GABAPENTIN HYDROCHLORIDE
Gabapentin
CAS: 60142-96-3
Molecular Formula: C9H17NO2
GABAPENTIN HYDROCHLORIDE - Names and Identifiers
| Name | Gabapentin |
| Synonyms | GOE-3450 neurontin NEURONTIN GABAPENTIN AKOS 92109 Gabapentin GABAPENTINE GABAPENTIN HYDROCHLORIDE 1-(AMINOMETHYL)CYCLOHEXANEACETIC ACID 1-(aminomethyl)cyclohexaneacetic acid [2-(aminomethyl)cyclohexyl]acetic acid (1-aminomethyl-cyclohexyl)-acetic acid (1-AMINOMETHYL-CYCLOHEXYL)-ACETIC ACID |
| CAS | 60142-96-3 |
| EINECS | 262-076-3 |
| InChI | InChI=1/C9H17NO2/c10-6-8-4-2-1-3-7(8)5-9(11)12/h7-8H,1-6,10H2,(H,11,12) |
| InChIKey | UGJMXCAKCUNAIE-UHFFFAOYSA-N |
GABAPENTIN HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C9H17NO2 |
| Molar Mass | 171.24 |
| Density | 1.058±0.06 g/cm3(Predicted) |
| Melting Point | 162°C |
| Boling Point | 314.4±15.0 °C(Predicted) |
| Flash Point | 9℃ |
| Water Solubility | H2O: 10 mg/mL |
| Solubility | H2O: 10mg/mL |
| Vapor Presure | 6.32E-05mmHg at 25°C |
| Appearance | solid |
| Color | off-white |
| Merck | 14,4319 |
| BRN | 2359739 |
| pKa | pKa1 (25°) 3.68; pKa2 10.70 |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.484 |
| Physical and Chemical Properties | Melting Point: 162°C |
| In vitro study | Gabapentin concentration-dependent inhibition of potassium (+)-induced increases in [Ca(2 )] in fura-2-loaded human neocortical synaptosomes, the IC 50 is 17 mM and the maximum suppression is 37%. Gabapentin binds to the α2 delta subunit of the calcium channel to selectively attenuate the Ca(2) channel of the (2) internal flow of the P / Q type of the Ca presynaptic induced by depolarization, this will result in a decrease in the release of glutamate/aspartate from the excitatory amino acid nerve terminals to the noradrenergic nerve terminals by AMPA heteroreceptors. In rat cortical astrocytes and synaptosomes, Gabapentin causes production of cytoplasmic alterations and changes in extracellular concentrations of several amino acids, including L-leucine, L-valine, and L-phenylalanine, it is assumed to be an effect of pharmacological significance. In GABA B receptors constitutively expressing heterodimers of gb1a-GB2 subunits, Gabapentin reduces potassium-evoked calcium influx through voltage-gated calcium channels. In GABA-positive rat spinal dorsal horn neurons, Gabapentin increases N-methyl-D-aspartate (NMDA)-evoked currents in the presence of protein kinase C, possibly by increasing the glycine sensitivity of the NMDA receptor complex. In rat dorsal root ganglion neurons, Gabapentin enhances delayed allosteric activity of indeterminate voltage-activated potassium currents. |
| In vivo study | In rats, Gabapentin dose-dependently (10-100 mg/kg, oral) blocks the effects of static and dynamic allodynia. |
GABAPENTIN HYDROCHLORIDE - Risk and Safety
| Risk Codes | R61 - May cause harm to the unborn child R36/37/38 - Irritating to eyes, respiratory system and skin. R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S53 - Avoid exposure - obtain special instructions before use. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. |
| UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
| WGK Germany | 3 |
| RTECS | GU6496000 |
| HS Code | 29224999 |
| Hazard Class | IRRITANT |
GABAPENTIN HYDROCHLORIDE - Nature
Open Data Verified Data
crystallized from ethanol monoethyl ether, melting point 162~166 ℃; Or 165~167 ℃.
Last Update：2024-01-02 23:10:35
GABAPENTIN HYDROCHLORIDE - Preparation Method
Open Data Verified Data
reaction of monomethyl 1, 1-cyclohexanediacetic acid with ethyl chloroformate (dissolved in triethylamine in acetone) and an aqueous solution of sodium azide, the resulting product is refluxed in hydrochloric acid, gabapentin.
Last Update：2022-01-01 09:09:45
GABAPENTIN HYDROCHLORIDE - Standard
Authoritative Data Verified Data
This product is l-(aminomethyl) cyclohexylacetic acid. The content of C9H17N02 shall not be less than 98.5% calculated as dry product.
Last Update：2024-01-02 23:10:35
GABAPENTIN HYDROCHLORIDE - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline or crystalline powder; Odorless.
- This product is soluble in water, slightly soluble in ethanol, insoluble in three gas methane.
Last Update：2022-01-01 11:42:51
GABAPENTIN HYDROCHLORIDE - Use
Open Data Verified Data
The antiepileptic drug first developed by the United States company Warner-Lanbert, was first listed in the UK in 1993. Gabapentin is a novel antiepileptic drug that has been shown to prevent epilepsy in a variety of animal models. Gabapentin has a high affinity for the novel binding sites of brain tissue, it can pass through the body through the amino acid transfer body some barrier, compared with other anticonvulsants, gabapentin has minor behavioral and cardiovascular side effects. Additional treatment for epileptic patients with localized seizures that cannot be satisfactorily controlled or tolerated by conventional antiepileptic drugs, as well as those with localized seizures and then generalized epilepsy.
Last Update：2022-01-01 09:09:47
GABAPENTIN HYDROCHLORIDE - Differential diagnosis
Authoritative Data Verified Data
- take about 2mg of this product, add 2ml of water to dissolve, add about 2mg of ninhydrin, heat, the solution shows blue purple.
- The infrared absorption spectrum of this product should be consistent with that of the reference product (General rule 0402).
Last Update：2022-01-01 11:42:51
GABAPENTIN HYDROCHLORIDE - Exam
Authoritative Data Verified Data
pH
take 0.5g of this product, Add 10ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 6.5~8.0.
clarity and color of solution
take 0.5g of this product and add 0901 of water to dissolve it. The solution should be clear and colorless; If the color is colored, it should not be deeper compared with the yellow-green No. 1 Standard Colorimetric solution (General rule first method).
chloride
take 0.25g of this product and check it according to law (General rule 0801). Compared with the control solution made of 0.020% of standard gasification sodium solution, it should not be more concentrated (). Cyanide take this product 1.0g, inspection according to law (General Principles 0806 The first law), should comply with the provisions.
Related substances
take an appropriate amount of this product, weigh it accurately, add the solvent (take potassium dihydrogen phosphate 1.2g, add water 1000ml to dissolve, adjust the pH value to 6.9 with 5mol/L potassium hydroxide solution) dissolve and dilute to make a solution containing about 14mg per 1ml as a test solution; Take about 14mg of the reference substance of impurity I, weigh it accurately, put it in a 10ml measuring flask, add 5ml of solvent, shake to dissolve, add 1ml of test solution accurately, dilute to scale with solvent, shake well, take 1ml accurately, put it in 100ml measuring flask, dilute to scale with solvent, as a control solution. According to high performance liquid chromatography (General 0512), silica gel was bonded with eighteen alkyl silane as filler; Phosphate buffer solution (1.2g of potassium dihydrogen phosphate, of water was added to dissolve, with 5mol/L potassium hydroxide solution to adjust the pH value to 6.9)-acetonitrile (94:6) as mobile phase A, phosphate buffer (take potassium dihydrogen phosphate 1.2g, add water ml to dissolve, adjust pH value to 6.9 with 5mol/L potassium hydroxide solution)-acetonitrile (7:3) as mobile Phase B, elute with linear gradient as shown below; The detection wavelength is 210nm; The flow rate is 1.5ml per minute; the column temperature was 40°C. 20ul of the control solution was taken and injected into the human Liquid Chromatograph. The order of peaks was gabapentin and impurity I, and the number of theoretical plates of the two peaks was not less than 3000. 20 u1 of each of the control solution and the test solution were accurately measured and injected into the human liquid chromatograph respectively, and the chromatogram was recorded. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of impurity I peak in the control solution, the peak area shall be calculated according to the external standard method, and shall not exceed 0.1%, the Peak area of other single impurity shall not be greater than the peak area of gabapentin in the control solution (0.1% ) , and the sum of the peak areas of other impurities shall not be greater than 5 times (0.5%) of the peak area of gabapentin in the control solution. The chromatogram of the test solution is 0.3 times smaller than that of the control solution, and the peak area of the peak is negligible (0.03%).
residual solvent
take about 0.2g of this product, precision weighing, top empty bottle, precision add water 5ml to dissolve, seal, as a test solution; Another methanol, dichloromethane, the appropriate amount of toluene and pyridine shall be accurately weighed, dissolved by adding water and quantitatively diluted to prepare a mixed solution containing 120ug,24ug,35.6UG and 8ug per lml respectively, and 5ml shall be accurately weighed and placed in the top empty bottle, sealed as a control solution. According to the test for determination of residual solvents (General rule 0861, second method), a capillary column with 5% diphenyl-95% dimethylpolysiloxane (or similar polarity) as the stationary liquid is used as the chromatographic column, and the initial temperature is 40°C, hold for 5 minutes, then raise the temperature to 240°C at a rate of 10°C per minute; The temperature of the injection port is 100°C, regardless of the flow, and the temperature of the detector is 260°C; the Headspace bottle equilibration temperature was 85°C and the equilibration time was 30 minutes. Take the reference solution into the headspace, the separation degree between the peaks should meet the requirements. Then take the reference solution and the test solution into the headspace respectively, record the chromatogram, and calculate the peak area according to the external standard method. The residual amounts of methanol, dichloromethane, toluene and pyridine shall be in accordance with the regulations.
loss on drying
take this product, with phosphorus pentoxide as desiccant, drying at room temperature and reduced pressure to constant weight, loss of weight shall not exceed 0.5% (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
This product l.Og, inspection according to law (General Principles 0821 The first law), containing heavy metals shall not exceed 20 parts per million.
Last Update：2022-01-01 11:42:52
GABAPENTIN HYDROCHLORIDE - Content determination
Authoritative Data Verified Data
take this product 0.15g, precision weighing, add glacial acetic acid 20ml, shake to dissolve, add crystal violet indicator solution 1 drop, with perchloric acid titration solution (0.1 mol/L) titration to the solution is blue-green, and the titration result is corrected by blank test. Each 1 ml perchloric acid titration solution (0.1 mol/L) corresponds to 17.12mg of C9H17N02.
Last Update：2022-01-01 11:42:53
GABAPENTIN HYDROCHLORIDE - Category
Authoritative Data Verified Data
antiepileptic drugs.
Last Update：2022-01-01 11:42:53
GABAPENTIN HYDROCHLORIDE - Storage
Authoritative Data Verified Data
sealed storage.
Last Update：2022-01-01 11:42:53
GABAPENTIN HYDROCHLORIDE - Gabapentin Tablets
Authoritative Data Verified Data
This product contains gabapentin (C9H17N02) should be 90.0% to 110.0% of the label.
trait
This product is white tablet.
identification
- take an appropriate amount of fine powder of this product (about 10 mg of gabapentin), add 10ml of water to dissolve, filter, take 2ml of filtrate, and add 2mg of ninhydrin. Heat, the solution shows blue purple color.
- 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.
examination
- relevant substances: Take appropriate amount of fine powder of this product, weigh it accurately, add solvent (take 1.2g of potassium dihydrogen phosphate, add 1000ml of water to dissolve, adjust pH value to 6.9 with 5mol/L potassium hydroxide solution) dissolve and dilute to make a solution containing about 14mg per 1ml, filter, take the filtrate as the test solution; Take the gabapentin impurity I reference product about 14mg, precision weighing, add 5ml of solvent into 10ml measuring flask, shake to dissolve, add lml of human test solution precisely, dilute to the scale with solvent, shake well, take 1ml precisely, set in a 100ml measuring flask, dilute to the scale with solvent, and shake to serve as a control solution. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of impurity I peak in the control solution, the peak area shall be calculated according to the external standard method, the Peak area of other individual impurities shall not exceed 0.4% of the labeled amount of gabapentin and shall not exceed 4 times (0.4%) The Peak area of gabapentin in the control solution, the sum of the peak areas of other impurities shall not be greater than 10 times (1.0%) of the peak area of gabapentin in the control solution. The chromatogram of the test solution showed 0. 3 times smaller peak area than that of the control solution.
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 first method), water 900ml as the dissolution medium, the speed of 75 rpm, according to the law, after 30 minutes, the solution was taken, filtered, and the filtrate was taken as the test solution, water was added to dissolve and quantitatively diluted to prepare a solution containing about 0.3mg per 1 ml as a control solution. The dissolution rate of each tablet was calculated according to the method under the content determination 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).
- color introduction conditions and system applicability test using eighteen alkyl silane bonded silica gel as filler; Phosphate buffer solution (1.2g of potassium dihydrogen phosphate, add water 940ml to dissolve, the pH value was adjusted to 6.9 with 5mol/L potassium hydroxide solution)-acetonitrile (94:6) as mobile phase; The detection wavelength was 2lonm.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 400mg equivalent to gabapentin), put in a 100ml measuring flask, add an appropriate amount of solvent (take 1.2g of potassium dihydrogen phosphate, add 6.9 of water to dissolve, adjust the pH value to with 5mol/L potassium hydroxide solution), shake to dissolve gabapentin, dilute to the scale with the above solvent, shake, filter, take the filtrate as the test solution, take 20 u1 with precision, inject the human liquid chromatograph, record the chromatogram; in addition, an appropriate amount of gabapentin reference substance was taken, dissolved and quantitatively diluted with the above solvent to prepare a solution containing about 4mg per 1 ml, and the same method was used for determination. According to the external standard method to calculate the peak area, that is.
category
with gabapentin.
specification
0.3g
storage
sealed storage.
Last Update：2022-01-01 11:42:54
GABAPENTIN HYDROCHLORIDE - Gabapentin capsules
Authoritative Data Verified Data
This product contains gabapentin (C9H17N02) should be 90.0% to 110.0% of the label.
trait
The contents of this product are white or off-white powder or granules.
identification
- take an appropriate amount of the contents of this product (about equivalent to 10 mg of gabapentin), add 10ml of water to dissolve, filter, take 2ml of filtrate, and add 2mg of ninhydrin. Heat, the solution shows blue purple color.
- 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.
examination
- relevant substances take appropriate amount of the contents of this product, weigh it accurately, add solvent (take potassium dihydrogen phosphate 1.2g, add water 1000ml to dissolve, adjust pH value to 6.9 with 5mol/L potassium hydroxide solution) dissolve and dilute to make a solution containing about 14mg per 1ml, filter, take the filtrate as the test solution; Take the gabapentin impurity I reference product about 14mg, precision weighing, add 5ml of solvent into 10ml measuring flask, shake to dissolve, add 1ml of human test solution precisely, dilute to scale with solvent, shake well, take 1ml precisely, set in a 100ml measuring flask, dilute to the scale with solvent, and shake to serve as a control solution. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of impurity I peak in the control solution, the peak area shall be calculated according to the external standard method, the Peak area of other individual impurities shall not exceed 0.4% of the labeled amount of gabapentin and shall not exceed 4 times (0.4%) The Peak area of gabapentin in the control solution, the sum of the peak areas of other impurities shall not be greater than 10 times (1.0%) of the peak area of gabapentin in the control solution. Test Solution
- the peak in the chromatogram which is 0.3 times smaller than the area of the peak of gabapentin in the control solution is negligible (0.03%).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 first method), with water as the dissolution medium, the speed is 100 rpm, according to the law, after 20 minutes, the solution was taken, filtered, and the continued filtrate was taken as the test solution, water was added to dissolve and quantitatively diluted to prepare about 0.1 mg per 1 mL (0.1G specification) or 0.3mg(0.3g specification) or 0.4mg(0.4g specification) solution, as a reference solution, measured according to the method under the content measurement item, calculate the dissolution amount of each particle. The limit is 80% 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 applicability test using eighteen alkyl silane bonded silica gel as filler; Phosphate buffer (take potassium dihydrogen phosphate 1.2G, add water 940ml to dissolve, the pH value was adjusted to 6.9 with 5mol /L potassium hydroxide solution)-acetonitrile (94:6) as mobile phase; The detection wavelength was 210nm.
- determine the contents under the item of difference in loading amount, mix evenly, accurately weigh an appropriate amount (about 400mg equivalent to gabapentin), and place it in a 100ml measuring flask, add an appropriate amount of solvent (take 1.2g of potassium dihydrogen phosphate, add 6.9 of water, adjust the pH value to with 5mol/L potassium oxychloride solution), shake to dissolve gabapentin, dilute to the scale with the above solvent, shake, filter, take the filtrate as the test solution, take 20 u1 with precision, inject into the liquid chromatograph, record the chromatogram; in addition, an appropriate amount of gabapentin reference substance is taken, dissolved and quantitatively diluted with the above solvent to prepare a solution containing 4mg per 1 ml, which is determined by the same method and calculated by peak area according to external standard method.
category
with gabapentin.
specification
(1)0.lg (2)0.3g (3)0.4g
storage
sealed storage.
Last Update：2022-01-01 11:42:55
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View History
GABAPENTIN HYDROCHLORIDE
芦荟大黄素8-0葡萄糖苷
(2-甲酰基苯并呋喃-5-基)氨基甲酸叔丁酯
2-羧乙基三苯基溴化L
5-[[2-(1-吡咯烷基)乙基]硫基]-2-噻唑胺
1-[5-(2-羟基乙基)硫代]-4-硝基-2-噻吩]乙基-1-酮
2-[3-[(甲巯基)羰基氨基]-1-金刚烷基]乙酸
1-苄基-2-(甲基磺基)-1H-咪唑-5-酰氯盐酸盐
吡啶(2-偶氮-4)间苯二酚
2-甲基-2-丙基(2-氨基-4-氟苯基)氨基甲酸酯
芦荟大黄素8-0葡萄糖苷
(2-甲酰基苯并呋喃-5-基)氨基甲酸叔丁酯
2-羧乙基三苯基溴化L
5-[[2-(1-吡咯烷基)乙基]硫基]-2-噻唑胺
1-[5-(2-羟基乙基)硫代]-4-硝基-2-噻吩]乙基-1-酮
2-[3-[(甲巯基)羰基氨基]-1-金刚烷基]乙酸
1-苄基-2-(甲基磺基)-1H-咪唑-5-酰氯盐酸盐
吡啶(2-偶氮-4)间苯二酚
2-甲基-2-丙基(2-氨基-4-氟苯基)氨基甲酸酯