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A sponsored Q & A discussion

Considerations in Ophthalmic Formulation Development for Various Ocular Diseases

and Intellectual Property, of Dow Pharmaceutical Sciences f to discuss ophthalmic formulation technology and the challenges for scientists and formulators who are interested in developing eye-care products. Dow has been involved with both generic and new product development. Could you explain how generic ophthalmic product development differs from new product development? Dr. Yunik Chang: For a generic ophthalmic product development, the formulation, that is, the quantitatively and the qualitatively equivalent to the branded product, is really important. However, for a new product formulation development, the physical chemical properties of an active agent and the targeted indications are more concerned. Does Dow have any particular preference for generic versus new ophthalmic product development? Dr. Chang: No, we dont. We really have both lines of product under development. Previously, we had more new ophthalmic product - projects than generic. For the new ophthalmic projects, what are or were the target indications of treatment? Dr. Chang: Some of the target indications of the products were antiglaucoma, anticataract, dry eye, age related macular degeneration and hyphema. What is hyphema and what is, or was, the formulation goal for products aimed at treating this condition? Dr. Chang: Hyphema is a hemorrhage in the anterior chamber of the eye. The goal of the formulation work was to enhance the ocular penetration of the active ingredient by selecting a proper penetration enhancer and optimizing the viscosity of the formulation. How do you go about selecting an ocular penetration enhancer? Dr. Chang: Ocular penetration enhancers are highly limited due to a possible ocular irritation. Based on our experience with the possible enhancers, we selected a few enhancers which are comparable with active pharmaceutical ingredient and conducted rabbit or bovine ocular membrane penetrative study for the final selection of the enhancer.

or more than 10 years, Dow Pharmaceutical Sciences has been intimately involved in ophthalmic formulation development for various ocular diseases such as cataract, ocular hyphema, dry-eye, age-related macular degeneration, glaucoma, etc. Dow provides regulatory affairs strategy and submissions, nonclinical plans, ophthalmic formulation and process development, analytical methods and stability testing, clinical manufacturing, clinical trial supplies and labeling, and distribution of topical products worldwide. Recently Pharmaceutical Technology talked with Dr. Yunik Chang, Director Ophthalmic Product Development

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Its been quite difficult to develop a topical formulation for the treatment of age related macular degeneration. Can you discuss how youre studying this problem? Dr. Chang: Well, we had an opportunity to study the deliver y of an active agent through the back of the eye, in other words, the vitreous humor. The molecule of the project was around 400 of molecular weight, and it was water soluble. The formulation was designed considering possible penetration through sclera and the conjunctiva of the eye by adjusting viscosity and the selected penetray tion enhancers. The final test of formulation was selected from the in vitro rabbit corneal penetration study, and then the selected formula was tested on the live rabbit for e the delivery of API in various tissues of the eye including f vitreous humor, sclera and retinal membranes. And we confirmed that this particular API was delivered to the back of the eye. Do you think it will be possible to develop an ophthalmic formulation for the treatment of age related macular degeneration? Dr. Chang: Based on our study it is feasible to deliver the active agent to the back of the eye. However, a sustained release device appears to be a better approach for the formulations. vitreal delivery rather than eye drop formulations In addition, we needed a good animal model for the clinical efficacy study.

Can you discuss your formulation work for the treatment of dry eye? Dr. Chang: Well, we have had multiple dry eye projects, and one of the projects was the estradiol ophthalmic formulation for dry eye treatment of post menopausal women. And we could complete Phase II clinical study, highly sucd cessfully. Did you manufacture batches of this product for the clinical study? Dr. Chang: For this particular clinical study, the clinical batches were manufactured by a contract manufacturer based on our batch records. However, before the end of this year, we will have our own sterile manufacturing facility. Then we can manage such manufacturing projects more effectively. What do you think are the most challenging aspects for developing a new ophthalmic formulation? Dr. Chang: Well, formulation stability, clinical efficacy or patient compliance as well as the formula are all important for successful market of the product.
To find out more about Dow Pharmaceutical Sciences, please visit them online at: dowpharmsci.com. To listen to a podcast of this conversation visit pharmtech.com and select multimedia/podcasts.

SPONSORED BY DOW PHARMA

Dow provides regulatory affairs strategy and submissions, nonclinical plans, ophthalmic formulation and process development, analytical methods and stability testing, clinical manufacturing, clinical trial supplies and labeling, and distribution of topical products worldwide. Serving clients since 1977, Dows focus is your success. To find out more about Dow, please visit them on the web at www.dowpharmsci.com.
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