Unlock instant, AI-driven research and patent intelligence for your innovation.

Berberine-phenylacetic acid derivative, pharmaceutically acceptable salt thereof and application thereof

A derivative, berberine technology, applied in the field of berberine-phenylacetic acid derivatives and pharmaceutically acceptable salts, can solve problems such as difficulty in dissolution and absorption, liver first-pass effect, increased toxicity, etc. Efficacy, reduce drug toxicity, enhance the effect of drug targeting

Inactive Publication Date: 2012-11-28
ARMY MEDICAL UNIV
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs also have some side effects while relieving symptoms and eliminating diseases for patients; and the common disadvantages of berberine drugs are that they are difficult to dissolve and absorb, and the first-pass effect of the liver.
Although many studies have shown that modifying the structure of berberine can overcome some disadvantages, most compounds increase their toxicity while improving their activity, and finally few drugs can be marketed through clinical trials

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
  • Berberine-phenylacetic acid derivative, pharmaceutically acceptable salt thereof and application thereof
  • Berberine-phenylacetic acid derivative, pharmaceutically acceptable salt thereof and application thereof
  • Berberine-phenylacetic acid derivative, pharmaceutically acceptable salt thereof and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: In vitro hypoglycemic activity experiment

[0040] 1. Experimental materials and methods

[0041] 1 Instruments and reagents

[0042] 1.1 Main experimental instruments

[0043] (1) SW-CJ-2F double-sided double-sided ultra-clean workbench (Suzhou Purification Equipment Co., Ltd.)

[0044] (2) MCO-150A carbon dioxide incubator (Japan SANYO company)

[0045] (3) Inverted Phase Contrast Microscope (Olympus CK40-F200)

[0046] (4) Automatic balance centrifuge (Reboer LDZ 4-1.2)

[0047] (5) 25cm2 culture flask, 48, 96-well culture plate (COSTAR, USA)

[0048] (6) SHH-W21-600 three-purpose electric heating constant temperature water tank (Tianjin Test Instrument Co., Ltd.)

[0049] (7) KQ-100DE CNC ultrasonic cleaner (Kunshan Ultrasonic Instrument Co., Ltd.)

[0050] (8) MLS-3020 high-pressure steam sterilizer (Japan SANYO company)

[0051] (9) DGX-9243B-2 blast drying oven (Shanghai Fuma Experimental Equipment Co., Ltd.)

[0052] (10) SN-3001 Microplate R...

Embodiment 2

[0093] Embodiment 2: the preparation method of the invented compound 1d tablet

[0094] prescription:

[0095]

[0096] Preparation method: prepare 4% propyl methylcellulose (E-30) solution, set aside. Weigh 10 g of starch and dry at 105°C for 5 hours for later use. Weigh 20g of starch and the invented compound 1d and microcrystalline cellulose of the prescribed amount, mix well, and pulverize through an 80-mesh sieve. Use 4% propyl methylcellulose (E-30) solution to make the material into soft material, granulate it with a 20-mesh sieve, and dry it at 50°C to 60°C until the water content in the granule is about 3%. Pass through a 20-mesh sieve for granulation, add dry starch (dried at 105°C for 5 hours) and magnesium stearate in the prescribed amount, and finally mix, measure the content of intermediates, and determine the tablet weight; tablet.

[0097] Usage and dosage: According to the patient's condition and individual differences, it is recommended to take 3-6 tabl...

Embodiment 3

[0098] Embodiment 3: the preparation method of invented compound 2i capsule

[0099] prescription:

[0100]

[0101] Preparation method: After the synthesized compound 2i is micronized and pulverized into very fine powder, it is uniformly mixed with auxiliary materials according to the above-mentioned formula ratio, and the soft material is made with water level wetting agent, and after being made into 12-14 mesh particles by a granulator, the Dry at 40-50°C; sieve to remove fine powder, and the finished product has uniform particles and consistent color. No moisture absorption caking. After the routine inspection of the Pharmacopoeia, it meets the relevant regulations and is qualified, and commercially available No. 3-5 capsules can be selected. After loading and sealing, the surface of the capsules is polished and printed, and the capsules can be prepared, bottled and packaged after checking the difference in filling volume and disintegration time limit according to the...

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

No PUM Login to View More

Abstract

The invention relates to a medical application of a berberine-phenylacetic acid derivative, its pharmaceutically acceptable salt and a pharmaceutical composition thereof for treating diabetes, metabolic syndrome and complications thereof. The application of the berberine-phenylacetic acid derivative or its pharmaceutically acceptable salt of the invention is capable of enhancing the medicine targeting, raising the drug effect and reducing the medicine toxicity, and provides a novel application for comprehensively utilizing the authentic Chinese medicinal material coptis resource.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to berberine-phenylacetic acid derivatives and pharmaceutically acceptable salts thereof, and also relates to the medical application of these compounds. Background technique [0002] Berberine (i.e. berberine: Berberine) is a quaternary amine isoquinoline alkaloid extracted from the rhizomes of Coptis chinensis, Cortex Phellodendron, Three Needles, and Shigongong. Its hydrochloride (berberine hydrochloride: Berberine Hydrochloride) is often used clinically, molecular formula: C 20 h 18 ClNO 4 2H 2 O. Molecular weight: 407.85. Its appearance is yellow needle-like crystal or powder, odorless and extremely bitter. It decomposes when heated to 160-220°C, and completely melts at 278-280°C. It is easily soluble in hot water, slightly soluble in cold water or ethanol, very slightly soluble in chloroform, and insoluble in ether (Jiang Biao. Coptidis hydrochloride extracted from Cor...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P3/10A61P3/00A61P5/48
Inventor 周向东方波陶凌晖张艺范昕建孟宪丽
Owner ARMY MEDICAL UNIV