GB845454A - Preparation of improved tetracycline antibiotic compositions - Google Patents
Preparation of improved tetracycline antibiotic compositionsInfo
- Publication number
- GB845454A GB845454A GB18163/57A GB1816357A GB845454A GB 845454 A GB845454 A GB 845454A GB 18163/57 A GB18163/57 A GB 18163/57A GB 1816357 A GB1816357 A GB 1816357A GB 845454 A GB845454 A GB 845454A
- Authority
- GB
- United Kingdom
- Prior art keywords
- pyridine
- alkaline earth
- methyl
- nicotinamide
- hydrogen
- 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.)
- Expired
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
- A61K31/65—Tetracyclines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pyridine Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A tetracycline antibiotic is solubilised in aqueous solution by the addition of a soluble non-toxic source of alkaline earth ions and a pyridine derivative having the formula: <FORM:0845454/IV(b)/1> wherein R is hydrogen or a N-alkylcarbamyl, N-alkanolcarbamyl, hydrazinocarbonyl, hydroxyl, hydroxyalkyl, alkoxycarbonyl or carboxyl radical or a salt of a carboxyl group with a soluble non-toxic metal; R1 is hydrogen or a methyl group and R11 and R111 are each hydrogen or a hydroxymethyl group. The tetracycline antibiotic is tetracycline, chlortetracycline, oxytetracycline, bromtetracycline or soluble salts thereof such as the hydrochloride and sulphate. Sources of alkaline earth ions are the chloride, sulphate, citrate, ascorbate, pantotherate, gluconate and lactate of calcium or magnesium. The alkaline earth ion and the pyridine derivative may be combined, e.g. magnesium nicotinate. One or more pyridine derivatives may be present. Examples are nicotinamide, isonicotinamide, N-ethanol nicotinamide, N-methyl nicotinamide, picolinamide, nicotinic acid hydrazide, isonicotinic acid hydrazide, methyl nicotinate, methyl isonicotinate, sodium nicotinate, pyridoxine hydrochloride, 4-propanol pyridine and 2-propanol pyridine. The molecular ratio of tetracycline antibiotic : alkaline earth ions : pyridine compound is at least 1:1:4 or 1: 1/2 :40 and is preferably 1:2.5:8. Specification 793,558 is referred to.ALSO:A tetracycline antibiotic composition of enhanced solubility and stability which is, or is adapted on addition of water to provide, a clear aqueous solution and comprises a tetracycline antibiotic, a soluble non-toxic source of alkaline earth ions, and a pyridine derivative having the formula: <FORM:0845454/VI/1> wherein R is hydrogen or a N-alkylcarbamyl, N-alkanolcarbamyl, hydrazinocarbonyl, hydroxyl, hydroxyalkyl, alkoxycarbonyl, or carboxyl radical or a salt of a carboxyl group with a soluble non-toxic metal; R1 is hydrogen or a methyl group and R11 and R111 are each hydrogen or a hydroxy-methyl group. The tetracycline antibiotic is tetracycline, chlortetracycline, oxytetracycline, bromtetracycline or soluble salts thereof such as the hydrochloride and sulphate. sources of alkaline earth ions are the chloride, sulphate, citrate, ascorbate, pantothenate, gluconate and lactate of calcium or magnesium. The alkaline earth ion and the pyridine derivative may be combined e.g. magnesium nicotinate. One or more pyridene derivatives may be present. Examples thereof are nicotinamide, isonicotinamide, N-ethanol nicotinamide, N-methyl nicotinamide, picolinamide, nicotinic acid hydrazide, isonicotinic acid hydrazide, methyl nicotinate, methyl isonicotinate, sodium nicotinate, pyridoxine hydrochloride, 4-propanol pyridine and 2-propanol pyridine. The molecular ratio of tetracycline: alkaline earth ions: pyridine compound is at least 1:1:4 or 1: 1/2 :40 and is preferably 1:2,5:8. For parenteral administration there may be present a soluble, non-toxic alpha hydroxy acid or a salt thereof. Other additions are (a) anaesthetic e.g. procaine (b) analgesic e.g. antipyrine (c) stabiliser e.g. sodium sulphite. Specification 793,558 is referred to.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US845454XA | 1956-06-27 | 1956-06-27 |
Publications (1)
Publication Number | Publication Date |
---|---|
GB845454A true GB845454A (en) | 1960-08-24 |
Family
ID=22185643
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
GB18163/57A Expired GB845454A (en) | 1956-06-27 | 1957-06-07 | Preparation of improved tetracycline antibiotic compositions |
Country Status (1)
Country | Link |
---|---|
GB (1) | GB845454A (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0052705A1 (en) * | 1980-11-24 | 1982-06-02 | Joel E. Bernstein, M.D. | Composition for treating acne vulgaris |
US9084802B2 (en) | 2010-05-12 | 2015-07-21 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
-
1957
- 1957-06-07 GB GB18163/57A patent/GB845454A/en not_active Expired
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0052705A1 (en) * | 1980-11-24 | 1982-06-02 | Joel E. Bernstein, M.D. | Composition for treating acne vulgaris |
US9084802B2 (en) | 2010-05-12 | 2015-07-21 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
US9278105B2 (en) | 2010-05-12 | 2016-03-08 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
US9744179B2 (en) | 2010-05-12 | 2017-08-29 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
US11944634B2 (en) | 2010-05-12 | 2024-04-02 | Melinta Subsidiary Corp. | Tetracycline compositions |
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