Methyldopa composition and methyldopa tablets as well as preparation methods thereof

A technology of methyldopa tablets and methyldopa, which is applied in the directions of drug combination, pill delivery, pharmaceutical formulation, etc., can solve the problem of harsh production conditions and can not improve the oxidative discoloration of methyldopa drugs and the graying of varieties. And other issues

Active Publication Date: 2018-08-10
南京泽恒医药技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, in the existing marketed preparations, edetate sodium, tartaric acid, and vitamin C are added as chelating agents in the prescription, so as to play an anti-oxidative effect; Granules, or reduce contact with metal containers, and increase film coating or sugar coating to increase stability, the composition of the formulation is complex, and the production conditions are harsh
However, according to the stability experiments of several existing varieties on the market, the above method cannot improve the oxidative discoloration of methyldopa drugs very well.
Even in the accelerated test, the commercially available foreign varieties that have been placed for a month all turn gray or even black

Method used

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  • Methyldopa composition and methyldopa tablets as well as preparation methods thereof
  • Methyldopa composition and methyldopa tablets as well as preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Methyldopa-Silicon Dioxide-Stearyl Alcohol Pharmaceutical Composition 1

[0043] Methyldopa (water)...960.0g

[0044] Colloidal silicon dioxide…………30.0g

[0045] Stearyl alcohol………………10.0g

[0046] 98% ethanol……………490g

[0047] ——A total of 1000g

[0048] Dissolve the prescribed amount of stearyl alcohol in 98% ethanol to prepare a stearyl alcohol solution for subsequent use; weigh the prescribed amount of methyldopa and colloidal silicon dioxide, place them in a fluidized bed, and mix them evenly. Spray stearyl alcohol solution, keep the temperature of the material at 25~35°C during the spraying period, and dry for 5~10min at the inlet air temperature of 30~35°C after spraying. After drying, pass the material through a 30-mesh sieve to obtain the methyldopa-silicon dioxide-stearyl alcohol pharmaceutical composition.

Embodiment 2

[0049] Example 2 Methyldopa-Silicon Dioxide-Stearyl Alcohol Pharmaceutical Composition 2

[0050] Methyldopa (water)...980.0g

[0051] Colloidal silicon dioxide…………14.0g

[0052] Stearyl alcohol………………6.0g

[0053] 95% ethanol………………300g

[0054] ——A total of 1000g

[0055] Preparation process: Dissolve the stearyl alcohol of the prescribed amount in 95% ethanol, prepare stearyl alcohol solution, and set aside; weigh the methyldopa and colloidal silicon dioxide of the prescribed amount, place them in a fluidized bed, mix uniform. Spray stearyl alcohol solution, keep the temperature of the material at 25~35°C during the spraying period, and dry for 5~10min at the inlet air temperature of 30~35°C after spraying. After drying, pass the material through a 24-mesh sieve to obtain the methyldopa-silicon dioxide-stearyl alcohol pharmaceutical composition.

Embodiment 3

[0056] Example 3 Methyldopa-Silicon Dioxide-Stearyl Alcohol Pharmaceutical Composition 3

[0057] Methyldopa (water)………970.0g

[0058] Colloidal silicon dioxide……………16.0g

[0059] Stearyl alcohol…………………… 14.0g

[0060] 95% ethanol………………450g

[0061] ——A total of 1000g

[0062] Preparation process: Dissolve the stearyl alcohol of the prescribed amount in 95% ethanol, prepare stearyl alcohol solution, and set aside; weigh the methyldopa and colloidal silicon dioxide of the prescribed amount, place them in a fluidized bed, mix uniform. Spray stearyl alcohol solution, keep the temperature of the material at 25~35°C during the spraying period, and dry for 5~10min at the inlet air temperature of 30~35°C after spraying. After drying, pass the material through a 24-mesh sieve to obtain the methyldopa-silicon dioxide-stearyl alcohol pharmaceutical composition.

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Abstract

The invention relates to a methyldopa-silicon dioxide-stearyl alcohol pharmaceutical composition and a preparation method thereof. The pharmaceutical composition is mainly applied to the preparation of methyldopa tablets. The pharmaceutical composition is prepared by carrying out polymerization on methyldopa, stearyl alcohol and colloidal silicon dioxide by using a spray drying technology; the Hausner ratio range of particles is 1.10-1.18, and the Carr index range of the particles is 10-15%; the pharmaceutical composition has good fluidity and compressibility, so that the compressibility and the tablet formation property are improved; furthermore, the medicine part is prevented from being oxidized and discoloring after being combined with water, so that the storage stability of the preparation is obviously improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a methyldopa pharmaceutical composition, a tablet and a preparation method thereof. Background technique [0002] Methyldopa is a decarboxylase inhibitor, suitable for the treatment of mild and moderate hypertension, renal hypertension, hypertension with left ventricular hypertrophy, heart failure, the elderly and pregnancy-induced hypertension. The antihypertensive effect of methyldopa is mild, durable, reliable, with few side effects, and has the advantages of reducing peripheral vascular resistance and increasing renal blood flow, and is suitable for hypertensive patients with renal insufficiency. Methyldopa is colorless or nearly colorless crystals or white to light yellow-white fine powder, the powder has strong plasticity, poor toughness, poor fluidity, poor compressibility when tableting, sticky punching, and low tablet hardness , prone to splitting and other phen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/198A61K47/04A61K47/12A61P9/12
CPCA61K9/2009A61K9/2013A61K31/198A61P9/12
Inventor 谢晓燕刘宇婧徐成
Owner 南京泽恒医药技术开发有限公司
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