Optimization of extraction of Silybum marianum fruits, presentation of three formulations of its active chemicals and designing a dissolution test method for silymarin tablet

Authors

Abstract

The milk thistle of commerce is a standardized preparation extracted from fruits of Silybum marianum, a plant native to the Mediterranean.
Silybum marianum extraction has been shown to be amazingly effective at protecting and repairing liver cells.
We studied quality of Silymarin distribution in Silybum marianum fruits and methods of increasing out put of extracting. We formulated the extract as oral drops and tablets.
Also inspite of absence of dissolution test in pharmacopea, we did it in order to compare tablet dosage form with standard preparation. (Legalon)
In order to study quality of Silymarin distribution in Silybum marianum fruits; Silymarin was isolated with preliminary de-fatting then was extracted with methanol and its content measured according to DAB10 method for assay. Since a large part of the oil present in pulp, was removed by separating husk from fruit mechanically in an invented method, using pressure, oven, blowing and milling. Then content of Silymarin in husk measured as DAB10 method.
Silymarin drops was fromulated with ethanol 40 in proportion of 1:5 and compared with standard fromulation, marindistel, for PH, density, dry residual and content of Silymarin. For tablet fromulation the extract was concentrated and used in silymarin tablet 35 mg, also silymarin tablet 70 mg was formulated using silymarin powder 80% from Nova-Linnea SA Company-Switzerland.
These products were compared with Legalon tablets for content of silymarin and dissolved percents.
A dissolution method was designed using apparatus II usp, medium consisted of 0.5% sodium lauryal sulfate, 900 ml, 100 rpm, 60 minute.
Results
1.Silymarin distribution:
Silymarin in fruits without de-fatting: 1.56%
Silymarin in defeated fruits: 2.2%
Silymarin in husk: 3.5%
Silymarin in pulp: 0.85%
2. Drops fromulation
PH Density Alcohol
Degree Dry
Residual Assay
Silymarin 5.7 0.94 41 2.4 g/100 ml 2.5 mg/ml
Marindistel 5.7 0.94 41 14 g/100 ml 2.2 mg/ml
3. Tablet fromulation
% dissolved Assay
Silymarin 35 100% 35 mg
Silymarin 70 97% 70 mg
Legalon 70 80% 70 mg
Extraction from the husk of silybum marianum fruits instead of the whole fruits is easier than previously known methods and increases out put.
This research showed that our fromulations are comparabale with standard fromulations according to dissolution profile in tablets and other criteria in another product.

Iranian Journal of Pharmaceutical Research (2004): Supplement 2

Iranian Journal of Pharmaceutical Research (2004): Supplement 2: 47-47
Poster Presentations
/Ethnopharmacy

2nd International Congress on Traditional Medicine and Materia Medica
October 4-7, 2004, Tehran, Iran

136

Optimization of extraction of Silybum marianum fruits, presentation of three formulations of its active chemicals and designing a dissolution test method for silymarin tablet

Khalilian A., Saffary N., Rahmani N., Eskandary S.

R&D department, Amin Pharmaceutical Company, Isfahan, Iran

The milk thistle of commerce is a standardized preparation extracted from fruits of Silybum marianum, a plant native to the Mediterranean.

Silybum marianum extraction has been shown to be amazingly effective at protecting and repairing liver cells.

We studied quality of Silymarin distribution in Silybum marianum fruits and methods of increasing out put of extracting. We formulated the extract as oral drops and tablets.

Also inspite of absence of dissolution test in pharmacopea, we did it in order to compare tablet dosage form with standard preparation. (Legalon)

In order to study quality of Silymarin distribution in Silybum marianum fruits; Silymarin was isolated with preliminary de-fatting then was extracted with methanol and its content measured according to DAB10 method for assay. Since a large part of the oil present in pulp, was removed by separating husk from fruit mechanically in an invented method, using pressure, oven, blowing and milling. Then content of Silymarin in husk measured as DAB10 method.

Silymarin drops was fromulated with ethanol 40 in proportion of 1:5 and compared with standard fromulation, marindistel, for PH, density, dry residual and content of Silymarin. For tablet fromulation the extract was concentrated and used in silymarin tablet 35 mg, also silymarin tablet 70 mg was formulated using silymarin powder 80% from Nova-Linnea SA Company-Switzerland.

These products were compared with Legalon tablets for content of silymarin and dissolved percents.

A dissolution method was designed using apparatus II usp, medium consisted of 0.5% sodium lauryal sulfate, 900 ml, 100 rpm, 60 minute.

Results

1.Silymarin distribution:

   Silymarin in fruits without de-fatting: 1.56%

   Silymarin in defeated fruits: 2.2%

   Silymarin in husk: 3.5%

   Silymarin in pulp: 0.85%

2. Drops fromulation

 

PH

Density

Alcohol Degree

Dry Residual

Assay

Silymarin

5.7

0.94

41

2.4 g/100 ml

2.5 mg/ml

Marindistel

5.7

0.94

41

14 g/100 ml

2.2 mg/ml

3. Tablet fromulation

 

% dissolved

Assay

Silymarin

35

100%

35  mg

Silymarin

70

97%

70  mg

Legalon

70

80%

70  mg

Extraction from the husk of silybum marianum fruits instead of the whole fruits is easier than previously known methods and increases out put.

This research showed that our fromulations are comparabale with standard fromulations according to dissolution profile in tablets and other criteria in another product.

Presenting Author: Eskandary, S. sharareh_skn@yahoo.com