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Tirofiban hydrochloride freeze-dried powder injection preparation and preparation method thereof

A technology of tirofiban and freeze-dried powder injection, which is applied in the field of medicine, can solve the problems of lactose without injection specifications, unproven safety, and hidden dangers of medication for patients, and achieve improved solubility, guaranteed safety, and convenient transportation Effect

Active Publication Date: 2010-06-02
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] ① Visible foreign matter is better than excipients such as mannitol and dextran, but it has not fundamentally solved the problem of visible foreign matter. Experiments have shown that there are still a few products with visible foreign matter that are unqualified after reconstitution, which brings certain hidden dangers to patients.
Solubility experiments have shown that within this range, the solubility of tirofiban hydrochloride is the highest. Above or below this range, the solubility will become smaller. However, in such a low pH range, injection administration has certain hidden dangers to the human body. As we all know, intravenous The closer the pH value of the administration injection is to the pH 7.4 of human blood, the safer it is for the human body. The pH of the patented liquid is far lower than the pH of blood, and there are certain unsafe factors
[0007] ③The excipient used is lactose, but lactose does not currently have specifications for injection. As an excipient for injection, the dosage is large, and its safety has not been proven, posing a safety hazard

Method used

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  • Tirofiban hydrochloride freeze-dried powder injection preparation and preparation method thereof
  • Tirofiban hydrochloride freeze-dried powder injection preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Tirofiban hydrochloride (calculated as tirofiban) 1 serving

[0038] Polyethylene glycol 4000 0.5 part

[0039] Mannitol 10 servings

[0040] Sodium hydroxide solution (0.05mol / l) to adjust pH to 2.0

[0041] Preparation Process:

[0042] (1) Weigh tirofiban hydrochloride and polyethylene glycol 4000 of recipe quantity, dissolve in 30 ℃ of ethanol, 40 ℃ of rotary evaporations, prepare solid dispersion, add solid dispersion to water for injection, stir to dissolve, then Add mannitol, stir to dissolve, adjust the pH to 2.0 with sodium hydroxide solution, then filter and sterilize the medicinal liquid through a 0.22 μm microporous filter membrane, and fill the filtrate into a vial after passing the test, and then half stopper, Put in freeze-drying box.

[0043] (2) Turn on the freeze dryer to pre-freeze the product, reduce the temperature of the product to about -35°C at 2°C / min, maintain this temperature for 9 hours, and after the product is completely frozen, turn on...

Embodiment 2

[0046] Tirofiban hydrochloride (calculated as tirofiban) 1 serving

[0047] Povidone k30 5 servings

[0048] Dextran 40 0.5 parts

[0049] Potassium hydroxide solution (0.05mol / l) to adjust pH to 7.0

[0050] Preparation Process:

[0051] (1) Weigh tirofiban hydrochloride and povidone k30 of recipe quantity, dissolve in 75 ℃ of ethanol, 80 ℃ of rotary evaporations, prepare solid dispersion, add solid dispersion to water for injection, stir to dissolve, then add Dextran 40, stir to dissolve, adjust the pH to 7.0 with potassium hydroxide solution, then filter and sterilize the medicinal liquid through a 0.22 μm microporous membrane, and fill the filtrate into a vial after passing the test, then half stopper, put into the freeze-drying box.

[0052] (2) Turn on the lyophilizer to pre-freeze the product, reduce the temperature of the product to below about -60°C at 0.5°C / min, and keep this temperature for about 3 hours. After the product is completely frozen, start vacuuming for...

Embodiment 3

[0055] Tirofiban hydrochloride (calculated as tirofiban) 1 serving

[0056] 1 part succinic acid

[0057] 1 part sodium chloride

[0058] Sodium hydroxide solution (0.05mol / l) to adjust pH to 8.0

[0059] Preparation Process:

[0060] (1) Weigh tirofiban hydrochloride and succinic acid of the recipe quantity, dissolve in 40°C 75% ethanol, rotate at 55°C to prepare a solid dispersion, add the solid dispersion to water for injection, stir to dissolve, then add Sodium chloride, stir to dissolve, adjust the pH to 8.0 with sodium hydroxide solution, then filter and sterilize the medicinal liquid through a 0.22 μm microporous membrane, and fill the filtrate into a vial after passing the test, and then half stopper, Put in freeze-drying box.

[0061] (2) Turn on the lyophilizer to pre-freeze the product, reduce the temperature of the product to about -50°C at 3°C / min, and maintain this temperature for about 4 hours. After the product is completely frozen, start vacuuming for free...

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Abstract

The invention relates to a tirofiban hydrochloride freeze-dried powder injection preparation and a preparation method thereof. The tirofiban hydrochloride freeze-dried powder injection preparation produced by a freeze-dried technology of the invention greatly enhances solubility of tirofiban hydrochloride; and since the pH of redissolved liquid medicine is within the range of 2.0-8.0 and visible particles and particulate matter satisfy the requirement of the pharmacopeia, the safety of medicine is greatly improved. The tirofiban hydrochloride freeze-dried powder injection preparation has simple preparation, controllable quality, stable physical and chemical properties and safe and effective use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tirofiban hydrochloride freeze-dried powder injection preparation and a preparation method thereof. Background technique [0002] Tirofiban (English name Tirofibon) is a non-titanium platelet glycoprotein GP IIb / IIIa receptor antagonist with anti-platelet aggregation. Its chemical name is: N-(n-butylsulfonyl)- O-[4-(4-Piperidinyl)butyl]-L-tyrosine hydrochloride monohydrate. Tirofiban hydrochloride is used for the treatment of patients with acute coronary syndrome (unstable angina or non-Q-wave myocardial infarction), and is also suitable for patients with coronary ischemic syndrome undergoing coronary angioplasty or intracoronary atherosclerosis block resection. Tirofiban hydrochloride reduced the incidence of the composite endpoint of death, myocardial infarction, and refractory myocardial ischemia / revascularization. [0003] At present, the dosage forms of tir...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4465A61K47/34A61K47/32A61K47/28A61K47/26A61K47/18A61K47/12A61P9/10A61K47/10
Inventor 赵志全郝贵周姜斌
Owner LUNAN PHARMA GROUP CORPORATION
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