Formulation Considerations

Chapter 4: Pharmaceutical and Formulation Considerations *missing data moved to Physical Pharmacy topics
Pharmaceutical EXCIPIENTS and INGREDIENTS
Stabilizers	Prevent decomposition Ex: chelating and antioxidants
Diluents or Fillers	Increase bulk
Binder	Adhesion  of powdered drug and other substance
Antiadherent or Lubricants	Assist smooth tablet formation
Disintegrating agent	Promote breakup after administration
	#refer to the HANDBOOK OF PHARMACEUTICAL EXCIPIENTS
Clarifying agent	Bentonite :Filtering aid
Humectant	Glycerin; P.G; Prevent drying of preparation ex: Ointment, creams
Enteric Coating	Cellulose acetate phthalate Shellac (35% alcohol, px glaze)
LMW salt	Salty taste
HMW salt	Bitter
Increase of –OH hydroxyl groups	Increase sweetness
Stevia powder Stevia rebaudiana bertoni	Natural 30x sweeter sucrose, cane
Colors
ANILINE dyes Aka SYNTHETIC ORGANIC DYES COAL TAR DYES	90% dyes derived  this colorless derivative of BENZENE; bituminous coal
FD&C	Food, drug, cosmetic
D&C	Drug cosmetic, medical devices
External D&C	Only on external use; excluding lips or in mucous membrane
POPULAR COLORINGS	0.0 0 0 5% to 0. 0 0 1 %
FD&C RED no. 2	Amaranth Withdrawn, unknown safety
FD&C Red no. 4	Maraschino Cherries Withdrawn Now used only externally
FD&C Yellow no. 5	TARTRAZINE “cause allergic reaction in many people” Must be listed in labels
Lake pigments FD&C Lake	Pigment consisting of substratum of ALUMINA HYDRATE on which the dye is precipitated or adsorbed *for low moisture prep
PRESERVATIVES
Sterilization of ophthalmic, injectables	Autoclaving 20 min 15 lb pressure 121 C Dry heat 180 C 1 hour Bacterial filtration
Generally 15% V/V ALCOHOL in Acid media 18 % V/V ALCOHOL in Alkaline media	Inhibit microbial growth
PROBABLE MODES OF ACTIONS OF PRESERVATIVES
Benzoic Acid Boric Acid p-hydroxybenzoate	Denaturation of Proteins
Phenols Chlorinated Phenolic cmpds	Lytic and denaturation on cytoplasmic membranes nad for chlorinated preservatives Oxidation of enzymes
Alcohols	Lytic action on membranes
Mercurials	Denaturation of enzymes by combining with  -SH group (thiol)
Propylparaben	Good against Fungi