Sugammadex sodium is a selective neuromuscular blocker antagonist that is used to reverse the effects of non-depolarizing neuromuscular blocking medicines such as rocuronium and vecuronium during surgery. It works by encapsulating the steroidal structure of the blocking medicines within its lipophilic core, inactivating the medicines and stopping them from binding to nicotinic acetylcholine receptors at the motor end plate. This article discusses the preparation of amorphous sugammadex sodium.
Properties of Sugammadex Sodium
Chemically, sugammadex sodium is referred to as (3R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile;phosphoric acid. Its molecular formula is C17H21N6O4P and molecular weight is 404.4 g/mol. Sugammadex sodium is a white to off-white powder that is freely soluble in water.
As the phosphate salt form, sugammadex sodium exhibits improved aqueous solubility and bioavailability compared to the free base. This property makes it suitable for formulation into oral and injectable dosage forms.
Manufacturers of Sugammadex Sodium
There are multiple manufacturers worldwide that supply sugammadex sodium. Some major sugammadex sodium manufacturers and their country of origin are listed in the table below:
| Company | Country |
|---|---|
| Sichuan Qingmu Pharmaceutical Co., Ltd. | China |
| Ningbo Menovo Pharmaceutical Co., Ltd. | China |
| Zhejiang Jiangshan Pharmaceutical Co., Ltd. | China |
| Cambrex Karlskoga AB | Sweden |
| Hangzhou Adways Biotechnology Co., Ltd. | China |
| Meenaxy Pharma Pvt. Ltd. | India |
Preparation of Amorphous Sugammadex Sodium
Conventional methods for producing sugammadex sodium yield crystalline products with distinct X-ray diffraction peaks. However, amorphous sugammadex sodium offers advantages such as improved solubility and dissolution rate. The Chinese patent CN109053933B describes a method for preparing amorphous sugammadex sodium without using alcohol solvents.
The method involves stirring an aqueous solution of sugammadex sodium and adding a non-alcoholic solvent such as 1,4-dioxane or tetrahydrofuran. Crystallization yields an amorphous product as verified by X-ray diffraction which shows no distinct peaks. Concentrating the sugammadex sodium solution to dryness is an alternative method. Process parameters like concentration, solvent dosage, temperature and stirring speed can be adjusted.
Compared to methods using alcohol crystallization, this process avoids potential clarity issues from insoluble residues and allows safer production of injectable sugammadex sodium formulations. It provides raw material of consistent quality meeting regulatory standards.
In summary, this article discussed the key properties of sugammadex sodium, its major global manufacturers and suppliers, and an optimized method for preparing amorphous sugammadex sodium. The amorphous form produced avoids quality issues associated with alcohol-based crystallization and ensures stable performance of sugammadex sodium-containing medicines.
