Design of Dosage Forms

design of dosage forms
To optimize the appearance of dosage is necessary to

have a perfect knowledge of the physical properties of
chemical ingredients formulated to dosage.
Drug substances are rarely given as a chemical entity
but is almost always given in some types of formulations.
The initial phase of each new formulation of a
preparation needed pre-formulation studies.
Prefomulation is the assessment to gather particulars
about the basic physical and chemical characteristics of
the drug substance
The purpose of preformulation is to assist in developing a
stable formulation, safe and effective
Several parameters were evaluated:

1. The shape and size of particles:
2. Solubility
3. Stability
4. Polymorphic
5.Partitioning effect
6.Permeability
7.Dissolution
Data obtained from the evaluation of enhanced with data
obtained from the preliminary study
Pre-formulation research is usually conducted after a fairly
active compound demonstrated useful in tests on humans
When the pre-formulations investigated perfect, the data
is record for its development
The shape and size of particles

Use of the desired form of fine powder in pharmaceutical products, one
of the basic properties of physics are common all fine powder distributed
Physical properties of substances and certain chemical drugs influenced
by the particle size distribution, including drug dissolution rate,
bioavailability, content uniformity and stability
Characteristics of flow and sedimentation rate are also important factors
related to particle size
Particle size proved to significantly affect oral absorption profile of
certain drugs
Substance satisfactory uniformity in the solid dosage forms is
dependent upon the particle size and distribution of the active
ingredient
Keseragaman isi yang memuaskan dalam bentuk sediaan padat sangat

tergantung kepada ukuran partikel dan distribusi bahan aktif
Ukuran partikel terbukti secara bermakna mempengaruhi profil absorpsi
There are several methods

available to evaluate the particle
size:
Sieving
Microscopic
Sedimentation
1. Sieving
- Used a series of sieves, ranging from 100 mesh to 10
mesh, sieve compiled from the largest aperture adjacent
the top to the smallest aperture on the bottom. The
powder is put on the top sieve done sifting the sieving
machine with a speed of 150 times / min. For the
powders in the range of approximately 44 microns or
larger. Screening is the most widely used method.
2. Microscopic
Optical microscopy is often the first step in determining
particle size and shape to the new drug substance. Used an
optical microscope, equipped with a glass object count rooms
that have a certain size scale, powder under the microscope.
3. Sedimentation
- Sedimentation technique using the relationship between the
rate of fall of particles and size. Particles suspended in a
carrier fluid is then allowed to occur precipitation. Diameter
can be calculated. This method is now enhanced by using a
coulter counter which can simultaneously measure the volume
of the particle.
Solubility
-An important physicochemical properties of a drug substance
is solubility, especially solubility in water systems.
A drug must have a solubility in water that is therapeutically
effective
In order for a drug gets to a system of circulation and produce
a therapeutic effect, it must first be in solution.
The compounds are relatively insoluble often showed
absorption is not perfect.
If the solubility of the drug substance is less than diingikan,
consideration should be given to improve the solubility.
Methods to help this depends on the chemical properties of
the drug.
For example, if the drug substance is acidic or alkaline

solubility may be affected by changes in pH.
But for many substances pH adjustment is not an
effective way to improve solubility.
In many ways it is desirable to use kosolven or other
techniques Reviews such as complexation or dispersion
of solids to improve water solubility.
The solubility of the drug is usually determined by the
method of equilibrium, in which the excess drug is
placed in a solvent and stirred at a constant
temperature for an extended period of time until
equilibrium is obtained.
Partition coefficient
A measurement of drug lipophilicity and an indication of its
ability to pass through the cell membrane is the partition
coefficient oil / water in systems such as octanol / water and
chloroform / water.
Partition coefficient is defined as the ratio of unionized drug
between the organic phase and the aqueous phase at
equilibrium.
To produce a biological response, the drug molecule must first
cross a biological membrane acts as a barrier fat for most drugs
and allow the absorption of substances that are soluble in fat by
passive diffusion, while substances that are not soluble in fat
can diffuse cross the barrier with great difficulty.
The relationship between dissociation constants lipid solubility,
and the pH at the site of absorption of various drugs are the
basis of the theory of partitions pH
Polymorphism
Polymorphism is the ability of a compound or element
to crystallize more than one type of different crystals to
obtain the drug in the two crystal forms.
An important factor that formulation was crystalline or
amorphous forms of the drug substance.
Forms of polymorphism usually show different
physicochemical properties including melting and
dissolution.
The energy required for a drug molecule to be free of a
crystal is much larger than that needed to be free from
an amorphous powder.
Therefore the amorphous form of a compound is always
more soluble than the crystalline form.
Changes in crystal characteristics can affect

bioavailability, chemical and physical stability and has
important implications for the functions the dosage form.
As an example can be a significant factor with respect to
the tablets because of the properties of the flow and
pengkompakan
Various techniques are used in determining the
properties of the crystal. The most widely used method is
the hot stage microscopy, thermal analysis, spektrokopy
infrared and x-ray diffraction.
Berbagai teknik digunakan dalam menentukan sifat-sifat
kristal. Metode yang paling luas digunakan adalah hot
stage microscopy, analisis panas, spektrokopy
inframerah dan difraksi sinar-x.
Dissolution
The difference in biological activity of a drug substance may
be caused by the rate at which the drug becomes available
to the organism.
Dissolution is the process by which a solid substance
dissolves
Dissolution is a requirement that a drug can be absorbed by
the digestive tract or the liquid part of the body.
In many ways the dissolution rate or the time it takes for the
drug to dissolve in the liquid at the site of absorption.
For drugs that are administered orally in solid form such as
tablets, capsules or suspension, as well as drugs that are
administered intramuscularly in the form of pellets or
suspension.
When the dissolution rate is the stage that determines

the rate, whatever influence it will affect absorption.
As a result of dissolution rate can affect the
bioavailability of the drug from the dosage form overall.
As previously discussed the dissolution rate can be
increased by increasing the particle size of the drug,
which increases the solubility in the diffusion layer.
Ways that are most effective in obtaining the dissolution
rate is to use a water-soluble salt of the parent
substance.
Permeability
Assessment modern prefomulasi includes inputs
beginning of the passage of drug molecules across
biological membranes.
The data obtained from the study of physics-chemistry,
solubility and dissolution rate gives an expected
absorption.
Stability
One of the most important activities in preformulasi work is the
evaluation of physical-chemical stability of the pure substances.
Assessment of the stability of which is connected in the phase
of pre-formulation, including the stability of the drug itself in
the solid state, solution phase stability and stability in the
presence of substances is expected.
Chemical instability of the drug substance can take many
forms, because the drugs used today are diverse chemical
constituents.
In chemical drug substance is alcohol, phenols, aldehydes,
ketones, esters, acids, salts, alkaloids, glycosides and others,
each with relative chemical groups that have different tendency
to chemical instability.
In the chemical process of damage is most often include

hydrolysis and oxidation.
Hydrolysis is a process solvolysis where drug molecules
interact with water molecules to produce a product
fractions with different chemical structures.
For example, aspirin or acetyl salicylic acid in
combination with a water molecule and hydrolyze into
one molecule of acetic acid.

Design of Dosage Forms

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Design of Dosage Forms

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design of dosage forms

To optimize the appearance of dosage is necessary to

Several parameters were evaluated:

The shape and size of particles

Keseragaman isi yang memuaskan dalam bentuk sediaan padat sangat

There are several methods

For example, if the drug substance is acidic or alkaline

Changes in crystal characteristics can affect

When the dissolution rate is the stage that determines

In the chemical process of damage is most often include

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