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Nifedipine sustained release preparation and preparation method thereof

A technology of nifedipine and nifedipine, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. It can improve the stability of the drug, avoid the phenomenon of crystal transformation, and achieve the effect of simple preparation process.

Active Publication Date: 2016-09-07
SINOPHARM GUANGDONG GLOBAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] a. Nifedipine is a short-acting calcium antagonist with a short duration of action and requires frequent administration; ordinary preparations are unstable in drug release, with large fluctuations in blood drug concentration, prone to reflexive heart rate acceleration, activation of the sympathetic nervous system, and adverse effects on the immune system. Adverse reactions such as myocardial ischemia and heart failure control
[0005] b. Nifedipine is poorly soluble in water, and a release blocker needs to be added in the preparation process of the sustained-release preparation, which may cause the drug to be released slowly in the early stage, and cannot take effect quickly to play a therapeutic role
[0006] c. Existing biphasic drug release system or controlled release system for nifedipine, although a relatively ideal drug release effect can be obtained, there are also disadvantages such as complex process, high manufacturing cost, and low production efficiency

Method used

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  • Nifedipine sustained release preparation and preparation method thereof
  • Nifedipine sustained release preparation and preparation method thereof
  • Nifedipine sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment one: the preparation of nifedipine sustained-release pellets

[0035] 1, the preparation of nifedipine aqueous dispersion:

[0036] Weigh each component according to the following formula:

[0037]

[0038] Micronize the nifedipine bulk drug, and the particle size is controlled at 1-5 μm; add povidone, sodium lauryl sulfate, and hypromellose into water, stir to dissolve, and add the micronized Nifedipine and talc, continue stirring to form a uniform aqueous suspension.

[0039] 2. Preparation of drug-containing sustained-release pellet core:

[0040] Weigh each component according to the following formula:

[0041]

[0042] Take nifedipine, microcrystalline cellulose and lactose, mix them evenly and use them as the substrate, use the mixture of acrylic acid copolymer RS30D and acrylic acid copolymer RL30D as the binder, and use a fluidized bed for spray granulation. Afterwards, drying is carried out to obtain drug-containing sustained-release pellet...

Embodiment 2

[0045] Embodiment two: the preparation of nifedipine slow-release tablet

[0046] Weigh each component according to the following formula:

[0047]

[0048]

[0049] Take the nifedipine sustained-release pellets prepared in Example 1, add cross-linked polyvinylpyrrolidone, silicon dioxide and magnesium stearate, mix evenly, and then perform tablet compression to obtain nifedipine sustained-release tablets.

Embodiment 3

[0050] Embodiment three: the drug release characteristic test of nifedipine sustained-release tablet

[0051] 1. Chromatographic conditions:

[0052] Mobile phase: 0.1% phosphoric acid-methanol-acetonitrile (40:30:30); flow rate: 1.0mL / min; chromatographic column: octadecylsilane bonded silica gel column (C 18 column); injection volume: 20 μL; detection wavelength: 235 nm.

[0053] 2. Release measurement method: dark operation

[0054] Get 4 parts of nifedipine slow-release tablets that embodiment two makes respectively, every part of 6, according to the first method of release assay method (two appendix X D of Chinese Pharmacopoeia version in 2010), adopt dissolution assay method (Chinese Pharmacopoeia Appendices X to Part Two of the 2010 edition C) The second method (paddle method) device, respectively use 900mL of water, pH 1.2 hydrochloric acid solution, pH 4.0 acetate buffer solution and pH 6.8 phosphate buffer solution as release Medium (both containing 0.3% Tween 80)...

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Abstract

The invention discloses a nifedipine sustained release preparation and a preparation method thereof. The nifedipine sustained release preparation is prepared from nifedipine sustained release pellets and pharmaceutically acceptable auxiliary materials, wherein the nifedipine sustained release pellets comprise medicine-containing sustained release pellet cores and medicine-containing quick release layers; and the medicine-containing quick release layers wrap the outer layers of the medicine-containing sustained release pellet cores through fluidized bed spraying of nifedipine aqueous dispersion. The nifedipine sustained release preparation has ideal medicine release characteristics. The preparation process is simple and efficient.

Description

technical field [0001] The present invention relates to a drug sustained-release preparation and a preparation method thereof, in particular to a nifedipine sustained-release preparation and a preparation method thereof. Background technique [0002] Nifedipine is a dihydropyridine calcium ion channel antagonist, which has a strong effect of dilating coronary arteries and peripheral arteries, and has a remarkable effect on inhibiting vasospasm. Prevention and treatment of angina pectoris. Its mechanism of action is mainly through selective inhibition of calcium influx in myocardial cell membranes, blocking myocardial cell excitation-contraction coupling, weakening myocardial contractility, reducing myocardial energy and oxygen consumption, and directly protecting cardiomyocytes by preventing calcium overload. [0003] Unfortunately, there are still deficiencies in the clinical application and preparation development of nifedipine, as follows: [0004] a. Nifedipine is a sh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K9/16A61K47/38A61K47/32A61K47/20A61K47/02A61P9/12A61P9/10
CPCA61K9/0002A61K9/1617A61K9/1623A61K9/1641A61K9/1647A61K9/1652A61K9/167A61K31/4422
Inventor 袁春平高永坚黄掌欣郭静张文芳区淑蕴
Owner SINOPHARM GUANGDONG GLOBAL PHARMA CO LTD