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Risperidone nano-suspension temperature sensitive gel and its preparation method

A temperature-sensitive gel and nano-suspension technology, which can be used in pharmaceutical formulations, aerosol delivery, and medical preparations containing active ingredients. Achieve broad application prospects, avoid the effects of less drug release and less residue

Inactive Publication Date: 2015-01-21
HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Risperidone microspheres for intramuscular injection have the advantages of long-acting, slow-release, and good patient compliance, but the preparation process of the microspheres is complicated, the price is high, and the corresponding drugs need to be taken orally in the first two weeks of injection of the microsphere preparation to achieve an effective effect. treatment, which brings a lot of inconvenience to patients and affects its clinical application

Method used

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  • Risperidone nano-suspension temperature sensitive gel and its preparation method
  • Risperidone nano-suspension temperature sensitive gel and its preparation method
  • Risperidone nano-suspension temperature sensitive gel and its preparation method

Examples

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Embodiment 1

[0042] The risperidone nano-suspension thermosensitive gel of this embodiment contains: risperidone 2g, docosahexaenoic acid 0.5g, poloxamer 407 (polyoxyethylene-polyethylene glycol) per 100ml nano-suspension thermosensitive gel Oxypropylene-polyoxyethylene triblock copolymer, F127) 20g, and the balance is water for injection.

[0043] The preparation method of the risperidone nano-suspension thermosensitive gel of the present embodiment comprises the following steps:

[0044]1) Dissolve 2g of risperidone and 0.5g of docosahexaenoic acid in 10ml of tetrahydrofuran to obtain an organic phase, and take water for injection as the aqueous phase;

[0045] 2) The organic phase obtained in step 1) was rotary evaporated to remove THF under reduced pressure, and dried in a vacuum oven at 35°C for 12 hours, then hydrated with 50ml of water phase, vortexed, and ultrasonically treated (400W, 4min) for dispersion. Obtain nano-suspension;

[0046] 3) Add 20g of poloxamer 407 (polyoxyethyl...

Embodiment 2

[0049] The risperidone nano-suspension thermosensitive gel of this embodiment, every 100ml nano-suspension thermosensitive gel contains: risperidone 1g, povidone 1g, poloxamer 407 (polyoxyethylene-polyoxypropylene-polyoxyethylene Ethylene triblock copolymer, F127) 15g, the balance is distilled water.

[0050] The preparation method of the risperidone nano-suspension thermosensitive gel of the present embodiment comprises the following steps:

[0051] 1) Dissolve 1g of risperidone and 1g of povidone in 10ml of chloroform to obtain an organic phase, and take distilled water as the aqueous phase;

[0052] 2) At room temperature, add the organic phase obtained in step 1) into 50ml of distilled water and stir at high speed (10000rpm, 10min) to disperse evenly to form a slightly light blue opalescent, translucent risperidone emulsion, which is then removed by rotary evaporation chloroform, and dried in a vacuum oven at 35°C for 12 hours to further remove the remaining chloroform to...

Embodiment 3

[0056] The risperidone nano-suspension thermosensitive gel of this embodiment contains: risperidone 0.25g, polyethylene glycol vitamin E succinate 1g, poloxamer 407 (polyoxyethylene) per 100ml nano-suspension thermosensitive gel - Polyoxypropylene-polyoxyethylene triblock copolymer, F127) 10 g, the remainder being distilled water.

[0057] The preparation method of the risperidone nano-suspension thermosensitive gel of the present embodiment comprises the following steps:

[0058] 1) Dissolve 0.25g of risperidone and 1g of polyethylene glycol vitamin E succinate in 50ml of methanol to obtain an organic phase, and take distilled water as the aqueous phase;

[0059] 2) Under stirring conditions at room temperature and a rotating speed of 10,000 rpm, add the organic phase obtained in step 1) into 50 ml of water phase and disperse evenly to form a translucent risperidone emulsion with slightly light blue opalescence, then remove methanol by rotary evaporation, and Dry in a vacuum...

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Abstract

The invention discloses a risperidone nano-suspension temperature sensitive gel and its preparation method. Each 100ml of the nanosuspension temperature sensitive gel contains 0.1-10g of risperidone, 0.1-5g of a stabilizer, 1-50g of a temperature sensitive gel material, 0-5g of an additive, and the balance of a water-based solvent. The risperidone nano-suspension temperature sensitive gel is a temperature sensitive controlled-release in situ gel. The above dosage form makes risperidone highly dispersed, so the gel has the advantages of good drug load and good stability; after the gel is administrated in a liquid form, phase transition occurs in applied sites, and the liquid becomes non-chemically-crosslinked semisolid gel, so the gel has good histocompatibility and improves the drug dissolution rate; and the administrated gel has a long retention time in the applied sites as a drug reservoir, so the gel has a slow release effect, prolongs the drug release time, improves the drug bioavailability, reduces the administration frequency and improves the drug effect and the patient compliance.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a risperidone nano-suspension temperature-sensitive gel, and also relates to a preparation method of the risperidone nano-suspension temperature-sensitive gel. Background technique [0002] Risperidone is a benzisoxazole derivative, which is a new generation of antipsychotics. It has a strong D2 antagonistic effect and is suitable for acute and chronic schizophrenia and various positive symptoms of psychosis (such as hallucinations, hallucinations, disordered thinking, Suspicion, hostility, etc.) and obvious negative symptoms (such as less speech, unresponsiveness, apathy, social apathy, etc.), can also reduce the emotional symptoms related to schizophrenia (such as depression, anxiety, guilt). Risperidone has significant curative effect, few side effects, and is widely used clinically. Currently, its commercially available preparations include oral liquid, or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/519A61P25/18
Inventor 和素娜杨晖李瑞芳杜景霞段冷昕
Owner HENAN UNIV OF SCI & TECH
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