1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol
Penfluridol
CAS: 26864-56-2
Molecular Formula: C28H27ClF5NO
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Names and Identifiers
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Physico-chemical Properties
| Molecular Formula | C28H27ClF5NO |
| Molar Mass | 523.97 |
| Density | 1.2425 (estimate) |
| Melting Point | 105-107°C |
| Boling Point | 587.7±50.0 °C(Predicted) |
| Flash Point | 309.2°C |
| Solubility | H2O: insoluble |
| Vapor Presure | 1.17E-14mmHg at 25°C |
| Appearance | powder |
| Color | white |
| Merck | 14,7087 |
| pKa | 13.49±0.20(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.552 |
| Physical and Chemical Properties | White crystalline powder. |
| Use | Suitable for the treatment of various types of psychosis |
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | TN6957000 |
| HS Code | 29333990 |
| Hazard Class | 6.1 |
| Packing Group | III |
| Toxicity | LD50 orally in mice (day 7): 86.8 mg/kg (Janssen) |
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Standard
Authoritative Data Verified Data
This product is 1-[4, 4-bis (4-fluorophenyl) butyl]-4-[4-chloro-3-(trifluoromethyl) phenyl]-4-piperidinol. Calculated as dried product, containing no less than 99.0% of C28H27C1F5N0.
Last Update：2024-01-02 23:10:35
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is soluble in methanol, ethanol, acetone or chloroform; Almost insoluble in water.
melting point
The melting point of this product (General 0612) is 105~108°C.
Last Update：2022-01-01 11:32:04
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Differential diagnosis
Authoritative Data Verified Data
- take this product, add ethanol to dissolve and dilute to make each lml containing 0. The 1 mg solution, as determined by UV-Vis spectrophotometry (General 0401), has a maximum absorption at wavelengths of NM and nm and a minimum absorption at wavelengths of 240nm and 270nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 41).
Last Update：2022-01-01 11:32:05
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Exam
Authoritative Data Verified Data
fluoride
take 0.40g of this product, add 50ml of water, shake for 5 minutes, filter, take 25ml of filtrate and put it into a 50ml Nessler's colorimetric tube, cool to below 15°C, add 2.0ml of acidic zirconium alizarin solution, dilute to the scale with water, shake well, and place it in the dark for 1 hour below 15°C, and add 0.0022% ml of 4.0 sodium fluoride solution to the control solution (add water to 25ml), operation with the same method) comparison, the color should not be lighter (0.02%).
Related substances
take this product, add mobile phase to dissolve and dilute to make a solution containing about 0.5mg per 1ml as a test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. Test according to high performance liquid chromatography (General 0512). Silica gel was bonded with eighteen alkyl silane as filler; 0.2% triethylamine solution (adjusted to pH 2.5 with phosphoric acid)-methanol (30:70) as mobile phase; The detection wavelength was 219nm. The number of theoretical plates shall not be less than 2000 based on the calculation of the peak of the five fluoride, and the separation degree between the peak of the five fluoride and the adjacent impurity peaks shall meet the requirements. The LOLs of the test solution and the control solution were respectively injected into the human liquid chromatograph, and the chromatogram was recorded to 2 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution.
loss on drying
take this product, dry to constant weight at 80°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Last Update：2022-01-01 11:32:05
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Content determination
Authoritative Data Verified Data
take this product about 0.lg, precision weighing, add ethanol 30ml dissolved, according to the potential titration method (General rule 0701 ) , with hydrochloric acid titration solution (0.025mol/L) the titration was carried out to a pH of 5.1 and the results of the titration were corrected for a blank test. Each 1 ml of hydrochloric acid titration solution (0. 025mol/L) corresponds to 13.10mg of GH27C1F5NO.
Last Update：2022-01-01 11:32:06
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Category
Authoritative Data Verified Data
antipsychotics.
Last Update：2022-01-01 11:32:06
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:32:06
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Pentafluridine tablets
Authoritative Data Verified Data
This product shall contain 90.0% to 110.0% of the labeled amount of pentafluridol (C28H27CIF5NO).
trait
This product is sugar-coated tablet or film-coated tablet, white or almost White after removing the coating.
identification
- a solution containing 0.10mg of pentafluridol per 1 ml was prepared by taking a fine powder of this product and adding ethanol, filtered, and the filtrate showed the same result according to the identification (1) Test under the item of pentafluridol.
- 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
- Related substances take an appropriate amount of this product's fine powder (about 50mg equivalent to pentafluridol), put it in a 100ml measuring flask, add an appropriate amount of mobile phase, shake to dissolve the pentafluridine, dilute it to the scale with the mobile phase, and shake it well, the filtrate was filtered and taken as a test solution; 1 ml was accurately measured, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken to serve as a control solution. If there are impurity peaks in the chromatogram of the test solution, except for the chromatographic peaks whose relative retention time is less than 0.3, the single impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution, and the sum of each impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution. The content uniformity of
- shall be calculated from the content of each tablet measured under the content determination item, and shall comply with the regulations (General rule 0941).
- 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; Methanol-0.2% triethylamine solution (adjusted to pH 2.5 with phosphoric acid)(70: 30) as mobile phase; the detection wavelength was 219nm. The number of theoretical plates shall not be less than 2000 based on the calculation of the peak of the five fluoride, and the separation degree between the peak of the five fluoride and the adjacent impurity peaks shall meet the requirements.
- determination: 10 tablets of this product were placed in the mortar separately, added with an appropriate amount of methanol, ground to dissolve the pentafluridine, transferred to a 100ml measuring flask, and washed with methanol in portions, fully shake, dilute to the scale with methanol, shake, filter, accurately take the appropriate amount of filtrate, dilute with methanol to make a solution containing about 50ug per 1 ml, as a test solution, lOul was injected into the liquid chromatograph accurately, and the chromatogram was recorded. An appropriate amount of the reference substance of pentafluridol was weighed accurately, dissolved with methanol and quantitatively diluted to prepare a solution containing about 50ug per 1 ml, which was determined by the same method. The content of each tablet was calculated by peak area according to external standard method, and the average content of 10 tablets was obtained.
category
Same as pentafluridol.
specification
(l)10mg (2)20mg
storage
sealed storage.
Last Update：2022-01-01 11:32:07
1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-a,a,a-trifluoro-m-tolyl)-4-piperidinol - Reference Information
| NIST chemical information | Information provided by: webbook.nist.gov (external link) |
| Antipsychotic drug | Penfluridol, also known as Semap, is a long-acting antipsychotic drug, which is a type of structure similar to butyrylbenzene The derivatives of diphenylbutylpyridines have strong antipsychotic effects, can block α-adrenergic receptors, and also have antiemetic effects, it is better to control hallucinations, delusions, light membranes, withdrawal and other symptoms. Clinically, it is mainly used for the maintenance treatment of chronic schizophrenia, and can also be used to treat the mental and behavioral disorders of acute schizophrenia and Alzheimer's disease. Fig. 1 is the structural formula |
| Pharmacological action | The effect is similar to that of phenothiazines, with strong antipsychotic effects, antiemetic effects and blocking α-adrenoceptor effects. |
| Pharmacodynamic | This product is a butyryl benzene antipsychotic, the effect is similar to haloperidol, but it has a long-acting effect. Oral absorption by the gastrointestinal tract, 24~72 hours to reach the blood concentration peak, can enter the adipose tissue storage, and then slowly released, and can slowly enter the brain tissue, so the effect is long-lasting, 1 medication can be maintained for 1 week. Most of the original drugs are excreted from the feces, and a small part is excreted from the urine with the metabolite 4,4-bis (p-fluorobenzene) butyric acid. |
| application | is mainly used for the treatment of chronic schizophrenia and maintenance treatment in remission period, with delusional, adolescent and undivided psychosis as well as mental and behavioral disorders of senile dementia. |
| usage and dosage | oral administration, the therapeutic dose range is 20~120mg(1~6 tablets), once a week. It is advisable to start from 10~20mg(0.5~1 tablet) per week and gradually increase by 10~20mg(0.5~1 tablet) per week or two weeks to reduce extrapyramidal reaction. The usual therapeutic dose is 30-60mg(1.5-3 tablets) a week, and the original dose is used to consolidate for 3 months after the symptoms disappear, and the maintenance dose is 10-20mg(0.5-1 tablet) a week. |
| adverse reactions | less side effects, common mild extrapyramidal symptoms. Occasionally, there are transient increases in aminotransferase, leukopenia, rash, convulsions, weakness, dizziness, insomnia, dry mouth, gastrointestinal dysfunction, anxiety, depression and ECG changes. Long-term heavy use can cause tardive dyskinesia. (2016-01-24) |
| precautions | 1. because this product has mild sedative effect and slow effect, it is necessary to take other antipsychotic drugs as appropriate for patients with acute attack, and then use this product alone for maintenance treatment after symptoms are controlled. 2. Liver and kidney damage is prohibited. 3. Elderly patients with tremor paralysis should not be used, and pregnant women should use it with caution. 4. Basal ganglion disease, Parkinson's disease, Parkinson's syndrome, myelosuppression are contraindicated. 5. Liver function and white blood cell count should be checked regularly. |
| drug interaction | 1. this product is combined with other central nervous system inhibitory drugs, and the central inhibitory effect is enhanced. 2. It should not be combined with other antipsychotics to avoid increasing the risk of extrapyramidal reactions. 3. This product is combined with antihypertensive drugs, which has the risk of increasing orthostatic hypotension. |
| drug overdose | 1. the main toxic reactions are myocardial damage and interference with intracardiac conduction, severe arrhythmia, chest tightness, suffocation, etc. 2. Treatment of this product for a long time, excessive poisoning should pay special attention to symptomatic treatment and supportive therapy, no special antidote. |
| Use | Oral long-acting antipsychotics Suitable for various types of psychosis. suitable for the treatment of various types of psychosis |
Last Update：2024-04-10 22:29:15
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