Application of HEPES |CAS 7365-45-9|in the field of medicine

HEPES is a zwitterionic buffer, belonging to good's buffer, with pKa 7.45 at 25℃ and pH buffer range of 6.8-8.2, so it is widely used in cell culture medium, IVD detection kits, cosmetics, medicine and other fields. This week, the editor of YACOO introduces the application of HEPES as a component of Irinotecan injection in the field of medicine.

ONIVYDE is a sterile, white to slightly yellow opaque isotonic liposomal dispersion. Irinotecan injection is indicated for the treatment of patients with metastatic adenocarcinoma of the pancreas whose disease has progressed on prior gemcitabine-based chemotherapy. Liposomes are unilamellar phospholipid bilayer vesicles approximately 110nm in diameter that surround an internal aqueous phase containing irinotecan in the form of a sucrose salt in a gel or precipitated state.

The finished product of irinotecan is a concentrate of an infusion solution containing 5mg/ml of irinotecan trihydrate (irinotecan sucrose salt) active substance encapsulated in liposomes. Other ingredients include the following two parts:

1.Lipids in the form of liposomes:  cholesterol, 1,2-distearoyl- SN-glycero-3-phosphocholine (DSPC),N-(carbonylmethoxy polyethylene glycol 2000) (DSPE-MPEG2000) -1,2-distearoyl-SN-glycerol-3- phosphoethanolamine sodium salt.

2.Other auxiliary materials: sucrose octasulfate salt, HEPES buffer, sodium chloride and water for injection.

Irinotecan hydrochloride trihydrate is present in liposomes in the form of irinotecan sucrose salt. The lipid membrane was composed of DSPC, cholesterol, and methoxy-terminated polyethylene glycol (MW 2000)- distearoylphosphatidylethanolamine (MPEG-2000-DSPE). Liposomes are dispersed in an aqueous buffer solution. Liposome formulations include: DSPC 6.81 mg/mL, cholesterol 2.22 mg/mL, and MPEG-2000-DSPE 0.12 mg/mL. Each ml also contains HEPES as buffer 4.05 mg/ml and sodium chloride as isotonic reagent 8.42 mg/ml.

References

CN108366965B Stabilized camptothecin pharmaceutical composition.