Rhizoma coptidis total alkaloids resin complexes, sustained-release preparation thereof and preparation method thereof

A resin compound, total alkaloid technology, applied in the directions of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problems of low bioavailability of berberine, poor patient compliance, frequent medication, etc. The effect of delaying hydrolysis and improving stability

Inactive Publication Date: 2011-03-02
GUANGANMEN HOSPITAL CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the taste of Coptidis Rhizome is extremely bitter, and the bioavailability of berberine is very low. During the treatment of diabetes, the number of medications is frequent, and the patient's compliance is poor.

Method used

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  • Rhizoma coptidis total alkaloids resin complexes, sustained-release preparation thereof and preparation method thereof
  • Rhizoma coptidis total alkaloids resin complexes, sustained-release preparation thereof and preparation method thereof
  • Rhizoma coptidis total alkaloids resin complexes, sustained-release preparation thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0068] 1. Preparation of reference substance solution: Accurately weigh 5 mg each of jatrorrhizine hydrochloride, coptisine hydrochloride, palmatine hydrochloride, and berberine hydrochloride, put them in 10 mL volumetric flasks respectively, add hydrochloric acid-methanol (1:100, v / v) to the scale, ultrasonically dissolved, and mixed to obtain the stock solution.

[0069] 2. Preparation of the test solution: take 0.1 g of the total alkaloids of Coptis chinensis, accurately weigh it, place it in a stoppered Erlenmeyer flask, add 100 mL of hydrochloric acid-methanol (1:100, v / v), weigh, and sonicate for 40 minutes , take it out and place it at room temperature, make up for the lost weight, filter, and take the continued filtrate.

[0070] 3 Chromatographic conditions:

[0071] Chromatographic column: Venusil XBP-C18 analytical column (250mm×4.6mm, 5μm) and Brava C 18 -BDS pre-column; mobile phase: acetonitrile: 0.05mol L -1 Potassium dihydrogen phosphate solution (pH4.54) = ...

Embodiment 1

[0081] Example 1. Preparation of Coptidis Rhizoma Total Alkaloid Resin Complex by Static Exchange Method

[0082] Precision Weighing Amberlite TM Pharmaceutical grade ion exchange resin (strong acid Na + Type IRP69 resin, weak acid H + Type IRP64 resin and weak acid K + type of IRP88 resin; Rohm&Hass company) is added to a certain concentration of drug solution in an appropriate amount, placed in a constant temperature water bath, fully stirred at different temperatures, and samples are taken at the set time. Formula (1) and formula (2) calculate the exchange drug amount (Q) and drug utilization rate (E) of the resin, and when the drug concentration is basically unchanged, the reaction reaches equilibrium.

[0083] Q = ( C 0 - C t ) V W ...

Embodiment 2

[0140] Example 2, Structural Verification of Coptis Rhizoma Total Alkaloid Resin Complex

[0141] Differential thermal analysis (DSC), infrared spectroscopy (Infrared spectrum), and X-ray diffraction (X-ray diffraction) were used to verify the binding mode of the total alkaloids of Coptidis rhizome and IRP88 resin in the drug resin complex prepared in Example 1.

[0142] 1. Differential scanning calorimetry (DSC)

[0143] Differential thermal analysis spectra of total alkaloids of Coptidis rhizome, ion exchange resin IRP88, drug resin complex, physical mixture of total alkaloids of Coptidis rhizome and ion exchange resin IRP88 (1:1, w / w) were recorded by differential scanning thermal analysis .

[0144] Measuring conditions: scanning range 25-350°C; heating rate 10.00°C / min; reference: blank aluminum dry pot; atmosphere: static air; sample weight about 4.0mg. See the test pattern Figure 6 .

[0145] Ion-exchange resins have certain characteristic melting endothermic peaks...

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Abstract

The invention discloses Rhizoma coptidis total alkaloids resin complexes, a sustained-release preparation thereof and a preparation method thereof. The Rhizoma coptidis total alkaloids resin complexes comprise Rhizoma coptidis total alkaloids and acidic K plus resin (Amberlite TMIRP88 resin). In 100g of the complexes, the total content of jateorrhizine, coptisine, palmatine and berberine is (67.75 plus / minus 1.26) g and the content of the berberine is (54.87 plus / minus 1.64) g. An assay determination of IR, DSC, X-ray diffraction, and the like, proves that the medical resin complexes are formed by bonding of Rhizoma coptidis lkaloids and cation exchange resin through the ionic bond rather than simple physical adsorption. An orally taken sustained-release preparation thereof is prepared by using the medical resin complexes as raw material and Carbopol 974 PNF as the sustained-release material. An in-vitro dissolving test proves that the sustained-release preparation has a good sustained-release function and can sustainably release for 8h to 24h according to different designs.

Description

technical field [0001] The invention relates to a total alkaloid resin complex of Coptis chinensis, its slow-release preparation and a preparation method thereof. Background technique [0002] Coptis chinensis is the dried rhizome of Coptis chinensis Franch, Coptis deltoidea C.Y. Chenget Hsiao and Coptis teeta Wall. Alkaloids are the main components of Coptis Rhizoma, including Berberine, Coptisine, Jatrorrhizine, Palmatine and Epiberberine hydrochloride, among which Berberine The highest content. [0003] Berberine hydrochloride (Berberine hydrochloride), also known as berberine, its molecular formula is [C 2 0H 18 NO 4 ] + Cl - , the structural formula is as follows: [0004] [0005] Molecular weight 371.8, yellow needle-like crystal, melting point 145°C, berberine hydrochloride has a relatively small solubility in water of 1:500, soluble in hot water and ethanol, insoluble in ether and benzene. [0006] Coptisine hydrochloride (Coptisine hydrochloride), the mo...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K36/718A61K9/00A61K9/22A61P31/04A61P3/10A61P1/00A61P1/04A61K125/00A61K47/59
Inventor 崔翰明金良白鸽张秋燕夏丕芳
Owner GUANGANMEN HOSPITAL CHINA ACAD OF CHINESE MEDICAL SCI
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