Biopharmaceutics and Pharmacokinetics

PHAR 460
Lab Manual

Fall 2021-2022
Preparation of Aspirin-Aerosil solid dispersion: Evaluation of the
effect of the water-insoluble carrier on the dissolution rate

The model drug, Aspirin:

- Aqueous solubility 1:300
- Acidic in nature (could be influenced by alkaline excipients  in situ salt
formation).
- Assayed by titration against NaOH using phenol red as an indicator (yellow-
red- persistent pink).

C9H8O4 + NaOH → NaC9H7O4 + H2O

Acid + base → salt + water

This is an acid-base reaction in which acetylsalicylic acid reacts with sodium

hydroxide to produce sodium acetylsalicylate and water.

Water-insoluble Carrier: e.g: aerosol

In this case, the drug is dissolved in a solvent that dissolves the drug but not the
carrier which is suspended in the drug solution.
Upon evaporation of the solvent, the drug will precipitate on the surface of
the carrier in a molecular (minuscular) state i.e. particle size reduction without
aggregation of the drug particles. This type of solid dispersion is known as a
surface solid dispersion.
Dissolution experiment:

- Weigh 600mg of Aspirin and mix with 4ml of alcohol

- Add 200mg of aerosil
- Evaporate the solvent and cool
- Weigh from the dispersion 400mg and dissolve in 100ml distilled water.
- For the control weigh 300mg of aspirin and add to 100ml distilled water.
- Take 5 ml sample and different time intervals (5,10,15,20,25) by
pipette using adaptor and cotton and replace with fresh 5 ml distilled water.
- Titrate against N/100 NaOH using phenol red (one or two drops) (yellow-
red pink persistent for 30 sec)

Calculations:

E.q  1.8 mg Aspirin ≡ 1ml NaOH N/100

𝑬. 𝒑 × 𝑬𝒒
𝒎𝒈 % 𝒐𝒇 𝒂𝒔𝒑𝒊𝒓𝒊𝒏 𝒅𝒊𝒔𝒔𝒐𝒍𝒗𝒆𝒅 𝒐𝒓 𝒓𝒆𝒍𝒆𝒂𝒔𝒆𝒅 = × 𝟏𝟎𝟎
𝟓

Sample tested Control

Time E.p mg% E.p mg%

10

15

20

25

Curve