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Matrix type sustained-release preparation containing basic drug or salt thereof

A technology of slow-release preparations and basic drugs, which is applied in the following fields of preparations, can solve the problems of reduced bioavailability and low release speed, and achieve the effects of reducing side effects, inhibiting the reduction of bioavailability, and reducing the risk of bioavailability

Inactive Publication Date: 2007-12-19
EISIA R&D MANAGEMENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The risk of occurrence of this side effect is particularly severe in basic drugs or salts thereof having strong side effects and basic drugs or salts thereof having a narrow safe range of blood concentration
[0008] The second problem is as follows: In the dissolution test, the release rate of the basic drug or its salt from the matrix-type sustained-release preparation is lower in the late stage of dissolution than in the early stage of dissolution
[0011] However, the above-mentioned prior art documents relate to matrix-type sustained-release preparations for the purpose of pH-independent release of drugs only, and the inventors have no idea how to eliminate or suppress the above-mentioned risk of side effects (the above-mentioned first problem) and slow-down time. Necessary studies should be carried out to determine the risk of reduced bioavailability due to the release profile (question 2 above)

Method used

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  • Matrix type sustained-release preparation containing basic drug or salt thereof
  • Matrix type sustained-release preparation containing basic drug or salt thereof

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preparation example Construction

[0065] Another aspect of the present invention also provides a method for preparing a matrix-type sustained-release preparation, the method comprising the following steps: mixing a basic drug or its salt and at least one enteric polymer, the basic drug or its salt The solubility in 0.1N hydrochloric acid solution and 50 mM phosphate buffer at pH 6.0 is higher than that in alkaline aqueous solution at pH 8.0; the mixture obtained in the above mixing step is compression molded. The present invention also provides another method for preparing a matrix-type sustained-release preparation, which includes the following steps: mixing (1) a basic drug or its salt and (2) at least one enteric base, the basic drug or The solubility of its salt in 0.1N hydrochloric acid solution and neutral aqueous solution with pH 6.0 is 1 mg / mL or more, and the solubility in alkaline aqueous solution with pH 8.0 is 0.2 mg / mL or less, and in pH 6.8 The solubility in a neutral aqueous solution is at least 2 t...

Embodiment 1

[0123] In a mortar, 300 mg of Donepezil Hydrochloride (Eisai), 1500 mg of Eudragit L100-55 (Rhm Gmbh & Co. KG), 1170 mg of lactose, and 30 mg of magnesium stearate (Mallinckrodt Baker, Inc.) were mixed. 200 mg of the above mixture was taken, and tablets were prepared using Autograph AG5000A (Shimadzu Corporation) to obtain tablets with a diameter of 8 mm containing 20 mg of donepezil hydrochloride. The results of the dissolution test are shown in Table 1.

Embodiment 2

[0125] Mix 300mg Donepezil Hydrochloride (Eisai), 750mg Ethocel 10FP (Ethylcellulose, Dow Chemical Company), 750mg Eudragit L100-55 (Rhm Gmbh&Co.KG), 1170mg lactose, 30mg hard fat in a mortar. Magnesium acid (Mallinckrodt Baker, Inc.). 200 mg of the above mixture was taken, and tablets were prepared using Autograph AG5000A (Shimadzu Corporation) to obtain tablets with a diameter of 8 mm containing 20 mg of donepezil hydrochloride. The results of the dissolution test are shown in Table 2.

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Abstract

A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution / dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

Description

Technical field [0001] The present invention relates to a matrix-type sustained-release preparation containing a basic drug or its salt, and in particular to a preparation that can not only inhibit the initial burst release of the drug in the dissolution test (the drug is released immediately after dissolution), but also It can ensure the low pH-dependent dissolution of the basic drug or its salt in the dissolution test at the initial stage of dissolution. The present invention also relates to a matrix type sustained-release preparation containing a basic drug or its salt, characterized in that the ratio of the dissolution rate of the basic drug or its salt in an acidic test solution to the dissolution rate in a neutral test solution (Dissolution rate in acidic test solution / Dissolution rate in neutral test solution), compared with the initial stage of dissolution, decreases with the dissolution time in the later stage of dissolution. Background technique [0002] Sustained-relea...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K9/14A61K9/22A61K9/54A61K31/13A61K31/445A61K47/10A61K47/26A61K47/38A61P25/28
Inventor 植木洋祐藤冈贤
Owner EISIA R&D MANAGEMENT CO LTD
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