Unlock instant, AI-driven research and patent intelligence for your innovation.

Riboflavin-5'-lauric acid monoester crystal form and preparation method thereof as well as medicine composite containing same

A technology of lauric acid monoester and riboflavin, which is applied in the direction of drug combination, medical preparations containing active ingredients, organic chemistry, etc., to achieve the effects of shortening the production cycle, large suction filtration resistance, and saving equipment

Inactive Publication Date: 2010-03-31
SHENZHEN SALUBRIS PHARMA
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, there is no report about riboflavin-5'-lauric acid monoester crystal form and its preparation method and pharmaceutical composition containing the crystal form

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Riboflavin-5'-lauric acid monoester crystal form and preparation method thereof as well as medicine composite containing same
  • Riboflavin-5'-lauric acid monoester crystal form and preparation method thereof as well as medicine composite containing same
  • Riboflavin-5'-lauric acid monoester crystal form and preparation method thereof as well as medicine composite containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 1 gram of riboflavin-5'-lauric acid monoester sample, add it to 10ml of N,N-dimethylformamide, raise the temperature to 70°C, stir and dissolve completely, pour it into 50ml of methanol in an ice-water bath, and stir to precipitate the solid Stirring was continued for half an hour, suction filtered, the precipitate was washed with methanol and vacuum-dried to constant weight to obtain 0.85 g of powdered riboflavin-5'-lauric acid monoester crystal form product. Gained riboflavin-5'-lauric acid monoester crystal form product adopts melting point measuring instrument to measure that its melting point is 250~252 ℃ of decomposition, and its X-ray diffraction pattern is as follows figure 1 As shown, its infrared spectrum is shown as figure 2 shown.

[0037] The resulting riboflavin-5'-lauric acid monoester crystal sample and riboflavin-5'-lauric acid monoester sample were subjected to the following stability test: two batches of samples were placed in a stability resea...

Embodiment 2

[0040]Take 100 grams of riboflavin-5'-lauric acid monoester sample, add it to 800ml N,N-dimethylformamide, heat up to 80°C, stir and dissolve completely, pour it into 4000ml ice-water bath methanol, and stir to precipitate the solid Stirring was continued for half an hour, suction filtered, the precipitate was washed with methanol and vacuum-dried to constant weight to obtain 87 g of powdered riboflavin-5'-lauric acid monoester crystal form product. The X-ray diffraction spectrum of the product obtained and the melting point measured by a melting point analyzer are basically consistent with the product obtained in Example 1.

Embodiment 3

[0042] Take 1 gram of riboflavin-5'-lauric acid monoester sample, add it to 6ml of N,N-dimethylacetamide, heat up to 100°C, stir to dissolve completely, pour it into 30ml of methanol in an ice-water bath, and stir to precipitate the solid Stirring was continued for half an hour, suction filtered, the precipitate was washed with methanol and vacuum-dried to constant weight to obtain 0.8 g of powdered riboflavin-5'-lauric acid monoester crystal form product. The X-ray diffraction spectrum of the product obtained and the melting point measured by a melting point analyzer are basically consistent with the product obtained in Example 1.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a riboflavin-5'-lauric acid monoester crystal form and a preparation method thereof as well as a medicine composite containing the same. The crystal form is expressed with 20 degrees angle as having peaks at degrees of 10.7, 20.1, 27.2 and 23.0 with error being +0.2 degree in X powder diffraction diagram. The preparation method thereof comprises adding riboflavin-5'-lauric acid monoester into low-molecular liquid acidamide for dissolution, and afterwards pouring into methanol, or acetone, or ethyl formate to precipitate the riboflavin-5'-lauric acid monoester crystal form. The invention also discloses a medicine composite containing the crystal form. The inventive riboflavin-5'-lauric acid monoester improves stability and greatly improves medicinal application prospect; the crystal form product of the invention is powdery, can be made into preparation by directly homogenizing without smashing, thus saving equipment, power and labor cost for industrialized production, and shortening production period.

Description

technical field [0001] The invention belongs to the field of preparation of pharmaceutical compounds, in particular to a crystal form of riboflavin-5'-lauric acid monoester, a preparation method thereof and a pharmaceutical composition containing the crystal form. Background technique [0002] Riboflavin is a component of the prosthetic group of flavin enzymes, participates in the complex oxidation process of the body, and has important pharmacological effects. Pharmacological studies in recent years have shown that, in addition to treating traditional riboflavin deficiency diseases, riboflavin also has pharmacological effects in treating coronary heart disease, hypertension complications, burns, etc. However, riboflavin is a water-soluble vitamin, which is easily excreted from sweat and urine, has a short half-life and low bioavailability. Therefore, when the intake of riboflavin is insufficient or needs to be increased, it is very easy to cause cheilitis, angular stomatit...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D475/14A61K31/525A61P3/02
Inventor 郑加林张昌中
Owner SHENZHEN SALUBRIS PHARMA