Written by pharmacy student Serabi Rembert, PharmD, Candidate, Mercer University College of Pharmacy
A six-part series of Pharmaceutical Excipients used in Non-Sterile Compounding was published in IJPC beginning 2019 and continuing through this year.
Please follow along with us for the next six weeks as we summarize the findings, highlighting the key aspect of the report.
What Are Excipients?
These ingredients are known to be substances other than the pharmacologically active drug or prodrug. The excipients are included either within the manufacturing process or within a finished pharmaceutical product dosage form. Each excipient is formulated with an active ingredient in medication and is included in order to instill long-term stabilization, to bulk up solid formulations containing potent active ingredients in small amounts, or to enhance the therapeutics on the active ingredient in the final dosage form (via easing drug absorption, reducing viscosity, or enhancing solubility).
What Are the Purposes of Excipients?
- Formation of suitable dosage forms
- Aids in stability
- Aids in administration
- Aids in producing a suitable drug release
- Aids with patient compliance/acceptability (looking and tasting better)
- Protects, supports, and/or enhances stability & bioavailability
- Assists in product identification and enhances attribute(s) of safety
- Assists in effectiveness and overall delivery of drug in use
- Aids in the manufacturing process
- Aids in the processing of drug delivery system during its manufacture
- Assists in maintaining integrity of drug product during storage
- Enhances attribute of safety and effectiveness of drug during storage and use
Examples of Excipients and Their Uses
Preparation of solutions:
- In the preparation of solutions, one or more SOLVENTS are used to dissolve the drug substance.
- FLAVORS and SWEETENERS are used to make a product more palatable.
- COLORANTS are added to enhance appeal.
- PRESERVATIVES may be added to prevent microbial growth.
- STABILIZERS, such as antioxidants and chelating agents, may be used to prevent decomposition.
Preparation of Tablets:
- DILUENTS or FILLERS are commonly added to increase the bulk of the formulation.
- BINDERS are used to cause adhesion of the powdered drug and pharmaceutical substances.
- ANTIADHERENTS or LUBRICANTS are used to assist smooth tablet formation.
- DISINTEGRATING AGENTS are used to promote tablet breakup after administration.
- COATINGS are used to improve stability, control disintegration, or enhance appearance.
Preparation of ointments, creams, and suppositories:
In the preparation of ointments, creams, and suppositories, they acquire their characteristic features from their pharmaceutical bases.
For each dosage form, the pharmaceutical ingredients establish the primary features of the product and contribute to the physical form, texture, stability, taste, and overall appearance.2
Added substances on commercially manufactured drug product labels:
All commercially manufactured drug products are labeled to state the identity of all added substances, but not the quantities. This information is generally in the “Description” portion of the official product package insert. Generally, if an ingredient is only present in a trace amount with no functional or technical effect on the product, it does not need to be listed. If it has been shown to cause sensitivity reactions or allergic responses, then it must be listed (along with dyes and coloring agents).
Sources of Excipients
Note: Tend to be organic chemicals and can be divided into the following:
- Carbohydrates (i.e., Sugars, Starches, Celluloses)
- Petrochemicals(i.e., Glycols, Povidones, Mineral hydrocarbons, Acrylic polymers, Others)
- Oleochemicals(i.e., Fatty alcohols, Mineral stearates, Glycerin, Others)
What Are the Incompatibilities Involving Excipients?
There are numerous incompatibilities involving various excipients within the literature.3,4 A prime example is noted in that calcium salts are sometimes used as fillers, and tetracycline interferes with absorption. Another example, in regards to tablets, is with lubricants. These excipients are hydrophobic, and the addition of excess lubricants may lead to an increase in tablet disintegration and a decrease in the drug dissolution rate.
Examples of Pharmaceutical Ingredients
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- Allen LV Jr. Basics: Excipients Used in Nonsterile Compounding, Part 1. Int J Pharm Compd. 2019;23(4):305-311.
- Allen LV, Jr. Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems. 11th ed. Baltimore, MD: Wolters Kluwer; 2018:76-126.
- Allen LV, Jr. The Art, Science, and Technology of Pharmaceutical Compounding. 5th ed. Washington, DC: American Pharmacists Association; 2016: 23–56.
- Sheskey PJ, Cook WG, Cable CG. Handbook of Pharmaceutical Excipients. 8th ed. London, UK: Pharmaceutical Press; 2017