IE781425L - Injectable chloroamphenicol solution - Google Patents
Injectable chloroamphenicol solutionInfo
- Publication number
- IE781425L IE781425L IE781425A IE142578A IE781425L IE 781425 L IE781425 L IE 781425L IE 781425 A IE781425 A IE 781425A IE 142578 A IE142578 A IE 142578A IE 781425 L IE781425 L IE 781425L
- Authority
- IE
- Ireland
- Prior art keywords
- chloramphenicol
- composition according
- pvp
- composition
- injectable
- Prior art date
Links
Classifications
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
Abstract
An injectable composition contains chloramphenicol, N-methylpyrrolidone and polyvinyl-pyrrolidone. The composition may also contain a pharmaceutically-acceptable solvent which is miscible with N-methylpyrrolidone. It is used in veterinary medicine and is stable, concentrated, exhibits constant blood levels and does not produce unpleasant side effects.
[GB2000970A]
Description
- 1 - 471 26 The present invention relates to a stable injectable chloramphenicol composition having a high content of chloramphenicol.
Chloramphenicol is utilised at present mainly for 'j veterinary purposes. It is desired to administer to a large animal a composition having a rither high content of chloramphenicol. Said large amount of chloramphenicol Bhould exhibit constant elood levels and be active for quite a long period of time. So far there has been injected sodium suocinate 10 of chloramphenicol in a concentration of 257* and there are also known some injectable compositions which comprise up to 25# of active compound. However, these compositions are not always satisfactory, i.e. in particular they are unstable and have a relatively short shelf life, and it was therefore 15 desirable to develop compositions which would have higher concentrations of chloramphenicol and would have the desired properties, i.e. exhibit constant blood levels and have a long shelf life. ;It has been foud that if chloramphenicol is dissolved 20 in K-methylpyrroiidone there may be prepared compositions having a higher concentration of chloramphenicol(about 50$). However, these compos tions had the following drawbacks: ;a. Erratic blood lelre .s were obtained^ ;b. Pain and irritation were caused to the animal treated with 2i> said injection. ;4 7 126 ;- 2 - ;For these reasons saic compositions were not applicable* It has nov surprisingly been found that with the addition of a certain amount of polyvinyl pyrrolitione(PVP) to said composition said drawbacks are overcome. ThiB is surprising as it could not be expected that PVP- would cause a constant blood level ana in particular that it would dispel the pain and irritation. The shelf life of said compositions is at least one year.
The present invention thus consists in an injectable composition comprising chloramphenicol, N-methylpyrrolidone, PVP and, if desired, a pharmaceutical^ acceptable solvent which is miscible vi;h N-methylpyrrolidone.
Compositions according to the present invention may comprise also, if desired, only small amounts of chloramphenicol. However, they should contain preferably at least 30% of chloramphenicol and especially 40-6C#(all percentages are given herein weight/volume). Compositions according to the present Invention having a lower content of chloramphenicol are also much better than those commercially available as they arc much more stable.
The amount of the PVP varies and it should be between 4-20^6 preferably between 5-105® of the entire composition.
Other solvents, if required, are utilised as diluents in order to get the required concentration of the composition. As suitable solvents one should mention water, ethanol and in particular, certain glycols, or derivatives thereof, e.g. propyleueglycoi, glycerol-formal, tertaglycol, polyethylene-glycol, etc. 47 126 The present invention will now be illustrated with reference xo the following examples without being restricted by their:.
The composition of che present invention were prepared b as follows ir. all examples: The chloramphenicol was dissolved in N-methylpyrrolidone• Thereafter the PVP was addea ana finally the additional solvent, if any, was admixed.
The PVP utilised is a product of General Aniline and 10 Film Corporation.The K numbers are derived from viscosity.
Example 1 Chloramphenicol 50.0 g N-Methylpyrrolidone 40.0 g PVP K30 6.0 g lb Propyleneglycol enough to make 100.0 ml At the end of two years storage at room temperature had only '5.5% of the chloramphenicol/degraded.
The volume needed of thi' composition (called the "50%" composition) to be injected to a ruminant for achieving a dose level 20 of SO mg/kg was compared with the following composition: Chloramphenicol 20 g (Jlycerolformal BO g rfater enough to make 100 ml The shelf life of the 20> composition was less than 25 ;• months (the degradation of chloramphenicol was about 40$).
The results are given in Table I, wh t.ch show comparitive blood levels of chloramphenicol affce." parenteral administration of 50 mg/kg of each of the compositions. 4 7 1 2 6 - 4 - TABLE 1 formulation Calf of 2we of Cow of Cow of 50 kg 65 kg 500 kg 650 kg 20% 12.5 ug/ml 16.25 ug/ml 125 ug/ml 162.5 ug/ml 50$ 5 ug/ml 6.5 ug/ml 50 ug/ml 65 ug/ml Similar comparisons with compositions having various concentrations of chloramphenicol showed the superiority of the 50$ composition.
Moreover, the mean serum chloramphenicol concentrations over a certain period of time following a single intramuscular injection of said formulations were compared.
The results are shown in the accompanying drawings in which: Fig.l shows the mean serum concentration of cStivee at a dose level of 50 mg/kg.
Pig.2 shows the mean serum concentration at cows at a dose level of 30 mg/kg; and Fig.3 shows the mean serum concentration of ewes at at a dose level of 50 mg/kg.
The tests were performed by known methods (see, for example, Glazko,(s), Set.al. Arch. Biochem. 22, 411-418,1949 and Ziv.b, et al. Zbl.Vet.Med.(A) 20.801-811.1973).
Example 2 Chloramphenicol 10.0 g N-Methylpyrrolidine 30.0 g PVP KL5 6.0 g Propyleneglycol enough to make 100.0 ml Example 5 Chloramphenicol §0.0 PVP K15 0.0 g M~KethylpyrrolitSone enough to maice 103.0 ml Xtuple A Chloramphenicol 5°»0 £ N-Methylpyrrclicione 40.0
Claims (11)
1. Claims L An injectable composition comprising chloramphenicol, N-methylpyrrolidone, PVP and, if aeaired, a pharmactiuti-cally acceptable Bolvent which is mlscible with N-methyl-b pyrrolidone.
2. A composition according to Claim 1 wherein the amount of chloramphenicol is at least 30$.
3. A composition according to Claim 1 or 2, wherein the amount of chloramphenicol is 40-60^.. 10
4. A composition according to any of Claims 1 to 3, wherein the amount of PVP is 4-20>.
5. A composition according to Claim 4, wherein the amount of PVP is 5-10%.
6. A composition according to any of Claims 1 to 5 wherein the lb additional solvent is water.
7. A composition according to any of Claims 1 to b wherein the additional solvent in ethanol.
8. A composition according to any of Claims 1 to 5 wherein the additional solvent is a glycol or a derivative thereof. 20
9. A composition according to Claim a, wherein the glycol is selected among the group comprising propyleneglycol, glycerolformal, tertrtglycol, polyethyleneglyccl.
10.An injectable composition, substantially ae hereinbefore described with reference to the Examples. 25
11.A method for the preparation of an injectable composition as defined in Claim 1, wherein the chloramphenicol is dissolved in the N-methylpyrrolidone, PVP is acdec to the solution and the additional solvent, if any, is added. Dated this 14th day of July 1978 BY: TOMKINS & CO., Appli«ints Agents, (Signed) /!>, Dartmouth Road, DUBLIN 6.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IL52533A IL52533A (en) | 1977-07-15 | 1977-07-15 | Injectable chloramphenicol composition |
Publications (2)
Publication Number | Publication Date |
---|---|
IE781425L true IE781425L (en) | 1979-01-15 |
IE47126B1 IE47126B1 (en) | 1983-12-28 |
Family
ID=11049656
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IE1425/78A IE47126B1 (en) | 1977-07-15 | 1978-07-14 | An injectable chloramphenicol composition |
Country Status (13)
Country | Link |
---|---|
JP (1) | JPS5420125A (en) |
AT (1) | AT360149B (en) |
AU (1) | AU3752578A (en) |
BE (1) | BE869001A (en) |
CA (1) | CA1112572A (en) |
DE (1) | DE2829408A1 (en) |
FR (1) | FR2397191A1 (en) |
GB (1) | GB2000970B (en) |
IE (1) | IE47126B1 (en) |
IL (1) | IL52533A (en) |
NL (1) | NL7807641A (en) |
NZ (1) | NZ187683A (en) |
ZA (1) | ZA783671B (en) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3064250D1 (en) * | 1979-07-02 | 1983-08-25 | Pfizer | Long acting sulfonamide injectable compositions |
NL8002636A (en) * | 1980-05-08 | 1981-12-01 | Gist Brocades Nv | SOLOATE OF AMOXICILLINE, METHOD FOR PREPARING IT AND METHOD FOR PREPARING INJECTION PREPARATIONS FROM THIS SOLVATE |
NL178941C (en) * | 1982-06-15 | 1986-06-16 | Aesculaap Bv | PROCESS FOR PREPARING AN AQUEOUS OXYTETRACYCLINE PREPARATION. |
JPS6031189A (en) * | 1983-07-30 | 1985-02-16 | カシオ計算機株式会社 | Musical sound generator |
US4696814A (en) * | 1985-08-21 | 1987-09-29 | Warner-Lambert Company | Parenteral phenytoin compositions |
IT1197481B (en) * | 1986-09-15 | 1988-11-30 | Zambon Spa | PHARMACEUTICAL PREPARATION FOR VETERINARY USE |
US20030068339A1 (en) * | 2001-10-02 | 2003-04-10 | Phoenix Scientific, Inc. | Veterinary florfenicol formulation that is syringeable under cold weather conditions |
WO2006067138A2 (en) * | 2004-12-21 | 2006-06-29 | Intervet International B.V. | Injectable veterinary composition |
CN113694018A (en) * | 2021-09-08 | 2021-11-26 | 海南制药厂有限公司制药二厂 | Chloramphenicol injection and preparation method thereof |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1538903A (en) * | 1975-04-11 | 1979-01-24 | Nelson Res & Dev | Carrier for a topically applied physiologically active agent or cosmetic agent |
-
1977
- 1977-07-15 IL IL52533A patent/IL52533A/en unknown
-
1978
- 1978-06-27 ZA ZA00783671A patent/ZA783671B/en unknown
- 1978-06-27 NZ NZ187683A patent/NZ187683A/en unknown
- 1978-06-28 AU AU37525/78A patent/AU3752578A/en active Pending
- 1978-07-04 FR FR7819873A patent/FR2397191A1/en active Granted
- 1978-07-05 DE DE19782829408 patent/DE2829408A1/en not_active Withdrawn
- 1978-07-14 CA CA307,371A patent/CA1112572A/en not_active Expired
- 1978-07-14 AT AT511878A patent/AT360149B/en not_active IP Right Cessation
- 1978-07-14 JP JP8665578A patent/JPS5420125A/en active Pending
- 1978-07-14 GB GB7829921A patent/GB2000970B/en not_active Expired
- 1978-07-14 IE IE1425/78A patent/IE47126B1/en unknown
- 1978-07-14 BE BE189287A patent/BE869001A/en unknown
- 1978-07-17 NL NL7807641A patent/NL7807641A/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
FR2397191B1 (en) | 1981-12-31 |
AT360149B (en) | 1980-12-29 |
ATA511878A (en) | 1980-05-15 |
CA1112572A (en) | 1981-11-17 |
IL52533A0 (en) | 1977-10-31 |
DE2829408A1 (en) | 1979-02-01 |
NL7807641A (en) | 1979-01-17 |
JPS5420125A (en) | 1979-02-15 |
IL52533A (en) | 1980-01-31 |
GB2000970A (en) | 1979-01-24 |
AU3752578A (en) | 1980-01-03 |
BE869001A (en) | 1979-01-15 |
GB2000970B (en) | 1982-03-17 |
FR2397191A1 (en) | 1979-02-09 |
IE47126B1 (en) | 1983-12-28 |
NZ187683A (en) | 1981-03-16 |
ZA783671B (en) | 1979-06-27 |
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