17 Modified-release products along with release mechanism.

Product Generic Manufacturer Release Mechanism of the MR product

Name Name
Toprol AstraZeneca Metoprolol The tablets comprise a multiple unit system containing metoprolol
XL succinate succinate in a multitude of controlled release pellets. Each pellet
acts as a separate drug delivery unit and is designed to deliver
metoprolol continuously over the dosage interval.
Concerta Ortho-McNeil- Methylphenidate Comprises an osmotically active trilayer core surrounded by a
Janssen semipermeable membrane with an immediate-release drug
overcoat. Uses osmotic pressure to deliver methylphenidate HCl
at a controlled rate.
Mirena Bayer Levonorgestrel Mirena is a tiny T-shaped piece of soft, flexible plastic, slowly
releases very small amounts of the hormone levonorgestrel directly
into your uterus. Mirena is programmed to release levonorgestrel
over five years. Following systemic application, levonorgestel
begins to flow through the rate-controlling membrane of the
system into the systemic circulation via the capillaries beneath the
skin.

Effexor XR Pfizer Venlafaxine Drug release is controlled by diffusion through the coating
hydrochloride membrane on the spheroids and is not pH dependent. The
spheroids comprise of venlafaxine hydrochloride, microcrystalline
cellulose and, optionally, hydroxypropylmethylcellulose coated
with a mixture of ethyl cellulose and
hydroxypropylmethylcellulose to control the release.

Madopar Roche Levodopa + Release of levodopa from the Madopar HBS capsules is controlled
benserazide by the rate of polymer swelling and is the release is thus sustained
over a long period of time.

Questran Par Cholestyramine Cholestyramine resin adsorbs bile acids by ion exchange in the
intestine to form an insoluble complex which is excreted in the
feces. This lowers the enterohepatic circulation of bile acids and
prompts the body oxidise more cholesterol to bile acids thus
lowering the cholesterol in the system.

Venlafaxine Teva Venlafaxine HCl Venlafaxine hydrochloride extended-release capsules are

HCl ER formulated as an extended-release capsule for once-a-day oral
administration. Drug release is controlled by diffusion through the
coating membrane on the spheroids and is not pH dependent.
Exelon Novartis Rivastigmine The patch comprises a four-layer laminate containing the backing
Patch Tartrate layer, drug matrix, adhesive matrix and overlapping release liner.
The release liner is removed and discarded prior to use.
COVERA Pfizer Verapamil Covera-HS is designed to initiate the release of verapamil 4 5
HS hydrochloride hours after ingestion. This delay is introduced by a layer between
the active drug core and outer semipermeable membrane. As water
from the gastrointestinal tract enters the tablet, this delay coating
is solubilized and released. As tablet hydration continues, the
osmotic layer expands and pushes against the drug layer, releasing
drug through precision laser-drilled orifices in the outer membrane
at a constant rate. This controlled rate of drug delivery in the
gastrointestinal lumen is independent of posture, pH,
gastrointestinal motility, and fed or fasting conditions.

Lupron Abbott Leuprolide Leuprolide acetate is released from a biodegradable matrix of dl-
depot acetate lactic acid/glycolic acid copolymer and gelatin.

Ocusert Alza Pilocarpine This delivery system is made of a core reservoir consisting of
ophthalmic pilocarpine and alginic acid surrounded by etheylene/vinyl acetate
copolymer (EVA) membrane which controls the diffusion of
pilocarpine from the system into the eye. The EVA polymer of the
Ocusert Pilo-40 also contains 2-ethyl hexyl phthalate to increase
the release rate. Alginic acid is not released from the core.

Propine Allergan Dipivefrin Propine is a prodrug of epinephrine formed by the diesterification

Pharmaceutical hydrochloride of epinephrine and pivalic acid. The addition of pivanoyl groups to
s the epinephrine molecule enhances its lipophilic character and as a
consequence, its penetration into the anterior chamber. Propine is
converted to epinephrine inside the human eye by enzyme
hyrolysis. The Propine prodrug delivery system is a more efficient
way of delivering the therapeutic effects of epinephrine with fewer
side effects than are associated with conventional epinephrine
therapy.
Herceptin Genentech Trastuzumab HER2 protein overexpression is observed in 25%-30% of primary
breast cancers. Trastuzumab has been shown, in both in vitro
assays and in animals, to inhibit the proliferation of human tumor
cells that overexpress HER2. Trastuzumab is a mediator of
antibody-dependent cellular cytotoxicity (ADCC). In vitro,
HERCEPTIN-mediated ADCC has been shown to be
preferentially exerted on HER2 overexpressing cancer cells
compared with cancer cells that do not overexpress HER2.

Nexium AstraZeneca esomeprazole NEXIUM Delayed-Release Capsules and NEXIUM For Delayed-
magnesium Release Oral Suspension contain a bioequivalent enteric-coated
granule formulation of esomeprazole magnesium. Bioequivalency
is based on a single dose (40 mg) study in 94 healthy male and
female volunteers under fasting condition. After oral
administration peak plasma levels (Cmax) occur at approximately
1.5 hours (Tmax)
Cymbalta Lilly Duloxetine Each capsule contains enteric-coated pellets of duloxetine
hydrochloride hydrochloride that are designed to prevent degradation of the drug
in the acidic environment of the stomach.

OxyContin Purdue Pharma Oxycodone Oxycodone hydrochloride particles being coated with an amount
hydrochloride of hydrophobic material effective to provide a sustained release
when the coated particles are exposed to an aqueous solution.
Oxycontin is designed to provide delivery of oxycodone over 12
hours.

Rituxan Genentech rituximab Rituximab binds specifically to the antigen CD20 (human B-
lymphocyte-restricted differentiation antigen, Bp35), a
hydrophobic transmembrane protein with a molecular weight of
approximately 35 kDa located on pre-B and mature B
lymphocytes. The antigen is expressed on >90% of B-cell non-
Hodgkins lymphomas (NHL), but the antigen is not found on
hematopoietic stem cells, pro-B-cells, normal plasma cells or other
normal tissues.