WO2000078149A1 - Anthelmintic compositions - Google Patents
Anthelmintic compositions Download PDFInfo
- Publication number
- WO2000078149A1 WO2000078149A1 PCT/EP2000/005169 EP0005169W WO0078149A1 WO 2000078149 A1 WO2000078149 A1 WO 2000078149A1 EP 0005169 W EP0005169 W EP 0005169W WO 0078149 A1 WO0078149 A1 WO 0078149A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- praziquantel
- sep
- mass
- polyethylene glycol
- composition
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Environmental Sciences (AREA)
- Wood Science & Technology (AREA)
- Plant Pathology (AREA)
- Dentistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
The composition may, for example, include levamisole, salts thereof or other derivatives thereof. Thus, the levamisole may be levamisole either as a base or as a hydrohalogen salt (e. g. the hydrochloride salt) or as a phosphate salt as a supplementary active ingredient. The levamisole may render the composition effective against roundworms as well. Other active ingredients such as niclosamide, and/or closantel, and/or oxyclozanide may also be included. The composition may also include other customary formulating agents. The composition of the present invention may be used as an anthelmintic for veterinary or human use. It may be administered orally or as a liquid in a capsule or in the form of a granulate or tablet made by using the aforementioned solution. The composition is manufactured by mixing the suitable amount of components in an apparatus usually suitable for that purpose. In a preferred embodiment of the invention the composition is administered at a rate of 2.5 mg/kg or above (praziquantel/body means of the person or animal administered to). Preferably it is administered at a rate of 3.75 mg/kg. These dosage rates are particularly suitable for sheep. The invention will now be further illustrated by way of example without thereby limiting the scope of the invention. Example 1 Polyethylene glycol solution of praziquantel 2.5 g praziquantel was added to 100 g polyethylene glycol and dissolved by stirring. In this way a 2.5% praziquantel solution was formed. Example 2 Efficacy evaluation of oral formulations of praziquantel against a confirme natural infestation of Moniezia expansa in lambs. The efficacy of a 2.5% praziquantel solution according to the invention, prepared as described in Example 1 ("The Test Article"), was tested at various dosage rates against a commercially available praziquantel formulation (Cestocur) made up as a suspension ("The Standard") for the control of Moniezia expansa. The Standard was administered at the prescribed dosage rate of 5 mg/kg that is 5 mg praziquantel per kg body mass of the animal. Examination of the ingesta and staining and identification of the Moniezia expansa was done in the laboratory. Dorper lambs of approximately two months of age were utilise during the trial. The lambs were housed in a kraal for the duration of the trial and fed lucerne with water available on tap. The cestocides were tested in naturally infested lambs which was confirmed on the trial premises. Moniezia expansa is readily diagnosed in the live animal. Diagnosis was done using egg morphology and excreted strobilae although these may be digested with corresponding difficulty of identification. The trial was done on the lines of a staggered critical control test. The animals were divided in groups and within each of the groups, and on three consecutive days, some animals were treated with the Test Article (various dosage rates) some with the Standard (prescribed dosage rate of 5 mg/kg) and some were untreated controls ("The Controls") for comparison. The animals involved in each stagger were equipped with faecal collection bags for one day pre-treatment and three days post-treatment. The faeces thus collected were examined for the presence of strobilae. The animals involved in each stagger were slaughtered four days post-treatment following the procedure hereunder: 1. Animals were euthanased, skinned and the abdominal cavity opened. The gastro-intestinal tract was removed and from this the small intestine and caecum/colon was recovered. These were labelled with the animal's number. 2. Intestines were placed in a bucket. Water was added to both ends of the intestine allowing filling at each end to approximately 1-2 meters. 3. The water was allowed to flow through the intestine from both ends until a loop was formed at the bottom end located in the bucket. 4. One end of the intestine was released and the water was forced from the intestine by sliding the organ gently between the fingers. 5. The organ was then opened along its entire length using a pair of bowel scissors after which the wall was thoroughly washed under a stream of water. The intestine was then sealed in a glass jar after the addition of formalin for preservation. This was done in case later examination might be required. 6. Ingesta was recovered, sluiced through an Endecotts sieve and stored in glass jars for examination in the laboratory under direct sunlight in the plastic pans. The results were as follows: EMI5.1 Number <SEP> of <SEP> Animals <SEP> Remedy <SEP> Dose <SEP> Rate* <SEP> Animals <SEP> infested <SEP> at <SEP> Post <SEP> Mortem <SEP> 1 <tb> <SEP> 7 <SEP> Test <SEP> Article <SEP> 1. <SEP> 25 <SEP> mg/kg <SEP> 6 <tb> <SEP> 7 <SEP> Test <SEP> Article <SEP> 1. <SEP> 25 <SEP> mg/kg <SEP> 0 <tb> EMI5.2 <tb> Number <SEP> of <SEP> DoseRate*AnimalsRemedy <SEP> infested <SEP> at <SEP> Post <SEP> Mortem <tb> <SEP> Article3.75mg/kg06Test <SEP> <tb> <SEP> 7 <SEP> Test <SEP> Article <SEP> 5 <SEP> mg/kg <SEP> 0 <tb> <SEP> 9 <SEP> Standard <SEP> 5 <SEP> mg/kg <SEP> 0 <tb> <SEP> 6 <SEP> Control--6 <tb> * The dosage rate is expressed as mg praziquantel per kg body mass of the animal. The results indicate that the Test Article is as effective as the Standard at a dosage rate as low as 2.5 mg/kg compared to the dosage rate of 5 mg/kg of the Standard. A dosage rate of 3.75 mg/kg provides consistent control and is preferred for sheep. It will be appreciated that when customary praziquantel suspensions are prepared, great care has to be taken to ensure that the correct particle size of the praziquantel is obtained. Additives to maintain the suspension and preserve the product are also required which adds to the costs of the product. The present invention does not require such excipients and is self-preserving. The present invention is also much easier to prepare. It will further be appreciated that many variations in details are possible without thereby departing from the scope and spirit of the invention.
Claims
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU55296/00A AU5529600A (en) | 1999-06-18 | 2000-06-06 | Anthelmintic compositions |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ZA99/4045 | 1999-06-18 | ||
ZA994045 | 1999-06-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2000078149A1 true WO2000078149A1 (en) | 2000-12-28 |
Family
ID=25587780
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2000/005169 WO2000078149A1 (en) | 1999-06-18 | 2000-06-06 | Anthelmintic compositions |
Country Status (2)
Country | Link |
---|---|
AU (1) | AU5529600A (en) |
WO (1) | WO2000078149A1 (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001089497A2 (en) * | 2000-05-23 | 2001-11-29 | Bayer Corporation | Praziquantel compositions for treating diseases due to sarcocystis, neospora, toxoplasma and isospora |
DE10331253B4 (en) * | 2003-01-28 | 2007-03-08 | Alpha-Biocare Gmbh | Therapeutics against parasites of fish |
WO2022035674A1 (en) * | 2020-08-12 | 2022-02-17 | Villya LLC | Praziquantel formulations |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0267404A2 (en) * | 1986-10-11 | 1988-05-18 | Bayer Ag | Use of praziquantel for the topical treatment of helminthiasis in cats |
WO1998006407A1 (en) * | 1996-07-30 | 1998-02-19 | Ashmont Holdings Limited | Anthelmintic formulations |
-
2000
- 2000-06-06 AU AU55296/00A patent/AU5529600A/en not_active Abandoned
- 2000-06-06 WO PCT/EP2000/005169 patent/WO2000078149A1/en active Application Filing
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0267404A2 (en) * | 1986-10-11 | 1988-05-18 | Bayer Ag | Use of praziquantel for the topical treatment of helminthiasis in cats |
WO1998006407A1 (en) * | 1996-07-30 | 1998-02-19 | Ashmont Holdings Limited | Anthelmintic formulations |
Non-Patent Citations (2)
Title |
---|
B. SALAFSKY, A. C. FUSCO, L. H. LI, J. MUELLER & B. ELLENBERGER: "Schistosoma mansoni: Experimental chemoprophylaxis in mice using oral anti-penetration agents.", EXPERIMENTAL PARASITOLOGY, vol. 69, no. 3, 1989, pages 263 - 271, XP000918456 * |
G. O. KOKWARO & G. TAYLOR: "Effect of experimentally induced hepatic cirrhosis on the pharmacokinetics of orally administered praziquantel in the rat.", EUR. J. DRUG METAB. PHARMACOKINET., vol. 15, no. 3, 1990, pages 199 - 202, XP000918455 * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001089497A2 (en) * | 2000-05-23 | 2001-11-29 | Bayer Corporation | Praziquantel compositions for treating diseases due to sarcocystis, neospora, toxoplasma and isospora |
WO2001089497A3 (en) * | 2000-05-23 | 2002-11-28 | Bayer Ag | Praziquantel compositions for treating diseases due to sarcocystis, neospora, toxoplasma and isospora |
DE10331253B4 (en) * | 2003-01-28 | 2007-03-08 | Alpha-Biocare Gmbh | Therapeutics against parasites of fish |
WO2022035674A1 (en) * | 2020-08-12 | 2022-02-17 | Villya LLC | Praziquantel formulations |
Also Published As
Publication number | Publication date |
---|---|
AU5529600A (en) | 2001-01-09 |
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