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OwnerFang Yu Lee, Shan Chiung Chen +2inventors
InventorsFang Yu Lee, Shan Chiung Chen, Bin Ken Chen, Chiung Ju Tsai
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The present invention provides a stable pharmaceutical composition which contains an acetic acid class of non-steroidal anti-inflammatory drug (NSAID), a phosphate solution, an isotonic agent, and water. The pharmaceutical composition is particularly suitable for parenteral injection such as intravenous or intramuscular injection. The preferred NSAID is ketorolac tromethamine, which includes any racemic mixture of [−]S and [+]R ketorolac tromethamine. The preferred phosphate solution contains sodium phosphate monobasic (NaH2PO4) or potassium phosphate monobasic (KH2PO4), with or without crystalline water. The preferred isotonic agent is NaCl. The pharmaceutical composition is preferably at pH 6.0 to 8.5 and with osmolarity within 0.5 to 3.
An injectable pharmaceutical composition comprising
A stable pharmaceutical composition comprising:
Dependencies are inferred from the claim text.
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Carboxylic acids, e.g. valproic acid: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
Galenical forms characterised by the site of application: injectable compositions; Intramuscular, intravenous, arterial, subcutaneous…
Medicinal preparations characterised by special physical form: solutions
Medicinal preparations containing antigens or antibodies: allergens
Term end not estimated
The present invention relates to an injectable pharmaceutical composition which contains an acetic acid class of non-steroidal anti-inflammatory drug (NSAID), a phosphate solution, an isotonic agent, and water; in particular, ketorolac tromethamine is the preferred NSAID, sodium phosphate monobasic (NaH2PO4) or potassium phosphate monobasic (KH2PO4), anhydrous or with hydrates, is the preferred phosphate for the phosphate solution, and NaCl is the preferred isotonic agent. The pharmaceutical composition is preferably at pH 6.0 to 8.5 and with osmolarity within 0.5 to 3 Osm. The present invention also relates to a method for preparing the injectable pharmaceutical composition. The injectable pharmaceutical composition of the present invention is stable and suitable for parenteral injection.
Non-steroidal anti-inflammatory drugs (NSAIDs) are a family of drugs that generally have analgesic, antipyretic, and anti-inflammatory activities. These activities derive from a common mechanism: the inhibition of cyclooxygenase, which is the critical enzyme for biosynthesis of prostaglandins, prostacyclin, and thromboxanes. Because prostaglandins are released in response to inflammatory stimuli, which in turn result in inflammatory responses (e.g., redness, pain, heat and swelling of tissue), inhibition of prostaglandins by NSAIDs results in analgesia. In the central nervous system, NSAIDs are antihyperalgesic through a direct action on the spinal cord.
Two NSAIDs, ketorolac and diclofenac, both belong to the acetic acid class of NSAIDs, are comparable to opioids in terms of providing pain relief. For example, the overall analgesic effect of 30 mg of ketorolac is equivalent to that of 6 to 12 mg of Morphine.
The pharmaceutical composition of the present invention was prepared as follows: 2 Ketorolac tromethamine 1800 g KH2PO4 300 g NaCl 261 g NaOH or HCl Adequate amount Water for Injection qs to 60 L
Procedures:
(1) Add KH2PO4 to 50 L of water; stir until KH2PO4 is dissolved.