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A sponsored Q & A discussion

Considerations in Ophthalmic Formulation Development for Various Ocular Diseases

F or more than 10 years, Dow Pharmaceutical Sciences has been intimately involved in ophthalmic formula- tion development for various ocular diseases such

as cataract, ocular hyphema, dry-eye, age-related macu- lar degeneration, glaucoma, etc. Dow provides regulatory affairs strategy and submissions, nonclinical plans, oph- thalmic formulation and process development, analytical methods and stability testing, clinical manufacturing, clini- cal trial supplies and labeling, and distribution of topical products worldwide. Recently Pharmaceutical Technology talked with Dr. Yunik Chang, Director Ophthalmic Product Development

Dr. Yunik Chang, Director Ophthalmic Product Development Sciences to discuss ophthalmic formulation technology and

Sciences

to discuss ophthalmic formulation technology and the chal- lenges for scientists and formulators who are interested in developing eye-care products.

and Intellectual Property, of Dow Pharmaceutical

f Dow Pharmaceutical
f Dow Pharmaceutical
Dow has been involved with both generic and new product development. Could you explain how
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 devel
opment, the formulation, that is, the quantitatively and the
qualitatively equivalent to the branded product, is
really im-

portant. However, for a new product formulation develop- ment, 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 don’t. We really have both lines of prod- uct under development. Previously, we had more new oph- thalmic 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 mac- ular 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 cham- ber 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
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?
enhancer?
Dr. Chang:
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 ingre
dient and conducted rabbit or bovine ocular membrane
penetrative study for the final selection of the enhancer.

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SECTION page_header page_header page_header page_header It’s been quite difficult to develop a topical formulation
SECTION page_header page_header page_header page_header It’s been quite difficult to develop a topical formulation

It’s been quite difficult to develop a topical formulation for the treatment of age related macular degeneration. Can you discuss how you’re studying this problem? Dr. Chang: Well, we had an opportunity to study the de-

Can you discuss your formulation work for the treat- ment of dry eye? Dr. Chang: Well, we have had multiple dry eye projects, and

livery of an active agent through the

water soluble. water soluble.
water soluble.
water soluble.
back of the eye, back of the eye, one of the projects was the estradiol
back of the eye,
back of the eye,
one of the projects was the
estradiol ophthalmic formula
tion for dry eye treatment of post menopausal women.
400 of molecular
400 of molecular
weight, and it was
And we could complete Phase II clinical study, highly suc- -
we could complete Phase II clinical study, highly suc
cessfully.
cessfully.

in other words, the vitreous humor. The molecule of the

project was around

The formulation was designed considering

possible penetration through sclera and the conjunctiva of the eye by adjusting viscosity and the
possible penetration through sclera and the conjunctiva of
the eye by adjusting viscosity and the selected penetra-
adjusting viscosity and the selected penetra-
tion enhancers.
tion enhancers.
The final test of formulation was selected

from the in vitro rabbit corneal penetration study, and

for

of the eye including

vitreous humor, sclera and retinal membranes. And we

then the selected formula was tested on the live rabbit

live rabbit
live rabbit
f API in various tissues
f API in various tissues

the delivery of API in various tissues

confirmed that this particular API was delivered to the back of the eye. back of
confirmed that this particular API was delivered to the
back of the eye.
back of the eye.
Do you think it will be possible to develop an oph-
thalmic 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
sustained
release device appears to be a better approach for
the
vitreal delivery rather than eye drop formulations. In ad-
vitreal delivery rather than eye drop formulation

dition, we needed a good animal model for the clinical efficacy study.

Did you manufacture batches of this product for the clinical study? Dr. Chang: For this particular clinical study, the clinical

manufacturer

based on our

this year, we will have our

records. However, before the end of

batches were manufactured by a

contract contract
contract
contract
batch batch
batch
batch
own sterile manufacturing facility. own sterile manufacturing facility.
own sterile manufacturing facility.
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 pa- tient 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
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, Dow’s focus is your success. To find out more

about Dow, please visit them on the web at www.dowpharmsci.com.