Octreotide acetate injection and preparation process thereof

Abstract

The invention belongs to the field of pharmaceutical preparations and provides an octreotide acetate injection and a preparation process thereof. According to the octreotide acetate injection provided by the invention, each 50000mL of the injection is prepared from the following components: 5.0g of octreotide acetate, 169.3g of lactic acid, 2200.0g to 2300.0g of mannitol, a proper amount of sodium hydrogen carbonate and the balance of injection water; the pH (Potential of Hydrogen) value of the octreotide acetate injection is 4.0 to 4.2. The preparation process provided by the invention is carried out under a sterile condition, and the pH value and temperature of the solution are controlled; a special material preparation system, and steps of magnetically stirring and carrying out secondary sterilization and filtering are adopted. The prepared injection can be preserved at room temperature for 6 months and can be refrigerated and preserved for 4 years; the octreotide acetate injection has good safety and the product is convenient to convey and distribute. The process provided by the invention is developed, has controllable quality and relatively low energy consumption and is economical and practical. The safe, effective and high-quality octreotide acetate injection is provided for clinical utilization.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an octreotide acetate injection and a preparation process thereof. Background technique [0002] Octreotide Acetate as D-Phenylalanyl-L-Cysteinyl-L-Phenylalanyl-D-Tryptophanyl-L-Lysyl-L-Threonyl-N-[2-Hydroxy-1 -(Hydroxymethyl)propyl]-L-cysteinamide ring (2→7)-disulfide bond acetate, based on anhydrous and acetic acid-free substances, containing octreotide (C 49 h 66 N 10 o 10 S 2 ) should be 95.0% to 102.0%. [0003] This product is the only gastrointestinal hormone analog that has been successfully used in treatment so far. It is a synthetic octapeptide containing a ring structure, and its partial amino acid sequence is similar to that of somatostatin. It has almost all the biological effects of somatostatin, such as inhibiting multiple A pituitary and gastrointestinal pancreatic hormone release, inhibit gastric acid, pancreatic juice and bile secreti...

AI Technical Summary

Problems solved by technology

However, because the acidity of lactic acid is stronger than that of acetic acid, the lactic acid pH regulator added in the octreotide acetate freeze-dried preparation makes part of the acetate free out of acetic acid, and part of the free acetic acid will be taken away during the freeze-drying and vacuum pumping process, and the acetic acid content will be reduced. , leading to faster growth of related substances and lower stability, thereby increasing the risk of the production process; octreotide acetate will inevitably be denatured or degraded during the freeze-drying process, resulting in the loss of part of the activity and the reduction of biological activity; freeze-drying in the production process The process will lead to increased scrap rate and cost, and correspondingly increase the economic burden of patients

[0007] The process risk of the freeze-dried composition of octreotide acetate for injection is high, and it will be denatured or degraded during the freeze-drying process. It is safer and more economical to prepare octreotide acetate into injection, but the stability of octreotide acetate injection in the prior art is poor at room temperature. short storage time

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