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Slow-release preparation of calcium antagonist and salt thereof and preparation method thereof

A technology of sustained-release preparations and calcium antagonists, which is applied in the field of pharmaceutical preparations and drug sustained-release preparations, and can solve problems such as increased adverse drug reactions

Inactive Publication Date: 2017-09-05
杨彦玲
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, increasing the dose will lead to an increase in the adverse reactions of the drug

Method used

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  • Slow-release preparation of calcium antagonist and salt thereof and preparation method thereof
  • Slow-release preparation of calcium antagonist and salt thereof and preparation method thereof
  • Slow-release preparation of calcium antagonist and salt thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0118] Example 1: Capsules Containing Sustained Release Pills

[0119] I) drug-loaded pellet core

[0120]

[0121]

[0122] II) Pack isolation gown

[0123]

[0124] III) Pack slow-release coat

[0125]

[0126] 1.1 Preparation of drug-loaded coating solution

[0127] Take an appropriate amount of binder (hydroxypropyl cellulose, copovidone or povidone), disperse it in 95% ethanol solution, and prepare a coating liquid with a solid content of 10%, fully mix it; then weigh The prescription amount of amlodipine is evenly dispersed in the above-mentioned coating solution, as the drug-loaded coating solution of the slow-release phase, for subsequent use.

[0128] 1.2 drug loading

[0129] Add blank pellet cores (microcrystalline cellulose pellet cores or sucrose pellet cores) into the fluidized bed, adjust operating parameters such as air intake volume, intake air temperature, and atomization pressure, and spray into the prepared slow-release phase drug-loaded coati...

Embodiment 2

[0134] Example 2: Capsules Containing Sustained Release Tablets

[0135]

[0136] The preparation method is as follows:

[0137] Amlodipine besylate, diluent (mannitol), sustained-release matrix matrix (hydroxypropyl cellulose, povidone, carbomer or polyoxyethylene) were uniformly mixed by equal addition method, and then added to the fluid Chemical bed; granulate with 80% ethanol solution as binder; dry until the water content is less than 5%, pass through a 20-mesh sieve for granulation, then add magnesium stearate, mix well, and use it as amlodipine besylate slow-release granules ; According to the prescribed amount, compressed into sustained-release tablets with suitable hardness.

[0138] Capsule filling: The sustained-release tablets prepared above are filled into capsules.

[0139] Release measurement method is with embodiment 1;

[0140] Among them, the release results of prescription 4 see Figure 8 , the drug release reaches 90% in 10 hours. Example 3: Sustain...

Embodiment 3

[0140] Among them, the release results of prescription 4 see Figure 8 , the drug release reaches 90% in 10 hours. Example 3: Sustained-release coated tablet with booster layer

[0141] ① Drug-containing layer

[0142]

[0143] ② Booster layer

[0144]

[0145] ③Semi-permeable membrane

[0146]

[0147] ④ Moisture-proof coating film

[0148]

[0149] The preparation method is as follows:

[0150] The preparation of drug-containing layer: amlodipine besylate and hydrophilic polymer (povidone, copovidone), iron oxide yellow, after adopting the equal amount addition method to mix uniformly, add fluidized bed; Spray into 95 % ethanol-water solution to granulate; dry until the water content is less than 5%, pass through a 20-mesh sieve, and granulate to obtain drug-containing granules, then add magnesium stearate, mix well, and set aside;

[0151] Preparation of the booster layer: mix sodium carboxymethyl starch, hydroxypropyl methylcellulose K15M, sodium chloride...

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Abstract

The invention provides a slow-release preparation of calcium antagonist and salt thereof and a preparation method thereof. The slow-release preparation comprises a slow-release phase which contains active pharmaceutical ingredients, the active pharmaceutical ingredients include 5-40mg of amlodipine or salt thereof calculated by amlodipine, 4-32mg of lacidipine or salt thereof calculated by lacidipine, 5-40mg of nisoldipine or salt thereof calculated by nisoldipine, 5-40mg of cilnidipine or salt thereof calculated by cilnidipine, 2-32mg of benidipine or salt thereof calculated by benidipine, 10-80mg of lercanidipine or salt thereof calculated by lercanidipine and 5-80mg of manidipine or salt thereof calculated by manidipine; in release media meeting sink conditions, higher than 90% of weight of the active pharmaceutical ingredients are released within a release period of 6-14h. The slow-release preparation is convenient to use, good in treatment effect, high in taking compliance, little in adverse reaction, quick in action, capable of maintaining stable and effective blood concentration for a long time, ingenious in design, simple in structure, high in stability and suitable for large-scale popularization and application.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to the technical field of sustained-release pharmaceutical preparations, in particular to a sustained-release preparation of a calcium antagonist or a salt thereof and a preparation method thereof. Background technique [0002] With the improvement of people's living standards, cardiovascular disease has become the number one cause of death in my country and the "number one killer" that threatens people's health and lives. The prevalence of hypertension among adults over the age of 18 in my country is as high as 33.5%, and the total number exceeds 330 million. The number of deaths caused by hypertension and its complications is as high as 9.4 million in the world every year, of which about 2 million people die of hypertension in my country every year. With the further aggravation of aging in our country, the morbidity and mortality of hypertension are still incre...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/00A61P9/12
CPCA61K45/00A61K9/0002
Inventor 杨彦玲李环何彧薛传校薛峰
Owner 杨彦玲
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