Olanzapine-containing biodegradable microsphere preparation and preparation method thereof

A technology of biodegradation and olanzapine, which is applied in the direction of drug combination, neurological diseases, bulk delivery, etc., can solve the problems that cannot meet the clinical application, and achieve the improvement of drug release in vitro, particle size distribution, and convenient operation Effect

Inactive Publication Date: 2013-12-04
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] As mentioned above, the existing technology fails to develop a once-a-month olanzapine long-acting carrier controlled release formulation, therefore, it cannot meet the needs of clinical application

Method used

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  • Olanzapine-containing biodegradable microsphere preparation and preparation method thereof
  • Olanzapine-containing biodegradable microsphere preparation and preparation method thereof
  • Olanzapine-containing biodegradable microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Preparation of olanzapine microspheres:

[0056] (1) Weigh 0.3g of PLGA (weight average molecular weight 6,5124, LA:GA is 75:25, molar ratio) and 0.2g of olanzapine dissolved in 6.5g of dichloromethane and N~methyl~pyrrolidone mixed solvent ( Volume ratio 1:9), add 0.05g macrogol glyceride oleate, mix to obtain oil phase;

[0057] (2) Weigh 5g of PVA in 500g of distilled water, heat to dissolve, cool to room temperature, add 1g of NaCl and stir to dissolve, adjust the pH of the water phase to 7.5 with NaOH, add a stirrer, and keep it at 15°C under water bath conditions;

[0058] Among them, the degree of alcoholysis of PVA is 90%, the average number of polymer chains is 1700, and the weight average molecular weight is 20,000;

[0059] Slowly inject the oil phase into the water phase under the liquid surface, stir and emulsify for 1 hour, replace the supernatant, add ethanol, the weight content of ethanol in the water phase is 20wt%, and after magnetic stirring at room ...

Embodiment 2

[0075] Preparation of olanzapine microspheres

[0076] Weigh 0.3 g of PLGA (molecular weight 9,5726, LA:GA 75:25) and 0.2 g of olanzapine dissolved in 5 g of dichloromethane and N-methyl-pyrrolidone mixed solvent (volume ratio 1:2), add 0.1 g glyceryl tricaprylate, mixed to obtain an oily phase;

[0077] Weigh 4g of PVA in 400g of distilled water, dissolve, cool to room temperature, add 1.5g of NaCl and stir to dissolve, adjust the pH of the water phase to 7.5 with NaOH, add a stirrer, and keep it at 20°C under water bath conditions;

[0078] The average alcoholysis degree of PVA is 87%, the average polymer chain number is 1750, and the weight average molecular weight is 10,000;

[0079] Inject the oil phase into the water phase under the liquid surface, stir and emulsify for 1 hour, replace the supernatant, add ethanol, the content of ethanol in the water phase is 20wt%, magnetically stir at room temperature for 1 hour, replace the supernatant, and continue stirring for 24 h...

Embodiment 3

[0088] Preparation of olanzapine microspheres

[0089] Weigh 0.275g of PLGA (molecular weight 10,5328, LA:GA 75:25) and 0.225g of olanzapine dissolved in 5g of dichloromethane and N~methyl~pyrrolidone mixed solvent (volume ratio 1:9), add 0.1 g dimyristoylphosphatidylcholine (DMPC) to obtain the oil phase;

[0090]Weigh 6g of PVA in 600g of distilled water, dissolve, cool to room temperature, add 1.5g of NaCl, stir to dissolve, adjust the pH of the water phase to 7.5 with NaOH, add a stirrer, and keep it at 15°C under water bath conditions;

[0091] The average alcoholysis degree of PVA is 88%, the average polymer chain number is 1720, and the weight average molecular weight is 10,500;

[0092] Inject the oil phase into the water phase under the liquid surface, stir and emulsify for 1 hour, replace the supernatant, add ethanol, the content of ethanol in the water phase is 30wt% ethanol, magnetically stir at room temperature for 1 hour, replace the supernatant, and continue st...

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Abstract

The invention discloses an olanzapine-containing biodegradable microsphere preparation and a preparation method thereof. The olanzapine-containing biodegradable microsphere preparation comprises 10-50wt% of olanzapine or its salt, 0.5-20wt% of release adjusting agents and 30-89.5% of PLGA. In the invention, the PLGA having a proper monomer LA:GA ratio is selected as a matrix material, and above one release adjusting agents are added, so the olanzapine loading is improved to above 30%, and the particle size distribution and the in-vitro drug release of microspheres are improved. The utilization of a biodegradable material to encapsulate olanzapine to prepare the microspheres realizes a good slow release effect and the maintenance of an in-vivo relatively-stable drug concentration for above 15-45d or more.

Description

technical field [0001] The invention relates to an antipsychotic olanzapine slow-release microsphere preparation and a preparation method thereof. Background technique [0002] Olanzapine (Olanzapine) is a new type of atypical antipsychotic drug based on clozapine and modified by chemical structure. Therapeutic effect on negative symptoms. Olanzapine was approved for marketing in the United States in 1996 and was the first antipsychotic approved for the long-term treatment of schizophrenia and acute bipolar mania. [0003] Olanzapine is a 5~serotonin / dopamine (5~HT / DA) dual antagonist, which has a selective effect on the limbic and mesencephalic cortex. It can quickly relieve acute mental symptoms, has significant curative effect on both negative and positive symptoms, and can improve patients' social and cognitive functions, and can effectively treat organic mental disorders, alcohol-induced mental disorders and schizophrenia . In addition, olanzapine blocks the D 2 , ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/5513A61K47/34A61P25/18
Inventor 王晓琳栾瀚森王浩
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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