Vermifuge Praziquantel Powder CAS 55268-74-1 ISO 9001 USP 39 Grade with GMP certificate

Pharmacology and toxicology

This product is effective to schistosoma, tapeworm, cysticercosis, clonorchis sinensis, pneumofluke, ginger chip. Can have two kinds of main pharmacological effects to insect body :(1) muscle of insect body produces tonic contraction and produces spastic paralysis. The tension of schistosomiasis increased only 20 seconds after exposure to low praziquantel concentration. When the concentration of praziquantel was more than 1mg/L, the contractures of schistosomiasis were immediately intense. The muscular contraction of the parasite may be related to the loss of intracellular calcium ions due to the increase of membrane permeability of the somatic cells by praziquantel. (2) Cortical damage and host immune function involvement

Fold edit this paragraph praziquantel introduction

Quinone had a rapid and obvious damage to the cortex of the parasite, causing swelling of the outer skin of the syncytium, vacuole, bullae and protrusion of the body surface, and finally erosion of the epidermis, almost all secretion bodies disappeared, and rapid dissolution of the annulus muscle and longitudinal muscle. In the host, external skin vacuolar degeneration was observed 15 minutes after administration. After the destruction of the cortex, the absorption and excretion functions of the parasite are affected. More importantly, the exposure of the body surface antigen makes the parasite vulnerable to the immune attack of the host. A large number of eosinophils attach to the skin lesions and invade, leading to the death of the parasite. In addition, praziquantel can also cause secondary changes, depolarizing the surface membrane of the insect body, significantly reducing the alkaline phosphatase activity of the cortex, resulting in inhibition of glucose uptake and depletion of endogenous glycogen. Praziquantel can also inhibit the synthesis of nucleic acids and proteins.

Fold this section to edit pharmacokinetics

After oral absorption is rapid, more than 80% of the drug can be absorbed from the intestine. The peak value of blood drug reached about 1 hour, and the drug was metabolized quickly after entering the liver, mainly forming hydroxyl metabolites, and only a very small amount of unmetabolized active drug entered the systemic circulation. The concentration in portal venous blood can be 10 times higher than that in peripheral venous blood. The concentration of cerebrospinal fluid is about 15%~20% of the concentration of blood drugs. After lactation patients take medicine, the concentration of drugs in their milk is equivalent to 25% in serum. After oral administration of 10~15mg/kg, the peak blood drug was about 1mg/L. Drugs are mainly distributed in liver, followed by kidney, lung, pancreas, adrenal gland, pituitary gland, salivary gland, etc., rarely through the placenta, no organ-specific accumulation phenomenon. T1/2 was 0.8~1.5 hours, and t1/2 of its metabolites was 4~5 hours. It is excreted mainly by the kidneys in the form of metabolites, 72% within 24 hours and 80% within 4 days.

Fold edit this section for indication

It is a broad - spectrum anti - fluke and tapeworm drug. It is suitable for various schistosomiasis, clonorchiasis, paragonimiasis, zingiasis, taeniasis and cysticercosis.

Fold edit this paragraph pharmacological action

This article mainly through the 5 - HT sample function to the host for the schistosomiasis, tapeworm spastic paralysis, for most tapeworm imago and immature insect body has good effect, also can affect the insect body muscle intracellular calcium ion permeability, increase the calcium ion internal flow, inhibiting the reuptake of sarcoplasmic reticulum calcium pump, insect body muscle intracellular calcium ion content increased, the insect body paralysis from falling out.

Fold edit this section for laboratory determination

Method name: Praziquantel tablets - praziquantel - high performance liquid chromatography

Application: This method uses high performance liquid chromatography to determine the content of praziquantel in praziquantel tablets.

This method is suitable for praziquantel tablets.

Method principle: the sample was refined, dissolved in internal standard solution, diluted with methanol, and then entered HPLC for chromatographic separation. Ultraviolet absorption detector was used to detect the peak area of praziquantel at wave length of 263nm, and its content was calculated.

Reagent: 1. Methanol

2. α -asaryl ethe

Equipment: 1. Equipment

1.1 High performance liquid chromatograph

1.2 the chromatographic column

Octadecylsilane bonded silica gel was used as filler

1.3 Ultraviolet absorption detector

2. Chromatographic conditions

2.1 Mobile phase: methanol water =100 40

2.2 Detection wavelength: 263nm

2.3 Column temperature: room temperature

Sample preparation: 1. Preparation of internal standard solution

Accurately weighing a proper amount of α -asaryl ethe, adding methanol to dissolve and dilute into a solution containing 0.4mg per 1mL, that is, the internal standard solution.

2. Preparation of reference solution

Weigh praziquantel reference about 100mg, place it in a 10mL flask, add 5mL internal standard solution, shake it to dissolve, dilute it with methanol to scale, shake it well, and the solution is the reference solution.

3. Preparation of test solution

Take 20 pieces of the test product, weigh and finely, weigh an appropriate amount (approximately equivalent to praziquantel 100mg), place them in a 10mL measuring bottle, add 5mL of internal standard solution precisely, shake to dissolve, dilute to scale with methanol, shake well, that is, the test product solution.

Note: "Precise weighing" means that the weight taken should be accurate to one thousandth of the weight taken. "Precision measurement" means that the accuracy of volume measurement shall conform to the accuracy requirements of the volume pipette specified in the national standard.

Operation steps: 10mL of reference solution and 10mL of test solution were accurately absorbed and injected into HPLC. The peak area of praziquantel (C19H24N2O2) was determined by uv absorption detector at the wavelength of 263nm, and its content was calculated.

References: Pharmacopoeia of the People's Republic of China, National Pharmacopoeia Committee (Ed.), Chemical Industry Press, 2005, part 2, p.251.

Fold edit the usage of this paragraph

Folding treatment of succuliasis

① schistosomiasis: all kinds of chronic schistosomiasis with a total dose of 60mg/kg 1 to 2 days of therapy, a daily dose of 2 to 3 times between meals. The total dose of acute schistosomiasis was 120mg/kg, taken 2~3 times a day for 4 days. Body weight over 60kg is calculated as 60kg. ② clonorchiasis: the total dose was 210mg/kg, 3 times a day for 3 days. ③ Paragonimiasis: 25mg/kg, 3 times a day, for 3 days. ④ Rhizopiosis of ginger: 15mg/kg, one dose.

Treatment of taeniasis by folding

Beef and pork tapeworm disease: 10mg/kg, morning meal, 1 hour after taking magnesium sulfate. (2) Hymenococcus pumilis and diphyllobothriasis latinosus: 25mg/kg, oral dose. (3) the total dose of cysticercosis 120~180mg/kg, divided into 3~5 days, 2~3 times a day.

Fold edit this section for adverse reactions

① Common side effects are dizziness, headache, nausea, abdominal pain, diarrhea, fatigue, limb pain, etc., generally mild, short duration, does not affect the treatment, do not need to deal with. (2) PALpitations, chest tightness and other symptoms were found in a few cases. Ecg showed T wave changes and external contraction, and supraventricular tachycardia and atrial fibrillation were occasionally seen. ③ Temporary elevation of transaminase may occur in a few cases. ④ Occasionally induce mental disorders or gastrointestinal bleeding.