Solid dispersion as well as preparation method and application thereof

A solid dispersion, mass percentage technology, applied in the field of medicine, can solve the problems of thermal decomposition of drugs and carriers, organic solvent residues, restrictions on wide application, etc., and achieve the effect of improving drug solubility, increasing solubility, and reducing dosage

Active Publication Date: 2017-02-22
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Except for the spray drying method, the above preparation methods require the preparation of the drug and the carrier in a molten state. Therefore, for the drug and the carrier with a higher melting point, it is easy to cause the thermal decomposition of the drug and the carrier, thereby limiting the wide application of this method. application
Spray drying has the advantages of strong mixing, good continuous operability, and low process temperature. However, the method of spray drying in the prior art needs to dissolve insoluble drugs in organic solvents first, so it has the disadvantage of organic solvent residues.

Method used

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  • Solid dispersion as well as preparation method and application thereof
  • Solid dispersion as well as preparation method and application thereof
  • Solid dispersion as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0060] Embodiment 1: Spray-drying method prepares diflunisal solid dispersion

[0061] A kind of diflunisal solid dispersion of the present embodiment is prepared by the spray drying method from the raw materials shown in the following table:

[0062]

[0063] Its preparation method specifically comprises the following steps:

[0064] (1) Take diflunisal, surfactant and water-soluble polymer material, mix evenly, add 100ml of secondary water and heat to 70°C in a water bath, stir magnetically until the solution is in a clear state, and obtain a mixed solution containing medicine .

[0065] (2) The obtained mixed solution containing medicine is spray-dried, the inlet air temperature of the spray drying is 120°C, the outlet air temperature is 75°C, and the air volume is 0.7m 3 / min, the atomization pressure is 9kPa, and the liquid flow rate is 2mL / min. During the spray drying process, the temperature of the drug-containing mixed solution is kept at 70°C.

[0066] (3) The s...

Embodiment 2

[0079] Embodiment 2: Spray-drying method prepares piroxicam solid dispersion

[0080] The preparation of a piroxicam solid dispersion in this embodiment is prepared by the spray drying method from the following raw materials: piroxicam as an active ingredient, Soluplus as a surfactant and povidone K25 as a water-soluble polymer material. into, wherein the mass content of piroxicam in the solid dispersion is 10%, and the mass ratio of Soluplus to povidone K25 is 4:6.

[0081] Its preparation method specifically comprises the following steps:

[0082] (1) Take 300mg of piroxicam, 1.08g of Soluplus and 1.62g of povidone K25, mix well, add 100ml of secondary water and heat to 75°C in a water bath, and magnetically stir until the solution is in a clear state to obtain a drug-containing mixed solution .

[0083] (2) The obtained mixed solution containing medicine is spray-dried, the inlet air temperature of the spray drying is 110°C, the outlet air temperature is 70°C, and the air...

Embodiment 3

[0094] Embodiment 3: spray drying method prepares carbamazepine solid dispersion

[0095] A kind of carbamazepine solid dispersion of the present embodiment is prepared by spray-drying method by following raw material: as the carbamazepine of active ingredient, as the Soluplus of surfactant and as the povidone K25 preparation of water-soluble macromolecular material; into, wherein the mass content of carbamazepine in the solid dispersion is 20%, and the mass ratio of Soluplus to povidone K25 is 2:8.

[0096] Its preparation method specifically comprises the following steps:

[0097] (1) Take 600mg of carbamazepine, 480mg of Soluplus and 1.92g of povidone K25, mix well, add 100ml of secondary water and heat to 80°C in a water bath, and magnetically stir until the solution is in a clear state to obtain a mixed solution containing medicine .

[0098] (2) The obtained mixed solution containing medicine is spray-dried, the inlet air temperature of spray drying is 130°C, the outle...

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Abstract

The invention relates to solid dispersion as well as a preparation method and an application thereof. The solid dispersion is prepared from indissolvable drugs, a surfactant and a water-soluble polymer material with a spray drying method after mixing and heating dissolution, wherein the surfactant is selected from at least one of sodium dodecyl sulfate, poloxamer, tween, alpha-tocopherol, succinate, polyethylene glycol, sodium cholate and polyethylene glycol/vinyl caprolactam/vinyl acetate copolymer; the water-soluble polymer material is selected from at least one of povidone, copovidone, hydroxypropyl methylcellulose and polyethylene glycol. An organic solvent is not required when the solid dispersion is prepared with the spray drying method, and the problem of organic solvent residues is solved. By means of the solid dispersion, the dissolvability of the indissolvable drugs is increased, the dissolution speed and the dissolubility are remarkably increased, and the bioavailability of the indissolvable drugs is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a solid dispersion and its preparation method and application. Background technique [0002] Oral administration is the simplest and easiest route of administration. Compared with other oral dosage forms, oral solid preparations have unique advantages, such as good stability of physical and chemical properties, simple production process, convenient taking and carrying, and accurate dosage. Oral solid dosage forms are the preferred drug delivery method for most new chemical entities under development. However, it is required to be effectively absorbed after oral administration and to produce a reproducible plasma concentration. Because the drug must be dissolved in the body before it can pass through the biofilm and be absorbed into the blood circulation to obtain ideal bioavailability. According to surveys, the proportion of BCS II drugs in the marketed drugs is 30%, and this...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/34A61K47/38A61K45/00A61K31/603A61K31/5415A61K31/55A61K31/343A61K31/496
CPCA61K45/00A61K9/1635A61K9/1641A61K9/1652A61K31/5415A61K31/55A61K31/496A61K31/343A61K31/603
Inventor 吴传斌冯地桑潘昕权桂兰黄莹陈航平
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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