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Alfacalcidol sustained-release granule and preparation method thereof

A technology of alfacalcidol and sustained-release granules, which is applied in bone diseases, medical formulas, medical preparations of non-active ingredients, etc., and can solve the problems of absorption, unsatisfactory treatment effect, short administration time interval, and blood drug concentration. Large fluctuations and other problems, to achieve the effect of stable product quality, reduced dosage, and convenient administration

Active Publication Date: 2013-06-12
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Alfacalcidol products produced by Danish Leo Pharmaceutical Company are currently the most sold in the world. my country has domestically produced products on the market since 1997. At present, there are mainly tablets and capsules of alfacalcidol in the domestic market. Monotonous and ordinary, affected by factors such as disintegration and drug release, short dosing intervals, large fluctuations in effective blood drug concentration, unsatisfactory absorption and therapeutic effects

Method used

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  • Alfacalcidol sustained-release granule and preparation method thereof
  • Alfacalcidol sustained-release granule and preparation method thereof
  • Alfacalcidol sustained-release granule and preparation method thereof

Examples

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Effect test

preparation example Construction

[0021] A preparation method for alfacalcidol sustained-release granules, comprising the following steps:

[0022] (1) Mix alfacalcidol and filler evenly, and use 85% ethanol as a binder to make immediate-release granule cores with 10-14 meshes for later use;

[0023] (2) Dissolving the slow-release material, plasticizer, porogen, and anti-tack agent with 80% ethanol to make a slow-release coating solution;

[0024] (3) Evenly spray the formulated sustained-release coating solution on the surface of the immediate-release granule core prepared in step (1), and dry to obtain alfacalcidol sustained-release granules.

Embodiment 1～4

[0025] Preparation of Examples 1-4 Alfacalcidol Sustained Release Granules

[0026] According to the raw and auxiliary materials in the following table, the alfacalcidol sustained-release granules of four examples were prepared according to the above-mentioned preparation method. Among them, " / " means not used.

[0027]

[0028] Test Example 1 Determination of Release of Alfacalcidol Sustained-release Granules Gained in Examples 1-4

[0029] According to the "Guidelines for Sustained and Controlled Release Preparations" in the appendix of the 2010 edition of the Pharmacopoeia of the People's Republic of China (Part II), 0.25% sodium lauryl sulfate was used as the release medium, and the preparations in Examples 1 to 4 were accurately weighed. The appropriate amount of alfacalcidol sustained-release granules (about 100 mg) was determined according to the first method of appendix XD of "Pharmacopoeia of the People's Republic of China" 2010 edition, and the peak area was dete...

Embodiment 5～7

[0034] Embodiments 5-7 Preparation of alfacalcidol sustained-release granules

[0035] According to the raw and auxiliary materials in the following table, according to the above-mentioned preparation method, alfacalcidol sustained-release granules were prepared in each embodiment. The weight ratio of the slow-release material of embodiment 5 and the plasticizer is 4:1, the weight ratio of the slow-release material of embodiment 6 and the plasticizer is 3:1, and the weight ratio of the slow-release material of embodiment 7 and the plasticizer The weight ratio is 2:1.

[0036]

[0037] Test Example 2 Determination of release rate of alfacalcidol sustained-release granules obtained in Examples 5-7

[0038] The measuring method is the same as that of Test Example 1. The measurement results are shown in Table 2.

[0039] Table 2 Examination of the Release Rate of Alfacalcidol Sustained-release Granules in Examples 5-7 (Dissolution Medium: 0.25% Sodium Lauryl Sulfate...

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Abstract

The invention discloses an alfacalcidol sustained-release granule and a preparation method thereof. The alfacalcidol sustained-release granule disclosed by the invention consists of a quick-release granule core and a sustained-release coating layer, wherein the quick-release granule core consists of alfacalcidol and filler, and the sustained-release coating layer consists of a sustained-release material, a plasticizer, a pore-forming agent and an antisticking agent; and during preparation, the alfacalcidol sustained-release granule is obtained through coating the sustained-release coating layer outside the quick-release granule core. According to the alfacalcidol sustained-release granule and the preparation method of the alfacalcidol sustained-release granule, the drug is convenient in taking and slow in release, the aims of long acting and curative effect improving can be reached, and the dosage can be reduced while the same drug action is maintained, so that side effects to patients caused by drug taking are reduced; and the preparation method is simple, the quality of obtained products is stable, and thus, the method is applicable to large-scale production application.

Description

technical field [0001] The invention relates to the technical field of western medicine preparations, in particular to alfacalcidol sustained-release granules, and also relates to a preparation method of the sustained-release granules. Background technique [0002] The chemical name of alfacalcidol is 9,10-cyclocholesteryl-5Z,7E,10(19)-triene-1α,3β-diol, which was first developed by Bone Health International Corporation of the United States, and has been established in Israel ( 1979), Germany (1979), Japan (1982), Italy (1985) were approved for marketing. Alfacalcidol is mostly used for calcium metabolism disorders caused by vitamin D metabolic disorders, clinically used for the treatment of osteoporosis, chronic renal insufficiency, hypothyroidism, anti-vitamin D rickets, osteomalacia, etc. Alfacalcidol products produced by Danish Leo Pharmaceutical Company are currently the most sold in the world. my country has domestically produced products on the market since 1997. At ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/593A61K47/12A61K47/14A61P3/14A61P19/10A61P13/12A61P5/14A61P19/08
Inventor 王明刚陈阳生任莉
Owner CP PHARMA QINGDAO CO LTD
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