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Pre Formulation

Preformulation involves determining the physicochemical properties of a new drug substance to help guide formulation development. Key goals are to establish parameters like particle size and shape, purity levels, and compatibility with excipients. This information generates useful data for designing an optimal drug delivery system prior to formal development of dosage forms. Characterization techniques evaluate attributes such as color, odor, taste, flow properties and how these may impact drug performance.

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Meghana J
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223 views15 pages

Pre Formulation

Preformulation involves determining the physicochemical properties of a new drug substance to help guide formulation development. Key goals are to establish parameters like particle size and shape, purity levels, and compatibility with excipients. This information generates useful data for designing an optimal drug delivery system prior to formal development of dosage forms. Characterization techniques evaluate attributes such as color, odor, taste, flow properties and how these may impact drug performance.

Uploaded by

Meghana J
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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 Preformulation.

• Preformulation is branch of Pharmaceutical science that utilizes


biopharmaceutical principles in the determination of
physicochemical properties of the drug substance.
• Prior to the development of any dosage form new drug , it is
essential that certain fundamental physical & chemical
properties of drug powder are determined .
• This information may dictate many of subsequent event &
approaches in formulation development.
• This first learning phase is called as preformulation.

DEFINITION:-
Investigation of physico-chemical properties of the new drug
compound that could affect drug performance and development
of an efficacious dosage form”.
Preformulation commences when a newly synthesized drug shows
a sufficient pharmacologic promise in animal model to warrant
evaluation in man.
• The preformulation is the first step in the rational development
of a dosage form of a drug substance alone and when combined
with excipients.
• Objective :
To generate useful information to the formulator to design
an optimum drug delivery system.
• Before embarking on a formal programme of preformulation,
scientist must consider the following :
1. Available physicochemical data (including chemical
structure, different salt available).
2. Anticipated dose.
3. Supply situation and development schedule.
4. Availability of stability – indicating assay.

GOALS OF PREFORMULATION.

• To establish the necessary physicochemical parameters of new


drug substances.
• To determine kinetic rate profile.
• To establish physical characteristics.
• To establish compatibility with common excipients.
Preliminary Evaluation.
a) Compound identity.
b) Formula and molecular weight.
c) Structure.
d) Therapeutic indications:
- Probable human dose.
- Desired dosage form(s)
- Bioavailability model
- Competitive products
e) Potential hazards
f) Initial bulk lots:
- Lot number
- Crystallization solvent(s)
- Particle size range
- Melting point
- % volatiles
g) Analytical methods:
- HPLC assay
- TLC assay
- UV/ Visible spectroscopy

• Color is generally a function of a drug’s inherent chemical


structure relating to a certain level of unsaturation.
• Color intensity relates to the extent of conjugated unsaturation
as well as the presence of chromophores.
• Some compound may appear to have color although structurally
saturated.

Odour.
• The substance may exhibit an inherent odor characteristic of
major functional groups present.
• Odor greatly affects the flavor of a preparation or food stuff.
 Taste:-
• If taste is considered as unpalatable, consideration is to be given
to the use of a less soluble chemical form of the drug.
• The odour and taste may be suppressed by using appropriate
flavors and excipients or by coating the final product.
PURITY.
• Designed to estimate the levels of all known & significant
impurities & contaminates in the drug substance under
evaluation.
• Study performed in an analytical research & development
group.
• It is another parameter which allows for comparison with
subsequent batches.
• Occasionally, an impurity can affect stability.
e.g.
- Metal contamination
- Appearance
• The techniques used for characterizing the purity of a drug are
the same as those used for other purpose in a preformulation
study.
• Thin layer chromatography is a wide ranging applicability & is
an excellent tool for characterizing the purity.
• HPLC, paper chromatography & gas chromatography are also
useful.
• More quantitative information can be obtained by using
quantitative differential scanning colorimetry.
PARTICLE SIZE.
• Particle size is characterized using these terms :
i. Very coarse (#8)
ii. Coarse (#20)
iii. Moderately coarse (#40)
iv. Fine (#60)
v. Very fine (#80)
• Particle size can influence variety of important factors :
- Dissolution rate
- Suspendability
- Uniform distribution
- Penetrability
- Lack of grittiness
Methods to Determine Particle Size.
• Sieving
• Microscopy
• Sedimentation rate method
• Light energy diffraction
• Laser holography
• Cascade impaction
1. Sieving method :
• Range : 50 – 150 µm
• Simple, inexpensive
• If powder is not dry, the apertures get clogged.
2. Microscopy :
• Range : 0.2 – 100 µm
• Particle size can be determined by the use of calibrated grid
background.
• Most direct method.
• Slow & tedious method.
4. Light energy diffraction :
• Range : 0.5 – 500 µm
• Particle size is determined by the reduction in light reaching the
sensor as the particle, dispersed in a liquid or gas, passes
through the sensing zone.
• Quick & fast.
5. Laser holography :
• Range : 1.4 – 100 µm
• A pulsed laser is fired through an aerosolized particle spray &
photographed in three dimensional with holographic camera,
allowing the particles to be individually imaged & sized.
6. Cascade impaction :
• The principle that a particle driven by an airstream will hit a
surface in its path, provide that its inertia is sufficient to
overcome the drug force that tends to keep in it in airstream.
POWDER FLOW PROPERTIES.
 Powder flow properties can be affected by change in particle
size, shape & density.
 The flow properties depends upon following-
1. Force of friction.
2. Cohesion between one particle to another.
 Fine particle posses poor flow by filling void spaces between
larger particles causing packing & densification of particles..
 By using glident we can alter the flow properties.
e.g. Starch, Talc.
PARTICLE SHAPE.
• Particle shape will influence the surface area, flow of particles,
packing & compaction properties of the particles.
• A sphere has minimum surface area per unit volume.
• Therefore, these properties can be compared for spheres &
asymmetric particles, in order to decide the shape.
• The following expression can be obtained:
Property Sphere particle
surface area πds2 α s x d p2
volume (1/6)πds3 αv x dp3
HOWEVER SIZE REDUCTION
IS NOT REQUIRED IN FOLLOWING CASES.
• WHEN DRUG IS UNSTABLE.
• DEGRADE IN SOLUTION FORM.
• PRODUCE UNDESIRABLE EFFECTS.
• WHEN SUSTAINED EFFECT IS DESIRED.

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