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BIOAVALIABILITY

In pharmacology, bioavailability (BA or F ) is a subcategory of absorption and is the fraction of an


administered dose of unchanged drug that reaches the systemic circulation, one of the principal
pharmacokinetic properties of drugs. By definition, when a medication is administered intravenously, its
bioavailability is 100%.[1] However, when a medication is administered via other routes (such as orally),
its bioavailability generallyTH[›] decreases (due to incomplete absorption and first-pass metabolism) or
may vary from patient to patient. Bioavailability is one of the essential tools in pharmacokinetics, as
bioavailability must be considered when calculating dosages for non-intravenous routes of
administration.

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Definitions of rancid
adjective
(of foods containing fat or oil) smelling or tasting unpleasant as a result of being old and stale.
If you don't know what it's supposed to smell like, it might smell a little like rancid butter.
synonyms: sour, stale, overstored, turned, rank, putrid, foul, rotten, bad, off, gamy, high, fetid, stinking, m
alodorous, foul-smelling, noisome

Basically, dielectric constant or relative permittivity is, effectively, the comparative decrease in the force
between two charged species in a particular medium as compared to vacuum (where the medium is
defined as producing no interference in the interaction between the two species). For example, if the
force between two charged species is 1000 N in vacuum and that between them at exactly the same
distance in a particular medium is 100 N, the dielectric constant of that particular medium is 10. If the
force in another medium is 10 N, the new medium has a dielectric constant of 100. As you can see, the
higher the dielectric constant, the lower the force between the two charged species, everything else
held the same.

Now let us get to the process of dissolution. A substance would dissolve in a liquid (or gas for that
matter) if the components of the substance overcome the initial cohesive force (attraction) between the
components (can be ions or molecules) and disperse among the species of the liquid. In case of ionic
solids, which is what most salts are, this refers to disruption of the attractive force of the crystal lattice
(the structure formed from the positive ions and the negative ions) and release of the ions in the liquid
medium. This process is energetically favorable if the forces between the ions in the medium is low
enough (this comes from hydration or solvation energy of the ions) to overcome the lattice energy. And
as we saw earlier, higher the dielectric constant, lower the force between the the ions and in essence,
higher the solvation energy and more the degree of dissolution.
And water has a pretty high dielectric constant (refer to the table in the wikipedia article). 30n (or
hydration) energy for most ions and hence it is able to dissolve many salts.

This means it has a high solvatioThe energy of solvation is the amount of energy associated with
dissolving a solute in a solvent. If it is a positive number, the dissolving process is endothermic; if it is
negative, it's exothermic.

Solute molecules are held together by certain intermolecular forces (dipole-dipole, induced
dipole-induced dipole, ion-ion, etc.), as are molecules of solvent. In order for dissolution to
occur, these cohesive forces of like molecules must be broken and adhesive forces between
solute and solvent must be formed.

The solubility of a drug in a given solvent is largely a function of the polarity of the solvent.
Solvents may be considered polar, semi-polar or non-polar. Polar solvents will dissolve ionic
and other polar solutes (i.e. those with an asymmetric charge distribution [like dissolves like]),
whereas, non-polar solvents will dissolve non-polar molecules. Semi-polar solvents (eg.
alcohols and ketones) may induce a certain degree of polarity in non-polar molecules and may
thus act to improve the miscibility of polar and non-polar liquids. The relationship between
polarity and solubility may be used in practice to alter the solubility of a drug in a
pharmaceutical solution.

One approach is to alter the polarity of the solute by shifting it between its molecular
(undissociated) and ionic (dissociated) states. A shift toward the ionic form improves solubility
of the solute in water and other polar solvents. A shift toward the molecular species improves
solute solubility in non-polar solvents. Such shifts may be produced by altering the pH of the
solution (or using the salt form of the compound).

Another approach is to mix solvents of different polarities to form a solvent system of


optimum polarity to dissolve the solute. Such solvents must, obviously, be miscible. This
method is referred to as solvent blending or cosolvency and uses the dielectric constant as
a guide to developing the cosolvent system. Since many solvents may be toxic when ingested,
most solvent blends are limited to mixtures containing water, ethanol, glycerin, propylene
glycol, polyethylene glycol 400 or sorbitol solution. The list is somewhat expanded for solutions
for external application.

The dielectric constant (δ) of a compound is an index of its polarity. A series of solvents of
increasing polarity will show a similar increase in dielectric constant.

Dielectric
Compound
constant, δ, @
20°C
N-methylformamide 190

Water 80

Sorbitol Solution USP (70% w/w) 62

Syrup USP 56

Glycerol (glycerin) 46

Methanol 33

Propylene glycol 32.1

Ethanol 25

n-Propyl alcohol 22

Acetone 21

Polyethylene glycol 400 12.4

Chloroform 5

Castor oil 4.6

Ethyl ether 4.3

Sucrose 3.3

Olive oil 3.1

Sesame oil 3.1

Benzene 2.2

Carbon tetrachloride 2.2

Octane 1.9

Solvents may be classified according to their dielectric constants as polar (δ > 50), semi-polar
(δ = 20 - 50), or non-polar (δ = 1 - 20).
The value of the dielectric constant for a mixture is obtained by multiplying the volume fraction
of each solvent times its dielectric constant and summing.

There are many pharmaceutical substances which are non-polar or which are weak acids and
bases whose ionized salt forms are unstable in solution. In order to dispense solutions of these
substances, we must derive a solvent of appropriate polarity (or non-polarity).

Practically speaking, this is a fairly simple problem to solve. Solutions are prepared containing
varying concentrations of ethanol or acetone in water, ranging from 0 to 100%. The required
concentration of drug is added to each solution and the solutions are refrigerated overnight,
then viewed for precipitation.

% v/v
0 10 20 30 40 50 60 70 80 90 100
ETOH
Precipitation + + + + + + - - - - -

In our example, we see that at least 60% v/v ethanol is required to solubilize our drug. This
leaves us with a problem since, from a flavoring standpoint, 60% ethanol is not considered
pharmaceutically elegant. (Why?) We can now take this information and determine the
dielectric constant of the solvent system which provides drug solubility.

From this information it is possible to formulate a vehicle, substituting other solvents, which is
of the necessary polarity and is pharmaceutically elegant.

These calculated values of δ are only approximate. Interactions between multiple solutes and
solvents may increase or decrease solubility. Nonetheless, the use of the dielectric constant in
formulating solvent systems gives us a simple and scientific approach to estimating our needs.
It is, therefore, a useful tool.

e.g. Formulate a vehicle containing water, ethanol, and glycerin with a δ = 47. Limit ethanol to
20% by volume.

ydration energy (also hydration enthalpy) is the amount of energy released when one mole
of ions undergo hydration which is a special case of solvation. It is a special case
of dissolution energy, with the solvent being water.
For example, upon dissolving a salt in water, the outermost ions (those at the edge of the
lattice) move away from the lattice and become covered with the neighbouring water
molecules. If the hydration energy is equal to or greater than the lattice energy, then the salt
is water-soluble. In salts for which the hydration energy is higher than the lattice energy,
solvation occurs with a release of energy in the form of heat. For instance, CaCl2 (anhydrous
calcium chloride) heats the water when dissolving. However, the hexahydrate, CaCl2·6H2O
cools the water upon dissolution. The latter happens because the hydration energy does not
completely over come the lattice energy, and the remainder has to be taken from the water in
order to compensate the energy loss.

See also

Thus, the vehicle is 20% v/v ethanol, 15% v/v water, and 65% v/v glycerin.

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