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Metoprolol salt oral administration impulse pellet preparation

A technology for pulsed pellets and preparations, applied in the field of metoprolol salt oral preparations and metoprolol salt oral pulsed pellet preparations, can solve problems such as difficulty in taking medicine by patients, achieve simple preparation process and improve compliance Effect

Inactive Publication Date: 2008-09-24
北京华禧联合科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As long as the patient takes the medicine before going to bed, and does not release the medicine for a period of time (people are in a period of low physiological level), the medicine is released quickly before the peak of angina pectoris and hypertension at 6-10 in the morning, and the blood drug concentration quickly reaches the therapeutic value, reaching The purpose of prevention and treatment, and at the same time solve the problem of patients' difficulty in taking medicine at night

Method used

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  • Metoprolol salt oral administration impulse pellet preparation
  • Metoprolol salt oral administration impulse pellet preparation
  • Metoprolol salt oral administration impulse pellet preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Prescription of quick-release pill core containing the main drug:

[0035] Starch sucrose blank core 400g

[0036] Metoprolol Tartrate 100g

[0037] 95% ethanol 1kg

[0038] Preparation process: Dissolve metoprolol tartrate in 95% ethanol, apply fluidized bed coating, temperature 32±1°C, flow rate 8mL / min, wrap metoprolol tartrate on the blank pellet core to obtain The main drug is the immediate-release pellet core. The average cumulative dissolution rate in 45 minutes was 93%.

[0039] Alkaline layer prescription: sodium bicarbonate 10% (w / v), add water to 100%.

[0040] Preparation process: Dissolve sodium bicarbonate in water, apply fluidized bed coating, temperature 50±1°C, flow rate 3mL / min, wrap sodium bicarbonate on the core of immediate-release pellets containing the main drug, and the weight of the coating increases by 20% , to prepare the ball core containing the basic layer.

[0041] Hysteresis layer prescription: w / v(%)

[0042] Polyacrylic resin III ...

Embodiment 2

[0047] Prescription of quick-release pill core containing the main drug:

[0048] Starch sucrose blank core 600g

[0049] Metoprolol Succinate 100g

[0050] 95% ethanol 1kg

[0051] The coating process is the same as in Example 1. Contain the main drug quick-release pellet core. The average cumulative dissolution rate was 90% in 45 minutes.

[0052] Alkaline layer prescription: Potassium dihydrogen phosphate 10% (w / v), add water to 100%, and the coating process is the same as in Example 1. The weight of the coating increased by 12%, and the ball core containing the basic layer was obtained.

[0053] Hysteresis layer prescription w / v(%)

[0054] Polyacrylic resin III (Eudragit S100) 6

[0055] Micronized silica gel 1.4

[0056] Add 95% ethanol to 100%,

[0057] The coating process is the same as in Example 1. Coating weight gain of 180%. The obtained pulse pellet release curve is shown in the appendix figure 2 : Lags for about 3.5 hours, then releases completely wi...

Embodiment 3

[0059] Whole prescription of immediate-release pill core containing main drug w / w(%)

[0060] Metoprolol Tartrate 30

[0061] Low-substituted hydroxypropyl cellulose 40

[0062] Microcrystalline Cellulose 30

[0063] Preparation process: add 5% HPMC in 70% ethanol solution to make soft material, extrude the soft material through the sieve plate of the extruder (aperture 0.8mm), put the strip-shaped particles in the spheronizer and spheronize, and dry the pellet core at 50°C After 5 hours, 18-24 mesh drug cores were sieved to obtain immediate-release pellet cores containing the main drug. The average cumulative dissolution rate in 45 minutes was 99%.

[0064] Basic layer: sodium carbonate 10% (w / v), add water to 100%, the coating process is the same as in Example 1. Coating weight gain 25%;

[0065] Hysteresis layer prescription w / v(%)

[0066] Polyacrylic resin III (Eudragit S100) 8

[0067] Dibutyl sebacate 1

[0068] Glycerin 0.2

[0069] Talc 1.5

[0070] Add 95% ...

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Abstract

The invention discloses the ingredients and the preparation method of an oral pulse pellet pharmaceutical preparation of metoprolol salts. The pharmaceutical preparation is a multi-layered coated pellet which has a basic structure of an immediate-release pellet core, an alkaline layer and a retardation layer containing remedium cardinale of 20 to 100 mg from inside to outside, wherein, the retardation layer contains polyacrylic resin 3, the weight increment of which is 100 to 240 percent of the immediate-release pellet core; the alkaline layer is a medicinal inorganic alkaline adjuvant, the weight of which is 10 to 30 percent of the immediate-release pellet core. After being taken, the pulse pellet begins to release immediately till a complete release is obtained after a time lag of 3 to 4 hours and achieves the effect of one pulse release. The oral pulse pellet pharmaceutical preparation can effectively prevent angina pectoris, hyperpiesis and other diseases from being triggered due to the rise of blood pressure and heart rate within a few hours after a patient awakens and wakes up in the early morning.

Description

[0001] Field [0002] The invention belongs to the technical field of pulse administration, and relates to oral preparations of metoprolol salts, more specifically, oral pulse pellet preparations of metoprolol salts. It is mainly used for the treatment of circadian rhythm diseases, and it is a pulse pellet preparation that can be released quickly after a certain time lag. Background technique [0003] With the development of chronopharmacology research, it has been found that the onset of many diseases shows obvious circadian rhythm changes, especially cardiovascular diseases such as hypertension, angina pectoris, myocardial infarction, and the morbidity and mortality of these diseases are highest in the early morning. If the optimal administration time is selected according to the biological rhythm of the onset of these diseases, the drug can exert the greatest therapeutic effect with the smallest therapeutic dose when it is most needed, while minimizing toxic and side effect...

Claims

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Application Information

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IPC IPC(8): A61K31/138A61K9/16A61K47/02A61K47/12A61K47/32A61P9/10A61P9/12
Inventor 刘衡钱云贤马滔刘欢王春龙
Owner 北京华禧联合科技发展有限公司
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