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Medicine composition containing Enalapril maleate, folic acid and acid stabilizer

A technology of enalapril maleate and acid stabilizer, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, and pill delivery, etc., can solve problems such as type II instability, and achieve improved performance. The effect of stability

Active Publication Date: 2017-08-04
NANJING YOKO PHARMA +2
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] (4) Select the appropriate crystal form. Enalapril maleate has polymorphism, which can be divided into type I and type II. Although it has been reported that the energy of the two crystal forms is similar, the difference is only 0.6kcal / mol, but Type II is more unstable in film
Since dissolution and dissolution of a drug have a significant impact on absorption, in vitro dissolution testing has the potential to predict its in vivo behavior

Method used

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  • Medicine composition containing Enalapril maleate, folic acid and acid stabilizer
  • Medicine composition containing Enalapril maleate, folic acid and acid stabilizer
  • Medicine composition containing Enalapril maleate, folic acid and acid stabilizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] A suitable stabilizer was screened by selecting different acids, citric acid, fumaric acid, malic acid, arginine and maleic acid, and no acid was added in the control, and the results are shown in Table 1.

[0044] Table 1 Acid Stabilizer Selection

[0045]

[0046] Preparation Process:

[0047] (1) Weigh folic acid and starch through a 60-mesh sieve and mix in equal increments, add acid stabilizer citric acid, fumaric acid, malic acid, arginine or maleic acid, and mix with enalapril maleate Pass 60 mesh sieve;

[0048] (2) Weigh the prescription amount of disintegrant croscarmellose sodium and binder povidone K30, pass through a 60-mesh sieve and mix uniformly by equal increment method, and mix with microcrystalline cellulose 102 to pass through 60 mesh screen;

[0049] (3) Add lubricant magnesium stearate, mix and press into tablets to make 1000 tablets.

[0050] Related substance detection method: Waters high performance liquid chromatography e2695-2489 instru...

Embodiment 2

[0053] Table 2 maleic acid dosage screening

[0054]

[0055] The preparation method is the same as in Example 1.

[0056] Be 0.1%~5% by weight percentage of maleic acid dosage to the stability influence of preparation, the preparation that prescription Rx6~Rx12 obtains is placed 10 days under 60 ℃ high temperature, humidity RH 92.5% and 4500lx strong light irradiation conditions Influencing factor experiment. As a result, it was found that the impurities of enalapril diketone, enalaprilat, and capric acid in the preparation did not change significantly under the conditions of humidity RH 92.5% and strong light irradiation of 4500lx, but under the high temperature condition of 60°C, enalapril Diketones still increase. With the increase of the amount of maleic acid in the prescription, the impurity of enalapril diketone gradually decreased, but when the amount of maleic acid increased to 5%, the impurity no longer decreased. Calculated by weight percentage, when the malei...

Embodiment 3

[0060] Table 3 Filler Screening

[0061] Element Rx13 Rx14 Rx15 Rx16 Rx17 Rx18 enalapril maleate 10.0g 10.0g 10.0g 10.0g 10.0g 10.0g folic acid 0.8g 0.8g 0.8g 0.8g 0.8g 0.8g starch 0 0 30.0g 30.0g 0 0 anhydrous lactose 80.0g 0 50.0g 0 0 0 lactose monohydrate 0 80.0g 0 50.0g 50.0g 50.0g Microcrystalline Cellulose 102 0 0 0 0 30.0g 0 Microcrystalline Cellulose 101 0 0 0 0 0 30.0g Croscarmellose Sodium 5.0g 5.0g 5.0g 5.0g 5.0g 5.0g Povidone K30 1.0g 1.0g 1.0g 1.0g 1.0g 1.0g maleic acid 2.0g 2.0g 2.0g 2.0g 2.0g 2.0g Magnesium stearate 1.0g 1.0g 1.0g 1.0g 1.0g 1.0g

[0062] Tablet preparation method is with embodiment 1.

[0063] According to the second method of appendix XC of the Chinese Pharmacopoeia in 2010, 500mL of 0.1M hydrochloric acid solution is the dissolution medium, and the rotating speed is 50rpm. Rx11~Rx16 and commercially ...

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Abstract

The invention provides a new Enalapril maleate and folic acid composite preparation. An acid stabilizer with weight ratio of 1%-5% is added in the preparation to improve the stability of the preparation at high temperature and long-term standing condition; and meanwhile, a mixture of microcrystalline cellulose and lactose monohydrate is selected asfiller, the dissolution of the folic acid in the 0.1M hydrochloric acid medium is improved, and a finally prepared tablet is basically consistent with the market tablet. The composition disclosed by the invention is good in stability, capable of guaranteeing the clinical safe use of the medicine, simple in process operation, and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing enalapril maleate, folic acid and an acid stabilizer. Background technique [0002] The disease spectrum of cardiovascular and cerebrovascular events in China is significantly different from that in Western populations. The annual incidence of stroke in my country is 250 / 100,000, and the annual incidence of cardiovascular events is 50 / 100,000. The incidence of stroke is five times that of cardiovascular events. In clinical trials to observe the effect of blood pressure reduction on cardiovascular and cerebrovascular events, the incidence ratio of stroke / myocardial infarction in Chinese hypertensive population is 6-13:1, while that of Western hypertensive population is about 1:1, suggesting that stroke is the high incidence rate in my country. The most important cardiovascular and cerebrovascular events in people with high blood pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/26A61K47/12A61K31/519A61K31/401A61K9/20
CPCA61K9/2013A61K9/2018A61K9/2054A61K31/401A61K31/519A61K2300/00
Inventor 张烨缪六舒薛峪泉朱素华张峰
Owner NANJING YOKO PHARMA
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