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Paliperidone derivative slow release microsphere preparation and preparation method thereof

A slow-release microsphere preparation, the technology of paliperidone, is applied in the field of paliperidone derivative sustained-release microsphere preparation, additives and microsphere preparation, to achieve the effects of alleviating pain, reducing toxic and side effects, and low dosage

Inactive Publication Date: 2014-09-03
南京锐利施生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention further provides hydrophobic fatty acid esters as additives for paliperidone derivative sustained-release microsphere preparations, by changing the structure of the microspheres, the drug in the microspheres The crystallinity and distribution solve the problem that paliperidone derivatives cannot be stably released for one month when preparing microspheres

Method used

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  • Paliperidone derivative slow release microsphere preparation and preparation method thereof
  • Paliperidone derivative slow release microsphere preparation and preparation method thereof
  • Paliperidone derivative slow release microsphere preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0051] Weigh 0.8743 g 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-2-methyl-4-oxo Di-6,7,8,9-tetrahydro-pyrido[1,2-α]pyrimidin-9-yl isobutoxycarboxylate (see structural formula II) and 2.04 g 75257E PLGA, weigh the above Add to 13.60 ml of dichloromethane to dissolve, inject it into 1700ml of aqueous solution containing 0.5% PVA (w / w) under homogeneous (1200 - 2400rpm) conditions, keep the above homogeneous conditions for 5 minutes, and then The solvent was evaporated at 1200rpm for 4 hours, filtered through a sieve with a pore size of 25 μm and 125 μm, the microspheres were washed three times with distilled water, and freeze-dried. Microspheres containing 26% of the drug were prepared, the embedding rate was 87.56%, and the measured particle size was 1-200 μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 1 ; The DSC experimental spectrum of sustained-release microsp...

Embodiment 2

[0053] Weigh 0.8743 g 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-2-methyl-4-oxo Generation-6,7,8,9-tetrahydro-pyrido[1,2-α]pyrimidin-9-yl isobutoxycarboxylate (see structural formula II), 2.04 g 75257E PLGA and 34.2 μl palmitic acid iso Propyl ester, add the above weighed substance into 13.60 ml of dichloromethane to dissolve, inject it into 1700ml of aqueous solution containing 0.5% PVA (w / w) under homogeneous conditions (1200 - 2400rpm), keep the above homogeneity Conditioned for 5 minutes, then the solvent was evaporated at a stirring speed of 1200 rpm for 4 hours, filtered through a sieve with a pore size of 25 μm and 125 μm, washed with distilled water three times, and freeze-dried. Microspheres containing 25.82% of the drug were prepared, the embedding rate was 86.05%, and the measured particle size was 1-200 μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 1...

Embodiment 3

[0055] Weigh 0.8743 g 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-2-methyl-4-oxo Generation-6,7,8,9-tetrahydro-pyrido[1,2-α]pyrimidin-9-yl isobutoxycarboxylate (see structural formula II), 2.04 g 75257E PLGA and 68.2 μl palmitic acid iso Propyl ester, add the above weighed substance into 13.60 ml of dichloromethane to dissolve, inject it into 1700ml of aqueous solution containing 0.5% PVA (w / w) under homogeneous conditions (1200 - 2400rpm), keep the above homogeneity Conditioned for 5 minutes, then the solvent was evaporated at a stirring speed of 1200 rpm for 4 hours, filtered through a sieve with a pore size of 25 μm and 125 μm, washed with distilled water three times, and freeze-dried. Microspheres containing 26.79% of the drug were prepared, the embedding rate was 89.30%, and the measured particle size was 1-200 μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 1...

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Abstract

The invention discloses a paliperidone derivative slow release microsphere preparation and a preparation method thereof. A hydrophobic aliphatic ester serves as an additive of the biological slow release microsphere preparation, and the problem that the paliperidone derivative cannot be stably and slowly released for one month in the preparation process of microspheres is solved by changing the microsphere structure and drug crystallinity and distribution in the microspheres. The drug can be slowly and stably released for one month, one month and a half even over two months, the drug administration frequency is greatly reduced, the bioavailability and treatment effect of the drug are improved, and the toxic and side effects are reduced, so that the pain of vast patients is greatly reduced, and the living quality is improved.

Description

technical field [0001] The invention discloses a paliperidone derivative sustained-release microsphere preparation, and also provides an additive and a microsphere preparation method of the paliperidone derivative sustained-release microsphere preparation, belonging to the technical field of medicine and pharmacy. Background technique: [0002] Because schizophrenia requires long-term administration and poor patient compliance, sustained-release microsphere preparations injected once every two weeks or once a month have shown great advantages in the treatment of such diseases. Paliperidone has low solubility in dichloromethane, and it is difficult to prepare polylactic-glycolic acid (PLGA) microspheres with higher drug loading by emulsification and volatilization method, so it is impossible to prepare PLGA for injection once every two weeks or once a month Microsphere formulations. The paliperidone derivatives involved in the present invention are rapidly metabolized into ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/519A61K47/14A61P25/18
Inventor 李又欣刘喜明孙凤英滕乐生王丹王乐希赵晓雷刘伟付璐代文文
Owner 南京锐利施生物技术有限公司
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