Studies on the promoting effects of carboxylic acid derivatives on the rectal absorption of .BETA.-lactam antibiotics in rats.

Nishimura, Kenichi; Nozaki, Yoshihiro; Yoshimi, Akira; Nakamura, Syohei; Kitagawa, Meiko; Kakeya, Nobuharu; Kitao, K.

doi:10.1248/cpb.33.282

Cited by 59 publications

(15 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Such a rule indicates that the surface saturation for surfactants will occur at lower concentrations, which is why CMC decreases so significantly with increasing alkyl chain length, and goes some way to explaining why there is such a significant increase in intestinal epithelial permeation enhancement in MCFA moving from C 8 to C 12 . When the CMC and efficiency of membrane insertion are both considered, the most effective alkyl chain length for MCFA and alkyl sulphates is between C 10 and C 12 [150,166]. Fatty acids of uneven chain length are less widely studied than conventional fatty acids, but they also demonstrate efficacy (e.g.C 9 , C 11 , in CMC between C 10 (23 mM) and saturated C 11:0 (5 mM) would suggest that a higher level of C 10 will be available to enhance permeability in instillations at a concentration of 100mM, yet unsaturation of the C 11:1 (17 mM) at carbon 10 significantly raises the CMC.…”

Section: Hlb In Permeation Enhancementmentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

291

201

View full text Add to dashboard Cite

Publication informationAdvanced Drug Delivery Reviews, (Part B): 277-319 Publisher ElsevierItem record/more information http://hdl.handle.net/10197/7800Publisher's statement þÿ T h i s i s t h e a u t h o r s v e r s i o n o f a w o r k t h a t w a s a c c e p t e d f o r p u b l i c a t i o n i n A d v a n c e d D r u g Delivery Reviews. Changes resulting from the publishing process, such as peer review,

show abstract

Section: Hlb In Permeation Enhancementmentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

291

201

View full text Add to dashboard Cite

show abstract

“…However, it is now clear that the CMC alone is not the overriding factor in determining the effectiveness of MCFAs in increasing transmucosal drug flux [179]. In general, both very non-polar and highly polar surfactants are poor promoters; the optimum is in the midrange [169].…”

Section: [222] Physicochemical Properties Of C 10 In Solutionmentioning

confidence: 99%

Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic

Maher

Leonard²,

Jacobsen

et al. 2009

Advanced Drug Delivery Reviews

201

176

View full text Add to dashboard Cite

A major challenge in oral drug delivery is the development of novel dosage forms to promote absorption of poorly permeable Class III drugs across the intestinal epithelium.To date, no absorption promoter has been approved in a formulation specifically designed for oral delivery of Class III molecules. Promoters that are designated safe for human consumption have been licensed for use in a recently approved buccal insulin spray delivery system and also for many years as part of an ampicillin rectal suppository.Unlike buccal and rectal delivery, oral formulations containing absorption promoters have the additional technical hurdle whereby the promoter and payload must be coreleased in high concentrations at the small intestinal epithelium in order to generate significant but rapidly reversible increases in permeability. The most advanced promoter in the clinic is the medium chain fatty acid (MCFA), sodium caprate (C 10 ) , a compound already approved as a direct food additive. We discuss how it has evolved to a matrix tablet format suitable for administration to humans under the headings of mechanism of action at the cellular and tissue level and in vitro and in vivo efficacy and safety studies.In specific clinical examples, we review how C 10 -based formulations are being tested for oral delivery of bisphosphonates using Gastro Intestinal Permeation Enhancement Technology, GIPET® (Merrion Pharmaceuticals, Ireland) and in a related solid dose format for anti-sense oligonucleotides (ISIS Pharmaceuticals, USA).Keywords: Oral drug delivery, Sodium caprate (C 10 ), absorption promoter, drug delivery platforms, clinical trials, oral formulation, drug delivery systems.3 TJs form a barrier to the uncontrolled absorption of noxious luminal antigens (gate function), and maintain epithelial polarity (fence function) [8,9]. In general, the TJ consists of a restrictive pathway (shunt) with a sharp molecular size cut off, and a second unrestrictive pathway (small pore) that permits paracellular permeation of molecules of radii <4.0 Å [10,11]. Depending on the intestinal region, TJ pore sizes range from 6-22Å, sufficient to permit mannitol (6.7 Å) and EDTA (10.8 Å) to permeate to an extent, whereas the passage of inulin (30-40 Å) and fluorescent-dextran 4kDa (FD-4, 26 Å) is essentially impeded [12][13][14][15][16].A number of approaches have been used to promote oral delivery of Class III drugs ( Alternatively, the use of nanoparticles comprising biocompatible polymers (e.g. chitosan,polylactide-co-glycolide, starch and glucans) can protect cargoes from GI proteases, increase GI retention and promote absorption across gut associated lymphoid tissue (GALT) and to a lesser extent, enterocytes [45][46][47]. Most data on nanoparticle absorption from rodent models suggest that M cells in the follicle-associated epithelium of Peyer's patches (PP) are the favored site of uptake for particles of diameter 500nm-1000nm [45].Given the paucity of M cells in the GI tract of adults, the relevance of PP uptake remains controversial ...

show abstract

“…2,4) In order to develop the safe formulation that can improve the absorption of drugs categorized into BCS Class IV such as rebamipide, [14][15][16][17][18][19][20] we have compared the suppository that contains sodium laurate (C12) as an absorption enhancer and taurine (Tau) as a cytoprotective adjuvant with the commercial suppository that contains sodium caprate (C10) as an absorption enhancer. [21][22][23] We have found that C12, a mediumchain fatty acid salt, is a promising absorption enhancer and better than C10 in terms of the absorption improving ability, 24) and that Tau has the most effective cytoprotective activity among amino acids examined. 25) Cytoprotective action by Tau has been evidenced by both biochemical [25][26][27] and histopathological 25) approaches and it has been partially related with the suppression of intracellular Ca 2ϩ level elevated by C12 and the inhibition of histamine release induced by C12.…”

mentioning

confidence: 99%

Optimization of Suppository Preparation Containing Sodium Laurate and Taurine That Can Safely Improve Rectal Absorption of Rebamipide

Miyake

Minami

Oka

et al. 2006

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

Drug absorption from gastrointestinal tract is mainly influenced by solubility and permeability. As a technique of the improvement of solubility, micronization, amorphousization and the addition of surfactant such as Tween 80 and Captisol ® are well known. As for the improvement of permeability, the use of absorption enhancers is well known, [1][2][3][4][5][6][7][8][9][10][11] but the practical use of them has been very limited 12,13) because of the potential local toxicity to gastrointestinal mucosa. 2,4) In order to develop the safe formulation that can improve the absorption of drugs categorized into BCS Class IV such as rebamipide, [14][15][16][17][18][19][20] we have compared the suppository that contains sodium laurate (C12) as an absorption enhancer and taurine (Tau) as a cytoprotective adjuvant with the commercial suppository that contains sodium caprate (C10) as an absorption enhancer. [21][22][23] We have found that C12, a mediumchain fatty acid salt, is a promising absorption enhancer and better than C10 in terms of the absorption improving ability, 24) and that Tau has the most effective cytoprotective activity among amino acids examined. 25) Cytoprotective action by Tau has been evidenced by both biochemical [25][26][27] and histopathological 25) approaches and it has been partially related with the suppression of intracellular Ca 2ϩ level elevated by C12 and the inhibition of histamine release induced by C12. L-Glutamine (L-Gln) also has the cytoprotective action, which is partially attributed to the induction of heat-shock protein 70 (HSP70), 27) a factor protecting cells from injuries caused by several kinds of stresses. 28,29) Furthermore, basic studies for suppository were performed in rats by administering the fatty or water-soluble base preparation containing rebamipide, C12 and Tau or L-Gln into rats. The combinatorial use of them, especially for the fatty base (FB) suppository, has been evidenced to be promising in terms of both improvement of bioavailability and safety to rat rectal mucosa.30) However, the success in the scaling-up study must be necessary for developing the formulation available for human use.In the present study, we have, therefore, performed the scaling-up study of animal and formulation size using FB suppositories of rebamipide and have compared our new preparations with the commercial suppository containing C10 (15 or 25 mg) in terms of the drug dissolution, absorption improvement and safety to the rectal mucosa of rabbits. MATERIALS AND METHODSMaterials C12, C10 and Tau were purchased from Tokyo Chemical Industry Co. (Tokyo, Japan). Hydroxypropyl methylcellulose (HPMC) TC-5E (HPMC 2910) was purchased from Shin-etsu Kagaku Co. (Tokyo). Witepsol ® H-15 was obtained from Mitsuba Boueki Co. Ltd. (Tokyo). Rebamipide and OPC-12853, an internal standard, were obtained from Otsuka Pharmaceutical Co. Ltd. (Tokushima, Japan). All other reagents were analytical grade commercial products.Animals Male Japan-White rabbits (Kitayama Labes, Ina, Japan), maintained at 23°C and 60% hum...

show abstract

Studies on the promoting effects of carboxylic acid derivatives on the rectal absorption of .BETA.-lactam antibiotics in rats.

Cited by 59 publications

References 0 publications

Intestinal permeation enhancers for oral peptide delivery

Intestinal permeation enhancers for oral peptide delivery

Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic

Optimization of Suppository Preparation Containing Sodium Laurate and Taurine That Can Safely Improve Rectal Absorption of Rebamipide

Contact Info

Product

Resources

About