Ozagrel sodium microballoon lyophilized preparation and preparation method thereof

A technology of ozagrel sodium and freeze-dried agent, which is applied in the field of medicine, can solve problems such as short storage time, clarity problems, suspended particles, etc., and achieve the effect of simple process, low production cost and good targeting

Inactive Publication Date: 2010-04-14
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But the solubility of ozagrel in water is small, therefore, it is usually made into sodium salt (that is, sodium ozagrel, English name: sodium ozagrel) in the art to improve its water solubility, but when it is made into After sodium salt, its stability in aqueous solution decreased (see JP2001316265)
At present, ozagrel is mainly sold in the market as the injection of ozagrel sodium, but due to the stability of the sodium salt and the characteristics of the injection itself, this sodium salt preparation may be partially isomerized during storage and transformed into It is cis-imidazolium methyl cinnamic acid, or ozagrel dimer and other insoluble substances appear, not only the storage time is short, the transportation is very inconvenient, but also may bring other potential problems to clinical medication
[0004] However, the current research on ozagrel (sodium) freeze-drying technology only stays in direct freeze-drying of ozagrel sodium or directly adding freeze-drying protective agent to freeze-drying. The biggest shortcoming is the clarity problem after reconstitution. There are color points, color blocks, turbidity, poor clarity and suspended particles in the final solution
These problems have not been well resolved

Method used

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  • Ozagrel sodium microballoon lyophilized preparation and preparation method thereof
  • Ozagrel sodium microballoon lyophilized preparation and preparation method thereof
  • Ozagrel sodium microballoon lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The composition of the freeze-dried agent:

[0035] Component Content

[0036] Sodium Ozagrel 20g

[0037] Chitosan 50g

[0038] Polyvinyl alcohol 1500 40g

[0039] Polysorbate 80 30g

[0040] Glucose 50g

[0041] Preparation:

[0042] (1) Dissolve 40g of polyvinyl alcohol 1500 in 500ml of distilled water, then add 30g of polysorbate 80, stir to dissolve completely, and obtain the water phase;

[0043] (2) 20g sodium ozagrel and 50g chitosan are dissolved in 500ml ethanol together, stir well, obtain oily phase;

[0044] (3) Slowly add the oil phase to the water phase, and keep stirring, the solution temperature is kept at 55°C, the oil phase rapidly diffuses into the water phase, forming an O / W or W / O emulsion;

[0045] (4) Heat the obtained emulsion to 80° C. under magnetic stirring, remove ethanol to obtain a suspension, centrifuge for 15-30 min, wash with distilled water to remove organic solvent and surfactant residues, and obtain microsphere precipitates;

...

Embodiment 2

[0048]The composition of the lyophilizer:

[0049] Component Content

[0050] Sodium Ozagrel 80g

[0051] Chitosan 150g

[0052] Polyvinyl alcohol 1500 100g

[0053] Poloxamer 188 120g

[0054] Mannitol 300g

[0055] Preparation:

[0056] (1) dissolve 100g polyvinyl alcohol 1500 in 1000ml distilled water, add 120g poloxamer 188 again, stir and dissolve completely, obtain water phase;

[0057] (2) co-dissolving 80 g of sodium ozagrel and 150 g of chitosan in 1000 ml of n-hexane, stirring evenly to obtain an oil phase;

[0058] (3) slowly adding the oil phase to the water phase, and stirring continuously, the solution temperature was maintained at 70°C, and the oil phase quickly diffused into the water phase to form an O / W or W / O type emulsion;

[0059] (4) heating the obtained emulsion to 80°C under magnetic stirring, removing n-hexane to obtain a suspension, centrifuging for 15 to 30 min, and washing with distilled water to remove organic solvent and surfactant residue ...

Embodiment 3

[0062] The composition of the lyophilizer:

[0063] Component Content

[0064] Sodium Ozagrel 40g

[0065] Chitosan 100g

[0066] Polyvinyl alcohol 2000 60g

[0067] Polysorbate 80 100g

[0068] Sorbitol 180g

[0069] Preparation:

[0070] (1) dissolve 60g polyvinyl alcohol 2000 in 800ml distilled water, add 100g polysorbate 80 again, stir and dissolve completely, obtain water phase;

[0071] (2) Dissolve 40 g of sodium ozagrel and 100 g of chitosan in 600 ml of ethanol, stir evenly, and it is an oil phase;

[0072] (3) slowly adding the oil phase to the water phase, and stirring continuously, the solution temperature was maintained at 60°C, and the oil phase quickly diffused into the water phase to form an O / W or W / O type emulsion;

[0073] (4) heating the obtained emulsion to 80°C under magnetic stirring, removing ethanol to obtain a suspension, centrifuging for 15 to 30 min, and washing with distilled water to remove organic solvent and surfactant residue to obtain a...

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Abstract

The invention relates to an ozagrel sodium microballoon lyophilized preparation and a preparation method thereof. The ozagrel sodium microballoon lyophilized preparation of the invention mainly includes the following components by weight part: 20-80 parts of ozagrel sodium, 50-150 parts of chitosan, 40-100 parts of polyvinyl alcohol, and 50-300 parts of lyophilization protective agent. The ozagrelsodium microballoon lyophilized preparation of the invention has the advantages of good stability and solubility, small grain diameter of lipidosome after hydration, strong targeting property, low production cost and the like.

Description

technical field [0001] The invention relates to a ozagrel sodium microsphere freeze-dried agent and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Ozagrel (English name: ozagrel) is a highly effective and selective inhibitor of thromboxane synthase, which inhibits thromboxane A2 (TXA 2 ) synthesis and promotion of prostacyclin (PGI 2 ), which has the effects of anti-platelet aggregation, reducing blood viscosity, promoting thrombus decomposition and dilating blood vessels. Therefore, it is especially suitable for inhibiting cerebral vasospasm, increasing cerebral blood flow, improving microcirculation disorders and abnormal energy metabolism in the brain, and improving cerebral ischemic symptoms and cerebral thrombosis (acute stage) patients after subarachnoid hemorrhage. movement disorders. Clinically, it is widely used in the treatment of acute thrombotic cerebral infarction and the movement disorder accompanied...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4164A61P7/02
Inventor 陶灵刚
Owner HAINAN MEIDA PHARMA
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