HP1003 USP EP Standard CAS 155206-00-1 Bimatoprost powder CAS NO.155206-00-1

Details:

1 basic information :

2  more information :

bimatoprost

bimatoprost is a powder, which is very soluble in ethyl alcohol and methyl alcohol and slightly soluble in water. treating increased pressure in the eye (ocular hypertension) and open-angle glaucoma.

its chemical name is (z)-7-[(1r,2r,3r,5s)-3,5-dihydroxy-2-[(1e,3s)-3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl]-n-ethyl-5-heptenamide, and its molecular weight is 415.58. its molecular formula is c25h37no4. its chemical structure is:

bimatoprost drops are a prostaglandin analog. it works to lower pressure in the eye by increasing fluid drainage from the eye.

bimatoprost ophthalmic solution

0.03% is indicated to treat hypotrichosis of the eyelashes by increasing their growth including length, thickness and darkness. 

clinical pharmacology

mechanism of action

bimatoprost is a structural prostaglandin analog. although the precise mechanism of action is unknown the growth of eyelashes is believed to occur by increasing the percent of hairs in, and the duration of the anagen or growth phase.

absorption

after one drop of bimatoprost ophthalmic solution 0.03% was administered once daily into both eyes (cornea and/or conjunctival sac) of 15 healthy subjects for two weeks, blood concentrations peaked within 10 minutes after dosing and were below the lower limit of detection (0.025 ng/ml) in most subjects within 1.5 hours after dosing. mean cmax and auc0-24hr values were similar on days 7 and 14 at approximately 0.08 ng/ml and 0.09 ng•hr/ml, respectively, indicating that steady state was reached during the first week of ocular dosing. there was no significant systemic drug accumulation over time.

distribution

bimatoprost is moderately distributed into body tissues with a steady-state volume of distribution of 0.67 l/kg. in human blood, bimatoprost resides mainly in the plasma. approximately 12% of bimatoprost remains unbound in human plasma.

metabolism

bimatoprost is the major circulating species in the blood once it reaches the systemic circulation. bimatoprost then undergoes oxidation, n-deethylation, and glucuronidation to form a diverse variety of metabolites.

elimination

following an intravenous dose of radiolabeled bimatoprost (3.12 mcg/kg) to six healthy subjects, the maximum blood concentration of unchanged drug was 12.2 ng/ml and decreased rapidly with an elimination half-life of approximately 45 minutes. the total blood clearance of bimatoprost was 1.5 l/hr/kg. up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.

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