Superfine Iguratimod powder and quick released oral preparation

A technology of powder and speed, applied in the field of insoluble drug Iilamod crystalline micropowder, can solve the problems of fine crystals and too late to grow, and achieve the effect of reducing drug particle size, increasing surface area and improving bioavailability

Inactive Publication Date: 2010-05-12
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the drug solution is poured into a large amount of insoluble solvent, because the solution is very dilute, although a large number of crystal nuclei are formed, it is too late to grow, so the precipitated crystals are very fine.

Method used

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  • Superfine Iguratimod powder and quick released oral preparation
  • Superfine Iguratimod powder and quick released oral preparation
  • Superfine Iguratimod powder and quick released oral preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of Airamod Crystalline Micropowder

[0037] Take 1.0g of the raw material of iguratimod and add 17.5ml of dimethylformamide to dissolve it, slowly (or drop it) into 500ml of water, add dropwise and stir at the same time, the stirring speed is 800r / min, iguratimod will precipitate and disperse immediately In the water. Filter, stir wash three times with distilled water, filter, and dry at 60°C for 2 hours. The above-mentioned powder was taken for powder X-ray diffraction measurement and powder particle size inspection, and the average particle size of the above-mentioned powder was about 4 μm. The yield was 97.5%. Powder X-ray Diffraction Pattern See figure 1 .

Embodiment 2

[0039] Preparation of Aguratimod Immediate Release Tablets (1000 Tablets):

[0040] Formulation composition Sample 1 Sample 2 Sample 3

[0041] Alamode Micronized Powder 25g 25g 25g

[0042] Lactose 50g 25g 50g

[0043] Microcrystalline Cellulose 50g 50g 25g

[0044] Mannitol / 37.5g /

[0045] Croscarmellose Sodium 20g 20g 24g

[0046] Sodium lauryl sulfate 4.5g 5g /

[0047] Povidone K30 appropriate amount appropriate amount

[0048] Magnesium Stearate 3g 3g 2.3g

[0049] Preparation Process:

[0050] (1) Crush the raw materials and auxiliary materials and pass through a 200-mesh sieve respectively, and set aside.

[0051] (2) In addition to povidone K30 and magnesium stearate, weigh the prescription amount according to the prescription, mix evenly with a 60 mesh sieve, add 10% PVP-K30 solution to make soft materials, granulate with a 30 mesh sieve, and dry at 60°C for 2 hours .

[0052] (3) Get above-mentioned granule, add the magnesium stearate of recipe quantity...

Embodiment 3

[0058] A pharmacokinetic study in Beagle dogs compared the in vivo release profile of Sample 1 with conventional tablets.

[0059] The trial employed 6 individuals and blood samples were collected at regular intervals and analyzed for iguratimod. The result is as follows:

[0060]

[0061] Results: The above pharmacokinetic parameters showed that the peak concentration (Cmax) and area under the curve (AUC) of sample 1 were significantly higher than those of conventional tablets, and the statistically significant difference was significant, and the bioavailability was significantly improved; the time to peak (Tpeak) was 1 Hours, but statistically insignificant; elimination rate constant (Ke) and elimination half-life (T 1 / 2Ke ) There was no difference between the two formulations.

[0062] The (Beagle dog) drug concentration-time curves of sample 1 and conventional tablets are shown in image 3 .

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Abstract

The present invention relates to the micronizing technology for insoluble polycrystal medicine Iguratimod, and the micronized Iguratimod has new crystallization and powder size of 1-10 microns. The orally taken quick release preparation with micronized Iguratimod as active component, high efficiency disintegrant, surfactant, diluent, etc has obviously improved in vitro leaching rate and in vivo absorption rate, and obviously raised bioavailability.

Description

technical field [0001] The invention relates to an insoluble drug iguratimod crystalline micropowder, a crystal form and a preparation method, an iguratimod immediate-release preparation, and a preparation method of the immediate-release preparation. Background technique [0002] According to the figures provided by the World Health Organization, there are currently about 350 million arthritis patients in the world, and the United States accounts for about 11.4%; while the global rheumatoid arthritis patients account for 1%. my country is a country with high incidence of rheumatism and rheumatoid. According to the survey by the Ministry of Health, due to climate, living standards and other issues, a total of 10 million people in my country suffer from rheumatism and rheumatoid diseases to varying degrees, and the incidence rate ranks among the highest in the world. This disease shows effect repeatedly, and is known as the title of "undead cancer", which brings long-term and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K9/14A61P29/00A61P19/02
Inventor 王杏林高晶梅林雨刘昌孝
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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