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Preparation for improving release efficiency

A technology of release efficiency and preparation, applied in the field of obeticholic acid dispersible tablets and its preparation, can solve problems such as large fluctuation range of tablet content, migration of soluble components of drugs, and influence on product efficacy, so as to increase solubility and dissolution rate, Enhance drug compliance and improve bioavailability

Inactive Publication Date: 2016-05-04
BEIJING KANG LISHENG PHARMA TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the preparation process of this method, a sufficient amount of organic solvent is required to dissolve it completely, so that the soft material is too soft, and the soluble components of the drug will migrate, resulting in unqualified content uniformity and a wide range of tablet content fluctuations. large, the difference in drug efficacy increases, and the blood pressure cannot be controlled smoothly during treatment, causing the patient's blood pressure to fluctuate
Thereby affecting the curative effect of the product, there is also the problem that the residual organic solvent exceeds the standard

Method used

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  • Preparation for improving release efficiency
  • Preparation for improving release efficiency
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Obeticholic Acid Dispersible Tablets are prepared from the following components, and the dosage is 1000 tablets:

[0028]

[0029] Its preparation method comprises the following steps:

[0030] (1) Take obeticholic acid, dissolve it in absolute ethanol, then add povidone, stir vigorously to dissolve it into a clear and transparent solution, then add Tween, and continue stirring for 0.5-3h to obtain obeticholic acid solution. The obeticholic acid solution is prepared into a dry obeticholic acid solid dispersion by spray drying;

[0031] (2) Gradually add diluent, disintegrant, anti-adhesive agent, lubricant, and glidant by equal-volume incremental method. After repeated sieving and mixing, directly compress into tablets to obtain obeticholic acid dispersible tablets.

[0032] test results:

[0033] Compressibility: good

[0034] Appearance: smooth and beautiful

[0035] Uniformity of dispersion: in compliance with regulations

[0036] Average dissolution rate: 26...

Embodiment 2

[0038]

[0039] Its preparation method comprises the following steps:

[0040] (1) Take obeticholic acid, dissolve it in absolute ethanol, then add povidone, stir vigorously to dissolve it into a clear and transparent solution, then add polyoxyethylene hydrogenated castor oil, and continue stirring for 0.5-3h to obtain obeticholic acid acid solution, the obeticholic acid solution is prepared into a dry obeticholic acid solid dispersion by spray drying;

[0041] (2) Gradually add diluent, disintegrant, anti-adhesive agent, lubricant, and glidant by equal-volume incremental method. After repeated sieving and mixing, directly compress into tablets to obtain obeticholic acid dispersible tablets.

[0042] test results:

[0043] Compressibility: good

[0044] Friability: in compliance with regulations

[0045] Appearance: smooth and beautiful

[0046] Uniformity of dispersion: in compliance with regulations

[0047] Average dissolution rate: 37%

Embodiment 3

[0049]

[0050]

[0051] Its preparation method comprises the following steps:

[0052] (1) Take obeticholic acid, dissolve it in absolute ethanol, then add povidone, stir vigorously to dissolve it into a clear and transparent solution, then add potassium oleate, and continue stirring for 0.5-3h to obtain obeticholic acid solution, The obeticholic acid solution is prepared into a dry obeticholic acid solid dispersion by spray drying;

[0053] (2) Gradually add diluent, disintegrant, anti-adhesive agent, lubricant, and glidant by equal-volume incremental method. After repeated sieving and mixing, directly compress into tablets to obtain obeticholic acid dispersible tablets.

[0054] test results:

[0055] Compressibility: good

[0056] Friability: in compliance with regulations

[0057] Appearance: smooth and beautiful

[0058] Uniformity of dispersion: in compliance with regulations

[0059] Average dissolution rate: 50%

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Abstract

The invention discloses a preparation for improving release efficiency. The preparation takes obeticholic acid as an active pharmaceutical ingredient and povidone as a carrier material, and is prepared into a solid dispersion by adoption of a spray drying technology, and then the solid dispersion is further prepared into a dispersible tablet, so that the solubility and dissolving-out speed of a medicine are increased, the absorption of the medicine in a body is promoted, and the bioavailability of the medicine is improved. The solid dispersion is prepared into the dispersible tablet to enhance the medicine-taking compliance of a patient.

Description

technical field [0001] The invention relates to a preparation for improving release efficiency, in particular to an obeticholic acid dispersible tablet and a preparation method thereof. Background technique [0002] Obeticholic acid, chemical name 6α-ethyl-3α, 7α-dihydroxy-5β-cholan-24-oicacid, common name obeticholic acid, molecular formula: C 26 h 44 o 4 , its structural formula is as follows: [0003] [0004] Obeticholic acid was successfully developed by Intercept Pharmaceutical Company of the United States. It is the first drug developed for the treatment of cholestatic liver disease in two decades. The study was performed in patients who did not respond adequately to or could not tolerate the older standard of care, ursodeoxycholic acid. Obeticholic acid increased levels of two biomarkers associated with reduced risk of liver transplantation in a placebo-controlled phase III trial. [0005] Obeticholic acid is a farnesoid X receptor agonist, which indirectly i...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/575A61K47/32A61P1/16
CPCA61K9/2027A61K31/575
Inventor 程刚
Owner BEIJING KANG LISHENG PHARMA TECH DEV
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