Liposome solid preparation of ozagrel

A technology of ozagrel hydrochloride and liposomes, which is applied in the field of medicine, can solve the problems of low bioavailability, long dissolution time, and affecting the therapeutic effect, and achieve high bioavailability, excellent dissolution, and good sustained-release effect Effect

Inactive Publication Date: 2013-05-29
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ozagrel hydrochloride ordinary compressed tablets are available in domestic and foreign marketed drugs at present, but this dosage form has the following problems: due to reasons such as preparation technology, all there is dissolution time long, dissolution rate is low after taking the oral preparation of most drugs, Poor absorption, many times of taking medicine, uncontrollable drug release, low bioavailability and other problems, which affect the efficacy of the drug and directly affect the therapeutic effect, so its bioavailability is low
CN101416943A discloses a kind of ozagrel liposome and preparation method thereof, and it is made up of active substance ozagrel, lipid for preparing liposome, buffer and propping agent, such as adopting ammonium sulfate shaving method to prepare ozagrel, Phospholipids, cholesterol, and phosphate buffered saline are prepared by adjusting the pH to 4.0-9, and the Ozagrel liposomes prepared by it have poor stability and high content of related substances
The ozagrel (sodium) liposome preparations that these documents relate to are all preparations for injection, or have poor stability or release faster, and the consumption of phospholipids and cholesterol is higher, resulting in high cost and low relative drug content, not Facilitate drug administration
[0013] Ozagrel hydrochloride liposome and its solid preparations designed for oral application are not disclosed in the prior art

Method used

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  • Liposome solid preparation of ozagrel
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  • Liposome solid preparation of ozagrel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Ozagrel Hydrochloride Liposome Tablets

[0074] The raw and auxiliary materials used are as follows:

[0075]

[0076] Adopt the following production process to prepare ozagrel hydrochloride liposome tablet:

[0077] (1) Accurately weigh 100g of ozagrel hydrochloride, 160g of hydrogenated egg yolk lecithin, 80g of dioleoylphosphatidylethanolamine, 120g of cholesterol succinate, and 40g of Span 20, and dissolve them in 3000ml of methanol and tert- In the butanol mixed solvent, stir to make it dissolve;

[0078] (2) Place the above solution in an eggplant-shaped bottle, remove methanol and tert-butanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0079] (3) Add 10000ml of phosphate buffer solution with a pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0080] (4) Filter the above solution w...

Embodiment 2

[0084] Example 2 Ozagrel Hydrochloride Liposome Tablets

[0085] The raw and auxiliary materials used are as follows:

[0086]

[0087] Adopt the following production process to prepare ozagrel hydrochloride liposome tablet:

[0088] (1) Accurately weigh 200g of ozagrel hydrochloride, 280g of hydrogenated egg yolk lecithin, 140g of dioleoylphosphatidylethanolamine, 210g of cholesterol succinate, 40g of Span 20, and dissolve them in 5000ml of methanol and t- In the butanol mixed solvent, stir to make it dissolve;

[0089] (2) Place the above solution in an eggplant-shaped bottle, remove methanol and tert-butanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0090] (3) Add 15000ml of phosphate buffer solution with a pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0091] (4) Filter the above solution with a ...

Embodiment 3

[0095] Example 3 Ozagrel Hydrochloride Liposome Tablets

[0096] The raw materials used are as follows:

[0097]

[0098] Adopt following production process to prepare ozagrel hydrochloride liposome tablet:

[0099] (1) Accurately weigh 200g of ozagrel hydrochloride, 240g of hydrogenated egg yolk lecithin, 120g of dioleoylphosphatidylethanolamine, 180g of cholesterol succinate, 80g of Span 20 and dissolve them in 4000ml of methanol and tert-butyl at a volume ratio of 2:1. In the mixed solvent of alcohol, stir to make it dissolve;

[0100] (2) Place the above solution in an eggplant-shaped bottle, remove methanol and tert-butanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0101] (3) Add 12000ml of phosphate buffer solution with a pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to make the film swell and hydrate;

[0102] (4) Filter the...

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Abstract

The invention discloses a liposome solid preparation of ozagrel and a preparation method thereof. In the invention, an active ingredient ozagrel hydrochloride and a special combination of hydrogenated yolk lecithin, dioleoyl-phosphatidyl-ethanolamine, cholesteryl succinate, and Span 20 are prepared into a liposome, thereby greatly improving stability, dissolubility, and bioavailability of the drug, and having stable and lasting effect and obvious curative effect. According to the invention, product quality of the preparation is improved, and the toxic side effect is reduced.

Description

technical field [0001] The invention relates to a new preparation of ozagrel hydrochloride, in particular to ozagrel hydrochloride liposome and its solid preparation and preparation method, belonging to the technical field of medicine. Background technique [0002] In recent years, a series of thromboembolic diseases such as cerebral thrombosis, myocardial infarction, peripheral arterial thrombosis, deep vein thrombosis, and pulmonary embolism have seriously threatened human health. According to statistics, the death caused by it has reached 51% of the total death toll in the world. Therefore, thrombus, the ghost in blood vessels, is the common opponent of specialist doctors and has become the greatest enemy of human health. The manifestations of thromboembolic disease range from head to toe. Cerebral vascular thrombosis can cause dysfunction of one side of the limbs of the patient, that is, hemiplegia, aphasia, visual and sensory impairment, coma, and can be disabled or f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/4174A61K47/28A61K47/24A61P7/02
Inventor 王明曹丽梅
Owner HAINAN YONGTIAN PHARMA INST
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