Biopharmaceutical Ingredients and Excipients

Definition and Types

Solvents used to dissolve the drug substances

Flavors & sweeteners used to make the product more palatable

Colorants added to enhance appeal

Preservatives prevent microbial growth

Stabilizers (ex. Antioxtidants & chelating agents) prevent decomposition

Diluents/fillers increase bulk

Binders cause adhersion of the powdered drug & pharmaceutical substances

Antiadherents/lubricants smooth tablet formation

Disintegrating agents promote tablet break up after administration

Coatings improve stability, control disintegration, or enchance appearance

Ointments and creams & suppositories acquire characteristic features from their pharmaceutical bases

All drug products should be labaled to state the indentity of all added substances (excipients)

In alphabetical order by name & be distinguished from the identification statement of active ing.

The name should be taken from the current ed. Of the ff:

A. USP/NF

B. USAN & USP Dictionary of Drug names

C. CTFA Cosmetic Ingridient Dictionary

D. Food chemical codes

If not listed, common/usual name/chemical name should be identified

If an ing. may or may not be present, it should be qualified by words: or may also contain

If ing. is trade secret, it may be omitted and words: and other ingredients must be used.

Ingredients only present in trace amount or has no functional effect on the drug may not be listed

Handbook of Pharmaceutical Excipients

Presents monographs on more than 300 excipients used in dosage form prep.

Include: non-proprietary, chemical, and commercial names; empirical and chem. formulas and MW.; pharmaceutical specifications and chem. & physical propertiesetc

Appearance and Palatability

Electronic tongue used to aid in providing a global taste fingerprint during formulation development. It provides info. on bitterness levels and stability of flavors in terms of taste.

Flavoring Pharmaceuticals

Primarily applies to liquids intented for oral administration.

10 000 taste buds; each have 30-60 receptor cells

Receptor cells interact with molecules dissolved in the saliva and produce a positive or negative taste sensation

Addition of flavouring agents masks the disagreeable taste

Color must have psychogenic balance with taste

Low molecular salts salty (chlorides of Na, K, Ammonium/ NaBr)

High molecular salts bitter (KI, MgSO4 epsom salt)

Increase # of hydroxyl groups (-OH) Increase sweetness (ex. Sucrose- 8 OH; Glycerin 3 OH groups)

Organic esters, alcohols and aldehydes are pleasant to taste

Nitrogen-containing compounds (Alkaloids) bitter

Nitrogen-containing compounds (aspartame) sweet

D-glucose sweet

L-glucose-slightly salty taste

Saccharin-sweet

N-methylsaccharin tasteless

Cocoa-flavored vehicles considered most effective for masking bitter taste

Fruit/citrus flavors combat sour or acid-tasting drugs

Cinnamon, orange, raspberry salty

Age of the intended ptx is also considered:

Children prefer sweet

Adults prefer less sweet (ex. Tart)

Flavors can consist of:

a. Oil soluble liquids soybeans & other edible oils

b. Water soluble carrier water, ethanol, propylene, glycol , glycerine, emulsifiers

c. Dry carriers maldodextrins, corn syrup solids, modified starches, gum Arabic, salt, sugars, whey protein.

Flavoring agents maybe derived from

a. Natural resources 1%-2%

b. Artificial 0.1% - 0.2%

Sweetening Pharmaceuticals

-Acesulfame potassium 200x

-Aspartame- 180-200x

- Sucralose 600x

-Saccharin 300x

Coloring Pharmaceuticals

Used in pharmaceutical prep for esthetics.

Synthetic coloring agents first prepared in the middle of 19th century from principles of coal tar.

Coal tar (pix carbonis) a thick, black, viscid liquid, a by-product of the destructive distillation of coal.

Products: anthracene, benzene, naphtha, creosote, phenol, pitch

90% of the dyes used in products FDA regulates are synthesized from a single colorless derivative of benzene: ANILINE (obtained from bituminous coal) come mainly from petroleum

Certified color additives are classified according to their approved use:

a. FD&C color additives

b. D&C color additives

c. External D&C

Current list of certified color additives are found at: 21CFR74

Amount of colorant generally added to liquid preparations ranges from 0.0005% - 0.001%

Lake pigments commonly used in the form of fine dispersions or suspensions. Pigment particles range from 1um 30um

FD&C lake a pigment consisting of a substratum of alumina hydrate on which the dye Is absorbed or precipitated.