Topical and Transdermal Formulation Development
Marc B. Brown, Adrian C. Williams in The Art and Science of Dermal Formulation Development, 2019
Excipients are the components of a formulation that in combination produce a “successful” pharmaceutical product. Although the drug or active pharmaceutical ingredient is of primary importance since it is responsible for the treatment of the disease, in order to “present and deliver” the drug, excipients play an equally important role. Whilst, traditionally, excipients have been used as “inert” material, such as bulking agents in dosage forms such as tablets, more recent development of drug delivery systems has used the benefit of excipient–drug interaction to produce formulations with specific properties and performance specifications. Thus, any interaction between excipients and the drug substance must be well understood and is fundamental in developing any drug product.
The administration of medicines to children
Evelyne Jacqz-Aigrain, Imti Choonara in Paediatric Clinical Pharmacology, 2021
To produce drug preparations appropriate for different routes of administration and to ensure their acceptability and long term stability requires the addition of certain other chemicals or substances called excipients. Excipients should be pharmacologically inactive but many have some effect and can produce adverse reactions in some patients. Those that are absorbed from the gut, skin and mucus membranes or injected, may have systemic effects and may be metabolised and eliminated by the liver and kidney. Developmental pharmacology may be as important for the handling of some excipients as it is for ‘active’ substances. Drug regulatory agencies determine which excipients are acceptable and they usually set exposure limits and labelling requirements for the finished product [1].
Fenugreek Based Products in USA, Australia, Canada, and India
Dilip Ghosh, Prasad Thakurdesai in Fenugreek, 2022
The TGA provides access to information about ingredients that are permissible to be used in the products. The TGA Business Services website has a searchable database of approved terminology for chemical, biological, and herbal ingredients, including the active ingredients, excipients, and components and equivalents of ingredients that may be used in TGA-regulated therapeutic goods. This database for ingredients is called the “Ingredients table”. There are two types of ingredients, active and excipients. An active ingredient is the therapeutically active component in a medicine’s final formulation that is responsible for its physiological action. An excipient ingredient is any component of a finished dosage form, other than an active ingredient. The ingredient searched in the ingredient table gives the “Ingredient summary” which provides the approved role of the ingredient (active or excipient). Fenugreek (the ingredient ID 59791) is summarized for use as “an active ingredient” in categories such as Export Only, Listed Medicines, Over the Counter, or Prescription Medicines. It is also available for use as a “Homoeopathic Ingredient” in “Listed Medicines” and for use as an “Excipient Ingredient” in categories of Export Only, Listed Medicines, Over the Counter, or Prescription Medicines.
Inhibitory effect of sixteen pharmaceutical excipients on six major organic cation and anion uptake transporters
Published in Xenobiotica, 2021
Ruicong Ma, Gentao Li, Xue Wang, Yajuan Bi, Youcai Zhang
Excipients are added into drug formulations to maintain drug stability, enhance the absorption of drugs, as well as deliver the desired color and taste to the drugs. Based on the applications, excipients are categorized into various classes, such as fillers, surfactants, suspending agents, preservatives, taste maskers, etc. (Goole et al., 2010). Much progress has been made to develop excipients that play a vital role in drug delivery systems (Kalász & Antal, 2006). Surfactants, such as sodium dodecyl sulfate (SDS), Triton X-100, and polysorbates (Tweens), can solubilize hydrophobic drugs by either a cosolvent approach or forming micelles (Strickley, 2004). Cyclodextrins can enhance the solubility of drugs by uptake of hydrophobic drugs or hydrophobic parts of drugs into their hydrophobic cavities (Hamman & Steenekamp, 2012). Polyethylene glycols (PEGs) can serve as permeation-enhancing agents to enhance the absorption of hydrophilic drugs (Hamman & Steenekamp, 2012).
Opportunities for enteral drug delivery for neonates, infants, and toddlers: a critical exploration
Published in Expert Opinion on Drug Delivery, 2022
Nicole Sheena Kaneria, Catherine Tuleu, Terry Ernest
Excipients generally recognized as safe for adults and possibly for older children/adolescents can be unsafe when dosed in under 2s due to their immaturity in ADME [11,18]. Those in intensive care are often polymedicated, leading to cumulative effects, drug interactions, and exacerbated adverse reactions, especially for preterm babies, with excipients in their treatment regime potentially exceeding the adult accepted daily intake. Therefore, when formulating suitable dosage forms for this group, the need for, type, and quantity of excipient used that does not deter its quality nor the bioavailability of the active pharmaceutical ingredient (API) should be considered [2,18,21]. Recent papers [22,23] highlight excipient concerns and mention studies such as ▣Safe Excipient Exposure in Neonates and Small Children (SEEN) and ▣European Study on Neonatal Exposure to Excipients (ESNEE) and their generation of an ‘excipients of interest list’ that demonstrate the achievability of progress in this area. The safety, tolerability, and exposure of excipients remain an underlying core consideration but will not be central to this review as it has been extensively detailed elsewhere [Walsh, et al., 2021 give an overview [4]].
Aloe vera and artemisia vulgaris hydrogels: exploring the toxic effects of structural transformation of the biocompatible materials
Published in Drug Development and Industrial Pharmacy, 2021
Taskeen Frasat, Ume Ruqia Tulain, Alia Erum, Uzma Saleem, Muhammad Farhan Sohail, Rizwana Kausar
The lacking of safety and regulatory provisions for the excipients initiated the development of the guidelines which redefined excipients as materials that display either no or very limited pharmacological activity and the reason being that safety assessment of excipients is less complex and less extensive as compared to that of active agents [8]. The development of novel drug delivery systems has led to the discovery and utilization of new pharmaceutical excipients, meeting these challenges. Thus, the safety evaluation of new excipients has now become a vital part of drug safety evaluation. Although the development of new excipients is a slow process due to cost and regulatory obstructions, yet all the new excipients must be extensively evaluated with particular nonclinical studies and undergo a specific Risk-Benefit assessment before entering the market [9].
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