A novel effervescent tablet of fenugreek extract
NB Banarase*, SS Khadabadi, IA Farooqui, PB Aswar and NM Bhopale
Dept. of Pharmacognosy and Phytochemistry, Government College of Pharmacy, Kathora Naka, Amravati- 444604 (M.S.)
* Corresponding Author E-mail: nbanarase7@gmail.com
ABSTRACT
A novel effervescent solid pharmaceutical dosage formulation using seed extract of Trigonella foenum-graecum Linn. (Leguminaceae) was proposed. The extraction of seeds was done by water. The effervescent tablets were produced by "Heat method" using aqueous fenugreek extract, hydrous citric acid, calcium carbonate, aspartame and other excipients. Three formulations were made and evaluated for various parameters according to IP. The TLC of trigonelline was done to confirm the availability of trigonelline after the complete disintegration of tablet.
KEY WORDS Aqueous fenugreek extract, Heat method, Effervescent tablet, TLC of trigonelline.
INTRODUCTION:
Currently, an increased use of ‘traditional medicine’ is observed in developed and developing countries (WHO Information 1996; Akerele 1991). This kind of therapeutic strategy is essentially based on the use of herbal medicines or ‘phytomedicines’. Owing to this, legal standards of quality control about these products have been enacted in several countries including India. Consequently, a set of regulations regarding all process involved in phytomedicine attainment (design, formulation and production) was established in order to fulfill with requirements of quality, safety and efficacy. Therefore, it is essential, on one hand, to establish the botanical, chemical and sanitary control of the plant material to be used and, on the other, a suitable design of the formulation and evaluation of its pharmaceutical properties; this latter guarantees the therapeutic efficacy. The design and formulation of tablets using plant extract, as active material have several technical drawbacks that conspire against the quality of the product. Many times the extract obtained could not completely dried and it could absorbed the moisture, which might lead the difficulty in formulation of tablet.1
Since, Fenugreek seeds had been used in India since ancient times for the treatment of the diabetes. Today the research proved that the aqueous extract of fenugreek seeds has potent antidiabetic action2.
However many conventional tablets of fenugreek extracts are available in the market. But it has number of drawbacks such as the slow onset of action, difficulty in swallowing of tablet especially in case of elderly patients and childrens.3
In this work, the design of novel effervescent tablet using the Trigonella foenum-fraecum Linn. (Leguminaceae) seeds aqueous extract is proposed, as the effervescent tablet can overcome all these drawbacks.
MATERIALS AND METHODS:
Extraction of plant material:
500g of powdered Trigonella foenum-graecum seeds were boiled in 2 liter distilled water for 30 minutes. Then, the decoction was cooled for 30 minutes at room temperature. Next, the cooled decoction was filtered through a coarse sieve twice. Finally, the filtrate was concentrated on water bath to a thick paste & dried under vacuum.
Materials:
It includes aqueous fenugreek extract prepared by above method, Calcium carbonate, Citric acid were purchased from Loba Chemicals (Mumbai, India). Aspartame was purchased from BDH Chemicals. Trigonelline hydrochloride was purchased from Sigma- Aldrich. All the other chemicals used were of high analytical grade.
Methods
Preparation of Effervescent Tablets:
Different Effervescent tablet formulations were prepared by “Heat method”. (Formulation I-III, Table 1). All the powders were passed through 80 mesh. Fenugreek extract was dissolved in sufficient quantity of water, then added calcium carbonate and aspartame in it and blended it to form semisolid mass, it was then passed through # sieve, dried it in oven at 50 degree celcius for 3 hours.4
Table 1. Tablet Formulations
|
Sr. No. |
Ingredients per Tablet (mg) |
F-I |
F-II |
F- III |
|
1. |
Aqs. Fenugreek extract |
180 |
180 |
180 |
|
2. |
Citric acid (hydrous) |
90 |
100 |
90 |
|
3. |
Calcium carbonate |
110 |
100 |
110 |
|
4. |
Aspartame |
1 |
1 |
1 |
|
5. |
Talc |
9 |
9 |
9 |
|
6. |
Magnesium stearate |
10 |
10 |
10 |
Secondly, took hydrous citric acid in, a large porcelain dish placed over the boiling water bath. Added the dried calcium carbonate powder prepared above slowly & blended it to form semisolid mass. The mass was sieved through 22/44 mesh. The granules were dried at 40°C for 12 hours. Once dry, the granules retained on 44 mesh were mixed with 15% of fines (granules that passed through 44 mesh). Talc and magnesium stearate were finally added as glidant and lubricant. Tablets were compressed (10 mm diameter, concave punches) using 10 stations single rotary tablet compression machine (Rolex Pharma, India). Each tablet contained 180 mg of fenugreek extract and other pharmaceutical ingredients as listed in Table 1. Prior to the compression, the granules were evaluated for several tests.
Evaluation of Granules (Table 2) Angle of Repose:
The angle of repose of granules was determined by the funnel method. The accurately weighed granules were taken in a funnel. The height of the funnel was adjusted in such a way that the tip of the funnel just touched the apex of the heap of the granules. The granules were allowed to flow through the funnel freely onto the surface. The diameter of the powder cone was measured and angle of repose was calculated using the following equation :
TBD = Weight of the powder/ Tapped volume of the packing.
Compressibility Index:
The compressibility index of the granules was determined by Carr’s compressibility index :
Carr’s index (%) = [(TBD-LBD) × 100] /TBD
Total Porosity:
Total porosity was determined by measuring the volume occupied by a selected weight of a powder (Vbulk) and the true volume of granules (the space occupied by the powder exclusive of spaces greater than the intermolecular space, V) :
Porosity (%) = Vbulk-V/Vbulk × 100.
Evaluation of Tablets (Table 3) Thickness:
The thickness of the tablets was determined using a thickness gauge (Mitutoyo, New Delhi, India). Five tablets from each batch were used, and average values were calculated.
Weight Variation Test:
To study weight variation, 20 tablets of each formulation were weighed using an electronic balance (Shimadzu AW 220, Japan), and the test was performed according to the official method.
Hardness and Friability:
For each formulation, the hardness and friability of 6 tablets were determined using the Monsanto hardness tester (Cad- mach, Ahmedabad, India) and the Roche friabilator (Camp- bell Electronics, Mumbai, India), respectively.
TLC OF TRIGONELLINE
Where, h and r are the height and radius of the powder cone.
Bulk Density:
Both loose bulk density (LBD) and tapped bulk density (TBD) were determined. A quantity of 2 g of powder from each formula, previously lightly shaken to break any agglomerates formed, was introduced into a 10-mL measuring cylinder. After the initial volume was observed, the cylinder was allowed to fall under its own weight onto a hard surface from the height of 2.5 cm at 2-second intervals. The tapping was continued until no further change in volume was noted. LBD and TBD were calculated using the following formulas :
LBD = Weight of the powder/ Volume of the packing.
TLC Photograph of Evaluation of Trigonelline
■E- Spot of extract. ■T- Spot of Tablet. ■S- Spot of Standard
(Trigonelline hydrochloride). ■Rf value- o.42.
Table 2. Evaluation of granules properties
|
Tablets |
Angle of repose |
Loose Bulk Density (g/ml) |
Tapped Bulk Density (g/ml) |
Compressibility Index (%) |
Total Porosity (%) |
|
F-I |
24.50±0.02 |
0.506±0.02 |
0.582±0.04 |
13.08±0.02 |
27.43±0.03 |
|
F-II |
22.10±0.01 |
0.512±0.04 |
0.581±0.02 |
11.82±0.03 |
26.92±0.03 |
|
F-III |
21.20±0.02 |
0.493±0.03 |
0.555±0.03 |
11.25±0.03 |
26.97±0.02 |
Table 3. Evaluation of tablets
|
Formulations |
% Weight variation |
Thickness (mm) |
Hardness (kg/cm2) |
% Friability |
Disintegration time (Min) |
|
F-1 |
1.17±0.49 |
3.41±0.01 |
4.10±0.1 |
0.30±0.05 |
4.45±0.05 |
|
F-2 |
1.42±0.53 |
3.53±0.01 |
4.14±0.08 |
0.29±0.01 |
4.60±0.45 |
|
F-3 |
1.10±0.43 |
3.43±0.02 |
4.06±0.04 |
0.33±0.02 |
4.15±0.03 |
Disintegration8 :
Disintegration time test involves placing one tablet in a 250 ml beaker containing water at 20 degree to 30 degree Celsius; numerous gas bubbles are evolved. When the evolution of gas around the tablet or its fragments has ceased the tablet shall have disintegrated, being either dissolved or dispersed in the water so that no agglomerates of particles remain. Repeat the operation on a further 5 tablets. The tablets comply with the test if each of the 6 tablets disintegrates in the manner prescribed within 5 minutes, unless otherwise stated in the individual monograph.
Evaluation of Trigonelline by TLC
Trigonelline is one of the important alkaloid of the fenugreek responsible for hypoglycemic action. It is reported that Trigonelline exhibited significant hypoglycemic action by inhibiting cortisone-induced hyperglycemia9.Many times during the effervescence formation in water the active constituent may get destroyed due to change in pH. So, it is necessary to determine whether the active constituent is present after disintegration or not. In this study the main aim was to determine whether the Trigonelline is present after the complete disintegration of the effervescent tablet or not.
In this TLC study three spots were applied on TLC plate. One was applied as a standard Trigonelline, second one was of extract and last one was of formulation i.e. of effervescent tablet after complete disintegration in water.
Mobile Phase Used :
The mobile phase used involves10: n-propanol:
methanol: water (4:1:4 v/v/v)
Sample preparation:
All the samples are prepared in distilled water including standard and extract. While the test sample from tablet is taken after the complete disintegration of tablet in water.
RESULTS AND DISCUSSION:
Present research work deals with the formulation and evaluation of novel effervescent tablet using aqueous fenugreek extract. The fenugreek has been used in India since ancient days for the treatment of the diabetes. Three formulations were prepared by using Fenugreek aqueous extract, citric acid, calcium carbonate, aspartame and other excipients. The Effervescent granules were prepared by using “Heat method” & evaluated for various parameters i.e. Bulk density, % Compressibility index, Angle of repose & Total porosity. These granules showed good properties. These Effervescent granules were then compressed into tablet and evaluated for various parameters i.e. Thickness, Hardness, Weight variation, Friability, Disintegration time. All these formulations passed the criteria of IP. The presence of trigonelline in the formulation was determined by TLC, as the trigonelline is the component of aqueous extract showing antidiabetic activity.
ACKNOWLEDGEMENT:
The authors are acknowledging to Mr. U.A. Deokate for their constant support throughout the research work.
REFERENCES:
1. http://www.pharmpedia.com/Effervescent_tablet. (Advantages of effervescent tablet.
2. Wan-Li-Xue, Xuan-She Li. Effect of Trigonalla foenum-graecum (fenugreek) extract on blood glucose, blood lipid and haemorheological properties in streptozocin-induced diabetic rats, Asia.Pac.J.Cli.Nutr, 2007; 16(supl 1): 422-426.
3. http://www.amerilabtech.com/docs/EffervescentTablets&Key Facts.pdf
4. RM Mehata, PHARMACEUTICS II, First edition 2002, Vallabh Prakashan,80-84.
5. Cooper J, Gunn C. Powder flow and compaction. In: Carter SJ, eds. TutorialPharmacy. New Delhi, India: CBS Publishers and Distributors; 1986:211-233.
6. Shah D, Shah Y, Rampradhan M. Development and evaluation of con-trolled release diltiazem hydrochloride microparticles using cross-linked polyvinyl alcohol. Drug Dev Ind Pharm. 1997;23(6):567-574.
7. Aulton ME, Wells TI. Pharmaceutics: The Science of Dosage Form Design. London, England: Churchill Livingstone; 1988.
8. Indian Pharmacopoeia –1996, Vol – 2, Govt. Of Indian, Ministry Of Health and Family Welfare, Published By Controller of Publication, New Delhi, 734-736.
9. Martin A. Micromeritics. In: Martin A, ed. Physical Pharmacy. Balti-more, MD: Lippincott Williams and Wilkins; 2001:423-454.
10. Williamson E.M, Dabour Ayurvedic Foundation, Major Herbs of Ayurveda, First Edition L.D Publisher: Churchil Livingstone, 315-320.
11. http://www.ualberta.ca/csps/JPPS9/Conference/Abstracts2006. htm.