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A kind of ginkgo ketone ester solid self-microemulsion sustained-release pellets and preparation method thereof

A technology of ginkgo ketone ester and sustained-release pellets is applied in the directions of medical raw materials derived from Ginkgo biloba, bulk delivery, cardiovascular system diseases, etc. It can improve the oral bioavailability, prolong the action time and improve the stability.

Active Publication Date: 2017-09-22
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention provides a ginkgo ketone ester solid self-microemulsion sustained-release pellet prepared by using the ginkgo ketone ester self-microemulsion as a binder, which can improve the poor solubility, low stability, and Low bioavailability and inability to maintain effective blood drug concentration for a long time

Method used

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  • A kind of ginkgo ketone ester solid self-microemulsion sustained-release pellets and preparation method thereof
  • A kind of ginkgo ketone ester solid self-microemulsion sustained-release pellets and preparation method thereof
  • A kind of ginkgo ketone ester solid self-microemulsion sustained-release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 45g of polyoxyethylene castor oil EL35, 45g of polyethylene glycol 400 and 10g of medium chain oil, stir evenly, add 10g of ginkgo ketone ester, stir for 24h, and filter to obtain ginkgo ketone ester self-microemulsion. In addition, 90 g of microcrystalline cellulose and 10 g of crospovidone were weighed, mixed evenly, and the above-mentioned ginkgo ketone ester self-microemulsion was added to prepare a soft material, which was extruded and spheronized to obtain a drug-containing pill core. Dry the pellet core containing the drug in a drying oven at 60°C for 2 hours, and take it out.

[0027] Preparation of coating solution: ethyl cellulose 1g, talc powder 0.3g and PEG4000 0.9g, dissolved in 100mL absolute ethanol solution to obtain coating solution; weigh 100g containing pill core, put it into extrusion spheronization coating machine for preheating After 10 minutes, coat with coating solution. After coating, the coated pellets were taken out and dried in a dryin...

Embodiment 2

[0029] Weigh 40 g of polyoxyethylene castor oil EL35, 40 g of polyethylene glycol 400 and 20 g of medium chain oil, stir well, add 20 g of ginkgo ketone ester, stir for 24 hours, and filter to obtain ginkgo ketone ester self-microemulsion. In addition, 90 g of microcrystalline cellulose and 10 g of crospovidone were weighed, mixed evenly, and the above-mentioned ginkgo ketone ester self-microemulsion was added to prepare a soft material, which was extruded and spheronized to obtain a drug-containing pill core. Dry the pellet core containing the drug in a drying oven at 60°C for 2 hours, and take it out.

[0030] Preparation of coating solution: ethyl cellulose 3g, talc powder 0.45g, PEG4000 0.4g, dissolved in 100mL absolute ethanol solution to obtain coating solution; weigh 100g containing pill core, put it into extrusion spheronization coating machine for preheating After 10 minutes, coat with coating solution. After coating, the coated pellets were taken out and dried in a ...

Embodiment 3

[0032] Weigh 42.5g of polyoxyethylene castor oil EL35, 42.5g of polyethylene glycol 400 and 15g of medium chain oil, stir evenly, add 20g of ginkgo ketone ester, stir for 24h, and filter to obtain ginkgo ketone ester self-microemulsion. In addition, 80 g of microcrystalline cellulose and 20 g of crospovidone were weighed, mixed evenly, and the above-mentioned ginkgo ketone ester self-microemulsion was added to prepare a soft material, which was extruded and spheronized to obtain a drug-containing pill core. Dry the pellet core containing the drug in a drying oven at 60°C for 2 hours, and take it out.

[0033] Preparation of coating liquid: ethyl cellulose 3g, talc powder 1.2g, PEG4000 0.6g, dissolved in 100mL absolute ethanol solution to obtain coating liquid; weigh 100g containing pill core, put it into extrusion spheronizing coating machine for preheating After 10 minutes, coat with coating solution. After coating, the coated pellets were taken out and dried in a drying ove...

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Abstract

A ginkgo ketone ester solid self-microemulsion sustained-release pellet. The sustained-release pellet is composed of a drug-containing pill core and a sustained-release layer. Ketone; the composition of the coating material of the sustained-release layer includes: ethyl cellulose, anti-sticking agent talcum powder and plasticizer polyethylene glycol 4000. The ginkgo ketone ester solid self-microemulsion sustained-release pellets of the present invention are used for oral administration. After entering the body, they can be self-micro-emulsified to form droplets less than 100nm under the action of gastrointestinal fluid, which not only increases the concentration of ginkgo ketone ester The solubility makes the ginkgo ketone ester release slowly within 24 hours, and has obvious slow-release characteristics. The results of pharmacokinetic research in Beagle dogs show that AUC0-24 and Cmax of the sustained-release pellets of the present invention all increase, t1 / 2 and MRT prolong, and Tmax prolongs 2h, which is comparable to the commercially available preparation Xingling Granules. Compared with that, the relative bioavailability of the sustained-release pellets of the present invention is 236.18%, and the oral bioavailability of the ginkgo ketone ester is significantly improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a ginkgo ketone ester solid self-microemulsion sustained-release pellet and a preparation method thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the most serious diseases threatening human beings in the world today. Its morbidity and mortality have surpassed tumor diseases and ranked first in the world. There is no breakthrough treatment method for chemical drugs in this respect: calcium ion blockers have a certain curative effect, but their neurotoxic side effects seriously affect their clinical application; although thrombolytic drugs have certain effects, they have certain hemorrhage-causing risk. [0003] Ginkgo ketone ester (GBE50) is a new generation of ginkgo biloba extract, containing a variety of active ingredients, which can improve human blood circulation, dilate coronary arteries and cerebral arteries; e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/16A61K9/16A61P9/00
Inventor 徐希明石小磊朱源余江南沈玉萍
Owner JIANGSU UNIV
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