Selected Calculations Associated

19
with Plant Extractives
Objectives
Upon successful completion of this chapter, the student will be able to:

• Differentiate between extracts, fluidextracts, and tinctures on the basis of active drug content.
• Perform calculations related to the concentration and dose of extracted botanicals.
• Perform calculations related to the concentration and dose of botanic dietary supplements.

Currently, the consuming public has renewed interest in the use of botanicals and dietary supple-
ments. These products are widely available to consumers, and a variety of governmental agencies
are trying to ensure their safety by setting appropriate quality standards.1 The United States
Pharmacopeia—National Formulary (USP/NF) includes official monographs, general tests, assays,
and manufacturing practices for a number of botanicals and dietary supplements.2 Included
among the official monographs for botanicals are those for echinacea, feverfew, garlic, ginkgo,
ginseng, goldenseal, hawthorn, Saint John’s wort, saw palmetto, and valerian. Dosage forms may
be prepared from the dried and pulverized plant parts (e.g., leaves) containing the desired
components.
Other pharmaceutical preparations are made by the process of extraction—that is, by remov-
ing desired constituents from plant materials through the use of select solvents. The plant materi-
als (termed crude drugs) include seeds, leaves, bark, or other plant parts that contain known or
suspected active therapeutic ingredients (ATIs) or active ingredients (AIs), including alkaloids,
glycosides, or other pharmacologically active complex organic molecules.
Two major processes are used for the extraction of active constituents from plant materials,
namely maceration and percolation.
The term maceration comes from the Latin macerare, meaning ‘‘to soak.’’ By this process,
comminuted crude drug is placed in a suitable vessel and allowed to soak in a solvent or mixture
of solvents (termed the menstruum) for a sufficient period to soften the botanic material and
effect the extraction of the soluble constituents. The menstruum selected is based on the solubility
characteristics of the desired constituents. Hydroalcoholic mixtures commonly are employed.
The dissolved constituents are separated from the exhausted crude drug (termed the marc) by
straining or filtration.
The term percolation is derived from the Latin per, meaning ‘‘through,’’ and colare, meaning
‘‘to strain.’’ By this process, comminuted crude drug is extracted of its soluble constituents by
the slow passage of a menstruum through a column of the botanic material. The crude drug is
carefully packed in an extraction apparatus (termed a percolator) and allowed to macerate for
a prescribed period of time prior to percolation. Percolators are of various sizes and construction.
Small-glass percolators, cone- or cylindrical-shaped, several inches in diameter, and about 12

319
320 PHARMACEUTICAL CALCULATIONS

inches in height, are available for laboratory use. In contrast, large stainless-steel percolators for
industrial use may be six to eight feet in diameter and 12 to 18 feet in height. An orifice at the
bottom of a percolator permits the convenient removal of the extractive (termed the percolate).
By maceration or percolation, therapeutically active as well as inactive constituents (e.g.,
sugars) that are soluble in the menstruum are extracted. Thus, an extractive is a mixture of plant
constituents.
The primary dosage forms of plant extractives are extracts, fluidextracts, and tinctures. Fre-
quently, however, the active therapeutic ingredient(s) are separated from plant extractives by
physicochemical methods and then chemically identified, purified, and used as single therapeutic
agents in various dosage forms (e.g., tablets, capsules, elixirs, syrups). In some instances, synthetic
replicas of the ATIs, or chemical congeners of them, are prepared and used in pharmaceutical
products rather than the naturally occurring therapeutic agents.

Extracts, Fluidextracts, and Tinctures

Extracts are concentrated preparations of vegetable (or animal) drugs. Most extracts are prepared
by percolation followed by the evaporation of all or nearly all the menstruum, yielding a pow-
dered or ointment-like product of extracted drug in concentrated form. On a weight-for-weight
basis, extracts commonly are two to six times as potent as the crude drug. In other words, 1
gram of extract may be equivalent in active constituents to 2 to 6 grams of the crude drug. Thus,
an extract may be described as a ‘‘2’’ (or other multiple) or as a ‘‘200%’’ (or other %) extract.
Among the extracts in the USP/NF are: Belladonna Extract, Cascara Sagrada Extract, Powdered
Echinacea pallida Extract, Powdered Ginkgo Extract, and Powdered Asian Ginseng Extract.3
Fluidextracts are liquid extractives of plant materials adjusted for drug content so that each
milliliter of fluidextract is equivalent in constituents to 1 gram of the crude drug that it represents.
Among the fluidextracts in the USP/NF are: Cascara Sagrada Fluidextract, Garlic Fluidextract,
Licorice Fluidextract, and Senna Fluidextract.3
Tinctures are alcoholic or hydroalcoholic solutions prepared from plant materials. (Tinctures
also may be prepared from chemical substances [e.g., iodine tincture].) Among the botanical
tinctures in the USP/NF are: Belladonna Tincture, Compound Cardamom Tincture, Opium Tincture,
Sweet Orange Peel Tincture, and Tolu Balsam Tincture.3 Although there is no set strength for
tinctures, those prepared from plant materials traditionally have used the following quantities
of crude drug in the preparation of each 100 mL of tincture:

Potent drug (e.g., belladonna leaf) 10 g crude drug

Nonpotent drug (e.g., tolu balsam) 20 g crude drug
Fruit/Flavor (e.g., sweet orange peel) 50 g crude drug

The relative strengths of extracts, fluidextracts, and tinctures are depicted in Figure 19.1, which
shows an example of the quantity of each that may be prepared from a quantity of crude drug.
In terms of equivalency:

1g 1 mL  0.25 g  10 mL
crude drug fluidextract ‘‘400%’’ extract ‘‘potent’’ tincture

Examples of calculations pertaining to plant extractives are as follows.

Example Calculations of Extracted Botanicals

If 1 mg of active ingredient (AI) is present in each gram of a crude drug, determine the concentration, in
mg/g or mg/mL, of AI in the corresponding (a) fluidextract, (b) ‘‘400%’’ extract, and (c) potent tincture.
 CHAPTER 19 • SELECTED CALCULATIONS ASSOCIATED WITH PLANT EXTRACTIVES 321

100 g
CRUDE
DRUG

OR OR

1000 mL Tincture 100 mL Fluidextract 25 g Extract

FIGURE 19.1 Depiction of the relative concentrations of a potent tincture, a fluidextract, and an extract using as
the example a ‘‘10%’’ tincture and a ‘‘400%’’ extract (see text for further explanation).

(a) Since, by definition, 1 mL of fluidextract is equivalent in active ingredient to 1 g of crude

drug, 1 mg of active ingredient would be present in 1 mL of fluidextract.
1 mg AI/mL, answer.
(b) A ‘‘400%’’ extract represents, in each gram, 4 g of crude drug. Thus:
1 g crude drug 1 mg AI
 ; x  4 mg AI/g crude drug, answer.
4 g crude drug x mg AI
(c) Since a ‘‘potent tincture’’ represents in each 100 mL, the AI from 10 g of crude drug, 0.1
g of crude drug would be needed to prepare 1 mL of tincture. Thus:
1 g crude drug 1 mg AI
 ; x  0.1 mg AI/mL tincture, answer.
0.1 g crude drug x mg AI
If the dose of belladonna tincture is 0.6 mL, determine the equivalent corresponding dose of (a)
belladonna leaf, (b) belladonna fluidextract, and (c) an extract (200%) of belladonna.
(a) Since a potent tincture contains in each 100 mL, the AI from 10 g of crude drug is:
100 mL tr. 10 g crude drug
 ; x  0.06 g, answer.
0.6 mL tr. x g crude drug
(b) Since 1 mL of fluidextract contains the AI from 1 g of crude drug:
1 g crude drug 1 mL fluidextract
 ; x  0.06 mL fluidextract, answer.
0.06 g crude drug x mL fluidextract
Or, since a fluidextract is 10 times as concentrated as a potent tincture, its dose would be
1
⁄10 that of a corresponding tincture:
1
⁄10 of 0.6 mL  0.06 mL, answer.
322 PHARMACEUTICAL CALCULATIONS

(c) Since a ‘‘400%’’ extract has four times the AI content as the crude drug, and since the
dose of the crude drug as calculated above is 0.06 g, the dose of the extract would be
1
⁄4 of that dose:
0.06 g  1⁄4  0.015 g or 15 mg, answer.

CASE IN POINT 19.1: An industrial pharmacist is charged with preparing a ‘‘400%’’

extract of cascara sagrada from 100 kg of crude drug.
(a) How many kilograms of the extract would be expected to be prepared?
(b) If the crude drug is assayed to contain 11% hydroxyanthracenes, what would
be the expected percentage strength of the resultant extract?

Botanic Dietary Supplements

The official monographs (USP/NF) for botanic dietary supplements include quality standards
for the content of their active constituents including, for example2:
Asian ginseng NLT 0.2% ginsenoside Rg1
NLT 0.1% ginsenoside Rb1
American ginseng NLT 4% ginsenosides
Black cohosh NLT 0.4% triterpene glycosides
Echinacea pallida NLT 0.5% phenols (caftaric acid, chicoric
acid, chlorogenic acid, and echinacoside)
Eleuthero NLT 0.8% eleutheroside and eleutheroside E
Ginkgo NLT 0.1% terpene lactones
Garlic NLT 0.5% alliin
Goldenseal NLT 2% hydrastine
NLT 2.5% berberine
Red clover NLT 0.5% isoflavones
Saint John’s wort NLT 0.3% hypericin extract
Valerian NLT 0.8% valeric acid

The following are examples of calculations applicable to botanic dietary supplements.

Example Calculations of Botanic Supplements

A batch of garlic is determined to contain 10 mg of allicin in a 4-g sample. How many micrograms
of allicin would be present in a 500-mg dose of garlic from this batch?
10 mg  10,000 ␮g
500 mg  0.5 g
4g 10,000 ␮g
 ; x  1250 ␮g, answer.
0.5 g x ␮g
The herb feverfew, when standardized as a powdered leaf, contains 0.2 percent of the agent partheno-
lide. How many milligrams of parthenolide would be present in a capsule containing 125 mg of powdered
feverfew?
125 mg  0.2%  0.25 mg, answer.