No. 5, October 2000
Excipients & Actives for Pharma
Publisher:BASF Aktiengesellschaft
Editorial staff:Dr. Volker Bühler, Valérie Filiatreau,Dr. Hubertus Folttmann, Patrick Glaser,Klaus Kalter, Dr. Karl Kolter, Dr. Siegfried Lang
Concept/Layout:MLW KommunikationsFormGmbH Werbeagentur, Mannheim
Print:Frotscher Druck, Darmstadt
Imprint
Calendar
P h a r m a I n g r e d i e n t s
The
for
SuccessyourChoice
Dear reader,
You may have known ExAct for nearly three years as a customer’snewsletter with its main focus on pharmaceutical excipients.
This year the pharma active ingredients business within the BASFgroup has been reorganized in order to provide you with anintensified and integrated service fulfilling your needs.
BASF now provides a whole range of pharma ingredients fromone source. By focusing on our comprehensive portfolio ofactives, excipients and vitamins and offering a complete technicalapplication and formulation support, we guarantee process safetyas well as freedom in application while enhancing our customers’long-term product and market success.
The ExAct newsletter will continue to provide you with recentfindings, application data and experience relating to our widenedproduct range for the pharmaceutical industry.
Yours sincerely,
BASF AktiengesellschaftMarketingPharma Ingredients
Gabriel Tanbourgi
30th January to 2nd February, 2001InformexNew Orleans* , USA
19th to 21st April, 2001PIM (Fair for Pharmaceutical Ingredients)Kuala Lumpur, Malaysia
11th to 13th June, 2001INTERPHEX Asia (Internat. Exposition for the Pharmaceutical Industry)Singapur, Singapore
23rd to 27th June, 200128th International Symposium on Controlled Release of Bioactive MaterialsSan Diego* , USA
10th to 12th July, 2001CPhI, Pharmaceutical Ingredients ChinaShanghai, China
3rd to 5th October, 2001CPhI, Pharmaceutical Ingredients WorldwideLondon*, United Kingdom
21st to 25th October, 2001AAPS (American Association of Pharmaceutical Scientists) Annual MeetingDenver*, USA
9th to 12th November, 2001PHARMA INDIA (Internat. Congress andExposition for the Pharmaceutical Industry)Mumbai, India
* BASF will be represented.
Riboflavin 100 page 2–3 KollicoatY SR 30 D page 4–5 KollidonY VA 64 page 6–7One Source:The Portfolio page 8–11
Preview page 12 News page 12New Media page 12
0.1 1.0 10.0 100.0 1000.0
Particle Diameter [µm]
Volume [%]
20
10
0
20
10
0
0.1 1.0 10.0 100.0 1000.0
Particle Diameter [µm]
Volume [%]
IntroductionIn general, direct-compressible actives have gainedmore and more importance. Expensive and timeconsuming granulation steps are avoided – if possible– and replaced by direct compression. Therefore thedemand for direct-compressible substances increasedwithin the last years. This is especially the case forsubstances which are difficult to handle in their purecrystalline form like Riboflavin. Crystalline Riboflavinshows poor flowability and bad dissolution properties.Therefore BASF invested in new technology toproduce an improved direct-compressible productspecially designed for the food/pharma requests.
Direct-compressible Riboflavin formulations generallyconsist of granules with a certain amount of excipientsto provide binding and disintegration properties. BASFoffers a direct-compressible 100% grade whichcombines the advantages of improved powder prop-erties and optimized release rates with the highestpossible potency: Riboflavin 100.
ManufactureRiboflavin 100 is manufactured by a natural fermenta-tion process using a non-GMO microorganism,Ashbaya gossypii. Since the soy products utilized forthe fermentation are also not genetically modified weare able to supply our customer with a GMO-freeproduct. The fermentation process guarantees aproduct of highest quality and purity.
Technical advantages of Riboflavin 100
Outstanding product properties: homogeneous particle size good flowability high purity reduced dusting good compressibility excellent dissolution
Particle formMany of the disadvantages in handling syntheticRiboflavin result from its particle form (2). Particles inform of needles show poor flow properties (6) and lowbulk density (4). Especially the production of highpotency Riboflavin tablets becomes difficult or evenimpossible. BASF’s Riboflavin 100 however consistsof round particles (1) with a smooth surface leadingto a higher bulk density (3).
FlowabilityDue to the round particle form and its slightly coarserparticle size (7, 8), Riboflavin 100 has an improvedflowability compared to the synthetic material (5).
Moreover it shows better results in the electrostaticcharging test. These two factors determine the superiorhandling and processing properties of Riboflavin 100.
PurityHPLC tests prove that beside its excellent physicalproperties Riboflavin 100 shows also outstandingquality regarding purity of the material. Whereassynthetic Riboflavin includes several by-products (10),BASF’s Riboflavin 100 has less additional peaks withremarkable lower quantity (9).
Food fortificationIn addition to its excellent handling properties, Ribo-flavin 100 shows good mixing behavior with reducedtendency to subsequent segregation. A typical examplein food fortification is the flour test. A flour mixture con-taining three percent of Riboflavin is mixed thoroughlyand sieved. The less flour mixture remains upon sieve250 µm the better the mixture. As can be seen inpicture (11), BASF’s Riboflavin 100 has considerablybetter mixing and sieving properties. These resultscan also be expected in the fortification of other foodproducts like instant powders. The fortification of softdrinks or other liquids in the range of typical pH valueswith Riboflavin 100 results in the same color as withsynthetic Riboflavin.
Microscope photograph of Riboflavin 100 (1) andsynthetic Riboflavin (2); magnification: x126.
Bulk density of Riboflavin 100 (3) [0.35 g/ml] andsynthetic Riboflavin (4) [0.12–0.18 g/ml].
Particle size distribution of Riboflavin 100. (7)
Flowability of Riboflavin 100 (5) and syntheticRiboflavin. (6)
Riboflavin 100Vitamin B2 in a new shape.U. Sindel
BASF ExAct page 2 – No. 5, October 2000
Tabletting propertiesIdentical coloration compared to synthetic Riboflavin isalso achieved for the use of Riboflavin 100 in pharmaapplications like tablets. Good flowability and homo-geneous particle size distribution result in excellenttabletting properties. Even formulations containing 50mg and more of Riboflavin per tablet are easily com-pressible and show excellent dissolution. The dissolu-tion in water has been improved compared to synthetic
Particle size distribution of synthetic Riboflavin. (8)
1 2
5 6
3 4
rele
ased
rat
e [%
]
0 30 60 90 120 150 180 210 240 270 300 330 360
minutes
100
80
60
40
20
0
100
80
60
40
20
0
5 10 15 20 25 min
mAU
Table 1: Composition per tablet
Riboflavin 100Kollidon CLLudipressAvicel PH 102Magnesium stearateAerosoil 200
Tablet mass
50 mg9 mg
160 mg80 mg2 mg6 mg
307 mg
page 3 – No. 5, October 2000 BASF ExAct
Flour test with Riboflavin 100 in comparison withsynthetic Riboflavin. (11)
100
80
60
40
20
0
5 10 15 20 25 min
mAU
HPLC chromatogramof Riboflavin 100. (9)
HPLC chromatogramof synthetic Riboflavin100. (10)
Dissolution profileof tablets containing50 mg of Riboflavin100. (12)
Riboflavin 100Vitamin B2
loss: 1–4%
SyntheticRiboflavin
Vitamin B2loss: 20–40%
upon sieve250 µm
through sieve50 µm
Riboflavin. This gives benefits in applications wherea high performance dissolution is required.
A tablet containing 50 mg of Riboflavin 100 wasmanufactured at a low compression force of 4 kNresulting in about 70 N hardness without any friability.
DissolutionThe USP requirement for the dissolution of tabletscontaining Riboflavin is 75% within 45 min. Figure(12) shows the dissolution profile of high-potencyRiboflavin 100 tablets. The release rate of 75% evenafter 30 minutes indicates clearly a high reliabilityregarding dissolution speed in tablet formulations.
ConclusionsRiboflavin 100 has demonstrated to be aproduct of high quality with good handling properties for food as well as pharma applica-tions. Therefore it should be the product ofchoice for difficult formulations where excellent powder properties are required.
BASF ExAct page 4 – No. 5, October 2000
rele
ased
dru
g [
%]
0 4 8 12 16 20 24
time [h]
◆ 10% Propylene glycol ▲ 10% Triethyl citrate ■ 5% Triethyl citrate● 5% Triacetin ▲ 5% Acetyl tributyl citrate
80
70
60
50
40
30
20
10
0
rele
ased
dru
g [
%]
0 4 8 12 16 20 24
time [h]
100
90
80
70
60
50
40
30
20
10
0
● 0% Talc ■ 25% Talc ▲ 50% Talc ◆ 75% Talc
Coating level 3mg/cm2
Coating level 3mg/cm2
Table 1: Composition andpreparation of the pellets
IngredientCaffeine powderAvicel PH 101Granulac 230Kollidon VA 64
Total
(%)1043.7543.75 2.5
100
Table 2: Composition and preparationof the spray suspension
Inlet air temperatureOutlet air temperatureAtomizing pressureSpraying rateDryingCoating levelSpraying timeSolids content ofthe spray suspension
60°C35°C1.0 bar11.5 g/min40°C/3 min3 mg/cm2
about 35 min
20%
Dissolution of caffeinepellets coated withKollicoat SR 30 D anddifferent plasticizerswithout furtheradditives.(Figure 1)
Influence of talc on therelease rate of caffeinepellets.(Figure 2)
was first added to the given amount of water. ThenKollidon SR 30 D was stirred in. The pigment disper-sion was homogenized using a corundum mill andadded slowly to the polymer dispersion while stirring.
IntroductionControlled release film coatings generally do notconsist only of the controlled release polymer but alsocontain various excipients such as plasticizers,coloring agents, antitack additives, pore formers orsuspension stabilizers. These additives have differingdegrees of influence on a variety of film properties, thedissolution rate and the film coating process. KollicoatSR 30 D is a new polyvinyl acetate based polymerdispersion for the manufacture of controlled releasecoated dosage forms [1]. While the influence ofplasticizers on the mechanical film properties hasalready been described [2], no data are yet availableconcerning the other excipients.
PurposeThis study was performed to determine the influenceof additives commonly used in coating formulationson the coating process and film properties. Thisknowledge can be used to optimize coating formula-tions and to improve and expedite their development.
Materials and MethodsMaterialsKollicoat SR 30 D is a polyvinyl acetate dispersionstabilized with polyvinylpyrrolidone and sodium laurylsulfate (BASF AG); caffeine (Knoll AG), Pharsil(dimethicone, Wacker); Aerosil 200 (Degussa),Granulac 230 (lactose, Meggle).
All ingredients were blended in a Diosna-mixer for 5minutes, moistened with water until a readily mould-able mass was obtained (approx. 48% water). Themass was then mixed thoroughly for another 3 minutesextruded in an Alexanderwerk apparatus with a vertical1.5 mm sieve and the resulting granules were trans-ferred to a spheronizer (Heller) and rounded for 10minutes. The still moist pellets were dried in a fluidizedbed granulator and then sieved to obtain the requiredparticle size (0.7–1.4 mm).
The recommended addition rate of 1,2 Propylene gly-col is 10% referred to the dry polymer. Propylene glycol
KollicoatY SR 30 DInfluence of additives on the properties of films and coated dosage forms.K. Kolter, T. Rock
Polymer dispersionParts byweight (g)
Compo-sition (%)
47.0 (14.1)
1.436.6
3.5 0.5 0.510.5
100
190.00(57.00) 5.66147.97
14.15 2.02 2.02 42.45
404.30
Kollicoat SR 30 D(dry polymer)1,2 Propylene glycolWater
Pigment dispersionTalcTitanium dioxideSicovitY Red 30Water
Total
Table 3: Coating processThe coating was applied on 0.5 kg caffeinepellets in a fluidized bed coater (AeromaticStrea 1) under the following conditions:
page 5 – No. 5, October 2000 BASF ExAct
rele
ased
dru
g [
%]
0 4 8 12 16 20 24
time [h]
100
90
80
70
60
50
40
30
20
10
0
■ 5% glycerol monostearate ▲ 50% glycerol monostearate● 25% dimethicone ◆ 50% dimethicone ◆ without additive
rele
ased
dru
g [
%]
0 4 8 12 16 20 24
time [h]
100
90
80
70
60
50
40
30
20
10
0
■ 25% Aerosil ▲ 25% Magnesium stearate ● 50% Magnesium stearate▲ 25% Tricalcium phosphate ● 50% Tricalcium phosphate ◆ 10% Aerosil
rele
ased
dru
g [
%]
0 4 8 12 16 20 24
time [h]
90
80
70
60
50
40
30
20
10
0
▲ 10% Propylene glycol (uncured) ▲ 10% Propylene glycol (cured 24h/60 °C)● 5% Triethyl citrate (uncured) ● 5% Triethyl citrate (cured 24h/60 °C) ◆ 10% Propylene glycol+ pigments (uncured) ◆ 10% Propylene glycol + pigments (cured 24h/60 °C)■ 5% Triethyl citrate + pigments (uncured) ■ 5% Triethyl citrate + pigments (cured 24h/60 °C)
Coating level 3mg/cm2
Coating level 3mg/cm2
Coating level 3mg/cm2
Influence of finelydispersed additiveson drug release ofcaffeine pellets.(Figure 3)
Influence of glycerolmonostearate anddimethicone on drugrelease of caffeinepellets.(Figure 4)
Curing effect ofcaffeine pellets withand without additives.(Figure 5)
DissolutionDissolution tester (Pharmatest PTW-S), medium:890 ml 0.08M HCl (0–2 h) and phosphate bufferpH 6.8 (2–24 h), paddle with 50 rpm.
Results and DiscussionThe use of different plasticizers resulted in very similardissolution rates (Figure 1). No differences wereapparent between propylene glycol 10% and triethylcitrate (5% and 10%), while triacetin (5%) and ATBC(5%) produced slightly slower dissolution rates.
The excipient talc – widely used in coating preparations– accelerated dissolution with increasing concentration(Figure 2) at constant coating level. It should benoted, however, that especially at very high talc con-centrations the polymer content was much lower andwas no longer sufficient to completely bind the solids.
Very fine particulate solids like Aerosil 200, magne-sium stearate or tricalcium phosphate in higher con-centrations interfere greatly with film formation, sincedissolution occurs very rapidly (Figure 3).Lipophilic antitack additives like glycerol monostearateor dimethicone slow down dissolution in the lowerconcentration range and accelerate it at higherconcentrations (Figure 4).
The additives had no impact on the curing behavior ofthe pellets. Even after high thermal stress (24 h/60 °C)dissolution was almost unchanged. Coating formula-tions with several additives also showed the samebehavior (Figure 5).
Conclusions The type of plasticizer used has almost no
influence on dissolution. Antitack additives in low to medium concentra-
tions also hardly affect dissolution. Fine particulate solids markedly accelerate
dissolution, especially at higher concentrations.
References[1] Technical Information KollicoatY SR 30 DJune 1999, BASF AG.[2] K. Kolter and F. RuchatzProceedings AAPS Congress New Orleans, November 1999, 4225.
BASF ExAct page 6 – No. 5, October 2000
Ratio: 6 : 4
Kollidon 30Kollidon VA 64MC PH 101HPMC 2910Maltodextrin DE 18
[°]
2835414244
[s]
7,5blockblockblockblock
MeanParticle Size
D [4,3]
BulkDensity
HausnerRatio
FlowabilityFlow timeTable 2 Angle of
Repose
PurposeDry binders are intended to improve tablet formationby direct compression with the main emphasis onimproving the mechanical properties [1], i. e. thehardness and friability of the tablets. Apart from mi-crocrystalline cellulose and the cellulose ethers,polyvinylpyrrolidone is probably the best-known drybinder. An almost unknown dry binder is Kollidon VA64 (copovidone), a vinylpyrrolidone vinyl acetate-copolymer (Figure 1)[2].
(Figure 1)
The objective of this study was to investigate theeffectiveness of different dry binders and to correlate itwith physicochemical properties.
Experimental MethodsMaterialsDry Binder: Kollidon 30 (povidone), Kollidon VA 64(copovidone) (BASF AG); Avicel PH 101 (microcrystal-line cellulose (FMC); Pharmacoat 606 (hydroxypropyl-methylcellulose 2910) (Shin Etsu); Maldex 18 (malto-dextrin) (Amylum).
IngredientsDi-Tab (Rhône-Poulenc); ascorbic acid powder,Ludipress, Kollidon CL (BASF AG); magnesiumstearate (Bärlocher); Aerosil 200 (Degussa).
MethodsThe dry binders were tested in several formulations(Table 1). A dicalcium phosphate tablet (A), withexcipients which are not soluble in water and a vitaminC tablet (B), with water-soluble constituents. To obtaindetailed information on their compression properties,the pure dry binders were compressed (C).
Powder properties■ bulk and tap density (Erweka volumeter)■ angle of repose (Pfrengle funnel)■ particle size (Malvern Mastersizer)
TabletingThe ingredients (Table 1) were passed through an800-µm sieve and blended for 10 min in a Turbulamixer. The tablets (A) and (B) with a weight of 500 mgwere produced on a Korsch PH 106 rotary press (30
rpm, 12 mm, beveled edge) and (C) with a weightof 500 mg on a Korsch EK0 single punch press(30 tablets/min, 12 mm, beveled edge) with variedcompression forces (10, 18, 25 kN).
Tablet propertiesHardness, weight and dimensions were determinedusing a Kraemer tablet tester (HT-TMB).
Results and DiscussionThe dry binders tested exhibited considerabledifferences in their powder properties (Table 2)which are of interest with reference to tabletability.
The particle size determinations clearly show thatKollidon VA 64 is the finest product and should, withits shell like structure (Figure 2), be able to coat drugand filler particles and bind them together under com-pression.
The hardness of the tablets (A) made with Kollidon VA64 places them in a class of their own (Figure 3).
At a compression force of 18 kN and a dry bindercontent of 50 mg, the hardness of the tablets exceedsthat of tablets without a dry binder by 120%. If the samecompression force is used in each case and the dry
binder content is increased from 25 to 50 to 75 mg,Kollidon VA 64 gives the steepest increase in hardness.
Vitamin C powder (B) was selected as a substancethat is very difficult to compress into tablets and inmix-tures with excipients, also greatly reducescompressibility. The compression force-hardnesscurves (Figure 4) are similar in appearance to thosefor the tablets of formulation A:
without dry binder: low hardnesswith HPMC 2910,Kollidon 30 andMC PH 101: slight improvementswith Kollidon VA 64: exceptional hardness
Because of the polymerized vinyl acetate component,Kollidon VA 64 is a softer and more plastic materialthan the other dry binders. This is confirmed by thelow glass transition temperature (103°C).
The plasticity values of the products (Figure 5) weredetermined from the force-displacement curves (C).Kollidon VA 64 possesses a high plasticity of over90% that remains constant from 10 to 18 to 25 kN.
KollidonY VA 64An excellent dry binder.D. Flick, K. Kolter
CH3
C
H––––––CH–CH2–––––––CH–CH2––––––H
N O O
n m
O
Di-TabAscorbic AcidLudipressDry BinderKollidon CLAerosil 200Magnesium Stearate
Total
Table 1Formulations
(A)%
90, 85, 80––
5, 10, 154.5–
0.5
100.0
–40.0
51.3, 46.3, 41.35, 10, 15
3.00.240.5
100.0
–––
99.5––
0.5
100.0
(C)%
(B)%
1,241,371,401,371,34
[ m]
5043658274
[g/ml]
0,3890,2410,3260,3670,522
page 7 – No. 5, October 2000 BASF ExAct
▲ Kollidon VA 64 ▲ Kollidon 30 ◆ HPMC 2910■ MC PH 101 ● without dry binder ● Maldex 18
140
120
100
80
60
40
20
0
hard
ness
[N
]
5 10 15 20 25 30compression force [kN]
■ 10 kN ■ 18 kN ■ 25 kN
100
80
60
40
20
0
Pla
stic
ity
in [
%]
Kollidon 30 Kollidon MC PH 101 HPMC 2910 Maldex 18 VA 64
without Kollidon 30 Kollidon MC PH 101 HPMC 2910 Maldex 18dry binder VA 64
100
80
60
40
20
0
Compression Force: 18 kN■ without dry binder ■ 25 mg dry binder■ 50 mg dry binder ■ 75 mg dry binder
hard
ness
[N
]
Hardness ofDicalcium Phoshatetablets withincreasing amountsof dry binders.(Figure 3)
Compression force –hardness profile ofVitamin C tablets.(Figure 4)
Plasticity ofdry binder.(Figure 5)
Scanning electron micros-copy Kollidon VA 64.
(Figure 2)
Conclusions Kollidon VA 64 possesses unique properties as
a dry binder, irrespective of the formulation,which far exceed those of all other materials tested.
Important information can be derived on the effectiveness of dry binders from force displace-ment curves.
The dry binding properties of a substance canbe attributed to various physical properties likeparticle shape and plasticity.
References[1] Lieberman, Lachman and Schwartz, Pharmaceutical Dosage Forms, Marcel Dekker (1998).[2] V. Bühler, Kollidon – Polyvinylpyrrolidone forthe pharmaceutical industry, BASF AG (1996).
50 mg dry binder
BASF ExAct page 8 – No. 5, October 2000
One SourceBASF – worldwide ingredient source for the pharma industry.
determine their quality. BASF products are manu-factured to the modern standards of quality manage-ment in the pharmaceutical industry, i. e. ISO standardsand Good Manufacturing Practice (GMP). Each batchis analyzed and issued with a Certificate of Analysisthat confirms its pharmacopoeia quality or specifica-tion requirements.
Our production facilities meet the requirements ofnational and international authorities. Highly motivatedstaff permanently contributes to the improvement ofthe quality standards and the reliability of BASFproducts.
BASF is one of the world’s leading chemical com-panies. Profound know-how in chemistry includingpolymer chemistry have yielded in a wide range ofhigh-quality bulk active ingredients, excipients andvitamins. With proven brands like Kollidon BASF haswritten history in pharmaceutical technology. For 60years BASF has been a reliable source of pharmaceu-tical ingredients and a partner for the pharmaceuticalindustry all over the world.
Pharmaceutical ingredients, like finished pharma-ceutical products are subject to strict quality require-ments. A variety of chemical and physical parameters
PortfolioBrochure Actives Excipients Vitamins
Analgesics
Ibuprofenanalgesic, anti-inflammatory
Purines
CaffeineCNS stimulant, analgesic
Theophyllineanti-inflammatory,bronchospasmolytical
PVP-Iodinedisinfectant with a broadantimicrobial spectrum
Crospovidoneindications: stomach andintestinal disorders
Ephedrines
Ephedrinesympathomimetic
Pseudoephedrinesympathomimetic
Actives
Acetylnorbornene
Amezinium Methyl Sulfateantihypotensive
Bamipine Lactatantihistaminic
Biperidene HCl+ Baseanticholinergic, antiparkinsonian
Carbidopaenzyme inhibitor, antiparkinsonian
Tretinoin/Isotretinoin
actives, mainly prescribedin the acne therapy
Retinolactives for oral and
parenteral applications
Hordenine Sulfate
Hydroxyfenone
Isometheptene-Mucateadrenergic,sympathomimetic
Levopropyl-hexedrine HCladrenergic,sympathomimetic
Mefloquine HClantimalarial
Cathine HClanorexic
Dibenzoyltartaric Acid
Dopamine HCl/Dobutamine HCl sympathomimetic, cardiotonic
Etafedrineadrenergic,sympathomimetic
Hippozympancreasenzyme supplement
Oxymetazoline HCl/ Xylometazoline HClsympathomimetic,vasoconstriction
Phenylpropandione
Pyridylacetonitrile
2-Thienylacetonitrile
Troxerutinedema protective
Verapamilcalcium-antagonist
Assorted Pharma Actives
Paracetamolanalgesic, antipyretic
page 9 – No. 5, October 2000 BASF ExAct
Quality,Supply safety,Global commitment.BASF – Yourpartner for thefuture.
BASF – Expertise in Health and Nutrition
MLW
Who can resist?KollicoatY MAE 30 DP, andKollicoatY MAE 100 P, ecologi-cally safe and state of the artagents for aqueous coating, are morecost effective and reliably generate higherresistance to gastric fluid than cellulosederivatives. These easy to use coating agentsshorten production processes and are supportedby BASF’s worldwide network of technical expertise.
BASF – Expertise in Health and Nutrition
MLW
Safety for your success: KollidonY. This wide range ofpolyvinylpyrrolidone products reliably ensures your production.Best product quality proves to be successful in a multitude of possible applications and
thus meets – supported by BASF’s worldwide services – the supreme requirements of the pharmaceutical industry.
QualitySupply safetyGlobal commitment.BASF – Yourpartner for thefuture.
BASF – Expertise in Health and Nutrition
a new excipient for smooth directcompression of sustained release dosage forms.
QualitySupply safetyGlobal commitment.BASF – Yourpartner for thefuture.
MLW
Sustained relief ! KollidonY SR,
Sustained release!Kollicoat EMM 30 D isa superior quality, totallyaqueous system for the manu-facture of pH-independent controlledrelease membrane coatings and matrixtablets. The cost effective excipient may also be applied
successfully in taste masking and protective coating. For bestresults BASF's technical expertise is always at your service – worldwide.
MLW
QualitySupply safetyGlobal commitment.BASF – Yourpartner for thefuture.
BASF – Expertise in Health and Nutrition
MLW
Breakthrough insustained release coating!KollicoatY SR 30 D is a stableaqueous dispersion, characterised by astrong release-retarding activity, a reliable
adjustment of the release rate, easy and costsaving coating processes, excellent film formingproperties, no curing effects, pH-independent releaseprofiles and high storage stability. For best results BASF’stechnical expertise is always at your service – worldwide.
QualitySupply safetyGlobal commitment.BASF – Yourpartner for thefuture.
BASF – Expertise in Health and Nutrition
Doxazosin Mesylateantihypertensive
Fluoxetine HClantidepressant
Omeprazoleinhibitior of gastric acid
secretion
Paroxetine HClantidepressant
Selegiline HCland free baseantidepressant,
antiparkinsonian
Sertraline HClantidepressant
Terazosin HClantihypertensive
KollidonY grades
solubilizers, bindersKollidonY 12 PF/17 PFKollidonY 25/30/90 F
disintegrants,suspension stabilizers
KollidonY CLKollidonY CL-M
(dry) binders, film formersKollidonY VA 64
KollicoatY grades
enteric film coatingsKollicoatY MAE 30 DPKollicoatY MAE 100 P
sustained releasefilm coatingsKollicoatY EMM 30 D
New Pharma Actives
Excipients
LudipressY grades
direct compression agentsLudipressY
LudipressY LCE
sustained releasefilm coatingsKollicoatY SR 30 D
sustained release excipientsKollidonY SR
BASF-Service/Support
LabPilot
ValidationDMF Production
R+D Design NDA/ANDA Market Launch
BASF ExAct page 10 – No. 5, October 2000
LutrolY grades
act e. g. as binders, film-formers, gelling agents,wetting and dispersing agentsLutrolY E gradesLutrolY F grades
Progress in pharmaceutical forms and the need forefficient manufacturing lead to growing sophisticationof active ingredients and excipients. Multi-disciplinaryR&D teams continuously develop variations onproven products and completely new products tofulfill the customer demands in the future.
Global AvailabilityAs a transnational company BASF is represented allover the world. To take care for the demands of ourcustomers the BASF companies have highly trainedsales teams in place. Various regional distributioncenters enable us to deliver the right product to theright place at the right time. Two production sites forKollidon provides a second-source backup. Withhigh-quality ingredients, a knowledgible technicalservice and a supply safety we aim to maintain aclose partnership with the pharmaceutical industry.
Your Partner for the Future
SolutolY HS 15
non-ionic solubilizer for injection solutions
CremophorY grades
solubilizers and emulsifying agentsCremophorY RH 40
CremophorY ELCremophorY ELP
CremophorY A 6/A 25
Solvents
solvent for veterinaryinjectionsSoluphorY P
solvent for oral, topicaland parenteral drugsPropylene Glycol
page 11 – No. 5, October 2000 BASF ExAct
MLW
BASF – Expertise in Health and Nutrition
Vitamins
Essential forlife! BASF offersa wide range of highly
pure and easy to handle
and Vitamin premixes as
well as Carotenoids, par-
ticularly developed for therequirements of the pharmaceutical
and nutritional supplement industry.
QualitySupply safetyGlobal commitment.BASF – Yourpartner for thefuture.
Tretinoin Isotretinoin Retinol Assorted
Pharma Actives New
Pharma Actives
Excipients KollicoatY
KollidonY LudipressY
LutrolY
CremophorY
SolventsY
SolutolY HS 15
Vitamins
Actives Analgesics Purines Ephedrines PVP-Iodine Crospovidone
BASF now provides a wholerange of pharma
ingredients
Fat-solubleVitamins
Vitamin A (retinol)Vitamin D2 (ergocalciferol)Vitamin D3 (cholecalciferol)
Vitamin E (tocopherol)Vitamin K1 (phytomenadione)
CarotenoidsBeta-carotene
Water-solubleVitamins
Vitamin B1 (thiamine)Vitamin B2 (riboflavin)
NiacinPantothenic acid
Vitamin B6 (pyridoxine)Vitamin B12 (cobalamin)
Vitamin H (d-biotin)Vitamin C (ascorbic acid)
Vitamins
Vitamin C
Preview
page 12 – No. 5, October 2000 BASF ExAct
ME
FMR
1000
1e
Aqueous Enteric Coating ofHumidity Sensitive Drugs.
Aqueous enteric coatings are gaining significantimportance and are substituting organic solventsin manufacturing processes for ecological andeconomical reasons.
It is expected that the large amounts of water inaqueous dispersions are going to interfere with thecore and lead to degradation in the core whenhumidity sensitive drugs, e.g. aspirin or pancreatine,are used. For this reason sometimes subcoatings
In addition to standard tests on Cremophor EL fouradditional specifications on acid-and peroxide value,water contents and limits of alcohol-soluble impuritiesare enclosed.
Since July 2000 a 3rd edition of the CD-ROM con-taining the folder “Generic Drug Formulations” and thebook “Kollidon – Polyvinylpyrrolidone for thepharmaceutical industry” is now available.
In the “Generic Drug Formulations” more than 30 newformulations of different drug forms were included.These formulations mainly are based on our newexcipients like for example the Kollicoat grades, Ludi-press LCE and the research product Kollidon SR.
In the Kollidon book 15 new paper references wereadded to the applications and some parts of theanalytical chapters were actualized (e.g. determina-tion of monomers and formic acid).
Contactare applied when using aqueous coating disper-sions. Among the aqueous enteric coatings, metha-crylic acid copolymer type C (Kollicoat MAE 30 DP)offers advantages in acid resistance and manufac-turing time compared to enteric cellulose derivatives.
ExAct No. 6 will inform you about the suitability ofKollicoat MAE 30 DP for enteric coating of a highlyhumidity sensitive active ingredient (aspirin) withoutusing a subcoating.
For information in advance: Please contact your localBASF company or one of our regional centres.
The United States Pharmacopoeial Conventionpublished a new monograph on “Purified Polyoxyl35 Castor Oil” in volume 26, number 4 of the Pharma-copoeial Forum issued July–August 2000.
Fax: **1/9734265355
Please contact your local BASF companyor one of the following regional centres:
Asia
BASF East Asia RegionalHeadquarters Ltd.Dr. Danilo Mercado7/F., Tower I, South Seas Centre EastTsim Sha TsuiP.O. Box 98427Kowloon, Hong-KongFax: **852/23122261
Europe
BASF AktiengesellschaftLNF/FP – J550Mr. Peter HoffmannD-67056 LudwigshafenGermanyFax: **49/62160-22627
NAFTA
BASF CorporationPharma IngredientsMr. Charles Dods3000 Continental Drive-NorthMount Olive, NJ 07828-1234USA
South America
BASF S.A.Fine ChemicalsMr. Claudio LehmannCaixa Postal 13609701-970 São Bernardo do Campo - SPBrazilFax: **55/117512255
Eastern Europe/Africa/West Asia
BASF AktiengesellschaftLRM/M – D 205Mr. Rolf Hanssen/Mr. Matthias HofD-67056 LudwigshafenGermanyFax: **49/62160-44689
Or visit our website:http://www.basf.de/pharma
NewsCremophor ELP: Monograph on “Purified Polyoxyl35 Castor Oil” published in Pharmacopoeial Forum.
New Media3rd edition of the CD-ROM“Generic Drug Formulation/Kollidon”.
TitelRiboflavin 100Kollicoat® SR 30 DKollidon® VA 64One Source: The PortfolioPreviewNewsNew Media
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