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Oral pharmaceutical composition comprising sargrelate or a salt thereof

A composition and drug technology, applied in the direction of drug delivery, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of patients' medication compliance, improve or treat ischemic symptoms, and prevent treatment period increased effect

Active Publication Date: 2022-06-28
KOREA UNITED PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, currently commercialized products containing (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3′-methoxybibenzyl hydrochloride The tablet has the following disadvantages, that is, it needs to be administered orally one tablet at a time three times a day, and the patient's medication compliance is reduced due to the necessity of frequent taking

Method used

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  • Oral pharmaceutical composition comprising sargrelate or a salt thereof
  • Oral pharmaceutical composition comprising sargrelate or a salt thereof
  • Oral pharmaceutical composition comprising sargrelate or a salt thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0022] Patent Document 2 discloses a method for preparing the above-mentioned crystal form. In a specific example, preferably, the above-mentioned pharmaceutical composition contains about 30% of (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3′ - Crystalline form II of methoxybibenzyl hydrochloride, more specifically, comprising more than about 70%.

[0023] In a specific example, the above-mentioned pharmaceutical composition may comprise about 95% or more or 98% or more of (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy] - Crystalline form II of 3'-methoxybibenzyl hydrochloride.

[0024] The above-mentioned active ingredients can be present in the above-mentioned immediate-release layer and the above-mentioned sustained-release layer in any proportion. It is present in a weight ratio of 1:1 to 3, and more specifically, can be present in a weight ratio of about 1:2 to 2.5. In a specific example, the immediate release layer may comprise 100 mg of (±)-2-[2...

Embodiment 1-10

[0064] Example 1-10: (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3′-methoxybibenzyl hydrochloride sustained-release preparation of tablet

[0065] According to the composition and content of the sustained-release layer shown in Table 1 below, a binding solution in which povidone was dissolved in absolute ethanol was prepared, respectively, and (±)-2-[2-(3-carboxypropionyloxy) was mixed with -3-dimethylaminopropoxy]-3'-methoxybibenzyl hydrochloride, lactose hydrate, hydroxypropyl methylcellulose carbomer 941 and sodium starch glycolate, combined with the above After the solutions were combined, granulated and dried together, the sustained-release layer granules were prepared by sieving and granulating using a No. 20 sieve. Then, the sustained-release layer granules prepared above are post-mixed with magnesium stearate. The above granules were compressed at a hardness of 14 kgf to prepare sustained-release tablets. Then, the Opadry white film coating of Table 2 b...

experiment example 1

[0069] Experimental Example 1: Sustained release containing (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3′-methoxybibenzyl hydrochloride Dissolution test of tablet (1)

[0070] (1) Prepare test solution

[0071] Dissolution conditions

[0072] Experimental device: The second method (paddle method) in the general experimental method of the Korean Pharmacopoeia

[0073] Dissolution: 900mL of water

[0074] Stirring speed: 50rpm

[0075] Test solution temperature: 37±0.5℃

[0076] According to the second method (paddle method) of the dissolution test method in the general test method of the Korean Pharmacopoeia, the dissolution test was carried out on each of the six sustained-release tablets prepared in the above Examples 1-10 under the above conditions. Filter through a syringe filter and discard 5 mL of the first filtrate, and use the subsequent filtrate as the test solution.

[0077] (2) Prepare standard solution

[0078] The standard product of (±)-2-[2-(...

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Abstract

One solution of the present invention provides (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3'-methoxybibenzyl hydrochloride ( (±)‑2‑[2‑(3‑carboxypropionyloxy)‑3‑dimethylaminopropoxy]‑3'‑methoxybibenzylhydrochloride) is a pharmaceutical composition as an active ingredient.

Description

technical field [0001] The present invention relates to a compound containing (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3′-methoxybibenzyl or a salt thereof as an active ingredient Oral pharmaceutical compositions, more particularly, involving (±)-2-[2-(3-carboxypropionyloxy)-3-dimethylaminopropoxy]-3' which can be administered once daily - A sustained-release oral pharmaceutical composition of methoxybibenzyl or a salt thereof. Background technique [0002] (±)-2-[2-(3-Carboxypropionyloxy)-3-dimethylaminopropoxy]-3'-methoxybibenzyl hydrochloride (sarpogrelate hydrochloride) )) is used as a platelet aggregation inhibitor, which has a novel mechanism of action of selectively antagonizing the serotonin receptor (5-HT2) of platelets and blood vessels. [0003] Drugs that prevent the formation of platelet clumps are called antiplatelet drugs, and most drugs have mechanisms that inhibit the process of clotting and platelet activation. Aspirin, which is a represe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K31/225A61K9/20A61K9/00
CPCA61K9/00A61K9/20A61K31/225
Inventor 崔然雄河大喆权仁浩金娥英宋熙用郑来勋崔宝滥
Owner KOREA UNITED PHARMA
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