Injection agent for protecting ischemic myocardium and preparation method of injection

A technique for myocardial and injection, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations, etc. It can solve the problems of poor water solubility, low oral bioavailability, and low drug concentration. Avoid systemic side effects, improve bioavailability, increase effective concentration

Active Publication Date: 2018-07-27
FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, currently marketed N-suberoylanilide hydroxamic acid preparations are limited to antitumor oral dosage forms
Due to the poor water solubility of N-suberoylanilide hydroxamic acid, and the obvious first-pass metabolic elimination of N-suberoylanilide hydroxamic acid after oral administration, its oral bioavailability is very low, and it cannot be used in cardiovascular and other related diseases. Form effective therapeutic concentrations in adipose tissue
In addition, N-suberoylanilide hydroxamic acid can only play a therapeutic role as a prototype, and its metabolites are inactive, so chemical derivatization cannot be used to improve its oral bioavailability
In addition, oral N-sub

Method used

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  • Injection agent for protecting ischemic myocardium and preparation method of injection
  • Injection agent for protecting ischemic myocardium and preparation method of injection
  • Injection agent for protecting ischemic myocardium and preparation method of injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] 1. Prescription 1

[0106] Name of raw material

Prescription volume (g)

N-suberoylanilide hydroxamic acid

15

Soy lecithin

10

Soybean Oil for Injection

100

Tween 80

3

Oleic acid

0.5

glycerin

12.5

Water for Injection

Appropriate amount

[0107] Makes 500ml.

[0108] 2. Process:

[0109] Weigh the prescribed amount of N-suberoylanilide hydroxamic acid, add Tween-80 and glycerin, heat to 80°C, add about 100ml of water, until the raw material drug is dissolved, add soybean lecithin, shear (6000rpm) and mix evenly, Prepare the water phase; weigh oleic acid and soybean oil for injection, and mix them uniformly to form the oil phase; mix the oil and water phases at 70° C. for 30 minutes at high speed shear (6000 rpm) to produce colostrum. The colostrum is homogenized under the pressure of 800bar, circulated 6 times, filled into ampoules, sealed, and sterilized at 115°C for 30 minutes.

Embodiment 2

[0111] 1. Prescription 2

[0112] Name of raw material

Prescription volume (g)

N-suberoylanilide hydroxamic acid

15

Soy lecithin

5

Soybean Oil for Injection

75

Poloxamer 188

3

Oleic acid

0.75

glycerin

12.5

Water for Injection

Appropriate amount

[0113] Makes 500ml.

[0114] 2. Process:

[0115] Weigh the prescribed amount of N-suberoylanilide hydroxamic acid, add poloxamer 188 and glycerin, heat to 80°C, add about 100ml of water, until the raw material drug is dissolved, add soybean lecithin, shear (6000rpm) and mix well , to make a water phase; weigh oleic acid and soybean oil for injection, and mix them uniformly to make an oil phase; the oil-water two phases are mixed at a high speed (5000rpm) at 80°C for 40 minutes to make colostrum. Homogenize the colostrum under the pressure of 700bar, circulate 6 times, put it into an ampoule, seal it, and sterilize it at 115°C for 30 minutes.

Embodiment 3

[0117] 1. Prescription 3

[0118] Name of raw material

Prescription volume (g)

N-suberoylanilide hydroxamic acid

15

Soy lecithin

12.5

Soybean Oil for Injection

50

Macrogol 15 Hydroxystearate

5

Oleic acid

0.25

glycerin

11.5

Water for Injection

Appropriate amount

[0119] Makes 500ml

[0120] 2. Process:

[0121] Weigh the prescribed amount of N-suberoylanilide hydroxamic acid, add polyethylene glycol 15 hydroxystearate and glycerin, heat to 80°C, add about 100ml of water, until the raw material is dissolved, add soybean lecithin, cut (5000rpm) mixed evenly to make the water phase; weighed oleic acid and soybean oil for injection, mixed evenly to make the oil phase; the oil-water two phases were mixed under high pressure shear (6000rpm) for 40 minutes at 80°C to make colostrum. The colostrum is homogenized under the pressure of 800bar, circulated 6 times, filled into ampoules, sealed, and...

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Abstract

The invention relates to an injection agent for protecting ischemic myocardium and a preparation method of the injection. Injection emulsion is prepared from the following raw materials in parts by mass: 1 to 5 parts of N-SAHA (Suberoylanilide Hydroxamic Acid), 0.2 to 12.5 parts of emulsifying agent, 2 to 100 parts of oil for injection, 0.02 to 5 parts of solubilizer, 0.03 to 0.4 part of oleic acid, 0.4 to 12.5 parts of glycerinum and the balance of water for injection. The injection emulsion can be effectively used for increasing local drug concentration of the N-SAHA in lipophilic organs such as angiocarpy and/or tissues before cardiac interventional operation, increasing the bioavailability of the N-SAHA, reducing general side effects of the N-SAHA, realizing effective protection on myocardium under an ischemic or reperfusion injury state and reducing or avoiding the occurrence of myocardial infarction; meanwhile, a new optional dosage form is provided for application of the N-SAHAin treating cancer by the injection emulsion.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an injection for protecting ischemic myocardium and a preparation method thereof, in particular to an emulsion for injection containing N-suberoylanilide hydroxamic acid for protecting ischemic myocardium and its preparation method. Background technique [0002] Histone deacetylase inhibitors (histone deacetylase inhibitors, HDACI) are a class of compounds that interfere with the function of histone deacetylases. research reports. [0003] It is known that N-suberoylanilide hydroxamic acid (SAHA, see formula I below for chemical structure) as a histone deacetylase (HDAC) inhibitor can induce cell differentiation and block cell cycle , Induce cell regulation and play a therapeutic role. In vitro studies have shown that N-suberoylanilide hydroxamic acid at nanomolar concentrations (IC 50 <86nmol / L) can inhibit HDAC 1, HDAC 2 and HDAC 3 (type I) and HDAC 6 (type II) e...

Claims

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Application Information

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IPC IPC(8): A61K31/167A61K47/26A61K47/10A61K47/14A61P9/10A61P35/00
CPCA61K47/10A61K47/14A61K47/26A61K9/0019A61K31/167A61P9/10A61P35/00A61K9/107A61K47/12A61K47/24A61K9/10A61K47/44
Inventor 唐熠达楚娜秦艳
Owner FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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