Sustained-release drug, its preparation method and application

A slow-release drug and drug technology, applied in the field of biomedicine, can solve problems such as inapplicable bones and joints

Active Publication Date: 2021-03-30
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current smart drug controlled release carriers all induce drug release by means of light, heat, pH, enzymes, redox agents, etc., and are not suitable for application in bone joints.

Method used

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  • Sustained-release drug, its preparation method and application
  • Sustained-release drug, its preparation method and application
  • Sustained-release drug, its preparation method and application

Examples

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preparation example Construction

[0050] The embodiment of the present invention also provides a preparation method of the sustained-release drug, comprising:

[0051] S10, providing the mesoporous silicon spheres;

[0052] S20, binding the guest molecule on the outer surface of the mesoporous silica sphere;

[0053] S30, loading the drug in the mesopore; and

[0054] S40, combining the host molecule with the guest molecule through host-guest interaction and at least partially blocking the opening of the mesopore.

[0055] In step S10, the mesoporous silicon spheres can be prepared by a template extraction method. In one embodiment, before step S20, it includes: modifying the mesoporous silicon spheres with amino groups. The amino modification step can be performed during the preparation of the mesoporous silicon spheres.

[0056] In one embodiment, the preparation of the mesoporous silicon spheres may include:

[0057] S12, mixing the silicon source, the templating agent and the morphology control cataly...

Embodiment 1

[0090] (1) Add 1 g of cetyltrimethylammonium bromide (CTAB) and 3.5 mL of sodium hydroxide solution (2 mol / L) into 480 mL of deionized water to obtain a mixed solution, and stir at 80°C for 30 min. 5 mL tetraethyl orthosilicate (TEOS) was added dropwise to the mixture, and stirring was continued at 80° C. for 2 h. Centrifuge, wash and dry in vacuo to obtain silica spheres.

[0091] (2) Disperse 1 g of the product of step (1) in 100 mL of anhydrous toluene, add 5 mL of 3-aminopropyltriethoxysilane (APTES), and reflux at 110° C. for 24 h. Centrifuge, wash and vacuum dry to obtain amino-modified silica spheres.

[0092] (3) Disperse 1 g of the product of step (2) in 100 mL of methanol, add 1 mL of concentrated hydrochloric acid, reflux at 60 ° C for 24 h, centrifuge, wash and dry in vacuum to obtain amino-modified mesoporous silica spheres (MSN-NH 2 ).

[0093] (4) Add 1.2 mL of thionyl chloride dropwise to 0.9 g of betaine hydrochloride, react at room temperature until no gas...

Embodiment 2

[0100] (1)-(3) Same as in the example, prepare amino-modified mesoporous silicon spheres.

[0101] (4) Dissolve 27g of cyclodextrin in 150mL of deionized water, add 9mL of NaOH solution (5.8mol / L) dropwise to the cyclodextrin solution, stir at room temperature for 30min, and the solution turns light green. Add 13 mL of acetonitrile solution of p-toluenesulfonyl chloride (1.58 mol / L) dropwise to the light green solution, and stir at room temperature for 3 h. Remove the precipitate by suction filtration, add hydrochloric acid (2mol / L) dropwise to the supernatant until the pH is 7.5, and place in the refrigerator overnight. The precipitate was collected by suction filtration and recrystallized three times with deionized water to obtain OTs group-modified cyclodextrin (OTs-CD).

[0102] (5) 100mg MSN-NH 2 Disperse into 20mL N,N-dimethylformamide (DMF), add 50mg OTs-CD and 2mL ethylenediamine (acid-binding agent), and stir at 110°C for 24h. Centrifuge, wash and dry in vacuum to ...

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Abstract

The invention discloses a slow-release drug. The slow-release drug is prepared from a mesoporous silicon sphere, a drug, a guest molecule and a host molecule; the mesoporous silicon sphere has a mesopore, and the drug is loaded in the mesopore; the guest molecule is combined with the outer surface of the mesoporous silicon sphere; the host molecule is combined with the guest molecule through interaction between a host and a guest, at least partially blocks the opening of the mesopore, and can be separated from the mesoporous silicon sphere under the action of force. The invention also discloses a preparation method and application of the slow-release drug.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a slow-release medicine, its preparation method and application. Background technique [0002] Osteoarthritis is a degenerative disease, which is the degeneration of articular cartilage, joint edge and subchondral bone reactive hyperplasia caused by aging, obesity, strain, trauma, joint deformity and many other factors. The incidence rate of osteoarthritis is very high, 70% of people over 60 years old and 90% of people over 80 years old have radioactive lesions of osteoarthritis. In the early stage of osteoarthritis, patients will feel joint pain and stiffness, in the middle stage, it will affect the normal activities of the patient, and in the late stage, the joints will fail and basically lose the ability to move. [0003] At present, the clinical treatment for advanced osteoarthritis is mainly artificial joint replacement, but there is no good treatment for early osteoarthritis. D...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/352A61P19/02A61P19/08
Inventor 张洪玉谭啸龙
Owner TSINGHUA UNIV
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