Gastrointestinal Dissolution and Absorption of Drugs

Granero, Gladys E.; Ramachandran, Chandrasekharan; Amidon, Gordon L.

doi:10.1002/3527601473.ch8

Cited by 9 publications

(9 citation statements)

References 39 publications

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“…Accordingly, ibuprofen may also fit in the newly proposed “intermediate solubility class” suggested for acids and bases that are highly soluble at either physiologically relevant pH 1.2 or 6.8 42,43. Current publications also suggest pH‐dependent soluble, highly permeable, weak acidic ionizable drug compounds should be handled like BCS class I drugs 44,45. This evaluation is supported by Rinaki et al46 who emphasized the dynamic character of the absorption process, as drug dissolution is promoted by high permeability for highly permeable acidic NSAIDs like ibuprofen.…”

Section: Discussionmentioning

confidence: 99%

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Ibuprofen**This paper reflects the scientific opinion of the authors and not the policies of regulating agencies.

Potthast

Dressman

Junginger

et al. 2005

Journal of Pharmaceutical Sciences

201

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Section: Discussionmentioning

confidence: 99%

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Ibuprofen**This paper reflects the scientific opinion of the authors and not the policies of regulating agencies.

Potthast

Dressman

Junginger

et al. 2005

Journal of Pharmaceutical Sciences

201

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“…solubility, diffusivity, stability, and p K a) and physiological barriers (e.g. transit time through the different GI segments and absorption mechanisms) [ 40 ] . Based on the biopharmaceutics classifi cation system (BCS), drug substances are classifi ed into four categories according to their solubility and permeability properties, as shown in Fig.…”

Section: Drugs Of Poor Oral Bioavailabilitymentioning

confidence: 99%

Drugs for Long Acting Injections and Implants

Shen

Burgess

2011

Long Acting Injections and Implants

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Long acting injections and implants have been developed for controlled drug delivery to improve therapeutic effects, decrease dosing frequency, and also avoid potential drug toxicity. Many pharmaceutical agents, such as biomacromolecules (e.g. peptides, proteins and gene therapeutics), drugs with poor bioavailability, and drugs for local delivery are good candidates for developing long acting injections and implants. However, not all drugs are suitable for these formulations (for example, drugs with high dose or narrow therapeutic index). IntroductionDrug formulations should deliver the API (active pharmaceutical agent) to the site of action at the correct therapeutic concentration for as long as the treatment is desired. The therapeutic and the physicochemical properties of a drug determine the preferred route of administration (oral or parenteral) as well as the most appropriate delivery systems.Due to convenience and patient acceptability, oral drug delivery is the most attractive and preferred route for administering medicines. However, some drugs cannot be tolerated via the oral route due to the acid environment and the variety of proteolytic enzymes (proteases) in the gastrointestinal tract (GIT). These conditions tend to degrade or metabolize drugs such as proteins and peptides, resulting in low bioavailability [ 1 ] . Moreover, patients who are unable to tolerate oral ingestion (e.g. patients with aspiration problems or GI disorders) require nonoral administration (e.g. parenteral administration) to receive medications and nutrition. Parenteral administration (e.g. intravenous, intramuscular, and subcutaneous) is also useful

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“…However, the intestinal transit time influences the absorption of drugs with limited mucosal permeability, carrier-mediated uptake, drugs subject to intestinal degradation, or products whose dissolution is the rate-limiting step the for systemic absorption (Martinez et al, 2002). In contrast to the gastric transit time, the intestinal transit time is independent of the feeding conditions and the physical composition of the intestinal contents (Garanero et al, 2005). The intestinal transit time in rats, dogs, and humans is around 3-4 h (Dressman, 1986;Stenberg et al, 2002).…”

Section: Physiological Factors That Impact Oral Drugmentioning

confidence: 99%