Total tanshinone composite preparation

A technology of compound preparation and total tanshinone, which is applied in the directions of antidote, pill delivery, drug combination, etc., can solve the problems of not comprehensively considering the effective components of tanshinone, low oral bioavailability of tanshinone, unsatisfactory absorption of tanshinone, etc., and achieves a control method. Convenience, improved bioavailability, enhanced metabolic stability

Inactive Publication Date: 2011-06-22
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although tanshinone has good efficacy, there are the following problems in tanshinone preparations at present: 1. Tanshinone has low solubility in water, and cannot be dissolved smoothly in the gastrointestinal tract after ordinary oral preparations; 2. The absorption of tanshinone in the gastrointestinal tract is not ideal, thereby causing Oral bioavailability is low, which seriously affects the efficacy of tanshinone; ③The existing drug-loading system is only for the single component of tanshinone IIA, and does not comprehensively consider other active components in tanshinone

Method used

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Examples

Experimental program
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Embodiment 1

[0032] Embodiment 1 Tanshinone self-microemulsion preparation and particle size determination

[0033] Weigh 4g of medium-chain triglyceride, 4g of polyoxyethylene (40) hydrogenated castor oil, and 2g of 1,2-propylene glycol, and mix the three evenly in a water bath at 60°C to obtain a clear blank self-microemulsion, and then add Salvia miltiorrhiza 100mg of total ketone powder, in a water bath at 60°C to 80°C, shake vigorously with a rapid mixer to fully dissolve tanshinone, and obtain a dark red clear tanshinone self-microemulsion.

[0034] Tanshinone is added 100 times of water dilutions from microemulsion, Malvern laser particle size analyzer (Malvern Zetasizer nano zs 90) measures particle size, the particle size distribution of formed microemulsion is as follows: figure 1 , The average particle size is 79.54nm, the dispersion is uniform, and the polydispersity index PDI is 0.219.

Embodiment 2

[0035] Embodiment 2 Tanshinone self-microemulsion preparation and absorption evaluation

[0036] Weigh 3 g of medium chain triglyceride, 4.7 g of polyoxyethylene (40) hydrogenated castor oil, and 2.3 g of 1,2-propanediol, and mix the three evenly in a water bath at 60° C. to obtain a clear blank self-microemulsion, and then Add 100 mg of total tanshinone powder, place in a water bath at 60°C to 80°C, and shake vigorously with a rapid mixer to fully dissolve tanshinone to obtain a dark red clear tanshinone self-microemulsion.

[0037]Add tanshinone from the microemulsion to 100 times of water to dilute to obtain the microemulsion for use, and simultaneously prepare 10 g of mixed surfactant according to the ratio of polyoxyethylene (40) hydrogenated castor oil: 1,2-propylene glycol 2:1 (w / w), Add 100 mg of tanshinone powder, shake vigorously in a water bath at 60°C to 80°C to fully dissolve tanshinone, add 100 times of water to dilute to obtain the corresponding tanshinone micel...

Embodiment 3

[0039] Embodiment 3 Preparation of tanshinone self-microemulsion-sodium alginate microspheres

[0040] Weigh 4g of medium-chain triglyceride, 4g of polyoxyethylene (40) hydrogenated castor oil, and 2g of 1,2-propylene glycol, and mix the three evenly in a water bath at 60°C to obtain a clear blank self-microemulsion, and then add Salvia miltiorrhiza 200 mg of total ketone powder, under a water bath at 60°C to 80°C, shake vigorously with a rapid mixer to fully dissolve tanshinone, and obtain a dark red clear tanshinone self-microemulsion.

[0041] Add the above-mentioned tanshinone self-microemulsion to 100 times of 0.75% ~ 2% 100cp sodium alginate solution, 100r min at 37°C -1 Shake at constant temperature for 10 minutes to emulsify completely, and drop 1.1% CaCl into the solution with an electrostatic droplet microcapsule preparation instrument 2 In the gel bath, tanshinone microspheres are formed, which look like Figure 5 , Tanshinone microcapsules are orange-red, smooth,...

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Abstract

The invention relates to a total tanshinone composite preparation, in particular to a self-microemulsion medicine carrying composite preparation for improving the oral administration bioavailability of total tanshinone, which comprises the following components in part by mass: 0.5 to 5 parts of tanshinone, 25 to 75 parts of oil phase, 35 to 70 parts of surfactant and 0 to 25 parts of cosurfactant. In addition, the preparation can be prepared into a solid preparation or a liquid preparation by combining with other solid materials or water, and after entering a gastrointestinal tract, the solidpreparation or the liquid preparation can be emulsified automatically to form microemulsion of which the grain diameter is less than 100 nanometers when contacting water so as to increase the dissolution speed of the tanshinone, promote the absorption of the tanshinone and improve the oral administration bioavailability of the tanshinone; and the preparation conditions of the total tanshinone composite preparation is mild, a control method is simple and convenient, and special equipment is not required.

Description

technical field [0001] The invention relates to a compound preparation of tanshinone, in particular to an oral drug-loading system of tanshinone, which is an oral self-microemulsion drug-loading compound preparation with tanshinone as the main drug. Background technique [0002] Tanshinone (tanshinones) is a fat-soluble active ingredient extracted from the root of the Chinese herbal medicine Salvia miltiorrhiza. Its common feature is that it has a structure of o-quinone or p-quinone. The main active ingredients are tanshinone I, tanshinone IIA, cryptotanshinone, dihydrotanshinone, etc. They are in A variety of biochemical reactions are prone to occur in organisms, showing a variety of pharmacological effects. According to pharmacological studies, tanshinone has anti-atherosclerosis effect, reduces myocardial infarction size, reduces myocardial oxygen consumption, anti-arrhythmia and other good therapeutic effects on cardiovascular diseases; It has good anti-tumor effects su...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/537A61K31/58A61K9/107A61K9/16A61K9/20A61K9/48A61K9/14A61K9/00A61P9/00A61P9/10A61P9/06A61P35/00A61P31/04A61P39/06A61K125/00
Inventor 马小军杨荣平汪圣华吕国军谢威扬赵姗
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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