Risperidone sustained-release gel injection and preparation method thereof

A technology of sustained-release gel injection and risperidone, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the complicated quality control of microsphere products and the loss of drugs and excipients , Syringe blockage and other problems, achieve good pharmacoeconomic value, good biocompatibility, and improve compliance

Active Publication Date: 2012-06-20
SHANGAI PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The process of collecting and screening microspheres leads to a large loss of drugs and excipients, so the yield of qualified microspheres is not high
The quality control of the finished microspheres is also quite complicated. In addition to the particle size of the microspheres must be controlled within a certain size range, a high drug encapsulation efficiency is also required, and the free risperidone usually does not exceed 10%.
If the microspheres cannot be sufficiently dispersed during injection, the aggregated microspheres will not be able to pass through the eye of the needle, resulting in blockage of the syringe and difficulty in administration
Due to various unfavorable factors in the preparation process, quality control and administration process, the technical barriers and production costs of risperidone microspheres are very high
In addition, the risperidone microspheres marketed abroad do not work in the first three weeks after administration, and risperidone still needs to be taken orally for treatment, which has caused great inconvenience clinically.

Method used

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  • Risperidone sustained-release gel injection and preparation method thereof
  • Risperidone sustained-release gel injection and preparation method thereof
  • Risperidone sustained-release gel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh 0.05 g of PLA (molecular weight 20,000 Daltons) and dissolve it in 0.2 g of NMP to form a blank polymer solution, then weigh 25.0 mg of risperidone and suspend and disperse it in the above solution to prepare a drug-loading solution. Put the prepared drug-loading solution in a 10ml vial, add a few drops of phosphate buffer solution with pH=7.4 to it to make it turn into a gel, and then soak the entire vial into phosphoric acid with pH=7.4 Release it in a reagent bottle with 2000ml of salt buffer. The release conditions were a constant temperature water bath at 37°C and a shaking speed of 100 rpm. 6 hours, 1, 2, 4, 7, 9, 11, 14, 17, 21, 25, 30, 35, 40, 45, and 49 days after the start of the release, take 2ml of the release medium and measure the content of risperidone in it , calculate the cumulative release percentage, and operate 3 copies in parallel, the results are shown in figure 1 .

Embodiment 2

[0036] Weigh 0.035g of PLA (molecular weight 20,000 Daltons) and dissolve it in 0.2g Glycofurol to form a blank polymer solution, then weigh 25.0mg of risperidone and suspend and disperse it in the above solution to make a drug-loading solution. Put the prepared drug-loading solution in a 10ml vial, add a few drops of phosphate buffer solution with pH=7.4 to it to make it turn into a gel, and then soak the entire vial into phosphoric acid with pH=7.4 Release it in a reagent bottle with 2000ml of salt buffer. The release conditions were a constant temperature water bath at 37°C and a shaking speed of 100 rpm. 6 hours after the start of release, 1, 2, 4, 7, 9, 11, 14, 17, 21, 25, 30, 40, 45, and 49 days, take 2ml of the release medium, measure the content of risperidone in it, and calculate Cumulative release percentage, 3 parallel operations, see the results figure 1 .

Embodiment 3

[0038] Weigh 0.05 g of PLGA (molecular weight 50,000 Daltons, polymer monomer mass ratio lactic acid: glycolic acid = 75:25) and dissolve it in 0.2 g TEC to form a blank polymer solution, then weigh 37.5 mg risperidone and mix it Suspended and dispersed in the above solution to make a drug-loading solution. Put the prepared drug-loading solution in a 10ml vial, add a few drops of phosphate buffer solution with pH=7.4 to it to make it turn into a gel, and then soak the entire vial into phosphoric acid with pH=7.4 Release it in a reagent bottle with 2000ml of salt buffer. The release conditions were a constant temperature water bath at 37°C and a shaking speed of 100 rpm. 6 hours after the start of the release, 1, 2, 4, 7, 9, 11, 14, 17, 21, 25, and 30 days, take 2ml of the release medium respectively, measure the content of risperidone in it, calculate the cumulative release percentage, and operate in parallel 3 copies, see results figure 2 .

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Abstract

The invention discloses a risperidone sustained-release gel injection and preparation method thereof. The risperidone sustained-release gel injection is composed of risperidone or analogue thereof, biological degradable polymer and biocompatible dissolvent, wherein the mass ratio between risperidone or analogue thereof and sum of biological degradable polymer and biocompatible dissolvant is 1:3-67. Continuous and constant-speed release of risperidone is up to several weeks immediately after the injection is injected into appropriate part in vivo, thereby improving compliance therapy in psychotic with risperidone analogue.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations and preparation thereof, in particular to a risperidone biodegradable long-acting sustained-release gel injection and a preparation method thereof. Background technique [0002] Risperidone is a new generation of atypical antipsychotic drugs, belonging to benzisoxazole derivatives, is a selective monoaminergic antagonist, it binds to 5-HT2 receptors of serotonin and dopamine Risperidone can also bind to α1-adrenergic receptors with high affinity, and bind to H1-histaminergic receptors and α2-adrenergic receptors with lower affinity. Risperidone does not bind to cholinergic receptors, is a powerful D2 antagonist, can improve the positive symptoms of schizophrenia, but it causes less motor function inhibition and catalepsy than classic antipsychotics . Its balance of serotonin and dopamine antagonism in the central system can reduce the possibility of extrapyramidal side effect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/519A61K47/34A61P25/18
Inventor 高科攀陈庆华包泳初潘峰潘弘杨怡静柯樱
Owner SHANGAI PHARMA GRP CO LTD
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