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Lacidipine dispersible tablet and preparation method thereof

A technology of lacidipine and dispersible tablets, which is applied in the field of lacidipine dispersible tablets and its preparation, can solve problems such as large fluctuation range of tablet content, influence on product curative effect, and difficulty in swallowing ordinary tablets by patients, so as to increase solubility and Dissolution rate, enhanced drug compliance, and improved bioavailability

Inactive Publication Date: 2014-08-27
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the preparation process of this method, a sufficient amount of organic solvent is required to completely dissolve it, so that the soft material is too soft, and the soluble components of lacidipine will migrate, resulting in unqualified content uniformity and fluctuations in tablet content The range is large, the difference in drug efficacy increases, and the blood pressure cannot be controlled smoothly during treatment, causing blood pressure fluctuations in patients
Thereby affecting the curative effect of the product, there is also the problem that the residual organic solvent exceeds the standard
[0008] At the same time, most hypertensive patients are elderly, and some patients have difficulty swallowing ordinary tablets

Method used

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  • Lacidipine dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Lacidipine 4.0 g Povidone 12.0 g Tween (solubilizer) 4 g Lactose (filler) 80.0 g Talc (anti-sticking agent) 40.0 g Crospovidone (disintegrant) 35.0 g Microcrystalline Cellulose (Filler) 40.0 g Croscarmellose sodium (disintegrant) 25.0 g Silica (lubricant) 2.0 g

[0024] Its preparation method comprises the following steps:

[0025] (1) Get lacidipine, be dissolved in dehydrated alcohol, add povidone after, stir violently and make it dissolve into a clear and transparent solution, add Tween after, continue to stir for 0.5-3 h, obtain lacidipine solution, the The lacidipine solution is prepared into a dry lacidipine solid dispersion by spray drying;

[0026] (2) Gradually add diluent, disintegrating agent, anti-adhesive agent, lubricant, glidant by equal amount incremental method, after repeated sieving and mixing, directly compress into tablets to obtain lacidipine dispersible tablets.

[0027] test results:...

Embodiment 2

[0035] Its preparation method comprises the following steps:

[0036] (1) Take lacidipine, dissolve it in absolute ethanol, then add povidone, stir vigorously to dissolve it into a clear and transparent solution, then add polyoxyethylene hydrogenated castor oil, and continue stirring for 0.5-3 h to obtain lacidipine Solution, the lacidipine solution is prepared into a dry lacidipine solid dispersion by spray drying;

[0037] (2) Gradually add diluent, disintegrating agent, anti-adhesive agent, lubricant, glidant by equal amount incremental method, after repeated sieving and mixing, directly compress into tablets to obtain lacidipine dispersible tablets.

[0038] test results:

[0039] Compressibility: good

[0040] Friability: in compliance with regulations

[0041] Appearance: smooth and beautiful

[0042] Uniformity of dispersion: in compliance with regulations

[0043] Average dissolution rate: 49.25%

[0044] Example 3:

Embodiment 3

[0046] Its preparation method comprises the following steps:

[0047] (1) Take lacidipine, dissolve it in absolute ethanol, then add povidone, stir vigorously to make it dissolve into a clear and transparent solution, then add potassium oleate, and continue stirring for 0.5-3 h to obtain the lacidipine solution. The lacidipine solution is prepared into a dry lacidipine solid dispersion by spray drying;

[0048] (2) Gradually add diluent, disintegrating agent, anti-adhesive agent, lubricant, glidant by equal amount incremental method, after repeated sieving and mixing, directly compress into tablets to obtain lacidipine dispersible tablets.

[0049] test results:

[0050] Compressibility: good

[0051] Friability: in compliance with regulations

[0052] Appearance: smooth and beautiful

[0053] Uniformity of dispersion: in compliance with regulations

[0054] Average dissolution rate: 61.25%

[0055] Example 4:

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Abstract

The invention discloses a lacidipine dispersible tablet and a preparation method thereof. A solid dispersion is prepared by adopting lacidipine as a medicinal active component and polyvinylpyrrolidone as a carrier material through a spray drying technology, and the solid dispersion is processed to prepare the dispersible tablet. The preparation of the solid dispersion from lacidipine and a proper amount of polyvinylpyrrolidone increases the solubility and dissolve-out speed of a medicine, promotes the absorption of the medicine in bodies and improves the bioavailability of the medicine. The preparation of the dispersible tablet from the solid dispersion enhances the medicine administration compliance of a patient.

Description

technical field [0001] The invention relates to a pharmaceutical preparation in the category of oral rapid release, in particular to a lacidipine dispersible tablet and a preparation method thereof. Background technique [0002] Lacidipine, the chemical name is (E)-4-[2-[3-(carboxy-tert-butyl)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6 -Dimethyl-3,5-pyridine-diethyl carboxylate, common name is lacidipine, molecular formula: C 26 h 33 NO 6 , molecular weight: 455.59, its structural formula is as follows: [0003] [0004] Lacidipine is a selective dihydropyridine calcium ion channel blocker developed by GlaxoSmithKline in the United Kingdom. It is an efficient, safe and well-tolerated drug for the treatment of hypertension, which can significantly and selectively act on vascular smooth muscle The calcium channel mainly expands peripheral arteries, reduces peripheral resistance, and has a strong and long-lasting antihypertensive effect. It has no significant effect on th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4422A61K47/32A61P9/12
Inventor 李艳莉翟志瑞郭夏
Owner AVENTIS PHARMA HAINAN
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