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Application of HPMC and naringenin isonicotinamide co-crystal in preparation of medicine for preventing and treating abdominal aortic aneurysm

An abdominal aortic aneurysm and isonicotinamide technology, applied in the field of medicine, can solve the problems of increasing absorption and drug efficacy, not increasing naringenin supersaturation, and not being clear

Active Publication Date: 2020-05-22
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported that NGN can form a co-crystal (NGN-INT) with isonicotinamide (INT) (Acta Pharmacologica Sinica 2017,52(4):625-633), but whether NGN-INT can promote the pharmacodynamic effect of NGN is still unclear
However, there is no relevant research report on the use of HPMC or PVP to increase the supersaturation of naringenin and increase its absorption and efficacy in vivo

Method used

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  • Application of HPMC and naringenin isonicotinamide co-crystal in preparation of medicine for preventing and treating abdominal aortic aneurysm
  • Application of HPMC and naringenin isonicotinamide co-crystal in preparation of medicine for preventing and treating abdominal aortic aneurysm
  • Application of HPMC and naringenin isonicotinamide co-crystal in preparation of medicine for preventing and treating abdominal aortic aneurysm

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、1

[0031] Embodiment 1, the influence of 1mg / mL HPMC on NGN-INT

[0032] Accurately weigh 252.2 mg of NGN and 226.2 mg of INT into 50 mL of ethyl acetate solution and stir until all solids are completely dissolved. The solution was stirred for an additional 12 hours until the ethyl acetate solution had completely evaporated at room temperature. The obtained crystals were vacuum-dried overnight, and white crystals of NGN-INT were collected. The characterization results are shown in figure 1 .

[0033] The prepared NGN-INT is passed through a 80-100 mesh sieve, so that the particle size of the powder is 165-200 μm. NGN-INT (equivalent to 75 mg NGN) was dissolved in 125 mL of dissolution medium (50 mM pH 6.8 PBS buffer containing 1 mg / mL HPMC) (SI=0.065) with magnetic stirring at room temperature. At 5, 10, 15, 20, 25, 30, 40, 60, 90, 120, 150, 180 and 240min, take out 1mL of solution from the medium, centrifuge the taken out solution (12000rpm, 3min), take the upper layer soluti...

Embodiment 2、10

[0034] Embodiment 2, the influence of 10mg / mL HPMC on NGN-INT

[0035] NGN-INT was prepared according to the method described in Example 1, and passed through a sieve of 80-100 mesh, so that the particle size of NGN-INT was 165-200 μm.

[0036]NGN-INT (equivalent to 75 mg NGN) was dissolved in 125 mL of dissolution medium (50 mM pH 6.8 PBS buffer containing 10 mg / mL HPMC) (SI=0.065) with magnetic stirring at room temperature. At 5, 10, 15, 20, 25, 30, 40, 60, 90, 120, 150, 180, and 240 min, take out 1 mL of solution from the medium, centrifuge the taken out solution (12000 rpm, 3 min), and take the upper layer solution. After passing through a 0.45 μm polyethersulfone filter membrane, the UV absorption of NGN at each time point was detected by UV spectrophotometry, and converted to the content of NGN in the dissolution medium, and the cumulative release was taken as the ordinate and time as the abscissa to draw the dissolution curve ( see the results figure 2 ).

[0037] D...

Embodiment 3

[0038] Example 3. HPMC / PVP promotes the release of NGN in NGN-INT

[0039] Sun[1] et al proposed the concept of sink-index to describe the dissolution conditions, and SI is used to represent the dissolution conditions below. Three parts of 75.0 mg NGN and three parts of NGN-INT (equivalent to 75.0 mg NGN) prepared in Example 1 above were passed through a 80-100 mesh sieve to make the particle size of the powder 165-200 μm. One part NGN and one part NGN-INT were dissolved in 125mL of 50mM PBS buffer, pH 6.8; one part NGN and one part NGN-INT were dissolved in 125mL of dissolution medium (50mM pH 6.8 PBS buffer containing 1mg / mL PVP). solution); one portion of NGN and another portion of NGN-INT were dissolved in 125 mL of dissolution medium (50 mM pH 6.8 PBS buffer containing 1 mg / mL HPMC) (SI=0.065) with magnetic stirring at room temperature. At 5, 10, 15, 20, 25, 30, 40, 60, 90, 120, 150, 180 and 240min, take out 1mL of solution from the medium, centrifuge the taken out solut...

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Abstract

The invention provides an application of an HPMC and naringenin (NGN) isonicotinamide (INT) co-crystal in preparation of a medicine for preventing and treating abdominal aortic aneurysm (AAA). According to the application, firstly the co-crystal (NGN-INT) of the NGN and the INT is prepared, HPMC and PVP are added to the NGN-INT co-crystal separately, the supersaturation effect of the NGN in the HPG / PVP extension co-crystal is investigated, and a blood concentration-time curve of different forms of the NGN in mice is investigated, and results show that the HPMC can significantly increase the oral bioavailability of the NGN in the NGN-INT co-crystal than that of the PVP, and significantly promote the anti-AAA efficacy of the NGN-INT.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to the application of HPMC and naringenin isonicotinamide co-crystal in the preparation of a medicine for preventing and treating abdominal aortic aneurysm. Background technique [0002] Abdominal aortic aneurysm (AAA) is a serious cardiovascular disease characterized by dilation of the diameter of the abdominal aorta, accompanied by the degradation of the extracellular matrix of the arterial wall and the occurrence of chronic inflammation, and death after aneurysm rupture. Very high rate. At present, surgical intervention measures are mainly used for large AAA in clinical practice, and there is still no specific drug for small AAA. Therefore, finding an effective drug to inhibit the expansion of small AAA has important clinical significance for reducing the risk of aneurysm rupture and reducing mortality in patients. [0003] Naringenin (Naringenin, NGN) is mainly derived from Rutaceae pl...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/44A61P35/00A61K9/14A61K47/38
CPCA61K9/146A61K31/352A61K31/44A61P35/00A61K2300/00
Inventor 祁荣黄延宾张星
Owner PEKING UNIV
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