Aripiprazole - Names and Identifiers
Name | Aripiprazole
|
Synonyms | OPC 31 ABILIFY ABILITAT OPC 14597 Aripiprazole ARIPIPRAZOLE ARIPIPRAZOLE-D8 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyril 7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone
|
CAS | 129722-12-9
|
EINECS | 603-355-5 |
InChI | InChI=1/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29) |
InChIKey | CEUORZQYGODEFX-UHFFFAOYSA-N |
Aripiprazole - Physico-chemical Properties
Molecular Formula | C23H27Cl2N3O2
|
Molar Mass | 448.39 |
Density | 1.263±0.06 g/cm3(Predicted) |
Melting Point | 139°C |
Boling Point | 646.2±55.0 °C(Predicted) |
Flash Point | 344.6°C |
Solubility | Soluble in Chloroform and Ethanol |
Vapor Presure | 1.38E-16mmHg at 25°C |
Appearance | Colorless flake crystalline solid |
Color | white to beige |
Merck | 14,785 |
pKa | 14.42±0.20(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
Refractive Index | 1.593 |
MDL | MFCD00892072 |
Use | Antipsychotics |
Aripiprazole - Risk and Safety
Risk Codes | R11 - Highly Flammable
R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed.
R36 - Irritating to the eyes
|
Safety Description | S16 - Keep away from sources of ignition.
S36/37 - Wear suitable protective clothing and gloves.
|
UN IDs | UN 1993C 3 / PGIII |
WGK Germany | 3 |
RTECS | VC8275950 |
HS Code | 29349990 |
Toxicity | TDLo ivn-dog: 0.03 mg/kg/10M TXAPA9 173,120,2001 |
Aripiprazole - Nature
Open Data Verified Data
colorless Flake Crystal, melting point l39.0 ~ 139.5 °c.
Last Update:2024-01-02 23:10:35
Aripiprazole - Preparation Method
Open Data Verified Data
7-(4-bromobutoxy)-3,4 dihydroquinolone and sodium iodide were refluxed in acetonitrile. 1-(2,3 dichlorophenyl) piperazine and triethylamine were added and refluxed. The solvent was distilled off, and the resulting material was dissolved in chloroform, washed with water, and dried over anhydrous magnesium sulfate. Recrystallization with ethanol is sufficient.
Last Update:2022-01-01 09:09:38
Aripiprazole - Standard
Authoritative Data Verified Data
This product is 7-[4-[4-(2, 3-dichlorophenyl)-l-farazinyl] butoxy]-3, 4-dihydroquinolone, calculated as dry product, containing no less than 98.5% of C23H27Cl2N3O2.
Last Update:2024-01-02 23:10:35
Aripiprazole - Trait
Authoritative Data Verified Data
This product is white or white crystalline powder, odorless.
This product is soluble in chloroform, methanol, acetone or acetonitrile slightly soluble in water, 0.lmol/L hydrochloric acid solution or 0.lmol/L sodium hydroxide solution is almost insoluble.
Last Update:2022-01-01 11:59:50
Aripiprazole - Introduction
Aripiprazole is a human 5-HT1A receptor agonist, Ki is 4.2 nM.
Last Update:2022-10-16 17:13:07
Aripiprazole - Use
Open Data Verified Data
The FDA approved the product on November 15, 2002. Quinolinone derivatives, is the third generation of atypical antipsychotic drugs. Aripiprazole, the first dopamine system stabilizer, has a significant effect on both positive and negative symptoms of schizophrenia. For the treatment of schizophrenia, can significantly improve this kind of schizophrenia, but there are not other common side effects of antipsychotic drugs, such as weight gain and involuntary muscle activity, but may cause Head Pain, anxiety and Sleep Initiation and Maintenance Disorders and other symptoms.
Last Update:2022-01-01 09:09:39
Aripiprazole - Differential diagnosis
Authoritative Data Verified Data
- an appropriate amount of aripiprazole control was taken, dissolved in methanol and diluted to prepare a solution containing about 0.2mg per 1 ml as a control solution. Test according to the chromatographic conditions under the items of related substances, take 10 u1 of each of the reference solution and the test solution under the items of related substances, respectively inject human liquid chromatography, record the chromatogram, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
- This product is dissolved in methanol and diluted to prepare a solution containing about 16ug per lml, which is determined by UV-Vis spectrophotometry (General 0401), there is an absorption maximum at a wavelength of 255nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 1291).
- Take appropriate amount of this product, according to X-ray diffraction method (General rule 0451 powder X-ray diffraction method) inspection, in the crystal plane spacing of 8.0a± 0.1A,6.2A ± 0.1A,5.3A ± 0.la, 4.6A ± 0.la, 4.4A ± 0.lA with 4.0a +0.lA should have characteristic diffraction peaks.
Last Update:2022-01-01 11:59:51
Aripiprazole - Exam
Authoritative Data Verified Data
Related substances
Take 10mg of this product, put it in a 50ml measuring flask, add methanol to dissolve and dilute to the scale, shake well, as a test solution; Take 1 ml of the test solution with precision, set in a 200ml measuring flask, dilute to the scale with methanol, and shake to serve as a control solution. According to the test of high performance liquid chromatography (General rule 0512), silica gel bonded with decylsilane was used as the filler, and citrate buffer solution (9.6g of diammonium citrate, 2.0g of citric acid and g of sodium dodecyl sulfate) was used, water was added to dissolve and diluted to 4.7 ml, and the pH was adjusted to with ammonia. Acetonitrile (55:45) was used as mobile phase; The detection wavelength was 255mn. Take the appropriate amount of impurity I, impurity II and aripiprazole reference, add methanol to dissolve and dilute to prepare a mixed solution containing about 5ug of impurity I, impurity II and aripiprazole in each lml, respectively, as the applicable solution of the system, 10ul injection liquid chromatograph is used to record the chromatogram. The order of peaks is impurity I, impurity I and aripiprazole, and the separation degree between chromatographic peaks should be greater than 3.0. 10 u1 of control solution and 10 u1 of test solution were respectively injected into human liquid chromatograph, and the chromatogram was recorded to 2 times of the retention time of principal component peak. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, impurity II is calculated as the corrected peak area (multiplied by the correction factor of 1.2) and shall not be greater than 0.2 times (0.1%) the area of the main peak of the control solution, other single impurity peak area shall not be greater than 0.2 times (0.1%) of the main peak area of the control solution, the sum of each impurity peak area (where the impurity n peak area is calculated by the principal component self-control method multiplied by the correction factor) not greater than the main peak area of the control solution (0.5%).
residual solvent
take about 0.lg of this product, weigh it accurately, put it in a 20ml headspace bottle, add 5ml of reference liquid to dissolve it, seal it, and use it as a test solution. Take an appropriate amount of anhydrous ethanol, precision weighing, and dimethyl sulfoxide dissolved and diluted to make each 1 ml of ethanol containing 0.1 mg of the solution was used as a reference stock solution, 5ml of which was precisely weighed, placed in a 20ml headspace bottle, and the mouth of the bottle was sealed to serve as a reference solution. According to the test for determination of residual solvents (General rule 0861, second method), the capillary column with 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polarity) as stationary liquid is used as the chromatographic column, and the initial temperature is 40 ℃, the temperature was maintained for 5 minutes and then increased to 180°C at a rate of 10°C per minute; The detector temperature was 250°C, the inlet temperature was 200°C; And the split ratio was 1:1. The Headspace bottle equilibration temperature was 80°C and the equilibration time was 30 minutes. Take the reference solution into the headspace, the separation degree between the ethanol peak and the solvent peak should meet the requirements, and the number of the theoretical plate should not be less than 5000 based on the ethanol peak. Then the reference solution and the test solution were injected into the headspace, and the chromatogram was recorded. According to the external standard method, the peak area is calculated, and after the ethanol peak area in the reference solution is subtracted, the residual amount of ethanol should comply with the regulations.
loss on drying
take l.Og of this product, dry to constant weight at 105°C, and lose no more than 0.5% of weight (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update:2022-01-01 11:59:52
Aripiprazole - Content determination
Authoritative Data Verified Data
take this product about 0.35g, precision weighing, add glacial acetic acid 30ml to dissolve, add crystal violet indicator solution 1 drop, with perchloric acid titration solution (0.1 mol/L) titration until the solution shows blue color, and the titration result is corrected by blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 44.84mg of C23H27Cl2N3O2.
Last Update:2022-01-01 11:59:52
Aripiprazole - Category
Authoritative Data Verified Data
Last Update:2022-01-01 11:59:53
Aripiprazole - Storage
Authoritative Data Verified Data
light-shielded, sealed, and stored in a dry place.
Last Update:2022-01-01 11:59:53
Aripiprazole - Aripiprazole orally disintegrating tablets
Authoritative Data Verified Data
This product contains aripiprazole (C23H27Cl2N3O2) should be 90.0% to 110.0% of the label.
trait
This product is white or off-white.
identification
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of the fine powder of this product, add methanol to dissolve and dilute to prepare a solution containing about 16 μl of aripiprazole per 1 ml, filter, and measure by UV-Vis spectrophotometry (General 0401), there is an absorption maximum at a wavelength of 255mn.
examination
- Related substances appropriate amount of fine powder of this product (about equivalent to 10 mg of aripiprazole) is placed in a 50ml measuring flask, dissolved with methanol and diluted to the scale, shaken and filtered, the filtrate was taken as a test solution; 1 ml was accurately measured, placed in a 200ml measuring flask, diluted to a scale with methanol, and shaken to obtain a control solution. Determination according to the method of aripiprazole related substances. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, impurity II is calculated as the corrected peak area (multiplied by the correction factor of 1.2) and shall not be greater than 0.4 times (0.2%) the area of the main peak of the control solution, other single impurity peak area shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, the sum of each impurity peak area (where the impurity n peak area is calculated by the principal component self-control method multiplied by the correction factor) not more than 2 times (1.0%) the area of the main peak of the control solution.
- Content uniformity take 1 tablet of this product, add methanol to dissolve aripiprazole and quantitatively dilute to prepare a solution containing 0.2mg per 1 ml, shake well, filter, and take the continued filtrate as the test solution. Determination of content according to the method under the content determination item, should comply with the provisions (General 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 third method), with 1% sodium dodecyl sulfate 0.100 ml of 1 mol/L hydrochloric acid solution is the dissolution medium, the rotation speed is rpm, and the operation is carried out according to law. After 30 minutes, 10ml of the solution is filtered, and the appropriate amount of the filtrate is taken, A solution containing about 20ug per 1 ml was prepared by quantitative dilution with dissolution medium as a test solution, the dissolution medium was added to dissolve and quantitatively dilute to prepare a solution containing about 20ug per 1 ml as a reference solution. Take the control solution and the test solution, according to the ultraviolet-visible spectrophotometry (General rule 0401), at the wavelength of nm, respectively, the absorbance is measured, calculate the amount of each dissolution. The limit is 70% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Citrate buffer (diammonium citrate 9.6g, citric acid 1.6g and sodium dodecyl sulfate 2.og, dissolved in water and diluted to 1000ml, the mobile phase was acetonitrile (55:45) and adjusted to pH 4.7 with ammonia; The detection wavelength was 255nm. Take appropriate amounts of impurity I, impurity II and aripiprazole reference, add methanol to dissolve and dilute to prepare a mixed solution containing about 5 Pure Solutions per 1 ml, respectively, as a system applicable solution, take 10ul injection liquid chromatograph and record the chromatogram. The order of peaks is impurity I, impurity II and aripiprazole, and the resolution between peaks should be greater than 3.0.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about 10mg equivalent to aripiprazole), put in 50ml measuring flask, add methanol to dissolve aripiprazole and dilute to the scale, shake well, filter, take the filtrate as a test solution, and inject 10ul into the liquid chromatograph to record the chromatogram, precision weighing, and methanol dissolved and quantitative dilution made per 1 ml containing 0.2mg of the solution, the same method. According to the external standard method to calculate the peak area, that is.
category
Same as aripiprazole.
specification
(l)5mg (2)10mg (3)20mg
storage
sealed storage.
Last Update:2022-01-01 11:59:54
Aripiprazole - Aripiprazole tablets
Authoritative Data Verified Data
This product contains aripiprazole (C23H27Cl2N3O2) should be 90.0% to 110.0% of the label.
trait
This product is white-like tablets or colored tablets or film-coated tablets, white or white after removing the coating.
identification
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of the fine powder of this product, add methanol to dissolve and dilute to prepare a solution containing 16ug of aripiprazole per lml, filter and measure by UV-Vis spectrophotometry (General rule 0401), there is an absorption maximum at a wavelength of 255nm.
examination
- Related substances take an appropriate amount of the fine powder of this product (about 10mg equivalent to aripiprazole), put it in a 50ml measuring flask, dissolve it in methanol and dilute it to the scale, shake it well and filter it through it, the filtrate was taken as a test solution; 1ml was accurately measured, placed in a 200ml measuring flask, diluted to a scale with methanol, and shaken to obtain a control solution. Determination according to the method of aripiprazole related substances. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, impurity II is calculated as the corrected peak area (multiplied by the correction factor of 1.2) and shall not be greater than 0.4 times (0.2%) the area of the main peak of the control solution, other single impurity peak area shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, the sum of each impurity peak area (where the impurity II peak area is calculated by the principal component self-control method multiplied by the correction factor) not more than 2 times (1.0%) the area of the main peak of the control solution.
- Content uniformity take 1 tablet of this product, put it in a 25ml(5mg, 15mg specification) or 50ml (10 mg specification) measuring flask, add an appropriate amount of methanol to dissolve aripiprazole and dilute it to the scale, shake, filter, take the filtrate as a test solution (5mg, l0mg specifications) or precision take 3ml, put it in a 10ml measuring flask, dilute to the scale with methanol, shake, as a test solution (15mg specification). Determination of content according to the method under the content determination item, should comply with the provisions (General 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with hydrochloric acid-potassium chloride buffer (potassium chloride 3.73g, add 0.2mol/L hydrochloric acid 425ml, add water to dissolve and dilute to 1000ml, shake well) 900ml as dissolution medium, rotate speed is 60 rpm, operate according to law, after 30 minutes, 20ml of the solution was filtered, and 10ml of the initial filtrate was discarded. The additional filtrate was taken as the test solution, solutions containing 10ug(10mg, 15mg specification) or 5ug( 5mg specification) per 1 ml were prepared as control solutions by quantitative dilution with dissolution medium. The dissolution amount of each tablet was calculated as measured by the method under the content measurement item. The limit is 75% of the labeled amount and shall be in accordance with the provisions
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; With citrate buffer (diammonium citrate 9.6g, citric acid 1.6g and sodium dodecyl sulfate 2.0g, water was added to dissolve and diluted to 4.7 ml, and the pH value was adjusted to with ammonia water)-acetonitrile (55:45) as mobile phase; The detection wavelength was 255nm. Take appropriate amounts of impurity I, impurity II and aripiprazole reference, add methanol to dissolve and dilute to prepare a mixed solution containing about 5ug per lml, respectively, as a system applicable solution, take 10u1 injection liquid chromatograph and record the chromatogram. The order of peaks is impurity I, impurity II and aripiprazole, and the degree of separation between peaks should be greater than 3.0.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 10mg equivalent to aripiprazole), put it in a 50ml measuring flask, add methanol to dissolve aripiprazole and dilute to the scale, shake well, filter, take the filtrate as a test solution, and inject 10u1 into the liquid chromatograph to record the chromatogram, precision weighing, and methanol dissolved and quantitative dilution made per 1 ml containing 0.2mg of the solution, the same method. According to the external standard method to calculate the peak area, that is.
category
Same as aripiprazole.
specification
(l)5mg (2)10mg (3)15mg
storage
light-shielded, sealed, and stored in a dry place.
Last Update:2022-01-01 11:59:55
Aripiprazole - Aripiprazole capsules
Authoritative Data Verified Data
This product contains aripiprazole (C23H27Cl2N302) should be 90.0% to 110.0% of the label.
trait
The content of this product is white powder.
identification
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of the contents of this product, add methanol to dissolve and dilute to make a solution containing about 16ug per lml, filter, and measure by UV-Vis spectrophotometry (General rule 0401), there is an absorption maximum at a wavelength of 255mn.
examination
- Related Substances: take an appropriate amount of the contents of this product (about 10 mg of aripiprazole), put it in a 50ml measuring flask, dissolve it in methanol, dilute it to the scale, shake it well, and filter it, the filtrate was taken as the test solution; 1ml was accurately measured and placed in a 200ml bottle, diluted to the scale with fermentation broth, and shaken well to serve as a control solution. Determination according to the method of aripiprazole related substances. If there are impurity peaks in the chromatogram of the test solution, the peak area of impurity I shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, impurity II is calculated as the corrected peak area (multiplied by the correction factor of 1.2) and shall not be greater than 0.4 times (0.2%) the area of the main peak of the control solution, other single impurity peak area shall not be greater than 0.4 times (0.2%) of the main peak area of the control solution, the sum of each impurity peak area (where the impurity II peak area is calculated by the principal component self-control method multiplied by the correction factor) not more than 2 times (1.0%) the area of the main peak of the control solution.
- Content uniformity: Take 1 capsule of this product, pour the content into a 25ml measuring flask, wash the capsule shell with toluene in portions, and incorporate the washing solution into the measuring flask, according to the method under the content determination item, from the time of "dissolving and diluting to the scale", the determination shall be carried out according to law and shall comply with the regulations (General 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 third method), with sodium dodecyl sulfate-sodium acetate buffer (take sodium dodecyl sulfate 5G, sodium acetate 2G, add water to dissolve and dilute to looml, adjust the pH value to 4.7 with acetic acid) 200ml as dissolution medium, rotate at 100 rpm, operate according to law, after 45 minutes, take 20ml of solution to filter, 10ml of the initial filtrate was discarded, and the secondary filtrate was taken as the test solution. An appropriate amount of the aripiprazole reference substance was also taken, and the solution was precisely weighed and dissolved by adding an appropriate amount of fermentation broth, quantitative dilution with the dissolution medium to make a solution containing 25 gm per 1 ml, as a control solution. According to the high performance liquid chromatography (General 0512) test, silica gel bonded with eighteen alkyl silane was used as the filler; Methanol-0.1% triethylamine solution (90:10) was used as the mobile phase; The detection wavelength was 255mn. The number of theoretical plates was not less than 1000 calculated by aripiprazole peak. 20 u1 of the test solution and the reference solution were respectively injected into the liquid chromatograph, and the chromatograms were recorded. According to the external standard method, the dissolution amount of each particle was calculated by the peak area. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica as filler; With citrate buffer (diammonium citrate 9.6g, 1.6g, sodium dodecyl sulfate was dissolved in water and diluted to 4.7 ml, and the pH value was adjusted to with ammonia water)-ethyl alcohol (55:45) as mobile phase; The detection wavelength was 255nm. Take appropriate amounts of impurity I, impurity II and aripiprazole reference, add methanol to dissolve and dilute to prepare a mixed solution containing about 5ug per lml, respectively, as a system applicable solution, take 10ul injection liquid chromatograph and record the chromatogram. The peak sequence is impurity I, impurity II and aripiprazole, and the resolution between each chromatographic peak should be greater than 3.0.
- determination Method: Take 20 capsules of this product, accurately weigh the contents, pour out the contents, accurately weigh the capsule shell, calculate the average loading, mix the contents evenly, add methanol to dissolve aripiprazole in a 50ml measuring flask and dilute it to the standard. Shake well, filter, and take the continued filtrate as the test solution, lOul was injected into human liquid chromatograph accurately, and the chromatogram was recorded. The appropriate amount of aripiprazole reference product was weighed accurately, dissolved with methanol and quantitatively diluted to prepare a solution containing 0.2mg per 1 ml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as aripiprazole.
specification
5mg
storage
sealed and stored in a dry place.
Last Update:2022-01-01 11:59:56