Nifedipine controlled release capsule and preparation method thereof

A technology for nifedipine and capsules, applied in the field of nifedipine controlled-release capsules and its preparation, which can solve problems such as the complex preparation process of osmotic pump preparations, and achieve the effects of avoiding blood drug concentration fluctuations, easy industrialization, and improving safety

Inactive Publication Date: 2020-05-22
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a nifedipine controlled-release capsule and its preparation method, to solve the problem of complex preparation process of the existing osmotic pump preparation

Method used

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  • Nifedipine controlled release capsule and preparation method thereof
  • Nifedipine controlled release capsule and preparation method thereof
  • Nifedipine controlled release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The prescription is shown in Table 1 (1000 capsules):

[0038] Table 1:

[0039]

[0040] Preparation process: 1. Preparation of capsules: After heating and dissolving polyethylene glycol 6000 at 60-80°C, add nifedipine and mix evenly, and cool to obtain nifedipine solid dispersion; grind the yellow solid dispersion and pass through 100 mesh Sieve; mix the solid dispersion powder, polyoxyethylene, citric acid, talcum powder and magnesium stearate, and put it in a hard capsule shell; 2. Coating operation: weigh the prescribed amount of cellulose acetate and poloxa M188 was dissolved in acetone solution. After the dissolution was completed, the above-mentioned nifedipine capsules were placed in a high-efficiency coating pot, and the coating liquid was sprayed onto the surface of the nifedipine capsules. The coating pot was set at a blast volume of 18 (m 3 / h), atomization pressure 1.6±0.2bar, spray speed 20±1g / min, air inlet temperature 45±2°C, material temperature 28...

Embodiment 2

[0043] Example 2 Pharmacokinetic study of nifedipine microporous osmotic pump controlled-release capsules

[0044] Six rabbits were randomly divided into two groups, and the rabbits were fasted (freely drinking water) for 12 h before administration. The self-made microporous osmotic pump capsules (prescription in Example 1) and the commercially available nifedipine controlled-release tablets (Baixintong, 30 mg / tablet) were respectively placed deep in the oral cavity of rabbits and swallowed whole. At 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24 and 36 h after administration, 0.5 mL blood was collected from the ear vein, and immediately transferred into heparin-treated Centrifuge at 4000 rpm for 10 min. Plasma was separated and stored in a -20°C refrigerator until use.

[0045] Precisely measure 200 μL of plasma sample, place in a 5 mL centrifuge tube, add 60 μL of ammonia water, vortex for 2 min, add 1.6 mL of anhydrous ether, vortex for 10 min, and centrifuge at 4000 r...

Embodiment 3

[0049] The prescription of embodiment 3 is shown in Table 2 (1000 grains):

[0050] Table 2:

[0051]

[0052] Preparation process: 1. Preparation of capsules: After heating and dissolving polyethylene glycol 6000 at 60-80°C, add nifedipine and mix evenly, and cool to obtain nifedipine solid dispersion; grind the yellow solid dispersion and pass through 100 mesh Sieve; mix the solid dispersion powder, polyoxyethylene, talcum powder and magnesium stearate, and put them in the hard capsule shell; 2, coating operation: take the prescribed amount of cellulose acetate, poloxamer 188 and dissolve in In the acetone solution, after the dissolution is completed, the above-mentioned nifedipine capsules are placed in a high-efficiency coating pan, and the coating liquid is sprayed onto the surface of the nifedipine capsules, and the coating pan setting condition is that the blast volume is 18 (m 3 / h), atomization pressure 1.6±0.2bar, spray speed 20±1g / min, air inlet temperature 45±2...

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Abstract

The invention provides a nifedipine controlled release capsule and a preparation method thereof. The controlled release capsule is prepared by filling a capsule shell with nifedipine, polyoxyethyleneand organic acid and coating the capsule shell. The mass ratio of nifedipine, polyoxyethylene and organic acid is (10-90):(1-15):(1-30); the coating is prepared from cellulose, a plasticizer and a pore-forming agent by mixing in a weight ratio of (10-50):(0-15):(1-25). Double-layer tabletting, laser or mechanical punching are not required, the preparation process is simple, the cost is low, the drug release rate is stable, zero-order release is basically achieved within 24 hours, and drug release is complete; the capsule is administered once a day, and thus, patient compliance is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a nifedipine controlled-release capsule and a preparation method thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases in the world today, and it is also a major risk factor for cardiovascular and cerebrovascular diseases. There are more than 100 million hypertensive patients in my country, and the number is increasing at a rate of more than 3 million people every year. Nifedipine, as the first-line antihypertensive drug, has a good curative effect. [0003] Nifedipine (Nifedipine) chemical name: dimethyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate, clinically used Prevention and treatment of coronary heart disease angina pectoris, suitable for various types of hypertension. Ordinary preparations of nifedipine need to be taken three times a day, which cannot control the stability of bl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/4422A61K47/10A61P9/12
CPCA61K9/4866A61K9/4891A61K31/4422A61K47/10A61P9/12
Inventor 胡连栋
Owner HEBEI UNIVERSITY
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