Acetaminophen (APAP) formulation by direct compression
Formulation Guideline

Acetaminophen (APAP) formulation by direct compression

Acetaminophen formulation demonstrating the excellent properties of MICROCEL® microcrystalline as directly compressible excipient for swallowable tablets

Objective

Acetaminophen formulation by direct compression based on different grades of microcrystalline cellulose (MCC)

Formula

Ingredient

Functionality of the ingredient

mg/tablet
(total weight: 250mg)

% by weight

Acetaminophen granulated

Active Pharmaceutical Ingredient

100

40

MICROCEL® 102 SD

MICROCEL® 200 SD

MICROCEL® MC-102

MICROCEL® MC-200

Direct compression filler-binder

Disintegrant

148.75

59.5

Magnesium stearate

Lubricant

1.25

0.5

Method

1. In a mixer, mix the ingredients MCC and acetaminophen for 5 minutes.
2. Add the magnesium stearate and mix for 3 minutes more.
3. Tablets made using 11.28 mm diameter (1 cm²) round, flat-faced TSM-D tooling with a target weight of 250 mg. 
4. Tablets were made under 15 kN using a Styl’One Evolution (Medel’Pharm, Beynost, France) at medium compression speed simulating Korsch XL-400 rotary compressor (35 rpm = 1015 tab/min).
5. Immediately after compression, tablets were weighted, the thickness, diameter and tablet breaking force were measured by hardness tester (MultiTest 50, SOTAX Corp., Westborough, MA, US). 
6. Dissolution profile was evaluated.

Additional comments

All grades (MICROCEL® 102 SD, MICROCEL® 200 SD, MICROCEL® MC-102 and MICROCEL® MC-200) prove to lead to tablets with good physical properties and 80% APAP dissolution within 30 minutes as per USP.

 

APAP 250mg tablets (Compression Force:15 kN)

Weight (mg)

Hardness (N)

Porosity (%)

MICROCEL® 102 SD

241.2

79.0

16.0

MICROCEL® MC-102

253.9

65.2

17.9

MICROCEL® 200 SD

256.8

70.8

16.2

MICROCEL® MC-200

233.3

69.6

18.7

Tablets passed the friability test based on USP criteria.

APAP released percentage during dissolution study:

Comment on Roquette product benefits

- MCC has many functionalities: filler, binder, filler/binder, disintegrant.
- MICROCEL® 102 SD, MICROCEL® 200 SD, MICROCEL® MC-102 and MICROCEL® MC-200 are excellent fillers/binders and disintegrants for direct compression with a high API dilution potential (up to 40% for APAP).

 

® Registered trademark(s) of Roquette Frères. MICROCEL® is a registered trademark in Benelux, Brazil, Canada, Chile, France, Germany, Italy, Mexico, the United Kingdom, and the United States of America and is pending in other countries or regions.

Disclaimer

This formula is a guideline for recommended use of our products; it does not imply consent to their use in violation of existing patent(s). 

These details are for information only, and we believe them to be reliable.

 

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