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Desheng talks about the development and utilization prospect of carbomer
The use of carbomer in oral protein drug preparations is also of great significance to the oral absorption of protein drugs. According to reports, carbomer can complex Ca2+ and Zn2+, and these two ions are the coenzymes of Typsin and Carboxypeptise A, respectively. , Thus the activity of the enzyme is inhibited; and carbomer has a large number of amino groups, which releases protons in the intestinal tract to form local acidity and inhibit the activity of microbial proteases. Because carbomer can complex Ca2+, improve the permeability of cell membrane, thereby promoting drug absorption.
Researchers have found that Carbomer 934P, 971P and 974P can strongly inhibit the proteolytic activity of microorganisms in the colon against insulin, calcitonin and insulin-like growth factor 1. In normal saline, 1% and 4% carbomer almost 100% inhibit the degradation of insulin by trypsin and chymotrypsin, but in Tris buffer, carbomer has almost no inhibitory effect. This is because it inhibits protein degradation by acidifying the environment of the medium to lower than the ideal pH value for enzyme activity. It is also reported that microemulsion containing carbomer 940 can increase the intestinal absorption of desmopressin, salmon calcitonin, etc., because carbomer wraps around the milk droplets to increase the adhesion time between the milk droplets and the intestinal wall mucosa At the same time, carbomer's protease inhibition and absorption promotion are also conducive to drug absorption. Carbomer can be used as an effective carrier for oral protein drugs, and it provides a good solution to the problem of low oral bioavailability of such drugs.
Application and utilization of carbomer in other dosage forms:
Carbomer can effectively inhibit the activity of colonic protease and increase the viscosity of the mucosa. It has been made into a colon-based drug delivery system. The use of carbomer in transdermal preparations can provide a uniform and stable system. Using 2% carbomer 934P and 940 as the drug dispersion gel matrix to prepare Ketoprofen (Ketoprofen) transdermal drug delivery system, the drug permeability can be increased by selecting a penetration enhancer. Since carbomer can improve the permeability of the mucosa, it can often be used to improve the bioavailability of drugs in ophthalmic and nasal preparations. In addition, carbomer can also be used as a binder and taste masking agent for granules.
Carbomer gel adheres to mucous membranes due to the formation of hydrogen bonds between the gel and mucous membranes, and carbomer is the proton donor of red bonds. Commonly used excipients, polyvinylpyrrolidone (PVP) and polyoxyethylene (POE) are the red bond proton acceptors of acrylic polymers, and their ability to accept protons is stronger than that of mucous membranes. Therefore, when carbomer is used with PVP or POE at the same time , May reduce the mucosal adhesion of carbomer gel.
Researcher Tohyn proved that the ability of PVP and POE to reduce the adhesion of carbomer gel is related to the concentration and molecular weight of PVP and POE used. 5% PVPK30 can significantly reduce the adhesion of carbomer gel, and the effect is small when the concentration drops to 0 to 0.5%. POE (100000) can weaken the mucosal adhesion of carbomer gel, while insoluble high molecular weight POE cannot. Because Carbomer has a certain buffering capacity, usually the pH of the medium cannot change this property of PVP and POE; but some people think that the maximum adhesion of Carbomer gel decreases with the increase of the pH of the medium. When HPC is combined with carbomer as a bioadhesive, increasing the concentration of HPC can speed up the release of the drug, and it is easy to shape. Increasing the concentration of carbomer will increase the absorption of water and increase the adsorption force of the mucosa. It has been reported that magnesium stearate can also reduce the adhesion of carbomer gel due to its fluidity.
Other factors affecting Carbomer:
The degree of crosslinking can affect the swelling of Carbomer. Lightly cross-linked carbomer is easy to absorb water and swell; highly cross-linked carbomer is not easy to swell due to its denser structure. Therefore, lightly cross-linked carbomer is easier to slow down the release of the drug than highly cross-linked carbomer. In addition, different molecular weights have different ability to form gels. In view of the many special structures and properties of carbomer relative to other pharmaceutical excipients, it is sighed for its outstanding use in the field of pharmacy. It has been widely used in the delivery of protein drugs and many other fields. Increasing the concentration of carbomer increases the amount of water absorption and the adsorption force on mucous membranes.
Carbomer has been widely used in disposable alcohol disinfection gels, lotions, and medicaments due to its viscosity and transparency. It is for this reason that carbomer has become an irreplaceable daily chemical product. As one of the manufacturers of Carbomer, Desheng can provide high-quality Carbomer 940 and 980. If you have any questions or needs, please click on the official website to consult customer service.