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Development for tanshinol-naringenin composite pellet

A technology of danshensu and naringenin, applied in the field of medicine

Inactive Publication Date: 2017-03-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The published patents on naringenin mainly involve the research on its extraction and preparation method and pharmacological activity. There are almost no published patents on naringenin instant-release pellets and patents on the compatible use of naringenin and danshensu.

Method used

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  • Development for tanshinol-naringenin composite pellet
  • Development for tanshinol-naringenin composite pellet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Preparation of Danshensu sustained-release pellets

[0020] Mix Danshensu and microcrystalline cellulose passed through 80-mesh sieve evenly in a mass ratio of 1:9, and use 5% PVP-K30 as a wetting agent to make a soft material. Put the soft material in the extruder, extrude it into strips at a certain extrusion speed of 10-15rpm, and then transfer the material to the spheronizer for spheronization, set the spheronization speed to 20-25hz and the spheronization time to 5-7min. Finally, the prepared pellets were dried in an oven (40° C. / RH 31%) for 12 hours, sieved through a sieve, and 20-30 mesh pellets were obtained. Surelease ethyl cellulose aqueous dispersion with 15% solid content was prepared as coating liquid. Assemble the fluidized bed, add the danshensu ball core prepared above from above the material barrel of the fluidized bed, and cover with a lid with a mesh. Turn on the blower, adjust the blast temperature to 28-35°C, the blast speed to 20-26Hz, and pr...

Embodiment 2

[0028] (1) Preparation of Danshensu sustained-release pellets

[0029] Mix danshensu and microcrystalline cellulose passed through 80 mesh sieve evenly according to the mass ratio of 1:1, 1:5 and 1:10, make a soft material with 5% PVP-K30 as a wetting agent, and extrude and spheronize Preparation of Danshensu ball core. Prepare 10% ethyl cellulose ethanol solution as the coating solution, and prepare Danshensu sustained-release pellets of various prescriptions according to the method described in Example 1.

[0030] (2) Preparation of naringenin quick-release pellets

[0031] Mix naringenin, microcrystalline cellulose, and sodium carboxymethyl starch through a 80-mesh sieve evenly in a mass ratio of 2:8:2, and use 5% PVP-K30 as a wetting agent to make a soft material. The method described in 1 prepares naringenin quick-release pellets.

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Abstract

The invention, which belongs to the medicine field, relates to development for a tanshinol-naringenin composite pellet. Tanshinol being a water-soluble component of the root of red-rooted salvia being Chinese medicine is effective in treating angina pectoris. At present, most of tanshinol preparations being available in the market are immediate-release dosage forms that can not satisfy the demand of long-term therapy for angina pectoris; the bioavailability, being lower than 10%, of the preparation is low and the metabolism is fast, wherein t1 / 2 is equal to 0.5h approximately; and the pure sustained-release pellet can not keep enough blood concentration for long time and thus is not effective in treating angina pectoris. Besides, naringenin is capable of inhibiting activity of P450enzymeCYP3A4; and after taking of the naringenin with tanshinol, the metabolic process of the tanshinol in vivo can be inhibited, so that the bioavailability of tanshinol is enhanced and the plasma clearance is reduced. Therefore, according to development provided by the invention, tanshinol and naringenin are prepared into a composite pellet. In addition, enterohepatic circulation exists during oral naringenin taking and thus a long-acting effect can be realized by an immediate-release dosage form, so that the naringenin is prepared into an immediate-release pellet and the tanshinol is prepared into a sustained-release pellet.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the development and application of a combination pellet of danshensu and naringenin. Background technique [0002] Danshensu is one of the main water-soluble components in the traditional Chinese medicine Danshen, which can relax coronary arteries and has a good protective effect on myocardial ischemia. Clinically, Danshensu is often used in the prevention and treatment of angina pectoris. Danshensu molecules contain phenolic hydroxyl groups and carboxyl groups, so Danshensu has strong water solubility, but it also leads to poor permeability, and it is difficult to pass through the lipid bilayer of cell membranes; Danshensu has obvious first-pass effect. It is metabolized in the liver before being absorbed into the blood circulation. These properties are the main factors leading to the low oral bioavailability of danshensu, which limits the clinical application of danshensu. Commerciall...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/38A61K31/192A61K31/352A61P9/10
CPCA61K9/0002A61K9/5047A61K31/192A61K31/352A61K2300/00
Inventor 刘建平夏毓龙于盼盼张双双
Owner CHINA PHARM UNIV
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