Use 5 Data tables and 3 figures provided.

Acetaminophen is well known pain reliver (it is an active ingredient in brand such as Tylenol).

Active drug is processed to make a D.C. grade and a coated grade of materials. 525 mg of D.C. material has 500 mg Active (formulation I and II); and 566 mg of Coated material has 500 mg of active (formulation III and IV).  This relates to 700 mg total weight of tablet. These two materials are used to develop formulation.

The properties are compared to crystalline powder, see the following Data.

Ingredients	Mean particle sizeμ	Bulk density (g/ml)	Tapped Density g/ml		Angle of repose
Acetaminophen Crystal	>355	0.382		0.259	Not done
Acetaminophen D.C.	>45	0.679		0.530	41.63
Acetaminophen coated	>250	0.469		0.417	39.52

The following Formulations compositions, % W/W, are studied.  Brand names of some excipients are also listed. Please do own research about these ingredients and other info.

Ingredients	Formulation I %w/w	Formulation II% w/w	Formulation III %w/w	Formulation IV %w/w
Acetaminophen D.C.	75	75	-	-
Acetaminophen coated	-	-	80.85	80.85
vinylpyrrolidone-vinyl acetate copolymers, Kolidon VA 64	4	4	2	2
Croscarmellose Sodium Vivasol©	-	5	-	5
crospovidone        Polyplasdone® XL-10	4	-	4	-
Microcrystalline Cellulose       Avicel PH 200	12.5	11.5	8.64	7.64
hydroxypropyl cellulose        Klucel EXF	2	2	2	2
PEG 4000	1	1	1	1
Mg-stearate	1	1	1	1
Fumed silica                        Aerosil 200	0.5	0.5	0.5	0.5

% W/W                   Total	100.0 %	100.0 %	100.0 %	100.0 %
Weight of Tablet     mg	700	700	700	700
Weight of material containing API:       mg	525	525	566	566
Acetaminophen Dose Potency                    mg	500	500	500	500

Question:  Please answer those questions from the data!!!

1. Write manufacturing procedure(s) in sufficient detail (not one liner) for 100 kg batch. Score 3
2. Provide equipment used in the process, explain equipment capacity, describe operating conditions, including size of tablet for 500 mg dose.  Score 3
3. Show (Draw) the Compaction profiles, i.e., Pressure vs Time for formulation during the pressing of powder for formulation of ONE formulation you concluded is the best. (If you give two or more formulations, then you will get 0) for entire test). 

Explain why did you the formulation is the best? Include several tables with analysis of data (tables and graphs) in your answers (Score 0 for only words).  Score 6

Final Powder mix	Mean particle size μ	Bulk density (g/ml)	Tapped Density g/mL
I:      Acetaminophen D.C.+Polyplasdone XL-10	>45	0.479	0.388
II:   Acetaminophen D.C.+Vivasol	>45	0.483	0.393
III:    Acetaminophen coated+Polyplasdone XL-10	>250	0.609	0.513
III:   Acetaminophen coated+Vivasol	>250	0.608	0.507

Tablet Physical Properties:

Tablet	Weight (g)	Porosity (%)	Hardness (N)	Friability (%)
Formula I	0.709±1.84	15.45	153.19	0.52
Formula II	0.705±0.43	59.43	150.46	0.51
Formula III	0.702±0.03	59.23	71.99	0.24
Formula IV	0.702±0.52	59.42	65.3	0.24
Brand as Reference	0.604±0.10	Not done	61.3	0.91

Data:  Dissolution at pH 1, 4.5 and 5.8    Formulations:  I, II, III and IV.

pH 1.2

pH; 4.5

 

pH 5.8

  
 

Transcribed Image Text:

110 100 90 80 70 60 50 40 30 20 10 5 10 15 Time [min] 20 25 30 35 Reference tbl ID.C+ Polyplasdone XL-10 PAR li. D.C. + Vivasol III coated Polyplasdone XL-10 IV coated + Vivasol 110 100 90 80 70 60 50 40 30 20 10 5 10 15 Time [min] 20 25 30 35 Reference tbl ID.C+ Polyplasdone XL-10 PAR li. D.C. + Vivasol III coated Polyplasdone XL-10 IV coated + Vivasol