Formulation development and evaluation of <i>Silybum marianum</i> tablets

Cianchino, Valeria Andrea; Favier, Laura Silvina; Ortega, Claudia Alicia; Peralta, Cecilia; Cifuente, Diego Alberto

doi:10.1590/2175-7860202071044

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Pharmacognosy • Rodriguésia 71 • 2020 • https://doi.org/10.1590/2175-7860202071044 copy

Formulation development and evaluation of Silybum marianum tablets

Authorship SCIMAGO INSTITUTIONS RANKINGS

Abstract

In popular medicine Silybum marianum is used as a hepatoprotective agent. Silymarin is the major constituent. The present work deals with the formulation and evaluation of S. marianum tablets from ethanolic extract by direct compression. The ethanolic extract was obtained from seeds by soxhlet extraction. Two pharmaceutical formulations were prepared using fluid extract as an active principle, and Aeroperl^® 300 Pharma as a carrier. In order to improve flow ability and compressibility, co-processed excipients MicroceLac^® 100 and FlowLac^® 90 were employed. Pre-compression and post-compression parameters were evaluated according to USP 34-NF 29. Besides, silymarin was determined by NMR spectral data. Both formulations showed excellent rheological properties and the best biopharmaceutical parameters were observed in F2 (S. marianum ethanolic extract, aeroperl^® 300 Pharma, flowLac^® 90, glycolate starch and magnesium stearate) in terms of the friability (0.82 %) and the disintegration time (8.05 min).

Key words:
direct compression; ethanolic extract; herbal tablets; quality controls; Silybum marianum

Components	Formulations
Components	F1	F2
Silybum marianum ethanolic extract (mL/tablet)	26	26
Aeroperl® 300 Pharma (mg/tablet)	26	26
MicroceLac® 100 (mg/tablet)	74.1	-----
FlowLac® 90 (mg/tablet)	-----	74.1
Glycolate starch (mg/tablet)	2.6	2.6
Magnesium stearate (mg/tablet)	1.3	1.3

Properties	Formulations
Properties	F1	F2
Bulk density (g/cm³)	0.54 ± 0.003	0.59 ± 0.001
Tapped density (g/cm³)	0.62 ± 0.004	0.67 ± 0.013
Compressibility (%)	14.39 ± 0.54	12.05 ± 0.005
Hausner ratio	1.16 ± 0.005	1.14 ± 0.02
Angle of repose (θ)	10.23 ± 1.2	8.7 ± 0.45

Properties	Formulations
Properties	F1	F2
Weight variation (mg)	129.7 ± 1.05	134.2 ± 0.61
Friability (%)	0.92 ± 0.015	0.82 ± 0.03
Disintegration time (min)	19.4 ± 0.15	8.05 ± 0.03
Hardness (kg/cm²)	4.40 ± 0.11	3.70 ± 0.17

Formulation	Silymarin Nominal quantity (mg)	Silymarin Found (mg) ± SD
F1	50	49.16 ± 0.0059
F2	50	50.47 ± 0.0067
CT	150	150.30 ± 0.0031

Areas	Protons	Assignment
A (δ 6.80~7.20)	H-2', H-5', H-6'	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
B (δ 5.93~6.05)	H-6, H-8	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
C (δ 5.56~5.60)	H-7"	Silychristin (II).
D (δ 4.95~5.15)	H-2	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
D (δ 4.95~5.15)	H-7"	Silybin A and B (I), Isosilybin A and B (I).
E (δ 4.60~4.70)	H-3	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
F (δ 4.10~4.25)	H-8"	Silybin A and B (I), Isosilybin A and B (I).
G (δ 3.72~3.90)	OCH₃	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
G (δ 3.72~3.90)	H-9"	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
H (δ 3.40~3.70)	H-8"	Silychristin (II).
H (δ 3.40~3.70)	H-9"	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).

Areas	Carbons	Assignment
A (δ 114.05~122.03)	C-2', C-5', C-6'	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
B (δ 96.17~97.24)	C-6, C-8.	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
C (δ 88.67)	C-7"	Silychristin (II).
D₁ (δ 84.20)	C-2	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
D₂ (δ 77.35)	C-7"	Silybin A and B (I), Isosilybin A and B (I).
E (δ 73.25)	C-3	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
F (δ 79.73)	C-8"	Silybin A and B (I), Isosilybin A and B (I).
G (δ 55.58)	OCH3	Silybin A and B (I), Isosilybin A and B (I), Silychristin II).
H₁ (δ 56.48)	C-8"	Silychristin (II).
H₂ (δ 61.95)	C-9"	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
I (δ 101.62)	C-10	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).
J (δ 129.31~198.19)	C-9, C-5, C-7, C-4, C-1', C-3', C-4', C-1", C-3", C-4"	Silybin A and B (I), Isosilybin A and B (I), Silychristin (II).

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[1] ⁴ Author for correspondence: laurasil65@gmail.com