A preparation method of hydrophobically modified sodium alginate amphiphilic copolymer colloidal particles
A technology of sodium alginate and colloidal particles is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, nano-drugs, etc. and other problems, to achieve the effect of avoiding synthesis steps, good biocompatibility, and improving drug loading
Active Publication Date: 2018-05-04
上海研诺医药科技有限公司
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Problems solved by technology
Moreover, the synthesis conditions are harsh, the cost is expensive, and high temperature and high vacuum are required at the same time, which consumes energy and time.
Method used
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Embodiment 1
[0021] Dissolve 1g of sodium alginate in 50ml of pure water, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide successively as catalysts, three The molar ratio was 1:1:1. After stirring for 10 minutes, 0.1 g of lactic acid was added dropwise, and stirred at room temperature for 24 hours at 25°. Add 20ml of chloroform to wash, separate and let stand. Take a 10ml sample, add a certain amount of ibuprofen, stir it evenly with a needle, drop it into a 0.2mol / L calcium chloride solution with a needle, after aging for 4H, wash it with distilled water three times, filter it with microspheres, and dry it at low temperature to constant weight , weighing.
Embodiment 2
[0023] Lactic acid addition is 0.2g, and other synthetic processes are identical with embodiment 1.
Embodiment 3
[0025] Lactic acid addition is 0.3, and other synthetic processes are identical with embodiment 1.
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Abstract
The present invention uses sodium alginate as a raw material, directly adds lower alkyd acid (lactic acid or glycolic acid) into the sodium alginate solution, and continues the reaction at normal temperature for 24 hours. The low-level alkyd is polycondensed into low-molecular chain segments, and at the same time directly connected to the sodium alginate chain to obtain hydrophobically modified sodium alginate amphiphilic copolymer colloidal particles. Then add ibuprofen into the colloidal solution, disperse evenly, and drop it into the calcium chloride solution to obtain a "ball-in-a-ball" product loaded with ibuprofen, the diameter of which is 1.5 mm. The drug-loaded microsphere can greatly increase the drug-loading capacity of hydrophobic drugs. The release process has obvious pH responsiveness and sustained release. The raw material cost of the present invention is low, the synthesis method is "one-step method", the synthesis is simple, avoids expensive materials and complicated processes, and is directly completed in the solution, and the preparation and use of the microspheres do not use any organic solvents in the whole process, which is non-toxic and environmentally friendly . The product is biodegradable and has good application prospects.
Description
technical field [0001] The invention relates to the preparation of hydrophobically modified sodium alginate amphiphilic copolymer colloid particles, belonging to the technical field of carriers and slow-release materials. Background technique [0002] Sodium Alginate (Alg), also known as sodium alginate, is a natural polymer composed of β-D-mannuronic acid (M) and α-L-guluronic acid (G). , can be compared with Ca 2+ 、Ba 2+ The divalent cations are cross-linked to form gel microspheres. It has good biocompatibility and degradability, and is widely used in many fields such as medicine and food. However, sodium alginate itself has strong hydrophilicity, and the loading capacity of hydrophobic drugs is not high, and it is prone to burst release. Ibuprofen has anti-inflammatory, analgesic, and antipyretic effects. It is the only antipyretic drug for children jointly recommended by the World Health Organization and the US FDA, and is recognized as the first choice anti-inflamm...
Claims
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IPC IPC(8): C08B37/04A61K47/36A61K9/14B82Y5/00B82Y40/00A61K31/192
Inventor 倪才华李旺张猛王洁张亚南
Owner 上海研诺医药科技有限公司