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Preparation method for obeticholic acid liposome tablets

A technology of obeticholic acid lipid and obeticholic acid lipid, which is applied in the field of preparation of obeticholic acid liposome tablets, and can solve the problem of increasing differences in drug efficacy, affecting product efficacy, and large fluctuation range of tablet content. question

Inactive Publication Date: 2020-03-10
HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, during the preparation process of this method, the fluctuation range of the tablet content is relatively large, and the drug effect difference increases.
thereby affecting the efficacy of the product

Method used

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  • Preparation method for obeticholic acid liposome tablets
  • Preparation method for obeticholic acid liposome tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation prescription of obeticholic acid liposome tablet:

[0035] Obeticholic Acid 5g

[0036] Lecithin 35g

[0037] Cholesterol 20g

[0038] Microcrystalline Cellulose 15g

[0039] Croscarmellose Sodium 1g

[0040] povidone k30 1g

[0041] Magnesium stearate 0.5g

[0042] Makes 1000 pieces

[0043] Its preparation method comprises the following steps:

[0044] Dissolve obeticholic acid in 20ml of ethanol, lecithin and cholesterol in 100ml of ethanol and chloroform (1:1) mixed solvent, then mix the two solutions evenly, heat and stir at 60°C for 2 hours, and then use a rotary evaporator The organic solvent was removed to obtain obeticholic acid liposomes, which were pulverized and passed through an 80-mesh sieve.

[0045] Mix the prepared obeticholic acid liposomes, microcrystalline cellulose, and croscarmellose sodium evenly, add 5% povidone K30 solution, make wet granules, dry, granulate, add stearin Magnesium acid mixed, pressed into tablets.

Embodiment 2

[0047] Preparation prescription of obeticholic acid liposome tablet:

[0048] Obeticholic Acid 10g

[0049] Lecithin 70g

[0050] Cholesterol 40g

[0051] Microcrystalline Cellulose 30g

[0052] Lactose 20g

[0053] Low-substituted hydroxypropyl cellulose 2g

[0054] Hypromellose 2g

[0055] Magnesium Stearate 1g

[0056] Makes 1000 pieces

[0057] Its preparation method comprises the following steps:

[0058] Dissolve obeticholic acid in 40ml of ethanol, lecithin and cholesterol in 200ml of ethanol and chloroform (1:1) mixed solvent, then mix the two solutions evenly, heat and stir at 60°C for 2 hours, and then use a rotary evaporator The organic solvent was removed to obtain obeticholic acid liposomes, which were pulverized and passed through an 80-mesh sieve.

[0059] Mix the prepared obeticholic acid liposomes, microcrystalline cellulose, lactose, and low-substituted hypromellose evenly, add 5% hypromellose solution, make wet granules, dry, granulate, add hard ...

Embodiment 3

[0061] Preparation prescription of obeticholic acid liposome tablet:

[0062] Obeticholic Acid 25g

[0063] Lecithin 150g

[0064] Cholesterol 75g

[0065] Microcrystalline Cellulose 70g

[0066] Mannitol 50g

[0067] Crospovidone 5g

[0068] povidone k30 5g

[0069] Magnesium Stearate 2.5g

[0070] Makes 1000 pieces

[0071] Its preparation method comprises the following steps:

[0072] Dissolve obeticholic acid in 100ml of acetone, lecithin and cholesterol in 500ml of ethanol and chloroform (1:1) mixed solvent, then mix the two solutions evenly, heat and stir at 60°C for 2 hours, and then use a rotary evaporator The organic solvent was removed to obtain obeticholic acid liposomes, which were pulverized and passed through an 80-mesh sieve.

[0073]Mix the prepared obeticholic acid liposomes, microcrystalline cellulose, mannitol, and crospovidone evenly, add 5% povidone K30 solution, make wet granules, dry, granulate, add stearin Magnesium acid mixed, pressed into ...

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Abstract

The invention discloses a preparation method for obeticholic acid liposome tablets, which is characterized in that the obeticholic acid liposome is composed of obeticholic acid, lecithin and cholesterol, and then the obeticholic acid liposome and proper auxiliary materials are prepared into the obeticholic acid liposome tablet. The obeticholic acid liposome contains the following components: 1 part of obeticholic acid, 5-10 parts of lecithin and 1-5 parts of cholesterol. The obeticholic acid liposome tablet comprises the following components in parts by weight: 1 part of obeticholic acid liposome, 1-5 parts of filler, 0-0.5 part of disintegrating agent, 0-0.5 part of adhesive and 0-0.2 part of lubricant. According to the technical scheme, by utilizing the advantages of the liposome, the drug absorption and utilization of obeticholic acid are improved, and the dosage can be effectively reduced.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. Specifically, the invention relates to a preparation method of obeticholic acid liposome tablets. Background technique [0002] Obeticholic acid is a farnesoid X receptor agonist, which indirectly inhibits the gene expression of cytochrome 7A1 (CYP7A1) by activating farnesoid X receptor. Since CYP7A1 is the rate-limiting enzyme of bile acid biosynthesis, obeticholic acid can inhibit bile acid synthesis for the treatment of primary biliary cirrhosis and nonalcoholic fatty liver disease. Obeticholic acid was successfully developed by Intercept Pharmaceuticals, Inc. in the United States. In May 2014, the US FDA granted Intercept Pharmaceuticals a fast track approval for obeticholic acid. Obeticholic acid is the first drug developed for the treatment of cholestatic liver disease in 20 years, and it is also the second drug approved by the FDA for the treatment of primary biliary c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/127A61K47/28A61K47/38A61K31/575A61P1/16
CPCA61K9/127A61K9/2054A61K9/2077A61K31/575A61K47/28A61P1/16
Inventor 沙薇黄普广李晨希
Owner HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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