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Antihypertensive Tablets Containing Sodium Chloride Drug Carrier

A sodium chloride and blood pressure-lowering technology, applied in the field of medicine, can solve the problems of degradation, inappropriate use of excipients, affecting the stability of candesartan medoxomil, etc., and achieve the effects of fast release, inhibition of crystal form confusion, and excellent compression moldability.

Active Publication Date: 2015-12-02
GUANGZHOU BAIYUSN TIANXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] European patent EP0546358B1 reveals that high moisture in the preparation will lead to the degradation of candesartan cilexetil, and high tableting pressure will affect the stability of candesartan cilexetil, so it is not suitable to use a large amount of some fibers with high water content and strong water absorption Vegetarian, starch, and polyvinylpyrrolidone-based excipients, and it is not suitable to use excipients that require high pressure to form tablets

Method used

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  • Antihypertensive Tablets Containing Sodium Chloride Drug Carrier
  • Antihypertensive Tablets Containing Sodium Chloride Drug Carrier
  • Antihypertensive Tablets Containing Sodium Chloride Drug Carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Preparation of candesartan cilexetil tablets

[0016] 1. Recipe: See Table 1

[0017] Table 1 formula of candesartan cilexetil tablets (1000 tablets, unit: g)

[0018]

[0019] 2. Preparation:

[0020] 1) Weigh polyethylene glycol 6000 according to the proportion of the formula, heat up to 70~75°C, and melt into a liquid ( ).

[0021] 2) Weigh candesartan cilexetil, sodium chloride, and croscarmellose sodium (or carboxymethyl starch sodium) according to the ratio of the formula, mix them evenly, add them into the turbine granulator, turn on the turbine granulator, and control The inlet air temperature keeps the material temperature at 25~40°C, and the ( ) is slowly sprayed onto the material by air-flow atomization, discharges the material after spraying, and granulates to obtain candesartan cilexetil granules ( ).

[0022] 3) take magnesium stearate and ( ) mixed evenly, at 15kN / cm 2 The following pressure tablet.

Embodiment 2

[0023] Example 2 Preparation of candesartan cilexetil tablets

[0024] 1. Formulation: See Table 2

[0025] Table 2 formula of candesartan cilexetil tablets (1000 tablets, unit: g)

[0026]

[0027] 2. Preparation Process:

[0028] 1) Weigh polyethylene glycol 8000 according to the proportion of the formula, heat up to 70~80°C, and melt into a liquid ( ).

[0029] 2) Weigh candesartan cilexetil, sodium chloride, and croscarmellose sodium (or carboxymethyl starch sodium) according to the ratio of the formula, mix them evenly, add them into the turbine granulator, turn on the turbine granulator, and control The inlet air temperature keeps the material temperature at 25~40°C, and the ( ) is slowly sprayed onto the material by air-flow atomization, discharges the material after spraying, and granulates to obtain candesartan cilexetil granules ( ).

[0030] 3) take magnesium stearate and ( ) mixed evenly, at 15kN / cm 2 The following pressure tablet.

[0031]...

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Abstract

The invention relates to a hypotensive tablet containing a sodium chloride medicine carrier, which is suitable for a pharmaceutical enterprise. The disclosed tablet comprises the sodium chloride, candesartan cilexetil, and pharmaceutically acceptable adjuvants. The sodium chloride is stable in property and good in water solubility and compressibility, and is well compatible with the candesartan cilexetil. The sodium chloride is taken as the carrier for the candesartan cilexetil; by injecting polyethylene glycol 6000 solution or polyethylene glycol 8000 solution, a medicine is loaded on the sodium chloride and the mixed carrier containing other pharmaceutically acceptable adjuvants of the medicine; the adjuvants, such as a lubricant, are added to mix uniformly, and the mixture is subjected to tabletting and can be molded by compression under a pretty low pressure; and, by reducing the pressure in the tabletting process, the transformation of the candesartan cilexetil to an unstable crystal form due to over-high pressure in the tabletting process can be prevented so that the reduction of the candesartan cilexetil content and the increasing of the impurity content in the storage process can be prevented. The candesartan cilexetil tablet prepared by the invention has good stability and is released quickly.

Description

technical field [0001] The invention specifically relates to a blood pressure-lowering tablet containing a sodium chloride drug carrier, which belongs to the technical field of medicine. Background technique [0002] The "Nutrition and Health Status of Chinese Residents" released by the Ministry of Health in 2004 showed that the prevalence of hypertension among residents aged 18 and over in my country was 18.8%, and it is estimated that the number of patients nationwide is more than 160 million. According to the "National Archives of Environmental Health" released by the World Health Organization in 2005, hypertension has become one of the top ten chronic diseases in my country, and it is also one of the ten diseases with the highest mortality rate. [0003] Candesartan cilexetil (hereinafter sometimes referred to as "active ingredient") is an angiotensin AT 1 Receptor antagonist, which is hydrolyzed into the active metabolite candesartan in the body, through the interact...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/4184A61K47/02A61P9/12
Inventor 谭胜连傅红燕杨轶群王衍成曾晓红
Owner GUANGZHOU BAIYUSN TIANXIN PHARMA
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