Reformulation and drop size of apraclonidine hydrochloride.
We performed a prospective, double-masked, placebo-controlled, six-period, cross-over study in which normal subjects were randomly assigned to treatment and compared three different formulations of apraclonidine hydrochloride (the present commercially available formulation, and formulations with hydroxypropylmethylcellulose or lysolecithin). We also evaluated the efficacy of a 16-microliters and 30-microliters drop size. The magnitude and duration of decrease in intraocular pressure was comparable for all formulations. Most subjects tolerated all formulations well with only a few reporting any side effects. The best-tolerated formulation was 0.5% apraclonidine hydrochloride delivered with a 16-microliters drop size. Dry mouth developed frequently with the commercially available 1% apraclonidine solution. Blurred vision complicated the use of the formulation containing hydroxypropylmethylcellulose. Both dry mouth (P less than .05) and blurred vision (P = .004) were statistically significant side effects.
Vocci
M J
MJ
Sinai Hospital, Baltimore, Maryland.
Robin
A L
AL
Wahl
J C
JC
Mayer
P
P
Graves
A
A
York
B
B
Enger
C
C
Sutton
J
J
D000316:Adrenergic alpha-Agonists / Q000008:administration & dosage* / Q000009:adverse effects; D000328:Adult; D003000:Clonidine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives*; D004311:Double-Blind Method; D005260:Female; D005569:Formularies as Topic; D006801:Humans; D065347:Hypromellose Derivatives; D007429:Intraocular Pressure / Q000187:drug effects*; D008244:Lysophosphatidylcholines / Q000008:administration & dosage / Q000009:adverse effects; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives; D008875:Middle Aged; D010919:Placebos; D011446:Prospective Studies; D014786:Vision Disorders / Q000139:chemically induced
D000316:Adrenergic alpha-Agonists; D008244:Lysophosphatidylcholines; D010919:Placebos; D065347:Hypromellose Derivatives; C016986:apraclonidine; D008747:Methylcellulose; D003000:Clonidine