Some Basic Facts About Active Pharmaceutical Ingredient Excipients for Drug Discovery


Pharmaceutical excipients are substances formulated with the active pharmaceutical ingredients (APIs) of the medicine, and the excipients make up the major part of the composition of the medicine. Excipients are designed to interact with and enhance the properties of APIs.

Excipients have various functions. In addition to acting as carriers and improving stability, pharmaceutical excipients are also conducive in terms of solubilization, sustained release and controlled release. Overall, these are important components that can affect the quality, safety, and effectiveness of drugs.

Excipients can be classified by source, function, route of administration, etc.

By origin

They can be divided into natural, semi-natural and fully synthetic excipients.

By function

They can be divided into solvents, propellants, solubilizers, cosolvents, emulsifierscolorants, binders, disintegrants, fillers, lubricants, wetting agents, osmotic pressure regulators, stabilizers, gliders, flavor correctors, preservatives, suspending agents, potting materials, fragrances, release agents, integrators, penetration enhancers , pH modifiersbuffers, plasticizers, surfactants, foaming agents, defoamers, thickeners, embedding agents, humectants, absorbents, thinners, flocculants and deflocculants, filter aids, release blockers, etc

By administration

Excipients can be added to develop different dosage forms, such as oral, injection, mucosal, transdermal or topical administration, nasal or oral inhalation administration and ocular administration.

Potential adverse effects caused by excipients

Adverse effects caused by excipients added to the drug are related to the properties of the excipients themselves. Some excipients themselves have a certain toxicity, once the concentration is too high, or used long term, they can cause undesirable effects. For example, when propylene glycol is used as an excipient to dissolve poorly soluble drugs, and if administered in large doses, propylene glycol will be converted into lactic acid by acetaldehyde dehydrogenase, and adverse effects such as lactic acidosis and hemolysis may occur. Long-term high-dose infusion may also cause kidney damage.

Also, during the preparation process, ethanol is used as a solvent for many insoluble drugs. However, ethanol can cause burning and pain during the medication process, and if the application site is close to nerve tissue, it can also cause nerve damage. For example, when cephalosporin antibiotics are used, if combined with drugs containing ethanol as excipients, there may be disulfiram-like reactions, with symptoms such as flushing, headache, nausea, vomiting, decreased blood pressure and even shock.

Preservatives are also excipients that must be added to many liquid preparations (such as eye drops and nose drops) to prevent the growth of microorganisms and ensure the stability of the preparation. However, long-term use of these eye drops containing preservatives will cause pathological damage to the ocular surface. Long-term use of nasal drops containing preservatives will damage the ciliated tissue of the nasal cavity, thereby reducing the respiratory system’s resistance to bacteria and its ability to trap dust particles.

Adverse effects caused by excipients are also related to the constitution of the patient. In fact, for most patients, a little excipient has no effect, but due to individual differences, a very small amount of excipient may cause allergic or other adverse reactions in a very small number. of patients. For example, lactose is a diluent for many tablets and capsules, but for lactose intolerant patients it can cause side effects such as diarrhea and abdominal pain. Tartrazine is a coloring excipient, but there is a cross-allergy to aspirin and some patients may experience acute bronchospasm, urticaria and even severe angioedema or anaphylactic shock.

CD Formulation’s cGMP laboratory has a team of experts specializing in drug formulation and manufacturing. Their expertise can facilitate the development of drugs, particularly with regard to the choice and preparation of the various excipients. Personalized pharmaceutical excipients will be manufactured to meet customers’ requirements for different projects. At the same time, this company, with its innovative spirit and down-to-earth attitude, also has the mission of helping researchers solve the difficulties encountered at the various stages of drug research and development.


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