Quality and functionality of excipients

Pifferi, G.; Santoro, Paola; Pedrani, Massimo

doi:10.1016/s0014-827x(98)00101-3

Cited by 111 publications

(71 citation statements)

References 11 publications

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“…The improvement in dissolution rate of the S2 formulation compared to S1 could be attributed to the use of a soluble solvent possessing reducing properties (Pifferi, Santoro, Pedrani, 1999). The addition of a larger proportion of directly compressed microcrystalline cellulose PH 102 may lead to more efficient disintegration, enhancing the dissolution of the active simvastatin (Shirzad, Roa, Raimar, 2007).…”

Section: Tablet Production and Characterizationmentioning

confidence: 99%

Rational use of antioxidants in solid oral pharmaceutical preparations

Celestino

Magalhães

Fraga

et al. 2012

Braz. J. Pharm. Sci.

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Antioxidants are currently used as efficient excipients that delay or inhibit the oxidation process of molecules. Excipients are often associated with adverse reactions. Stability studies can guide the search for solutions that minimize or delay the processes of degradation. The ability to predict oxidation reactions in different drugs is important. Methods: This study was conducted to assess the rational use of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), sodium metabisulfite (SMB), propyl gallate (PG) and cysteine (CYS) in tablet formulations of simvastatin and ketoconazole. These antioxidants were evaluated according to stability parameters and the relationship between efficiency of the antioxidant and chemical structure of the drugs. Results were compared with DPPH tests and computational simulations. BHT was most efficient regarding simvastatin stability, and the most effective BHT concentrations for maintaining stability were 0.5 and 0.1%. In relation to ketoconazole, SMB was most efficient for maintaining content and dissolution profile. The evaluation by DPPH showed that the largest percentage of absorbance reduction was observed for PG, while SMB proved most efficient and had lower consumption of DPPH. The same pattern was observed, albeit with lower efficiency, for the other lipophilic antioxidants such as BHT and BHA. The results of the molecular modeling study demonstrated that electronic properties obtained were correlated with antioxidant activity in solution, being useful for the rational development of liquid pharmaceutical formulations but not for solid oral formulations. This study demonstrated the importance of considering stability parameters and molecular modeling to elucidate the chemical phenomena involved in antioxidant activity, being useful for the rational use of antioxidants in the development of pharmaceutical formulations.Uniterms: Antioxidants/rational use. Excipients/evaluation. Butylated hydroxyanisole/rational use. Butylated hydroxytoluene/rational use. Sodium metabisulfite/rational use. Propyl gallate/rational use. Cysteine/rational use. Simvastatin/tablets/evaluation. Ketoconazole/tablets/evaluation. Atualmente, antioxidantes são usados como excipientes eficientes, que retardam ou inibem o processo de oxidação de moléculas. Excipientes são frequentemente associados a efeitos adversos. Estudos de estabilidade podem ajudar na busca por possíveis soluções para minimizar ou retardar os processos de degradação. A habilidade de prever as reações de oxidação em diferentes fármacos é importante. O estudo foi conduzido com o objetivo de avaliar o uso racional de hidroxianisol butilado (BHA), hidroxitolueno butilado (BHT), metabissulfito sódico (SMB), galato de propila (PG) e cisteína (CYS) em formulações de comprimidos de sinvastatina e cetoconazol. Eles foram avaliados por parâmetros de estabilidade e pela relação entre a eficiência dos antioxidantes e a estrutura química do fármaco. Os resultados foram comparados com testes de DPPH e simulações em computador. BHT f...

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Section: Tablet Production and Characterizationmentioning

confidence: 99%

Rational use of antioxidants in solid oral pharmaceutical preparations

Celestino

Magalhães

Fraga

et al. 2012

Braz. J. Pharm. Sci.

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“…Such excipients are called binders and include substances such as gelatin, sucrose, cellulose, polyvinylpyrrolide, starch or polyethelene glycol (PEG). 168,172 Polymers such as polylactide-co-glycolide acid (PLGA) or chitosan may become more relevant for oral delivery, as several have been shown to efficiently incorporate potential antigens into the polymer matrix and maintain integrity through the gut, although delivery of their contents to the intestinal epithelium has not been shown consistently. 173 Chitosan has also been shown to prolong gastric transit time, allowing greater opportunity for absorption of the vaccine.…”

Section: Correlates Of Immune Protectionmentioning

confidence: 99%

Recent advances inEbolavirusvaccine development

Richardson

Dekker

Croyle³

et al. 2010

Human Vaccines

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“…The requirement of therapeutic efficacy for drugs is replaced by that of functionality for excipients, defined as 'the physical, physicochemical and biopharmaceutical properties' of the same. The concepts of quality and functionality were reviewed by one of the Authors in a recent review in this magazine, and those who wish to go more deeply into these aspects are invited to refer to it [10].…”

Section: Principal Requirements Of Excipientsmentioning

confidence: 99%

The safety of pharmaceutical excipients

Pifferi¹,

Restani²

2003

Il Farmaco

Self Cite

169

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The most important part of a medicine as far as its weight is concerned, is constituted by its excipients, which have the important functions of guaranteeing the dosage, stability and bioavailability of the active principle. The components employed as excipients must present the characteristics required by their technological function but, as with any substance administered to man, they must also correspond to suitable safety requirements. In fact, in the past the importance of evaluating the possible adverse effects of excipients was underestimated, because their inertia and innocuity were taken for granted. The safety profile of these substances is more deeply researched as regards the toxicological aspect only if they are also employed in the food industry (anti-oxidants, sweeteners, colouring agents, etc.). Indeed, in this case, the International Toxicological Committees (among which the Joint Expert Committee on Food Additives, a mixed committee of the WHO/FAO) demand thorough studies in laboratory animals, with the intent of protecting the consumer's safety. Tackling the question of the toxicity of excipients thoroughly is not a simple matter for several reasons: the large number of substances on the market and the diversity of their chemical profiles, their sources, their technological functions, and the presence of secondary products and/or contaminants that may be the true causes of adverse effects. In this article we shall review the principal classes of excipients and their respective side effects. Then we shall proceed to their toxicological evaluation, giving examples of: (a) intrinsic toxicity, or adverse effects that may be encountered in the whole population; and (b) specific toxicity, which manifests only in people who are carriers of a transmissible disease or who are genetically predisposed, such as people with allergies and intolerances.

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Quality and functionality of excipients

Cited by 111 publications

References 11 publications

Rational use of antioxidants in solid oral pharmaceutical preparations

Rational use of antioxidants in solid oral pharmaceutical preparations

Recent advances inEbolavirusvaccine development

The safety of pharmaceutical excipients

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