A kind of stable α crystal form perindopril tert-butylamine tablet and its preparation method
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A technology of tert-butylamine tablets and perindopril, which is applied in the field of medicine, can solve the problems of impurity degradation rate and difficult crystal form transformation, and achieve the effect of reducing water control and disintegration risks, using fewer types of excipients, and facilitating stability
Active Publication Date: 2019-06-18
NINGBO MENOVO TIANKANG PHARMA CO LTD
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Problems solved by technology
In summary, the degradation rate and crystal transformation of impurities in the stability of perindopril are the difficulties in product development
Method used
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Embodiment 1
[0038] A kind of perindopril tablet, described perindopril tablet is made up of following components according to parts by weight:
[0039] Alpha crystal form perindopril tert-butylamine: 4 parts;
[0040] Lactose: 65 parts;
[0041] Microcrystalline cellulose: 20 parts;
[0042] Magnesium stearate: 1 part.
[0043] The tablet weighing about 90mg of last system, its preparation process comprises the following steps:
[0044] (1) Take lactose and microcrystalline cellulose and pass through a 50-mesh sieve respectively, mix, dry until the moisture is lower than 4.5%, divide into 3 parts, and control the humidity in the process to be lower than 40% RH.
[0045] (2) Take one portion and mix it with perindopril tert-butylamine passing through a 80-mesh sieve, and pass through a 60-mesh sieve to mix;
[0046] (3) Continue to add a part of the mixed auxiliary materials in (1) and mix;
[0047] (4) Mix (3) with the remaining auxiliary materials in (1) for 20 minutes;
[0048] (5) ...
Embodiment 2
[0054] Embodiment 2: a kind of perindopril tablet, described perindopril tablet is made up of following components according to parts by weight:
[0055] Alpha crystal form perindopril tert-butylamine: 4 parts;
[0056] Lactose: 60 parts;
[0057] Microcrystalline cellulose: 25 parts;
[0058] Magnesium stearate: 1 part.
[0059] The tablet weighing about 90mg of last system, its preparation process comprises the following steps:
[0060] (1) Take lactose and microcrystalline cellulose and pass through a 50-mesh sieve respectively, mix, dry until the moisture is lower than 4.5%, divide into 3 parts, and control the humidity in the process to be lower than 40% RH;
[0061] (2) Take one portion and mix it with perindopril tert-butylamine through a 60-mesh sieve, and mix evenly through a 60-mesh sieve;
[0062] (3) Continue to add a part of the mixed auxiliary materials in (1) and mix;
[0063] (4) Mix (3) with the remaining auxiliary materials in (1) for 20 minutes;
[006...
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Abstract
The invention provides a stable alpha-crystalline form perindopril tert-butylamine tablet, which consists of perindopril tert-butylamine, lactose, microcrystalline cellulose and magnesium stearate. A preparation method, by virtue of a powder direct compression process, comprises the following steps: firstly, sieving and mixing the lactose and the microcrystalline cellulose, and drying the lactose and the microcrystalline cellulose; respectively sieving and mixing some lactose and microcrystalline cellulose with perindopril tert-butylamine; finally, adding the magnesium stearate and mixing; sampling and detecting, tabletting and packaging an obtained tablet with an aluminum-plastic foamed mask, wherein the interior of the aluminum-plastic foamed mask contains a drying agent and the exterior of the aluminum-plastic foamed mask is covered by a composite film bag. The perindopril tert-butylamine tablet prepared by the method disclosed by the invention has no significant change with published products in character, dissolution rate, moisture, content, crystalline form as well as dissolution behaviors in mediums at different pH values, and the perindopril tert-butylamine tablet is more stable than the published products in production and storage stability, so that the clinical effectiveness and safety of the medicine during taking are guaranteed. The perindopril tert-butylamine tablet preparation method provided by the invention is simple, and the production cost of the medicine is reduced.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a stable α-crystal form perindopril tert-butylamine tablet and a preparation method thereof. Background technique [0002] Perindopril and its salts belong to angiotensin and are widely used in the treatment of cardiovascular diseases, especially in the fields of hypertension and heart failure. Although perindopril was initially synthesized in the form of sodium salt, its stability was not good, so more stable perindopril tert-butylamine and arginine salts were successively synthesized, which also reduced the safety risk. Perindopril arginine salt and perindopril tert-butylamine have been developed into various forms of single or compound preparations. Traditional perindopril tert-butylamine tablet formulations often use fillers (such as lactose, microcrystalline cellulose) , binders (such as hydroxypropyl cellulose, povidone, hydroxypropyl methyl cellulose), disint...
Claims
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