Pharmaceutical excipients play a vital yet often overlooked role in medicine formulation and delivery. Excipients help improve drug stability, absorption, delivery and patient acceptability. However, most people are unaware of the various types of excipients used and their purposes.
Types of Excipients
Pharmaceutical Excipients can be broadly classified into several categories based on their roles in drug products:
Fillers and Diluents: Fillers and diluents like lactose, microcrystalline cellulose, starch, sucrose etc are used to provide bulk quantity to tablets and capsules. They allow proper filling of dosage forms and allow adjustment of dosage amounts.
Binders and Adhesives: Binders like povidone, gelatin help improve cohesion between other ingredients during formulation. They provide structure and binding properties. Adhesives like sodium carboxymethylcellulose, polyvinylpyrrolidone help coat tablets for improved aesthetic appeal and protection.
Disintegrants: Superdisintegrants like crospovidone, sodium starch glycolate are added in very small amounts, typically 1-5% in tablets, to facilitate rapid breakup of tablets upon ingestion for quick dissolution and absorption. This allows efficient breakup and dispersal of ingredients in body fluids.
Lubricants: Lubricants such as magnesium stearate, stearic acid help improve flow properties of powder blends to allow efficient tableting process. They prevent adhesion of ingredients to machinery surfaces during compression.
Coatings: Film coatings like hydroxypropyl methylcellulose enhance appearance and protect tablets from chipping, breakage and erosion during storage, packaging and distribution. They allow branding and identification. Enteric coatings like hypromellose phthalate or methacrylic acid copolymers protect pH-sensitive drugs from degradation in stomach.
Preservatives: Preservatives inhibit microbial growth and maintain sterility during long term storage of liquid dosage forms. Benzoic acid, methyl paraben are commonly used preservatives.
Flavoring Agents and Sweeteners: Flavoring agents and sweeteners improve taste acceptability, especially for pediatric medications. Sugar, sorbitol, sucralose enhance patient compliance by improving palatability.
Importance of Excipients
Excipients significantly impact important quality attributes like stability, bioavailability, ease of manufacturing and patient compliance. Appropriate selection based on both functional and safety characteristics is essential for successful formulations. Some key ways excipients determine effectiveness include:
Improving stability: Excipients protect drug molecules from degradation during storage. They minimize hydrolysis, oxidation and other degradation pathways leading to longer shelf life stability.
Controlling release: Targeted release excipients modulate drug release kinetics as per body sites. Enteric polymers protect drugs in stomach and release in intestine. Sustained release matrices extend effects over time.
Enhancing solubility and absorption: Absorption enhancing excipients like cyclodextrins complex hydrophobic drugs, improving solubility and gastrointestinal absorption. Surfactants also influence dissolution and membrane permeability.
Facilitating manufacturing: Excipients allow tableting, encapsulation and other processes for large scale production. Binders impart mechanical strength to tablets. Lubricants aid equipment efficiency. Proper selection enables seamless production.
Improving patient adherence: Excipients that confer pleasing taste and odour, soft gelatin capsules with easy swallowing help compliance especially for pediatric/geriatric groups. This translates to better therapeutic outcomes.
Ensuring safety and efficacy: Toxicological evaluation during product development and continuous monitoring ensures absence of harmful effects from excipient impurity levels overShelf-life. This maintains consistent safety and performance.
Challenges with Excipients
While excipients enable formulation and delivery advantages, they also present unique challenges:
Product quality issues: Certain excipients may interact deleteriously with active ingredients under stressed conditions affecting stability, solubility and bioavailability.
Raw material variability: Variation in excipient sources and manufacturing processes can impact batch to batch consistency in critical quality attributes implicating safety and efficacy.
Toxicological potential: Certain excipients may show signs of toxicity under specific conditions, acute or chronic usage frequencies especially in susceptible populations like neonates.
Regulatory requirements: Stringent control of impurities, identification and quantification and toxicological profiles required by global regulatory guidelines expanding quality burden.
Innovation barrier: Development of alternate safe and functional substitute excipients for new delivery systems and formulation approaches require extensive research investments limiting innovation.
Conformance to cGMPs: Maintaining excipient quality systems as per current Good Manufacturing Practices throughout global supply chains is a major resource intensive task for manufacturers.
Harnessing the full potential of excipients and overcoming these challenges requires extensive multidisciplinary scientific efforts focused on continuous innovation, improved understanding of biological interactions and collaborative global regulatory frameworks. With advancing formulation technologies and evolving scientific insights, excipients will continue playing an indispensable role in developing more efficacious and safer medicinal products ensuring better population health.
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1. Source: Coherent Market Insights, Public sources, Desk research
2. We have leveraged AI tools to mine information and compile it