alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Names and Identifiers
Name | S-(-)-carbidopa
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Synonyms | mk486 MK 486 Carbidopa CCRIS 5093 Tocris-0455 MLS000069628 SMR000058235 S(-)-CARBIDOPA S-(-)-carbidopa NCGC00024596-01 N-Aminomethyldopa HYDROCINNAMIC ACID Carbidopa anhydrous Benzenepropanoic acid Carbidopum [INN-Latin] alpha-Methyldopahydrazine alpha-methyldopahydrazine Hadrazino-alpha-methyldopa hydrazino-alpha-methyldopa l-alpha-methyldopahydrazine L-alpha-Methyldopahydrazine alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- -Hydrazino-3,4-dihydroxy-methylhy-drocinnamicacid 1-(Mesithylene-2-sulfonyl)-3-nitro-1,2,4-triazole alpha-HYDRAZINO-3,4-DIHYDROXY-alpha-METHYL-L-KINSON -Hydrazino-3,4-dihydroxy-methylbenzenep-ropanicacid 4-dihydroxy-alpha-methyl-alpha-hydrazino-l-hydrocinnamicaci L-3-(3,4-Dihydroxyphenyl)-2-methyl-2-hydrazinopropionic acid 3-(3,4-DIHYDROXY-PHENYL)-2-HYDRAZINO-2-METHYL-PROPIONIC ACID 3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methyl-propanoic acid 4-dihydroxy-alpha-methyl-alpha-hydrazino-(s)-benzenepropanoicaci (2S)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methyl-propanoic acid (-)-L-alpha-Hydrazino-3,4-dihydroxy-alpha-methylhydrocinnamic acid alpha-Hydrazino-alpha-methyl-beta-(3,4-dihydroxyphenyl)propionic acid L-alpha-Methyl-alpha-hydrazino-beta-(3,4-dihydroxyphenylpropionic acid L-alpha-Methyl-beta-(3,4-dihydroxyphenyl)-alpha-hydrazinopropionic aci d
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CAS | 28860-95-9
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EINECS | 657-445-4 |
InChI | InChI=1/C10H14N2O4.H2O/c1-10(12-11,9(15)16)5-6-2-3-7(13)8(14)4-6;/h2-4,12-14H,5,11H2,1H3,(H,15,16);1H2/t10-;/m0./s1 |
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Physico-chemical Properties
Molecular Formula | C10H14N2O4
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Molar Mass | 226.23 |
Density | 1.2616 (rough estimate) |
Melting Point | 203-205° (dec); mp 208° |
Boling Point | 367.84°C (rough estimate) |
Specific Rotation(α) | D -17.3° (methanol) |
Flash Point | 273.5°C |
Solubility | Slightly soluble in water, very slightly soluble in ethanol (96 per cent), practically |
Vapor Presure | 5.27E-12mmHg at 25°C |
Appearance | Solid powder |
Color | White to Off-White |
pKa | 3.40±0.14(Predicted) |
Storage Condition | -20°C |
Stability | Unstable in Solution |
Refractive Index | 1.5000 (estimate) |
MDL | MFCD00889211 |
Physical and Chemical Properties | Crystal. Melting point 203-205 °c (decomposition). |
Use | For various causes of Parkinson's disease. |
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Risk and Safety
WGK Germany | 3 |
RTECS | MW5298000 |
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Standard
Authoritative Data Verified Data
This product is (S)-a-methylhydrazino-3, 4-dihydroxyphenylpropionic acid monohydrate. The content of C10H14N204 shall not be less than 99.0%, calculated as anhydrous.
Last Update:2024-01-02 23:10:35
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Trait
Authoritative Data Verified Data
- This product is white or white villous crystal; Almost odorless.
- This product is slightly soluble in water or fermentation broth, almost insoluble in ethanol or chloroform; Soluble in dilute hydrochloric acid.
specific rotation
take this product, precision weighing, add aluminum chloride solution (take aluminum chloride hexahydrate 40g, add appropriate amount of water, heat to dissolve, dilute to 60ml with water, shake, such as color, add 0.5g of activated carbon, stir for 10 minutes, filter, filtrate with 1% sodium hydroxide solution to adjust the pH value to 1.5, that is, dissolve and dilute to make a solution containing about l0mg per lml, measured according to law (General rule 0621), the specific rotation is -22.5 ° to -26.5 °.
absorption coefficient
take this product, precision weighing, plus O. 1 mol/L hydrochloric acid solution is dissolved and quantitatively diluted to prepare a solution containing about 50ug per 1 ml, and the absorbance is measured at the wavelength of 281nm by UV-visible spectrophotometry (General rule 0401), the absorption coefficient is 117 to 129.
Last Update:2022-01-01 11:37:00
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Differential diagnosis
Authoritative Data Verified Data
The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 97).
Last Update:2022-01-01 11:37:00
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Exam
Authoritative Data Verified Data
Related substances
take this product, precision weighing, add 0.1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing about 5mg per 1 ml, which was used as a test solution (new system). In addition, weigh about 5mg of Methyldopa reference substance accurately, put it in 200ml children's bottle, add 1ml of test solution accurately, add 0.1 mol/L hydrochloric acid solution methyldopa was dissolved and diluted to the scale, and shaken to serve 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, and 0.05mol/L sodium dihydrogen phosphate solution (adjusted to pH 2.7 with phosphoric acid) was used in the experiment: 5) as mobile phase, the detection wavelength was 280mn. The number of theoretical plates shall not be less than 5000 based on the carbidopa peak, and the separation degree between methyldopa peak and carbidopa peak shall be greater than that of precision. 20ul of test solution and 20ul of control solution shall be injected into human liquid chromatograph respectively, the chromatogram was recorded to 8 times of the retention time of the main component peak. If the methyl dopa peak in the chromatogram of the test solution is shown, the peak area shall not exceed 0.5% based on the external standard method, and the peak area of other individual impurities shall not be greater than the main peak area of the control solution (0.5% ) ; the total amount of impurities should not exceed 1.0%.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 6.9% ~ 7.9%.
ignition residue
This product l.O g, inspection according to law (General 0841), residue 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 11:37:01
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Content determination
Authoritative Data Verified Data
take this product about 0.25g, precision weighing, precision plus perchloric acid titration solution (0.lmol/L)15ml dissolved, add 15ml of acetic anhydride and crystal violet indicator 2 drops, with sodium acetate titration solution (0.1 mol/L) titration to the solution is green, and the result of the titration is corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 22.62mg of C10H14N2O4.
Last Update:2022-01-01 11:37:02
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Category
Authoritative Data Verified Data
decarboxylase inhibitors.
Last Update:2022-01-01 11:37:02
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update:2022-01-01 11:37:02
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Carbidopa tablets
Authoritative Data Verified Data
This product contains anhydrous carbidopa (C10H14N204) should be 90.0% to 110.0% of the label children.
trait
This product is white-like tablets.
identification
- take an appropriate amount of fine powder of this product (about equivalent to 10 mg of carbidopa), add 10ml of methanol, shake to dissolve carbidopa, filter, and the filtrate is divided into two parts, add 1ml of newly prepared 0.2% ferrous sulfate solution and 1% potassium sodium tartrate solution in one portion, add about 20~40mg of ammonium acetate, that is, Blue Purple, add 1 drop of concentrated ammonia solution, shake, purple is darkened; Add P-dimethylaminobenzaldehyde solution (take p-dimethylaminobenzaldehyde 0.4g, add 0.1 mol /L sulfuric acid solution to 10ml)0.5, that is, orange yellow.
- the solution under the content measurement item was measured by ultraviolet-visible spectrophotometry (General 0401), and there was a maximum absorption at a wavelength of Nm.
examination
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.lmol/L hydrochloric acid solution 750ml is the dissolution medium, the rotation speed is 50 rpm, the operation is carried out according to law, after 30 minutes, the solution is taken, filtered, and the filtrate is taken according to the method under the content determination item, from the "UV-visible spectrophotometry", the dissolution amount of each tablet was calculated according to the law. 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
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to carbidopa 50mg), put it in a 100ml measuring flask, add 0.1 mol/L hydrochloric acid solution appropriate amount, shake to dissolve carbidopa, and dilute to the scale, shake, filter, take the continuous filtrate 5ml, put it in 50ml measuring flask, use 0. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, measure the absorbance at the wavelength of 281nm by UV-visible spectrophotometry (General rule 0401), and calculate according to the absorption coefficient of 123, that's right.
category
Same as carbidopa.
specification
25mg (as C10H14N204)
storage
light shielding, sealed storage.
Last Update:2022-01-01 11:37:03
alpha-hydrazino-3,4-dihydroxy-alpha-methyl-(S )- - Compound carbidopa tablets
Authoritative Data Verified Data
This product contains carbidopa (C10H14N2O4) and levodopa (C9H11NO4) should be 90.0% to 110.0% of the label amount.
prescription
carbidopa 25g
Levodopa 250g
Appropriate amount of excipients
Made into 1000 tablets
trait
This product is light blue.
identification
- in the chromatogram recorded under the content determination item, the retention time of the two main peaks of the test solution should be consistent with the retention time of the corresponding two main peaks of the control solution.
- take an appropriate amount of fine powder of this product (about 20mg equivalent to carbidopa), put it in a 100ml measuring flask, and add O.lmol/L hydrochloric acid solution 25ml and water 25ml, shake for 20 minutes, dilute to the scale with methanol, shake well, filter, as a test solution, use 0.1 mol/L hydrochloric acid solution-water-methanol (1:1:2) was prepared as a control solution containing 0.2mg of carbidopa and 2mg of levodopa per 1 ml; absorb the above two Solutions 10 u1, respectively, on the same silica gel G thin plate, with acetone-chloroform-n-butanol-glacial acetic acid-water (60:40:40:40:35) for the development of the solvent, it was developed, dried, sprayed with ninhydrin test solution, and heated at 105 ° C. For color development. The position and color of the two main spots displayed by the test solution should be consistent with the corresponding main spots of the control solution.
- two items (1) and (2) above can be selected as one item.
examination
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.lmol/L hydrochloric acid solution (750ml) is the dissolution medium, and the rotation speed is 50 revolutions per minute, which is operated according to the law. After 30 minutes, the appropriate amount of the solution is taken, filtered, and the chromatographic conditions under the content determination are taken, 20ul of the continuous filtrate was injected into the human liquid chromatograph, and the chromatogram was recorded. 1 mol/L hydrochloric acid solution was dissolved and quantitatively diluted to prepare a solution containing 33ug of carbidopa and 330ug of levodopa per 1 ml, and the dissolution amount of carbidopa and levodopa in each tablet was calculated by the same method. The limit is 80% 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; Sodium dihydrogen phosphate solution (take sodium dihydrogen phosphate 11.04g, add water 950ml to dissolve, add 0.024% sodium decanesulfonate 1.3ml, diluted to 2.8 mL with water, adjusted to pH with phosphoric acid) as mobile phase; The detection wavelength was 280nm. The number of theoretical plates shall not be less than 1000 calculated by the carbidopa peak, and the separation degree of carbidopa peak and levodopa peak shall meet the requirements.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 50mg equivalent to levodopa), put in a 100ml measuring flask, add 0.033mol/L phosphoric acid solution (10ml), slightly heat to dissolve carbidopa and levodopa, cool, dilute with water to scale, shake, filter, and take the continued filtrate as the test solution, injection of 20ul into the liquid chromatograph accurately, record the chromatogram; Take the appropriate amount of carbidopa reference substance and levodopa reference substance, and prepare the solution containing about 50ug carbidopa and 500ug levodopa per 1 ml by the same method, as the reference solution, the same method of determination, according to the external standard method to calculate the peak area, that is.
category
antiparkinsonian drugs.
storage
light-shielded, sealed, and stored in a dry place.
Last Update:2022-01-01 13:43:16