31 Payuran, Joselle Anne F.

2E-PH
32 Que, Bill A. September 12,
2014

Alekseev, K.V, Blynskaya, E.V., Tikhonova, N.V., Alekseev, V.K., Uvarov, N.A., Chernova, O.A.
(2010).Polymers in the Formulation of Drug Dosage Forms with Modified Release. The
Russian Journal of General Chemistry, 2012, 82 (3), pp. 564571.
Polymers in the Formulation of Drug Dosage Forms with Modified Release
This journal contains the new polymer based dosage forms with their pharmaceutical properties and
descriptions of the different modified release dug dosage forms. This study was done using a descriptive
method of research. The contents were collected using peer reviewed journals and studies regarding
polymers used in the pharmaceutical industry to produce modified release drug dosage forms.
In the production of solid dosage forms, manufacturers employ wide range auxiliary substances including
polymers. These auxiliary substances may be directly incorporated during the production or applied as
film coatings to achieve overall stability, physicochemical, and biopharmaceutical properties. The
introduction of polymers into the pharmaceutical practice led the way to designing new drug dosage forms
with modified release of active ingredients as well as those with preset biopharmaceutical properties.
Polymers allow the programming of the size and release of the drug from pills in humans. The drug
dosage forms with continued release have common features that include a preset extended or accelerated
delivery of an active ingredient to the bio phase and the release time.

The process of releasing the active ingredient is controlled if: (1) the mathematical equations and formula
that relates to the quantity of substance released within the boundary of controlling process is known; (2)
the release of substances is according to the pharmacokinetic program; (3) the physiologic conditions do
not greatly or directly affect the rate of release. Dosage forms with extended release provide slow release
and extended action of the drug. This lessens the frequency of the administration of drugs and that it
alleviates the side effects that drug may impart. The rate of the drug release depends on the nature of the
excipient and the overall solubility of the drug, as well as the porosity. Extended release dosage forms are
provided through the use matrix tablets or film coatings. In the matrix tablets, the active drug is directly
incorporated into mixture of hydrophilic or gel forming substances, or insoluble polymers. This creates the
sustainability of the drug release evenly for a long time and act sustainably. Different types of matrix
tablets include: carcass, skeleton, insoluble carcass, and durules. Carcass tablets matrix is formed by
network of polymers with the drugs included in its structure. The matrix tablets provide modified release
of drug. The controlled regimens include: extended release is formed from insoluble carcass; controlled
release forms pH-dependent release; and accelerated release contains solid drug dispersions.

Matrices that provide extended release

Tablet matrices can preserve their geometric shape throughout the time they stay in the body and can be
excreted intact. They can also swell and slowly dissolve that makes it possible extended release. The rate
of release depends on the pH of the medium of the body with different variations depending on the part of
the digestive tract. It can also depend on the content of the digestive enzymes. Polymer excipients are
divided into hydrophilic and hydrophobic depending on their interaction medium of the body. Meanwhile,
in terms of capacity to release drug depending on the pH of the medium, polymer excipients are divided
into pH-dependent and pH-independent (inert matrices). Swelling polymers forms hydrophilic matrices,
which include derivatives of cellulose, acrylic acid, and polyvinyl alcohol. On the other hand, inert
matrices are made of water-insoluble polymers that include polyvinyl chloride, polyethylene,
polyurethanes, and co-polymers of vinyl acetate and vinyl chloride, and ethyl cellulose. For gradual drug
release, the water insoluble polymer and water-soluble components should have a link with each other and
thus polyethylene glycol, polyvinylpyrrolidone, lactose, and pectin must be introduces in the matrix to
wash out these components from the tablet carcass. Ion-exchange resin is used to precipitate the drugs to
induce extension of drug release. The advantage of this method is that the rate of release of drug is
independent of the pH of the medium, activity of the digestive enzymes, peristalsis and other physiologic
factors. Moreover, it depends exclusively on the concentration of the counter ions and the rate of diffusion
of exchanging ions. Extended-action drugs with ion exchange matrices are known as ionexiten, resonates,
ion exchange salts, and ion-exchange complexes.

Cellulose derivatives are among the hydrophilic polymers used as matrices for extended action drugs. One
example of this matrix is hydroxypropyl methylcellulose, which creates a diffusion barrier and has a wide
range of molecular weight that makes it possible to obtain gels and also important in the production of
soluble matrix tablets. Cellulose derivatives are applied as binders or film formers in water based film
coating and they are pH independent matrices. Carbopols strongly swell in water to form a gel layer. The
gel layer forms within 10 min at pH 4.0-6.0.

Controlled Drug Release Matrices
Interpolymer complexes formed by reactions of complementary macromolecules. Drug release from the
matrix tablets on the basis of a composite polymer carrier that is an interpolymer complex of poly
(methacrylic acid) and poly (ethylene glycol). Controlled release drug release drugs in portions to mimic
circadian drug intake. The drug is released in intervals (irrespective of where the tablet resides in the
gastrointestinal tract) .
Sustained release drug dosage forms are produced using special auxiliary substances. The initial drug dose
is released immediately after intake, and further doses are released gradually at a constant rate to the
excretion rate. It is more efficient than pulsed release forms. Special polymers are used for the production
of hydrodynamically balanced tablets, which float in the gastric juice and preserve the property.
Hydrocarbonates impart to the floatability if tablets. The evolution of carbon dioxide accelerated
hydration of floating tablets.

Matrices Providing Accelerated Drug Release

Advantages of solid disperse systems include: (1) enhanced bioavailability of hardly soluble and extended
action of readily soluble substances; (2) accelerated initiation of therapeutic action; (3) decreased
therapeutic dose at the same therapeutic effect; and (4) less frequent side effects. These systems are
produced through direct extrusion or hot melt extrusion. Polymers that should be used must be stable, non-
toxic, and moisture-insensitive, and their glass transition state should be between 50-180C. These systems
must also have the following characteristics: (1) lipophicity, (2) proton donor or acceptor ability, and (3)
presence of an amido group to enhance solubilizing capacity. Production of nanoparticles and
microspheres is an important direction in the development of pharmacy. Particle size affects drug release
profile and action site. The pharmaceutical industry produces delivery systems containing extended
release microspheres.

Drug dosage forms with polymer film coatings

The progress in the technology of production of tablets with film polymer coatings is favored by the
advantages offered by such drug dosage forms. These include selective solubility of tablets in the stomach
or intestine; controlled rate of drug adsorption; possibility to combine incompatible active substances in a
single dosage form; preservation of the physical, chemical and mechanical properties of tablet core; lower
weight compared with encapsulating coatings; and possibility of automation of the coating process.
At present, more than 50-film forming materials are used .For water-soluble film coatings, metolose,
CEKOL, Aquacoat ECD, and surelease are the materials often used. Intestine-soluble film on the other
hand uses hypromellose phthalate, Aquacoat CPD, Pharmacoat Shin-Esti, OPADRY, and Sepifil as the
film material. Commercial film-forming materials for intestine-soluble coatings include materials such as
Sureteric, Kollicoat MAE 30 DP , and Kollicoat MAE 100P.
Conclusion
The production of modified release dosage forms is based on the application of polymers so as to preset
biopharmaceutical properties and barriers to provide stability and physicochemical properties.
Reflection
This journal has a great significance in the study of pharmacy especially on the production and research of
new drugs that will improve the quality of life of many people. Modified release dosage forms greatly
improve the patient compliance and reduce the possible side effects of drugs to our body. These polymers
improves the dosage form through stabilization of the dosage forms and physical properties to produce the
various requirements for creation of different modified release dosage forms so as to protect the drug and
effectively release the drug in required time notwithstanding the presence of physical conditions inside the
body like the pH and etc.
This journal was very in-depth research project. The introduction, discussion, and conclusion were well
written and well organized. The contents were all procured in valid sources. Overall, it was very
interesting and a significant contribution to the practice of pharmacy as well as to the improvement of
delivery of drugs to improve the health care system.