Impact of Excipient Interactions on Drug Bioavailability from Solid Dosage Forms

Panakanti, Ravikiran; Narang, Ajit S.

doi:10.1007/978-3-319-20206-8_10

Cited by 13 publications

(21 citation statements)

References 149 publications

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“…Modeling showed that the disintegration time increased with increasing tableting pressure ( Figure 3) reflecting a reduced porosity of the FDF surface which limits access of the dissolution medium (Panakanti and Narang, 2012). The estimated DIC indicated liberation of API particles via surface erosion (DIC > 0) without significant anisotropy.…”

Section: Discussionmentioning

confidence: 98%

“…Drug instability or formation of drug complexes with low solubility in the GI tract can negatively affect bioavailability (Panakanti and Narang, 2012). Accounting for the potential degradation of the API under in vitro conditions is therefore important and was thus incorporated into our model via equations (A.1), (3.8), (3.11), (3.12).and (4.4).…”

Section: Discussionmentioning

confidence: 99%

“…form(s) with lower solubility] (Ostwald, 1897;Shefter and Higuchi, 1963). Chemical instability of dissolved API represents an additional complexity that may influence the dissolution profiles and bioavailability (Panakanti and Narang, 2012;Singhal and Curatolo, 2004). Overall, these processes impose challenges for the precise determination of API solubility and the description of dissolution profiles by current models that usually do not account for disintegration.…”

Section: Introductionmentioning

confidence: 99%

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Population data analysis of dissolution time profiles: Assessment of physicochemical properties of the drug, drug particles and the pharmaceutical formulation

Horkovics-Kovats

Brunovský

Pichler

et al. 2015

European Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Population data analysis of dissolution time profiles: Assessment of physicochemical properties of the drug, drug particles and the pharmaceutical formulation

Horkovics-Kovats

Brunovský

Pichler

et al. 2015

European Journal of Pharmaceutical Sciences

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“…The term bioavailability refers to the rate and extent at which the active drug reaches the systemic circulation [17,18,19]. Many factors may influence the bioavailability of drugs, which may be related to the dosage form, the manufacturing process and the drug itself [20,21,22,23].…”

Section: Oral Administration Of Poorly Water-soluble Drugsmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology.

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“…The 'ideal' excipient should be pharmacologically inactive, physically and chemically inert, compatible with other formulation components, colorless, has a good flowability, available from many sources, cost effective and stable (Pifferi et al, 1999). The use of poor excipient can cause drug instability, decreased bioavailability or interaction with a drug to become toxic and harmful to the patient (Panakanti and Narang, 2012).…”

Section: Introductionmentioning

confidence: 99%

Antisolvent precipitation of novel xylitol-additive crystals to engineer tablets with improved pharmaceutical performance

Kaialy

Maniruzzaman

Shojaee

et al. 2014

International Journal of Pharmaceutics

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The purpose of this work was to develop stable xylitol particles with modified physical properties, improved compactibility and enhanced pharmaceutical performance without altering polymorphic form of xylitol. Xylitol was crystallized using antisolvent crystallization technique in the presence of various hydrophilic polymer additives, i.e., polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) at a range of concentrations. The crystallization process did not influence the stable polymorphic form or true density of xylitol. However, botryoidal-shaped crystallized xylitols demonstrated different particle morphologies and lower powder bulk and tap densities in comparison to subangular-shaped commercial xylitol. Xylitol crystallized without additive and xylitol crystallized in the presence of PVP or PVA demonstrated significant improvement in hardness of directly compressed tablets; however, such improvement was observed to lesser extent for xylitol crystallized in the presence of PEG. Crystallized xylitols produced enhanced dissolution profiles for indomethacin in comparison to original xylitol. The influence of additive concentration on tablet hardness was dependent on the type of additive, whereas an increased concentration of all additives provided an improvement in the dissolution behavior of indomethacin. Antisolvent crystallization using judiciously selected type and concentration of additive can be a potential approach to prepare xylitol powders with promising physicomechanical and pharmaceutical properties.

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Impact of Excipient Interactions on Drug Bioavailability from Solid Dosage Forms

Cited by 13 publications

References 149 publications

Population data analysis of dissolution time profiles: Assessment of physicochemical properties of the drug, drug particles and the pharmaceutical formulation

Population data analysis of dissolution time profiles: Assessment of physicochemical properties of the drug, drug particles and the pharmaceutical formulation

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Antisolvent precipitation of novel xylitol-additive crystals to engineer tablets with improved pharmaceutical performance

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