Injection grade histidine (H-116) and hydrochloride (H-117)

PfanstiehlInjection grade histidine (H-116) and hydrochloride (H-117)

Histidine and histidine hydrochloride often work synergistically in biopharmaceutical formulations, jointly ensuring the stability, safety, and efficacy of drugs. Their applications cover various dosage forms from liquid formulations to freeze-dried formulations, and they are important excipients in modern biopharmaceutical research and production. Among the monoclonal antibodies that have been approved for marketing, more than40%The formulation added histidine and histidine hydrochloride, such as“KPabolilizumab Injection（Keytruda）, as well as Daretomumab Injection（Darzalex）Sikuximab Injection（Cosentyx）Wait.The main applications of histidine and histidine hydrochloride in biopharmaceuticals include the following aspects.

1. pHBuffering agent

Histidine is a widely used amino acid buffer in monoclonal antibody preparationspHThe buffer range is5.5-6.5Histidine is usually used in combination with histidine hydrochloride to maintain the solutionpHStable and can significantly reduce protein aggregation. Especially at high temperatures（40-57The stability of antibodies can still be maintained under the same temperature (℃) environment. Studies have shown that under the same conditionspHUnder the conditions of value and ionic strength, the hydrolysis rate of the hinge region is lower when using histidine as a buffer compared to phosphate.

2. Protein Stabilizer

Histidine maintains the stability of the protein's natural conformation by binding to specific residues on the protein surface, preventing denaturation under conditions such as high temperature and mechanical stress. In addition, histidine can also shield hydrophobic regions on protein surfaces, reduce the tendency of protein molecules to aggregate, lower solution viscosity, and improve the physical stability of formulations.

3. Freeze drying protection

Histidine can form a glassy matrix during freeze-drying, encapsulating protein molecules and limiting their migration and aggregation, thereby protecting the structure and activity of proteins. It can replace water molecules to form hydrogen bonds with polar groups on the surface of proteins, reducing the risk of protein denaturation during the drying process, especially playing an important role in low-temperature freezing and drying stages.

4. antioxidant

The imidazole side chain of histidine has a unique chemical structure that can directly scavenge reactive oxygen species such as hydroxyl radicals and singlet oxygen in solution, reducing protein oxidative damage caused by free radicals. In addition, some trace metal ions (such as copper, iron, etc.) can also pass throughFentonCatalytic free radical generation through reaction and other pathways accelerates protein oxidation. Histidine can form stable complexes with metal ions, reducing their activity and thereby inhibiting the production of free radicals, indirectly exerting antioxidant effects.

5. Promoting solvent

The imidazole group of histidine can interact with hydrophobic regions on the surface of protein molecules, increasing protein solubility and helping to prevent protein precipitation due to hydrophobic aggregation, maintaining its stability and solubility in solution. Histidine can also form hydrogen bonds with polar groups (such as amino, carboxyl, hydroxyl, etc.) in protein molecules, increasing the interaction between proteins and water molecules, thereby improving protein solubility.

Pfanstiehl's histidineH-116Histidine hydrochlorideH-117It is developed specifically for injectable biomacromolecule drugs, with ultra-high purity, ultra-low endotoxin, ultra-low metal ion content, and high-quality injection grade excipients that comply with multiple pharmacopoeias. Whether it is global declaration or the development of increasingly complex biopharmaceutical formulations,PfanstiehlThey can all provide solid guarantees.

Pfanstiehl's histidineH-116Histidine hydrochlorideH-117The advantages mainly include the following aspects:

• conform toUSP, EP, BP, JP, ChPMulti country pharmacopoeia;

• Ultra high purity, ultra-low endotoxin, ultra-low microbial content;

• Low metal residue,29Detect metal ions separately, all as low asppbLevel;

• Detecting residues of lipase, protease, and phosphatase;

• detectionDNATheRNATheDNaseTheRNaseresidual;

• Detecting nitrite residues;

• Detecting β-Glucansresidual;

• DMF/CDE filing,CDEstatusA.

PfanstiehlInjection grade histidine (H-116) and hydrochloride (H-117)

Product Information

PfanstiehlHistidine and histidine hydrochloride are currently selling well in stock,If you are interested in the above products, please feel free to contact usPfanstiehlBeijing Ximeijie Technology Co., Ltd., the agent in China, obtained detailed product overview documents and applied for test samples.

Beijing Ximeijie Technology Co., LtdPfanstiehlChinese agent, providing customers with * technical support and after-sales service.Beijing Ximeijie is the agent of Pfanstiehl, the agent of Pfanstiehl in China, the agent of Pfanstiehl in Beijing, the general agent of Pfanstiehl, and the agent of Pfanstiehl in Shanghai, ， Pfanstiehl Northwest Agent, Pfanstiehl Southwest Agent, Pfanstiehl Northeast Agent, Pfanstiehl North China Agent, Pfanstiehl South China Agent, Pfanstiehl Central China Agent, responsible for Pfanstiehl's related business in China.