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Nisoldipine liposome solid preparation

A solid preparation, dipine fat technology, applied in the field of medicine, can solve the problems of low bioavailability, long dissolution time, many times of taking medicine, etc., and achieve the effects of high bioavailability, good sustained-release effect, and excellent dissolution.

Inactive Publication Date: 2012-04-11
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there are nisoldipine ordinary compressed tablets, sustained-release tablets, capsules and buffer capsules in the domestic marketed drugs. However, these dosage forms have the following problems: due to reasons such as preparation technology, most of the oral preparations of drugs are dissolved after taking. Long dispersion time, low dissolution rate, poor absorption, frequent doses, uncontrollable drug release, hepatoenteric first-pass effect and low bioavailability, etc., which affect the efficacy of the drug and directly affect the therapeutic effect, so its low bioavailability
[0016] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Nisoldipine liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Example 1 Nisoldipine liposome tablet

[0078] The raw and auxiliary materials used are as follows:

[0079]

[0080] Adopt following production process to prepare nisoldipine liposome tablet:

[0081] (1) Accurately weigh 5g nisoldipine, 200g phosphatidylethanolamine, 100g phosphatidylcholine distearate, 230g cholesterol acetyl ester, 50g Tween 80, dissolve in 1200ml volume ratio of dichloromethane and In a mixed solvent of isopropanol, stir to dissolve;

[0082] (2) Place the above solution in an eggplant-shaped bottle, remove methylene chloride and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0083] (3) Add 1200ml of phosphate buffer solution with a pH value of 7.0 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;

[0084] (4) The above solution is filtered with a 0.45 μm microporous membrane, the filtrate...

Embodiment 2

[0088] Example 2 Nisoldipine liposome tablet

[0089] The raw and auxiliary materials used are as follows:

[0090]

[0091] Adopt following production process to prepare nisoldipine liposome tablet:

[0092] (1) Accurately weigh 10g nisoldipine, 300g phosphatidylethanolamine, 150g phosphatidylcholine distearate, 225g cholesterol acetyl ester, 80g Tween 80, dissolve in 1500ml volume ratio of dichloromethane and In a mixed solvent of isopropanol, stir to dissolve;

[0093] (2) Place the above solution in an eggplant-shaped bottle, remove methylene chloride and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0094] (3) Add 1500ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate in a 45°C water bath under normal pressure to swell and hydrate the film;

[0095] (4) The above solution is filtered with a 0.45 μm microporous membrane, the filtrate...

Embodiment 3

[0099] Example 3 Nisoldipine liposome capsules

[0100] The raw and auxiliary materials used are as follows:

[0101]

[0102]

[0103] Adopt following production process to prepare nisoldipine liposome capsules:

[0104] (1) Accurately weigh 10g nisoldipine, 300g phosphatidylethanolamine, 150g phosphatidylcholine distearate, 250g cholesterol acetyl ester, 120g Tween 80 and dissolve in 2000ml volume ratio of 2:1 dichloromethane and iso In the mixed solvent of propanol, stir to make it dissolve;

[0105] (2) Place the above solution in an eggplant-shaped bottle, remove methylene chloride and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0106] (3) Add 2000ml of phosphate buffer solution with a pH value of 7.0 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;

[0107] (4) The above solution is filtered with a 0.45...

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Abstract

The invention discloses a nisoldipine liposome solid preparation and a preparation method thereof. The liposome is prepared from an active component nisoldipine and specifically combined phosphatidyl ethanolamine, phosphatidylcholine distearate, acetyl cholesterol and tween 80, so that the stability, solubility and bioavailability of the medicament can be greatly improved, the action is smooth and durable, and the curative effect is remarkable. According to the preparation, the product quality of the preparation is increased, and toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a new preparation of nisoldipine, in particular to a nisoldipine liposome and its solid preparation and preparation method, and belongs to the technical field of medicine. Background technique [0002] Cardiovascular and cerebrovascular disease is one of the diseases with the highest morbidity and mortality in the world today. It is the primary cause of death and the number one killer of health. The incidence of cardiovascular system diseases in my country is basically the same as that in the world. In the 1960s, the cause of death has risen from the seventh to the first. Every year, 3 million people die due to cardiovascular and cerebrovascular diseases, and 10 million people are disabled due to cardiovascular and cerebrovascular diseases. Almost every cardiovascular and cerebrovascular patient has clinical symptoms of elevated blood pressure and needs antihypertensive treatment. The market for antihypertensive drugs is huge. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/48A61K31/4422A61K47/34A61P9/04A61P9/10A61P9/12
Inventor 杨明贵曹丽梅
Owner HAINAN MEILAN SMITH KLINE PHARMA
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