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Nilvadipine liposome tablets

A technology of nilvadipine and dipine fat, which is applied in the field of medicine, can solve the problems of less nilvadipine, etc., and achieve the effects of high encapsulation rate, improved stability, and high stability

Inactive Publication Date: 2010-12-15
HAINAN SHU ER PHARMA RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Nilvadipine was first listed in Japan in 1989 and was developed by Fujisawa Pharmaceutical Co., Ltd. At present, there are few reports about Nilvadipine at home and abroad

Method used

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  • Nilvadipine liposome tablets
  • Nilvadipine liposome tablets
  • Nilvadipine liposome tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The preparation of embodiment 1 nilvadipine liposome sheet

[0057] prescription:

[0058] Nilvadipine 2g

[0059] Hydrogenated Soy Lecithin 5g

[0060] Cholesterol 1.6g

[0061] Tween 80 1g

[0062] Starch 48g

[0063] Dextrin 40g

[0064] Low-substituted hydroxypropyl cellulose 6g

[0065] Hypromellose 1g

[0066] Talc powder 3g

[0067] Micronized silica gel 2g

[0068] Preparation Process

[0069] (1) Dissolve 5g of hydrogenated soybean lecithin, 1.6g of cholesterol, and 1g of Tween 80 in 200ml of water, mix well, and remove water under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0070] (2) Add potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane, high-speed homogeneous emulsification, and filter through a 0.45 μm microporous membrane to obtain a blank lipid body suspension;

[0071] (3) 2g nilvadipine was...

Embodiment 2

[0076] The preparation of embodiment 2 nilvadipine liposome sheet

[0077] prescription:

[0078] Nilvadipine 2g

[0079] Hydrogenated Soy Lecithin 13.2g

[0080] Cholesterol 8g

[0081] Tween 80 6.6g

[0082] Starch 34g

[0083] Microcrystalline Cellulose 25g

[0084] Carboxymethyl Starch Sodium 5g

[0085] Povidone K30 2.5g

[0086] Talc powder 3g

[0087] Magnesium Stearate 1g

[0088] Preparation Process

[0089] (1) 13.2g of hydrogenated soybean lecithin, 8g of cholesterol, and 6.6g of Tween 80 were dissolved in 500ml of water, mixed uniformly, and removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0090] (2) Add citric acid-sodium citrate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane, high-speed homogeneous emulsification, and filter through a 0.45 μm microporous membrane to prepare blank liposomes suspension;

[0091] (3) 2g of nilvadipine was dissolved in ...

Embodiment 3

[0096] The preparation of embodiment 3 nilvadipine liposome sheet

[0097] prescription:

[0098] Nilvadipine 4g

[0099] Hydrogenated Soy Lecithin 4.8g

[0100] Cholesterol 1.2g

[0101] Tween 80 0.8g

[0102] Lactose 55g

[0103] Microcrystalline Cellulose 64g

[0104] Crospovidone 6g

[0105] Povidone K30 3g

[0106] Magnesium Stearate 2g

[0107] Preparation Process

[0108] (1) 4.8g hydrogenated soybean lecithin, 1.2g cholesterol, 0.8g Tween 80 were dissolved in 300ml water, mixed uniformly, and water was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0109] (2) Add acetic acid-sodium acetate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane, emulsify at a high speed, and filter through a 0.45 μm microporous membrane to obtain a blank liposome suspension;

[0110] (3) 4g nilvadipine was dissolved in 200ml chloroform, then added to the blank liposome suspension,...

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PUM

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Abstract

The invention provides nilvadipine liposome tablets, which are characterized by consisting of the following components in part by weight: 1 part of nilvadipine, 1.2 to 10 parts of hydrogenated soybean phosphatidylcholine, 0.3 to 6 parts of cholesterol, 0.2 to 5 parts of Tween 80 and 30 to 60 parts of other pharmaceutically acceptable excipients. The prepared nilvadipine liposome has the advantages of high entrapment rate, small side effect, great improvement on the stability and water solubility and facilitating to dissolution of the medicinal preparations.

Description

technical field [0001] The present invention relates to a kind of liposome tablet, be specifically related to a kind of nilvadipine liposome tablet and preparation method thereof, further relate to its application in the treatment of cerebrovascular disease, ischemic heart disease and hypertension drug, It belongs to the field of medical technology. Background technique [0002] Nilvadipine, chemical name: 3-methoxycarbonyl-6-methyl-4-(3-nitrophenyl)-2-cyano-1,4-dihydropyridine-5-carboxylate isopropyl ester , the molecular formula is C 19 h 19 N 3 o 6 , the molecular weight is 385.38, and the structural formula is: [0003] [0004] Nilvadipine is a dihydropyridine calcium antagonist that interacts with Ca 2+ The binding force of the specific site of the channel is 10 times stronger than that of nifedipine, and the duration of action is also 2-3 times longer than that of nifedipine. The vasodilator has a strong selective effect and has a small effect on the heart, ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/127A61K9/30A61K31/4422A61K47/28A61K47/24A61K47/34A61P9/10A61P9/12A61K47/26
Inventor 陶灵刚
Owner HAINAN SHU ER PHARMA RES
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