Ursodesoxycholic acid capsule and preparation method thereof

A technology of ursodeoxycholic acid and capsules, which is applied in the field of ursodeoxycholic acid capsules and its preparation, can solve the problems of great influence on the viscosity of starch slurry, differences between product batches, and high granule strength, and achieve easy control of granule size, The effect of small batch-to-batch variation and uniform particle size

Pending Publication Date: 2020-05-12
安士制药(中山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Starch is used as a binder in this prescription, and starch slurry needs to be prepared during the production process. It needs to be boiled at high temperature or boiled in boiling water. There is a risk of high temperature burns during the production process. At the same time, the difference in the preparation of starch slurry affects the viscosity of starch slurry Large, there will be batch-to-batch variation in the prepared product
Moreover, the traditional high-efficiency wet granulator produces the required granules through high-speed shearing and stirring, but there are problems such as high granule hardness, high granule strength, and difficult granulation.

Method used

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  • Ursodesoxycholic acid capsule and preparation method thereof
  • Ursodesoxycholic acid capsule and preparation method thereof
  • Ursodesoxycholic acid capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The impact of embodiment 1 different processes on product stripping

[0048] In this example, under the condition that the components and dosage of ursodeoxycholic acid capsules are the same, the influence of different production processes on the dissolution of the product is studied. The specific process parameters are shown in Table 1.

[0049] Table 1 List of different granulation process parameters

[0050]

[0051] Determination of the dissolution curves of ursodeoxycholic acid capsules prepared according to the above-mentioned granulation process and the reference preparation Ursifer, and using the similarity factor f 2 The evaluation results are shown in Table 2.

[0052] Table 2 Dissolution curve data of different production processes

[0053]

[0054] Result analysis:

[0055] Powder mixed directly: the content density is low, so it needs to be filled with 00# capsules, the capsules are too big to be swallowed, and the dissolution profile is not simila...

Embodiment 2

[0059] The impact of embodiment 2 different raw material particle diameters on product stripping

[0060] In this example, under the condition that the components and dosages of ursodeoxycholic acid capsules are the same, the effect of different raw material particle sizes on the dissolution of the product is studied. The specific raw material particle size parameters are shown in Table 3.

[0061] Table 3 List of particle sizes of different raw materials

[0062]

[0063] The preparation method of the ursodeoxycholic acid capsule of the present embodiment comprises the following steps:

[0064] (1) Add ethanol to purified water, add povidone K30 after mixing, stir until the povidone K30 is completely dissolved, the solution is in a clear state, and an adhesive solution is obtained, which is set aside;

[0065] (2) The ursodeoxycholic acid raw material is passed through a 20-mesh sieve, the microcrystalline cellulose and lactose are passed through a 40-mesh sieve, and set ...

Embodiment 3

[0073] The influence of embodiment 3 different fillers on product stripping

[0074] To study the influence of different fillers on product dissolution, the specific prescription of the contents of ursodeoxycholic acid capsules is shown in Table 5.

[0075] Table 5 List of prescriptions for different fillers

[0076]

[0077]

[0078] The preparation method of ursodeoxycholic acid capsules with different fillers in this embodiment comprises the following steps:

[0079] (1) Add ethanol to purified water, add povidone K30 after mixing, stir until the povidone K30 is completely dissolved, the solution is in a clear state, and an adhesive solution is obtained, which is set aside;

[0080] (2) Raw materials of ursodeoxycholic acid with a size of 18μm≤d50≤50μm and 80μm≤d90≤250μm were passed through 20 meshes, lactose from prescription 6, mixture of microcrystalline cellulose and lactose from prescription 7, and microcrystalline cellulose from prescription 8 were all passed t...

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Abstract

The invention discloses an ursodesoxycholic acid capsule and a preparation method thereof. The ursodesoxycholic acid capsule comprises a content and a capsule shell, wherein the content comprises ursodesoxycholic acid, filling agents, an adhesive and lubricants; the filling agents are microcrystalline cellulose and lactose; the adhesive is povidone K30; and the lubricants are magnesium stearate and silicon dioxide. The ursodesoxycholic acid capsule is obtained by mechanically crushing an ursodesoxycholic acid raw material, the raw material does not need to be micronized, the process is simpleand controllable, types and amounts of the filling agents and the lubricants are optimally selected, parameters of a one-step pelletizing process are optimized, and the prepared ursodesoxycholic acidcapsule product is good in dissolution, small in inter-batch difference and stable in quality, and has dissolution behaviors identical to those of a reference parameter, namely Ursofalk, in five different mediums of a hydrochloric acid solution of which the pHvalue is 1.2, an acetate buffer of which the pH value is 4.5, a phosphate buffer of which the pH value is 6.8, a phosphate buffer of which the pH value is 7.2 and a phosphate buffer of which the pH value is 7.5.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to ursodeoxycholic acid capsules and a preparation method thereof. Background technique [0002] Ursodeoxycholic acid (Ursodeoxycgolic acid, UDCA), is the main component of bear bile, its chemical name is (3α, 7β)-dihydroxy-5β cholic acid, which is the 7-hydroxy difference of chenodeoxycholic acid (Chenodeoxycholic acid) to isomers. Since it was discovered in the 1980s that ursodeoxycholic acid can effectively dissolve cholesterol gallstones, new studies have shown that ursodeoxycholic acid has a positive effect on gallbladder benefit and liver protection. In recent years, it has been reported abroad that UDCA not only has a good effect on the treatment of primary biliary cirrhosis, primary sclerosing cholangitis, and chronic active hepatitis, but also can be used to treat chronic hepatitis and rejection after liver transplantation. Ursodeoxycholic acid can inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/575A61K47/38A61K47/32A61K47/26A61K47/04A61P1/16
CPCA61K9/4866A61K9/4858A61K9/485A61K31/575A61P1/16
Inventor 张俊林李静阮琼婷刘晓敏
Owner 安士制药(中山)有限公司
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