Triprorelin acetate is an acetate of triprorelin, the active ingredient of which is triprorelin, a synthetic highly potent agonist analogue that was first marketed in Germany in 1986. In order to improve bioavailability, many salts increase solubility and improve bioavailability. Therefore, the pharmacological effects and adverse reactions of the two are consistent. Triprerelin acetate is available in two dosage forms: injection and slow-release preparation. Triprerelin acetate is a 5-oxo-prolinyl-L-histaminoyl-L-trypanoyl-l-tyrosyl-d-trypanoyl-l-leucoyl-l-arginoyl-l-prolinyl-l-glycinamide acetate with molecular formula C64H82N18O13.XC2H4O2 and molecular weight 1311.46.X60.02. According to the calculation of no Chemicalbook water and no acetic acid, the content of C64H82N18O13 should be 97.0% ~ 103.0%. The active component of triprerelin acetate is the analogue of synthetic gonadotropin releasing hormone, and its structural improvement is to replace the sixth L-glycine in the natural molecular structure with D-tryptophan, so that its promoting effect is more significant and the plasma halftime is longer. After injection, the drug initially stimulates the pituitary gland to release luteinizing hormone and oocyte maturation hormone. When the pituitary gland enters the refractory period after prolonged stimulation, the release of gonadotropin is reduced, thus reducing the sex steroids to castrating levels. These effects are reversible. Subcutaneous administration of the drug was rapidly absorbed, the plasma concentration reached the peak 15-60min, and the maximum effect reached 1h. Intramuscular injection of the sustained-release preparation could maintain the curative effect for more than 28d.
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