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Levoamlodipine besylate liposome tablet

A technology of L-amlodipine besylate and L-besylate, which is applied in the field of liposome solid preparations, can solve the problems of poor dispersibility and absorption, poor product stability, and low bioavailability, and achieve simple excipients Inexpensive, easy to operate, high economic value effect

Inactive Publication Date: 2011-01-19
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent CN101559043A discloses a kind of levamlodipine besylate tablet and its preparation method. Ingredient levamlodipine besylate is sensitive to light and heat, has poor solubility, and the resulting product has poor stability and low dissolution rate
[0006] Chinese patent CN1981759A discloses a kind of levamlodipine besylate dripping pills and a preparation method thereof, and Chinese patent CN1899268A discloses a kind of levamlodipine besylate dropping pills and a preparation method thereof. The drop pills prepared by the above-mentioned patents have great limitations in taking, poor dispersibility and absorbability, complicated preparation process, slow onset and low bioavailability

Method used

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  • Levoamlodipine besylate liposome tablet
  • Levoamlodipine besylate liposome tablet
  • Levoamlodipine besylate liposome tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation of embodiment 1 levamlodipine besylate liposome tablet

[0043] prescription:

[0044] Component Dosage

[0045] Levoamlodipine Besylate 2.5g

[0046] Egg yolk lecithin 10g

[0047] Cholesterol 1.25g

[0048] Poloxamer 188 2.5g

[0049] Starch 60g

[0050] Microcrystalline Cellulose 40g

[0051] Croscarmellose Sodium 13g

[0052] Povidone K30 5g

[0053] Micronized silica gel 5g

[0054] Magnesium Phosphatidate 2g

[0055] Preparation Process:

[0056] (1) Dissolve 10 g of egg yolk lecithin, 1.25 g of cholesterol, and 2.5 g of poloxamer 188 in 600 ml of a mixed solvent of ethanol and acetone with a volume ratio of 1:1, mix well, and remove the mixture under reduced pressure on a rotary thin film evaporator. Solvent to prepare phospholipid film;

[0057] (2) Add 300ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 6.8, adjust the pH value to 5.8 with 10% phosphoric acid solution, shake and s...

Embodiment 2

[0062] The preparation of embodiment 2 levamlodipine besylate liposome tablet

[0063] prescription:

[0064] Component Quantity

[0065] Levoamlodipine Besylate 5g

[0066] Egg yolk lecithin 50g

[0067] Cholesterol 25g

[0068] Poloxamer 188 15g

[0069] Microcrystalline Cellulose 90g

[0070] Mannitol 40g

[0071] Carboxymethyl Starch Sodium 15g

[0072] Povidone K30 10g

[0073] Talc powder 10g

[0074] Micronized silica gel 10g

[0075] Preparation Process:

[0076] (1) 50g egg yolk lecithin, 25g cholesterol, and 15g poloxamer 188 are dissolved in 1500ml of ethanol and acetone mixed solvent with a volume ratio of 1: 1, mix well, remove the mixed solvent under reduced pressure on a rotary thin film evaporator, Prepare phospholipid film;

[0077] (2) Add 800ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 6.8, adjust the pH value to 7.0 with 2mol / L potassium hydroxide solution, shake and stir to completely hy...

Embodiment 3

[0083] The preparation of embodiment 3 levamlodipine besylate liposome sheet

[0084] prescription:

[0085] Component Dosage

[0086] Levoamlodipine Besylate 2.5g

[0087] Egg yolk lecithin 20g

[0088] Cholesterol 10g

[0089] Poloxamer 188 5g

[0090] Microcrystalline Cellulose 60g

[0091] Dextrin 26g

[0092] 10g pregelatinized starch

[0093] Hypromellose 4g

[0094] Talc powder 6g

[0095] Stearic acid 4g

[0096] Preparation Process:

[0097] (1) 20g egg yolk lecithin, 10g cholesterol, 5g poloxamer 188 are dissolved in the dichloromethane solvent of 800ml, mix uniformly, remove mixed solvent under reduced pressure on the rotary thin film evaporator, make phospholipid film;

[0098] (2) Add 400ml of boric acid-borax buffer solution with a pH value of 6.8, adjust the pH value to 6.5 with 5% citric acid solution, shake and stir to completely hydrate the phospholipid film, and emulsify it 4 times with a high-speed tissue masher , 4min each time, rotating speed ...

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Abstract

The invention discloses a levoamlodipine besylate liposome tablet and application thereof in the preparation of medicines for treating primary hypertension. The levoamlodipine besylate liposome tablet comprises the following components of levoamlodipine besylate, yolk lecithin, cholesterol, Poloxamer 188 and other medically used excipients according to the weight proportion ratio of 1 to (4-10) to (0.5-5) to (1-3) to (35-50). The liposome tablet greatly enhances the stability and the dissolution rate of the levoamlodipine besylate and has the advantages of less side effects, more remarkable curative effect, high utilization degree, less pollution, high economic value, and the like.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome tablet of levamlodipine besylate, and further relates to its application in treating essential hypertension, which belongs to the technical field of medicine. Background technique [0002] With the aging of the social population, the incidence of hypertension in the elderly is increasing year by year. Hypertension is the most common cardiovascular and cerebrovascular risk factor, but hypertension is a controllable risk factor. A number of clinical studies have shown that long-term effective control of blood pressure can significantly reduce the risk of cardiovascular and cerebrovascular diseases. Therefore, antihypertensive treatment has become an important strategy for the prevention of cardiovascular and cerebrovascular diseases, and blood pressure control is the core of the entire antihypertensive strategy. [0003] Calcium antagonists (CAS) are recognized as effecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4422A61K47/34A61P9/12A61K47/10A61K47/24A61K47/28
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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