CA1085296A - Long acting preparation of cefalexin for effective treatments of bacterial infection sensitive to cefalexin - Google Patents
Long acting preparation of cefalexin for effective treatments of bacterial infection sensitive to cefalexinInfo
- Publication number
- CA1085296A CA1085296A CA276,514A CA276514A CA1085296A CA 1085296 A CA1085296 A CA 1085296A CA 276514 A CA276514 A CA 276514A CA 1085296 A CA1085296 A CA 1085296A
- Authority
- CA
- Canada
- Prior art keywords
- cefalexin
- preparation
- coated
- normal
- granules
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 229940106164 cephalexin Drugs 0.000 title claims abstract description 91
- 238000002360 preparation method Methods 0.000 title claims abstract description 79
- 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 title claims abstract description 16
- 238000011282 treatment Methods 0.000 title abstract description 5
- 208000035143 Bacterial infection Diseases 0.000 title abstract description 4
- 208000022362 bacterial infectious disease Diseases 0.000 title abstract description 4
- 239000002552 dosage form Substances 0.000 claims abstract description 20
- 238000004090 dissolution Methods 0.000 claims abstract description 18
- 238000000576 coating method Methods 0.000 claims abstract description 16
- 239000011248 coating agent Substances 0.000 claims abstract description 15
- 239000000463 material Substances 0.000 claims abstract description 12
- 210000000936 intestine Anatomy 0.000 claims abstract description 8
- 210000002784 stomach Anatomy 0.000 claims abstract description 7
- 239000002775 capsule Substances 0.000 claims abstract description 5
- 239000002245 particle Substances 0.000 claims abstract description 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract 11
- 239000008187 granular material Substances 0.000 claims description 31
- 239000011324 bead Substances 0.000 claims description 7
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims description 3
- 229920001577 copolymer Polymers 0.000 claims description 3
- 239000003094 microcapsule Substances 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 239000011247 coating layer Substances 0.000 abstract description 6
- 230000001419 dependent effect Effects 0.000 abstract description 5
- 239000003826 tablet Substances 0.000 abstract description 5
- 239000010410 layer Substances 0.000 abstract description 4
- AVGYWQBCYZHHPN-CYJZLJNKSA-N cephalexin 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=CC=C1 AVGYWQBCYZHHPN-CYJZLJNKSA-N 0.000 description 75
- 230000036765 blood level Effects 0.000 description 33
- 239000003814 drug Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 13
- 238000002474 experimental method Methods 0.000 description 13
- 239000004615 ingredient Substances 0.000 description 12
- 241000894006 Bacteria Species 0.000 description 9
- 238000000034 method Methods 0.000 description 9
- 230000000844 anti-bacterial effect Effects 0.000 description 8
- 208000015181 infectious disease Diseases 0.000 description 7
- 230000036325 urinary excretion Effects 0.000 description 7
- 239000007931 coated granule Substances 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 6
- 235000012054 meals Nutrition 0.000 description 6
- 241000191967 Staphylococcus aureus Species 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 5
- 230000007423 decrease Effects 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- 230000002123 temporal effect Effects 0.000 description 5
- 230000007704 transition Effects 0.000 description 5
- 210000002700 urine Anatomy 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 230000003247 decreasing effect Effects 0.000 description 4
- 230000029142 excretion Effects 0.000 description 4
- 239000002609 medium Substances 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 208000035473 Communicable disease Diseases 0.000 description 3
- 229920003136 Eudragit® L polymer Polymers 0.000 description 3
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 238000002512 chemotherapy Methods 0.000 description 3
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 3
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 3
- 238000011835 investigation Methods 0.000 description 3
- 150000002500 ions Chemical class 0.000 description 3
- 230000036962 time dependent Effects 0.000 description 3
- 206010056396 Asymptomatic bacteriuria Diseases 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 210000003608 fece Anatomy 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 230000000979 retarding effect Effects 0.000 description 2
- 238000004088 simulation Methods 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 235000011960 Brassica ruvo Nutrition 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 241000588722 Escherichia Species 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 229920003137 Eudragit® S polymer Polymers 0.000 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 241000588748 Klebsiella Species 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241000589516 Pseudomonas Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 241000193996 Streptococcus pyogenes Species 0.000 description 1
- 241000187747 Streptomyces Species 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 230000000845 anti-microbial effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000036983 biotransformation Effects 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 208000037516 chromosome inversion disease Diseases 0.000 description 1
- 230000002301 combined effect Effects 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 210000001198 duodenum Anatomy 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 239000012055 enteric layer Substances 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 239000002054 inoculum Substances 0.000 description 1
- 210000001630 jejunum Anatomy 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 150000004682 monohydrates Chemical class 0.000 description 1
- 239000006916 nutrient agar Substances 0.000 description 1
- 229940124588 oral cephalosporin Drugs 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 229940086255 perform Drugs 0.000 description 1
- DBABZHXKTCFAPX-UHFFFAOYSA-N probenecid Chemical compound CCCN(CCC)S(=O)(=O)C1=CC=C(C(O)=O)C=C1 DBABZHXKTCFAPX-UHFFFAOYSA-N 0.000 description 1
- 229960003081 probenecid Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 208000018556 stomach disease Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Cephalosporin Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5492576A JPS52139713A (en) | 1976-05-13 | 1976-05-13 | Sustained release cefalexin preparations |
| JP054925/1976 | 1976-05-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1085296A true CA1085296A (en) | 1980-09-09 |
Family
ID=12984185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA276,514A Expired CA1085296A (en) | 1976-05-13 | 1977-04-20 | Long acting preparation of cefalexin for effective treatments of bacterial infection sensitive to cefalexin |
Country Status (27)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5545601A (en) * | 1978-09-26 | 1980-03-31 | Toyo Jozo Co Ltd | Long-acting cephalexin and its preparation |
| FR2453639A1 (fr) * | 1979-04-09 | 1980-11-07 | Sanofi Sa | Composition medicamenteuse a liberation programmee immediate-retard a base de naftidrofuryl |
| JPS5659707A (en) * | 1979-10-19 | 1981-05-23 | Toyo Jozo Co Ltd | Lasting antibiotic pharmaceutical and its preparation |
| JPS5826816A (ja) * | 1981-08-11 | 1983-02-17 | Teisan Seiyaku Kk | 球形顆粒からなる持続性複合顆粒剤 |
| JPS5846019A (ja) * | 1981-09-14 | 1983-03-17 | Kanebo Ltd | 持続性ニフエジピン製剤 |
| JPS5883613A (ja) * | 1981-11-10 | 1983-05-19 | Toa Eiyou Kagaku Kogyo Kk | 硝酸イソソルビト−ル製剤 |
| JPS5883106U (ja) * | 1981-11-30 | 1983-06-06 | 松下電工株式会社 | 電磁石装置に於けるオイルダツシユポツト |
| US4525339A (en) * | 1982-10-15 | 1985-06-25 | Hoffmann-La Roche Inc. | Enteric coated oral dosage form |
| JPS601128A (ja) * | 1983-06-15 | 1985-01-07 | Shionogi & Co Ltd | 作用持続型セフアクロル製剤 |
| JPS6144811A (ja) * | 1984-08-10 | 1986-03-04 | Ss Pharmaceut Co Ltd | 徐放性ジクロフエナクナトリウム製剤 |
| FR2577800B1 (fr) * | 1985-02-22 | 1990-09-07 | Grimberg Georges | Medicament sous forme galenique gastro-resistante |
| JPS62226926A (ja) * | 1986-03-27 | 1987-10-05 | Teisan Seiyaku Kk | 持続性複合顆粒剤 |
| WO2006110807A1 (en) * | 2005-04-12 | 2006-10-19 | Elan Pharma International Limited | Controlled release compositions comprising a cephalosporin for the treatment of a bacterial infection |
| CN114617855A (zh) * | 2020-12-14 | 2022-06-14 | 江苏贝佳制药有限公司 | 头孢氨苄胶囊的制备方法 |
-
1976
- 1976-05-13 JP JP5492576A patent/JPS52139713A/ja active Granted
-
1977
- 1977-04-20 CA CA276,514A patent/CA1085296A/en not_active Expired
- 1977-04-26 NZ NZ183927A patent/NZ183927A/xx unknown
- 1977-05-03 NL NL7704879A patent/NL7704879A/xx active Search and Examination
- 1977-05-05 PT PT66514A patent/PT66514B/pt unknown
- 1977-05-09 IE IE940/77A patent/IE45415B1/en unknown
- 1977-05-09 ZA ZA00772757A patent/ZA772757B/xx unknown
- 1977-05-11 DK DK208077A patent/DK208077A/da not_active Application Discontinuation
- 1977-05-11 SE SE7705502A patent/SE426780B/xx not_active IP Right Cessation
- 1977-05-11 ES ES458710A patent/ES458710A1/es not_active Expired
- 1977-05-11 AU AU25078/77A patent/AU508793B2/en not_active Expired
- 1977-05-11 GB GB19853/77A patent/GB1543543A/en not_active Expired
- 1977-05-11 FI FI771491A patent/FI771491A7/fi not_active Application Discontinuation
- 1977-05-12 RO RO7790312A patent/RO72935A/ro unknown
- 1977-05-12 GR GR53444A patent/GR68895B/el unknown
- 1977-05-12 HU HU77SI1575A patent/HU184196B/hu unknown
- 1977-05-12 MX MX775739U patent/MX5976E/es unknown
- 1977-05-12 PL PL1977198058A patent/PL111183B1/pl unknown
- 1977-05-12 AT AT341877A patent/AT351159B/de not_active IP Right Cessation
- 1977-05-12 IL IL52075A patent/IL52075A/xx unknown
- 1977-05-12 SU SU772485596A patent/SU1218919A3/ru active
- 1977-05-12 FR FR7714616A patent/FR2350836A1/fr active Granted
- 1977-05-13 BE BE177585A patent/BE854640A/xx unknown
- 1977-05-13 DD DD7700198922A patent/DD132232A5/xx unknown
- 1977-05-13 CS CS773167A patent/CS208196B2/cs unknown
- 1977-05-13 DE DE19772721785 patent/DE2721785A1/de active Granted
- 1977-05-13 AR AR267621A patent/AR224494A1/es active
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |