Praziquantel for system suitability
praziquantel
CAS: 55268-74-1
Molecular Formula: C19H24N2O2
Praziquantel for system suitability - Names and Identifiers
Praziquantel for system suitability - Physico-chemical Properties
| Molecular Formula | C19H24N2O2 |
| Molar Mass | 312.41 |
| Density | 1.1209 (rough estimate) |
| Melting Point | 136-138 C |
| Boling Point | 1377℃ |
| Flash Point | >110°(230°F) |
| Water Solubility | Freely soluble in ethanol or dichloromethane. Slightly soluble in water |
| Solubility | Easily soluble in dimethyl sulfoxide, insoluble in ether. |
| Appearance | White or almost white crystalline powder |
| Color | Crystals from EtOAc/hexane |
| Merck | 13,7802 |
| BRN | 761557 |
| pKa | -0.98±0.20(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Sensitive | Easily absorbing moisture |
| Refractive Index | 1.5600 (estimate) |
| MDL | MFCD00058531 |
| Physical and Chemical Properties | White or off-white crystalline powder, odorless, slightly bitter, hygroscopic. Solubility (g/100 ml): ethanol 9.7, chloroform 56.7, water 0.04. Soluble in dimethyl sulfoxide, insoluble in ether. The melting point was 136-141 °c. Acute toxicity LD50 mice and rats (mg/kg):2000~3000 oral,>3000 subcutaneous injection. |
| Use | Anti-helminth drugs, mainly used for schistosomiasis, can also be used for schistosomiasis, Taeniasis, Paragonimiasis, cysticercosis and so on |
Praziquantel for system suitability - Risk and Safety
| Risk Codes | R11 - Highly Flammable R34 - Causes burns |
| Safety Description | S16 - Keep away from sources of ignition. 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.) S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 1 |
| RTECS | UQ4150000 |
| HS Code | 29339900 |
| Toxicity | LD50 in mice, rats (mg/kg): 2000-3000 orally; >3000 s.c. (Muermann) |
Praziquantel for system suitability - Nature
Open Data Verified Data
white or off-white crystalline powder, odorless, slightly bitter, hygroscopic. mp 136~138 ℃. Solubility (g/lOOmL): ethanol 9.7, chloroform 56.7, water 0.04. Soluble in dimethyl sulfoxide, insoluble in ether.
Last Update：2024-01-02 23:10:35
Praziquantel for system suitability - Preparation Method
Open Data Verified Data
using phenylethylamine as raw material, after acylation with Chloroacetyl Chloride, and then using potassium benzyldimethylamide for amination reaction to introduce amino group, under the action of phosphorus oxychloride, 3, 4-dihydroisoquinoline derivatives were obtained, by hydrogenation, hydrolysis of 1 ammonia methyl tetrahydroquinoline, successively with cyclohexanoyl chloride and Chloroacetyl Chloride acylation, finally get praziquantel. Alternatively, using isoquinoline as a raw material, the reaction is Reissem, the introduction of cyano and nitrogen in the l position is benzoylated, and then hydrogenated, and the benzoyl group is transferred to the amino group of the side chain, A Chloroacetyl group is then introduced at the amino group on the ring. Praziquantel was obtained by cyclization, hydrolysis, and cyclohexylformylation.
Last Update：2022-01-01 09:09:50
Praziquantel for system suitability - Standard
Authoritative Data Verified Data
This product is 2-(cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-4h-pyrazino [2,l-a] isoquinolin-4-one. The content of C19H24N202 shall be 98.0% ~ 102.0% calculated as dry product.
Last Update：2024-01-02 23:10:35
Praziquantel for system suitability - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder.
- This product is soluble in chloroform, soluble in ethanol, insoluble in ether or water.
melting point
The melting point of this product (General 0612) is 136 ~ 14rC.
Last Update：2022-01-01 11:57:00
Praziquantel for system suitability - Introduction
Soluble in chloroform, dimethyl sulfoxide, soluble in ethanol, insoluble in water, insoluble in ether. It tastes bitter.
Last Update：2022-10-16 17:26:17
Praziquantel for system suitability - Use
Open Data Verified Data
This product is a new broad-spectrum antiparasitic drug. It is effective for schistosomiasis japonica, Taeniasis, clonorchiasis, Paragonimiasis, etc. Since the product also has efficacy in killing cercariae and miracidia, it is also used to prevent schistosome infection. There is also the treatment of cerebral cysticercosis with this product. Broad-spectrum antiparasitic pain medication. It is used for the treatment and prevention of schistosomiasis, cysticercosis, Paragonimiasis, echinococcosis, gingerosis, echinococcosis and helminth infection. It is effective for schistosomiasis japonica, Taeniasis, clonorchiasis, Paragonimiasis, etc. Since the product also has efficacy in killing cercariae and miracidia, it is also used to prevent schistosome infection.
Last Update：2022-01-01 09:09:50
Praziquantel for system suitability - Differential diagnosis
Authoritative Data Verified Data
- take this product and add ethanol to make a solution containing mg per 1 ml, and measure it by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at a wavelength of 264nm and 272nm.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 190).
Last Update：2022-01-01 11:57:01
Praziquantel for system suitability - Safety
Open Data Verified Data
LDso( mg/kg) in mice and rats: 2000-3000 by mouth,>3000 by subcutaneous injection.
Last Update：2022-01-01 09:09:51
Praziquantel for system suitability - Exam
Authoritative Data Verified Data
acidity
take 0.50g of this product, add neutral ethanol (neutral to methyl red indicator solution) 15ml to dissolve, add 1 drop of Methyl red indicator solution and O.Olmol/L sodium hydroxide solution 0.10, should be yellow.
Related substances
Take 20mg of this product, put it in a 100ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake well, and use it as a test solution, A solution containing 2ug per 1 ml was prepared as a control solution by quantitative dilution with mobile phase. According to the chromatographic condition test under the content determination item, take the control solution and the test solution with 20 u1 respectively, and inject the human liquid chromatograph respectively, the chromatogram was recorded to 4 times 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 the main peak area of the control solution (1.0%).
loss on drying
take this product, dry to constant weight at 105°C, weight loss 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
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 11:57:01
Praziquantel for system suitability - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with eighteen alkyl silane was used as a filler; Acetonitrile-water (60:40) was used as a mobile phase; And the detection wavelength was 210mn. The number of theoretical plates is not less than 3000 based on the praziquantel peak.
assay
take about 50mg of this product, weigh it accurately, put it in a 100ml measuring flask, add an appropriate amount of mobile phase, shake it to dissolve it, dilute it with mobile phase to the scale, and shake it well. 5ml was accurately weighed, placed in a 50ml measuring flask, diluted to scale with mobile phase, and shaken. 20u1 was injected into the liquid chromatograph, and the chromatogram was recorded. According to the external standard method to calculate the peak area, that is, get
Last Update：2022-01-01 11:57:02
Praziquantel for system suitability - Category
Authoritative Data Verified Data
anthelmintic drug.
Last Update：2022-01-01 11:57:02
Praziquantel for system suitability - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:57:02
Praziquantel for system suitability - Praziquantel tablets
Authoritative Data Verified Data
This product contains praziquantel (C19H24N202) should be 93.0%-107.0% of the label.
trait
This product is white tablet.
identification
take an appropriate amount of fine powder of this product (about 10mg of praziquantel), add 20ml of ethanol, shake to dissolve praziquantel, filter, and take the filtrate, absorption maxima were determined by UV-Vis spectrophotometry (General 0401) at wavelengths of NM and Nm.
examination
- dissolution dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.2% of hydrochloric acid solution containing sodium dodecyl sulfate (9-1000) as the dissolution medium, speed of 50 revolutions per minute, according to the law, after 60 minutes, take the solution filtration, take the filtrate (0.2g specifications) or dilute the filtrate with dissolution medium to a solution containing about 0401 mg per 1 mL (G specification), and measure the absorbance at the wavelength of 263mn by UV-Vis spectrophotometry (general rule); in addition, an appropriate amount of praziquantel reference substance is accurately weighed and diluted quantitatively with dissolution medium to make a solution containing about 0.2 mg per 1 ml. The absorbance is measured by the same method to calculate the dissolution amount of each tablet. 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
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about 50mg equivalent to praziquantel), put it in a 100ml measuring flask, add mobile phase and shake to dissolve bquinone, dilute to the scale with mobile phase, shake, filter, and take the filtrate, according to the method under the content determination of pioglitazone, since the "precision measurement of 5ml", according to the law, that is obtained.
category
Same as praziquantel.
specification
(1)0.2g (2)0.6g
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:57:03
Praziquantel for system suitability - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| insecticide | praziquantel (praziquantel) is a broad-spectrum anthelmintic synthetic drug discovered abroad in the 70s. after it was reported to be effective against schistosomiasis in 1977, it was trial-produced in China in the same year and proved to have remarkable curative effect on schistosomiasis japonica. this product is colorless crystalline powder, odorless and slightly bitter, and stable under normal conditions. Soluble in chloroform, dimethyl sulfoxide and other organic solvents, slightly soluble in ethanol, insoluble in water. Histochemical observations of in vivo and in vitro tests showed that after the action of the drug, the glycogen of the schistosomiasis was significantly reduced, ribonucleic acid and alkaline phosphatase also decreased, and the activity of alkaline protein reaction or acid phosphatase increased. |
| mechanism of action | praziquantel has a significant effect on killing schistosome adults. Its insecticidal mechanism, from the molecular level, is that praziquantel quickly destroys the Ca2 balance in the insect body. On the one hand, it causes the activity of the worm body to be excited and muscle contracture, so that the schistosomiasis parasitic in the portal system cannot be adsorbed on the blood vessel wall and is brought into the blood stream. The liver (liver migration) is damaged; the second is that the syncytial cortex of schistosomiasis is damaged, in addition to affecting the absorption, excretion and secretion functions of the worm, in addition to the disorder of sugar metabolism and enzyme system, the body surface antigenic determinants of the insect are exposed, and the host's immune system is recognized, attracting a large number of inflammatory cells such as neutrophils, eosinophils, macrophages and other aggregates around the insect body to attack. |
| side effects | common side effects of praziquantel are as follows: 1. dizziness, headache, nausea, abdominal pain, diarrhea, fatigue, limb soreness, etc. may occur 1 hour after the first medication, generally mild, short duration, does not affect treatment, and does not need treatment. 2. A few cases have symptoms such as palpitations and chest tightness. The electrocardiogram shows T wave changes and extrasystoles, and occasionally supraventricular tachycardia and atrial fibrillation. 3. A few cases may have transient transaminase elevation, toxic hepatitis, etc. 4, occasionally can induce mental disorders or gastrointestinal bleeding. 5. Brain hernia, allergic reactions (rash, asthma), etc. are also seen. |
| pharmacokinetics | praziquantel is a commonly used drug for the treatment of schistosomiasis. it is extremely toxic to animals and is rapidly absorbed in the digestive tract after oral administration. Peak blood drug time: 5 minutes for mice, l5 ~ 30 minutes for rats, 30~120 minutes for dogs and about 2 hours for sheep. After absorption, the drug is widely distributed in all tissues and organs, and can even penetrate the blood-brain barrier of rats, and can enter the bile of dogs, which can promote the influx of Ca2 outside the cell membrane of the schistosome muscle, causing muscle contracture and losing absorption The ability of parasitic parts. At the same time, it causes disorders of sugar metabolism and energy metabolism, the "accompanying immunity" state is destroyed, and then passes through the host immune system, and finally eliminates the worm body, which is effective against Schistosoma sinensis, tapeworm, paragonimiasis, cysticercosis and immature worms (cercaridia, miracidia) have a good killing effect. |
| use | praziquantel is a broad-spectrum anti-parasitic drug that is effective against Schistosoma japonicum, Schistosoma mansoni and Schistosoma japonicum, Clonorchis sinensis, Paragonimus, ginger, tapeworm and cysticercus. In particular, it has a strong killing effect on tapeworms and is currently the best one of schistosomiasis drugs. |
| Production method | Using phenethylamine as raw material, acylation with chloroacetyl chloride, and then amination reaction with phenyldicarboxamide potassium to introduce the amino group, Under the action of phosphorus oxychloride, 3,4-dihydroisoquinoline derivatives are cyclosynthesized, and 1-aminomethyl tetrahydroquinoline is obtained by hydrogenation and hydrolysis, and cyclohexanoyl chloride and chloroacetyl chloride are successively acylated, finally dehydrochlorination cyclization to obtain praziquantel. You can also use isoquinoline as a raw material. After a Reissert reaction, the cyano group and nitrogen are introduced at the l position for benzoylation, and then hydrogenated. At the same time, the benzoyl group is transferred to the amino group of the side chain, and then the amino group on the ring is introduced. Chloroacetyl group, and then cyclization, hydrolysis, cyclohexanoylation to obtain praziquantel. There are many synthetic routes in industrial production: isoquinoline route, piperazine route and phenethylamine route, of which quinoline route is better. The addition of isoquinoline with benzoyl chloride and potassium cyanide, catalytic hydrogenation, rearrangement to obtain 1-benzoylaminomethyl-1, 2,3, 4-tetrahydroisoquinoline, and then chloroacetylation and cyclization, Pressure hydrolysis, cyclohexylation to obtain praziquantel. |
| toxicity classification | poisoning |
| acute toxicity | oral-rat LD50; 2840 mg/kg; Oral-mouse LD50: 2454 mg/kg |
| flammability hazard characteristics | combustible; combustion produces toxic nitrogen oxide smoke |
| storage and transportation characteristics | ventilation and low temperature drying |
| fire extinguishing agent | dry powder, foam, sand, carbon dioxide, mist water |
Last Update：2024-04-09 02:00:09
Supplier List
Product Name: praziquantel Request for quotation
CAS: 55268-74-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 55268-74-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Praziquantel Visit Supplier Webpage Request for quotationCAS: 55268-74-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: praziquantel Request for quotation
CAS: 55268-74-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 55268-74-1
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Praziquantel Visit Supplier Webpage Request for quotationCAS: 55268-74-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History