The application of macroporous ion exchange resin in the pharmaceutical flavoring agent

Up to now, most of the pharmaceutical preparations listed in the world are oral preparations This is because oral preparations (tablets, capsules or lozenges, etc.) have many advantages, mainly convenient to carry and easy to take However, for the special population (about 1 / 4 of the total number of patients) who have difficulty swallowing solid preparations, such as children or elderly patients, oral liquid preparations are almost more popular However, there is a general problem in liquid medicine (such as solution, suspension, syrup or spirit) that the taste of most of the chemical synthetic drugs is extremely bitter, which makes such patients fearful and difficult to adhere to the medicine How to improve the taste of bitter drugs in the processing of liquid drugs, so that most patients are willing to accept, has always been an important issue faced by preparation scientists This problem can be solved by choosing the right "flavor stabilizer" The so-called "flavor rectifying agent" refers to the pharmaceutical excipients used to improve or shield the bitter taste of drugs, making it difficult for patients to detect the strong bitter taste (or other peculiar smell such as spicy, stimulating, etc.) of drugs Up to now, the flavoring agents used or being used in pharmaceutical processing include: all kinds of flavoring agents, fatty substances (including lecithin and surfactant), hydrophilic drug embedding agent materials (such as polyacrylic resin medical coating agents, modified starch carbohydrates, cyclodextrin glucose oligomers, etc.) and ion exchange Resins, proteins, zeolites and other new pharmaceutical excipients Ion exchange resin has developed rapidly in recent years among various kinds of medicinal flavor rectifiers As the bitterness improver of liquid medicine, it has a good effect and has emerged in the production of liquid medicine As a new auxiliary material for medicine, ion-exchange resin has attracted wide attention of pharmaceutical workers all over the world Ion exchange resin is not a new product As early as 60 years ago, Dow Chemical Company of the United States has produced * batch of industrial ion exchange resins Nowadays, ion exchange resin has been widely used in petrochemical, light industry, pharmaceutical, water treatment and other industries The appearance of medical ion exchange resin began in the mid-1950s Firstly, the ion exchange resin used for medicine is the macroporous resin amferlite irc50 (belonging to weak acid cation exchange resin), which is mainly used to purify the finished product of streptomycin Since then, many antibiotic products have been purified with macroporous resin to remove impurities In the early 1990s, pharmacists found that some ion exchange resins can be directly used in oral preparations to improve the taste, improve the palatability of the liquid medicine and control the release of drugs in the body Due to its advantages of high molecular weight, almost insoluble in water and not digested and absorbed by human body, macroporous ion exchange resin has been officially approved by the pharmaceutical administration of western countries and can be directly used as pharmaceutical excipients in oral preparations By the end of 1990s, amferlite macroporous resin had been used as a medicinal flavoring agent in a number of foreign newly marketed liquid pharmaceutical products These liquid preparations include the seroxal oral liquid produced by Stryker and the liquid preparations produced by other pharmaceutical companies containing drugs such as mesafulin, pseudoephedrine and dextromethorphan The amount of macroporous ion exchange resin used to improve bitterness can vary with the variety of drugs In principle, the molar ratio of the dosage of the main drug and the ion exchange resin should be between 0.1 (1:10) and 0.75 (3:4) Too little resin will not improve the bitterness, too much resin will have side effects Zui's macroporous ion exchange resin suitable for use as a medicinal flavoring agent shall be "amferlite IRP 88" or "amferlite IRP 64" Both of the macroporous resins are produced by Rohm & itaas The results show that the two resins can effectively improve the palatability of the bitter medicine liquid preparation and prolong the action time of the medicine in vivo, so they can be used as one of the best Zui options of the medicine flavor straightener Foreign experiments in vitro and in vivo have proved that this kind of macroporous resin Zui can be excreted from the intestine eventually, and there is no risk of cumulative poisoning to human body As a macroporous resin used to improve the taste, the particle diameter of amferlite IRP 64 or 88 is very important Because the patients with too large particles will have a "sense of powder and sand" in their mouth when taking the liquid medicine The results show that the particle diameter of Zui suitable ion exchange resin should be between 53-150 μ M Too small or too large particles are not suitable as auxiliary materials of medicinal flavor straightening agent Secondly, in order to solve the problem of the deposition of macroporous resin in the liquid medicine, Zui should properly add medicinal thickeners (such as xanthan gum, guar gum, tragacantha gum, gaita gum, sophora bean gum, Arabic gum, etc.) into the liquid medicine formula In this way, macroporous resin can be evenly distributed in the medicament and microcrystalline cellulose can be maintained CMC and other cellulose esters can also solve the problem of precipitation of macroporous resin in the medicament solution Western companies use aricel CL 611, a pharmaceutical adjuvant of Zui multi, which is a mixture of microcrystalline cellulose and sodium carboxymethylcellulose If aricel CL 611 is added in 3% proportion, a uniform suspension can be formed, which is in the state of opaque glue, and the storage time of the product can be prolonged correspondingly.