CN104606133A - Oral lurasidone suspension and preparation method thereof - Google Patents
Oral lurasidone suspension and preparation method thereof Download PDFInfo
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- CN104606133A CN104606133A CN201510005600.1A CN201510005600A CN104606133A CN 104606133 A CN104606133 A CN 104606133A CN 201510005600 A CN201510005600 A CN 201510005600A CN 104606133 A CN104606133 A CN 104606133A
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- lurasidone
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Abstract
The invention discloses an oral lurasidone suspension and a preparation method thereof. The lurasidone suspension is a pharmaceutical composition which comprises lurasidone or salt thereof, a suspending aid, a wetting agent, a pH regulator, a preservative, a sweetening agent and a corrigent, wherein the particle size range of the lurasidone or salt thereof is 0.1-20 microns. The prepared oral suspension has the characteristics of being stable in quality and favorable in taste, facilitates dose distribution, and is beneficial to the acceptance of schizophrenia patients, simple in preparation method and suitable for industrial production.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to and a kind ofly comprise oral administration mixed suspension of Lurasidone or its salt and preparation method thereof.
Background technology
Schizophrenia (schizophrenia) is the not bright major psychosis of one group of cause of disease, current global number of the infected is up to 2,400 ten thousand, patient often loses independent living ability when showing effect, and homicide rate is high, in addition with obesity, hypertension, diabetes and cardiovascular disease etc.Although achieve preeminent accomplishment in recent years in treatment of schizophrenia, still have the symptom of the patient of 30% to alleviate, in rehabilitation clients, have 60% can cause recurrence because of some reason in 2 years.Along with modern society's pressure increase, schizophrenic gets more and more, and market is also increasing.
Lurasidone (lurasidone) is a kind of novel atypical antipsychotic, ratify its listing food and medicine Surveillance Authority of the U.S. on October 28 in 2010 (FDA), commodity are called Latuda, it is not fully aware of yet that it treats schizoid precise mechanism, may be relevant with the antagonism of dopamine D 2 and 5-hydroxy tryptamine 2A receptor.
The Lurasidone of current listing only has oral ordinary tablet, and for this special colony of schizophrenic, oral administration mixed suspension has drug effect and plays advantage that is fast, that be convenient to divided dose, improve patient's compliance, is more conducive to the treatment of disease.
Summary of the invention
In view of the above circumstances, the present invention comprises oral administration mixed suspension of Lurasidone or its salt and preparation method thereof by providing a kind of.The technical problem solved prepares the Lurasidone oral administration mixed suspension of steady quality, good mouthfeel, so that the compliance of divided dose and raising schizophrenic medication.
Lurasidone oral administration mixed suspension provided by the invention, in every 100mL, the consumption of each composition is as follows:
Lurasidone or its salt 0.1 ~ 2.0g
Suspending agent 0.1 ~ 5.0g
Wetting agent 0.05 ~ 2.5g
PH adjusting agent 0.05 ~ 1.0g
Antiseptic 0.01 ~ 0.5g
Sweeting agent 1.0 ~ 50.0g
Correctives 0.1 ~ 3.0g
Purified water is settled to 100mL.
Lurasidone described in the present invention or the preferred Lurasidone HCl of its salt, its particle size range is 0.1 ~ 20 μm, preferably 0.1 ~ 10 μm.
The pH value range of the oral administration mixed suspension of Lurasidone described in the present invention is 2 ~ 6.
Suspending agent described in the present invention is one or more in xanthan gum, arabic gum, colloidal silica, sodium carboxymethyl cellulose, hypromellose, polyvidone; Described wetting agent is one or more in Polysorbate, poloxamer, phospholipid, glycerol; Described pH adjusting agent is one or more in citric acid buffer salt, acetate buffer salt, phosphate-buffered salt; Described antiseptic is one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, benzoic acid, sodium benzoate, sorbic acid; Described sweeting agent is one or more in xylitol, mannitol, saccharin sodium, sucrose, aspartame; Described correctives is one or more in strawberry essence, cherry essence, fragrant citrus essence, flavoring banana essence, menthol.
The preparation method of the oral administration mixed suspension of Lurasidone described in the present invention is as follows:
(1) purified water is heated, add antiseptic, dissolve and make antiseptic solution;
(2) pH adjusting agent, sweeting agent, correctives are added in the obtained antiseptic solution of step (1), stirring and dissolving, for subsequent use;
(3) under magnetic stirring, suspending agent is added in step (2) obtained solution, be uniformly dispersed, be prepared into uniform suspending system;
(4) purified water is mixed with into dispersion liquid with wetting agent;
(5) micronized Lurasidone is mixed homogeneously with dispersion liquid obtained in step (4), join in the mixture of step (3) gained, by the abundant homogenize of homogenizer, to obtain final product.
Lurasidone oral administration mixed suspension steady quality, good mouthfeel that the present invention prepares, be convenient to divided dose, be conducive to schizophrenic and accept, preparation method is simple, adopts ordinary preparation equipment, is suitable for suitability for industrialized production.
Detailed description of the invention
Below in conjunction with specific embodiment, the invention will be further described, can better understand the present invention and can be implemented, but illustrated embodiment is not as a limitation of the invention to make those skilled in the art.
Embodiment 1:
| Components Name | Consumption (g/100mL) |
| Lurasidone HCl | 0.25 |
| Hypromellose | 0.5 |
| Polyoxyethylene sorbitan monoleate | 0.05 |
| Citric acid | 0.2 |
| Sodium citrate | 0.05 |
| Ethyl hydroxybenzoate | 0.05 |
| Mannitol | 10 |
| Strawberry essence | 0.5 |
| Purified water | Add to 100mL |
Preparation method:
(1) get 50mL purified water and be heated to 80 ~ 90 DEG C, add ethyl hydroxybenzoate, stirring and dissolving;
(2) citric acid, sodium citrate, mannitol, strawberry essence are added in the obtained ethyl hydroxybenzoate solution of step (1), stirring and dissolving, for subsequent use;
(3) under magnetic stirring, hypromellose is joined in the obtained solution of step (2), be uniformly dispersed, be prepared into uniform suspending system;
(4) 20mL purified water is mixed homogeneously with polyoxyethylene sorbitan monoleate, be prepared into dispersion liquid;
(5) micronized Lurasidone HCl is mixed homogeneously with dispersion liquid obtained in step (4), join in the suspending system of step (3) gained, add purified water to 100mL, be uniformly mixed, by the abundant homogenize of homogenizer, to obtain final product.
Embodiment 2:
| Components Name | Consumption (g/100mL) |
| Lurasidone HCl | 0.5 |
| Xanthan gum | 0.3 |
| Colloidal silica | 1.0 |
| Polyoxyethylene sorbitan monoleate | 0.25 |
| Citric acid | 0.2 |
| Sodium citrate | 0.05 |
| Ethyl hydroxybenzoate | 0.05 |
| Xylitol | 20 |
| Strawberry essence | 0.5 |
| Purified water | Add to 100mL |
Preparation method:
(1) get 50mL purified water and be heated to 80 ~ 90 DEG C, add ethyl hydroxybenzoate, stirring and dissolving;
(2) citric acid, sodium citrate, xylitol, strawberry essence are added in the obtained ethyl hydroxybenzoate solution of step (1), stirring and dissolving, for subsequent use;
(3) under magnetic stirring, xanthan gum, colloidal silica are joined in the obtained solution of step (2), is uniformly dispersed, is prepared into uniform suspending system;
(4) 20mL purified water is mixed homogeneously with polyoxyethylene sorbitan monoleate, be prepared into dispersion liquid;
(5) micronized Lurasidone HCl is mixed homogeneously with dispersion liquid obtained in step (4), join in the suspending system of step (3) gained, add purified water to 100mL, be uniformly mixed, by the abundant homogenize of homogenizer, to obtain final product.
Embodiment 3:
| Components Name | Consumption (g/100mL) |
| Lurasidone HCl | 1.0 |
| Sodium carboxymethyl cellulose | 3.0 |
| PLURONICS F87 | 1.0 |
| Citric acid | 0.2 |
| Sodium citrate | 0.1 |
| Sodium benzoate | 0.2 |
| Xylitol | 30 |
| Fragrant citrus essence | 1.0 |
| Purified water | Add to 100mL |
Preparation method:
(1) get 50mL purified water, add sodium benzoate, stirring and dissolving;
(2) citric acid, sodium citrate, xylitol, fragrant citrus essence are added in the obtained PhCOONa solution of step (1), stirring and dissolving, for subsequent use;
(3) under magnetic stirring, sodium carboxymethyl cellulose is joined in the obtained solution of step (2), be uniformly dispersed, be prepared into uniform suspending system;
(4) 20mL purified water is mixed homogeneously with PLURONICS F87, be prepared into dispersion liquid;
(5) micronized Lurasidone HCl is mixed homogeneously with dispersion liquid obtained in step (4), join in the suspending system of step (3) gained, add purified water to 100mL, be uniformly mixed, by the abundant homogenize of homogenizer, to obtain final product.
Embodiment 4:
| Components Name | Consumption (g/100mL) |
| Lurasidone HCl | 2.0 |
| PVP K30 | 5.0 |
| PLURONICS F87 | 2.0 |
| Citric acid | 0.2 |
| Sodium citrate | 0.2 |
| Sodium benzoate | 0.2 |
| Saccharin sodium | 1.0 |
| Cherry essence | 2.0 |
| Purified water | Add to 100mL |
Preparation method:
(1) get 50mL purified water, add sodium benzoate, stirring and dissolving;
(2) citric acid, sodium citrate, saccharin sodium, cherry essence are added in the obtained PhCOONa solution of step (1), stirring and dissolving, for subsequent use;
(3) under magnetic stirring, PVP K30 is joined in the obtained solution of step (2), be uniformly dispersed, be prepared into uniform suspending system;
(4) 20mL purified water is mixed homogeneously with PLURONICS F87, be prepared into dispersion liquid;
(5) micronized Lurasidone HCl is mixed homogeneously with dispersion liquid obtained in step (4), join in the suspending system of step (3) gained, add purified water to 100mL, be uniformly mixed, by the abundant homogenize of homogenizer, to obtain final product.
Confirmatory experiment:
Measure the sedimentation volume ratio of embodiment 1 ~ 4 sample with reference to Chinese Pharmacopoeia two (2010 editions) annex IO, and taste mouthfeel by healthy volunteer, result is as follows:
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | |
| Sedimentation volume ratio | 0.93 | 0.98 | 0.96 | 0.95 |
| Mouthfeel | Well, without bitterness | Well, without bitterness | Well, without bitterness | Well, without bitterness |
Embodiment 1 ~ 4 sample sedimentation volume ratio is all not less than 0.90, and interpret sample has good stability.Attempt according in healthy volunteer's mouth, embodiment 1 ~ 4 sample is all without bitterness and sweet taste is moderate.Therefore, Lurasidone oral administration mixed suspension steady quality, good mouthfeel prepared by embodiment 1 ~ 4, be convenient to the compliance of divided dose and raising patient medication.
Claims (8)
1. comprise an oral administration mixed suspension for Lurasidone or its salt, it is characterized in that oral administration mixed suspension also can contain the pharmaceutic adjuvant of the acceptable suspending agent of pharmacy, wetting agent, pH adjusting agent, antiseptic, sweeting agent and correctives.
2. oral administration mixed suspension according to claim 1, is characterized in that Lurasidone salt is Lurasidone HCl.
3. oral administration mixed suspension according to claim 2, is characterized in that Lurasidone HCl raw material particle size scope is 0.1 ~ 20 μm.
4. oral administration mixed suspension according to claim 2, is characterized in that Lurasidone HCl raw material particle size scope is 0.1 ~ 10 μm.
5. oral administration mixed suspension according to claim 1, is characterized in that the pH value range of suspension is 2 ~ 6.
6. oral administration mixed suspension according to claim 1, is characterized in that described suspending agent is one or more in xanthan gum, arabic gum, colloidal silica, sodium carboxymethyl cellulose, hypromellose, polyvidone; Described wetting agent is one or more in Polysorbate, poloxamer, phospholipid, glycerol; Described pH adjusting agent is one or more in citric acid buffer salt, acetate buffer salt, phosphate-buffered salt; Described antiseptic is one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, benzoic acid, sodium benzoate, sorbic acid; Described sweeting agent is one or more in xylitol, mannitol, saccharin sodium, sucrose, aspartame; Described correctives is one or more in strawberry essence, cherry essence, fragrant citrus essence, flavoring banana essence, menthol.
7. oral administration mixed suspension according to claim 1, is characterized in that the concrete consumption of each composition in every 100mL suspension is as follows: Lurasidone or its salt 0.1 ~ 2.0g, suspending agent 0.1 ~ 5.0g, wetting agent 0.05 ~ 2.5g, pH adjusting agent 0.05 ~ 1.0g, antiseptic 0.01 ~ 0.5g, sweeting agent 1.0 ~ 50.0g, correctives 0.1 ~ 3.0g.
8. oral administration mixed suspension according to claim 1, is characterized in that comprising following preparation method:
Purified water is heated, adds antiseptic, dissolve and make antiseptic solution;
PH adjusting agent, sweeting agent, correctives are added in the obtained antiseptic solution of step (1), stirring and dissolving, for subsequent use;
Under magnetic stirring, suspending agent is joined in step (2) obtained solution, be uniformly dispersed, be prepared into uniform suspending system;
Purified water is mixed with into dispersion liquid with wetting agent;
Micronized Lurasidone is mixed homogeneously with dispersion liquid obtained in step (4), joins in the mixture of step (3) gained, by the abundant homogenize of homogenizer, to obtain final product.
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| CN201510005600.1A CN104606133A (en) | 2015-01-07 | 2015-01-07 | Oral lurasidone suspension and preparation method thereof |
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| CN201510005600.1A CN104606133A (en) | 2015-01-07 | 2015-01-07 | Oral lurasidone suspension and preparation method thereof |
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| CN201510005600.1A Pending CN104606133A (en) | 2015-01-07 | 2015-01-07 | Oral lurasidone suspension and preparation method thereof |
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Cited By (6)
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| CN104983679A (en) * | 2015-06-24 | 2015-10-21 | 万特制药(海南)有限公司 | Sustained-release suspension with lurasidone and preparation method of sustained-release suspension |
| WO2018043613A1 (en) * | 2016-08-31 | 2018-03-08 | 大日本住友製薬株式会社 | Aqueous suspension preparation |
| CN108721325A (en) * | 2017-04-13 | 2018-11-02 | 辽宁大熊制药有限公司 | Smectite turbid liquor and preparation method thereof |
| CN109998991A (en) * | 2019-04-28 | 2019-07-12 | 中国药科大学 | A kind of long-acting intramuscular injection nanosuspension of Lurasidone HCl and preparation method thereof |
| WO2019167977A1 (en) * | 2018-02-28 | 2019-09-06 | 大日本住友製薬株式会社 | Aqueous suspension-type pharmaceutical preparation |
| WO2019167978A1 (en) * | 2018-02-28 | 2019-09-06 | 大日本住友製薬株式会社 | Aqueous suspension-type pharmaceutical preparation having controlled dissolution |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983679A (en) * | 2015-06-24 | 2015-10-21 | 万特制药(海南)有限公司 | Sustained-release suspension with lurasidone and preparation method of sustained-release suspension |
| WO2018043613A1 (en) * | 2016-08-31 | 2018-03-08 | 大日本住友製薬株式会社 | Aqueous suspension preparation |
| CN109640996A (en) * | 2016-08-31 | 2019-04-16 | 大日本住友制药株式会社 | Aqueous suspension type preparation |
| JPWO2018043613A1 (en) * | 2016-08-31 | 2019-06-24 | 大日本住友製薬株式会社 | Aqueous suspension formulation |
| EP3508203A4 (en) * | 2016-08-31 | 2020-05-27 | Sumitomo Dainippon Pharma Co., Ltd. | Aqueous suspension preparation |
| CN108721325A (en) * | 2017-04-13 | 2018-11-02 | 辽宁大熊制药有限公司 | Smectite turbid liquor and preparation method thereof |
| WO2019167977A1 (en) * | 2018-02-28 | 2019-09-06 | 大日本住友製薬株式会社 | Aqueous suspension-type pharmaceutical preparation |
| WO2019167978A1 (en) * | 2018-02-28 | 2019-09-06 | 大日本住友製薬株式会社 | Aqueous suspension-type pharmaceutical preparation having controlled dissolution |
| CN109998991A (en) * | 2019-04-28 | 2019-07-12 | 中国药科大学 | A kind of long-acting intramuscular injection nanosuspension of Lurasidone HCl and preparation method thereof |
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