Carbopol 1

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Carbopol polymers are polymers of acrylic acid cross-linked with polyalkenyl ethers or divinyl

glycol. They are produced from primary polymer particles of about 0.2 to 6 micron average
diameter. The flocculated agglomerates cannot be broken down into the ultimate particle when
produced.

Each primary particle can be viewed as a network structure of polymer chains interconnected
by cross-links. Without the cross-links, the primary particle would be a collection of linear
polymer chains intertwined but not chemically bonded. Carbopol polymers, along with
Pemulen® and Noveon® polymers are all cross-linked. They swell in water up to 1000 times
their original volume (and 10 times their original diameter) to form a gel when exposed to a pH
environment above 4.0 to 6.0. Because the pKa of these polymers is 6.0 to 0.5, the carboxylate
groups on the polymer backbone ionize, resulting in repulsion between the negative charges,
which adds to the swelling of the polymer. The glass transition temperature of Carbopol
polymers is 105°C (221°F) in powder form. However, the glass transition temperature decreases
significantly as the polymer comes into contact with water. The polymer chains start gyrating,
and the radius of gyration becomes increasingly larger. Macroscopically, this phenomenon
manifests itself as swelling.

The readily water-swellable Carbopol polymers are used in a diverse range of pharmaceutical
applications to provide:

 Controlled release in tablets. Carbopol polymers offer consistent performance over a


wide range of desired parameters (from pH-derived semi-enteric release to near zero-
order drug dissolution kinetics) at lower concentrations than competitive systems.
 Bioadhesion in buccal, ophthalmic, intestinal, nasal, vaginal, and rectal applications.
 Thickening at very low concentrations (less than 1%) to produce a wide range of
viscosities and flow properties in topical lotions, creams and gels, oral suspensions, and
in transdermal gel reservoirs.
 Permanent suspensions of insoluble ingredients in oral suspensions and topicals.
 Emulsifying topical oil-in-water systems permanently, even at elevated temperatures,
with essentially no need for irritating surfactants.

Oral Suspension Applications of Cabopol

Carbopol polymers have been used worldwide in oral suspensions for many years to thicken,
modify flow characteristics, suspend insoluble ingredients, and to provide bioadhesion. These
cross-linked polymers of acrylic acid provide excellent suspending ability for insoluble
ingredients, and virtually eliminate the problem of settling, even when used at very low levels.
Carbopol polymers swell when hydrated and neutralized, forming a colloidal dispersion. The
insoluble ingredients in the suspensions are then permanently trapped in the interstitial spaces
between the hydrogel particles.

Controlled-Release & Solid Dosage Applications of Carbopol

Although Carbopol polymers have enjoyed success in controlled-release solid dose


formulations, the number of companies developing and commercializing controlled-release
tablets using Carbopol and Noveon polymers has increased significantly in recent years. In
response to this commercial interest, we have tested a variety of excipients and active drug
ingredients in tablet models using both direct-compression and wet granulation methods.
These polymers can be successfully formulated into a variety of different tablet forms, including
the traditional swallowable tablets, chewable tablets, buccal tablets, sublingual tablets,
effervescent tablets, and suppositories; providing controlled-release properties as well as good
binding characteristics.

Tablet formulations using Carbopol polymers have demonstrated zero-order and near zero-
order release kinetics. These polymers are effective at low concentrations (less than 10%) and
feature extremely rapid and efficient gelation characteristics under both simulated gastric fluid
(SGF) and simulated intestinal fluid (SIF) test conditions. They also produce tablets of excellent
hardness and low friability over a range of compression forces, as well as demonstrably longer
dissolution times at lower concentrations than other controlled-release excipients. Greater
formulating latitude in dosage forms is therefore possible using Carbopol polymers as the
functional controlled-release excipient.

Because Carbopol polymers swell rapidly in water and absorb great quantities, to avoid the use
of flammable solvents, we use roller compaction as the method to prepare a new form of
Carbopol polymer. It is compressed into tapes, which are fed into a mill where the particle size
is reduced to the desired range.

Carbopol polymer 71G NF is a useful and versatile controlled-release additive for tablet
formulations in direct compression with the following characteristics:

 Good tableting formulation flowability,


 Good tablet hardness with press-operating latitude,
 Good tablet friability over variations in press speed and compression pressure,
 Long drug release profiles (often zero order),
 Release profiles can be controlled by varying Carbopol 71G NF polymer levels,
 Can be processed by wet granulation if desired, and
 Can give Drug Release Profiles similar to Carbopol 971P NF polymer, but with less dust
and better handling characteristics.

Bioadhesive Applications of Cabopol

Bioadhesion (or mucoadhesion) is generally understood to define the ability of a biological or


synthetic material to “stick” to a mucous membrane, resulting in adhesion of the material to
the tissue for a protracted period of time. This concept has received a significant degree of
attention due to potential applications in drug delivery and enhanced drug bioavailability, which
results from the lengthened period of time in which the bioadhesive dosage form is in contact
with the absorbing tissue versus a standard dosage form.
Many commercial oral and topical products available today have been formulated with
Carbopol and Noveon polymers, as they have numerous features that provide key benefits in
bioadhesive formulations.Carbopol and Noveon polymers:

 Are safe and effective in oral and topical applications,


 Are bioadhesive, enabling increased bioavailability of ophthalmic, nasal, buccal,
intestinal, rectal, and vaginal formulations,
 May protect proteins and peptides from degradation by proteolytic enzymes, enabling
increased bioavailability of protein- or peptide-based formulations, and
 Are approved by many of the world’s pharmacopoeias, facilitating regulatory approvals
worldwide.

Topical Applications of Cabopol

Carbopol, Pemulen, and Noveon polymers are very well suited to aqueous formulations of the
topical dosage forms. Many commercial topical products available today have been formulated
with these polymers, as they provide the following numerous benefits to topical formulations:

 Safe & Effective — Carbopol, Pemulen, and Noveon polymers have a long history of safe
and effective use in topical gels, creams, lotions, and ointments. They are also supported
by extensive toxicology studies.
 Non-Sensitizing — Carbopol, Pemulen, and Noveon polymers have been shown to have
extremely low irritancy properties and are non-sensitizing with repeat usage.
 No Effect on the Biological Activity of the Drug — Carbopol polymers provide an
excellent vehicle for drug delivery. Due to their extremely high molecular weight, they
cannot penetrate the skin or affect the activity of the drug.
 Excellent Thickening, Suspending, & Emulsification Properties for Topical Formulations

Products with a wide range of viscosities and flow properties have been successfully formulated
and commercialized. Carbopol polymers are used to permanently suspend the active
ingredients in Transdermal reservoirs as well as in topical gels and creams. Pemulen polymeric
emulsifiers can be used to prepare stable emulsions, such as turpentine liniment, without the
use of surfactants. Carbopol polymers and Pemulen polymeric emulsifiers are often the
thickener and emulsifier of choice in topical lotions.

Taste Masking Application of Carbopol

Carbopol polymer is widely used in formulation & development of taste masked of bitter active
pharmaceutical ingredients, because more than 50% of the pharmaceutical formulation having
a bitter taste and for the patient convince and pediatric patients it require to mask the bitter
taste with suitable method.

Chewable dosage forms of Carbopol

Disclosed is a soft, chewable dosage form, including a matrix of hydrogenated starch


hydrolysate, a water soluble bulking agent, and a water insoluble bulking agent. The present
invention also includes a method of preparing a soft, chewable dosage form, including the steps
of mixing under high shear force, a hydrogenated starch hydrolysate, a water soluble bulking
agent, and a water insoluble bulking agent until a uniformly blended matrix is obtained. Active
ingredients may optionally be incorporated in the matrix.

Physical Properties

The three dimensional nature of these polymers confers some unique characteristics, such as
biological inertness, not found in similar linear polymers. The Carbopol resins are hydrophilic
substances that are not soluble in water. Rather, these polymers swell when dispersed in water
forming a colloidal, mucilage-like dispersion.

Carbopol polymers are bearing very good water sorption property. They swell in water up to
1000 times their original volume and 10 times their original diameter to form a gel when
exposed to a pH environment above 4.0 to 6.0. Because the pKa of these polymers is 6.0 to 0.5,
the carboxylate moiety on the polymer backbone ionizes, resulting in repulsion between the
native charges, which adds to the swelling of the polymer. The glass transition temperature of
Carbopol polymers is 105°C (221°F) in powder form. However, glass transition temperature
decreases significantly as the polymer comes into contact of water. The polymer chains start
gyrating and radius of gyration becomes increasingly larger. Macroscopically, this phenomenon
manifests itself as swelling.

Table No.1 Physical and Chemical Properties of Carbopol 6

Appearance Fluffy, white, mildly acidic polymer


Bulk Density Approximately 208 kg/m 3 (13 lbs. ft 3 ) *
Specific gravity 1.41
Moisture content 2.0% maximum
Equilibrium moisture content 8-10% (at 50% relative humidity)
PKa 6.0 ± 0.5
pH of 1.0% water dispersion 2.5 - 3.0
pH of 0.5% water dispersion 2.7 - 3.5
Equivalent weight 76 ± 4
Ash content 0.009 ppm (average) **
Glass transition temperature 100-105 0 C (212-221 0 F)

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