Cyclosporin oral solution

Cyclosporine oral solution each milliliter contains cyclosporin 100 mg and alcohol 12.5% by volume dissolved in an olive oil, Labrafil M 1944 CS (polyoxyethy-lated oleic glycerides) vehicle that must be further diluted... 

Cyclosporine injection Cyclosporine oral solution Desflurane... 

Ahsan N, Johnson C, GonwaT, Halloran P, Stegall M, Hardy M, Metzger R, Shield C, III, Rocher L, Scandling J, Sorensen J, Mulloy L, Light J, Corwin C, DanovitchG,WachsM, VanVeldhuisen P, Salm K,Tolzman D, Fitzsimmons WE. Randomized trial of tacrolimus plus mycophenolate mofetil or azathioprine versus cyclosporine oral solution (modified) plus mycophenolate mofetil after cadaveric kidney transplantation results at 2 years. Transplantation 2001 72 245-250. 

An order was written for 30 mg Cyclosporine (immunosuppressant) oral solution to be administered to a pediatric patient. However, for several days, the nurse administered 300 mg believing that the syringe was calibrated in mg not mL. The oral solution is available as 100 mg/mL. As the pharmacist reviewed the error, he noted that the syringes accompanying the medication were never designed for pediatrics. It is not possible to calculate any dose less than 50 mg. It is imderstandable how the nurse assumed that the 3 mark was for 30 mg since it is positioned between 2,5 and 3,5 (which are European style for the decimals 2.5 and 3.5). To harmonize products in the global market, the manufacturer chose to follow European convention for expressing numbers which uses commas and decimals in the reverse manner as in the United States. 

NEORAL (Novartis) (cyclosporine capsules, oral solution, USP) March 2004 labeling... 

Similar labeling language also in the labeling of PROGRAF (Fujisawa) tacrolimus capsules, tacrolimus injection (for intravenous infusion only), July 2001 RAPAMUNE (Wyeth-Ayerst) (sirolimus) oral solution and tablets, August 2004 and GENGRAF capsules (Abbott) (cyclosporine) capsules, USP, January 2003. 

Erratic absorption of soft gelatin capsules and oral solution necessitates 2 Si. repeated monitoring of cyclosporine blood levels... 

The first commercial formulation of cyclosporin (Sandimmun) contained drug, LCT, ethanol, and polyglycolized LCT administered as either an oral solution/dispersion in water or milk or filled into a soft gelatin capsule. The soft-gel formulation produced a crude oil in water emulsion on capsule rupture in situ. The biopharmaceutical performance of the Sandimmun formulation, however, was relatively poor, because absorption was variable, incomplete (=30%), and affected by food [63-67],... 

Propylene glycol, 42% ethanol, glycerin, Gremophor RH 40, peppermint oil, water. 11.9% Ethanol, dl-Q -tocopherol, corn oil-mono-di-triglycerides, Gremophor RH 40, propylene glycol. Kaletra oral solution (Lopinavir and ritonavir) Neoral oral solution (Cyclosporin A)... 

Italia JL, Datta P, Ankola DD, Kumar MNVR. Nanoparticles enhance per oral bioavaUabiUty of poorly available molecules Epigallocatechin gallate nanoparticles ameUorates cyclosporine induced nephrotoxicity in rats at three times lower dose than oral solution. / Biomed Nanotechnol. 2008 4(3) 304-312. 

Surfactants are employed in nanoparticle suspensions. Chen et al. (2002) evaluated the pre paration of amorphous nanoparticle suspensions containing cyclosporine A using the evaporative precipitation into aqueous solution (ERAS) system. The effect of particle size was studied varying the drug surfactant ratios, type of surfactants, temperature, drug load, and solvent. Acceptable particle sizes suitable for both oral and parenteral administration were also studied. Additional articles in the nanoparticle delivery of poorly water-soluble drugs include Kipp (2004), Perkins et al. (2000), Young et al. (2000), and Tyner et al. (2004). 

Paclitaxel is an antitumor drug, with a low oral bioavailability (6%) [96] due to poor water solubility, hydrophobicity (log P = 4), and its high affinity to P-gp and CYP3A4. A novel SMEDDS of paclitaxel increased the bioavailability by up to 1.5-fold in comparison to the commercial micellar solution taxol. Concomitant intake of cyclosporine A, a known P-gp inhibitor, further increased paclitaxel bioavailability (1.8-fold in comparison to taxol) [97]. 

C. T. Ueda, M. Lemaire, G. Gsell, and K. Nussbaumer, Intestinal lymphatic absorption of cyclosporin A following oral administration in an olive oil solution to rats, Biopharm. Drug. Dispos. 4 113-124 (1983). 

An enhancement in the absorption of orally administered cyclosporin A (10 mg) was observed, as evidenced by an increase in the AUC, when a solution... 

Unfortunately, the number of commercial formulations is very limited, primarily because of stability and manufacturing problems encountered during large-scale production. The list includes Sandimmune Neoral (cyclosporine A Novartis AG, Switzerland), which contains a microemulsion preconcentrate and is available as soft gels and solutions. Sandimmune (cyclosporine A Novartis AG, Switzerland), which contains an emulsion preconcentrate, and lipid soluble vitamins. Both formulations of cyclosporine have self-emulsifying properties and spontaneously form an o/w microemulsion (particle size <0.15 pm) and an o/w emulsion, respectively in the aqueous fluids of the GI tract. Although the discussion concerning potential of liposomes, niosomes, microemulsions, and solid dispersions for oral delivery is outside the scope of this chapter, the interested reader is referred to recently published reviews on these topics. " ... 

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