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Berberine hydrochloride self-microemulsion preparation having good oral bioavailability and preparation method thereof

A technology for berberine hydrochloride and an emulsion preparation is applied in the field of berberine hydrochloride self-microemulsion preparation and its preparation, which can solve the problem of not being able to ensure that berberine hydrochloride is not metabolized in the intestinal tract and the like, and achieves the improvement of oral bioavailability and the avoidance of The effect of intestinal metabolism, carrying and taking convenience

Active Publication Date: 2015-08-12
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved in the present invention is to overcome the defects and deficiencies of the existing berberine hydrochloride self-microemulsion drug delivery system, that is, it cannot guarantee that berberine hydrochloride will not be metabolized in the intestinal tract

Method used

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  • Berberine hydrochloride self-microemulsion preparation having good oral bioavailability and preparation method thereof
  • Berberine hydrochloride self-microemulsion preparation having good oral bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 berberine hydrochloride self-microemulsion preparation

[0029] 1. Prepare the following components in mass ratio: 3-5% berberine hydrochloride, 3-5% penetration enhancer, 40-50% oil phase, 30-40% emulsifier and 10-20% co-emulsifier.

[0030] Wherein, the penetration enhancer is sodium caprate or sodium oleate; the oil phase is isopropyl myristate, isopropyl palmitate, peppermint oil, rose oil or lemon oil. The emulsifier is polyoxyethylene ether-40 hydrogenated castor oil, polyoxyethylene 10 oleyl ether, poloxamer PF127 or poloxamer PF68; the co-emulsifier is ethanol or glycerin.

[0031] 2. Preparation:

[0032] S1. according to the formula described in claim 1, berberine hydrochloride, oil phase, emulsifier and co-emulsifier are mixed, heated and stirred to obtain clear solution, i.e. pre-microemulsion;

[0033] S2. Add the pre-microemulsion obtained in S1 into distilled water at 37° C. and stir slightly to form a self-microemulsion.

Embodiment 2

[0034] Example 2 SD rat bioavailability experiment

[0035] 1. Dosing regimen

[0036] Healthy SD rats (200 ± 20 g) were given different cinnamon preparations (100 mg / kg), and intravenous (intravenous, iv) injection (6 mg / kg) was used as the control preparation, before and after administration, respectively At 0.167 h, 0.5 h, 1.0 h, 1.5 h, 2.0 h, 4.0 h, 6.0 h, 8.0 h, 10 h, and 12 h, 0.40 mL of blood was taken from the orbital vein, and the blood samples were processed according to the assay method, and the blood drug concentration was determined by HPLC .

[0037] 2. Blood sample processing

[0038] Take 0.45 mL of blood from SD rats and put it in a centrifuge tube treated with sodium heparin, centrifuge at 3500 rpm for 15 min, take 0.15 mL of supernatant plasma, add 0.30 mL of acetonitrile to precipitate protein, vortex for 3 min, then centrifuge at 10000 rpm for 10 min, take The supernatant was passed through a 0.22 μm filter membrane, and the BBR content was determined...

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Abstract

The invention discloses a berberine hydrochloride self-microemulsion preparation having good oral bioavailability and a preparation method thereof. The berberine hydrochloride self-microemulsion preparation comprises the following ingredients by mass ratio: 3-5% of berberine hydrochloride, 3-5% of penetration enhancing agent, 40-50% of oil phase, 30-40% of emulsifier and 10-20% of co emulsifier. The penetration enhancing agent is sodium caprate or sodium oleate; and the oil phase is isopropyl myristate, isopropyl palmitate, oleum menthae, rose oil or lemon oil. According to the invention, BBR is coated in an oil core through microemulsion, intestinal tract metabolism is avoided, biomembrane permeability is increased, bioavailability is increased, dosage is reduced, and constipation is avoided; production technology is simple, a solid preparation has the advantages of stabilization and convenient transport, carrying and administration, bitter taste is avoided, acceptability is good, and the berberine hydrochloride self-microemulsion preparation has good popularization application prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. More specifically, it relates to a berberine hydrochloride self-microemulsion preparation with good oral bioavailability and a preparation method thereof. Background technique [0002] Berberine (BBR) is the main active ingredient of Chinese medicine Coptis chinensis, and it has been clinically used for many years in the treatment of intestinal infection and bacillary dysentery. A large number of recent experiments and clinical studies have shown that BBR can also effectively reduce blood sugar and blood lipids, and has a wide range of pharmacological effects. However, due to poor biofilm permeability of BBR (accounting for 56% of the administered dose) and significant intestinal first-pass elimination (accounting for 43.5% of the administered dose), its absolute bioavailability is extremely low (0.52%), and large doses ( 0.9-1.5 g / day) long-term use can cause problems such ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4375A61K47/14A61K47/44A61K47/12A61P1/00A61P31/04
Inventor 龙晓英刘昌顺郑玉蓉张颖峰
Owner GUANGDONG PHARMA UNIV
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