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Candesartan cilexetil and hydrochlorothiazide co-amorphous substance and preparation method thereof

A technology of candesartan cilexetil and hydrochlorothiazide, which is applied in the field of medicine, can solve the problems that antihypertensive drugs cannot meet the clinical treatment requirements, achieve good application development prospects, and improve the effect of solubility and dissolution rate

Active Publication Date: 2020-11-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since the treatment of hypertensive diseases is long-term, a single antihypertensive drug cannot meet the clinical treatment requirements at present, and drug combination has become a generally applicable initial treatment strategy

Method used

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  • Candesartan cilexetil and hydrochlorothiazide co-amorphous substance and preparation method thereof
  • Candesartan cilexetil and hydrochlorothiazide co-amorphous substance and preparation method thereof
  • Candesartan cilexetil and hydrochlorothiazide co-amorphous substance and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of co-amorphous substance of candesartan cilexetil and hydrochlorothiazide

[0037] Weigh about 0.305g of candesartan cilexetil crystals and 0.149g of hydrochlorothiazide crystals into the same 100mL eggplant-shaped bottle, add about 40mL of ethanol, and shake thoroughly to obtain a clear and transparent solution. The solution was placed on a rotary evaporator, the temperature of the water bath was set at 55 °C, and the ethanol was removed by rotary evaporation under reduced pressure to obtain the corresponding solid product. It was dried in a vacuum oven for 48 h to remove the residual solvent in the rotary evaporated product.

Embodiment 2

[0039] Preparation of co-amorphous substance of candesartan cilexetil and hydrochlorothiazide

[0040] Weigh about 1.221g of candesartan cilexetil crystals and 0.149g of hydrochlorothiazide crystals respectively into the same 100mL eggplant-shaped bottle, add about 50mL of methanol, and shake fully to obtain a clear and transparent solution. The solution was placed on a rotary evaporator, the temperature of the water bath was set at 35 °C, and the methanol was removed by rotary evaporation under reduced pressure to obtain the corresponding solid product. It was dried in a vacuum oven for 48 h to remove the residual solvent in the rotary evaporated product.

Embodiment 3

[0042] Preparation of co-amorphous substance of candesartan cilexetil and hydrochlorothiazide

[0043] Weigh about 0.305g of candesartan cilexetil crystals and 0.595g of hydrochlorothiazide crystals into the same 100mL eggplant-shaped bottle, add about 60mL of acetonitrile, and shake thoroughly to obtain a clear and transparent solution. The solution was placed on a rotary evaporator, the temperature of the water bath was set at 65 °C, and the acetonitrile was removed by rotary evaporation under reduced pressure to obtain the corresponding solid product. It was dried in a vacuum oven for 48 h to remove the residual solvent in the rotary evaporated product.

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Abstract

The invention discloses a candesartan cilexetil and hydrochlorothiazide co-amorphous substance formed by combining candesartan cilexetil and hydrochlorothiazide. According to a powder X-ray diffraction spectrum, a DSC spectrum and an infrared spectrum, the co-amorphous substance is a novel solid form completely different from each monomer and a physical mixture thereof. The candesartan cilexetil and the hydrochlorothiazide are used for preparing the co-amorphous substance, so that the solubility and the dissolution rate of the candesartan cilexetil can be significantly improved, and the co-amorphous substance is expected to become a new raw material solid form of a candesartan cilexetil / hydrochlorothiazide compound tablet and has good application development prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-amorphous candesartan cilexetil hydrochlorothiazide formed by combining candesartan cilexetil and hydrochlorothiazide and a preparation method thereof. Background technique [0002] Candesartan cilexetil, the chemical name is 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4- Base] methyl]-1H-benzimidazole-7-carboxylic acid-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester, the molecular formula is C 33 h 34 N 6 o 6 , the chemical structure is shown in Formula I. As one of the main products of selective angiotensin II receptor antagonist (ARB), candesartan cilexetil can reduce blood pressure, diuresis and natriuresis by specifically blocking angiotensin II-mediated vasoconstriction and aldosterone secretion. effect. Candesartan cilexetil belongs to BCS class II drugs, is insoluble in water, has low oral bioavailability, and unilateral preparations are likely t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/549A61K31/4184A61K9/14A61P9/12
CPCA61K31/4184A61K31/549A61K9/14A61P9/12A61K2300/00
Inventor 高缘王维洁刘蕾
Owner CHINA PHARM UNIV
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