In-situ preparation method for starch-ibuprofen clathrate compound of V-type crystal structure

A technology of in-situ preparation and crystalline structure, applied in the directions of pharmaceutical formulation, drug combination, drug delivery, etc., can solve the problems of high price of β-cyclodextrin, limited application range, poor starch emulsification, etc., and achieves low cost and simplification. The preparation process and the effect of high product yield

Inactive Publication Date: 2016-02-03
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with starch, the price of β-cyclodextrin is higher, and its application scope as the main body of inclusion compound is not wide, which limits its industrial application to a certain extent
However, the emulsification of native starch is p...

Method used

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  • In-situ preparation method for starch-ibuprofen clathrate compound of V-type crystal structure
  • In-situ preparation method for starch-ibuprofen clathrate compound of V-type crystal structure
  • In-situ preparation method for starch-ibuprofen clathrate compound of V-type crystal structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] a. Accurately weigh a certain amount of ibuprofen (the ratio of ibuprofen and starch is 1:4) and add it to the ethanol solution with a dilution of 70%, stir to make it completely dissolve, then add a certain amount of potato starch to adjust The concentration is 70g / L starch milk, put it into a constant temperature stirrer and keep it at 45°C, and keep stirring;

[0025] b. Add a certain amount of 8mL3mol / L NaOH dropwise into the starch milk at a constant speed of 4mL / min. After the dropwise addition, stir at constant temperature for 60min to make it fully react;

[0026] c. After the reaction is completed, the starch milk is suction-filtered, and the filter cake is dispersed with 60% ethanol solution 20 times the weight of the starch, and the pH is adjusted to 7.0 with 3% (V / V) hydrochloric acid-ethanol solution, and the suction filtration is continued to obtain the filter cake Wash 3 times with 95% ethanol, then wash 1 time with absolute ethanol;

[0027] d. The prod...

Embodiment 2

[0030] a. Accurately weigh a certain amount of ibuprofen (the ratio of ibuprofen and starch is 1:4) and add it to the ethanol solution with a dilution of 50%, stir to make it completely dissolve, then add a certain amount of potato starch to adjust The concentration is 80g / L starch milk, put it into a constant temperature stirrer and keep it at 50°C, and keep stirring;

[0031] b. Add a certain amount of 8mL3mol / L NaOH dropwise to the starch milk at a constant speed of 4mL / min. After the dropwise addition, stir at constant temperature for 40min to make it fully react;

[0032] c. After the reaction is completed, the starch milk is suction-filtered, and the filter cake is dispersed with 60% ethanol solution 20 times the weight of the starch, and the pH is adjusted to 7.0 with 3% (V / V) hydrochloric acid-ethanol solution, and the suction filtration is continued to obtain the filter cake Wash 3 times with 95% ethanol, then wash 1 time with absolute ethanol;

[0033] d. The produc...

Embodiment 3

[0036]a. Accurately weigh a certain amount of ibuprofen (the ratio of ibuprofen and starch is 1:4) and add it to the ethanol solution with a dilution of 50%, stir to make it completely dissolve, then add a certain amount of potato starch to adjust Starch milk with a concentration of 70g / L, put it in a constant temperature stirrer and keep it at 55°C, and keep stirring;

[0037] b. Add 12mL of 3mol / L NaOH dropwise to the starch milk at a constant speed of 4mL / min. After the dropwise addition, stir at constant temperature for 30min to make it fully react;

[0038] c. After the reaction is completed, the starch milk is suction-filtered, and the filter cake is dispersed with 60% ethanol solution 20 times the weight of the starch, and the pH is adjusted to 7.0 with 3% (V / V) hydrochloric acid-ethanol solution, and the suction filtration is continued to obtain the filter cake Wash 3 times with 95% ethanol, then wash 1 time with absolute ethanol;

[0039] d. The product obtained abov...

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Abstract

The invention belongs to the field of pharmaceutical technologies, and particularly relates to an in-situ preparation method for a starch-ibuprofen clathrate compound of a V-type crystal structure. The method includes the steps that with potato starch as the raw material, ibuprofen is dissolved in a diluted ethanol solution, a certain amount of potato starch is added, an NaOH solution is slowly added, mixing and sufficient constant-temperature stirring are performed, and the mixed solution is kept reacting for certain time; then, the mixed solution is titrated through a hydrochloric acid ethanol solution to have the pH of 7.0 and slowly stirred for certain time, and extraction, washing, drying and smashing are performed to obtain the starch-ibuprofen clathrate compound. The starch-ibuprofen clathrate compound is structurally characterized by being of the V-type crystal structure, the preparation process is simple, and cost is low. The accumulative release rate of the starch-ibuprofen clathrate compound in simulated gastric fluid (pH 1.2) is smaller than 7%, and an active compound is slowly released in simulated intestinal fluid (pH 7.4) under the action of enzyme to take effect, so that drug bioavailability is improved, and the side effect of stimulating the gastrointestinal tract is avoided.

Description

technical field [0001] The invention relates to a method for in-situ preparation of starch ibuprofen inclusion compound with V-type crystal structure. In the process of preparing cold-water soluble starch by alcohol-alkali method, ibuprofen raw material is added to prepare starch and ibuprofen in-situ V-type crystal structure clathrate, the clathrate can realize the controlled release of ibuprofen through α-amylase enzymatic hydrolysis of starch, and reduce the side effect of ibuprofen on gastrointestinal stimulation, the invention belongs to the field of pharmaceutical technology research . Background technique [0002] Ibuprofen is a non-steroidal anti-inflammatory drug (Nonsteroidal Antiinflammatory Drugs, NSAIDs), has a variety of medicinal effects, such as antipyretic, analgesic, anti-inflammatory effects, used for antipyretic and analgesic, treatment of rheumatism and rheumatoid joints Inflammation and so on. However, it has been found in clinical practice that the b...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/192A61K9/22A61K9/52A61P29/00A61P19/02A61K47/61
Inventor 张黎明郑超云申蕊曹杰康彩彩张恺骅刘娜
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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