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Novel controlled release-niacin formulation

A technology for controlled-release preparations and niacin, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc. Irregular release patterns, etc.

Inactive Publication Date: 2009-03-11
SEOUL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in known controlled-release formulations of niacin, the water-soluble matrix releases the active ingredient, niacin, due to irregular erosion
Therefore there are disadvantages in this formulation that it cannot maintain its own shape resulting in an irregular release pattern, an increased risk of unanticipated drug release leading to unwanted side effects of niacin, release of the active ingredient Might be done before the time required and stable bioavailability cannot be expected at each time point and in each formulation and patient
Despite the above problems, only sustained-release formulations of niacin are disclosed, wherein polymers such as HPMC and / or carboxyvinyl polymers or mixtures thereof are used alone to form a water-soluble matrix, thereby delaying the release of the drug, And there is no mention of a method of maintaining the shape of the matrix for the required period of time

Method used

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Examples

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preparation example Construction

[0048] When preparing the niacin controlled-release preparation of the present invention, the solvent added to the powder mixture includes all solvents that do not affect the activity of the active ingredient niacin, and is usually used in the preparation of granules. This solvent is known in the prior art. Examples thereof may include one or a mixture selected from the group consisting of water, ethanol, isopropanol, glycerol, propylene glycol, and polyethylene glycol, but are not limited thereto. As the liquid solvent, ethanol or a mixed solvent of water and ethanol is preferably used. At this time, when the solvent is water alone or a mixed solvent of water and ethanol, based on the total weight of the drug, the solvent is preferably used in an amount of 5 to 40% by weight, more preferably 10 to 23% by weight. In addition, in a preferred embodiment, the preparation method of the present invention may further include a step of mixing an adhesive in step (a).

[0049] In a specif...

Embodiment 1

[0053] Example 1: Swelling reagents for different types of polymer substrates

[0054] Perform different types of polymer-based swelling reagents to observe whether the niacin preparation of the present invention releases the drug within the required time period, and maintains its matrix shape during the drug release process.

[0055] Specifically, niacin preparations were prepared according to the following preparation examples 1 to 4.

[0056] Preparation example 1 (No. 46)

[0057] Mix 500.0 mg of niacin as a drug, 90 mg of lactose as an excipient, and 90 mg of microcrystalline cellulose to increase the fluidity of the drug. 170 mg of HPMC2208 (100,000 cps) as a polymer base was added to the powder mixture and mixed uniformly. Subsequently, 0.01 ml of ethanol was sprayed to prepare wet granules.

[0058] The prepared particles were dried in an oven at 60°C and then uniformly ground. Subsequently, 16 mg of magnesium stearate was mixed for the molding of the formulation. Tabl...

Embodiment 2

[0070] Example 2: Comparative dissolution experiment of a commercial formulation and the formulation of the present invention

[0071] A dissolution experiment was conducted to confirm whether the controlled-release niacin formulation and commercial sustained-release formulation of the present invention can maintain their matrix shape for the required time period (24 hours or longer). According to the present invention, a niacin controlled-release preparation containing 500 mg of niacin (components: 500 mg of niacin, 90 mg of lactose, 90 mg of microcrystalline cellulose, 170 mg of HPMC, and 16 mg of magnesium stearate) and commercial cigarettes Acid sustained-release preparation, Niaspanor TM The swelling experiment was carried out at 37°C at 50 rpm and 900 ml of water for 24 hours. The dissolution experiment was performed using the dissolution experiment equipment PT4005956 produced by Pharma Experimental Plant (Germany) and the stirring method of the United States Pharmacopoei...

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Abstract

The present invention relates to a controlled-release niacin formulation. In particular, the present invention relates to a controlled-release niacin formulation, comprising niacin; hydroxypropyl methylcellulose; and a carboxyvinyl polymer, in which the carboxyvinyl polymer and hydroxypropyl methylcellulose are contained in a predetermined weight ratio, and to a preparation method thereof. The controlled-release niacin formulation according to the present invention maintains its matrix shape until completion of release, and maintains its release pattern without fluctuation for a desired time period, unlike a commercial formulation. In particular, since niacin formulations are used for long-term treatment of hyperlipidemia, the controlled-release niacin formulation of the present invention, capable of maintaining effective blood concentration and high stability for a long period of time, is very useful.

Description

Technical field [0001] The invention relates to a controlled-release oral preparation of niacin. In particular, the present invention relates to a niacin controlled-release preparation comprising niacin for the treatment of hyperlipidemia; hydroxypropyl methylcellulose; and carboxyvinyl polymer, wherein when administered orally, the The carboxypropyl methyl cellulose absorbs water to form a water-soluble matrix system to control the release of drugs, the carboxyvinyl polymer controls the release of drugs according to the pH value, and the hydroxypropyl methyl cellulose And the carboxyvinyl polymer are mixed in a predetermined ratio. Therefore, unlike other commercially available formulations, the niacin controlled-release formulation of the present invention maintains its matrix shape until all released within the expected time period, and maintains its release pattern without fluctuations. In addition, the release of drugs can be precisely controlled in the gastrointestinal tract...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/22A61K31/455A61K47/38A61K47/32A61P3/06
CPCA61K9/2054A61K31/455A61K9/2027A61P3/06A61P9/10A61K47/50A61K9/20A61K47/38
Inventor 崔然雄柳柄焕郑镛美张宰常
Owner SEOUL PHARMA
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