In-vitro permeability of porcine oral mucosa after epithelial separation, stripping and hydration

Squier, C. A.; Hall, B.K.

doi:10.1016/0003-9969(85)90095-0

Cited by 54 publications

(13 citation statements)

References 16 publications

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“…Le Brun et al15 preserved the buccal tissue in PBS (pH 7.4) for several days and found that the permeability of propranolol decreased over the storage period. Other investigators, however, have shown an increase in permeability after storage in aqueous buffers 21. de Vries et al22 stored the buccal mucosa at room temperature up to 24 h prior to conducting the experiments.…”

Section: Discussionmentioning

confidence: 98%

“…Therefore, successful removal of the connective tissue is essential to minimize the variability between the tissue specimens and, hence, of the permeability measurements. Since the procedure of removing connective tissue with surgical scissors is time consuming and requires skill and patience, many researchers have developed chemical,7, 21, 45 thermal,7 and enzymatic methods (such as the use of collagenase46–49) for teasing away the buccal epithelium from the underlying connective tissue. Mechanical separation with a dermatome7, 50 or other surgical instrument18, 26 was also tried.…”

Section: Discussionmentioning

confidence: 99%

“…Mechanical separation with a dermatome7, 50 or other surgical instrument18, 26 was also tried. However, the dermatome may damage the tissue and render it fragile 21. Mechanical separation with a dermatome may also cut through the papillae,21 while surgical separation with scissors and forceps is technically difficult and time‐consuming.…”

Section: Discussionmentioning

confidence: 99%

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Porcine buccal mucosa as in vitro model: Effect of biological and experimental variables

Kulkarni

Ravichandran

Pather

et al. 2010

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

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Porcine buccal mucosa as in vitro model: Effect of biological and experimental variables

Kulkarni

Ravichandran

Pather

et al. 2010

Journal of Pharmaceutical Sciences

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“…In-vitro and in-vivo Study Methods 19,20,21,22 Animal Models for Studies: The limited available tissue area in the human buccal cavity has encouraged the use of animal models that may mimic human oral mucosal absorption. Rats, hamsters, dogs, rabbits, guinea pigs, and rhesus monkeys have all been used in buccal studies.…”

Section: Fig 7: Three Stages In the Interaction Between A Mucoadhesimentioning

confidence: 99%

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2012

IJPSR

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Oral mucosal drug delivery system is widely applicable as novel site for administration of drug for immediate and controlled release action by preventing first pass metabolism and enzymatic degradation due to GI microbial flora. Oral mucosal drug delivery system provides local and systemic action. In this review, attention is focused to give regarding physiology of oral mucosal including tissue permeability, barriers to permeation and route of permeation, biopharmaceutics of buccal and sublingual absorption, factors affecting drug absorption, detailed information of penetration enhancers, design of oral mucosal drug delivery system and role of mucoadhesion and various theories of bioadhesion. Evaluation techniques and selection of animal model for in-vivo studies are also discussed.

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“…Because of thin mucosa (190 μm) and excellent blood flow in the sublingual region, rapid absorption leading to the rapid onset of action is possible following sublingual administration of propranolol, in view of its molecular size and lipophilicity (9). In addition, the high liver first-pass effect of propranolol can also be avoided with the sublingual route, leading to a higher bioavailability, since the drug can be absorbed directly into the systemic circulation (10). Not surprisingly, sublingual propranolol administration has been demonstrated to result in a higher bioavailability than that following oral administration of the conventional tablet (Inderal ® ) (11).…”

Section: Introductionmentioning

confidence: 99%

Clinical Pharmacokinetics of Buffered Propranolol Sublingual Tablet (Promptol™)—Application of a New “Physiologically Based” Model to Assess Absorption and Disposition

Wang

Zuo

et al. 2013

AAPS J

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Abstract. Sublingual administration of certain buffered propranolol may improve the rate and extent of absorption compared to oral administration. The main objectives of this study were to (1) compare the plasma propranolol concentrations (Cp-prop) following sublingual administration of a specially buffered formulation (Promptol™) to that following oral administration of Inderal ® and (2) evaluate the utility of a special pharmacokinetic model in describing the Cp-prop following sublingual administration. Eighteen healthy volunteers received 10 mg sublingual Promptol™ or oral Inderal ® . Multiple Cp-prop were determined and their pharmacokinetics compared. Additional data following sublingual 40 mg Promptol™ or Inderal ® were utilized for evaluation of a special advanced compartmental absorption and transit (ACAT) model. For model simulation, the physicochemical parameters were imported from AMET predictor, whereas the pharmacokinetic parameters were calculated and optimized by Gastroplus ® . Based on this model, the quantity of drug absorbed via buccal/sublingual mucosa was estimated. Cp-prop was higher at earlier times with 3-fold greater relative bioavailability following sublingual Promptol™ compared to that from oral Inderal ® . The special ACAT model provided excellent goodness of fit of Cp-prop-time curve and estimated a 56.6% increase in absorption rate from Promptol™ and higher initial Cp-prop compared to the regular formulation. The modified ACAT model provided a useful approach to describe sublingual absorption of propranolol and clearly demonstrated an improvement of absorption of Promptol™. The sublingual 10 mg Promptol™ achieved not only a similar systemic exposure as 30 mg oral Inderal ® but an earlier effective Cp-prop which may be advantageous for certain clinical conditions.

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In-vitro permeability of porcine oral mucosa after epithelial separation, stripping and hydration

Cited by 54 publications

References 16 publications

Porcine buccal mucosa as in vitro model: Effect of biological and experimental variables

Porcine buccal mucosa as in vitro model: Effect of biological and experimental variables

Untitled

Clinical Pharmacokinetics of Buffered Propranolol Sublingual Tablet (Promptol™)—Application of a New “Physiologically Based” Model to Assess Absorption and Disposition

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