Gastrodin multiphase liposome injection

A multiphase liposome and gastrodin technology, applied in the field of medicine, can solve the problems of incomplete encapsulation of gastrodin and unsatisfactory compatibility, so as to improve bioavailability, improve product quality of preparations, and good encapsulation rate Effect

Inactive Publication Date: 2012-08-08
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0015] Patent document CN1411803A discloses adopting lecithin, phosphatidylcholine / cholesterol, soybean lecithin, stearylamide to prepare the method for the proliposome of gastrodin, yet because the compatibility of gastrodin and above-mentioned film-forming material is not ideal enough , resulting in liposomes not completely encapsulating gastrodin

Method used

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  • Gastrodin multiphase liposome injection
  • Gastrodin multiphase liposome injection
  • Gastrodin multiphase liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Preparation of Gastrodin Multiphase Liposome Injection

[0060] The components and weights of the raw and auxiliary materials used are as follows:

[0061]

[0062] The gastrodin heterogeneous liposome injection was prepared by the following preparation process:

[0063] (1) 50g Tween 80, 50g polyoxyethylene 40 hydrogenated castor oil, 200g cholesterol and 200g soybean phosphatidylinositol were dissolved in 500ml pH value of phosphate buffered saline solution of 6.8, stirred and ultrasonically pulverized twice, each 10 minutes each time, then add 60g trehalose and mix evenly, freeze-dry under vacuum condition, make the heterogeneous liposome of unencapsulated medicine;

[0064] (2) Dissolve 100g gastrodin in 200ml of phosphate buffer solution with a pH value of 6.8, dissolve it, and process it twice by ultrasonication for 10 minutes each time;

[0065] (3) Add gastrodin buffered saline and EDTA-2Na to the heterogeneous liposome of unencapsulated medicin...

Embodiment 2

[0067] Example 2 Preparation of Gastrodin Multiphase Liposome Injection

[0068] The components and weights of the raw and auxiliary materials used are as follows:

[0069]

[0070] The gastrodin heterogeneous liposome injection was prepared by the following preparation process:

[0071] (1) 70g Tween 80, 70g polyoxyethylene 40 hydrogenated castor oil, 300g cholesterol and 300g soybean phosphatidylinositol were dissolved in 1000ml pH value of phosphate buffered saline solution of 6.8, stirred, ultrasonic pulverization was processed twice, each 10 minutes each time, then add 40g trehalose and mix evenly, freeze-dry under vacuum condition, make the heterogeneous liposome of unencapsulated medicine;

[0072] (2) 200g gastrodin was dissolved in 400ml of phosphate buffered saline solution with a pH value of 6.8, dissolved, and subjected to ultrasonic treatment twice, each time for 10 minutes;

[0073] (3) Add gastrodin buffered saline and EDTA-2Na to the heterogeneous liposo...

Embodiment 3

[0075] Example 3 Preparation of Gastrodin Multiphase Liposome Injection

[0076] The components and weights of the raw and auxiliary materials used are as follows:

[0077]

[0078]

[0079] The gastrodin heterogeneous liposome injection was prepared by the following preparation process:

[0080] (1) 100g Tween 80, 100g polyoxyethylene 40 hydrogenated castor oil, 200g cholesterol and 400g soybean phosphatidylinositol were dissolved in 2000ml pH value of phosphate buffered saline solution of 6.8, stirred, ultrasonic pulverized twice, each 10 minutes each time, then add 150g trehalose and mix evenly, freeze-dry under vacuum condition, make the heterogeneous liposome of unencapsulated medicine;

[0081] (2) 500g gastrodin was dissolved in 1000ml of phosphate buffer solution with a pH value of 6.8, dissolved, and subjected to ultrasonic treatment twice, each time for 10 minutes;

[0082] (3) Add gastrodin buffered saline and EDTA-2Na to the heterogeneous liposome of unen...

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Abstract

The invention discloses a gastrodin multiphase liposome injection and a preparation method thereof. Gastrodin, soybean phosphatidylinositol, cholesterol, Twain 80, polyoxyethylene 40, hydrogenated castor oil, trehalose and EDTA-2Na which have specific weight ratios are prepared into the gastrodin multiphase liposome injection. The gastrodin multiphase liposome injection provided by the invention has excellent preparation stability and meets the demand of intravenous injection; after the gastrodin multiphase liposome injection is stored for a long time, the excellent encapsulation of the liposome is kept; the solubility of gastrodin is increased; the quality of preparation product is increased; the toxic side effect is reduced; the retention time of medicine in systemic circulation is increased; the bioavailability of the medicine is increased; the curative effect is obviously increased; and the preparation method is simple and is suitable for industrial production in bulk.

Description

technical field [0001] The invention relates to a gastrodin injection, in particular to a gastrodin multiphase liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] In the current market, Gastrodin (Glastrodin) is the dry root extract of the orchid plant Gastrodia elata, and the origin of the raw material is Yunnan. The chemical name of gastrodin is: 4-hydroxymethylbenzene-β-D glucopyranoside hemihydrate, molecular formula: C 13 h 18 o 7 1 / 2H 2 O, molecular weight 295.38, structural formula: [0003] [0004] Gastrodin injection can expand cerebral blood vessels, improve the ability of brain cells to resist hypoxia, increase cerebral blood flow, and reduce cerebral vascular resistance. In particular, it has a good effect on improving the blood flow of the vertebral-basilar artery, so that the cerebral blood supply of patients with vertebral-basilar artery insufficiency can be significantly imp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7034A61K47/44A61P25/00A61P25/06A61P9/00A61P25/02A61P1/08A61P27/16A61P9/10A61K47/26A61K47/28
Inventor 陈彦陶灵刚
Owner 灵康药业集团股份有限公司
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