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A kind of composition for improving the bioavailability of crocus acid and oral preparation thereof

A technology of crocetin and oral preparations, which is applied in the direction of drug combinations, anhydride/acid/halide active ingredients, medical preparations of non-active ingredients, etc., and can solve low bioavailability, low solubility, poor stability, etc. problem, to achieve the effect of large contact area, simple process, and pH improvement

Active Publication Date: 2022-05-17
HANGZHOU JIURUTANG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to overcome the deficiencies in the prior art and solve the problems of low solubility, poor absorption, low bioavailability, and poor stability in the preparation of crocetin preparations in the prior art, the invention provides a method for improving insoluble drug crocetin. Composition, oral preparation and preparation method of safflower acid bioavailability

Method used

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  • A kind of composition for improving the bioavailability of crocus acid and oral preparation thereof
  • A kind of composition for improving the bioavailability of crocus acid and oral preparation thereof
  • A kind of composition for improving the bioavailability of crocus acid and oral preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1-3

[0068] The preparation of embodiment 1-3 crocetin composition

[0069] prescription

[0070]

[0071] Preparation Process:

[0072] ①Take the prescribed amount of crocetin, Soluplus and meglumine and carry out manual sieving and mixing for 3 times to obtain mixture I.

[0073] 2. Add the mixture I and the grinding beads with a weight ratio of 1:20 to the ball mill jar and install it on the ball mill, set the ball milling time to 1 minute, the ball milling frequency to 60 Hz, the intermittent time to 60 seconds, and the number of cycles to be 15 times to obtain Crocetin Composition II.

[0074] Measure the in vitro dissolution of embodiment 1-3 respectively, take pH6.8 phosphate buffer as the dissolution medium, the dissolution medium volume is 900ml, and the rotating speed is 75 revs / min, adopts slurry method to carry out dissolution experiment, high performance liquid chromatography measures Dissolution results, calculate the cumulative dissolution rate, the results are...

Embodiment 4-6

[0078] The preparation of embodiment 4-6 crocetin composition

[0079] prescription

[0080]

[0081] Preparation Process:

Embodiment 4

[0083] ①Take the prescribed amount of crocetin, Soluplus and meglumine and carry out manual sieving and mixing for 3 times to obtain mixture I.

[0084] 2. Mixture I and the grinding beads of weight ratio 1:20 are added in the ball mill tank and installed on the ball mill, the setting ball milling time is 1 minute, the ball milling frequency is 60 Hz, the intermittent time is 60 seconds, and the number of cycles is 5 times, to obtain Crocetin Composition II.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a composition for improving the bioavailability of an insoluble drug crocetin, an oral preparation and a preparation method thereof. The composition for improving the bioavailability of insoluble drug crocetin according to the present invention is as follows: 1 part of insoluble drug crocetin, 1-10 parts of hydrophilic polymer carrier material, 1-10 parts of pH regulator share. The preparation method of the composition is to use the principle of mechanochemistry to ball mill crocetin, a hydrophilic polymer carrier and a pH regulator to obtain a crocetin composition, and then mix the composition with a suitable diluent , disintegrating agent, binding agent, and lubricant are prepared into oral preparations of crocetin according to a conventional solid preparation preparation process. The oral preparation of crocetin prepared by the present invention dissolves rapidly in vitro and is rapidly absorbed in the body after oral administration, which greatly improves the oral bioavailability of crocetin. The preparation process of the preparation is simple and reproducible, and is suitable for industrialization Production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a composition for improving the bioavailability of an insoluble drug crocetin, an oral preparation and a preparation method thereof, in particular to a method for improving the bioavailability of an insoluble drug crocetin Compositions, oral preparations and preparation methods thereof. Background technique [0002] Saffron is the traditional Chinese medicine name of Crocus sativus of the family Iridaceae. It is native to southern Europe and is cultivated in Zhejiang, Anhui, Shanghai, Sichuan, Xinjiang, Guangxi and other places in my country. The main producing areas of saffron in the world are Iran. Saffron is sweet in taste, flat in nature, home to the heart and liver meridian, has the functions of promoting blood circulation and removing blood stasis, cooling blood and detoxification, relieving stagnation and calming the nerves, etc. Madness an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/557A61K36/88A61K47/02A61K47/10A61K47/18A61K47/32A61P3/06A61P9/10A61P9/12A61P25/08A61P25/20A61P25/28
CPCA61K9/2054A61K9/1652A61K31/557A61K47/32A61K47/10A61K47/183A61K47/18A61K47/02A61K36/88A61P25/08A61P25/20A61P25/28A61P9/12A61P3/06A61P9/10Y02A50/30
Inventor 王平徐子金童哲仁
Owner HANGZHOU JIURUTANG BIOTECH