Drop pills of nitrendipine, and preparation method

A technology of nitrendipine and flat dropping pills, which is applied in the field of nitrendipine dropping pills and its preparation, can solve the problems of hepatic and intestinal first-pass effect, low bioavailability, and affecting therapeutic effect, and achieve accurate dosage and high bioavailability , The effect of simple production process and equipment

Inactive Publication Date: 2006-12-06
GUOSONG MEDICINES TECH NANJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, most of the nitrendipine preparations widely used by domestic clinicians are tablets and capsules. Due to the preparation technology and other reasons, there are problems such as long dissolution time, low dissolution rate, poor absorption, hepatic and intestinal symptoms after taking the tablets or capsules. Problems such as excessive effect and low bioavailability, which affect the efficacy of the drug and directly affect the effect of treatment

Method used

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  • Drop pills of nitrendipine, and preparation method

Examples

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Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 A kind of Nitrendipine dripping pills is made of the following raw materials in proportions by weight:

[0027] (1) 1 part of nitrendipine, 4 parts of polyethylene glycol 4000;

[0028] (2) 1 part of nitrendipine, 4 parts of sodium stearate;

[0029] (3) 1 part of nitrendipine, 5 parts of poloxamer;

[0030] (4) 1 part of nitrendipine, 3 parts of polyethylene glycol 6000, 1 part of stearic acid, and 1 part of poloxamer.

Embodiment 2

[0031] The preparation method of embodiment 2 nitrendipine dropping pills, its preparation steps are as follows:

[0032] a. Take Nitrendipine 100g that is pulverized until more than 90% of the particle size reaches below 50 microns;

[0033] b. Take 400g of polyethylene glycol (molecular weight: 4000), heat it to 95°C, add the above-mentioned nitrendipine after melting, and mix well;

[0034] c. Transfer the above-mentioned Nitrendi mixed with auxiliary materials into a special dripping machine for drip irrigation, and adjust the temperature of the dripper to 90°C;

[0035] d. Drop into liquid paraffin at 8°C;

[0036] e. After being shrinked and formed, take it out, remove the surface condensing agent, dry it, and pack it to obtain nitrendipine dripping pills, each weighing 25 mg, containing 5 mg of the main drug nitrendipine.

Embodiment 3

[0037] The preparation method of embodiment 3 nitrendipine dropping pills, its preparation steps are as follows:

[0038] a. Take Nitrendipine 100g that is pulverized until more than 90% of the particle size reaches below 50 microns;

[0039] b. Take 1000g of polyethylene glycol mixture (PEG6000:PEG4000=1:1), heat to 90°C, add the above-mentioned nitrendipine after melting, and mix well;

[0040] c. Transfer the above-mentioned Nitrendi mixed with auxiliary materials into a special dripping machine for drip irrigation, and adjust the temperature of the dripper to 80°C;

[0041] d. Drop into methyl silicone oil at 10°C;

[0042] e. After being shrinked and molded, take it out, remove the surface condensing agent, dry it, and pack it to obtain nitrendipine dripping pills, each weighing 22 mg, containing 2 mg of the main drug nitrendipine.

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Abstract

A dripping pill of nitrendipine for treating hypertension is proportionally prepared from nitrendipine and the matrix chosen from polyethanediol 4000, 6000 or 10000, stearic acid, sodium stearate, poloxamer, glycerin gelatin, monoglyceride stearate, shellac and polyoxyvinyl monostearate through thermally fusing said matrix, mixing it with nitrendipine, dripping in condensing agent, removing the condensing agent from their surface, drying in air and packing.

Description

1. Technical field [0001] The invention relates to an improved dosage form of nitrendipine medicine for treating hypertension-nitrendipine dropping pills and a preparation method thereof. 2. Background technology [0002] Nitrendipine, English name: Nitrendipine; chemical name is 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-methylethyl pyridinedicarboxylate. Molecular formula: C 18 h 20 N 2 o 6 ;Molecular weight: 360.37. The structural formula is: [0003] [0004] Nitrendipine is a new drug first listed in Europe and the United States in the 1980s. It is a second-generation calcium blocker and a derivative of nifedipine. Its antihypertensive effect is stronger and more durable than that of nifedipine. Its main pharmacological effects are Antagonize the calcium flow of the slow channel, thereby reducing the calcium current correspondingly, preventing the contraction of vascular smooth muscle, causing systemic arterial relaxation, mainly reducing diastolic blood pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K9/20A61K47/34A61P9/12A61P9/10A61K47/10A61K47/12A61K47/30A61K47/42
Inventor 李学松
Owner GUOSONG MEDICINES TECH NANJING
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