IE47126B1 - An injectable chloramphenicol composition - Google Patents
An injectable chloramphenicol compositionInfo
- Publication number
- IE47126B1 IE47126B1 IE1425/78A IE142578A IE47126B1 IE 47126 B1 IE47126 B1 IE 47126B1 IE 1425/78 A IE1425/78 A IE 1425/78A IE 142578 A IE142578 A IE 142578A IE 47126 B1 IE47126 B1 IE 47126B1
- Authority
- IE
- Ireland
- Prior art keywords
- chloramphenicol
- composition
- methylpyrrolidone
- composition according
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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.
Description
The present invention relates to a stable injectable chloramphenicol composition having a high content of chloramphenicol.
Cnloramphenicol is stilise·' at present mainly for 5 veterinary purposes. It is desired to administer to a large animal a composition having a rather high content of chloramphenicol. Said large amount of chloramphenicol should exhibit constant clood levele and be active for quite a long period of time. So far there has been injected sodium succinate of chloramphenicol in a concentration of 25% 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 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 in N-methylpyrrolidone 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. rain and irritation were caused to the animal treated with said injection.
- 2 •· 4 7 12 6
For these reasons said compisitince were not applicable. It has now surprisingly been found that with the addition of a certain amount of polyvinyl pyrrolidone(PVP) to said composition said drawbacks are overcome. This is surprising ae it could not he expected that PVP- would cause a constant blood level and 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 10 composition comprising chloramphenicol, N-methylpyrrolidone,
PVP and, if desired, a pharmaceutically acceptable solvent which is miscible wish N-methylpyrrolidone.
Compositions according to the present invention may comprise also, if desired, only small amounts of chloramphe15 nicol. However, they should contain preferably at least 30# of chloramphenicol and especially 4Q-6O#(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
2ti they are much more stable.
The amount of the PVP varies and it should be between 4-20# preferably between 5-10# of the entire composition.
Other solvents, if required, are utilised ae diluents in order to get the required concentration of the composition.
As suitable solvent?; one should mention water, ethanol and ln particular, certain glycols, or derivatives thereof, e.g. propyleueglycoi, glycerol-formal, tertaglycol, polyethyleneglycol, etc.
126
The present invention will now be illustrated with reference to the following examples without being restricted by them.
The composition of the present invention were prepared as follows in all examples:
ihe chloramphenicol was dissolved in N-methylpyrrolidone. Thereafter the PVP was adder ana finally the additional solvent, if any, was admixed.
The PVP utilised is a product of General Aniline and Film Corporation.The K numbers are derived from viscosity.
Example 1
Chloramphenicol 50«0 g
N-Methylpyrrolidone 40.0 g
PVP K50 6.0 g
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 d06e level cf SO mg/kg was compared with the following composition:
Chloramphenicol 20 g
Glycerolformal 80 g «i&ter enough to make 100 ml
The shelf life cf the 20?· composition was less than 2 months (the degradation of chloramphenicol was about 40%).
The results are given in Table 1, wh t.ch show comparitive blood levels of chloramphenicol after parenteral administration of 50 mg/kg of each of the compositions.
7 12 6
- 4 TABLE 1
Formulation Calf of 50 kg Ewe of 65 kg Cow of 500 kg Cow of 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 c&lves 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 eerum concentration of ewes at 15 at a dose level of 50 mg/kg.
The tests were performed by known methods (see, for example, Glazko,(e), Set.al. Arch. Biochero. 23 . 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 K15 6.0 g
Propyleneglycol enough to make
100.0 ml
1 an
Example 5
Ohioram ph βnic oi
FVP XI5 §0.0 ;;
0.0 g
N-ftethylpyrrolidone enough: to make 100.0 ml
Mtople 4
Chloramphenicol N-Methylpyrrcliuone
FVF K30
Glyceroli'ormal enough to make
Example 5Chloramphenicol
N-Methylpyrrolidone
FVF K30
Tetraglycol enough to make
Example b
Chloramphenicol h-Me thylpy rro1id one
PVF K15
Polyethyleneglycol 500 enough
Example *?
Chloramphenicol fl-Methylpyrrolidone
FVF K15
Ethanol 951 enough to make
50.0 R
40.0 g
1C.0 g
100.0 ml
50.0 g
40.0 g
1.0 fi
100.0 ml
40.0 g 40.0 g
.0 g o make 100.0 ml
.0 g 40.0 g 20.0 g 100.0 ml.
Example 6
Chloramphenicol k-Methylpyrrolidone
PVF KL5 water enough to make 100 ml
Claims (11)
1. An injectable composition comprising chloramphenicol, N-methylpyrrolidone, PVP and, if aesired, a pharmaceutically acceptable solvent which is miscible with N-methylpyrrolidone.
2. A composition according to Claim 1 wherein the amount of chloramphenicol is at least 5. A composition according to Claim 1 or 2, wherein the amount of chloramphenicol is 40-60¾.
3. 4. A composition according to any of Claims 1 to 3, wherein the amount of PVT is 4-20?«.
4. 5. A composition according to Claim 4, wherein the amount of PVP is 5-10%.
5. 6. A composition according to any of Claims 1 to 5 wherein the additional solvent is water.
6. 7. A composition according to any of Claims 1 to 5 wherein the additional solvent is ethanol.
7. 8. A composition according to any of Claims 1 to 5 wherein the additional solvent is a glycol or a derivative thereof.
8. 9. A composition according to Claim 8, wherein the glycol is selected among the group comprising propyleneglycol, glycerolformal, tertraglycol, polyethyleneglycol.
9. 10. An injectable composition, substantially as hereinbefore described with reference to the Examples.
10.
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 solution and the additional solvent, if any,
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 IE781425L (en) | 1979-01-15 |
IE47126B1 true 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 |
PL1830885T3 (en) | 2004-12-21 | 2009-04-30 | Intervet Int Bv | Injectable veterinary composition comprising florfenicol |
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 AT AT511878A patent/AT360149B/en not_active IP Right Cessation
- 1978-07-14 JP JP8665578A patent/JPS5420125A/en active Pending
- 1978-07-14 BE BE189287A patent/BE869001A/en unknown
- 1978-07-14 IE IE1425/78A patent/IE47126B1/en unknown
- 1978-07-14 CA CA307,371A patent/CA1112572A/en not_active Expired
- 1978-07-14 GB GB7829921A patent/GB2000970B/en not_active Expired
- 1978-07-17 NL NL7807641A patent/NL7807641A/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
NL7807641A (en) | 1979-01-17 |
NZ187683A (en) | 1981-03-16 |
ZA783671B (en) | 1979-06-27 |
DE2829408A1 (en) | 1979-02-01 |
IL52533A (en) | 1980-01-31 |
AU3752578A (en) | 1980-01-03 |
ATA511878A (en) | 1980-05-15 |
FR2397191A1 (en) | 1979-02-09 |
IL52533A0 (en) | 1977-10-31 |
IE781425L (en) | 1979-01-15 |
GB2000970A (en) | 1979-01-24 |
AT360149B (en) | 1980-12-29 |
JPS5420125A (en) | 1979-02-15 |
FR2397191B1 (en) | 1981-12-31 |
GB2000970B (en) | 1982-03-17 |
CA1112572A (en) | 1981-11-17 |
BE869001A (en) | 1979-01-15 |
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