December 2002
Volume 43, Issue 13
Free
ARVO Annual Meeting Abstract  |   December 2002
Timolol LA: A Double-masked, Active-controlled, Randomized, Crossover, Comfort, Ocular Safety, and Systemic Bioavailability Study in Healthy Volunteers
Author Affiliations & Notes
  • GD Novack
    PharmaLogic Development Inc San Rafael CA
  • TK Mundorf
    Charlotte NC
  • RS Crockett
    DATA Inc Mobile AL
  • T Ogawa
    Senju Pharmaceutical Co Ltd Osaka Japan
  • N Inui
    Senju Pharmaceutical Co Ltd Osaka Japan
  • H Naka
    Senju Pharmaceutical Co Ltd Osaka Japan
  • Footnotes
    Commercial Relationships    G.D. Novack, Senju Pharmaceutical Co., Ltd. C; T.K. Mundorf, Senju Pharmaceutical Co., Ltd. F; R.S. Crockett, Senju Pharmaceutical Co., Ltd. C; T. Ogawa, Senju Pharmaceutical Co., Ltd. E; N. Inui, Senju Pharmaceutical Co., Ltd. E; H. Naka, Senju Pharmaceutical Co., Ltd. E. Grant Identification: Support: Senju Pharmaceutical Co., Ltd.
Investigative Ophthalmology & Visual Science December 2002, Vol.43, 4066. doi:
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    • Get Citation

      GD Novack, TK Mundorf, RS Crockett, T Ogawa, N Inui, H Naka; Timolol LA: A Double-masked, Active-controlled, Randomized, Crossover, Comfort, Ocular Safety, and Systemic Bioavailability Study in Healthy Volunteers . Invest. Ophthalmol. Vis. Sci. 2002;43(13):4066.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Abstract: : Purpose: A new formulation of timolol with sorbic acid, Timolol-LA (TLA) has been developed which increases its ocular bioavailability (Higashiyama et al, ARVO 1999, S85). In the present study, we desired to evaluate the ocular comfort and systemic bioavailability of TLA in healthy volunteers in comparison to standard timolol maleate ophthalmic solution (TIM). Methods: This study was a randomized, double-masked, active-controlled, crossover evaluation of 0.5% TLA and 0.5% TIM, b.i.d., in 12 normal healthy volunteers. Visits were at Days 0, 1, 2, 4 and 8 in each period, and there was a minimum 7 day interperiod washout. Results: After 8 days of dosing, morning pre-dose values for TLA, 0.09 ng/mL, were 0.11 ng/mL less than with TIM, 0.20 ng/mL (p=0.034). On an individual basis, the highest concentration for TLA was 0.28 ng/mL, and for TIM was 0.69 ng/mL. Detectable timolol concentrations were found in 6 of 12 subjects treated with TLA, and with 7 of 12 subjects treated with TIM. Overall, the ocular and systemic safety profile of TLA was similar to that of TIM. In general, most symptoms were mild in intensity, and no subject discontinued treatment due to ocular discomfort. Both treatments decreased IOP to a similar level. Conclusion: 0.5% TLA was relatively comfortable, with a safety profile consistent with further clinical development, and with a systemic bioavailability similar to that of timolol maleate ophthalmic solution 0.5%.

Keywords: 514 pharmacology • 357 clinical (human) or epidemiologic studies: treatment/prevention assessment/controlled clinical trials • 369 cornea: clinical science 
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