Praziquantel Formulations

Abstract

Praziquantel may be formulated to enhance its pharmacokinetic, toxicity, and palatability properties. It can be stored and/or dispensed as a liquid, powder, or tablet. Reduction in the most common side effects improves patient compliance and satisfaction. Altered taste profile improves patient compliance and satisfaction. Once formulated it can be used to treat a variety of blood flukes and worms in human and veterinary subjects.

1 . A liquid pharmaceutical formulation in a vehicle consisting of an aqueous vehicle, said formulation comprising:
 (a) polyethylene glycol (PEG);   (b) rubusoside; and   (c) praziquantel.   
     
     
         2 . The liquid pharmaceutical formulation of  claim 1  wherein the PEG is polydisperse. 
     
     
         3 . The liquid pharmaceutical formulation of  claim 1  wherein the PEG has an average molecular weight of 2000-6000. 
     
     
         4 . The liquid pharmaceutical formulation of  claim 1  wherein the PEG is PEG 3350. 
     
     
         5 . The liquid pharmaceutical formulation of  claim 1  wherein the weight ratio of PEG to praziquantel is between 5:1 and 10:1. 
     
     
         6 . The liquid pharmaceutical formulation of  claim 1  wherein the weight ratio of rubusoside to praziquantel in the liquid pharmaceutical formulation is between 2:1 and 10:1. 
     
     
         7 . A method of treating an infection by a blood fluke or tapeworm in a patient, comprising:
 administering the liquid pharmaceutical formulation of  claim 1  to the patient.   
     
     
         8 . The method of  claim 7  wherein the patient is a human. 
     
     
         9 . The method of  claim 7  wherein the patient is a veterinary patient. 
     
     
         10 . The method of  claim 7  wherein the infection is schistosomiasis. 
     
     
         11 . The method of  claim 7  wherein the blood fluke is  Clonorchis sinensis.    
     
     
         12 . The method of  claim 7  wherein the blood fluke is  Opisthorchis viverrini.    
     
     
         13 . The method of  claim 7  wherein the blood fluke is  Opisthorchis felineus.    
     
     
         14 . The method of  claim 7  wherein the tapeworm is  Taenia saginata.    
     
     
         15 . The method of  claim 7  wherein the tapeworm is  Taenia solium.    
     
     
         16 . The method of  claim 7  wherein the tapeworm is  Taenia asiatica.    
     
     
         17 . The method of  claim 7  wherein the infection is Echinococcosis. 
     
     
         18 . The method of  claim 7  wherein the patient is selected from the group consisting of a horse, dog, cat, poultry, and ruminant. 
     
     
         19 . The method of  claim 7  wherein the dose of praziquantel is between 10 and 40 mg per kg of patient weight. 
     
     
         20 . The method of  claim 7  wherein the patient is human and is administered 3 doses daily of between 10 and 40 mg per kg of patient weight. 
     
     
         21 . The method of  claim 7  wherein the dose of praziquantel is between 10 and 40 mg per kg of patient weight. 
     
     
         22 . The method of  claim 7  wherein the patient is human and is administered 3 doses daily of between 10 and 40 mg per kg of patient weight. 
     
     
         23 . A powdered formulation of praziquantel and a vehicle consisting of an aqueous vehicle for reconstitution of said powdered formulation and subsequent administration to a patient as an aqueous liquid formulation, said powdered formulation comprising:
 (a) polyethylene glycol (PEG);   (b) rubusoside; and   (c) praziquantel.   
     
     
         24 . The powdered formulation of  claim 23  wherein the PEG is polydisperse. 
     
     
         25 . The powdered formulation of  claim 23  wherein the PEG has an average molecular weight of 2000-6000. 
     
     
         26 . The powdered formulation of  claim 23  wherein the PEG is PEG 3350. 
     
     
         27 . The powdered formulation of  claim 23  wherein the weight ratio of PEG to praziquantel is between 5:1 and 10:1. 
     
     
         28 . The powdered formulation of  claim 23  wherein the weight ratio of rubusoside to praziquantel in the powdered formulation is between 2:1 and 10:1. 
     
     
         29 . (canceled) 
     
     
         30 . (canceled) 
     
     
         31 . The liquid pharmaceutical formulation of  claim 1  which consists of the aqueous vehicle and:
 (a) polyethylene glycol (PEG); 
 (b) rubusoside; and 
 (c) praziquantel. 
 
     
     
         32 . The powdered formulation and the vehicle of  claim 23  wherein the powdered formulation consists of:
 (a) polyethylene glycol (PEG); 
 (b) rubusoside; and 
 (c) praziquantel. 
 
     
     
         33 . The liquid pharmaceutical formulation of  claim 1  which contains one or more components selected from the group consisting of: buffered aqueous solution, an aqueous beverage, croscarmellose sodium, povidone, brilliant blue FCF, and a flavor enhancer. 
     
     
         34 . The liquid pharmaceutical formulation of  claim 1  which consists of the aqueous vehicle and
 (a) polyethylene glycol (PEG); 
 (b) rubusoside; and 
 (c) praziquantel, and optionally one or more components selected from the group consisting of buffered aqueous solution, an aqueous beverage, croscarmellose sodium, povidone, brilliant blue FCF, and a flavor enhancer. 
 
     
     
         35 . The powdered formulation and the vehicle of  claim 23  wherein the powdered formulation consists of:
 (a) polyethylene glycol (PEG); 
 (b) rubsoside; and 
 (c) praziquantel; and optionally one or more components selected from the group consisting of: croscarmellose sodium, povidone, brilliant blue FCF, and a flavor enhancer. 
 
     
     
         36 . A method of formulating a powdered formulation of praziquantel for administration to a patient as an aqueous liquid formulation, said method comprising mixing a powdered formulation comprising:
 (a) polyethylene glycol (PEG);   (b) rubusoside; and   (c) praziquantel;   
       with a vehicle consisting of an aqueous vehicle.