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Bilobalide B injection and preparation thereof

A technology of ginkgolide and injection, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as difficulty in industrialization, difficulty in injections, poor solubility, etc., and achieve cost Inexpensive, excellent stability, good stability effect

Active Publication Date: 2008-11-12
NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The content of Ginkgolide B in Ginkgo biloba and Ginkgo leaf extract is very low. The ginkgo preparations that appear on the market currently mainly use total ginkgo lactones and total flavonoids as the effective parts, and there is no monomer Ginkgo preparation. Currently, Ginkgo The acquisition of ester B monomer is mainly through liquid phase preparation, which is difficult to form industrialization
At the same time, ginkgolide B has poor solubility in water, and Span and Tween-80, which can be used to aid in dissolution, have been clearly identified as excipients that cause adverse reactions in injections by experts from the National Bureau of Medicine.
At present, it is difficult to make ginkgolide B into injections, so it is difficult to give full play to its therapeutic advantages

Method used

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  • Bilobalide B injection and preparation thereof
  • Bilobalide B injection and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Preparation of Ginkgolide B injection:

[0039] prescription:

[0040] Ginkgolide B 2g

[0041] Ethanol 150ml

[0042] PEG600 200ml

[0043] Glycerin 50ml

[0044] Water for injection 600ml

[0045] Preparation method: Take the above prescription amount of Ginkgolide B (Taiyuan Xingyuan Biochemical Co., Ltd.), add 150ml of ethanol, PEG600200ml, and 50ml of glycerin, heat to 60℃ and stir to fully dissolve the Ginkgolide B, then add 600ml of water for injection. Heat to 100°C and stir and mix well, add 0.3g activated carbon, stir for 15min, decarbonize, filter, potting, sterilize, light inspection, and packaging to obtain ginkgolide B water injection.

Embodiment 2

[0047]1. Preparation of Ginkgolide B: Weigh 10kg of Ginkgo biloba leaves, add 500L of 1% hydrochloric acid and cook for 30min, filter to obtain 480L of filtrate, extract with 480L of n-butanol, concentrate the extract to an appropriate amount, add an appropriate amount of 100-200 mesh Silica gel, mix and dry, apply to silica gel column (diameter-to-height ratio is 1:1, silica gel dosage is 3kg), prepare mobile phase with the ratio of ethyl acetate:acetone 4:6, control the flow rate 210ml / min, collect the ginkgo The 40L effluent of ester B was concentrated to dryness to obtain 6 g of dry paste, and 180 ml of 95% ethanol was added to crystallize to obtain 2.3 g of ginkgolide B raw material, in which the content of ginkgolide B was 91.5%.

[0048] 2. Preparation of Ginkgolide B injection:

[0049] prescription:

[0050] Ginkgolide B 4g

[0051] Ethanol 400ml

[0052] PEG600 100ml

[0053] Glycerin 50ml

[0054] Water for injection 450ml

[0055] Preparation method: Take prescription ...

Embodiment 3

[0057] 1. Preparation of Ginkgolide B: Weigh 1 kg of Ginkgo biloba extract (in accordance with the requirements of the Chinese Pharmacopoeia 2000 Edition, Taiyuan Xingyuan Biochemical Co., Ltd.), add 5L of 0.1% hydrochloric acid for 30min, filter, and obtain 4.8L of filtrate , Extract with 4.8L of ethyl acid, concentrate the extract to an appropriate amount, add an appropriate amount of 100-200 mesh silica gel, mix and dry, and load on a silica gel column (diameter-to-height ratio of 1:1, silica gel dosage 2.5kg), with n-butyl The mobile phase was prepared with a ratio of alcohol: petroleum ether of 8:2, the flow rate was controlled to 360ml / min, the 35L effluent was collected, concentrated to dryness to obtain 5g of dry paste, and 150ml of 95% ethanol was added to crystallize to obtain 1.7g of ginkgolide B raw material, in which, Ginkgolide B content is 90.7%.

[0058] 2. Preparation of Ginkgolide B injection:

[0059] prescription:

[0060] Ginkgolide B 0.5g

[0061] Ethanol 100...

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Abstract

The invention relates to a ginkgolide B injection and a method for making the same. The method comprises the following steps that: ginkgolide B is taken as a raw material and is added in ethanol, glycerol and PEG600, wherein the ratio between the ginkgolide B and the ethanol is between 1:25 and 1:200; the ratio between the ginkgolide B and the PEG600 is between 1:25 and 1:600; and the ratio between the ginkgolide B and the glycerol is between 1:12.5 and 1:50. The ginkgolide B injection has good stability and low cost, and each index of the injection meets the requirements of preparation; moreover, the making process of the injection has the characteristics of quick dissolution of a raw material and simple process, and is suitable for industrialized production.

Description

Technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and specifically relates to a ginkgolide B injection and a preparation method thereof. technical background [0002] Ginkgolide is currently one of the powerful specific platelet activating factor (PAF) receptor blockers. Ginkgolide B has the strongest blocking effect on PAF receptor among ginkgolides, and can be eliminated in a dose-dependent manner. The platelet aggregation caused by PAF prevents the formation of thrombus, but has no effect on platelet aggregation induced by adenosine diphosphate, arachidonic acid, collagen and epinephrine. The latest pharmacological research shows that Ginkgolide B has anti-allergic, anti-inflammatory, anti-shock effects, and also has a protective effect on ischemic injury and rejection of organ transplantation. [0003] The content of Ginkgolide B in Ginkgo biloba leaves and Ginkgo biloba extracts is very low. Ginkgo biloba preparations current...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/365A61K47/34A61P9/10A61K47/10
Inventor 许益清徐林张朝波朱敬
Owner NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD
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