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Terlipressin preparation and preparations method thereof

A technology of terlipressin and preparations, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, cardiovascular system diseases, etc., can solve the problems that plague the application of terlipressin, and achieve the extension of the drug effect period, Stability improvement, stability improvement effect

Inactive Publication Date: 2011-05-25
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Terlipressin is easily degraded under acid, alkali, light, oxidation, and high temperature conditions. This problem has long plagued the application of terlipressin in pharmacy

Method used

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  • Terlipressin preparation and preparations method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Terlipressin 0.86g

[0033] Lactose 10g

[0034] Adjust pH to 4.0±0.5 with citric acid

[0035]

[0036] Make 1000 pieces

[0037] Weigh an appropriate amount of lactose, dissolve it in sterile water for injection, ultrafilter to remove the heat source, add a certain amount of active ingredient terlipressin according to the formula, dissolve and mix well, and adjust the pH value to 4.0 with citric acid ±0.5, set the volume to 1000ml. After filtering through a 0.22 μm microporous membrane, measure the content of terlipressin in the solution, divide it into glass bottles according to the content of 0.86 mg terlipressin in each bottle, and freeze-dry it under sterile conditions. Pre-freeze at 30°C to -70°C for 2-5 hours, then freeze and dry in vacuum. The primary drying time is between 10-30 hours, the secondary drying time is between 2-15 hours, and the constant temperature time is 2-10 hours, so that the moisture content of the freeze...

Embodiment 2

[0039] Terlipressin 0.86g

[0040] Lactose 15g

[0041] Adjust pH to 7.0±0.5 with citric acid

[0042]

[0043] Make 1000 pieces

[0044] Weigh an appropriate amount of lactose, dissolve it in sterile water for injection, remove the heat source by ultrafiltration, add a certain amount of active ingredient terlipressin according to the formula, dissolve and mix well, and adjust the pH value to 7.0 with citric acid ±0.5, set the volume to 1000ml. After filtering through a 0.22 μm microporous membrane, measure the content of terlipressin in the solution, divide it into glass bottles according to the content of 0.86 mg terlipressin in each bottle, and freeze-dry it under sterile conditions. Pre-freeze at 30°C to -70°C for 2-5 hours, then freeze and dry in vacuum. The primary drying time is between 10-30 hours, the secondary drying time is between 2-15 hours, and the constant temperature time is 2-10 hours, so that the moisture content of the freeze...

Embodiment 3

[0046] Terlipressin 0.86g

[0047] Mannitol 10g

[0048] Adjust pH to 4.0±0.5 with acetic acid

[0049]

[0050] Make 1000 pieces

[0051] Weigh an appropriate amount of mannitol, dissolve it in sterile water for injection, remove the heat source by ultrafiltration, add a certain amount of active ingredient terlipressin according to the formula, dissolve and mix well, and adjust the pH value to 4.0± with acetic acid 0.5, set the volume to 1000ml. After filtering through a 0.22 μm microporous membrane, measure the content of terlipressin in the solution, divide it into glass bottles according to the content of 0.86 mg terlipressin in each bottle, and freeze-dry it under sterile conditions. Pre-freeze at 30°C to -70°C for 2-5 hours, then freeze and dry in vacuum. The primary drying time is between 10-30 hours, the secondary drying time is between 2-15 hours, and the constant temperature time is 2-10 hours, so that the moisture content of the freez...

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Abstract

The invention discloses a terlipressin preparation and a preparations method thereof, belonging to the field of medical preparations. The terlipressin preparation comprises active components and auxiliary materials; the active components include terlipressin and pharmaceutically acceptable salts; the auxiliary materials include excipient and a pH regulator; and the weight part ratio of the terlipressin to the excipient to the pH regulator is (1-50):(1-1000):(1-200). Because the terlipressin is easy to degrade under the condition of acid or base, found by research of the invention, the stability of the active components in the terlipressin preparation can be greatly enhanced by selecting a proper pH range. With the pH range determined in the proportion range of the active components to the excipient to the pH regulator determined by the invention, researched by stability test, the stability of the active components is greatly enhanced, and the drug effect period of the active components is greatly prolonged under the same storage condition.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a terlipressin preparation and a preparation method thereof. Background technique [0002] The chemical structure of terlipressin is: [0003] [0004] Chinese chemical name: triglycine-8-lysine vasopressin. [0005] Terlipressin is a synthetic polypeptide analog of the hormone secreted by the posterior pituitary gland. After injection, its triglycyl group will be excised by enzymes in the body to slowly release active substances such as vasopressin, which can contract smooth muscle and last for 10 hours. Vasopressin mainly has two effects: one is the obvious effect of constricting blood vessels, thus reducing the venous blood flow to the hepatic portal system, thereby lowering the portal blood pressure and having a hemostatic effect; the other is that it can act on some kidneys. Receptor, prevents excessive loss of water in urine, has anti-enuresis fu...

Claims

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Application Information

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IPC IPC(8): A61K38/11A61K9/19A61P9/12A61K38/095
Inventor 谢圣坤陶安进龙镭李红玲马亚平袁建成
Owner HYBIO PHARMA
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