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Combined formulation with improved stability

A stabilizer and preparation technology, which is applied in the field of oral administration combination preparations, can solve problems such as the difficulty in preparing the middle layer and the inability to ensure the uniformity of the middle layer, and achieve the effects of inhibiting platelet aggregation, improving storage stability, and preventing the formation of thrombus

Inactive Publication Date: 2014-01-22
BORYUNG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the above formulations, it is difficult to prepare an intermediate layer containing a mixture of drug and stabilizer, the uniformity of the prepared intermediate layer cannot be ensured, and the storage stability of acid-labile cholesterol-lowering drugs is still a problem

Method used

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  • Combined formulation with improved stability
  • Combined formulation with improved stability
  • Combined formulation with improved stability

Examples

Experimental program
Comparison scheme
Effect test

preparation example A-1

[0092] Preparation example A-1 (preparation of small aspirin tablets)

[0093] The ingredients and amounts of the aspirin minitablets used in the pharmaceutical dosage form of the present invention are shown in Table 1 below.

[0094] [Table 1]

[0095] Composition of aspirin tablets

[0096]

[0097] (1) Preparation of small pieces

[0098] Aspirin, microcrystalline cellulose and Kollidon VA64 (obtained from BASF) were mixed in the amounts shown in Table 1 using a V-shaped mixer, and the resulting mixture was then placed in a tablet press equipped with a multi-head punch (KT-10S, available in from Sejong Pharmatech) and compressed under a pressure of 1 KN to prepare round pellets with a diameter of 1.5-7.5 mm and a weight of 2-50 mg.

[0099] (2) Enteric coating

[0100] Mix the pharmaceutically acceptable enteric coating material (hydroxypropyl methylcellulose phthalate, diethyl phthalate, wheat starch and magnesium stearate) in the amount shown in Table 1, Dissolve ...

preparation example A-2

[0101] Preparation example A-2 (preparation of small aspirin tablets)

[0102] The ingredients and amounts of the aspirin minitablets used in the pharmaceutical dosage form of the present invention are shown in Table 2 below.

[0103] [Table 2]

[0104] Composition of aspirin tablets

[0105]

[0106] (1) Preparation of small pieces

[0107] Aspirin and microcrystalline cellulose were mixed in the amounts shown in Table 2 using a high-speed mixer (available from Sejong Pharmatech), and then granulated with the previously prepared binder solution (hydroxypropylcellulose solution dispersed in purified water). The granules thus obtained were dried, sieved to have a predetermined particle size (mesh opening: 25-30 mesh), and mixed using a V-shaped mixer, and then the mixture was placed in a tablet press equipped with a multi-head punch (KT-10S , from Sejong Pharmatech) and compressed under a pressure of 1 KN to prepare round pellets with a diameter of 1.5-7.5 mm and a weight...

preparation example A-3

[0110] Preparation A-3 (preparation of aspirin pellets)

[0111] The ingredients and amounts of the aspirin pellets used in the pharmaceutical dosage form of the present invention are shown in Table 3 below.

[0112] [table 3]

[0113] Composition of aspirin pellets

[0114]

[0115] (1) Preparation of aspirin pellets

[0116] Aspirin and microcrystalline cellulose were mixed in the amounts of Table 3 using a high-speed mixer (available from Sejong Pharmatech), and granulated with the previously prepared binder solution (hydroxypropylcellulose solution dispersed in purified water). The granules thus obtained were extruded with an extruder (from Sejong Pharmatech) and spheronized using a spherical granulator (Marumerizer, from Sejong Pharmatech) to prepare spherical pellets.

[0117] (2) Enteric coating

[0118] The pharmaceutically acceptable enteric coating material (hydroxypropyl methylcellulose phthalate, diethyl phthalate, wheat starch and magnesium stearate) was m...

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Abstract

Disclosed is a combined formulation for oral administration to treat cardiovascular disease, including (a) cholesterol lowering agent mini-tablet having a diameter of 7.5 mm or less, which contain a cholesterol lowering agent, a stabilizer thereof and a pharmaceutically acceptable excipient and have a coating layer on the surface thereof, and (b) antithrombotic agent mini-tablets or mini-pellets having a diameter of 7.5 mm or less, which contain an antithrombotic agent and a pharmaceutically acceptable excipient and include an enteric coating film on the surface thereof. This formulation can improve treatment compliance depending on a combination prescription, and is controlled so that the cholesterol lowering agent is released in the gastrointestinal tracts and the antithrombotic agent is released in the intestines, thus suppressing the reactions and the side-effects between the drugs, inducing synergic effects of these drugs in vivo, and achieving improved stability.

Description

technical field [0001] The present invention relates to an oral administration combination preparation, which can be used for the treatment of cardiovascular diseases. Background technique [0002] Aspirin (acetylsalicylic acid) is known to prevent stroke or myocardial infarction due to thrombosis when it is administered in low doses over a long period of time to patients at high risk of cardiovascular disease-related diseases. For this purpose, 100 mg of aspirin in the form of tablets or sustained-release capsules is administered orally once a day. It is also known that by administering low doses (approximately 80 mg) of aspirin daily, mortality from heart attack, stroke and cardiovascular disease is reduced by at least 25%. The preventive effect of aspirin on cardiovascular diseases is based on multiple mechanisms, among which the inhibition of thrombus is the most critical pharmacological mechanism. [0003] Aspirin irreversibly acetylates and inactivates cyclooxygenase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/28A61K31/60A61P7/02
CPCA61K9/2866A61K9/4808A61K31/22A61K31/40A61K31/47A61K31/505A61K31/60A61K31/616A61K45/06A61K9/5042A61K9/5084A61P3/06A61P7/02A61K2300/00A61K9/16A61K9/28A61K9/51
Inventor 金济学南京完朴柱垣
Owner BORYUNG PHARMA CO LTD
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