# US 4,399,127 A · Injectable oxytetracycline compositions

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- Number: US 4,399,127 A
- Document ID: US4399127A
- Status: Granted
- Kind: A
- Application number: 06/300,007
- Filed: 1981-09-08
- Granted: 1983-08-16
- Earliest claimed: 1980-04-10
- Assignees: Diamond Shamrock Corporation
- Inventors: Walter Hacke; Herman Horn
- Web page: https://patentgrep.com/patent/US4399127A

## CPC

- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 47/02: Inorganic compounds
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Increased antibiotic content of oxytetracycline injectable compositions containing glycerol formal as the solvent is achieved by utilization of particular magnesium compounds, viz., magnesium oxide, magnesium hydroxide, magnesium carbonate, magnesium acetate and magnesium chloride. Magnesium chloride is utilized with oxytetracycline base only.

## Claims

### Claim 1

A stable, injectable antibiotic composition of increased antibiotic concentration for parenteral administration comprising:
(a) from about 15 to about 35 parts by weight of an antibiotic selected from the group consisting of oxytetracycline base and an acid addition salt thereof,
(b) a magnesium compound selected from the group consisting of magnesium oxide, magnesium hydroxide and magnesium carbonate present in a molar ratio from about 0.8 to about 1.2 moles per mole of said antibiotic,
(c) from about 50 to about 95 parts by weight of glycerol formal selected from the group consisting of 4-hydroxymethyl-1,3-dioxolane, 5-hydroxy-1,3-dioxane and mixtures thereof,
(d) from about 10 to about 45 parts by weight of water,
(e) an antioxidant in an amount sufficient to stabilize said composition, and
(f) a buffering agent in an amount sufficient to provide a pH of from about 6 to about 9.5 in said composition.

### Claim 2 (depends on 1)

The composition of claim 1 wherein said antibiotic is oxytetracycline base, said magnesium compound is magnesium oxide and said glycerol formal is a mixture of 4-hydroxymethyl-1,3-dioxolane and 5-hydroxy-1,3-dioxane.

### Claim 3 (depends on 1)

The composition of claim 1 wherein said antibiotic is oxytetracycline hydrochloride, said magnesium compound is magnesium oxide and said glycerol formal is a mixture of 4-hydroxymethyl-1,3-dioxolane and 5-hydroxy-1,3-dioxane.

### Claim 4 (depends on 2)

The composition of claim 2 wherein the mole ratio of said magnesium compound to said oxytetracycline base is about 1 to 1.

### Claim 5 (depends on 4)

The composition of claim 4 wherein the amount of oxytetracycline base present is about 20 % by weight of the total composition.

### Claim 6 (depends on 3)

The composition of claim 3 wherein the mole ratio of said magnesium compound to said oxytetracycline hydrochloride is 0.8 to 1.

### Claim 7 (depends on 1)

The composition of claim 1 wherein said antioxidant is sodium formaldehydesulfoxylate.

### Claim 8 (depends on 1)

The composition of claim 1 wherein said buffering agent is monoethanolamine.

### Claim 9 (depends on 1)

The composition of claim 1 wherein substantially all particles thereof are smaller than 0.20 microns.