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Emodin-berberine hydrochloride pharmaceutical co-crystal and preparation method thereof

A technology of berberine hydrochloride and emodin, applied in organic chemistry methods, organic chemistry, etc., to achieve the effects of simple and easy preparation methods, increased maximum concentration of drugs, and clear crystal structure

Inactive Publication Date: 2018-09-14
MINJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no public report on the drug co-crystal formed by berberine and emodin

Method used

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  • Emodin-berberine hydrochloride pharmaceutical co-crystal and preparation method thereof
  • Emodin-berberine hydrochloride pharmaceutical co-crystal and preparation method thereof
  • Emodin-berberine hydrochloride pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] 0.742 g of berberine hydrochloride and 0.540 g of emodin were suspended in 20 mL of acetonitrile, and stirred for 48 hours to obtain a large amount of yellow precipitate, which was filtered with suction. The crystals were recrystallized from acetonitrile to obtain yellow crystals.

[0028] figure 1 This is the XRD pattern of an emodin-berberine hydrochloride drug co-crystal prepared in Example 1. Depend on figure 1 It can be seen that the prepared crystal has a diffraction angle of 2 θ ° ± 0.1 is expressed as: 8.3°, 9.1°, 10.0°, 10.4°, 12.0,°12.5°, 14.0°, 15.0°, 16.7°, 18.2°, 18.5°, 20.1°, 20.4°, 20.7°, 21.4° , 23.0°, 24.0°, 24.7°, 25.3°, 25.9°, 26.5°, 27.0°, 28.0°, 30.0°, 30.6°, 31.4°, 32.2° have characteristic diffraction peaks.

[0029] figure 2 It is the crystal structure unit of an emodin-berberine hydrochloride drug co-crystal prepared in Example 1. Depend on figure 2 It can be known that the prepared drug co-crystal includes berberine cation, chloride...

Embodiment 2

[0033] Pharmacokinetic parameters of emodin-berberine hydrochloride co-crystal in rats:

[0034] The SD male rats weighing 190-210 g were raised in conventional feeding conditions, drinking water freely, and after fasting for 12 hours, press

[0035] 40 mg / kg (emodin dose) was administered by gavage, before and after administration at 0.10, 0.17, 0.35, 0.53, 0.68, 0.87, 1, 1.5, 2, 4, 6, 8, 12, 24, About 0.5 ml of blood was collected from the retrobulbar venous plexus at 36 h, and centrifuged at 4000 rpm for 10 min. Take 200 μl of plasma, add 400 μl of methanol, vortex for 2 min, centrifuge at 10,000 rpm for 10 min, take the supernatant and blow dry with nitrogen. 100 μl of mobile phase (methanol:water=50:50) was added, vortexed for 1 min, centrifuged at 15,000 rpm for 1 min, and 40 μl of the supernatant was taken for HPLC-MS detection. The HPLC-MS detection system is Aligent 1260 LC-6410 MS high performance liquid chromatography system, and the chromatographic column is Ultima...

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Abstract

The invention discloses an emodin-berberine hydrochloride pharmaceutical co-crystal and a preparation method thereof, and belongs to the technical field of pharmaceutical crystallization. The preparation method is characterized in that the berberine hydrochloride and the emodin are dissolved into acetonitrile according to the ratio of 1 to 1 to form the emodin-berberine hydrochloride pharmaceutical co-crystal; a co-crystal structural unit is prepared from berberine hydrochloride molecules and emodin molecules, wherein the molar ratio of the berberine hydrochloride molecules to the emodin molecules is 1 to 1 and the molecular formula is [C15H10O5][C20H18ClNO4]. The preparation method disclosed by the invention is simple and feasible and the cost is low. In addition, the relative bioavailability of the emodin in the prepared pharmaceutical co-crystal in rats is significantly improved compared with that of pure emodin, and the relative bioavailability of the emodin in the prepared pharmaceutical co-crystal is 1.7 times that of the pure emodin.

Description

technical field [0001] The invention belongs to the technical field of drug crystallization, in particular to an emodin-berberine hydrochloride drug co-crystal and a preparation method thereof. Background technique [0002] The solid crystal form of drug molecules is the core restricting factor for solid drugs to exert their efficacy. For a specific drug, different crystalline forms such as polymorphism, salt form, and co-crystal determine different pharmaceutical effects. Drug co-crystals have attracted great attention as a new drug crystal form. Drug co-crystals can be formed by combining drug molecules with other physiologically acceptable small organic molecules in the form of hydrogen bonds. On the premise of not destroying the molecular structure of the drug, the formation of co-crystals can improve the water solubility and dissolution rate of the drug, thereby improving the oral bioavailability of the drug. In July 2015, the U.S. FDA approved Novartis' new anti-hea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03
CPCC07D455/03C07B2200/13
Inventor 娄本勇张燕杰黄雅丽张梅黄晓东
Owner MINJIANG UNIV
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