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Lafutidine liposome solid preparation and preparing method thereof

A technology for lafutidine and futidine is applied in the field of medicine to achieve the effects of high product quality, long retention time and significant curative effect

Inactive Publication Date: 2014-02-26
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Lafutidine liposome solid preparation and preparing method thereof
  • Lafutidine liposome solid preparation and preparing method thereof
  • Lafutidine liposome solid preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Preparation of Lafutidine Liposome Tablets

[0070]

[0071]

[0072] Adopt following production process to prepare lafutidine liposome tablet:

[0073] (1) Dissolve 5g of lafutidine, 125g of dipalmitoylphosphatidylglycerol, 125g of sodium deoxycholate and 50g of Span 80 in 2000ml of methanol, and stir to dissolve;

[0074] (2) Put the above solution in an eggplant-shaped bottle, remove methanol under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0075] (3) Add 2000ml of acetate buffer solution with a pH value of 6.2 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;

[0076] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a refrigerator at -20°C to freeze overnight, then take it out and thaw it, freeze and thaw repeatedly three times, and spray dry to obtain lafutidine li...

Embodiment 2

[0080] Example 2 Preparation of Lafutidine Liposome Capsules

[0081]

[0082] Adopt following production process to prepare lafutidine liposome capsule:

[0083] (1) Dissolve 10g of lafutidine, 300g of dipalmitoylphosphatidylglycerol, 150g of sodium deoxycholate and 80g of Span 80 in 2000ml of methanol, and stir to dissolve;

[0084] (2) Put the above solution in an eggplant-shaped bottle, remove methanol under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0085] (3) Add 2000ml of acetate buffer solution with a pH value of 6.2 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;

[0086] (4) Filter the above solution with a 0.45 μm microporous membrane, freeze the filtrate overnight in a -20°C refrigerator, take it out and thaw it, freeze and thaw repeatedly three times, and spray dry to obtain lafutidine liposome powder.

[0087] (...

Embodiment 3

[0090] Example 3 Preparation of Lafutidine Liposome Dispersible Tablets

[0091]

[0092] Adopt following production process to prepare lafutidine liposome dispersible tablet:

[0093] (1) Dissolve 5g of lafutidine, 150g of dipalmitoylphosphatidylglycerol, 100g of sodium deoxycholate and 100g of Span 80 in 2000ml of methanol, and stir to dissolve;

[0094] (2) Put the above solution in an eggplant-shaped bottle, remove methanol under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0095] (3) Add 2000ml of acetate buffer solution with a pH value of 6.2 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;

[0096] (4) Filter the above solution with a 0.45 μm microporous membrane, freeze the filtrate overnight in a -20°C refrigerator, take it out and thaw it, freeze and thaw repeatedly three times, and spray dry to obtain lafutidine liposo...

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Abstract

The invention discloses a lafutidine liposome solid preparation and a preparing method thereof. Lafutidine liposome excellent in quality can be prepared through lafutidine, dipalmitoylglycero-phosphoglycerol, deoxysodium cholate and span 80, and then the lafutidine liposome can be prepared into solid preparation through a general preparation method. Compared with the existing preparation, the lafutidine liposome solid preparation greatly improves stability and bioavailability, improves quality of preparation products, reduces toxic and side effects and is remarkable in curing effect.

Description

technical field [0001] The invention relates to a liposome solid preparation and a preparation method thereof, in particular to a lafutidine liposome, a solid preparation and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Lafutidine, its chemical name is: (+ / -)-2-[(2-furylmethyl)sulfinyl]-N-[4-[4-(1-piperidinylmethyl)- 2-pyridyl]oxy-(Z)-2-butenyl]acetamide, molecular formula: C 22 h 29 N 3 o 4 S, molecular weight: 431.55, structural formula: [0003] [0004] Lafutidine is an anti-ulcer drug jointly developed by Fujirebio and Taiho in Japan. This product is a potent and long-acting second-generation histamine H2 receptor antagonist with a unique Gastric protection. It was launched in Japan in April 2000. Lavutidine is a second-generation H2 receptor antagonist, mainly used in the treatment of peptic ulcer, which can reduce the basal secretion of gastric acid and inhibit the secretion of gastric acid stimu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/16A61K9/48A61K31/4545A61K47/28A61K47/24A61P1/04
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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