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Chemical Compound Review

FODIPIR     2-[2-[carboxymethyl-[[3- hydroxy-2-methyl-5...

Synonyms: CHEMBL1208640, AC1L1TPQ, LS-187177, D04241, 118248-91-2, ...
 
 
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Disease relevance of FODIPIR

  • METHODS: Six episodes of acute pancreatitis were repeatedly induced at weekly intervals in mice receiving either recombinant TGF-beta (4 micrograms in 4 days) or excipient alone at each induction [1].
  • Likewise, animals bearing MCA-105 and -106 sarcomas treated with 6 to 10 micrograms rHTNF had significantly increased survival compared with excipient-treated control animals [2].
  • Twenty-four hours after embolization and treatment with either thrombolytic agent or excipient, the brains are removed, fixed, and evaluated for cerebral hemorrhage [3].
  • Purulent sputa from 18 patients with cystic fibrosis (CF) were incubated with either rhDNase (4 microg/ml) or control excipient [4].
  • Hypophysectomized rats were given daily sc injections of excipient, hGH, rhGHBP, or rhGH plus rhGHBP (produced in Escherichia coli) for 7 days [5].
 

High impact information on FODIPIR

 

Chemical compound and disease context of FODIPIR

 

Biological context of FODIPIR

  • All were in a stable clinical state at the commencement of the study, and they received (1) rhDNase 2.5 mg twice daily, (2) rhDNase once daily, or (3) placebo (excipient only) inhalation [16].
  • This study of healthy volunteers shows that the relative bioavailability of albendazole formulations that use arachis oil-polysorbate 80 or hydroxypropyl-beta-cyclodextrin as an excipient was enhanced 4.3- and 9.7-fold compared to the results seen with commercial tablets [17].
  • When a high content of a water-insoluble excipient (i.e., microcrystalline cellulose) was used to fabricate the tablets, the release kinetics deviated from linearity (n = 0.73) [18].
  • The physical state of lactose remained constant throughout the duration of the study, and the rate of hydrolysis was not significantly different from the control formulation containing no excipient [19].
  • Prednisolone's therapeutic indications and therapeutic index, pharmacokinetics, and the possibility of excipient interactions were also taken into consideration [20].
 

Anatomical context of FODIPIR

  • To eliminate possible contributions to increased permeability by (a) LAK cells generated in vivo, or (b) circulating leukocytes, we isolated lungs from normal rats and perfused them for 5 min with a cell-free perfusate containing IL-2 (2, 10, or 5 X 10(-3) U/ml) excipient or 0.9% NaCl placebo [21].
  • G-CSF triggered marked recruitment of dendritic cells (DCs), particularly immature CD11c(lo)B220(+) plasmacytoid DCs, with reduced costimulatory signal expression and higher interferon-alpha but lower interleukin-12p70 release capacity than DCs in excipient-treated mice [22].
  • It also did not prevent the T-lymphocyte recruitment associated with HP, although these cells did not proliferate in response to the F. rectivirgula antigen, in contrast to BAL cells from F. rectivirgula-challenged mice treated with excipient only.(ABSTRACT TRUNCATED AT 250 WORDS)[23]
  • Biodegradable controlled-release microspheres made with the biocompatible biodegradable polyester excipient poly (DL-lactide-co-glycolide) represent a new technology for drug delivery to the central nervous system (CNS) [24].
  • In other experiments, animals were gavaged with Scios SD-169 (10 or 30 mg/kg) or excipient (PEG300) 1 day before and daily after crush injury to the sciatic nerve [25].
 

Associations of FODIPIR with other chemical compounds

 

Gene context of FODIPIR

  • IL-2, but not the excipient detergents included in the rIL-2 preparation, induced the synthesis of both cytokines [30].
  • Other groups received hGH (500 microg/day, sc, bid), recombinant human insulin-like growth factor (rhIGF)-1 (750 microg/day, sc, infusion) or excipient, alone or in combination [31].
  • These MPO levels contrasted with our earlier studies in normal rats which revealed no significant difference in tissue MPO levels following injection of excipient or rTNF-alpha [32].
  • Preparation of excipient-free recombinant human tissue-type plasminogen activator by lyophilization from ammonium bicarbonate solution: an investigation of the two-stage sublimation phenomenon [33].
  • The recombinant production of the VP1 protein offers a save way to obtain a highly purified, non pathogenic pharmaceutical excipient [34].
 

Analytical, diagnostic and therapeutic context of FODIPIR

  • Following a 1-h postinfusion survival time, the brain tissue of five rIL-2 infused and three excipient infused animals was processed and examined by light microscopy and electron microscopy for evidence of altered cerebrovascular permeability to systemically circulating horseradish peroxidase [35].
  • FTIR imaging shows great promise in its ability to visualize the drug and excipient distribution in pharmaceutical formulations such as tablets and therapeutic transdermal systems, as well as to reveal the mechanism of drug release [36].
  • Addition of excipient stabilized the secondary structure upon lyophilization to a varying extent depending on the formulation [37].
  • The polymer generated within this study represents a promising novel excipient for various drug delivery systems in which in situ gelling properties are favorable [38].
  • Four intact and four ovariectomized heifers received subcutaneous injection of bGH (15 mg/day) for 15 weeks starting at 176 +/- 3 days of age (147 +/- 3 kg body weight), while the remaining eight heifers received an equal volume of excipient [39].

References

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  2. Studies on the anti-tumor efficacy of systemically administered recombinant tumor necrosis factor against several murine tumors in vivo. Asher, A., Mulé, J.J., Reichert, C.M., Shiloni, E., Rosenberg, S.A. J. Immunol. (1987) [Pubmed]
  3. A long-half-life and fibrin-specific form of tissue plasminogen activator in rabbit models of embolic stroke and peripheral bleeding. Thomas, G.R., Thibodeaux, H., Errett, C.J., Badillo, J.M., Keyt, B.A., Refino, C.J., Zivin, J.A., Bennett, W.F. Stroke (1994) [Pubmed]
  4. Improvement of cystic fibrosis airway mucus transportability by recombinant human DNase is related to changes in phospholipid profile. Zahm, J.M., Galabert, C., Chaffin, A., Chazalette, J.P., Grosskopf, C., Puchelle, E. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  5. Recombinant human growth hormone (GH)-binding protein enhances the growth-promoting activity of human GH in the rat. Clark, R.G., Mortensen, D.L., Carlsson, L.M., Spencer, S.A., McKay, P., Mulkerrin, M., Moore, J., Cunningham, B.C. Endocrinology (1996) [Pubmed]
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  13. Hydroxyectoine is superior to trehalose for anhydrobiotic engineering of Pseudomonas putida KT2440. Manzanera, M., García de Castro, A., Tøndervik, A., Rayner-Brandes, M., Strøm, A.R., Tunnacliffe, A. Appl. Environ. Microbiol. (2002) [Pubmed]
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  15. Development of aqueous parenteral formulations for carbamazepine through the use of modified cyclodextrins. Brewster, M.E., Anderson, W.R., Estes, K.S., Bodor, N. Journal of pharmaceutical sciences. (1991) [Pubmed]
  16. Short-term recombinant human DNase in bronchiectasis. Effect on clinical state and in vitro sputum transportability. Wills, P.J., Wodehouse, T., Corkery, K., Mallon, K., Wilson, R., Cole, P.J. Am. J. Respir. Crit. Care Med. (1996) [Pubmed]
  17. Relative bioavailability of three newly developed albendazole formulations: a randomized crossover study with healthy volunteers. Rigter, I.M., Schipper, H.G., Koopmans, R.P., van Kan, H.J., Frijlink, H.W., Kager, P.A., Guchelaar, H.J. Antimicrob. Agents Chemother. (2004) [Pubmed]
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  19. The effect of bulking agent on the solid-state stability of freeze-dried methylprednisolone sodium succinate. Herman, B.D., Sinclair, B.D., Milton, N., Nail, S.L. Pharm. Res. (1994) [Pubmed]
  20. Biowaiver monographs for immediate release solid oral dosage forms: Prednisolone. Vogt, M., Derendorf, H., Kr??mer, J., Junginger, H.E., Midha, K.K., Shah, V.P., Stavchansky, S., Dressman, J.B., Barends, D.M. Journal of pharmaceutical sciences (2007) [Pubmed]
  21. Increase of rat pulmonary microvascular permeability to albumin by recombinant interleukin-2. Fairman, R.P., Glauser, F.L., Merchant, R.E., Bechard, D., Fowler, A.A. Cancer Res. (1987) [Pubmed]
  22. Treatment with granulocyte colony-stimulating factor prevents diabetes in NOD mice by recruiting plasmacytoid dendritic cells and functional CD4(+)CD25(+) regulatory T-cells. Kared, H., Masson, A., Adle-Biassette, H., Bach, J.F., Chatenoud, L., Zavala, F. Diabetes (2005) [Pubmed]
  23. Murine hypersensitivity pneumonitis: a study of cellular infiltrates and cytokine production and its modulation by cyclosporin A. Denis, M., Cormier, Y., Laviolette, M. Am. J. Respir. Cell Mol. Biol. (1992) [Pubmed]
  24. Transmitter-loaded polymeric microspheres induce regrowth of dopaminergic nerve terminals in striata of rats with 6-OH-DA induced parkinsonism. McRae, A., Dahlström, A. Neurochem. Int. (1994) [Pubmed]
  25. Inhibition of p38 MAP kinase activity enhances axonal regeneration. Myers, R.R., Sekiguchi, Y., Kikuchi, S., Scott, B., Medicherla, S., Protter, A., Campana, W.M. Exp. Neurol. (2003) [Pubmed]
  26. Rapidly disintegrating tablets prepared by the wet compression method: mechanism and optimization. Bi, Y., Yonezawa, Y., Sunada, H. Journal of pharmaceutical sciences. (1999) [Pubmed]
  27. Physical stability of salmon calcitonin spray-dried powders for inhalation. Chan, H.K., Clark, A.R., Feeley, J.C., Kuo, M.C., Lehrman, S.R., Pikal-Cleland, K., Miller, D.P., Vehring, R., Lechuga-Ballesteros, D. Journal of pharmaceutical sciences. (2004) [Pubmed]
  28. FTIR characterization of the secondary structure of proteins encapsulated within PLGA microspheres. Fu, K., Griebenow, K., Hsieh, L., Klibanov, A.M., LangerR, n.u.l.l. Journal of controlled release : official journal of the Controlled Release Society. (1999) [Pubmed]
  29. Promoter- and strain-selective enhancement of gene expression in a mouse skeletal muscle by a polymer excipient Pluronic P85. Yang, Z., Zhu, J., Sriadibhatla, S., Gebhart, C., Alakhov, V., Kabanov, A. Journal of controlled release : official journal of the Controlled Release Society. (2005) [Pubmed]
  30. IL-2 stimulates the production of IL-1 alpha and IL-1 beta by human peripheral blood mononuclear cells. Numerof, R.P., Aronson, F.R., Mier, J.W. J. Immunol. (1988) [Pubmed]
  31. Growth hormone secretagogues stimulate the hypothalamic-pituitary-adrenal axis and are diabetogenic in the Zucker diabetic fatty rat. Clark, R.G., Thomas, G.B., Mortensen, D.L., Won, W.B., Ma, Y.H., Tomlinson, E.E., Fairhall, K.M., Robinson, I.C. Endocrinology (1997) [Pubmed]
  32. Effects of an intratumoral injection of human recombinant tumor necrosis factor-alpha on cerebrovascular permeability and leukocytic infiltration in a rat glioma model. Wright, J.L., Merchant, R.E. Acta Neuropathol. (1997) [Pubmed]
  33. Preparation of excipient-free recombinant human tissue-type plasminogen activator by lyophilization from ammonium bicarbonate solution: an investigation of the two-stage sublimation phenomenon. Overcashier, D.E., Brooks, D.A., Costantino, H.R., Hsu, C.C. Journal of pharmaceutical sciences. (1997) [Pubmed]
  34. Recombinant virus like particles as drug delivery system. Georgens, C., Weyermann, J., Zimmer, A. Current pharmaceutical biotechnology. (2005) [Pubmed]
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  36. Pharmaceutical applications of Mid-IR and Raman spectroscopy. Wartewig, S., Neubert, R.H. Adv. Drug Deliv. Rev. (2005) [Pubmed]
  37. Effect of excipients on the stability and structure of lyophilized recombinant human growth hormone. Costantino, H.R., Carrasquillo, K.G., Cordero, R.A., Mumenthaler, M., Hsu, C.C., Griebenow, K. Journal of pharmaceutical sciences. (1998) [Pubmed]
  38. Improvement in the in situ gelling properties of deacetylated gellan gum by the immobilization of thiol groups. Krauland, A.H., Leitner, V.M., Bernkop-Schnürch, A. Journal of pharmaceutical sciences. (2003) [Pubmed]
  39. Effect of exogenous bovine growth hormone and ovariectomy on prepubertal mammary growth, serum hormones and acute in-vitro proliferative response of mammary explants from Holstein heifers. Purup, S., Sejrsen, K., Foldager, J., Akers, R.M. J. Endocrinol. (1993) [Pubmed]
 
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