WO2023283671A1 - Oral antibiotic formulation - Google Patents
Oral antibiotic formulation Download PDFInfo
- Publication number
- WO2023283671A1 WO2023283671A1 PCT/AU2022/050519 AU2022050519W WO2023283671A1 WO 2023283671 A1 WO2023283671 A1 WO 2023283671A1 AU 2022050519 W AU2022050519 W AU 2022050519W WO 2023283671 A1 WO2023283671 A1 WO 2023283671A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- antibiotic
- antibiotic formulation
- formulation
- animal
- administering
- Prior art date
Links
- 238000009472 formulation Methods 0.000 title claims abstract description 199
- 239000000203 mixture Substances 0.000 title claims abstract description 199
- 229940127249 oral antibiotic Drugs 0.000 title description 2
- 230000003115 biocidal effect Effects 0.000 claims abstract description 214
- 241001465754 Metazoa Species 0.000 claims abstract description 116
- 239000007788 liquid Substances 0.000 claims abstract description 72
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims abstract description 47
- 239000002132 β-lactam antibiotic Substances 0.000 claims abstract description 47
- 229940124586 β-lactam antibiotics Drugs 0.000 claims abstract description 47
- 230000037396 body weight Effects 0.000 claims description 24
- 239000000796 flavoring agent Substances 0.000 claims description 22
- 235000013355 food flavoring agent Nutrition 0.000 claims description 22
- 239000003242 anti bacterial agent Substances 0.000 claims description 19
- ZAIPMKNFIOOWCQ-UEKVPHQBSA-N cephalexin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=CC=C1 ZAIPMKNFIOOWCQ-UEKVPHQBSA-N 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 16
- 229940106164 cephalexin Drugs 0.000 claims description 15
- 229930186147 Cephalosporin Natural products 0.000 claims description 8
- 229940124587 cephalosporin Drugs 0.000 claims description 8
- 150000001780 cephalosporins Chemical class 0.000 claims description 8
- XIURVHNZVLADCM-IUODEOHRSA-N cefalotin Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC(=O)C)C(O)=O)C(=O)CC1=CC=CS1 XIURVHNZVLADCM-IUODEOHRSA-N 0.000 claims description 6
- RDLPVSKMFDYCOR-UEKVPHQBSA-N cephradine Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CCC=CC1 RDLPVSKMFDYCOR-UEKVPHQBSA-N 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 5
- FMZXNVLFJHCSAF-DNVCBOLYSA-N (6R,7R)-3-[(4-carbamoyl-1-pyridin-1-iumyl)methyl]-8-oxo-7-[(1-oxo-2-thiophen-2-ylethyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound C1=CC(C(=O)N)=CC=[N+]1CC1=C(C([O-])=O)N2C(=O)[C@@H](NC(=O)CC=3SC=CC=3)[C@H]2SC1 FMZXNVLFJHCSAF-DNVCBOLYSA-N 0.000 claims description 4
- UQLLWWBDSUHNEB-CZUORRHYSA-N Cefaprin Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC(=O)C)C(O)=O)C(=O)CSC1=CC=NC=C1 UQLLWWBDSUHNEB-CZUORRHYSA-N 0.000 claims description 4
- JFPVXVDWJQMJEE-QMTHXVAHSA-N Cefuroxime Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)C(=NOC)C1=CC=CO1 JFPVXVDWJQMJEE-QMTHXVAHSA-N 0.000 claims description 4
- 229960003972 cefacetrile Drugs 0.000 claims description 4
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- 229960004841 cefadroxil Drugs 0.000 claims description 4
- NBFNMSULHIODTC-CYJZLJNKSA-N cefadroxil monohydrate Chemical compound O.C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=C(O)C=C1 NBFNMSULHIODTC-CYJZLJNKSA-N 0.000 claims description 4
- FUBBGQLTSCSAON-PBFPGSCMSA-N cefaloglycin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)COC(=O)C)C(O)=O)=CC=CC=C1 FUBBGQLTSCSAON-PBFPGSCMSA-N 0.000 claims description 4
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- MLYYVTUWGNIJIB-BXKDBHETSA-N cefazolin Chemical compound S1C(C)=NN=C1SCC1=C(C(O)=O)N2C(=O)[C@@H](NC(=O)CN3N=NN=C3)[C@H]2SC1 MLYYVTUWGNIJIB-BXKDBHETSA-N 0.000 claims description 4
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- CZTQZXZIADLWOZ-CRAIPNDOSA-N cefaloridine Chemical compound O=C([C@@H](NC(=O)CC=1SC=CC=1)[C@H]1SC2)N1C(C(=O)[O-])=C2C[N+]1=CC=CC=C1 CZTQZXZIADLWOZ-CRAIPNDOSA-N 0.000 claims description 2
- 229960002420 cefatrizine Drugs 0.000 claims description 2
- UOCJDOLVGGIYIQ-PBFPGSCMSA-N cefatrizine Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)[C@H](N)C=2C=CC(O)=CC=2)CC=1CSC=1C=NNN=1 UOCJDOLVGGIYIQ-PBFPGSCMSA-N 0.000 claims description 2
- HGXLJRWXCXSEJO-GMSGAONNSA-N cefazaflur Chemical compound CN1N=NN=C1SCC1=C(C(O)=O)N2C(=O)[C@@H](NC(=O)CSC(F)(F)F)[C@H]2SC1 HGXLJRWXCXSEJO-GMSGAONNSA-N 0.000 claims description 2
- 229950004359 cefazaflur Drugs 0.000 claims description 2
- 229960005312 cefazedone Drugs 0.000 claims description 2
- VTLCNEGVSVJLDN-MLGOLLRUSA-N cefazedone Chemical compound S1C(C)=NN=C1SCC1=C(C(O)=O)N2C(=O)[C@@H](NC(=O)CN3C=C(Cl)C(=O)C(Cl)=C3)[C@H]2SC1 VTLCNEGVSVJLDN-MLGOLLRUSA-N 0.000 claims description 2
- FLKYBGKDCCEQQM-WYUVZMMLSA-M cefazolin sodium Chemical compound [Na+].S1C(C)=NN=C1SCC1=C(C([O-])=O)N2C(=O)[C@@H](NC(=O)CN3N=NN=C3)[C@H]2SC1 FLKYBGKDCCEQQM-WYUVZMMLSA-M 0.000 claims description 2
- 229960003844 cefroxadine Drugs 0.000 claims description 2
- RDMOROXKXONCAL-UEKVPHQBSA-N cefroxadine Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)OC)C(O)=O)=CCC=CC1 RDMOROXKXONCAL-UEKVPHQBSA-N 0.000 claims description 2
- 229960004366 ceftezole Drugs 0.000 claims description 2
- DZMVCVMFETWNIU-LDYMZIIASA-N ceftezole Chemical compound O=C([C@@H](NC(=O)CN1N=NN=C1)[C@H]1SC2)N1C(C(=O)O)=C2CSC1=NN=CS1 DZMVCVMFETWNIU-LDYMZIIASA-N 0.000 claims description 2
- 229940099739 duricef Drugs 0.000 claims description 2
- 239000008157 edible vegetable oil Substances 0.000 claims description 2
- 229940041010 fourth-generation cephalosporins Drugs 0.000 claims description 2
- 235000011389 fruit/vegetable juice Nutrition 0.000 claims description 2
- 229940090589 keflex Drugs 0.000 claims description 2
- 239000008267 milk Substances 0.000 claims description 2
- 235000013336 milk Nutrition 0.000 claims description 2
- 210000004080 milk Anatomy 0.000 claims description 2
- 229940041009 monobactams Drugs 0.000 claims description 2
- WSHJJCPTKWSMRR-RXMQYKEDSA-N penam Chemical compound S1CCN2C(=O)C[C@H]21 WSHJJCPTKWSMRR-RXMQYKEDSA-N 0.000 claims description 2
- 150000002959 penams Chemical class 0.000 claims description 2
- 150000002961 penems Chemical class 0.000 claims description 2
- 229940041008 second-generation cephalosporins Drugs 0.000 claims description 2
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- 229940049588 velosef Drugs 0.000 claims description 2
- 229940088710 antibiotic agent Drugs 0.000 description 11
- 208000035143 Bacterial infection Diseases 0.000 description 8
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- 238000002347 injection Methods 0.000 description 8
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- 210000002421 cell wall Anatomy 0.000 description 6
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- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 description 1
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- 229930193140 Neomycin Natural products 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- 108010013639 Peptidoglycan Proteins 0.000 description 1
- 206010066901 Treatment failure Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
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- 229940126575 aminoglycoside Drugs 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61D—VETERINARY INSTRUMENTS, IMPLEMENTS, TOOLS, OR METHODS
- A61D7/00—Devices or methods for introducing solid, liquid, or gaseous remedies or other materials into or onto the bodies of animals
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
- A61J1/05—Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids ; Infusion or perfusion containers
- A61J1/06—Ampoules or carpules
- A61J1/067—Flexible ampoules, the contents of which are expelled by squeezing
Definitions
- the present invention relates to an antibiotic formulation and method of administering the antibiotic formulation.
- the present invention relates, but is not limited, to an orally administered antibiotic formulation for animals including cats and dogs.
- Reference to the orally administered antibiotic formulation for cats and dogs is provided by way of example but the invention is not limited to this use.
- veterinary antibiotics is administered either by injection or orally to an animal.
- Oral administration is typically in the form of a tablet.
- Antibiotics generally have a bitter taste and therefore the antibiotic tablet may be rejected by the animal when administered orally. Although it may be possible to mask the bitter taste by mixing the tablet into food, the animal may still reject the antibiotic tablet.
- the present invention broadly resides in an orally administered antibiotic formulation for treating an animal including at least one beta-lactam antibiotic in a form that is suitable for mixing with a liquid.
- the at least one beta-lactam antibiotic includes but not limited to one or more of the following: penams, carbapenams, clavams, penems, carbapenems, cephems, carbacephems, oxacephems and monobactams.
- the cephems includes but is not limited to one or more of cephalosporins and cephamycins.
- the cephalosporins includes but is not limited to one or more of first-generation cephalosporins, second-generation cephalosporins, third- generation cephalosporins, fourth-generation cephalosporins and fifth-generation cephalosporins.
- the first-generation cephalosporins includes but is not limited to one or more of cefacetrile (or cephacetrile), cefadroxil (or cefadroxil, Duricef), cephalexin (or cefalexin, Keflex), cefaloglycin (or cephaloglycin), cefalonium (or cephalonium), cefaloridine (or cephaloradine), cefalotin (or cephalothin, Keflin), cefapirin (or cephapirin, cefadryl), cefatrizine, cefazaflur, cefazedone, cefazolin (or cephazolin, Ancef, Kefzol), cefradine (or cephradine, Velosef), cefroxadine and ceftezole.
- the at least one beta-lactam antibiotic is cephalexin.
- the antibiotic formulation contains 1 to 20% of beta-lactam antibiotic, more preferably contains 13 to 17% of beta-lactam antibiotic.
- the antibiotic formulation contains substantially 15% of beta-lactam antibiotic.
- the antibiotic formulation contains 10 to 200 mg/g of beta-lactam antibiotic, more preferably contains 130 to 170 mg/g of beta-lactam antibiotic.
- the antibiotic formulation contains substantially 150 mg/g of beta-lactam antibiotic.
- the antibiotic formulation is in dry granular from. In another embodiment, the antibiotic formulation is in dry powder form. In another embodiment, the antibiotic formulation is in a dry pellet form.
- the antibiotic formulation is reconstituted in a liquid before administering to the animal.
- the liquid is suitable for oral administration.
- the liquid is water.
- the liquid is milk, juice or edible oil.
- the reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic between 1 to 20 %w/v, more preferably between 5 to 15 %w/v.
- the reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 10 %w/v.
- the reconstituted antibiotic formulation has a concentration of the at least one beta- lactam antibiotic between 10 to 200 mg/ml, more preferably between 50 to 150 mg/ml.
- the reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 100 mg/ml.
- the antibiotic formulation further includes a flavouring agent.
- the flavouring agent is a natural flavouring agent.
- the flavouring agent is an artificial flavouring agent.
- the flavouring agent is a natural and artificial flavouring agent.
- the flavouring agent improves the palatability of the antibiotic formulation.
- the flavouring agent improves the aroma of the antibiotic formulation.
- the flavouring agent is sucrose.
- the present invention broadly resides in an orally administered antibiotic formulation for an animal including at least one beta-lactam antibiotic in a form that is suitable for mixing with a liquid, wherein the antibiotic formulation is reconstituted in the liquid before administering to the animal.
- the present invention broadly resides in an orally administered liquid form antibiotic formulation for an animal including at least one beta-lactam antibiotic, and a liquid.
- the liquid form antibiotic formulation has a concentration of beta- lactam antibiotic between 1 to 20 %w/v. More preferably, the liquid form antibiotic formulation has a concentration of beta-lactam antibiotic between 5 to 15 %w/v. Preferably, the liquid form antibiotic formulation has a concentration of beta-lactam antibiotic of substantially 10 %w/v. Preferably, the liquid form antibiotic formulation has a concentration of beta-lactam antibiotic between 10 to 200 mg/ml, more preferably between 50 to 150 mg/ml. Preferably, the liquid form antibiotic formulation has a concentration of beta-lactam antibiotic of substantially 100 mg/ml.
- the liquid form antibiotic formulation further includes a flavouring agent.
- the flavouring agent is a natural flavouring agent.
- the flavouring agent is an artificial flavouring agent.
- the flavouring agent is a natural and artificial flavouring agent.
- the flavouring agent improves the palatability of the antibiotic formulation.
- the flavouring agent improves the aroma of the antibiotic formulation.
- the flavouring agent is sucrose.
- the present invention broadly resides in a system for orally administering an antibiotic formulation as herein described to an animal, the system including a container and an applicator, wherein the antibiotic formulation can be orally administered to the animal by the applicator.
- the antibiotic formulation is contained within the container.
- the antibiotic formulation contained within the container is in dry granular form. In another embodiment, the antibiotic formulation contained within the container is in dry powder form. In another embodiment, the antibiotic formulation contained within the container is in a dry pellet form.
- the antibiotic formulation in the container can be reconstituted by introducing a liquid into the container.
- the antibiotic formulation contained within the container is in liquid form.
- the applicator is a dropper.
- the dropper includes at least one dosage mark for measuring a desired dosage of the antibiotic formulation for administering to the animal.
- a desired amount of the antibiotic formulation is measured by the dropper and then orally administered to the animal through the dropper.
- the applicator is a nozzle that is attachable to the container.
- the nozzle is located at an opening of the container.
- the nozzle includes at least one dosage mark for measuring a desired dosage of the antibiotic formulation for administering to the animal.
- a desired amount of the antibiotic formulation is measured by the nozzle and then orally administered to the animal through the nozzle.
- the container is squeezable such that the antibiotic formulation can be poured out from the container into the nozzle.
- the container can be tilted such that the antibiotic formulation can poured out of the container into the nozzle due to gravity.
- the container can be tilted and squeezed such that the antibiotic formulation can poured out of the container into the nozzle due to gravity.
- the system further includes a lid that covers the opening of the container.
- the lid can be used as a measuring cup.
- the lid can be used to measure a desired amount of liquid for reconstituting the antibiotic formulation.
- the lid can be used to measure a desired dosage of the antibiotic formulation for administering to the animal.
- the present invention broadly resides in a treatment for an animal using an orally administered antibiotic formulation as herein described, wherein substantially 10 to 300 mg of the at least one beta-lactam antibiotic is administered to the animal.
- the antibiotic formulation is orally administered to the animal directly in liquid form. In another embodiment, the antibiotic formulation is orally administered to the animal in liquid form by adding to the animal’s food.
- the antibiotic formulation is administered to the animal at a rate of substantially 10 to 30 mg of the at least one beta-lactam antibiotic per kg body weight of the animal. More preferably, the antibiotic formulation is administered to the animal at a rate of substantially 10 to 15 mg of the at least one beta-lactam antibiotic per kg body weight of the animal.
- the antibiotic formulation is reconstituted in a liquid before administering to the animal.
- the reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 100 mg/ml.
- the reconstituted antibiotic formulation is administered at a rate of substantially 1 to 3 ml of the antibiotic formulation per 10 kg body weight of the animal. More preferably, the antibiotic formulation is administered to the animal at a rate of substantially 1 to 1.5 ml of the antibiotic formulation per 10 kg body weight of the animal.
- the antibiotic treatment is administered to the animal for at least 2 to 10 days. More preferably, the antibiotic treatment is administered to the animal for substantially 5 days.
- the antibiotic treatment is administered to the animals at least once daily. More preferably, the antibiotic treatment is administered to the animals at least twice daily.
- the antibiotic treatment is effective for treating bacterial infections in an animal.
- the antibiotic treatment is effective for treating bacterial infections of the skin, urinary tract, respiratory tract, or bones and joints of an animal.
- the present invention broadly resides in an orally administered antibiotic treatment for an animal including an orally administered antibiotic formulation as herein described, wherein the antibiotic formulation is a liquid form antibiotic formulation and wherein substantially 10 to 300 mg of the at least one beta-lactam antibiotic is administered to the animal.
- liquid form antibiotic formulation is orally administered to the animal directly. In another embodiment, the liquid form antibiotic formulation is orally administered to the animal by adding to the animal’s food.
- the liquid form antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 100 mg/ml.
- substantially 0.1 to 3 ml of the liquid form antibiotic formulation is administered to the animal.
- the liquid form antibiotic formulation is administered to the animal at a rate of substantially 10 to 30 mg of the at least one beta-lactam antibiotic per kg body weight of the animal. More preferably, the antibiotic formulation is administered to the animal at a rate of substantially 10 to 15 mg of the at least one beta-lactam antibiotic per kg body weight of the animal.
- the liquid form antibiotic formulation is administered at a rate of substantially 1 to 3 ml of the antibiotic formulation per 10 kg body weight of the animal. More preferably, the liquid form antibiotic formulation is administered to the animal at a rate of substantially 1 to 1.5 ml of the antibiotic formulation per 10 kg body weight of the animal.
- the liquid form antibiotic treatment is administered to the animal for at least 2 to 10 days. More preferably, the liquid form antibiotic treatment is administered to the animal for substantially 5 days. Preferably, the liquid form antibiotic treatment is administered to the animals at least once daily. More preferably, the liquid form antibiotic treatment is administered to the animals at least twice daily.
- the present invention broadly resides in a method of administering an antibiotic formulation as described herein to an animal, the method includes orally administering a dose of the antibiotic formulation in liquid form to the animal.
- the step of orally administering the dose in liquid form includes orally administering the dose directly in liquid form to the animal. In another embodiment, the step of orally administering the dose in liquid form includes the step of adding the dose of the antibiotic formulation to a food and feeding the animal with the food.
- the dose of the antibiotic formulation is substantially 10 to 300 mg of the at least one beta-lactam antibiotic.
- the step of administering the antibiotic formulation includes administering the antibiotic formulation at a rate of substantially 10 to 30 mg of the at least one beta-lactam antibiotic per kg body weight of the animal. More preferably, the step of administering the antibiotic formulation includes administering the antibiotic formulation at a rate of substantially 10 to 15 mg of the at least one beta- lactam antibiotic per kg body weight of the animal.
- the method further includes a step of reconstituting the antibiotic formulation in a liquid before the step of administering the antibiotic formulation to the animal.
- the reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 100 mg/ml.
- the step of administering the antibiotic formulation includes administering the reconstituted antibiotic formulation at a rate of substantially 1 to 3 ml of the reconstituted antibiotic formulation per 10 kg body weight of the animal. More preferably, the step of administering the antibiotic formulation includes administering the reconstituted antibiotic formulation at a rate of substantially 1 to 1.5 ml of the reconstituted antibiotic formulation per 10 kg body weight of the animal.
- the step of administering the antibiotic formulation includes administering the antibiotic formulation for at least 2 to 10 days. More preferably, the step of administering the antibiotic formulation includes administering the antibiotic formulation for substantially 5 days. Preferably, the step of administering the antibiotic formulation includes administering the antibiotic formulation at least once daily. More preferably, the step of administering the antibiotic formulation includes administering the antibiotic formulation at least twice daily.
- the orally administered antibiotic formulation is effective for treating bacterial infections in an animal.
- the orally administered antibiotic formulation is effective for treating bacterial infections of the skin, urinary tract, respiratory tract, or bones and joints of an animal.
- the orally administered antibiotic formulation is effective for alleviating symptoms of bacterial infections in an animal.
- the orally administered antibiotic formulation is effective for alleviating symptoms of bacterial infections of the skin, urinary tract, respiratory tract, or bones and joints of an animal.
- the present invention broadly resides in a method of administering an antibiotic formulation as described herein to an animal, the method including the step of orally administering a dose of the antibiotic formulation to the animal, wherein the antibiotic formulation is a liquid form antibiotic formulation.
- the dose of the antibiotic formulation is substantially 10 to 300 mg of the at least one beta-lactam antibiotic.
- the step of orally administering a dose of the antibiotic formulation includes administering the liquid form antibiotic formulation at a rate of substantially 10 to 30 mg of the at least one beta-lactam antibiotic per kg body weight of the animal. More preferably, the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at a rate of substantially 10 to 15 mg of the at least one beta-lactam antibiotic per kg body weight of the animal.
- the liquid form reconstituted antibiotic formulation has a concentration of the at least one beta-lactam antibiotic at substantially 100 mg/ml.
- the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at a rate of substantially 1 to 3 ml of the liquid form antibiotic formulation per 10 kg body weight of the animal. More preferably, the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at a rate of substantially 1 to 1.5 ml of the liquid form antibiotic formulation per 10 kg body weight of the animal.
- the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at least once daily for at least 2 to 10 days. More preferably, the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at least once daily for substantially 5 days. Preferably, the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at least once daily. More preferably, the step of administering the antibiotic formulation includes administering the liquid form antibiotic formulation at least twice daily.
- the present invention broadly resides in a method of preparing an orally administered antibiotic formulation for animals as described herein, the method includes adding a sufficient amount of liquid to dissolve the antibiotic formulation; and mixing the antibiotic formulation and the liquid.
- the antibiotic formulation is prepared by micronization into dry granules that can be dissolved in the liquid.
- the antibiotic formulation is prepared by micronization into dry powder that can be dissolved in the liquid.
- the antibiotic formulation is prepared by micronization into a dry tablet that can be dissolved in the liquid.
- the animal is a dog or a cat.
- Figure 1 is a perspective view of how to orally administer an antibiotic formulation to an animal according to an embodiment of the present invention.
- FIG. 1 there is shown a perspective view of administering an antibiotic formulation to an animal 10 with an example of a dog according to a preferred embodiment.
- the antibiotic formulation includes 150 mg/g of cephalexin and sucrose, which is micronized in order to prepare the antibiotic formulation in dry granular form.
- the resulting antibiotic formulation in dry granular form is stable and has a shelf life of 24 months when stored at room temperature.
- the antibiotic formulation in dry granular form is also easily reconstituted for administration and absorbed by the animal.
- Cephalexin (also referred to as Cefalexin) is a semisynthetic first-generation cephalosporin antibiotic. It is one of the most widely prescribed antibiotics that is often used for the treatment of bacterial infections of the animal’s skin, urinary tract, respiratory tract, bones and joints. Cephalexin is effective against most gram positive bacteria through its inhibition of the cross-linking reaction between N-acetyl muramic acid and N-acetyl glucosamine in the cell wall, leading to cell lysis. Cephalexin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.
- PBPs penicillin-binding proteins
- PBPs are involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during bacterial cell growth and cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell rupture. Cephalexin is not recommended for animals allergic to penicillin or cephalosporins and caution is recommended in relation to use in pregnant and nursing animals and in animals that are concurrently being given probenecid or aminoglycosides such as neomycin and gentamicin. Similarly, caution is recommended when it is given with other drugs that may affect the kidneys.
- sucrose is used as a flavouring agent. Pure cephalexin has a bitter taste and therefore orally administration of such may be rejected by the animal. Adding sucrose to the antibiotic formulation helps to minimise resistance of the animal to the administration of the antibiotic formulation.
- the antibiotic formulation is reconstituted by adding water into container 12.
- the liquid form antibiotic formulation 13 in the container 12 has a concentration of cephalexin at 100 mg/ml.
- the liquid form antibiotic formulation 13 can be administered directly into the animal’s mouth such that the animal is not able to reject the dose or part of the dose.
- a dropper 16 is filled with a dosage of the antibiotic formulation 13.
- the antibiotic formulation 13 is then administered directly into the mouth of animal 10.
- the antibiotic formulation 13 is administered at a rate of 10 to 15 mg per kg body weight of the animal 10. That is, 1 to 1.5 ml of the antibiotic formulation 13 per 10 kg body weight is administered to animal 10.
- 0.5 to 1 ml of the antibiotic formulation 13 can be administered to animal 10 with a body weight up to 5 kg; 0.5 - 1.5 ml of the antibiotic formulation 13 can be administered to animal 10 with a body weight between 6 to 10 kg; 1 to 3 ml of the antibiotic formulation 13 can be administered to animal 10 with a body weight between 11 to 20 kg.
- the antibiotic formulation 13 is applied at least twice daily for five days.
- the liquid form antibiotic formulation 13 is stable and has a shelf life of 10 days after reconstitution when stored at room temperature.
- the liquid form antibiotic formulation 13 should be used within 10 days of reconstitution.
- An advantage of the preferred embodiment of the present invention includes providing an alternative option of an antibiotic formulation that can be easily and effectively administered orally to an animal. Another advantage of the preferred embodiment of the present invention includes providing an alternative antibiotic formulation that minimizes resistance or rejection by an animal to the orally administration of the antibiotic formulation. A further advantage of the preferred embodiment of the present invention includes providing an alternative antibiotic formulation that can be easily prepared in the correct and effective dosage for treatment. Another advantage of the preferred embodiment of the present invention includes providing an alternative antibiotic formulation that can be consistently and accurately administered at the correct and effective dosage for treatment. A further advantage of the preferred embodiment of the present invention includes providing an alternative antibiotic formulation that is stable at room temperature for storage. Another advantage of the preferred embodiment of the present invention includes providing an alternative antibiotic formulation that can be easily reconstituted with a liquid before use.
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Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2004014337A2 (en) * | 2002-08-02 | 2004-02-19 | Ranbaxy Laboratories Limited | A process for the preparation of dispersible tablet of cephalexin |
WO2013059664A1 (en) * | 2011-10-21 | 2013-04-25 | Seachaid Pharmaceuticals, Inc. | Pharmaceutical compositions and uses thereof |
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Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2004014337A2 (en) * | 2002-08-02 | 2004-02-19 | Ranbaxy Laboratories Limited | A process for the preparation of dispersible tablet of cephalexin |
WO2013059664A1 (en) * | 2011-10-21 | 2013-04-25 | Seachaid Pharmaceuticals, Inc. | Pharmaceutical compositions and uses thereof |
Non-Patent Citations (4)
Title |
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ALBARELLOS GABRIELA A., SABRINA M PASSINI, MARTÍN P LUPI, SILVIA ARAMAYONA, PAULA M LORENZINI, LAURA MONTOYA, MARIA F LANDONI : "Effect of food on the pharmacokinetics of oral cefuroxime axetil in dogs", J VET PHARMACOL THER., vol. 43, no. 3, pages 297 - 302, XP093025076, DOI: 10.1111/jvp.12854 * |
DATABASE GNPD 1 January 2019 (2019-01-01), MUNDO ANIMAL PETSPORIN: "Antibiotic Bactericide for Cats and Dogs ", XP009542709, retrieved from MINTEL Database accession no. 6272515 * |
PRAGMA PHARMACEUTICALS, KEFLEX® CEPHALEXIN ORAL SUSPENSION, USP, PRAGMA PHARMACEUTICALS, LLC, pages 1 - 8, XP009542697, Retrieved from the Internet <URL:https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050406s013lbl.pdf> [retrieved on 20220615] * |
YAMANAKA HIDEAKI, KAWABATA KOHJI, MIYAI KENJI, TAKASUGI HISASHI, KAMIMURA TOSHIAKI, MINE YASUHIRO, TAKAYA TAKAO: "STUDIES ON p-LACTAM ANTIBIOTICS X. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 7p-[(Z)-2-(2-AMINO-4-TH IAZOLYL)-2-(CARBOYMETHOXY- IMINO)ACETAMIDOJCEPHALOSPORIN DERIVATIVES", THE JOURNAL OF ANTIBIOTICS, 1 January 1986 (1986-01-01), pages 101 - 110, XP093025080 * |
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