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Hyaluronic acid-parecoxib PLGA microsphere as well as preparation method and application thereof

A technology of hyaluronic acid and parecoxib, which is applied in the field of preparation of new sustained-release microspheres, which can solve the problems of repeated injections and achieve the effect of uniform size

Active Publication Date: 2020-09-15
STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Aiming at the problem that the drug injected into the joint cavity will be quickly metabolized and absorbed, and repeated injections are often required, the present invention provides a hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application

Method used

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  • Hyaluronic acid-parecoxib PLGA microsphere as well as preparation method and application thereof
  • Hyaluronic acid-parecoxib PLGA microsphere as well as preparation method and application thereof
  • Hyaluronic acid-parecoxib PLGA microsphere as well as preparation method and application thereof

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preparation example Construction

[0036] A preparation method of hyaluronic acid-parecoxib PLGA microspheres, comprising the following steps:

[0037] a. Modify the hydrophilic hyaluronic acid, and transform it into an amphiphilic polymer by grafting hyaluronic acid with stearic acid, which is used as a surfactant in the subsequent microsphere preparation process;

[0038] b. Using double emulsification solvent volatilization method, dissolve PLGA in an appropriate amount of organic solvent, add a small amount of aqueous solution containing water-soluble drugs in proportion, add modified hyaluronic acid, and process it by ultrasonic or vibration to obtain the state Stable W / O emulsion;

[0039] c. Add a large amount of aqueous phase solution for the second emulsification treatment to obtain a W / O / W emulsion;

[0040] d. Remove the organic solvent by stirring and evaporating to obtain a microsphere suspension, and freeze-dry to obtain a microsphere powder.

[0041] Specifically, a preparation method of hyalur...

Embodiment 1

[0047] A preparation method of hyaluronic acid-parecoxib PLGA microspheres, comprising the following steps:

[0048] 1) Dissolve 200 mg of hyaluronic acid in 5 ml of deionized water, 80 mg of stearic acid in 25 ml of DMSO, add EDC to activate, mix the two solutions, add DMAP and stir overnight, precipitate with 300 ml of ethanol, and freeze-dry.

[0049] 2) Dissolve 40 mg parecoxib in 0.2 ml deionized water to form a uniform inner water phase, dissolve 240 mg PLGA in 2 ml dichloromethane as an oil phase, add the oil phase to the inner water phase, and add Amphiphilic hyaluronic acid (as surfactant).

[0050] 3) Immerse in an ice-water bath and stir for 1 min at high speed with a ultrasonic emulsifier to obtain colostrum. Drop the colostrum into 8ml of 4% PVA solution at a uniform speed and stir at high speed for 2 min to obtain double milk.

[0051]4) Transfer the double emulsion to a large volume of 100 ml 4% PVA aqueous solution, stir at a low speed for 3 hours to completel...

Embodiment 2

[0053] Example 2 Determination of drug loading and encapsulation efficiency

[0054] Weigh the weight of drug-loaded microspheres after lyophilization. Accurately weigh 20mg of microspheres and place them in a centrifuge tube, add 2ml of dichloromethane, and ultrasonically shake for 2 minutes to dissolve the microspheres; then dilute to 10ml with water, shake for 1 minute, let stand for 5 minutes, centrifuge at 10,000 rpm for 10 minutes, and take the supernatant ; Repeat the above steps twice more, collect all the supernatant, and measure the absorbance value (A) with a UV spectrophotometer, drug loading = (mass of drug in microspheres / mass of drug-containing microspheres) × 100%, Encapsulation efficiency = (actual drug content in microspheres / theoretical drug content in microspheres) × 100%.

[0055] The drug loading rate of the microsphere obtained by the present invention is 20.95%, and the encapsulation rate is 54.70%.

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Abstract

The invention discloses a hyaluronic acid-parecoxib PLGA microsphere as well as a preparation method and application thereof. Hydrophilic hyaluronic acid is modified, transparency is grafted with stearic acid so as to form amphiphilic macromolecules as a surfactant, so that the water-oil interfacial tension is reduced, and better adsorption of medicines is facilitated. A re-emulsifying solvent evaporation method is adopted. The preparation method comprises the following steps: dissolving PLGA into a proper amount of organic solvent, adding a small amount of a water-phase solution containing water-soluble medicines in a proportion, adding modified hyaluronic acid, carrying out ultrasonic treatment or oscillation treatment to obtain a W / O emulsion with a stable state, adding a large amount of an aqueous phase solution, carrying out secondary emulsification treatment to obtain a W / O / W emulsion, carrying out stirring evaporation to remove an organic solvent, and carrying out freeze dryingto obtain microsphere powder. By injecting the sustained-release microsphere, the acting time of the medicine can be effectively prolonged, the toxicity of the medicines is reduced, the irritation isreduced, and the medicines can be slowly released within several weeks.

Description

technical field [0001] The invention belongs to the technical field of preparation of novel sustained-release microspheres for drug administration, and in particular relates to a hyaluronic acid-parecoxib PLGA microsphere and a preparation method and application thereof. Background technique [0002] As a new type of sustained-release preparation for controlled administration, microspheres can maintain long-term effective drug concentrations, reduce dosing frequency, and reduce drug toxicity and irritation. At present, for patients with temporomandibular joint pain, intra-articular injections of local anesthetics, non-steroidal anti-inflammatory drugs, hormones or hyaluronic acid have good curative effects. HA can nourish articular cartilage, reduce synovial inflammation and enhance joint lubrication. As a new type of non-steroidal anti-inflammatory drug, parecoxib is a potent and specific cyclooxygenase-2 inhibitor. Because of its good analgesic effect, good tolerance and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/36A61K47/34A61K31/42A61P29/00A61P19/02
CPCA61K9/5031A61K47/36A61K9/0019A61K31/42A61P29/00A61P19/02
Inventor 朱东望徐万宁白浩冉邓嘉胤
Owner STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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