PHA 6114C Drug Excipients and Solid Dosage Form Tech (Lecture 17)

Excipients

inactive pharmaceutical ingredients

Unshaped

are powders an example of a shaped or unshaped dosage form?

Tablet

what is the most common dosage form with 63% of the top 100 best selling drugs being represented in this category?

Manufacturing, Reproducible Release, and Desired Rate

excipients are used because they improve ________

Handbook of Pharmaceutical Excipients

collects essential data on the physical properties of excipients and organizes it into an easy-to-use format for drug safety and potential drug toxicity

Manufacturing

excipients in the granule such as diluents, binders, and disintegrants would be important in which process?

Disintegration

excipients mixed after granulation such as anti-adherents, die wall lubricants, and surfactants are important for which process?

Lactose

a popular excipient used in many solid dosage forms such as tablets and capsules

Spray Dried and Anhydrous Lactose

what are the two important forms of lactose?

Amorphous

does amorphous or crystalline lactose have better compression?

Plastic

the amorphous form of lactose is ________ in nature

Cyclodextrins

cyclic oligomers of glucose that can form water-soluble inclusion complexes with small molecules and portions of large compounds

Low Toxicity, Water-Soluble, and Biocompatible

advantages of using cyclodextrins for delivery of hydrophobic drugs

Cholesterol

a disadvantage of using cyclodextrins is their high affinity for _________

Kidney

cyclodextrins will precipitate in the _________ because of their poor solubility, making parenteral use impossible

True

T/F: milling will convert crystalline lactose to amorphous lactose

Co-Processed Excipients

a combination of two or more pharmaceutical substances that are physically mixed without a significant chemical change

Prosolv Easytab

an all-in-one, ready-to-use, high functionality excipient that combines binder/filler, glidant, superdisintegrant, and lubricant for rapid formulation development and convenient tablet manufacturing

Eudragit Polymers

diverse range of polymethacrylate-based copolymers that are colon-specific/enteric-coated/sustained release drug delivery and tablet masking functionalities

True

T/F: each step in the manufacturing process is an individual activity and is individually optimized to produce consistent material

Crystallization

particle size, shape, and distribution is controlled by ____________

Diffusion Mixers

commonly used in pharmaceutical industry and include V-blenders, double cone blenders, bin blenders, and drum blenders

Convection Blenders

mechanical mixing machines such as ribbon blenders, screw blenders, planetary blenders, and high-intensity blenders

Granulation

the process of particle agglomeration and size of powdered ingredients to achieve desirable processing properties such as improved flow or compression

Drying

process that removes excess water or other granulation liquids and reduces moisture content to acceptable level

Dry Heating

direct contact between wet mass and heated air such as a tray placed in the oven

Fluidized Bed Drying

physically move the moist granulation with heating to cause evaporation and used in industrial large scale applications

Lubrication

the last step before tablet compression or capsule filling and moistens or reduces friction

Film Wrapper

sealed around the product and/or product container

Blister/Strip Pack

individually sealed dose units and removal requires tearing or breaking individual compartment

Bubble Pack

product and container sealed in plastic, usually mounted on display card, and plastic must be cut or broken open to remove the pack

Shrink Seal, Band

band or wrapper shrunk by heat or drying to conform to the cap, and must be torn to open package

Foil, Paper, and Plastic Pouch

sealed individual packet must be torn to reach product

Bottle Seal

paper or foil sealed to mouth of container under cap and must be torn to reach the product

Tape Seal

paper or foil sealed over carton flap or bottle cap and must be torn or broken to remove

Hydrolysis

esters, amides, and lactones are degraded by _________

Oxidation

aldehydes, alcohols, phenols, alkaloids, unsaturated fats, and oils are degraded by _____________

Isomerization

conversion of a chemical into its optical or geometric isomer

Photolysis

oxidation-reduction, ring alterations, and polymerization ca be catalyzed or accelerated by exposure to light; leads to discoloration and chemical transformation

Polymerization

intermolecular reactions lead to dimeric or higher weight species