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Silibinin injection composition and preparation process

A technology of silibinin and injection, which is applied in the field of composition and preparation of silibinin injection, can solve the problems of inability to obtain microparticle preparations, poor compatibility, poor fat solubility, etc., and achieve low toxicity and stability Good performance and low dosage of excipients

Inactive Publication Date: 2013-12-11
SHANGHAI TIANSHILI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used solubilizers include Tween 80, polyoxyethylene castor oil, etc., and this solubilizer has severe hemolysis and allergic reactions, and there are many reports of clinical adverse reactions; the encapsulated particle preparation is a water-insoluble drug encapsulated in a carrier material , common microparticle preparations include liposomes, emulsions, etc., but due to the poor fat solubility of silibinin and poor compatibility with such packaging materials, safe and stable microparticle preparations cannot be obtained

Method used

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  • Silibinin injection composition and preparation process
  • Silibinin injection composition and preparation process
  • Silibinin injection composition and preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: A kind of composition of silybin injection

[0040] Preparation of silybin injection:

[0041] Weigh 1 g of silibinin and 0.5 g of citric acid, add it to 90 g of polyethylene glycol 400, stir and dissolve at 70°C, then dilute to 100 ml with polyethylene glycol 400; add 0.1 g of activated carbon for needles , adsorbed at a temperature of 70°C for 30 minutes, then filtered with a capsule filter, divided into 5ml / branches, sealed, and sterilized at 121°C in a high-pressure steam sterilizer for 15 minutes to obtain silybin injection.

[0042] Preparation of emulsion:

[0043] Weigh 100 grams of caprylic triglyceride for injection, 100 grams of soybean oil, heat in a water bath to 75°C, add 12 grams of egg yolk phospholipids for injection, cut to dissolve, stir and mix to obtain the oil phase; measure 700 grams of water for injection milliliter, add 22.5 grams of glycerin, stir to dissolve, and heat to 75°C to obtain the water phase; mix the oil phase and the...

Embodiment 2

[0046] Embodiment 2: A kind of composition of silybin injection

[0047] Preparation of silybin injection:

[0048] Weigh 2 grams of silibinin and 1 gram of lactic acid, add it to 90 grams of polyethylene glycol 400, stir and dissolve at 60°C, then use polyethylene glycol 400 to make the volume to 100 ml; add 0.2 grams of activated carbon for needles, Adsorbed at a temperature of 70°C for 60 minutes, then filtered with a microporous membrane, divided into 2ml / bottle, sealed, and sterilized in a circulating steam sterilizer at 100°C for 30 minutes to obtain silybin injection.

[0049] Preparation of emulsion:

[0050] Weigh 200 grams of caprylic triglyceride for injection, heat it in a water bath to 65°C, add 12 grams of egg yolk phospholipids for injection, cut to dissolve, stir and mix to obtain the oil phase; measure 700 ml of water for injection, add glycerin 22.5 grams, stirred to dissolve, heated to 65°C to obtain the water phase; the oil phase and the water phase were ...

Embodiment 3

[0053] Embodiment 3: A kind of composition of silybin injection

[0054] Preparation of silybin injection:

[0055] Weigh 10 grams of silibinin, 0.1 grams of tartaric acid, and 0.1 grams of vitamin E, add to 80 grams of polyethylene glycol 400, stir and dissolve at 70 ° C, and then use polyethylene glycol 400 to make up to 100 ml; Adjust the pH value to 3.5; add 0.25 grams of activated carbon for needles, absorb at 70°C for 45 minutes, then filter with a microporous membrane, pack into 2.5ml / branch, seal, and use a rotary autoclave at 121°C Sterilize for 15 minutes to obtain silibinin injection.

[0056] Preparation of emulsion:

[0057] Weigh 300 grams of soybean oil for injection, heat it in a water bath to 80 ° C, add 3 grams of egg yolk phospholipids for injection, shear to dissolve, stir and mix to obtain an oil phase; measure 600 milliliters of water for injection, add 20 grams of glycerin, and stir to make Dissolve and heat to 80°C to obtain the water phase; mix the ...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, develops safe and reliable silibinin injection to overcome the shortcoming of poor solution of silibinin in water and shortcomings of existing preparations, and provides silibinin injection composition which comprises silibinin injection and emulsion. The silibinin injection is mixed with the emulsion prior to being directly subjected to intravenous drip or intravenous infusion during use of the silibinin injection composition. The invention further provides a preparation process of the silibinin injection composition. The silibinin injection contains no solubilizer which has high toxic and side effects, silibinin is dissolved in organic solvent for injection to prepare the injection which forms a water-free system, and accordingly the problem that medicine in water systems is easy to degrade during storage is solved, and clinical safety of medicine use is improved. In addition, the silibinin injection composition has the advantages of high loading capacity, low consumption of auxiliaries, low toxicity, high stability and the like, and the situation that silibinin intravenous administration preparations are difficult to develop is broken subtly.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a composition of silibinin injection and a preparation method thereof. Background technique [0002] Silibinin, English name: Silibinin, is an active ingredient extracted from the fruit of the botanical drug Silybum marianum (Jose F, Alvarez B. Extraction of nutraceuticals from milk thistle[J]. Appl Biochem Biotechnol, 2003, 10: 105-108 .), which belong to flavonoid lignans. Structural formula: [0003] [0004] Flavonoids (flavonoids), the basic structural features are 2-phenylbenzo [α] pyran or flavan nucleus, including two benzene rings (A and B) connected by a heterocyclic-pyran ring (C), according to The degree of oxidation of the central three-carbon chain, the position of the B-ring link and whether the three-carbon chain constitutes a ring, etc., the main flavonoids can be divided into flavonoids, flavonols, dihydroflavones, flavonolignans, dihydr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/357A61K47/44A61K47/34A61K47/32A61K47/24A61P3/06A61P1/16
Inventor 金文斌
Owner SHANGHAI TIANSHILI MEDICAL TECH