by Introduction
Pharmaceutical excipients play an important role in drug product development and manufacturing. Excipients are the ingredients other than the active pharmaceutical ingredients (API) that have been added intentionally during the manufacturing process of a drug product. Excipients help optimize drug performance and ensure patient safety.
Properties of excipients
Excipients are selected based on their physicochemical properties to suit specific dosage form and drug delivery technology requirements. Some key properties evaluated for excipient selection include particle size, density, flowability, compressibility, solubility, stability, miscibility etc. Excipients can be classified based on their functional roles as fillers, binders, diluents, lubricants, disintegrants, flavors, colors etc. Understanding excipient properties helps develop robust formulation with desired product quality attributes.
Role of excipients in dosage forms
Pharmaceutical Excipients play a vital role in determining the safety, efficacy and acceptability of a drug product. In oral solid dosage forms like tablets and capsules, excipients help improve manufacturability, control release of API and facilitate administration. Fillers and diluents provide bulk quantity; binders lend cohesiveness during compaction; disintegrants facilitate breakdown in gastrointestinal fluids; coatings enable targeted delivery and improve palatability. Even parenteral and topical formulations rely on excipients for viscosity adjustment, prevention of irritation and maintenance of stability and sterility.
Pharmaceutical properties of common excipients
Lactose is commonly used as a filler and diluent in oral dosage forms due to its good compressibility, tableting properties and stability. Microcrystalline cellulose is another multi-functional excipient used as a filler, binder and disintegrant owing to its plastic and swelling characteristics. Starch and starch derivatives find application as disintegrants, binders and viscosity enhancing agents. Magnesium stearate is frequently employed as a lubricant to facilitate tablet manufacturing process. Glycerol and propylene glycol are commonly added solubilizers and humectants in oral and topical formulations.
Regulatory considerations for excipients
Regulatory agencies require thorough characterization and safety evaluation of excipients used in drugs. The International Council on Harmonisation (ICH) Q3D guideline provides a framework for the structure and content of excipient monographs. The US FDA Inactive Ingredient Database and European Pharmacopeia monographs define permissible daily exposure limits for different excipient classes based on their toxicity profiles. Any changes to excipient supplier or specifications during product lifecycle may warrant additional evaluation like stability testing. Adherence to cGMP ensures consistent quality of excipients used.
Role of advanced excipients
With advancing drug delivery technologies, novel excipients are being engineered to overcome formulation and biopharmaceutical challenges. Liposomes, solid lipid nanoparticles and polymeric nanoparticlesfind application as carrier systems for optimal delivery of APIs. Solubilizers like polyvinylpyrrolidone and cyclodextrins enhance dissolution of poorly soluble drugs. Sodium lauryl sulphate acts as a permeation enhancer for transdermal patches. Excipient selection plays a pivotal role in the design and performance of such complex drug delivery systems.
Excipient safety assessment
Given that excipients form a major part of drug products, their effects o human health are important to establish. While most excipients are generally recognized as safe (GRAS), studies are conducted as per ICH Q3D to identify potential toxicity issues. Safety endpoints evaluated include acute oral toxicity, genotoxicity, local tolerance, repeated dose toxicity and reproductive/developmental toxicity. Excipients judged safe based o this extensive risk assessment data are permitted for use in various dosage forms and routes of administration in permissible daily intake quantities. Proper excipient characterization and GMP limits help ensure their consistent safety in pharmaceutical applications.
Excipients bring multifarious advantages to drug product development like facilitating manufacturing processes, controlling drug release and improving patient acceptance. Thorough understanding of their physicochemical properties and interactions with API aids rational selection suited for a specific dosage form and delivery system. Robust safety assessment as per global regulatory standards assures acceptably low risk to human health from excipient exposure levels. Advanced excipients further expand opportunities for designing novel dosage forms needed to address current treatment challenges. Overall, excipients are indispensable formulation components that synergize with APIs to produce safe and effective medicines.
*Note:
1. Source: Coherent Market Insights, Public sources, Desk research
2. We have leveraged AI tools to mine information and compile it
