Iloperidone sustained release microsphere and preparation method thereof

A technology for slow-release microspheres and iloperidone, applied in the field of medicine, can solve the problems of uneven release, poor particle uniformity, irregular shape of the microspheres, etc., and achieve the effects of good uniformity, stable release and regular shape.

Inactive Publication Date: 2014-02-26
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After research, it was found that although the technical scheme described in CN101912367 A accounted for 60-80% of the drug dosage, the shape of the microspheres was irregular and the particle uniformity was poor, resulting in uneven release. The key factor of microspheres, the irregularity of microspheres is an important factor affecting clinical efficacy and safety, and the sustained release of drugs in the prior art is maintained for 2 weeks

Method used

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  • Iloperidone sustained release microsphere and preparation method thereof
  • Iloperidone sustained release microsphere and preparation method thereof
  • Iloperidone sustained release microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Weigh 200.21mg of PLGA (50 / 50, molecular weight 32000), 20.16mg of iloperidone, add 5mL of dichloromethane to stir and dissolve the clear solution to form an oil phase (O), quickly drop the oil phase into 75mL containing 1% In the PVA water phase (W), it was emulsified at 10,000 rpm for 90 s at high speed to form an O / W emulsion, and then the water phase was diluted with purified water by one time, and the obtained O / W emulsion was placed on a magnetic stirrer for Stir at 500rpm for 6 hours to volatilize and remove the organic solvent to solidify the microspheres, collect the microspheres by centrifugation, wash with purified water for 3 times, and then vacuum freeze-dry to obtain iloperidone microspheres. The drug loading was 7.61%, and the encapsulation efficiency was 83.18%.

Embodiment 2-7

[0029] Its prescription and process conditions are shown in Table 1.

[0030] The prescription and processing condition of table 1 embodiment 2~7

[0031]

[0032] The microsphere preparation step of embodiment 2~7 is the same as embodiment 1

Embodiment 8-14

[0034]Its prescription and technological conditions are shown in Table 2.

[0035]

[0036] The prescription and processing condition of table 2 embodiment 8~14

[0037]

[0038] The microsphere preparation step of embodiment 8~14 is the same as embodiment 1

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Abstract

The invention relates to an iloperidone sustained release microsphere and a preparation method thereof. The sustained release microsphere mainly comprises iloperidone and a biodegradable pharmaceutical polymer material PLGA (poly lactic-co-glycolic acid), wherein the molar ratio of lactic acid of PLGA to glycolic acid is (75-50):(25-50), the dosing weight ratio of the iloperidone to the PLGA is 1:(1-10), and the iloperidone is 3.5-15.5% of the total weight of the microsphere. According to the prepared iloperidone sustained release microsphere, the medicine encapsulation efficiency is high, the drug loading capacity is high, and the surface of the microsphere is smooth and round. The sustained release microsphere is used for curing psychosis, can prolong the action time of the medicine, reduces the dosing times, and greatly improves the obedience of patients in taking medicine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to iloperidone sustained-release microspheres and a preparation method thereof. Background technique [0002] Schizophrenia is a common major mental disorder, the etiology of which has not yet been fully elucidated. Most of the onsets are in young adults, and there are often obstacles in perception, thinking, emotion, and behavior. The course of the disease is often protracted. According to the World Health Organization, the lifetime prevalence rate of schizophrenia in the world is about 3.8‰~8.4‰. Research in the United States shows that the lifetime prevalence rate is as high as 13‰. New cases occur every year, and the annual incidence rate is about is 0.22‰. Once suffering from schizophrenia, patients need to take anti-schizophrenia drugs continuously for life. Since the development of antischizophrenia drugs in the 1950s, chlorpromazine represents the central D 2 After rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/454A61K47/34A61P25/18
Inventor 张涛张雁翎林丽邓杰
Owner CHONGQING PHARMA RES INST
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