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Iloperidone PLGA microsphere for injection, and preparation process thereof

A technology of iloperidone and microspheres, applied in the field of medicine, can solve the problems of iloperidone bitterness, poor water solubility, and poor patient compliance of oral preparations

Inactive Publication Date: 2018-03-23
天津双硕医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] As mentioned above, in order to solve the technical problems of bitter taste of iloperidone, poor water solubility and poor patient compliance of oral preparations

Method used

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  • Iloperidone PLGA microsphere for injection, and preparation process thereof
  • Iloperidone PLGA microsphere for injection, and preparation process thereof
  • Iloperidone PLGA microsphere for injection, and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of embodiment 1 iloperidone PLGA microspheres (unit: g)

[0046] prescription:

[0047]

[0048] The iloperidone drug-loaded PLGA microspheres are prepared through the following steps:

[0049] 1) dissolving prescription amount iloperidone and PLGA in an organic solvent to form oily phase A;

[0050] 2) Disperse the stabilizer hydrophilic nanocellulose into the water for injection, and dissolve the prescription amount of sodium chloride, which is the water phase B;

[0051] 3) Inject the oil phase A obtained in step 1) into the water phase B in step 2), and ultrasonicate to form an O / W emulsion;

[0052] 4) Dilute the aqueous phase in step 3) by one time, continue to stir at low speed until the organic solvent is evaporated, solidify the microspheres, collect the microspheres by centrifugation, wash with purified water for 3 times, and then vacuum freeze-dry to obtain iloperidone microspheres .

[0053] 5) Place the iloperidone microspheres obtain...

Embodiment 2

[0054] Embodiment 2: electron microscope morphology observation

[0055] The morphology of the iloperidone microspheres obtained from the nine prescriptions in Example 9 was observed with a scanning electron microscope, and an appropriate amount of sample was taken from each prescription microsphere, and dried with liquid carbon dioxide in a critical point dryer. The dried sample was placed in the sample aluminum holder, and the gold film was sprayed with the SPI-MODULE ion sputtering coating machine, and the voltage of the scanning electron microscope was adjusted to 25KV. Pictures of the five prescription samples, as attached figure 1 - attached Figure 9 shown.

[0056] The median particle size of iloperidone PLGA microspheres obtained from prescriptions 1-9 is shown in the table below:

[0057]

Embodiment 3

[0058] Embodiment 3: release curve

[0059] Measure the dissolution curve of the iloperidone microspheres obtained by the five prescriptions in Example 1 by the paddle method, and the five prescriptions respectively take microsphere samples containing about 10 mg iloperidone, each sample is taken in triplicate, and the final results are averaged value. Use 500ml, 0.1N HCl as the dissolution medium, the rotation speed is 50rpm, the medium temperature is 37±0.5°C, and samples are taken at 1h, 2h, 4h, 12h, 1 day, 2 days, 4 days, 8 days, 12 days, 24 days, and 36 days , and add the same amount of dissolution medium, the results of cumulative release are shown in the following table:

[0060]

[0061] As can be seen from the data in the above table, due to the different composition of the prescriptions, the release behavior of each prescription is different, but on the 36th day, iloperidone is basically released in each prescription.

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Abstract

The technical problems that iloperidone has bad taste and low water solubility and an oral preparation has low compliance on patients are solved. Through deep research, an iloperidone PLGA microspherefor injection, and a preparation process thereof are obtained. The administration cycle of the medicine is prolonged and the compliance of the patients is improved by changing the administration route, improving the formula and the preparation process and administrating through subcutaneous injection. The problems that the raw material medicine is bitter and low in water solubility are effectively solved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to iloperidone PLGA microspheres for injection and a preparation process. Background technique [0002] Schizophrenia is a common disease in psychiatry, and currently commonly used antipsychotic drugs are divided into two categories: typical and atypical according to their receptor blocking effects: typical antipsychotic drugs are represented by chlorpromazine and haloperidol, and their main effects are: The mechanism is to block dopamine receptors. It has a good curative effect on the positive symptoms of schizophrenia (hallucinations, delusions, agitation, impulsive behavior, etc.), while extrapyramidal reactions (EPS) are common, but it has a curative effect on negative symptoms (apathy, lack of thinking, loss of will, etc.) Poor; atypical anti-schizophrenia drugs have a wider therapeutic spectrum, and their effect on negative symptoms is significantly better than t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61K31/454A61P25/18
CPCA61K9/0019A61K9/1647A61K9/1682A61K31/454
Inventor 不公告发明人
Owner 天津双硕医药科技有限公司
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