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Rheochrysidin and micro-capsule of derivative of rheochrysidin as well as preparation method and application of rheochrysidin

A technology of emodin methyl ether and derivatives, which is applied in the direction of microcapsules, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of low bioavailability and poor drug absorption

Inactive Publication Date: 2017-09-22
潘小平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Emodin methyl ether has low bioavailability and poor drug absorption when taken orally, so it has certain limitations in clinical application

Method used

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  • Rheochrysidin and micro-capsule of derivative of rheochrysidin as well as preparation method and application of rheochrysidin
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  • Rheochrysidin and micro-capsule of derivative of rheochrysidin as well as preparation method and application of rheochrysidin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] (1) Take 300 mg of emodin methyl ether powder, disperse and dissolve it in 5 ml of cod-liver oil, and ultrasonically assist it as an oil phase solution;

[0099] (2) adopting 3% sodium alginate aqueous solution as the aqueous phase solution;

[0100] (3) The ratio of water to oil is 8:1;

[0101] (4) Slowly add the oil phase solution into the water phase solution at 23° C., and stir continuously with a magnetic stirrer until an emulsion is formed. The viscosity of the emulsion is relatively high, the time for mixing to form milk is prolonged, and the difficulty of dripping increases;

[0102] (5) Continuously instill the emulsion to 4% concentration of CaCl with a No. 5 needle syringe at a rate of 40 drops / min 2 In the solution, the magnetic stirrer was continuously stirred during the period to form a vortex, equilibrated for 1 hour, filtered, and washed twice with distilled water to form wet microcapsules;

[0103] (6) 1% chitosan solution adjusts pH=6;

[0104] (7)...

Embodiment 2

[0107] (1) Take 300 mg of emodin methyl ether powder, disperse and dissolve it in 5 ml of cod-liver oil, and ultrasonically assist it as an oil phase solution;

[0108] (2) adopting 2% sodium alginate aqueous solution as the aqueous phase solution;

[0109] (3) The ratio of water to oil is 9:1;

[0110] (4) Slowly add the oil phase solution into the water phase solution at 23°C, and stir continuously with a magnetic stirrer until an emulsion is formed;

[0111] (5) Continuously instill the emulsion to 4% concentration of CaCl with a No. 5 needle syringe at a rate of 60 drops / min 2 In the solution, the magnetic stirrer was continuously stirred during the period to form a vortex, equilibrated for 1 hour, filtered, and washed twice with distilled water to form wet microcapsules;

[0112] (6) 1% chitosan solution adjusts pH=6;

[0113] (7) Put the wet microcapsules into the chitosan solution and incubate for 40 minutes, rinse with distilled water twice, and dry naturally to obt...

Embodiment 3

[0116] (1) Take 2000 mg of emodin methyl ether powder, disperse and dissolve it in 35 ml of cod liver oil, and ultrasonically assist it as an oil phase solution;

[0117] (2) adopting 2% sodium alginate aqueous solution as the aqueous phase solution;

[0118] (3) The ratio of water to oil is 10:1;

[0119] (4) Slowly add the oil phase solution into the water phase solution at 25°C, and stir continuously with a magnetic stirrer until an emulsion is formed;

[0120] (5) Continuously drip the emulsion to 3% concentration of CaCl with a No. 5 needle syringe at a rate of 60 drops / min 2In the solution, the magnetic stirrer was continuously stirred during the period to form a vortex, equilibrated for 1 hour, filtered, and washed twice with distilled water to form wet microcapsules;

[0121] (6) 1% chitosan solution adjusts pH=6;

[0122] (7) Put the wet microcapsules into the chitosan solution and incubate for 40 minutes, rinse with distilled water twice, and dry naturally to obta...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to rheochrysidin and a micro-capsule of a derivative of rheochrysidin as well as a preparation method and application of rheochrysidin. The invention provides an enteric-coated preparation including rheochrysidin used as an active ingredient or the derivate of the rheochrysidin, and sodium alginate-chitosan used as a capsule material. According to the rheochrysidin prepared by the invention and the enteric-coated preparation as the derivative of the rheochrysidin, the phenomenon that a conventional oral preparation is hydrolyzed and inactivated by gastric acid when the oral preparation flows through the stomach is avoided; meanwhile, by utilizing a slow release effect, the bioavailability is improved, and anti-tumor effects of the rheochrysidin and the derivate thereof are facilitated. In a preparation process of the enteric-coated preparation, a preparation technology is optimized, and the simple, feasible, safe and environment-friendly preparation method can be obtained. The multi-batch rheochrysidin and the enteric-coated preparation as the derivate of the rheochrysidin prepared according to an optimized condition are naturally dried to form white particles, and the white particles are spherical and round, uniform in size and good in dispersibility; the particle size, the drug-loading rate and the entrapment rate all keep stable, and the white particles are applied to large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to microcapsules of emodin methyl ether and derivatives thereof, a preparation method and application thereof. Background technique [0002] Rheum offcinale (Rheum offcinale Baill), Rheum palmatum L., and Rheum tanguticum Maxim.ex Balf are the dried roots and rhizomes of Polygonaceae plants. Rhubarb is cold in nature and bitter in taste. It has the functions of purging and attacking stagnation, clearing heat and purging fire, cooling blood and detoxifying, removing blood stasis and stimulating menstruation, promoting dampness and reducing jaundice. Rhubarb can also be used for excess heat stagnation, constipation, blood heat, spit at the nose, red eyes and throat, carbuncle furuncle, intestinal ulcer abdominal pain, amenorrhea due to blood stasis, postpartum stagnation, bruises, damp heat dysentery, jaundice, red urine, stranguria syndrome, edema; external tre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/122A61K47/36A61P35/00A61P35/02
CPCA61K9/0002A61K9/5036A61K31/122
Inventor 潘小平
Owner 潘小平
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