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. Author manuscript; available in PMC: 2014 Nov 14.
Published in final edited form as: Recent Pat Nanomed. 2012;2(2):82–95. doi: 10.2174/1877912311202020082

Table 2.

Pharmacokinetic Parameters of 14C-Voclosporin Following Single or Repeat (QD for 7 Days) Dose of Mixed Nanomicellar Voclosporin Formulation in Female New Zealand Albino Rabbits

Ocular Tissue(s)/Fluids
& Blood
Cmax (ng eq./g) AUC (hr* ng eq./g) Tmax (hr) t1/2 (hr)
SD RD Ratio SD RD Ratio SD RD SD RD
Aqueous Humor 6 13 2.3 45 96 2.1 0.5 0.5 - 14
Choroid/Retina 48 76 1.6 472 897 1.9 1.0 2 23 -
Cornea 1203 3382 2.8 23166 54624 2.4 8.0 0.5 - -
Iris/Ciliary body 20 119 5.8 382 1952 5.1 24.0 1 - -
Lacrimal Gland 31 120 3.9 416 1109 2.7 2.0 4 - 6
Lens 4 26 6.7 47 356 7.5 24.0 0.5 - -
Lower Bulbar 1810 2929 1.6 12029 16585 1.4 0.5 0.5 10 7
Conjunctiva Lower Eyelid 20814 41635 2.0 207630 358791 1.7 1.0 0.5 - -
Nictitating membrane 1716 2468 1.4 12135 15964 1.3 0.5 0.5 7 8
Optic Nerve 83 164 2.0 569 1805 3.2 0.5 0.5 - 16
Sclera 223 367 1.6 2646 3825 1.4 0.5 0.5 - 16
Submandibular 74 120 1.6 893 1190 1.3 2.0 2 - -
Lymph Node Tear 20246 30904 1.5 168259 230878 1.4 0.5 0.5 - 7
Upper Bulbar 2235 3170 1.4 14782 19944 1.3 0.5 0.5 7 7
Conjunctiva Upper Eyelid 9896 17500 1.8 114651 98656 0.9 1.0 0.5 - 4
Vitreous Humor 2 2 1 27 23 0.9 8.0 4 - -
Blood BQL BQL NC NC NC NC NC NC NC NC
a

Time needed to achieve peak IOP increase.

b

Duration of IOP increase response (the time interval needed for the IOP to return to its normal pretreatment value).

c

Approximate values calculated from the slope ln (% increase in IOP)/Δt for the terminal points of % increase in IOPt versus t curves.

d

Ratio of AUC to the value for the commercial DEX (0.1, w/v, %) eye drops.

*

Statistically significant difference as compared with commercial DEX (0.1, w/v, %) eye drops (p < 0.05).

SD = Single dose;

RD = Repeat dose;

Ratio = Repeat dose/Single Dose.;

- = Insufficient tissue concentration to determine t1/2;

BQL = Below Quantifiable Limit (<0.1 ng/mL);

NC = Not calculated.