GB2063669A - Injectable solutions of sodium dicloxacillin - Google Patents
Injectable solutions of sodium dicloxacillin Download PDFInfo
- Publication number
- GB2063669A GB2063669A GB8037236A GB8037236A GB2063669A GB 2063669 A GB2063669 A GB 2063669A GB 8037236 A GB8037236 A GB 8037236A GB 8037236 A GB8037236 A GB 8037236A GB 2063669 A GB2063669 A GB 2063669A
- Authority
- GB
- United Kingdom
- Prior art keywords
- pvp
- dicloxacillin
- molecular weight
- compositions
- composition
- 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.)
- Granted
Links
- SIGZQNJITOWQEF-VICXVTCVSA-M dicloxacillin sodium monohydrate Chemical compound O.[Na+].N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C([O-])=O)=O)C(=O)C1=C(C)ON=C1C1=C(Cl)C=CC=C1Cl SIGZQNJITOWQEF-VICXVTCVSA-M 0.000 title claims abstract description 20
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 48
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 48
- 239000000203 mixture Substances 0.000 claims abstract description 43
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 19
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229940102223 injectable solution Drugs 0.000 claims abstract description 11
- YFAGHNZHGGCZAX-JKIFEVAISA-N dicloxacillin Chemical class N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=C(Cl)C=CC=C1Cl YFAGHNZHGGCZAX-JKIFEVAISA-N 0.000 claims description 10
- 239000002253 acid Substances 0.000 claims description 8
- 239000000243 solution Substances 0.000 claims description 8
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 claims description 6
- 229930182555 Penicillin Natural products 0.000 claims description 4
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 claims description 4
- 238000009472 formulation Methods 0.000 claims description 4
- 239000004615 ingredient Substances 0.000 claims description 4
- 229940049954 penicillin Drugs 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- 229920003081 Povidone K 30 Polymers 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000003125 aqueous solvent Substances 0.000 claims description 2
- 229960001585 dicloxacillin Drugs 0.000 claims description 2
- 238000005227 gel permeation chromatography Methods 0.000 claims description 2
- 239000011521 glass Substances 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 239000000463 material Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 239000000178 monomer Substances 0.000 claims description 2
- 229920000642 polymer Polymers 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
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
- A61K9/0012—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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A pharmaceutical composition, which on reconstitution with water yields an injectable solution, which composition comprises sodium dicloxacillin, and polyvinylpyrrolidone of molecular weight 1000 to 50,000.
Description
SPECIFICATION
Injectable penicillin formulations
This invention relates to an injectable penicillin
formulation.
More specifically this invention relates to an
injectable sodium dicloxacillin composition which
has improved solubility at higher injection strengths
and at lower temperatures.
Accordingly the present invention provides a
pharmaceutical composition, which on reconstitution with water yields an injectable solution, which com
position comprises sodium dicloxacillin, and
polyvinylpyrrolidone of molecular weight 1000 to 50,000.
The polyvinyl pyrrolidone (hereinafter referred to
as PVP) used in the composition of this invention has
a molecular weight of from 1000 to 50,000. Since the
material is a polymer it will be realised by a chemist that the molecular weight referred to is an average
molecular weight. A suitable method of determining
the average molecular weight of PVP for use in this
composition is gel permeation chromatography. The
PVP should not contain molecules with molecular weight of more than 60,000 similarly it should not
have a monomer content of more than 1%. The K
value of suitable PVP will generally be between 10
and 18.
Favourably the PVP employed will have a molecu
larweight of 1000 to 12,000 more suitably 1500 to
6000.
A preferred PVP for use in the composition will
have a molecular weight of 2000 to 3500. A PVP of this kind is Kollidon CE 5080 (Kollidon is a Registered
Trade Mark) which is available from BASF
Aktiengesselschaft, D-6700 Ludwigshafen, Federal
Republic of Germany. This PVP has a K value of 12 to
14, which is a favoured range.
Normally the weight ratio of the dicloxacillin salt
(taken as the free acid equivalent weight) to PVP in the compositions of the invention will be 10:1 to 1:5,
more suitably 2:1 to 1:3.
The compositions of this invention may be reconstituted with an aqueous solvent, for example water,
in conventional manner, the ingredients either being
dissolved simultaneously or consecutively.
Normally sufficient composition will be dissolved to provide a solution containing 50 to 200 mg/ml of .s$icloxacillin (as free acid), more suitably 100 to 150
mg/ml.
One particularly useful aspect of the invention is
an injectable solution containing 125 to 200 mg/ml of sodium dicloxacillin (as free acid), and PVP. Prefer
ably such solutions contain 125 or 150 mg/ml of active ingredient.
The compositions ofthe invention may be presented in any convenient manner. For example a
mixture of the sodium dicloxacillin and the PVP may
be filled into a single container, such as a glass vial.
Alternatively the compositions may be presented as twin packs or the like, in which for example the sodium dicloxacillin and the PVP are in different
parts of the pack -- in such an embodiment of course the PVP may be presented in aqueous solution so that the composition may simply be reconstituted by mixing together the parts of the pack.
It will be appreciated that as the compositions of the invention are to be used only after reconstitution into a solution, then the exact physical form of the dicloxacillin salt and the PVP in the (dry) compositions in unimportant although they will conveniently be in powder form.
The following Examples illustrate this invention.
EXAMPLE 1
The following Compositions were prepared by mixing together the stated ingredients in the stated proportions. The PVP used was Kollidon CE 5080 in
Compositions 1 to 5 and Kollidon 30 (also available from BASF, molecularweight40000) in Compositions 6 and 7.
Composition Wt. of sodium Wt. of PVP Number dicloxacillin mg.
(p.f.a.), mg.
1 300 100 2 300 200 3 300 300 4 300 400 5 300 500 6 300 200 7 300 400 EXAMPLE2
The Compositions prepared in Example 1 were each dissolved in sufficient water to give 2 mls of clear solution having a sodium dicloxacillin concentration (as free acid) of 150 mg/ml.
1. A pharmaceutical composition, which on reconstitution with water yields an injectable solution, which composition comprises sodium dicloxacillin, and polyvinylpyrrolidone of molecular weight
1000 to 50,000.
2. A pharmaceutical composition as claimed in claim 1 wherein the polyvinylpyrrolidone has molecular weight of 1000 to 12000.
3. A pharmaceutical composition as claimed in claims 1 or 2 wherein the polyvinylpyrrolidone has molecular weight of 1500 to 6000.
4. A pharmaceutical composition as claimed in any one of claims 1 to 3 wherein the weight ratio of dicloxacillin salt to polyvinylpyrrolidone is in the range 10:1 to 1:5.
5. A pharmaceutical composition as claimed in any one of claims 1 to 4, wherein the weight ratio of dicloxacillin salt to polyvinylpyrrolidone is in the
range 2:1 to 1:3.
6. A pharmaceutical composition as claimed in any one of claims 1 to 5, which on reconstitution with water provides an injectable solution containing 125-200 mg/ml of sodium dicloxacillin.
7. A pharmaceutical composition as claimed in
any one of claims 1 to 6, which on reconstitution with water provides an injectable solution containing 125 - 150 mg/ml of sodium dicloxacillin.
8. A pharmaceutical composition as claimed in any one of claims 1 to 5 wherein thedicloxacillin salt
**WARNING** end of DESC field may overlap start of CLMS **.
Claims (8)
1. A pharmaceutical composition, which on reconstitution with water yields an injectable solution, which composition comprises sodium dicloxacillin, and polyvinylpyrrolidone of molecular weight
1000 to 50,000.
2. A pharmaceutical composition as claimed in claim 1 wherein the polyvinylpyrrolidone has molecular weight of 1000 to 12000.
3. A pharmaceutical composition as claimed in claims 1 or 2 wherein the polyvinylpyrrolidone has molecular weight of 1500 to 6000.
4. A pharmaceutical composition as claimed in any one of claims 1 to 3 wherein the weight ratio of dicloxacillin salt to polyvinylpyrrolidone is in the range 10:1 to 1:5.
5. A pharmaceutical composition as claimed in any one of claims 1 to 4, wherein the weight ratio of dicloxacillin salt to polyvinylpyrrolidone is in the
range 2:1 to 1:3.
6. A pharmaceutical composition as claimed in any one of claims 1 to 5, which on reconstitution with water provides an injectable solution containing 125-200 mg/ml of sodium dicloxacillin.
7. A pharmaceutical composition as claimed in
any one of claims 1 to 6, which on reconstitution with water provides an injectable solution containing 125 - 150 mg/ml of sodium dicloxacillin.
8. A pharmaceutical composition as claimed in any one of claims 1 to 5 wherein thedicloxacillin salt and the polyvinylpyrrolidone are in powder form.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8037236A GB2063669B (en) | 1979-11-27 | 1980-11-20 | Injectable solutions of sodium dicloxacillin |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB7940908 | 1979-11-27 | ||
| GB8037236A GB2063669B (en) | 1979-11-27 | 1980-11-20 | Injectable solutions of sodium dicloxacillin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB2063669A true GB2063669A (en) | 1981-06-10 |
| GB2063669B GB2063669B (en) | 1984-02-15 |
Family
ID=26273696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB8037236A Expired GB2063669B (en) | 1979-11-27 | 1980-11-20 | Injectable solutions of sodium dicloxacillin |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2063669B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0125725A1 (en) * | 1983-05-09 | 1984-11-21 | Gist-Brocades N.V. | Oxytetracyclin solutions |
-
1980
- 1980-11-20 GB GB8037236A patent/GB2063669B/en not_active Expired
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0125725A1 (en) * | 1983-05-09 | 1984-11-21 | Gist-Brocades N.V. | Oxytetracyclin solutions |
Also Published As
| Publication number | Publication date |
|---|---|
| GB2063669B (en) | 1984-02-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PCNP | Patent ceased through non-payment of renewal fee |