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Ibuprofen quick-release and slow-release nanoparticle and preparation method thereof

A nanoparticle, slow-release technology, applied in the direction of nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of inability to exert drug efficacy for a long time, slow initial release, loss of drug efficacy, etc., to achieve continuous maintenance of blood drug concentration, Quick release, prolonged storage effect

Pending Publication Date: 2021-12-07
HUAZHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent document CN104606145A discloses a kind of ibuprofen granule and its preparation method. The ibuprofen granule is made of the following raw materials in parts by weight: 1 part of ibuprofen, 1 to 100 parts of filler, 0.1 to 100 parts of corrective agent 10 parts, 1 to 20 parts of adhesive, the filler is composed of sucrose and sodium cyclamate, the program adjusts the irritating smell of the ibuprofen drug itself through the filler and the adhesive in combination with a specific ratio of raw materials , and the taste of ibuprofen granules dissolved in water. The obtained ibuprofen granules dissolve quickly in water and form a clear and transparent solution with good taste. It is easy to take, has high bioavailability, good taste and medium viscosity, and is easier to accept , although the above-mentioned ibuprofen granules can disintegrate quickly in water, and can quickly exert the drug effect, the drug effect will be lost soon, and the drug effect cannot be exerted for a long time
[0004] Chinese patent document CN105343033 B discloses a kind of ibuprofen sustained-release pellets and a preparation method thereof, the ibuprofen sustained-release pellets comprise: drug-containing pills and sustained-release materials coated on the surface of the drug-containing pills, The drug-containing pills include the following components: 55-75 parts of ibuprofen, 15-35 parts of disintegrants, 1-15 parts of fillers, 1-5 parts of binders, the drug-containing pills and slow-release The mass ratio of the materials is 100: (1-5). Through the interaction between the disintegrating agent and the sustained-release material, the drug release rate can be effectively controlled, so that the sustained-release effect of the product is good and stable. The ibuprofen sustained-release pellets 2h The release rate is less than 12%, and the 10h cumulative release rate is greater than 85%. However, for the efficacy of the drug, when the drug enters the body through the carrier coating, it needs to release a large amount of drug in a short period of time to reach a certain concentration before the drug begins to exert its efficacy. Slow release of the drug is required to enhance the long-term effect of the drug. In this patent document, after the drug enters the body, there is a problem that the initial release is too slow

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  • Ibuprofen quick-release and slow-release nanoparticle and preparation method thereof

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Embodiment 1

[0031] The preparation method of described ibuprofen quick-release sustained-release nanoparticles, comprises the steps:

[0032] S1. Dissolving PLGA and a part of ibuprofen in ethanol to obtain an oil phase material; then dissolving carboxymethyl dextran in water, the PLGA copolymer, the carboxymethyl dextran and the part of cloth The mass ratio of profen is 15:3:0.5 to obtain the water phase material;

[0033] S2. Slowly add the oil phase material obtained in step S1 into the water phase material, stir and mix evenly, and then perform shearing and high-pressure homogenization. The shearing conditions are as follows: shear emulsification at 10,000 rpm for 25 minutes The conditions of the high-pressure homogenization are as follows: the homogenization temperature is 20°C, the homogenization pressure is 130 par, and the homogenization is performed twice; the organic solvent is removed to obtain the inner core emulsion of the slow-release layer;

[0034]S3, dissolving the crosc...

Embodiment 2

[0036] The preparation method of described ibuprofen quick-release sustained-release nanoparticles, comprises the steps:

[0037] S1. Dissolve PLGA and a part of ibuprofen in chloroform and ether to obtain an oil phase material; then dissolve carboxymethyl dextran in water, the PLGA copolymer, the carboxymethyl dextran and the The mass ratio of a part of ibuprofen is 18:6:1.0 to obtain the water phase material;

[0038] S2. Slowly add the oil phase material obtained in step S1 into the water phase material, stir and mix evenly, and then perform shearing and high-pressure homogenization. The shearing conditions are as follows: shear emulsification at 12000rpm for 30min The conditions of the high-pressure homogenization are as follows: the homogenization temperature is 25°C, the homogenization pressure is 140 par, and the homogenization is performed 3 times; the organic solvent is removed to obtain the inner core emulsion of the slow-release layer;

[0039] S3, dissolving the s...

Embodiment 3

[0041] The preparation method of described ibuprofen quick-release sustained-release nanoparticles, comprises the steps:

[0042] S1. Dissolve PLGA and a part of ibuprofen in acetone to obtain an oil phase material; then dissolve carboxymethyl dextran in water, the PLGA copolymer, the carboxymethyl dextran and the part of cloth The mass ratio of profen is 20:8:1.5 to obtain the water phase material;

[0043] S2. Slowly add the oil phase material obtained in step S1 into the water phase material, stir and mix evenly, and then perform shearing and high-pressure homogenization. The shearing conditions are as follows: shear emulsification at 15,000 rpm for 35 minutes The conditions of the high-pressure homogenization are as follows: the homogenization temperature is 30°C, the homogenization pressure is 150 par, and the homogenization is performed 4 times; the organic solvent is removed to obtain the inner core emulsion of the slow-release layer;

[0044] S3, dissolving the crospo...

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Abstract

The invention discloses an ibuprofen quick-release and slow-release nanoparticle, the ibuprofen quick-release and slow-release nanoparticle comprises a quick-release layer shell and a slow-release layer core, the slow-release layer core is formed by crosslinking a PLGA (poly (lactic-co-glycolic acid)) copolymer and carboxymethyl glucan, and a part of ibuprofen is wrapped in the slow-release layer core; the surface of the slow-release layer core is coated with the quick-release layer shell, the quick-release layer shell comprises chitosan quaternary ammonium salt, a disintegrating agent and an adhesive, and the other part of ibuprofen is coated between the slow-release layer inner core and the quick-release layer shell; and the ibuprofen quick-release and slow-release nanoparticles prepared by the invention can realize quick release and continuous slow release of ibuprofen, and achieve the effects of quickly taking effect and continuously maintaining effective blood concentration.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical preparations, and in particular relates to an ibuprofen quick-release sustained-release nanoparticle and a preparation method thereof. Background technique [0002] Ibuprofen is a white crystalline powder, insoluble in water, easily soluble in ethanol, chloroform, ether, acetone and other solvents, has a peculiar smell, tasteless, easily soluble in sodium hydroxide or sodium carbonate test solution, and is aromatic Organic acid, reacts easily with alkali and alkaline substances. Due to the presence of carboxyl groups, esterification (or substitution) and neutralization reactions can occur, while the methyl and 2-methylpropyl groups on the benzene ring can be oxidized to carboxyl groups by strong oxidants, and the benzene ring can undergo nitration substitution and catalysis Hydrogenation and other reactions. Ibuprofen is an antipyretic and analgesic, non-steroidal anti-infl...

Claims

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Application Information

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IPC IPC(8): A61K9/54A61K47/36A61K47/34A61K47/38A61K47/32A61K31/192A61P29/00B82Y5/00B82Y30/00B82Y40/00
CPCA61K9/5192A61K9/5161A61K9/5138A61K9/5153A61K31/192A61P29/00B82Y5/00B82Y30/00B82Y40/00
Inventor 詹顺昌罗浩李新宇马桂生邹谨霜王霜
Owner HUAZHONG PHARMA
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