Preparation method of lacidipine composition

A technology of lacidipine and composition, which is applied in the direction of drug combination, non-active ingredient medical preparations, medical preparations containing active ingredients, etc. It can solve the problems of low fat solubility, slow release and absorption, and unsatisfactory drug dissolution rate, etc. problem, to achieve the effect of increasing dissolution rate

Inactive Publication Date: 2021-08-10
HAYAO GRP SANJING MINGSHUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This feature distinguishes lacidipine significantly from other calcium antagonists, which are less lipid soluble and thus have a shorter duration of action
Lacidipine tablets currently available in the market have two specifications of 4mg / tablet and 6mg / tablet. The content of the main drug is very low, and it is difficult to mix the drugs evenly when mixing the drugs, which makes it difficult to ensure the uniformity of the product content; Lacidipine is a fat-soluble drug that is released in vivo The absorption is slow. During the in vitro dissolution test, we found that the dissolution rate of the drug is not ideal, and it is difficult to reach more than 70%.

Method used

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  • Preparation method of lacidipine composition

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] The formula of lacidipine tablets is as follows, according to the dosage per 1000 tablets:

[0013] Lacidipine 4g;

[0014] Poloxamer 188 40g;

[0015] Polyvinylpyrrolidone (PVP) K30, 3g;

[0016] Crospovidone 2g;

[0017] Lactose 70g;

[0018] Magnesium stearate 1g.

[0019] The preparation process is as follows: take 40g of poloxamer 188, heat it in a water bath at 65°C until it melts, take 4g of lacidipine raw material drug and disperse it in the melted poloxamer 188, stir until the lacidipine is completely dissolved, and then cool to 0°C Finally, crush (control the temperature not to exceed 35°C) and pass through a 120-mesh sieve, add polyvinylpyrrolidone (PVP) K30, crospovidone, and lactose, mix evenly, granulate with a 24-mesh sieve dry granulator, and granulate with a 24-mesh sieve Add the magnesium stearate of formula quantity, under 150MPa pressure, direct compression obtains the lacidipine sheet of embodiment 1.

Embodiment 2

[0021] The formula of lacidipine tablets is as follows, according to the dosage per 1000 tablets:

[0022] Lacidipine 4g;

[0023] Poloxamer 188 60g;

[0024] Polyvinylpyrrolidone (PVP) K30, 3g;

[0025] Crospovidone 2g;

[0026] Lactose 50g;

[0027] Magnesium stearate 1g.

[0028] The preparation process is as follows: take 60g of poloxamer 188, heat it in a water bath at 65°C until it melts, take 4g of lacidipine crude drug and disperse it in the melted poloxamer 188, stir until the lacidipine is completely dissolved, and then cool to 0°C Finally, crush (control the temperature not to exceed 35°C) and pass through a 120-mesh sieve, add polyvinylpyrrolidone (PVP) K30, crospovidone, and lactose, mix evenly, granulate with a 24-mesh sieve dry granulator, and granulate with a 24-mesh sieve Add the magnesium stearate of formula quantity, under 150MPa pressure, direct compression obtains the lacidipine tablet of embodiment 2.

Embodiment 3

[0030] The formula of lacidipine tablets is as follows, according to the dosage per 1000 tablets:

[0031] Lacidipine 6g;

[0032] Poloxamer 188 60g;

[0033] Polyvinylpyrrolidone (PVP) K30, 3g;

[0034] Crospovidone 2g;

[0035] Lactose 70g;

[0036] Magnesium stearate 1g.

[0037] The preparation process is as follows: take 40g of poloxamer 188, heat it in a water bath at 65°C until it melts, take 6g of lacidipine raw material drug and disperse it in the melted poloxamer 188, stir until the lacidipine is completely dissolved, and then cool to 0°C Finally, crush (control the temperature not to exceed 35°C) and pass through a 120-mesh sieve, add polyvinylpyrrolidone (PVP) K30, crospovidone, and lactose, mix evenly, granulate with a 24-mesh sieve dry granulator, and granulate with a 24-mesh sieve Add the magnesium stearate of formula quantity, under 150MPa pressure, direct compression obtains the lacidipine sheet of embodiment 3.

[0038] By comparing the lacidipine prepa...

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Abstract

The invention discloses a preparation method of a lacidipine composition. The preparation method is characterized by comprising the following steps: (1) dispersing lacidipine in molten poloxamer 188; (2) cooling and solidifying the product obtained in the step (1), and performing low-temperature crushing and sieving to obtain lacidipine solid dispersion powder; (3) mixing the mixture obtained in the step (2), polyvinylpyrrolidone (PVP) K30, cross-linked povidone and lactose, and carrying out dry granulation; and (4) uniformly mixing the mixture obtained in the step (3) with a proper amount of magnesium stearate and tabletting. According to the method, the content uniformity of the lacidipine preparation can be ensured, and the dissolution rate of the lacidipine preparation is improved, so that the bioavailability of the lacidipine is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a lacidipine composition. Background technique [0002] Lacidipine is a dihydropyridine calcium antagonist. Calcium channel with high selectivity for smooth muscle. It mainly expands peripheral arteries, reduces peripheral resistance, and has a strong and lasting antihypertensive effect. It has no significant effect on the cardiac conduction system and myocardial systolic function. And can improve the diastolic function of the damaged hypertrophic left ventricle, and anti-atherosclerosis. Lacidipine is highly lipid soluble, it is deposited in the lipid fraction and is continuously released to the binding site during the clearance phase. This feature distinguishes lacidipine significantly from other calcium antagonists, which are less fat-soluble and therefore have a shorter duration of action. Lacidipine tablets currently available in the market have...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/10A61K47/32A61K47/26A61K31/4422A61P9/12
CPCA61K9/2031A61K9/2027A61K9/2018A61K31/4422A61P9/12
Inventor 王敬伟赵业辉秦洪波王博妍董志娟张伟李洪宇
Owner HAYAO GRP SANJING MINGSHUI PHARMA CO LTD
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