Thymalfasin crystal and pharmaceutical composition thereof

A thymus method and composition technology, applied in the field of medicine, can solve the problems of easy production of impurities, unqualified quality, low bioavailability, etc., achieve good stability and solubility, ease the blood drug concentration curve, and bioavailability Improved effect

Active Publication Date: 2016-07-13
广东泽盛药业有限公司
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AI Technical Summary

Problems solved by technology

[0006] The Chinese patent application number 201310737572.3 discloses a freeze-dried pharmaceutical composition containing thymusfasin and its preparation method. Every 1000 freeze-dried injections use thymusfasin 1.6g, 20% mannitol injection 250ml, and chlorogenic acid 10g , 100ml of 0.1mol / L sodium phosphate buffer solution, fixed to 1000ml with water for injection, the present invention injects thymofasin and chlorogenic acid at the same time when studying chlorogenic acid and finds that the vascular irritation is greatly reduced, and simultaneously chlorogenic acid Preparation of lyophilized preparations together with thymusfasin can speed up the reconstitution speed of the drug, which is beneficial to the use of lyophilized preparations, but the stability of the thymusfasin solution in this application is not good, and the stability is poor, and it is easy to produce Impurities
[0007] The Chinese patent application number 201210052708.2 discloses a thymus method new liposome agent for injection and its preparation method. Sucrose ester and pharmaceutically acceptable carrier are made, and described carrier is preferably mannitol and trehalose, although the liposome injection of this invention has good lipid stability, liposome will not be due to fusion, ice crystal during freezing process. etc. rupture, improve the solubility to a certain extent, improve the quality of the preparation product, and reduce the toxic and side effects, but the preparation process of this method is complicated, the test conditions are strict, and it is not suitable for industrial production.
[0008] At present, the stability of Thymus Faxin freeze-dried powder preparations mostly considers the adjustment of pH or excipients. Although its stability has been improved to a certain extent, it still cannot meet the stability requirements of injections after long-term storage, and the preparation process is complicated. and low bioavailability; the quality of the solution is unstable during the preparation process, and degradation reactions are prone to occur, the freeze-drying process of the product is difficult to control, and the finished product often has problems such as poor appearance and unqualified quality

Method used

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  • Thymalfasin crystal and pharmaceutical composition thereof
  • Thymalfasin crystal and pharmaceutical composition thereof
  • Thymalfasin crystal and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation method of the new crystal of embodiment 1 thymus method:

[0040] (1) thymus fasin is dissolved in the aqueous solution mixed with methylene chloride and ethyl bromide, the volume ratio of methylene chloride and ethyl bromide is 2:11, the total mass fraction of methylene chloride and ethyl bromide is 50%, the solution The pH value is 7, and the temperature is 25°C;

[0041] (2) Stir the above solution to cool down, the stirring rate is 5rmp, the stirring time is 45min, cool down to -40°C, the cooling rate is 1.5°C / h, and stand for 10h;

[0042] (3) After washing, filtering, and drying, the moisture content after drying is 3.9%, and the thymus method new crystals are obtained.

[0043] The X-ray powder diffraction spectrum that the obtained thymus method uses Cu-Kα ray measurement to obtain is as follows figure 1 shown.

Embodiment 2

[0044] The preparation method of the new crystal of embodiment 2 thymus method

[0045] (1) Thymofasin is dissolved in the aqueous solution mixed with bromoethane, the volume ratio of dichloromethane to bromoethane is 2:13, the total mass fraction of dichloromethane and bromoethane is 52%, the pH value of the solution 7. The temperature is 25°C;

[0046] (2) Stir the above solution to cool down, the stirring rate is 4rmp, the stirring time is 40min, cool down to -20°C, the cooling rate is 1.0°C / h, and stand for 7h;

[0047] (3) After washing, filtering and drying, the moisture content after drying is 3.0%, and the thymus method new crystals are obtained.

[0048] The X-ray powder diffraction spectrum obtained by measuring the thymus method using Cu-Kα rays is basically consistent with that of Example 1.

Embodiment 3

[0049] The preparation method of the new crystal of embodiment 3 thymus method

[0050] (1) thymus fasin is dissolved in the aqueous solution mixed with bromoethane, the volume ratio of dichloromethane to bromoethane is 5:11, the total mass fraction of dichloromethane and bromoethane is 60%, the pH value of the solution 6. The temperature is 15°C;

[0051] (2) Stir the above solution to cool down, the stirring rate is 2rmp, the stirring time is 30min, cool down to -40°C, the cooling rate is 0.5°C / h, and stand for 5h;

[0052] (3) After washing, filtering and drying, the moisture content after drying is 4.9%, and the thymus method new crystal is obtained.

[0053] The X-ray powder diffraction spectrum obtained by measuring the thymus method using Cu-Kα rays is basically consistent with that of Example 1.

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Abstract

The invention belongs to the technical field of medicine and particularly relates to a thymalfasin crystal and a pharmaceutical composition thereof.An X-ray powder diffraction pattern obtained by Cu-K alpha ray measurement of the thymalfasin crystal is as shown in the figure 1.The pharmaceutical composition of the thymalfasin crystal is freeze-dried powder injection which is prepared from, by weight, 1-2 parts of the thymalfasin crystal, 45-70 parts of mannitol, 0.1-0.5 part of monosodium phosphate, 2.6-3.5 parts of sodium hydrogen phosphate and 100-200ml of tert-butyl alcohol.The thymalfasin crystal is high in stability and solubility and less prone to deterioration in long-time storage and has a gradual blood concentration curve, and bioavailability is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new thymus crystal and a pharmaceutical composition thereof. Background technique [0002] The amino acid sequence of thymosin (also known as thymosin α1, English name Thymosin α1) is: N-Acety1-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, molecular formula C 129 h 215 N 33 o 35 , with a molecular weight of 3180.280. Thymosin is a protein and polypeptide hormone produced by animal thymus. It mainly exists in thymus epithelial cells and widely exists in spleen, lung, kidney, brain and other tissues and organs. It has high homology. It is clinically used in my country. The application has a history of more than 20 years. Thymofaxin is a high-end product among thymosin peptides. It is the main bioactive component of thymosin and is an important immunoregulatory substance in the human body. It c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575C07K1/36C07K1/34C07K1/30A61K38/22A61K9/19A61P31/14A61P31/20A61P1/16A61P35/00A61P37/04A61P31/18
CPCA61K9/19A61K38/00A61K47/26C07K14/57581
Inventor 钟正明
Owner 广东泽盛药业有限公司
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