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Apremilast sustained-release preparation and preparation method thereof

A sustained-release preparation, the technology of Apremilast, applied in pill delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of psoriasis patients being unsuitable, affecting curative effect, and side effects of steroid hormones

Pending Publication Date: 2020-10-27
SHANGHAI JINGXIN BIOLOGICAL MEDICAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] For the treatment of psoriasis patients on the market, local psoriasis drugs are used, but there are the following limitations: 1. It is not suitable for those with large skin lesions; 2. It is not suitable for patients with intractable localized psoriasis; 3. The dosage It is difficult to standardize and affect the curative effect; 4. Local steroid hormones are easy to withdraw due to side effects, and the condition is prone to rebound after drug withdrawal (safety issue)
The release rate of the tablet or capsule prepared according to the described method is not smooth enough, and the release amount is not constant
[0008] WO2013119607 discloses a sustained-release pharmaceutical composition using high-molecular polymers such as hydroxypropyl cellulose as a sustained-release matrix material. The release rate of the sustained-release drug exhibits a linear relationship and cannot achieve a good sustained-release release effect.

Method used

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  • Apremilast sustained-release preparation and preparation method thereof
  • Apremilast sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Described loaded pill prescription is as follows:

[0061] Table 1 Apremilast loaded pill prescription

[0062] composition Dosage (mg / capsule) APIs 60 HPMC E5 32 Absolute ethanol 666.7 Micropowder silica gel 1.7 water 608 blank core 200

[0063] Remarks: Solvents are removed during the coating process.

[0064] The preparation process of drug-loaded pellet coating solution is as follows:

[0065] (1) 5% HPMC E5 solution preparation: take the prescription amount HPMC E5 and add water and stir to make it dissolve completely;

[0066] (2) API grinding: Weigh the prescribed amount of API in a mortar, add a little 5% HPMC E5 solution and grind it into a paste;

[0067] (3) Transfer: After transferring (2) to a beaker, add the remaining 5% HPMC E5 solution to dilute and rinse the mortar;

[0068] (4) Mixing: add the prescribed amount of absolute ethanol and micropowder silica gel and stir overnight to make it fully mixed...

Embodiment 2

[0096] The formulation of the drug-loaded pill, the preparation process of the drug-loaded pellet coating solution, the preparation process of the sustained-release component coating solution, the formulation of the enteric-coated layer, the preparation process of the enteric-coated layer coating solution, and the preparation method of the Apremilast sustained-release preparation Same as Example 1; the difference lies in the sustained-release components, wherein the sustained-release pellets are composed of sustained-release pellets I and sustained-release pellets II, and the sustained-release pellets I and the sustained-release pellets II The weight ratio is 1:2;

[0097] The preparation process of the coating liquid in the described slow-release component I is as follows (there is no porogen in the slow-release component coating liquid):

[0098] Weigh 38.40 g of Surelease water dispersion (solid content 25%), add 25.60 g of purified water and stir to dilute to 15% solid con...

Embodiment 3

[0124] The formulation of the drug-loaded pill, the preparation process of the drug-loaded pellet coating solution, the preparation process of the sustained-release component coating solution, the formulation of the enteric-coated layer, the preparation process of the enteric-coated layer coating solution, and the preparation method of the Apremilast sustained-release preparation Same as Example 1; the difference lies in the slow-release component coating liquid, the weight ratio of the water dispersion and the porogen in the slow-release component coating liquid is 95.5:4.5; the specific preparation process is as follows:

[0125] Weigh 38.2 g of Surelease aqueous dispersion (solid content 25%), add 9 g of 5% HPMC E5 solution and 40 g of purified water and stir to dilute to obtain the coating solution of sustained release component.

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Abstract

The invention discloses an apremilast sustained-release preparation. An FDA apremilast dissolution assay method is adopted to perform measurement; and obtained sustained release has the characteristics that 40-50 wt% of apremilast is released after 2 hours, 50-70 wt% of apremilast is released after 4 hours, 75-85 wt% of apremilast is released after 12 hours and 85-90 wt% of apremilast is releasedafter 16 hours. The sustained-release preparation can prolong acting time, reduce the frequency of administration and enhance the medication compliance of patients; the blood medicine concentration can be more stable, so that anti-inflammatory and analgesic effects can be achieved; and sustained-release effects can achieve 16 hours, so that the sustained-release preparation is high in product stability, and has high clinical application values and excellent effects.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an apremilast sustained-release preparation and a preparation method thereof. Background technique [0002] Apremilast, chemical name N-[2-[(1S)-1(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-2H -1,3-Dioxy-1H-isoindol-4-yl]acetamide. [0003] Apremilast can inhibit the production of various pro-inflammatory mediators (PDE-4, TNF-α, IL-2, interferon r, leukotrienes, NO synthase) to play an anti-inflammatory effect; phosphodiesterase 4 ( PDE4) selective inhibitors, in addition to being approved for psoriatic arthritis, FDA approved in September 2014 for the treatment of patients with moderate to severe plaque psoriasis with phototherapy or systemic therapy; it is the first and only approved use A PDE4 inhibitor for the treatment of plaque psoriasis; clinical trials have shown that OTEZLA can reduce erythema, thickening and desquamation in patients with moderat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4035A61P17/06A61P19/02
CPCA61K31/4035A61K9/2866A61K9/2886A61P19/02A61P17/06
Inventor 黄悦朱丹
Owner SHANGHAI JINGXIN BIOLOGICAL MEDICAL