Medicament carrying microballoons of hydrophobic nature medicament and method of preparing the same

A hydrophobically modified, gel microsphere technology, applied in the field of gel microsphere synthesis and drug embedding materials, can solve the problems of harsh reaction conditions, low reactivity, affecting gelling performance, etc., and achieves drug loading capacity. Improve, the synthesis steps are simple, and the effect of slow release is good

Inactive Publication Date: 2008-09-03
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reactivity of -OH and -COOH is not high, the reaction conditions are harsh, and the reaction of -COOH will affect the subsequent reaction with Ca 2+ gel-forming properties

Method used

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  • Medicament carrying microballoons of hydrophobic nature medicament and method of preparing the same
  • Medicament carrying microballoons of hydrophobic nature medicament and method of preparing the same
  • Medicament carrying microballoons of hydrophobic nature medicament and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] In a single-necked flask covered with aluminum foil, prepare a sodium alginate (SA) solution (2% w / v, 250mL), add a certain amount of sodium periodate, seal it and stir it with magnetic force, react for 24 hours, add 1mL of ethylene glycol Alcohol terminates the oxidation reaction for 15 minutes, and it is very important to avoid light for this process. The resulting mixed solution was fully dialyzed and freeze-dried, and the oxidized sodium alginate ( OSA). The amount of sodium periodate added to 250 mL of the above 2% w / v sodium alginate solution is 0-0.022 mol, then oxidized sodium alginate with an oxidation degree of 0-62.4% can be obtained.

[0020] The introduction of the hydrophobic alkyl segment is in the reducing agent sodium cyanoborohydride (NaCNBH 3 ) under the action. Take 2.0g OSA and dissolve in 100mL phosphate buffer (pH 7.0) to make a uniform solution, add 0.46gNaCNBH 3 , then add 50mL of methanol solution containing dodecylamine 0.01-0.04g / mL, stir...

Embodiment 2

[0024] Dissolve 400mg SA-NHR polymer in 40mL water, stir this high viscosity liquid mechanically for 8h (speed 5000rpm), add drug 100mg ibuprofen into the polymer solution, and disperse in 2%w / v. In 40mL NaCl aqueous solution, add NaCl (2% w / v) and CaCl after stirring at high speed 2 (3% w / v) 1:1 (v / v) mixed solution 80 mL.

[0025]

[0026] The obtained microspheres were centrifuged, the surface was rinsed with deionized water, and dried. In vitro simulated release was performed in pure water and PBS buffer (pH 6.8). Taking sodium alginate gel microspheres modified with dodecylamine as an example, the embedding rates of the hydrophobic drug ibuprofen were 69.3%, 12%, and 15% respectively for SA-NHR with grafting rates of 8%, 12%, and 15%. 74.6%, 80.3%, while the original sodium alginate is only 46.6%.

[0027] Sustained release results such as figure 2 As shown, the modified SA-NHR microspheres stabilize the polymer network due to the hydrophobic association, and the...

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Abstract

Drug-loaded microspheres of a hydrophobic drug and a preparation method thereof belong to the technology fields of the synthesis of gel microspheres and the drug embedding materials. An oxidized sodium alginate which is adopted by the invention is reacted with alkylamine under the function of a reducing agent, the obtained polymer solution after the modification is strongly stirred and dispersed in a NaCl/CaCl2 mixed solution to form gel microspheres; and the embedding release research is carried out to the hydrophobic drug of ibuprofen. The hydrophobic alkyl chain section is grafted on the sodium alginate frame by a simple chemical method, then the gen microspheres are prepared, the obtained amphoteric gel microspheres can greatly improve the embedding efficiency of the hydrophobic drug and have great sustained-release performance, thus expanding the application range of the sodium alginate in the drug-loaded field.

Description

technical field [0001] A drug-loaded microsphere of hydrophobic drugs and a preparation method thereof belong to the technical field of synthesis of gel microspheres and drug embedding materials. Background technique [0002] Sodium alginate (SA) is a natural polymer composed of β-D-mannuronic acid (M) and α-L-guluronic acid (G), which is widely found in various brown seaweeds , can form a simple gel with multivalent cations, and the conditions for gelation are mild. The gel can generate mannuronic acid and glucuronic acid by enzymatic hydrolysis in the organism, which is non-toxic to the body and is suitable as a drug embedding material. However, sodium alginate is too hydrophilic, and the loading capacity of hydrophobic drugs is not high, so it is prone to burst release. It has been reported in the literature to modify the hydrophobicity of sodium alginate through -COOH or -OH reaction, such as Journal of Colloid and Interface Science2006, Eilish Broderick, Henry Lyons et...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/36
Inventor 李志勇倪才华张丽萍
Owner JIANGNAN UNIV
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