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Long-acting injection microsphere containing meloxicam and preparation method of long-acting injection microsphere

A technology of meloxicam and microspheres, applied in the field of pharmaceutical preparations, can solve problems such as low bioavailability and poor patient compliance, and achieve the effects of good encapsulation efficiency, prolonged drug release period, and good drug loading capacity of microspheres

Inactive Publication Date: 2021-09-17
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Meloxicam (Meloxicam) is a non-carrier anti-inflammatory drug, a commonly used drug for osteoarthritis, its oral preparation and injection dosage are both 7.5mg / person / day, due to frequent administration, its bioavailability is low, and patients obey poor sex

Method used

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  • Long-acting injection microsphere containing meloxicam and preparation method of long-acting injection microsphere
  • Long-acting injection microsphere containing meloxicam and preparation method of long-acting injection microsphere

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Embodiment 1 Preparation of meloxicam microspheres:

[0022] The present invention adopts S / W / O (water-in-oil-in-oil) process to prepare meloxicam microspheres, and the specific preparation method is:

[0023] Weigh 800mg of PLGA and dissolve it in 20mL of dichloromethane, add 110mg of meloxicam to it to obtain a meloxicam-PLGA suspension, and ultrasonically disperse the suspension at high speed (10000r / min, 5min);

[0024] Quickly drop meloxicam-PLGA dispersion solution into 1% polyvinyl alcohol (PVA) aqueous solution, stir and emulsify at 3000r / min for 5min, quickly transfer to 0.1%PVA, magnetically stir for 6h to remove dichloromethane, 1000-1200 mesh The washed balls were collected by sieving and freeze-dried to obtain the finished meloxicam microspheres.

[0025] Add meloxicam to the PLGA solution to form a meloxicam-PLGA suspension, and after ultrasonication and high-speed dispersion, it is important to quickly drop it into a 1% mass concentration polyvinyl alcoh...

Embodiment 2

[0026] Example 2 Quality evaluation of meloxicam microspheres:

[0027] (1) Microsphere morphology observation:

[0028] Evenly disperse 10 mg of the meloxicam microspheres prepared in Example 1 on the conductive adhesive, spray gold at 10Kv, and observe the appearance of the microspheres with a scanning electron microscope. The microspheres obtained in this study are round in shape and smooth in surface , the observation results see figure 1 .

[0029] The type and viscosity of PLGA are shown in Table 1.

[0030] The type and viscosity of the PLGA of table 1 embodiment 1-6

[0031] Example PLGA model PLGA Viscosity (dL / g) 1 5050 (A) 0.15-0.25

[0032] Remarks: In the PLGA model, 5050 means that the lactic acid / glycolic acid (LA / GA) in the polymer material is 50:50, A means that the polymer is terminated with a carboxyl group, and E means that the polymer is terminated with an ester group.

[0033] (2) Determination of drug loading and encapsulatio...

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Abstract

The invention relates to a long-acting injection microsphere containing meloxicam and a preparation method of the long-acting injection microsphere. The meloxicam microspheres are prepared by adopting a water-in-oil solid-in-oil (S / W / O) process, solid drugs are uniformly dispersed in an oil phase, and the obtained microspheres are good in drug loading capacity and good in encapsulation efficiency and can effectively prolong the drug release period.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a long-acting injection microsphere containing meloxicam and a preparation method thereof. Background technique [0002] Osteoarthritis is one of the most common joint diseases. Drug therapy is the main treatment. The half-life of common oral preparations and injections is short, and frequent administration is required to achieve effective blood drug concentrations. [0003] Meloxicam (Meloxicam) is a non-carrier anti-inflammatory drug, a commonly used drug for osteoarthritis, its oral preparation and injection dosage are both 7.5mg / person / day, due to frequent administration, its bioavailability is low, and patients obey Poor sex. [0004] Therefore, it will be the pursuit of those skilled in the art in research to develop a safe and stable joint cavity sustained-release preparation drug, which can not only improve its bioavailability, but also enhance the drug effect,...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/34A61K31/5415A61P19/02A61P29/00
CPCA61K9/5031A61K9/5089A61K9/0019A61K31/5415A61P19/02A61P29/00
Inventor 郑鹏许卉孙正
Owner YANTAI UNIV
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