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GOHSENOL EGas an excipient
Confidential As of 1, Dec. 2012
NIPPON GOHSEI
Contents
1. Product Information Grade Line up
Production
Regulatory
2. Application Information FDA approved Drug list which contains PVA
Detailed information of each Applications Film Coating
Binder
Cataplasm/Gel Patch
Ophthalmic
Film Drugs
Confidential
What’s Gohsenol EG?
Polyvinyl alcohol is a polyvinyl resin having hydroxyl groups
and is obtained through saponification of polyvinyl acetate.
GOHSENOL EG is a series of high-quality polyvinyl alcohols
with the Extra High purity property.
Make use of this character, GOHSENOL EG series are widely
used for the application of pharmaceuticals, cosmetics,
electronics materials and ceramics.
Structural formula-(CH2-CH)m-(CH2-CH)n-
| |OH【Hydroxyl group】 OCOCH3【Acetic group】
Polymerization degree : m+nSaponification degree : 〔m / (ｍ+n) 〕×100
Structural formula-(CH2-CH)m-(CH2-CH)n-
| |OH【Hydroxyl group】 OCOCH3【Acetic group】
Polymerization degree : m+nSaponification degree : 〔m / (ｍ+n) 〕×100
Production
Information of the manufacturing site Located in Kuamoto Prefecture Japan
Plant Completion: April 2012
Dedicated to EG-grades
Approx. 500kg / Batch
Confidential
More information of Nippon Gohsei group
Product Information
Grade Line up
Fine Powder
Granule
Fine Powder
Granule
Fine Powder
Granule
Productform
86.5-89.0BinderEG-30PW
Binder SREG-40PW
Ophthalmic
40.0-46.0EG-40P
Ophthalmic
27.0-33.0EG-30P
Film CoatingEG-05PW
Binder IR
4.8-5.8EG-05P
MainApplication
4% Viscosity
[mPa･s]
Degree of
Hydrolysis
[mol%]
Grade
ConfidentialIR / SR : immediate / sustained release
Regulatory
Gohsenol EG DMF No. 26119
CAS No. 25213-24-5
HS No. 39053000
EP, USP, JPE compliant
E1203 Food Additives by EG-05PW
The following Certificates/Statements available
Kosher and Halal Certificate under consideration
GMO Free
Gluten Free
OVI Free
BSE/TSE Free
Residual Solvent
Allergens statement
BfR status
Radiation Free
Confidential
Application Information
FDA Approved Drugs which contain PVA More than 800 drugs
Tablets >700, Solution, Liquid >60, Patch >30
More than 40 API’s
Major API’s and number of drugs
acetaminophen 179(13)
ibuprofen 80(16)
naproxen sodium 65(11)
levetiracetam 31
tramadol hydrochloride 21(14)
metformin hydrochloride 16(5)
topiramate 15
phenylephrine hydrochloride 12
sertraline hydrochloride 10
zolpidem tartrate 10
ibuprofen
naproxen
acetaminophen
Confidential
Application
Recommended Grade and Expected advantages
Tablets
Granulating Agent
EG-05P, EG-05PW
Moisture Barrier, Oxygen Barrier
Binder, immediate release
EG-05PW
Less impurity compared to other polymers
Binder, sustained release
EG-40PW
Less impurity compared to other polymers
Film Coating, immediate release
EG-05PW
Moisture barrier, Gas Barrier, Taste Masking
Confidential
Binder Application
HPMC, high viscosity
PVP, high viscosity
Sustained release
(SR)
Immediate release
(IR)Functions
Sustained releaseproperty
Fast Disintegrationtime
Advantages of PVA
HPMC, low viscosity
PVP, low viscosityCompete with
EG-40PWEG-05PWRecommended
Grades
Confidential
21
Formulation for Tablet
Confidential
100650Total Weight
16.5Magnesium StearateLubricant
213Croscarmellose SodiumDisintegrant
1.332.5Several Different
PolymersBinder
15.198Microcrystalline Cellulose
(PH-101)Diluent
76.9500Metformin hydrochlorideAPI
%mg
Quantity for 1 tabletIngredientFunction / Purpose
EG-05PW as immediate release binder
- Lab test by ICT / Mumbai -
28
Evaluation of powder performancewith different binders
Confidential
Polyvinyl pyrrolidone
( PVP )
Polyvinyl alcohol
( PVA )Polymer
2.523.163.70Moisture Content [%]
1.2731.3381.265Hausner Ratio
21.425.320.9Carr’s Index
0.4790.5570.531Tap Density [g/ml]
0.420
25.7
EG-05PW
0.416
29.8
K-30
0.376Bulk Density [g/ml]
30.0Angle of repose
[Degree]
K-90Grade
EG-05PW as immediate release binder
- Lab test by ICT / Mumbai -
22
Process flow sheet for the tablet
Sifting Metformin hydrochloride and Microcrystalline Cellulose
Dry Mixing in Double Cone Blender
Granulation
Drying
Sizing
Lubrication
Tablet Compression
Confidential
←Addition of Binder
EG-05PW as immediate release binder
- Lab test by ICT / Mumbai -
28
Evaluation Result ofmetformin hydrochloride Tablet
Confidential
Polyvinyl pyrrolidone
( PVP )
Polyvinyl alcohol
( PVA )Polymer
101.5±0.64103.0±1.7102.2±5.7Drug Content
12.96±0.402.26±0.121.71±0.30Disintegration time
[min]
0.310.320.36Friability [%]
5.58±0.3705.91±0.5806.16±0.408Hardness [kg/cm2]
4.61±0.024
649.5±3.8
EG-05PW
4.63±0.01
651.4±3.3
K-30
4.70±0.012Thickness [mm]
652.0±3.7Weights [mg]
K-90Grade
EG-05PW as immediate release binder
EG-40PW performs same as other binders such as PVP and HPMC
EG-40PW as binder forsustained Release
Confidential
API: metfolmin hcl
EG-40PW as sustained release binder
- Lab test by ICT / Mumbai -
Film Coating Application
Immediate release, Gastric coatingApplications
Plasticizer required
Formulation required
Sticking
No Enteric coating
Disadvantage of PVA
Film properties
Moisture, Gas Barrier
Less dosage
Better productivity
Advantages of PVA
KOLLICOAT IRHPMC, low viscosityCompete with
EG-05PWRecommended
Grades
Confidential
18
Comparison ofEG-05PW and HPMC polymer film
106115Linear Expansion (%)
0.00800.0649Adhesion force of film (N)
2251672Younge modulus (MPa)
17657Glass transition Temp. (oC)
Hydroxypropyl MethylCellulose(HPMC)
Polyvinyl Alcohol
(PVA)Product
METHOCEL-E5-LV*EG-05PWGrade
47119Tensile Strength (MPa)
103188Elongation (%)
HighLowWater vapor permeability
Confidential
EG-05PW as immediate film coating
* Dow
- Lab test by ICT / Mumbai -
Water Vapor Permeability ofPolymer film
0.00
0.01
0.02
0.03
0.04
2 4 6 8 10 12 24 48 72 96 120
Time(hr)
Avera
ve
WV
P(g･ m
m/m
2･ h
･ kP
a)
EG-05PW
HPMC
Confidential
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
Moisture barrier coating
Many Pharmaceutical actives are degraded
by atomospheric agents such as
oxygen or light, particularly where there
are opportunities for the ingress of
atomospheric moisture during storage.
Coating system can be formulated to
provide, effective barrier to water vapor,
oxygen and light and can thus provide
an effective means of improving stability
and increasing product shelf life.
>>> What’s EG’s performance?
The most important performance for the film coating
Confidential15
Good for moisture sensitive APIs Aspirin
Talc 0.2%w/wAnti-tacking
agent
Titanium Dioxide 0.2%w/wOpacifier
---
---
+++
---
+++
---
+
---
++
PEG-6000
---
---
++
---
++
---
+
---
++
PEG-4000
---
---
+
---
+
---
---
---
---
PEG-1500
+++
---
+++
+++
++
---
+++
---
---
PEG-400
+++
---
+++
++
++
---
++
---
---
Glycerol
++
---
+++
+++
+++
---
+++
---
++
Triethylcitrate
-Plasticizer
1%w/w
EG-05PW 10%w/wPVOH
++Roughness
+Picking
---Splitting
---Cracking
+++Orange Peel
---Twinning
+++Chipping
---Blooming
+Blistering
Visual observations for defects- Effect of Plasticizers -
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
Best!
26
Formulation for film coating
HPMCPVAProduct
Solvent
Opacifier
Anti-tacking agent
Plasticizer
Polymer
Grade
←
←
←
←
10
-
METHOCEL-E5-LV
0.2Titanium Dioxide
1PEG-1500
0.2Talc
q.s.Purified Water
-HPMC
10EG-05PW
EG-05PW
(wt%)
Confidential
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
Coating Machine & Conditions
30±5oCBed temperature
60±5oCDry air temperature
Circular, occasionally ellipticalSpray pattern type
Process variables Adjusted specifications
25-30cmBed to Gun Distance
30rpmRotational Speed of Pan
40-50p.s.i.Spray Pressure (Operational)
45gmPan load
12cm diameter with 3 bafflesPan design / Baffling
Coating Machine Lab-scale pan coater (Alfred Herbert Ltd., India)
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
28
The results of Coated Tablets
-
43
0.26
5.4
-
UncoatedTablet
7.14.4Weight
Gain(%)
171
-
-
0.18±0.01
HPMC
-Friability(%)
58Disintegration
time (sec)
-Diametral crushing
strength(kg/cm2)
0.11±0.01Cast film
thickness (mm)
EG-05PW
Confidential
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
29
HPMCPVAProduct
++Roughness
+---Picking
---
---
---
---
---
---
---
METHOCEL-E5-LV
---Splitting
---Cracking
+Orange Peel
---Twinning
---Chipping
---Blooming
---Blistering
EG-05PWGrade
Visual observations fordefects in the coated formulations
Yes-(+++), Slight-(++), Very Slight-(+), No-(---)
Confidential
EG-05PW as immediate film coating
- Lab test by ICT / Mumbai -
Other Application
Recommended Grade and Expected advantages
Ophthalmic
EG-05P, 30P, 40P Thickener, preventing dry-eyes
Injection EG-05P
Cataplasms/Gel Patches EG-05P,PW, EG-18P, EG-30P,PW
For base material
Confidential
Ophthalmic Application
To prevent dry eyes
ThickenerFunctions
TBCDisadvantage ofPVA
Making aqueous film on eye surface.
Variety of ViscosityAdvantages of PVA
HPMC, PVP
Hyaluronic acidCompete with
EG-05P, EG-30P, EG-40PRecommended
Grades
Confidential
Cataplasms/Gel Patches
Keep moisture and API’sFunctions
Solvent InsolubleTBCDisadvantage ofPVA
Less odor
Less skin irritationAdvantages of PVA
PVPPoly Acrylic AcidCompete with
EG-05P,30P,40P
EG-05PW, 30PW, 40PW
RecommendedGrades
Confidential
?QUESTION?
Thank you for your attention
Please visit our web site ;Company : http://www.nichigo.co.jp/english/index.htmlGohsenol EG : http://www.gohsenol.com/doc_e/spcl/spcl_01/spcl_08.shtml
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