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Prasugrel liposome solid preparation

A technology of liposomes and liposomes, applied in the field of liposome solid preparations, can solve problems such as not easy to dissolve, unfavorable preparation of pharmaceutical preparations, low solubility, etc., to achieve improved stability, easy removal by decompression evaporation, and small side effects Effect

Inactive Publication Date: 2010-09-01
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] As a potent adenosine diphosphate receptor antagonist, prasugrel has low solubility in water, and under the influence and inhibition of pharmaceutical excipients, it is not conducive to the preparation of pharmaceutical preparations and is not easy to dissolve in pharmaceutical preparations

Method used

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  • Prasugrel liposome solid preparation
  • Prasugrel liposome solid preparation
  • Prasugrel liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The preparation of embodiment 1 prasugrel liposome sheet

[0060] prescription:

[0061] Prasugrel 5g

[0062] Egg Yolk Phosphatidylglycerol 20g

[0063] Cholesterol 5.5g

[0064] Sodium Glycocholate 7.5g

[0065] Microcrystalline Cellulose 35g

[0066] Lactose 25g

[0067] Carboxymethyl Starch Sodium 10g

[0068] Povidone K30 2g

[0069] Talc powder 2g

[0070] Magnesium Stearate 1g

[0071] Preparation Process

[0072] (1) 20g egg yolk phosphatidylglycerol, 5.5g cholesterol, 7.5g sodium glycocholate are dissolved in the mixed solvent of isopropanol and acetone with a volume ratio of 5:2 in 500ml, mix well, and reduce Remove the mixed solvent under pressure to obtain a phospholipid film;

[0073] (2) Add 300ml of phosphoric acid-sodium hydrogen phosphate buffer solution with a pH value of 5.2, shake and stir to completely hydrate the phospholipid membrane, emulsify at a high speed, and filter through a 0.45 μm microporous membrane to prepare a blank liposome...

Embodiment 2

[0079] The preparation of embodiment 2 prasugrel liposome sheet

[0080] prescription:

[0081] Prasugrel 10g

[0082] Egg Yolk Phosphatidylglycerol 120g

[0083] Cholesterol 50g

[0084] Sodium Glycocholate 80g

[0085] Microcrystalline Cellulose 240g

[0086] Lactose 100g

[0087] Carboxymethyl Starch Sodium 30g

[0088] Povidone K30 10g

[0089] Talc powder 13g

[0090] Magnesium Stearate 7g

[0091] Preparation Process

[0092] (1) Dissolve 120g egg yolk phosphatidylglycerol, 50g cholesterol, and 80g sodium glycocholate in a mixed solvent of isopropanol and acetone with a volume ratio of 5:2 in 1500ml, mix well, and remove under reduced pressure on a rotary thin film evaporator Mixing solvents to prepare a phospholipid film;

[0093] (2) Add 600ml of phosphoric acid-sodium hydrogen phosphate buffer solution with a pH value of 5.2, shake and stir to completely hydrate the phospholipid membrane, emulsify at a high speed, and filter through a 0.45 μm microporous me...

Embodiment 3

[0099] The preparation of embodiment 3 prasugrel liposome sheet

[0100] prescription:

[0101] Prasugrel 5g

[0102] Egg Yolk Phosphatidylglycerol 40g

[0103] Cholesterol 150g

[0104] Sodium Glycocholate 25g

[0105] Starch 64g

[0106] Lactose 50g

[0107] Crospovidone 20g

[0108] Hypromellose 2g

[0109] Micronized silica gel 10g

[0110] Magnesium Stearate 4g

[0111] Preparation Process

[0112] (1) Dissolve 40g of egg yolk phosphatidylglycerol, 150g of cholesterol, and 25g of sodium glycocholate in a mixed solvent of isopropanol and acetone with a volume ratio of 5:2 in 500ml, mix well, and remove under reduced pressure on a rotary thin film evaporator. Mixing solvents to prepare a phospholipid film;

[0113] (2) Add 300ml of phosphoric acid-sodium hydrogen phosphate buffer solution with a pH value of 5.2, shake and stir to completely hydrate the phospholipid membrane, emulsify at a high speed, and filter through a 0.45 μm microporous membrane to prepare a ...

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Abstract

The invention provides a Prasugrel liposome solid preparation, which is characterized by being prepared by the following main components in parts by weight: 1 part of Prasugrel, 2-18 parts of yolk phosphatidylglycerol, 0.6-9 parts of cholesterol, 1.2-12 parts of sodium glycyl-cholate and 4-80 parts of other pharmaceutically accepted excipients. The Prasugrel liposome prepared by the invention has high entrapment rate and little side effect, improves stability of aqueous solubility thereof greatly and is favor of dissolving medicinal preparation out.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a prasugrel liposome tablet and a preparation method thereof, and further relates to its application in the treatment of atherosclerosis and acute coronary syndrome, belonging to medical technology field. Background technique [0002] Cardiovascular disease is on the rise year by year, and it is one of the serious diseases that cause human disability and death. The emergence of adenosine diphosphate receptor inhibitors is an important milestone in antiplatelet therapy, which can reduce the risk of cardiovascular events in high-risk patients, prevent sudden distal vascular obstruction in patients undergoing percutaneous coronary intervention, and significantly reduce myocardial infarction, Incidence and mortality of stroke, pulmonary or venous thrombosis. [0003] Following ticlopamide and clopidogrel, a new generation of platelet adenosine diphosphate receptor blocker, prasugrel,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/127A61K31/4365A61K47/28A61P9/10
Inventor 廖爱国
Owner HAINAN LINGKANG PHARMA CO LTD
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