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A kind of lacidipine solid dispersion and preparation method thereof

A technology of solid dispersion and lacidipine, applied in the field of medicine, can solve problems such as slow dissolution rate, and achieve the effects of improved dissolution rate, improved bioavailability and simple preparation method

Active Publication Date: 2021-07-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, recent research reports have shown that when the selected polymer has better compatibility with the drug and has a significant inhibitory effect on crystallization, its dissolution rate is often slower under non-sink conditions.
The racidipine amorphous solid dispersion prepared in the literature at present mainly uses polyvinylpyrrolidone (PVP), hypromellose (HPMC), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus ) etc. as carrier materials, there are still certain limitations in drug dissolution

Method used

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  • A kind of lacidipine solid dispersion and preparation method thereof
  • A kind of lacidipine solid dispersion and preparation method thereof
  • A kind of lacidipine solid dispersion and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1 crystal nucleation inhibitor and dissolution accelerator ratio are on the influence of drug supersaturation (attachment figure 1 )

[0045] Choose Soluplus as the crystal nucleus inhibitor, and GA as the dissolution accelerator.

[0046] The effect of the ratio of crystal nucleus inhibitor / dissolution accelerator on the supersaturation of the drug was investigated by solvent change method. The operation method was as follows: the ratio of lacidipine / carrier material was fixed at 1:5, and a certain amount of GA and Soluplus were weighed respectively. , Dissolved in 500mL PBS6.8 buffer solution. In addition, weigh 10 mg of lacidipine and add 1 mL of absolute ethanol to make a clear solution. With reference to the 2015 edition Chinese Pharmacopoeia Dissolution Determination Method (Appendix X C second method), the above-mentioned PBS buffer solution containing GA and Soluplus is used as the medium, and the rotating speed is 50 revolutions per minute, and the...

Embodiment 2

[0048] The impact of embodiment 2 carrier material proportions on the degree of supersaturation of medicine (attachment figure 2 )

[0049] Soluplus, GA was selected as the carrier material, and the effect of the ratio of drug / carrier material on the supersaturation of lacidipine was investigated by solvent change method.

[0050] The specific operation method is as follows: Weigh 10 mg of lacidipine, add 1 mL of absolute ethanol to make a clear solution. In addition, the ratio of Soluplus / GA was fixed at 3:1, and 500 mL of PBS6.8 buffer solutions containing different amounts of carrier material were prepared respectively, so that the ratio of lacidipine / carrier material was 1:1-1:7. With reference to the 2015 edition Chinese Pharmacopoeia Dissolution Determination Method (appendix X C second method), the above-mentioned PBS buffer solution containing different amounts of carrier materials is adopted as the medium, and the rotating speed is 50 revolutions per minute, and the...

Embodiment 3

[0052] The preparation of embodiment 3 lacidipine solid dispersion

[0053] Adopt spray-drying method to prepare lacidipine solid dispersion, typical preparation process is as follows:

[0054] Preparation of ternary solid dispersion: Dissolve 750mg Soluplus and 250mg GA in 500mL distilled water to form solution A, and dissolve 200mg lacidipine in 50mL absolute ethanol to form solution B, add solution B to solution A, and stir until Form a clear solution, adopt spray drying method (Buchi 290mini spray drier, Switzerland) at 100 ℃ inlet temperature, 600m 3 Under the conditions of air flow rate / h and 2mL / min liquid supply speed, carry out spray-drying, make lacidipine ternary solid dispersion.

[0055] Preparation of binary solid dispersion (control group): 1000mg Soluplus was dissolved in 500mL distilled water to form solution A, 200mg lacidipine was dissolved in 50mL absolute ethanol to form solution B, solution B was added to solution A, and stirred until Clear solution, us...

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Abstract

The invention belongs to the technical field of medicine, and relates to a lacidipine solid dispersion and a preparation method thereof, in particular to a lacidipine ternary solid dispersion and a preparation method thereof. The ternary solid dispersion comprises lacidipine, a crystal nucleus inhibitor and a dissolution accelerator. The crystal nucleus inhibitor is a water-soluble polymer material, and the stripping accelerator is an anionic polymer. The crystal nucleus inhibitor can inhibit the drug from forming a crystal nucleus by forming hydrogen bonds with the drug, so that the drug can maintain a supersaturated state for a long time. The dissolution accelerator can stabilize the crystal nuclei that have appeared in the system and prevent its further growth. At the same time, because the dissolution accelerator itself has high water solubility, under the joint action of the two, it can further improve the concentration of lacidipine in the non-sink tank. release rate under the condition. The system can significantly improve the dissolution rate and bioavailability of lacidipine.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a lacidipine solid dispersion and a preparation method thereof, in particular to a lacidipine ternary solid dispersion and a preparation method thereof. The system can significantly improve the dissolution rate and bioavailability of lacidipine Spend. Background technique [0002] Lacidipine is a new long-acting dihydropyridine calcium channel antagonist, its chemical name is (E)-4-[2-[3-(carboxy-tert-butyl)-3-oxo-1 -Propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridine-dicarboxylic acid diethyl ester, the molecular formula is C 26 H 33 NO 6 , the molecular weight is 455.59, and the structural formula is as follows. It is a highly selective calcium channel antagonist developed by GlaxoSmithKline, and is a highly effective, safe and well-tolerated drug for the treatment of hypertension. It can selectively act on calcium channels in vascular smooth muscle, dilate peripheral art...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4422A61K47/32A61K47/36A61K47/22A61K47/38A61P9/12
CPCA61K31/4422A61K47/22A61K47/32A61K47/36A61K47/38A61P9/12
Inventor 毛世瑞关健张欣
Owner SHENYANG PHARMA UNIVERSITY
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