MCE | 助溶劑 (Co-Solvents) : 協助藥物溶解的「魔法藥劑」

MCE | 助溶劑 (Co-Solvents) : 協助藥物溶解的「魔法藥劑」

2025.01.01

MedChemExpress-Master of Small Molecules (Inhibitors. Screening Libraries. Proteins)

What are Co-solvents?

Currently, over 70% of drugs are screened for poor aqueous solubility, which can result in low oral bioavailability, low half-life, poor tissue distribution, fast pre-systemic metabolism, high dosages, potential toxicity and difficulties in formulation[1][2]. Therefore, in the process of drug development and use, increasing drug solubility is the key to the effective action of drugs.

Co-solvents are a substance incorporated during the dissolution process that can improve the solubility of drugs. They are usually low molecular weight compounds. Their mechanism of action typically involves the formation of water-soluble complexes, or double salts between drugs and small molecule substances. Common co-solvents include oils, cyclodextrins, solvents, multi-component compounds, polymers, etc.

How to Choose your Co-Solvent?

Consulting and referencing literature for dissolution solutions can assist with selecting the correct co-solvent for your drug. MedChemExpress provides a selection of co-solvents, in which we can suggest the appropriate substance for your molecule:

Drugs with lipidsolubility may require lipid co-solvents for improved solubility, such as: lipid co-solvents (e.g. Corn oil); Cyclodextrins (e.g. SBE-β-CD). They can also be used for various administration routes, such as intraperitoneal, intragastric, and intravenous (clear) administration;

CMC-Na can be used for intraperitoneal and gastric lavage; Lipids (e.g. Corn oil) are commonly used for intraperitoneal and gavage administration due to their relative viscosity and suitability for shorter dosing cycles;

PEG300 has the advantages of low immunogenicity and low viscosity, commonly used for intraperitoneal administration;

Mixing surfactants and other co solvents can be used for Intraperitoneal injection or oral administration;

Phosal 50 PG can be used for oral administration.

Figure 1. Conventional methods for solubility enhancement[3].

Advantages of MedChemExpress’s Co-solvent

• Provide a full range of co-solvent,100+ in total

• Through endotoxin testing, suitable for in vivo experiments

• Detailed dissolution plan

• Comprehensive QC system

MedChemExpress Products

Drug Name

Description

SBE-β-CD

A sulfobutylether β-cyclodextrin derivative used as an excipient or a formulating agent to increase the solubility of poorly soluble agents.

DMSO

An aprotic solvent that dissolves polar and non-polar compounds.

PEG300

A water-soluble, low immunogenic and biocompatible polymer formed by repeating units of ethylene glycol.

Corn Oil

Extracted from the germ of corn, can be used as a carrier for agent molecules.

Phosal 50 PG

A co-solvent (standardised phosphatidylcholine concentrate).

Tween 20

A surfactant reduce bacterial attachment and inhibit biofilm formation.

Methyl-β-cyclodextrin

A cyclic heptasaccharide used to deliver hydrophobic agents based on its property of solubilizing non-polar substances.

Poloxamer 407 (F127)

It is a nonionic surfactant that is relatively non-toxic to cells at low concentrations.

Sodium carboxymethyl cellulose (CMC-Na)

A  co-solvent that can be used as viscous agent, paste and barrier agent.

References:

[1] SNCHES B M A, et al. Int J Pharm, 2019, 568: 118498.
[2] GOKE K, et al. Eur J Pharm Biopharm, 2018, 126: 40-56.
[3] Kumari L, et al. Life (Basel). 2023;13(5):1099.

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