Amifostine slow-release microspheres for subcutaneous injection and preparation method thereof

A technology of using amifostine and slow-release microspheres, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problem that the advantages of sustained-release preparations are discounted, amifostine Rapid gushing and other problems, to overcome the uneven release of subcutaneous injection, solve unfavorable factors, and achieve the effect of long-acting drug release

Active Publication Date: 2016-10-12
SHANGHAI PULMONARY HOSPITAL
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

On the one hand, they found that the subcutaneous sustained-release dosage form had the same protective effect on mice after radiation exposure as the conventional subcutaneous injection method. The data of the three groups of amifostine subcutaneous sustained-release dosage forms showed that the effective concentration of the mouse blood compound WR1065 was maintained for more than 2 hours; Severe early burst release was observed after subcutaneous injection of polymer microspheres, which degraded rapidly under in vitro conditions, resulting in a large amount of amifostine gushing out of the capsule quickly, and the advantages of sustained-release preparations were compromised

Method used

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  • Amifostine slow-release microspheres for subcutaneous injection and preparation method thereof
  • Amifostine slow-release microspheres for subcutaneous injection and preparation method thereof
  • Amifostine slow-release microspheres for subcutaneous injection and preparation method thereof

Examples

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preparation example Construction

[0026] The invention provides a method for preparing amifostine sustained-release microspheres for subcutaneous injection, comprising the following steps:

[0027] Step 1, dissolving amifostine in dimethyl sulfoxide to obtain amifostine solution S;

[0028] Step 2, dissolving the biodegradable polymer material in an organic solvent to obtain an oil phase O;

[0029] Step 3, preparing 1-4% polyvinyl alcohol aqueous solution as the water phase W;

[0030] Step 4, transfer the amifostine solution S obtained in the step 1 into the oil phase O obtained in the step 2, and emulsify with a ultrasonic emulsifier to obtain an S / O type primary emulsion;

[0031] Step 5, inject the primary emulsion S / O obtained in step 4 into the water phase W prepared in step 3, and emulsify with an ultrasonic emulsifier to obtain a S / O / W type secondary emulsion;

[0032] Step 6, centrifuge the S / O / W type secondary emulsion obtained in step 5 at a speed of 300-900rpm for 1-10 hours; then centrifuge at ...

Embodiment 1

[0034] Example 1 Preparation of amifostine sustained-release microspheres for subcutaneous injection

[0035]In this embodiment, the degradable polymer material is poly(lactic-co-glycolic acid) (PLGA), and the organic solvent is dichloromethane. Dissolve 20 mg of amifostine in 0.5 ml of dimethyl sulfoxide to obtain amifostine solution S; dissolve 100 mg of PLGA in 3 ml of dichloromethane to form oil phase O; dilute and prepare 2% polyvinyl alcohol aqueous solution as the water phase W; transfer the obtained amifostine solution S into the oil phase O obtained in step 2, emulsify with a ultrasonic emulsifier to obtain an S / O primary emulsion, then inject it into the water phase W with a glass syringe, and perform ultrasonic emulsification Emulsified with a device to obtain S / O / W type secondary emulsion; then the S / O / W type secondary emulsion was centrifuged at a speed of 500rpm for 4 hours; then centrifuged at a speed of 4000rpm for 15 minutes to obtain precipitated microspheres...

Embodiment 2

[0036] Example 2 Morphological determination of amifostine sustained-release microspheres for subcutaneous injection

[0037] The surface morphology of the sustained-release microspheres prepared in Example 1 was observed with a scanning electron microscope. like figure 1 As shown, the surface of the amifostine sustained-release microspheres prepared in Example 1 is quite smooth, with only some small depressions (related to the evaporated organic solvent during the drying process).

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Abstract

The invention discloses amifostine slow-release microspheres for subcutaneous injection and a preparation method thereof. A unique two-way emulsion-solution evaporation technology is adopted, the prepared amifostine slow-release microspheres for subcutaneous injection can reach relative constant and long-acting drug release in a subcutaneous injection scene, in-vitro release is even, release time can be as long as 300 hours or above, the protection function is stable, adverse factors brought by the fact that existing amifostine can only adopt an intravenous injection drug application mode are avoided, and the problem that drug release is not uniform and lasting through subcutaneous injection is also solved.

Description

technical field [0001] The invention relates to a sustained release agent and a corresponding preparation method, in particular to an amifostine sustained release microsphere for subcutaneous injection and a preparation method thereof. Background technique [0002] Amifostine is an organothiophosphate drug, which is metabolized by alkaline phosphatase in the body into active free thiol metabolites, mainly relying on the removal of oxygen free radicals produced by chemotherapy drugs and radiotherapy, and exerts the chemical repair function of hydrogen atoms to regulate Mechanisms such as gene expression in cell death and DNA repair, attenuating the toxicity of chemotherapy drugs and radiation exposure to normal tissues. Because the alkaline phosphatase activity and pH value in the capillaries of normal tissues are higher than those in tumor tissues, and the distribution of blood vessels is better, amifostine thus protects normal tissues. Amifostine is rapidly metabolized int...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/661A61K47/34A61K47/36A61K47/42A61P39/06A61P35/00
Inventor 吴红宇
Owner SHANGHAI PULMONARY HOSPITAL
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