IE47126B1 - An injectable chloramphenicol composition - Google Patents

An injectable chloramphenicol composition

Info

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
Application number
IE1425/78A
Other versions
IE781425L (en
Original Assignee
Abic Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Abic Ltd filed Critical Abic Ltd
Publication of IE781425L publication Critical patent/IE781425L/en
Publication of IE47126B1 publication Critical patent/IE47126B1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable 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)

Claims
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,
IE1425/78A 1977-07-15 1978-07-14 An injectable chloramphenicol composition IE47126B1 (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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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