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Freeze-dried powder injection of ligustrazine phosphate for injection and preparation method thereof

A technology of ligustrazine phosphate and freeze-dried powder injection, which is applied in freeze-dried delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem that the safety of stabilizers is not fully guaranteed and affects The problems of product solubility, hygroscopicity, and poor product stability have achieved the effect of good resolubility, suitable for industrial production, and improved drug safety.

Inactive Publication Date: 2016-01-06
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] During the long-term storage of existing ligustrazine phosphate injections on the market, ligustrazine phosphate has strong hygroscopicity, and after absorbing moisture, it melts and degrades, resulting in a decrease in the content of the preparation, an increase in related substances, and a deepening of the color. The stability of this product is related to its own pH , when the pH is between 2.4 and 2.6, the stability is better, and the low or high pH can affect the solubility and hygroscopicity of the product. The existing manufacturers have added citric acid as a stabilizer in the injection, but The drug safety of the stabilizer is not fully guaranteed. At the same time, due to the need for high-temperature sterilization, the stability of the product is not good. The related substances increase significantly after sterilization, and the drug is prone to hydrolysis during storage.

Method used

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  • Freeze-dried powder injection of ligustrazine phosphate for injection and preparation method thereof
  • Freeze-dried powder injection of ligustrazine phosphate for injection and preparation method thereof
  • Freeze-dried powder injection of ligustrazine phosphate for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The formula of described ligustrazine phosphate freeze-dried powder for injection consists of:

[0029]

[0030] Its preparation method:

[0031] (1) Add the prescribed amount of water for injection into the batching tank.

[0032] (2) Weigh the prescribed amount of mannitol, add it into the batching tank, stir and dissolve, and cool down to below 25°C.

[0033] (3) Weigh the prescribed amount of Ligustrazine Phosphate into the batching tank and stir until fully dissolved, and control the pH at 2.0-3.0. If the pH>3.0, add phosphoric acid solution to adjust the pH to 2.0-3.0.

[0034] (4) Filling after sterilization and filtration

[0035] (5) Drugs are loaded into a freeze dryer and pre-frozen at -42°C for 1.5 hours, raised to -5°C for 10 hours, raised to 0°C for 2 hours, raised to 15°C for 3 hours.

[0036] (6) Capping, packaging, full inspection, and storage.

[0037]

[0038] Its preparation method:

[0039] (1) Add the prescribed amount of water for injec...

Embodiment 3

[0047]

[0048] Its preparation method:

[0049] (1) Add the prescribed amount of water for injection into the batching tank.

[0050] (2) Weigh the prescribed amount of mannitol, add it into the batching tank, stir and dissolve, and cool down to below 25°C.

[0051] (3) Weigh the prescribed amount of Ligustrazine Phosphate into the batching tank and stir until fully dissolved, and control the pH at 2.0-3.0. If the pH>3.0, add phosphoric acid solution to adjust the pH to 2.0-3.0.

[0052] (4) Filling after sterilizing and filtering.

[0053] (5) Put the drug into the freeze dryer for pre-freezing at -42°C, maintain for 1.8h, raise the medium to -5°C, maintain for 11h, raise the medium to 0°C, maintain for 2.5h, raise the medium to 15°C, and maintain for 3.5h.

[0054] (6) Capping, packaging, full inspection, and storage.

Embodiment 4

[0056]

[0057] Its preparation method:

[0058] (1) Add the prescribed amount of water for injection into the batching tank.

[0059] (2) Weigh the prescribed amount of mannitol, add it to the batching tank, stir and dissolve, and cool down to below 25°C.

[0060] (3) Weigh the prescribed amount of Ligustrazine Phosphate into the batching tank and stir until fully dissolved, and control the pH at 2.0-3.0. If the pH>3.0, add phosphoric acid solution to adjust the pH to 2.0-3.0.

[0061] (4) Filling after sterilizing and filtering.

[0062] (5) Put the drug into the lyophilizer for pre-freezing at -42°C, maintain for 1.5h, raise the medium to -5°C, maintain for 10h, raise the medium to 0°C, maintain for 2h, raise the medium to 15°C, and maintain for 3h.

[0063] (6) Capping, packaging, full inspection, and storage.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations and particularly relates to a freeze-dried powder injection of ligustrazine phosphate for injection and a preparation method thereof. The freeze-dried powder injection is prepared from ligustrazine phosphate and mannitol according to the mass ratio of 1 to 0.90-1.5. The stability of the freeze-dried powder injection is remarkably improved compared with that of liquid injections; moreover, since glycine and other substances used as stabilizers are omitted, the safety of medication is improved. The invention further provides the preparation method of the freeze-dried powder injection. According to the preparation method, mannitol is used as the excipient, phosphoric acid solution is used for regulating pH to be between 2.0 and 3.0, and therefore the stability of basic remedy is improved; acceleration tests show that within six months, the product is stable in content, related substances change a little, and therefore the storage period of the preparations is prolonged; the preparation method is simple in process and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a ligustrazine phosphate freeze-dried powder for injection and a preparation method thereof. Background technique [0002] For ischemic cerebrovascular diseases (such as cerebral insufficiency, cerebral thrombosis, cerebral embolism). After years of clinical use, the curative effect is definite, and its main mechanism of action is: this product has the effect of anti-platelet aggregation, and has a depolymerization effect on the aggregated platelets. In addition, it still has the effects of dilating small arteries, improving microcirculation and increasing cerebral blood flow, thereby producing antithrombotic and thrombolytic effects. [0003] During the long-term storage of existing ligustrazine phosphate injections on the market, ligustrazine phosphate has strong hygroscopicity, and after absorbing moisture, it melts and degrades, resulting in a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4965A61K47/26A61P9/10A61P7/02
Inventor 苗得足张光明艾全陈付杰张国明王元英黄芳生
Owner REYOUNG PHARMA
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