Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Stable candesartan cilexetil tablet combination

A technology of sartan cilexetil tablet and candesartan cilexetil, which is applied in the field of candesartan cilexetil C-type crystal tablet composition, can solve the problems of difficult process operation and long time consumption, and meet the friability requirements , The preparation process is simple and easy, and the effect of good stability

Active Publication Date: 2013-06-05
DISHA PHARMA GRP
View PDF7 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 200810020603.2 discloses the composition of candesartan cilexetil and phospholipids, and candesartan cilexetil can be embedded or wrapped in the hydrophobic layer of the center of the phospholipid bilayer to prepare a stable composition; Chinese patent 201110203975.0 discloses the use of polyethylene glycol Alcohol-coated candesartan cilexetil polymer, this method is difficult to operate and takes a long time; Chinese patent 200910016928.8 discloses a dry tableting method without polyethylene glycol, which is difficult to operate

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Stable candesartan cilexetil tablet combination

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Candesartan cilexetil C crystal 8.000g, hydroxypropyl cellulose 12.000g, lactose 55.000g, starch 15.000g, microcrystalline cellulose 30.000g, carboxymethylcellulose sodium 0.700g, magnesium stearate 1.200g g, make 1000 pieces according to the following method.

[0016] The first step is to weigh the auxiliary materials according to the prescription and pass through a 120-mesh sieve.

[0017] In the second step, add the prescription amount of sodium carboxymethylcellulose into an appropriate amount of 95% ethanol, stir until it is completely dissolved, then add an appropriate amount of purified water, stir evenly, and prepare a 50% ethanol solution containing 1% of sodium carboxymethylcellulose (w / w) as a binder, set aside.

[0018] The third step is to add the prescribed amount of hydroxypropyl cellulose, lactose, starch, and microcrystalline cellulose to the wet granulator in order for dry mixing, and stir and mix for 5 minutes. Then slowly add the prescrib...

Embodiment 2

[0023] Example 2 Candesartan cilexetil C-type crystal 8.000g, hydroxypropyl cellulose 12.000g, lactose 55.000g, starch 15.000g, microcrystalline cellulose 30.000g, carboxymethylcellulose sodium 0.700g, magnesium stearate 1.200g g, made into 1000 pieces. Prepared according to the method of Example 1, the difference is that the tabletting pressure is 35 kN.

[0024] According to the method prescribed in the Pharmacopoeia of the People's Republic of China, the hardness of the tablet was measured to be 2.60 kg.

Embodiment 3

[0025] Example 3 Candesartan cilexetil C crystal 8.000g, hydroxypropyl cellulose 12.000g, lactose 55.000g, starch 15.000g, microcrystalline cellulose 30.000g, carmellose sodium 0.700g, magnesium stearate 1.200g g, made into 1000 pieces. Prepared according to the method of Example 1, the difference is that the tabletting pressure is 30 kN.

[0026] According to the method prescribed in the Pharmacopoeia of the People's Republic of China, the hardness of the tablet was measured to be 2.52 kg.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Hardnessaaaaaaaaaa
Hardnessaaaaaaaaaa
Hardnessaaaaaaaaaa
Login to View More

Abstract

The invention relates to a candesartan cilexetil tablet combination and a preparation method. The candesartan cilexetil tablet combination is characterized in that a combination of a unit dose comprises a candesartan cilexetil C type crystal of 8 milligrams, hydroxypropylcellulose of 12 milligrams, lactose of 55 milligrams, starch of 15 milligrams, microcrystalline cellulose of 30 milligrams, sodium carboxymethylcellulose of 0.7 milligram and magnesium stearate of 1.2 milligrams. The hardness of a tablet is in a range of 2.20-2.60 kilograms. The preparation method is characterized in that the candesartan cilexetil C type crystal does not participate in granulating, and the tablet manufacturing pressure is 10-35 kilonewtons.

Description

technical field [0001] The invention relates to a candesartan cilexetil C-type crystal tablet composition and a preparation method, and the composition is used for the treatment of hypertension. Background technique [0002] Candesartan cilexetil is an antihypertensive drug developed by Takeda Corporation of Japan. Its chemical name is (±)-1-[[(cyclohexyloxy)carbonyl]oxo]ethyl-2-ethoxy-1-[[ 2'-(1H-tetrazolyl-5)-[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylate. Molecular formula: C 33 h 34 N 6 o 6 , Molecular weight: 610.66, for the treatment of essential hypertension. [0003] Candesartan cilexetil is white or off-white powder, soluble in methanol, insoluble in water. The type C crystal used to make the tablet composition is stable to temperature, water vapor and light when it is placed alone, but if the crystal form is affected by a relatively strong extrusion collision or damp heat, the crystal form is easy to change, and the composition is made according ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/20A61K31/4184A61K47/38A61P9/12
Inventor 龙连清王寅峰岳丽萍
Owner DISHA PHARMA GRP
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products