UNIT 2 (Pharmaceutics I) PDF
UNIT 2 (Pharmaceutics I) PDF
UNIT 2 (Pharmaceutics I) PDF
2.Trituration
3.Geometric dilution
i) Imperial System:
Is the oldest system of weight and measures.
It involves the measures of weight i.e. mass.
It is further classified as Avoirdupois System and Apothecaries
System.
a. Avoirdupois system
In this system “pound” (Lb) is the standard unit for weight (mass).
Used to measure weight in day-to-day life.
Used in pharmaceutical measurement of bulk quantity at the time
of buying or selling of pharmaceutical product.
Eg.
1 lb =l6 (oz) ounce
1 lb = 7000 grains
1 oz. = 7000 /16 grains = 437.5 grains
b. Apothecaries system
.
ISOTONIC SOLUTIONS
The methods of calculating isotonicity of are :
Microcrystallince cellulose
Viscosifying agent
Humectants Prevent the evaporation of liquid Propylene glycols, Glycerol,
from the preapration Polyethylene glycol.
Chelating agents It forms complexes with metal ions Disodium EDTA, Dihydroxy ethyl
and prevent drug from the glycine, Citric acid and Tartaric acid.
oxidative reaction
Emulsifying agents Reduce interfacial tension and Sodium Lauryl Sulphate, Cetrimide,
prevent coalescence of the Macrogol esters, Sorbitan esters.
dispersed globules
Flocculating It act by preventing cake formation Starch, Sodium alginate, Carbomer.
in suspension and the sediments
agents
are loosely packed which are easily
redispersed.
Sweetening Impart sweetness and mask the Sucrose, Sorbitol, Saccharin,
bitter taste of the oral liquid Aspartame,
agents
preparations Sucralase.
Colors Impart color to the liquid orals Amaranth, Erythrosin, Eosin,
Tartarazine.
Flavors Impart flavors to the liquid orals Aromatic waters, Syrup.
Solubility Enhancement Technique
A. Physical modification
1) Eutectic mixture:
When the eutectic mixtue is exposed to water the soluble
carrier dissolves leaving the drug in a microcrystalline state
which solubilize rapidly.
e.g: Mixture of paracetamol and urea.
2. Size Reduction:*
B. Chemical modification
3.Salt formation:
Salts have improved solubility in comparison to the original
drug.
e.g: Alkali metal salts of acidic drugs like penicillin and strong
acid salt of basic drugs like atropin are water soluble than
parent drugs.
Eg. Increase of Diclofenac by making its salt form i.e. Diclofenac Sodium
2. Particle Size Reduction:*
Size reduction increase the surface area of the drug particles
which increase the solubility.
Size reduction can be achieved by
a. Micronization & b. Nanosuspension
a.Micronization :
• The solid drug particles size between 1 to 10 microns by micro-
milling
• Micronization of drugs is done by milling techniques using jet
mill, rotor stator colloid mills etc.
• Micronization is not suitable for drugs having a high dose
number because it does not change the saturation solubility of
the drug .
2. Particle Size Reduction:*
b. Nanosuspension :
•Nanosuspensions are sub-micron colloidal dispersion of pure
particles of the drug, which are stabilized by surfactants.
• Nanosuspension technology is used for efficient delivery of
hydrophobic drugs .
•The particle size distribution of the solid particles in nano-
suspensions is usually less than one micron with an average
particle size ranging between 200 and 600 nm.
•Advantage : Increased dissolution rate due to larger surface area
exposed.
•Eg., Nanosuspension approach has been employed drugs like
paclitaxel, tarazepide, amphotericin B which are still on research
stage.
4.Change of pH:
This can be achieved in two ways
a) In situ salt formation
b) Addition of buffers to formulation.
e.g: Buffered aspirin tablet.
5. Complexation:
The beta and gamma cyclodextrin having ability
to form molecular inclusion complexes with
hydrophilic drug having poor aqueous solubility.
Cyclodextrin are versatile in having hydrophobic
cavity of suitable enough to accomodate the
lipophilic relatively hydrophilic ---- improved
aqueous solubility
e.g: Barbiturates, Benzodiazepines.
C. Miscellaneous methods
6. Use of surfactant: Surfactant reduced the interfecial tension.
Enhance solubility by promoting wetting and penetration of
dissolution fluid into the solid drug particles.
e.g: Spironolactone(steroids)--- increased solubility by using
surfactant(non ionic polysorbates).
7.Co-solvency : Co-solvents are prepared by mixing miscible or
partially miscible solvents. Weak electrolytes and non-polar
molecules have poor water solubility and it can be improved by
altering polarity of the solvent. The addition of an organic cosolvent
to water can dramatically change the solubility of drugs. Cosolvent
system works by reducing the interfacial tension between the aqueous
solution and hydrophobic solute. Aqueous solvent - Ethanol, sorbitol,
glycerin, propylene glycol. Non aqueous solvent - glycerol dimethyl
ketal, glycerol formal, glycofurol, dimethyl acetamide.
SOME PERANTRALPRODUCT THAT CONTAIN COSOLVENT
1.Diazepam - 10% ethanol + propylene glycol
2.Digoxin - 10% ethanol + propylene glycol