IE781425L - Injectable chloroamphenicol solution - Google Patents

Injectable chloroamphenicol solution

Info

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
Application number
IE781425A
Other versions
IE47126B1 (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

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.
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 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)

* 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
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)

* 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
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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