End Semester Presentation on Carbopols & Its pharmaceutical application

Supervisor Prof. R. N. Saha Presented By

Satish Reddi
(2011PHXF410P)

Outline
Introduction Types of Carbopols Properties of Carbopols Applications References

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Introduction
Carbopols are high molecular weight, cross-linked, acrylic acid polymers. The first Carbopol polymers, developed in 1958 by Noveon. Noveon was acquired by Lubrizol in 2004. In various pharmacopeia, Carbopols also termed as

carbomers, carboxyvinyl polymer, carboxy polymethylene, etc. The main differences among the Carbopols are related to the

cross-linker type and density, and presence of hydrophobic

comonomers as summarized below.
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Types of carbopol
Carbopol homopolymers are polymers of acrylic acid cross-

linked with allyl sucrose or allylpentaerythritol.

Carbopol copolymers (Pemulen) are polymers of acrylic acid and C10-C30 alkyl acrylate cross-linked with allyl

pentaerythritol. Carbopol interpolymers are carbomer homopolymers or copolymers that contain a block copolymer of polyethylene glycol and a long chain alkyl acid ester. Noveon polycarbophil is a polymer of acrylic acid cross-linked
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with divinyl glycol.

Types of carbopol
Class Carbopol homopolymers Carbopol interpolymers Carbopol grades Carbopol 971P NF, Carbopol 974P NF, Carbopol 71G NF, Carbopol 980 NF, Carbopol 981 NF and Carbopol 5984 EP Carbopol ETD 2020 NF and Carbopol Ultrez 10 NF

Carbopol
copolymers Noveon

Pemulen TR-1 NF and Pemulen TR-2 NF

polycarbophil
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Noveon AA-1 USP

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Benzene solvent toxicity

Starting in the 1980s new products and processes using ethyl acetate and ethyl acetate/cyclohexane co-solvents were introduced to enhance product safety.
Benzene grade polymer Carbopol 934 NF Recommended non-benzene grade polymer Carbopol 5984 EP and Carbopol Ultrez 10 NF

Carbopol 934P NF
Carbopol 940 NF Carbopol 941 NF Carbopol 1342 NF
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Carbopol 974P NF
Carbopol 980 NF and Carbopol Ultrez 10 NF Carbopol 71G NF, Carbopol 971P NF and Carbopol

981NF
Pemulen TR-1 NF and Pemulen TR-2 NF
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Chemical nature
General structure

Carbopol polymers have an average equivalent weight of 76 per carboxyl group.

The carboxyl groups provided by the acrylic acid backbone of

the polymer are responsible for many of the product benefits.
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Typical properties of carbopols

Carbopol polymers are offered as fluffy, white powder. The molecular weight of these polymers is theoretically estimated to range from 700,000 to 3 or 4 billion. These are flocculated powders averaging 2 to 7 microns in diameter. Carbopols are insoluble in water but they swell in water up to 1,000 times their original volume (and ten times their

original diameter).
Carbopols form gel when exposed to pH above 4 to 6.
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Typical properties of carbopols

pKa : 6 0.5 Glass transition temperature: 105oC Melting Point : Unknown Bulk Density: approximately 208 Kg/m3

Specific gravity: 1.41

pH of 1.0% water dispersion: 2.5 - 3.0 Moisture content: 2.0% maximum Equilibrium moisture content: 8-10% (at 50% relative humidity)
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Applications of carbopols
Oral grades of Carbopols: 1. Carbopol 974P 2. Carbopol 971P 3. Carbopol 71G

4. Carbopol 934P
5. Noveon AA-1 US

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Applications of carbopols
Carbopol 971P NF : controlled release tablets, oral suspensions and bioadhesive provides thickening, suspending and emulsion stabilizing properties to low viscosity systems for topical applications Carbopol 71G NF : granular form of Carbopol 971P NF polymer ideal for use in direct compression for tablets

same chemical with no additives and improved flow properties

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Applications of carbopols
Carbopol 974P NF : Controlled release tablets, oral suspensions and bioadhesive Provides thickening, suspending and emulsion stabilizing properties to high viscosity systems for topical applications Noveon AA-1 USP: Industry standard bioadhesive Buccal, intestinal, nasal, vaginal and rectal bioadhesive

products can all be formulated

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Applications of carbopols
As extended release oral solid dosage form Bioadhesion in buccal, ophthalmic, intestinal, nasal, vaginal and rectal applications Permanent suspensions of insoluble ingredients in oral suspensions and topical formulations Emulsifying topical oil-in-water systems permanently, even at elevated temperatures, with essentially no need for irritating

surfactants

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Applications of carbopols
Rheology modification at very low concentrations (less than 1%) to produce a wide range of viscosities and flow properties in lotions, creams and gels, oral suspensions, and in transdermal gel reservoirs.

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References
Lubrizol: Polymers for pharmaceutical application. Pharmaceutical Bulletin. Bulletin-1, 31May 2011. http://www.pharmainfo.net/reviews/carbopol-and-its-pharmaceuticalsignificance-review Lubrizol: Lubrizol pharmaceutical polymer for controlled release tablets and capsules. Pharmaceutical Bulletin. Bulletin-30, 31May 2011. Lubrizol: Lubrizol pharmaceutical polymer for controlled release tablets and capsules. Pharmaceutical Bulletin. Bulletin-31, 31May 2011. Guo J. Carbopol polymers for pharmaceutical drug delivery Wednesday, 05 June 2013 15 applications Drug development and delivery. 2003, 3:21-26

Thank you