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A kind of pharmaceutical composition containing uric acid transport protein inhibitor and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of dissolution and the decrease of the dissolution rate of pharmaceutical compositions, etc.

Active Publication Date: 2021-10-08
FUJIAN SHENGDI PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The researchers found that after 1-((6-bromoquinolin-4-yl)thio)cyclobutylcarboxylic acid or its pharmaceutically acceptable salt was prepared into a solid pharmaceutical composition, the dissolution rate of the pharmaceutical composition decreased after long-term storage, and at the same time, The composition has the characteristics of easy degradation, even if the prepared pharmaceutical composition is placed under very harsh storage conditions, it is still unavoidable
For this reason, the present invention provides a kind of pharmaceutical composition that contains uric acid transporter (URAT1) inhibitor, solves the problem that contains uric acid transporter inhibitor 1-((6-bromoquinolin-4-yl)thio)cyclobutylcarboxylic acid Dissolution and stability problems after long-term placement of its pharmaceutically acceptable salts

Method used

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  • A kind of pharmaceutical composition containing uric acid transport protein inhibitor and preparation method thereof
  • A kind of pharmaceutical composition containing uric acid transport protein inhibitor and preparation method thereof
  • A kind of pharmaceutical composition containing uric acid transport protein inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The active pharmaceutical ingredient 1-((6-bromoquinolin-4-yl)thio)sodium cyclobutanate is mixed with lactose and microcrystalline cellulose, and then respectively mixed with low-substituted hydroxypropyl cellulose and cross-linked polyvinylpyrrolidone , sodium carboxymethyl starch and croscarmellose sodium are mixed, the binder is polyvinylpyrrolidone K30 aqueous solution, the granules are prepared by a high-speed shear granulation process, and then the granules are dried, sieved, and then mixed with stearin Magnesium acid is mixed evenly and pressed into tablets. See Table 1 for specific data.

[0050] Table 1

[0051]

[0052] Put the tablets prepared in Experimental Examples 1 to 4 into aluminum foil bags, place them under the condition of 40°C / RH75%, and take samples at 0, 1, 2, and 3 months to determine the dissolution rate and impurity A content of the tablets in 45 minutes , to investigate the stability of the tablet. The results are shown in Table 2.

[...

Embodiment 2

[0057] The active pharmaceutical ingredient 1-((6-bromoquinolin-4-yl)sulfanyl) sodium cyclobutanate is mixed with mannitol and microcrystalline cellulose, the binder is polyvinylpyrrolidone K30 aqueous solution, and a fluidized bed is used for one step The granulation process produces granules which are then dried and sieved. The prepared granules are respectively mixed with low-substituted hydroxypropyl cellulose and cross-linked polyvinylpyrrolidone, then mixed with magnesium stearate and uniformly pressed into tablets. See Table 3 for the tablet compositions of Experimental Examples 5 to 6.

[0058] table 3

[0059]

[0060] The tablets prepared in Experimental Examples 5 and 6 were put into aluminum foil bags, placed under the condition of 40°C / RH75%, and the 45-minute dissolution rate and related substances of the tablets were sampled and determined in 0 and January, and the properties of the tablets were investigated. stability. The results are shown in Table 4.

...

Embodiment 3

[0065] The active pharmaceutical ingredient 1-((6-bromoquinolin-4-yl)thio)sodium cyclobutanate is mixed with lactose and microcrystalline cellulose, respectively mixed with low-substituted hydroxypropyl cellulose and cross-linked polyvinylpyrrolidone , and then mixed with talcum powder and magnesium stearate evenly and compressed into tablets. See Table 5 for the tablet compositions of Experimental Examples 7 to 8.

[0066] table 5

[0067]

[0068] The tablets prepared in Experimental Examples 7 and 8 were put into aluminum foil bags, placed under the condition of 40°C / RH75%, and samples were taken in 0 and January to determine the dissolution rate and related substances of the tablets in 45 minutes, and the properties of the tablets were investigated. stability. The results are shown in Table 6.

[0069] Table 6

[0070]

[0071] The above results show that during the stability test, when low-substituted hydroxypropyl cellulose is selected for use in the pharmaceut...

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Abstract

The invention relates to a pharmaceutical composition containing a uric acid transport protein inhibitor and a preparation method thereof. Specifically, the pharmaceutical composition contains 1-((6-bromoquinolin-4-yl)thio)cyclobutanecarboxylic acid or a pharmaceutically acceptable salt thereof, and low-substituted hydroxypropyl cellulose, and the pharmaceutical composition The product has good dissolution rate and excellent stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a pharmaceutical composition containing a uric acid transporter (URAT1) inhibitor. Background technique [0002] In recent years, with the improvement of economic and living standards, the prevalence of gout has increased year by year, and the age of onset has shown a trend of younger age. It is more common in men and menopausal women, and the peak incidence is at the age of 40-50. Its clinical manifestations are hyperuricemia, recurrent gouty acute arthritis, tophi deposition, characteristic chronic arthritis and joint deformities, often involving the kidneys and causing chronic interstitial nephritis and renal uric acid stones. The prerequisite for the onset of gout is hyperuricemia, that is, at 37°C, the saturation concentration of serum uric acid is about 420umol / L (70mg / L), and a value higher than this value is hyperuricemia. However, only a part of patients with hyperuricem...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/48A61K47/38A61K31/47A61P19/06
CPCA61K9/2054A61K9/4866A61K31/47
Inventor 奚宏磊陈茜史皓如潘晓晨
Owner FUJIAN SHENGDI PHARM CO LTD
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