Professional Documents
Culture Documents
RAJEEV S. RAGHUVANSHI
Ph.D.
5th Oct07, Mumbai
R&D
TRANSDERMAL
12.3%
TRANSMUCOSAL
26.3%
LIPOSOMES
1.5%
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INJECTABLES
8%
PULMONARY
18.5%
FUTURE
4 ONCE-A-DAY + Value Addition
9 Safety profile improvement
9 Better therapeutic efficacy
9 Better tolerability
NDDS A tool for product life cycle management
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BLOOD PROFILES
Controlled Release vs. Immediate Release
30
3rd dose
2nd dose
25
Blood Conc.
Side Effects
4th dose
1st dose
20
15
Effective Therapy
10
Ineffective Level
5
IR
CR
0
0
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10 12 14 16 18Hrs.
Schematic of dissolution
from different types of delivery systems
100
%Drug Dissolved
80
60
40
IR
ER
20
DR
0
0
10
12
Time (h)
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14
16
18
20
22
24
50
IR
ER
40
DR
30
20
10
0
0
10
12
Time (h)
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14
16
18
20
22
24
OCRDDS: advantages
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Matrix Expansion
(swelling)
Drug Diffusion
Soluble matrix
erosion
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Smooth &
continuous
release for
extended
time
Technology:
Film Coated Matrix tablets comprising Hypromellose as a release
controlling polymer with diffusion and erosion controlled release
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Products in market:
Cordicant -uno
Madopar DR
SULAR ER
Nisoldipine OD
Innovator Sular ER 10, 20, 30 and 40mg
Previous Technology: Press-coated tablet
Immediate release core with enteric coating
Sustained release coating
Drug is present in both core and coat
Film Coating
New Technology - Geomatrix, to be developed by SkyePharma
sNDA filed, Expected Launch Early 2008.
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Inert core
Drug Layer
Advantage : COMPARTMENTALIZATION
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Carvedilol ER
Carvedilol ER
Specific advantage:
Delivery profile designed to compliment the circadian pattern of blood pressure
Controlled onset, extended release delivery system
Rate of release essentially independent of pH, posture and food
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Case studies 1
Study Design:
8 male volunteers
Cross-over
Results:
Safe/Effective
Bioavailability
Rate of Uptake
Case study 2
12
Time
Sand immune
16
20
24
LEDDS Cyclosporine
400
350
Anticipated results:
300
250
200
150
100
50
0
0
Sandimmune (200mg)
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12
Time
16
20
24
Broad GIT dispersion, limiting local irritation and increasing absorption co-efficient
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are locally active in the stomach (e.g., misoprostol, antacids, antibiotics against Helicobacter
pylori
have an absorption window in the stomach or in the upper small intestine,(e.g., L- DOPA, paminobenzoic acid, furosemide, riboflavin),
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A) The device significantly swells on contact with gastric fluids (to a few hundred times of the original
volume); B D) the gastric contraction pushes the hydrogel to the pylorus; E) the gastric contraction
slips over the surface of the hydrogel; and F) the hydrogel is pushed back into the body of the stomach.
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Promising delivery of acid and enzymes labile substances thorough colon made this
delivery route popular
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GI PHYSIOLOGY
WINDOW OF ABSORPTION
SPATIAL DELIVERY
COST
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1.
2.
3.
4.
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Drug
Company
Approval date
Technology
CLARINEX-D 12
HOUR tablets
Schering
February 01,
2006
Bilayer tablets
(Desloratidine as IR
and Pseudoephedrine
as ER)
OPANA ER
tablets
Oxymorphone HCl
(5/10/20/40 mg)
Endo
Matrix tablets
COREG CR
capsules
Carvedilol phosphate
(10/20/40/80 mg)
SB Pharmco
October 20,
2006
Multiparticulates
Janssen
December 19,
2006
OROS
Cyclobenzaprine
hydrochloride (15/30 mg)
ECR
February 01,
2007
Multiparticulates
Quetiapine fumarate
(50/200/300/400 mg)
Astrazeneca
Matrix tablets
Zileuton 600 mg
Critical
Matrix tablets
Trospium chloride 60 mg
Indevus
August 03,
2007
INVEGA tablets
AMRIX ER
capsules
SEROQUEL XR
tablets
ZYFLO CR
tablets
SANCTURA XR
tablets
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Company
Development stage
J&J
GSK
Approvable
Wyeth
Approvable
Tacrolimus MR
Astellas
NDA filed
Requip ER (Ropinirole)
GSK
NDA Filed
GSK
Phase III
Gepirone ER
GSK
Phase III
Rosiglitazone XR
GSK
Phase III
GSK
Phase III
Depomed
Phase III
Gabapentin GR
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THANK YOU
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