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Method for preparing carvedilol solid dispersions by virtue of supercritical anti-solvent technique

A supercritical anti-solvent, solid dispersion technology, applied in pharmaceutical formulations, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of obvious first-pass effect and low bioavailability, and achieve outstanding substantial Characteristics, optimization methods, effects of improving bioavailability

Active Publication Date: 2017-01-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Carvedilol belongs to Class II drugs in the Biopharmaceutical Classification System (BCS), and is insoluble in water. The drug is rapidly absorbed orally, but the first-pass effect is obvious, and the bioavailability is low, only about 25%.

Method used

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  • Method for preparing carvedilol solid dispersions by virtue of supercritical anti-solvent technique
  • Method for preparing carvedilol solid dispersions by virtue of supercritical anti-solvent technique
  • Method for preparing carvedilol solid dispersions by virtue of supercritical anti-solvent technique

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: single factor method determines the preferred value range of each key parameter

[0032] Instruments and materials

[0033] See Table 1 for experimental materials and Table 2 for experimental equipment.

[0034] Table 1 Experimental materials

[0035] material name Specification Manufacturer Carvedilol ≥99％ Wuhan Xingyinhe Chemical Co., Ltd. CO 2

≥99％ Nanjing Tongqi Gas Company Dichloromethane Analytical pure Nanjing Chemical Reagent Co., Ltd. Methanol Analytical pure Nanjing Chemical Reagent Co., Ltd. PVPK30 Premium Pure Shanghai Yuanye Biotechnology Co., Ltd.

[0036] Table 2 Experimental Instruments

[0037] device name model Manufacturer Supercritical Particle Preparation System Helix Applied Separations, USA Intelligent Dissolution Tester ZRS-8L Tianjin Tianda Tianfa Technology Co., Ltd. UV-visible spectrophotometer UV-1800 Shimadzu Corporatio...

Embodiment 2

[0066] Embodiment 2: Orthogonal experiment optimizes optimal parameters within the preferred range of each key parameter

[0067] Orthogonal experimental design and results

[0068] Carvedilol solid dispersion optimization process takes 60min cumulative dissolution rate as the main evaluation index, and selects three factors that have a more obvious impact on the index, crystallization pressure (A), crystallization temperature (B), and solution volume flow rate (C). To investigate, use L 9 (3 4 ) Orthogonal experimental design is carried out experiment, and its factor level has been determined by the single factor experiment of embodiment 1, see table 3. Other process conditions are CO 2 The exhaust volume flow rate is 3L / min, the ratio of carvedilol to PVP K30 is 1:2, and the organic solvent is dichloromethane. The experimental design and results are shown in Table 4.

[0069] Table 3 Orthogonal experiment factors and levels

[0070]

[0071] Table 4 Orthogonal exp...

Embodiment 3

[0083] A kind of supercritical antisolvent technology prepares the method for carvedilol solid dispersion, comprises the steps:

[0084] Step S1, dissolving carvedilol and a water-soluble carrier in an organic solvent to obtain a carvedilol-carrier mixed solution;

[0085] Step S2, the CO 2 Pass into the crystallization kettle, adjust the temperature and pressure in the crystallization kettle;

[0086] Step S3, continue to feed CO 2 , maintaining the temperature and pressure in the crystallization kettle constant, while passing the mixed solution prepared in step S1 into the crystallization kettle;

[0087] Step S4, after the carvedilol-carrier mixed solution is passed through, continue to pass through CO 2 , keep the temperature and pressure in the crystallization kettle constant, and finally release the pressure; when the pressure in the crystallization kettle drops to atmospheric pressure, open the crystallization kettle to collect carvedilol solid dispersion;

[0088] ...

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Abstract

The invention discloses a method for preparing carvedilol solid dispersions by virtue of a supercritical anti-solvent technique. The method comprises the following steps: (S1) dissolving carvedilol and a water-soluble carrier into an organic solvent, so as to obtain a carvedilol-carrier mixed solution; (S2) introducing CO2 into a crystallization kettle, and regulating the temperature and pressure in the crystallization kettle; (S3) continuing to introduce CO2 to keep the temperature and pressure in the crystallization kettle constant, and simultaneously introducing the mixed solution prepared in the step (S1) into the crystallization kettle; and (S4) after the carvedilol-carrier mixed solution is introduced, continuing to introduce CO2 to keep the temperature and pressure in the crystallization kettle constant, finally relieving the pressure, and after the pressure in the crystallization kettle is decreased to the atmospheric pressure, opening the crystallization kettle, and collecting the carvedilol solid dispersions. By virtue of the method, the carvedilol solid dispersions with obviously improved dissolution characteristics can be prepared, and furthermore, the bioavailability of indissolvable drugs can be improved.

Description

technical field [0001] The invention relates to the preparation of carvedilol solid dispersion, in particular to a method for preparing carvedilol solid dispersion by applying supercritical antisolvent technology. Background technique [0002] Solid dispersion technology is one of the methods to improve the dissolution rate of poorly soluble drugs. The principle of solubilization is mainly that the drug is highly dispersed in the corresponding carrier in the form of particles, microcrystals, molecules, colloids or amorphous state, and the carrier increases the wettability of the drug so that Improve its dissolution and absorption. Commonly used carrier materials for preparing solid dispersions include water-soluble carriers, poorly water-soluble carriers, and enteric carriers; preparation techniques include hot melt method, solvent method, and solvent-melt method And spray freeze drying method (spray / freezing drying method), etc. In recent years, the new supercritical anti...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61K9/14A61K47/32A61P9/12A61P9/10A61P9/04A61P9/06A61P27/06
CPCA61K9/146A61K31/403
Inventor 王志祥周进莉王为彦宋雅琴刘尚德张依缪虹刚
Owner CHINA PHARM UNIV
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