Characterization of adsorption behavior by solid dosage form excipients in formulation development

Senderoff, Richard I.; Mahjour, Majid; Radebaugh, Galen W.

doi:10.1016/0378-5173(82)90009-6

Cited by 13 publications

(5 citation statements)

References 8 publications

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“…Thus, those parameters can be lumped into single K Ads parameter. That is, the adsorption of active compound to the surface of the excipient is, in this case, mainly a function of the microcrystalline cellulose content, which is in agreement with (3,14).…”

Section: (3)supporting

confidence: 68%

“…Since most dosage forms comprise not only the active ingredient but also excipients, the overall rate of API release depends on the properties of both of these components (1)(2)(3)(4). Moreover, it also depends on the arrangement and interaction of individual components of the dosage form, which in turn depend on the dosage form processing history, such as a dry or wet agglomeration process.…”

mentioning

confidence: 99%

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Analysis of Drug Release from Different Agglomerates Using a Mathmatical Model

Petrů¹,

Zámostný²

2014

Dissolution Technol.

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The release rate of an active ingredient from a dosage form may be affected by the agglomeration of an active ingredient before tablet compression. This study is aimed at establishing the effects of the agglomerates on active ingredient release profiles. A model substance, caffeine, was tested in the powdered form and in the two agglomerated forms prepared by wet granulation and compaction. The profiles of caffeine release from these forms were measured using a flow-through cell dissolution apparatus (USP 4) in an open-loop arrangement. To identify the particular processes responsible for the differences in the dissolution profiles of the model forms, we developed a mathematical description of the dissolution profiles. Using this mathematical approach, we proposed that caffeine was adsorbed to the microcrystalline cellulose present in the granulated and compacted form and that diffusion of the active ingredient was inhibited in the presence of a binder in the granulate. Both of these effects resulted in imperfections in the shape of dissolution profiles and in a decrease in the dissolution rate of caffeine. The mathematical model is based on generic parameters, thus it is transferable to other pharmaceutical substances in powdered and agglomerated forms.

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Section: (3)supporting

confidence: 68%

mentioning

confidence: 99%

Analysis of Drug Release from Different Agglomerates Using a Mathmatical Model

Petrů¹,

Zámostný²

2014

Dissolution Technol.

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“…For horses, ruminants, and pigs, medications are often administered to fed animals or in medicated feed. Therefore, drug adsorption onto the GI contacts may influence in vivo drug solubilization [ 102 , 103 ]. On the one hand, adsorption of drug molecules onto the surface of excipients or materials such as hay can reduce drug particle size and increase the surface area of the drug available to the dissolution medium.…”

Section: Impact On Formulation Strategies: How Species Gi Fluid Diffe...mentioning

confidence: 99%

Impact of gastrointestinal differences in veterinary species on the oral drug solubility, in vivo dissolution, and formulation of veterinary therapeutics

2022

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Many gaps exist in our understanding of species differences in gastrointestinal (GI) fluid composition and the associated impact of food intake and dietary composition on in vivo drug solubilization. This information gap can lead to uncertainties with regard to how best to formulate pharmaceuticals for veterinary use or the in vitro test conditions that will be most predictive of species-specific in vivo oral product performance. To address these challenges, this overview explores species-specific factors that can influence oral drug solubility and the formulation approaches that can be employed to overcome solubility-associated bioavailability difficulties. These discussions are framed around some of the basic principles associated with drug solubilization, reported species differences in GI fluid composition, types of oral dosage forms typically given for the various animal species, and the effect of prandial state in dogs and cats. This basic information is integrated into a question-and-answer section that addresses some of the formulation issues that can arise in the development of veterinary medicinals.

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“…Taki efekt może prowadzić do niekorzystnych zmian. Przykładowo w literaturze opisana jest adsorpcja niektórych agonistów k-opioidowych na celulozie mikrokrystalicznej, kroskarmelozie i sodowym glikolanie skrobi, co modyfikuje kinetykę rozpuszczania substancji, a w konsekwencji zmienia jej biodostępność [35]. Adsorpcji mogą ulegać również cząsteczki wody, np.…”

Section: Charakterystyka Oddziaływań Między Cząsteczkami Substancji Punclassified