A stable torasemide injection and its preparation method

A technology of torasemide and injection, which is applied in blood diseases, pharmaceutical formulations, extracellular fluid diseases, etc., and can solve problems such as poor stability, slow dissolution rate, and large growth of substances

Inactive Publication Date: 2007-08-01
YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Under the existing prescription and production process, torasemide injection uses phosphate or acetate buffer salt system to dissolve torasemide, the dissolution rate is slow, and the dosing time exceeds 2 hours; sodium thiosulfate is used , Sodium sulfite, vitamin C, etc. are used as antioxidants. After potting, the related substances increase greatly before and after sterilization, and the stability is not good. At the same time, during the accelerated test and long-term test process, the related substances also grow faster.

Method used

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  • A stable torasemide injection and its preparation method

Examples

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Comparison scheme
Effect test

example 1

[0019] Prescription 1

[0020] Preparation process: Measure a certain amount of water for injection, add torasemide after adding a solubilizer, add a stabilizer after the dissolution is complete, add water to the full amount, stir evenly, add activated carbon for high-temperature adsorption for 30 minutes, decarbonize and filter, add medicine with Alkali (NaOH, sodium acetate buffer solution), adjust the pH to 9.5, sterilize and filter, fill after passing the intermediate inspection, sterilize, pack and store.

[0021] Stability test is carried out on the samples prepared by prescription 1, prescription 2 and prescription 3, and the results of related substances are shown in the table

[0022] 1. High temperature 60℃ influence factor test

[0023] relative substance%

[0024] 2. Accelerated 40°C test

[0025] relative substance%

[0026] The results showed that the stability of the injection after adding stabilizers and solubilizers was sig...

example 2

[0028] Prescription 4

[0029] Preparation process: Measure a certain amount of water for injection, add propylene glycol, add torasemide, add tromethamine after the dissolution is complete, replenish water to the full amount, stir evenly, add activated carbon for high temperature adsorption for 30 minutes, decarbonize and filter, add NaOH Gradually adjust the pH to 4.5, 7.0, and 9.0 for sterilizing and filtering, and after passing the intermediate inspection, fill, sterilize, and pack for storage.

[0030] Comparing the growth degree of related substances before and after sterilization of injections with different pH values

[0031]

[0032] The results show that when the pH value of the injection is greater than 9.0, there is almost no growth of related substances before and after sterilization, and the stability is significantly better than that of the injection with a pH value of less than 9.0.

example 3

[0034] Prescription 5

[0035] Preparation process: Measure a certain amount of water for injection, add propylene glycol, add torasemide, add tromethamine after the dissolution is complete, replenish water to the full amount, stir evenly, add activated carbon for high temperature adsorption for 30 minutes, decarbonize and filter, add NaOH Gradually adjust the pH to 4.5, 7.0, and 9.0 for sterilizing and filtering, and after passing the intermediate inspection, fill, sterilize, and pack for storage.

[0036] The samples of prescription 4-prescription 8 are tested for influencing factors, and the changes of related substances are shown in the table

[0037] relative substance%

[0038] As can be seen from the table, the stabilizer trometamol is added in the prescription, and the consumption is 0.1%-5%, and the indicated sample has better stability.

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PUM

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Abstract

There is provided an injection with torasemide as the main active ingredient in the invention, the preparing method of the injection is also included in the invention. The stability of the injection in the invention has been greatly improved. There is solubilizing agent and stabilizer in the preparation, the pH value is 9.0 or larger. The preparing method includes the following steps: adding 1-50% (by weight) of solubilizing agent to certain amount of injecting water; adding torasemide to the water, after it is completely dissolved, adding 0.1-5% part of stabilizer; adding water to requested amount and stirring uniformly; adding activated char to adsorb for 30min at high temperature; decarbonizing and filtering; adding medically used alkali to regulate the ph value to 9.0 or larger; aseptically filtering; after the assay is approved, packaging, degerming and stocking. The advantages of the invention include: high stability, short preparing time, low cost, no haemolyticus, blood vessel stimulus and allerfic response, low growing speed of relative substances.

Description

technical field [0001] The torasemide injection of the present invention is used for medicine, and the main route of administration is intravenous injection. The injection of the present invention has good stability. Torsemide, the chemical name is: 1-isopropyl-3-[(4-m-tolylamino-3-pyridyl)sulfonyl]urea, clinically used for diuresis and Na excretion + and row Cl - data of. technical background [0002] Torasemide is a pyridine sulfonylurea mixed diuretic, its chemical name is: 1-isopropyl-3-[(4-m-tolylamino-3-pyridyl)sulfonyl]urea, The structural formula is as follows: [0003] [0004] Molecular formula: C 16 h 20 N 4 o 3 S [0005] Molecular weight: 348.42 [0006] Loop diuretics are widely used to treat various types of edema, and the common adverse reaction is hypokalemia. Torasemide not only has a strong diuretic effect but also has less potassium loss, which is related to its competitive inhibition of aldosterone. [0007] Torsemide can be used for the t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61K9/08A61K47/34A61P7/10A61K47/10
Inventor 贾树田张现涛刘实李迪
Owner YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD
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