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Therapeutic composition containing amlodipine salt and losartan medicine

A composition and technology of dipine salts, which are applied in the field of amlodipine series salts, can solve the problem of slow onset of amlodipine, affecting the bioavailability and onset time of amlodipine, and the lack of light resistance of amlodipine besylate, etc. question

Inactive Publication Date: 2009-07-01
BEIJING ROCK PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, amlodipine besylate does not have good enough solubility in water, especially when it is close to the physiological pH7.4 state. As we all know, amlodipine itself has the weakness of slow onset of action, which will further affect amlodipine bioavailability and onset time of dipine, in addition, amlodipine besylate does not have sufficient photostability
At the same time, the use of benzenesulfonic acid in the production process has disadvantages, namely, benzenesulfonic acid is difficult to handle industrially due to its corrosion and toxicity, and its highly hygroscopic nature also requires specific transportation and use steps

Method used

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  • Therapeutic composition containing amlodipine salt and losartan medicine
  • Therapeutic composition containing amlodipine salt and losartan medicine
  • Therapeutic composition containing amlodipine salt and losartan medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment 1 The general preparation method of valsartan / amlodipine series salt tablet

[0075] Valsartan and amlodipine series salts were pulverized, passed through a 100-mesh sieve, and set aside; lactose, microcrystalline cellulose, pregelatinized starch, carboxymethyl starch sodium, and magnesium stearate were respectively passed through a 80-mesh sieve, set aside.

[0076] Take amlodipine series salts and valsartan according to the prescription quantity, mix uniformly, and then mix homogeneously with carboxymethyl starch sodium, lactose, microcrystalline cellulose and pregelatinized starch successively according to the equal amount incremental method.

[0077] Add an appropriate amount of purified water to make a uniform soft material, pass through a 20-mesh sieve to granulate, dry at 50°C for 2 hours, add the prescribed amount of magnesium stearate, pass through a 20-mesh sieve for granulation, and mix well.

[0078] Determine the particle content, and adjust the ...

Embodiment 2

[0081] Embodiment 2 Light fastness experiment

[0082] The pharmaceutical composition of the research product amlodipine series salts (5 mg) and valsartan (80 mg) is as described in Examples 1-4 (specifically the following table). The research article and the reference article (amlodipine besylate / valsartan composition) were exposed to 50°C and placed under an incandescent lamp (220V, 100W) at 30cm above the sample for 4 weeks, and then the relative composition of each composition was determined. substance. It is evident from the above results that, compared with the reference product, the study product exhibited improved photostability except for the L-aspartate amlodipine / valsartan and maleate amlodipine / valsartan compositions Properties (in the table below, according to the stability of the related substances and compositions produced, they are arranged from high stability to low stability).

[0083] Table 2. Photostability of the composition of amlodipine series salts

...

Embodiment 3

[0086] Embodiment 3 Amlodipine series salt solubility test

[0087] Sufficient solubility is a necessary condition for the drug to obtain good bioavailability. However, amlodipine besylate does not have sufficient solubility in water, especially when it is close to the physiological pH7.4. Therefore, we also investigated camphorsulfonic acid Solubility of amlodipine, amlodipine pyroglutamate, amlodipine L-aspartate, amlodipine maleate, amlodipine mesylate and amlodipine besylate (as reference substance) As we all know, the pH of the above-mentioned saturated salt was also investigated, and the closer to pH 7.4, the better the biocompatibility. From the above results, it is evident that the study articles all exhibited improved solubility compared to the control, while having better or comparable pH at saturation, compared to the control.

[0088] Table 4. Solubility and saturation pH of amlodipine series salts

[0089]

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Abstract

The invention relates to amlodipine series salt, generally comprising camphor sulfonic acid salt, L-aminobutanedioic acid salt, maleic acid salt and methanesulfonic acid salt and sartan compound or pharmaceutical composition of pharmaceutically acceptable thereof and preparation method of same, and kit for drug combination containing amlodipine serious salt and sartan compound composition. The composition or kit can be applied to treat patient suffering angina pectoris, atherosclerosis, and / or hypertension complicated with hyperlipemia and patient having risk of heart diseases (including human).

Description

technical field [0001] The present invention relates to amlodipine series salts, specifically including camphorsulfonate, pyroglutamate, L-aspartate, maleate and methanesulfonate, and sartan compounds or pharmaceutically acceptable salts thereof The pharmaceutical composition and the preparation method thereof, the present invention also relates to a combined medicine kit comprising amlodipine series salt composition and sartan compound composition. The above compositions or kits can be used to treat patients suffering from hypertension, angina pectoris, atherosclerosis, and / or combined hypertension and patients (including humans) with cardiac risk symptoms. Background technique [0002] Hypertension has become one of the main killers endangering human health. At present, the incidence of hypertension in some European and American countries has reached 20%. According to statistics, 43 million people in the United States suffer from hypertension; the average incidence of hyp...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/4184A61K31/41A61P9/12A61P9/10
Inventor 王海勇陈艳明付俊昌
Owner BEIJING ROCK PHARMA
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