bottle, stir to elute the phospholipid membrane and fully swell and hydrate it. Massage 4 to 6 times, and filter through a 0.22 μm microporous membrane to obtain thymofaxin liposomes;

[0085] ...

Embodiment 2

[0086] The preparation of embodiment 2 thymus method new liposome preparations for injection

[0087] The components and weights of the raw and auxiliary materials used are as follows:

[0088]

[0089] The new liposome preparation of thymus method for injection is prepared by preparation process:

[0090] (1) 70g cholesterol, 220g egg yolk lecithin, 40g phosphatidylinositol and 30g sucrose ester S15 are placed in a pear-shaped bottle, added to 10000ml chloroform, heated and stirred to make it dissolve, and then the chloroform is removed under reduced pressure on a rotary evaporator, Form a uniform and transparent phospholipid film on the bottle wall;

[0091] (2) Under the protection of nitrogen, add 1.6g of thymus fasin dissolved in 500ml of water for injection into the bottle, stir to elute the phospholipid membrane and fully swell and hydrate it. Massage 4 to 6 times, and filter through a 0.22 μm microporous membrane to obtain thymofaxin liposomes;

[0092] (3) Und...

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Abstract

The invention discloses a thymalfasin liposome preparation for injecting and a preparation method thereof. The thymalfasin liposome preparation for injecting is prepared from thymalfasin, cholesterol, egg yolk lecithin, phosphatidyl inositol, sucrose ester and a pharmaceutically-acceptable carrier in a specific weight ratio, wherein the carrier is preferably mannitol and fucose. A liposome injection disclosed by the invention has high preparation stability, a liposome is prevented from cracking due to fusion, ice crystals and the like in a cooling process, and the liposome still keeps high packing rate and high stability after long-time storage. Due to the adoption of the thymalfasin liposome preparation, the solubility of thymalfasin is increased, the quality of a preparation product is improved, toxic and side effects are reduced, the retaining time of a medicament in body circulation is prolonged, the bioavailability of the medicament is increased, and a curative effect is increased remarkably; and moreover, the preparation method is simple, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a new thymus method liposome preparation for injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Thymosin α1, also known as thymosin α1, thymosin α1, its polypeptide sequence is: N-Acceyl-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr -Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn-OH, the molecular formula is: C 129 h 215 N 33 o 35 , Molecular weight: 3108.28, is the main bioactive component of thymosin, and is an important immune regulatory substance in the body. Studies have shown that thymus fasin promotes the development and differentiation of bone marrow stem cells into pro-lymphocytes and pro-lymphocytes; induces the differentiation and maturation of T lymphocytes, and further differentiates mature T cells into several different subgroups, such as killer cells a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K38/22A61K47/36A61K47/28A61K47/26A61K47/24A61P1/16A61P31/20A61P31/14A61P35/00A61P31/00A61P37/04
Inventor 陶灵刚李岱山
Owner HAINAN LINGKANG PHARMA CO LTD
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