A preparation method and application method of ultrasound-targeted microbubbles carrying simvastatin

A simvastatin and targeted microbubble technology, applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc. The effect of drug action time, stable properties and strong drug targeting

Active Publication Date: 2022-04-01
NANJING FIRST HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Aiming at the problem that ultrasonic microbubble targeted rupture technology combined with statins is not applied to the treatment of arthritis, ultrasonic targeted statins are used in the treatment of osteoarthritis, and there is no uniform standard for ultrasonic intensity and time, the purpose of the present invention is to provide a portable Simvastatin-loaded ultrasound-targeted microbubbles and their use in the treatment of osteoarthritis

Method used

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  • A preparation method and application method of ultrasound-targeted microbubbles carrying simvastatin
  • A preparation method and application method of ultrasound-targeted microbubbles carrying simvastatin
  • A preparation method and application method of ultrasound-targeted microbubbles carrying simvastatin

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Effect test

Embodiment 1

[0028] A preparation method of ultrasound-targeted microbubbles carrying simvastatin, the steps are as follows:

[0029] (1), dissolve simvastatin in tetrahydrofuran and dissolve, then add physiological saline and dilute into 0.05mg / mL simvastatin solution;

[0030] (2), adding trimethyl chitosan in the simvastatin solution, the final concentration is 1-3%;

[0031] (3), add sodium tripolyphosphate in the mixture that step (2) obtains, then-OH of simvastatin structure, trimethyl chitosan structure-NH2, the-OH on sodium tripolyphosphate structure, through Lorentz forces combine to form a stable spatial network, and the resulting mixture is a fluorescent emulsion. The particle size is about 500nm through electron microscope detection.

[0032] (4) Freeze-dry the suspension obtained in step (3), add the reconstitution agent sodium alginate to dissolve completely, transfer the obtained liquid to a vial filled with C3F8 gas, and vibrate the vial with a mechanical oscillator to for...

Embodiment 2

[0034] Embodiment 2 compares the impact of different ultrasonic targeting conditions on the rupture of simvastatin microbubbles;

[0035] 1) Experimental process:

[0036]Take 12 healthy New Zealand white rabbits, all of which are adult males. Three of them are randomly selected as a group, and they are divided into 4 groups. 200 μL of simvastatin microbubbles are injected into the right knee joint respectively. 1, 2 W / cm outside the right knee joint cavity 2 Ultrasonic intensity and irradiation time of 2 and 5 minutes were irradiated, and the optimal ultrasonic parameters were screened according to the ultrasonic images to observe the rupture of simvastatin microbubbles.

[0037] 2) Experimental results:

[0038] figure 2 In order to compare the effect of simple statin drug therapy and ultrasonic targeted statin drug therapy on OA cartilage, the rupture of simvastatin microbubbles under different ultrasonic parameters in the ultrasonic images: non-cavitated microbubbles s...

Embodiment 3

[0039] Example 3 Comparison of the effects of simple statin drug therapy and ultrasound-targeted simvastatin microbubble therapy on OA cartilage

[0040] 1. Experimental process:

[0041] (1) Grouping: The OA experimental rabbits were randomly divided into 3 groups, 6 in each group, and the pathological changes of the knee articular cartilage surface in each group were compared by Safranin O Fast Green staining.

[0042] Group 1# was given simvastatin (PSV): 0.1 mg / mL simvastatin solution was injected into the right knee joint cavity

[0043] Group 2# ultrasound-targeted simvastatin microbubbles group (USV group); USV group was injected with 0.1mg / mL simvastatin microbubbles into the right knee joint cavity, and at the same time 1MHz, 2W / cm 2 , the on-off ratio was 20%, and the irradiation time was 5 minutes to induce microbubble rupture, and 200 μL was injected into the knee joint cavity of each rabbit. At the same time, different dosage groups (0.1, 0.2, 0.3, 0.4, 0.5mg / ml...

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Abstract

The invention relates to a preparation method of ultrasound-targeted microbubbles carrying simvastatin, which comprises dissolving simvastatin in tetrahydrofuran and diluting physiological saline to a concentration of 0.01-0.1 mg / mL; adding trimethyl chitosan, Sodium tripolyphosphate, then, compounded into a stable space network, obtained a suspension, freeze-dried and redissolved, transferred the obtained liquid to a vial filled with C3F8 gas, and vibrated the vial with a mechanical oscillator to form a 0.05 mg / mL simvastatin microbubbles, fill the remaining space of the vial with high-pressure C3F8 gas and seal it up, and refrigerate it for later use; inject simvastatin microbubbles into the knee joint cavity and apply ultrasound at the same time, control the ultrasound intensity and time, and target to induce microbubble rupture to reach the maximum ratio. The administration is highly targeted, the medication cycle is shortened, the side effects of long-term medication are reduced, and the dosage of the medication is reduced.

Description

technical field [0001] The invention belongs to the field of new drug dosage forms and applications thereof, and in particular relates to an ultrasound-targeted microbubble carrying simvastatin and its application for treating osteoarthritis. Background technique [0002] Arthritis (osteoarthritis, OA) is a common clinical chronic, articular cartilage degenerative disease, the main symptoms are joint pain, stiffness and dysfunction. In my country, OA mainly occurs in middle-aged and elderly people, and the incidence rate increases with age. Epidemiological surveys show that 90% of women and 80% of men over 65 years old suffer from OA, and the prevalence of knee OA exceeds 10%. %, is the leading cause of physical disability in the elderly population. With the increase of sports trauma and life expectancy, the incidence of OA is increasing year by year, and the average age of OA tends to be younger. With the progress of OA-related epidemiology and molecular biology research, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K31/366A61K47/52A61K47/61A61P19/02A61P29/00
Inventor 李雪萍夏鹏陈安亮王馨伟程凯林强俞长君杨婷高明霞王晓菊王琪宋九龙
Owner NANJING FIRST HOSPITAL
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