Acetyl tanshinol freeze-dried powder injection and preparation method thereof

A technology of freeze-dried powder injection and acetyldanshen, which is applied in the field of medicine, can solve the problems of poor stability and low solubility of acetyldanshensu, and achieve the effects of improved stability, excellent appearance, and small weight loss on drying

Active Publication Date: 2015-04-01
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a kind of acetyldanshensu freeze-dried powder injection and its preparation method for the problem of low solubility and poor stability of acetyldanshensu

Method used

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  • Acetyl tanshinol freeze-dried powder injection and preparation method thereof
  • Acetyl tanshinol freeze-dried powder injection and preparation method thereof
  • Acetyl tanshinol freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the influence of cosolvent on the solubility of acetyldanshensu

[0023] In order to improve the solubility of acetyldanshensu and ensure its stability, it is necessary to add certain co-solvents in water, such as ethanol, PEG-400, 1,2-propylene glycol, sodium bicarbonate, disodium hydrogen phosphate, sodium citrate, spit One or more of Wen-80 and poloxamer.

[0024]

[0025] The results showed that the selected co-solvents could increase the solubility of acetyldanshensu to different degrees, and the content remained basically stable.

Embodiment 2

[0026] Embodiment 2: The influence of pH on the stability of acetyldanshensu

[0027] Weigh an appropriate amount of acetyldanshensu, add 20% ethanol and 15% PEG-400 to aid dissolution, and prepare a 50 mg / mL acetyldanshensu solution with water for injection, and use 0.1moL / L hydrochloric acid or 0.1moL / L sodium hydroxide solution respectively Adjust the pH to 3.5, 4.5, 5.0, 5.5, 6.0, 6.5, 7.5, and 8.5, and investigate the changes in the content of acetyldanshensu after being placed under different conditions for different periods of time. The results are shown in Table 2.

[0028]

[0029] The results showed that as the pH of the solution increased, the degradation of acetyldanshensu became faster and the color of the solution became darker. Combined with the pH range (4.0-9.0) required for intravenous injection, the pH range of the acetyldanshensu solution is selected to be 4.0-6.0, preferably 4.5-5.5.

Embodiment 3

[0030] Example 3: Effect of excipients on product formability

[0031] Choose 10% sodium citrate as co-solvent to prepare 15% acetyldanshensu solution. Mannitol and dextran were selected as excipients, and the following prescription was designed for lyophilization. The results are shown in Table 3.

[0032]

[0033] According to the results of the prescription screening test, when the prescription contains 10% sodium citrate, without adding excipients, it can be prepared into white fine and loose block freeze-dried products with complete skeleton and good formability, with uniform texture and good resolubility. Well, dissolve immediately (within 10 seconds) after adding water and shaking. Considering the cost saving of freeze-drying, when the prescription contains sodium citrate, there is no need to use excipients.

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PUM

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Abstract

The invention discloses an acetyl tanshinol freeze-dried powder injection which comprises acetyl tanshinol, a cosolvent and a complexing agent in a mass ratio of (1-30): (2-40): (0.01-0.1). According to the acetyl tanshinol freeze-dried powder injection disclosed by the invention, the solubility of acetyl tanshinol in water is improved by 10-100 times, the stability of acetyl tanshinol is greatly improved, and the acetyl tanshinol freeze-dried powder injection is quick and simple to rehydrate and easy to be dissolved by a common solvent and can coexist with a compatibility solution for a relatively long time, so that the problems of reduced curative effect caused by drug degradation and potential safety hazard caused by increase of related substances to drug use of patients are solved.

Description

technical field [0001] The invention relates to an acetyldanshensu freeze-dried powder injection capable of preventing and treating cardiovascular and cerebrovascular diseases and their complications and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Acetyldanshensu is the acetylated derivative of the three hydroxyl groups in the Danshensu structure, and its chemical name is: R -(+)-3-(3,4-diacetoxyphenyl)-2-acetoxypropionic acid, the chemical structure is: [0003] [0004] The molecular formula is: C 15 h 16 o 8 Molecular weight: 324.08. [0005] Compared with danshensu, acetyldanshensu has the advantages of increasing fat solubility, changing absorption performance, relatively increasing stability, and improving drug efficacy. In addition, it has obvious effects on preventing and treating cardiovascular and cerebrovascular diseases and their complications. Therefore, acetyldanshensu It is imminent to deve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/222A61P9/00
Inventor 文爱东翁琰奚苗苗王艳华卫国段佳林郭超朱艳荣关月殷英
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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