Design and Evaluation of Binding Properties of Cassia roxburghii Seed Galacto mannan and Moringa oleifera Gum in the Formulation of Paracetamol Tablets

 

MR Shivalingam¹,  KSG Arul Kumaran², D Jeslin², KV Ch Madhusudhan Rao¹ and M Tejaswini¹

¹Department of Pharmaceutics, Victoria College of Pharmacy, Guntur, AndhraPradesh

²K.M.C.H. College of Pharmacy, Coimbatore, Tamilnadu

*Corresponding Author E-mail:

ABSTRACT:

Plant gums and mucilage widely have been used in Pharmaceuticals and in other various industries due to their abundance in nature and low cost. In view of importance of binders in pharmaceuticals for the manufacture of tablets and capsules, gum isolated from the seeds of Cassia roxburghii Linn, and the stem of Moringa oleifera has been evaluated for their binding properties in the formulation of Paracetamol tablet containing 2%, 4% and 6% binding concentration. The binding properties of both gums were evaluated in relation to conventional binder like guar gum, gelatin, Sod.CMC at different parameter like percentage of fines, tablet hardness, disintegration time, dissolution and friability and found that 2% binding concentration of both gum shows superior binding properties when compared to the other binders. Increase in concentration of filtered and defatted C. roxburghii gum, M. oleifera gum from 2% to 6%; decrease the percentage of fine, increase the hardness, increase the disintegration time, decrease the percentage of friability and decrease % cumulative release. Hence Paracetamol tablets were formulated using combination of (1% C.rox+1%M.oleifera) binding concentration and evaluated. The binder-excipients interaction study was also carried out by using FTIR i.e. by KBr pellet method which showed that C. Roxburghii gum, M.oleifera gum is compatible with drug and all excipients in the formulation. Results indicates that Paracetamol tablets prepared with 2 % ( 1% C. roxburghii + 1% M. oleifera) of mucilage were found to be ideal for the preparation of uncoated tablet formulation when high mechanical strength is more essential.  Hence these gums shows better tabletting characteristics have high potentials for the substitution for more expensive binders.

 

 

 

INTRODUCTION

Plant gums and mucilage widely have been used in various industries like paper, textile, food,  ink, cosmetics, petroleum and frequently used in pharmaceuticals as thickening, binding, emulsifying, suspending,  stabilizing agents and coating materials in micro encapsulation. In view of importance of binders in pharmaceuticals for the manufacture of tablets and capsules, Cassia roxburghii seed gum, Moringa Oleifera bark gum were undertaken to evaluate its binding properties through assessment of various parameters essential for pharmaceutical formulation^{1, 5}

 

MATERIALS AND METHOD:

Collection of seeds:

C. roxburghii seeds, M. oleifera gum were collected from Tamil University, Thanjavur, and the same was authenticated by G. V. S. Moorthy, Botanical Survey of India (BSI), Southern circle, Coimbatore, Tamil Nadu. Paracetamol pure drug was obtained as a gift sample from Tablets India Ltd Chennai.

 

Isolation of seed gum: ^{6, 7}

The seeds of C. roxburghii were coarsely powdered, defatted by soxhlet extraction using petroleum ether (60-80⁰ C). Then extracted mucilage was precipitated with acetone and freeze dried to get fine gum powder. Yield was found to be 24%.

 

Filtered gum:

C. roxburghii seed powder was soaked in sufficient water kept over boiling water bath for 30 min. with occasional stirring, left overnight and filter using muslin cloth and precipitated with acetone. Then the mucilage obtained was freeze dried to get gum powder.  Yield was found to be 22%.

Formulations (Table-1)

 

Table-1

F1	Paracetamol formulation with 2%    C. rox. Filtered seed gum.
F2	Paracetamol formulation with 2% C. rox. Defatted seed gum.
F3	Paracetamol formulation with 2% M. oleifera gum.
F4	Paracetamol formulation with 2% Gelatin.
F5	Paracetamol formulation with 2% Guargum.
F6	Paracetamol formulation with  2% SCMC
F7	Paracetamol formulation with 4% C. rox. Filtered seed gum.
F8	Paracetamol formulation with 4%  C. rox. Defatted seed gum
F9	Paracetamol formulation with  4%  M. oleifera gum
F10	Paracetamol formulation with 6% C. rox. Filtered seed gum.
F11	Paracetamol formulation with 6% C. rox. Defatted seed gum .
F12	Paracetamol formulation with 6%  M. oleifera gum.
F13	Paracetamol formulation with  2% combination of (1%C. rox. Filtered seed gum + 1% M. oleifera gum).

 

Fig 1In-vitro Dissolution Graph for 2% Binding Concentration

 

Fig 2

 

Isolation of M. oleifera gum:

The gum was collected from trees (injured site). It was dried, ground, and passed through sieve no 80. Dried gum (10 g) was stirred in distilled water (250 ml) for 6-8 h at room temperature. The supernatant was obtained by centrifugation. The residue was washed with water and the washings were added to separate supernatant. The procedure was repeated four more times. Finally the supernatant was made up to 500 ml and treated with twice the volume of acetone by continuous stirring. The precipitated material was washed with distilled water and dried at 50-60° under vacuum.

Fig 3: Overlay FTIR Spectra of C.Rox formulation and M.oleifera formulation with Paracetamol Spectra.

 

Precompression parameters:

Bulk Density, Tapped density, Angle of repose, Carr’s Index were determined for Paracetamol granules prepared by using various binders with different binding concentrations ^{3, 4}

 

Method of formulation: ⁸

Paracetamol tablets were prepared by wet granulation method, by using C. Roxburghii filtered gum, and C.rox defatted gum, Sod.CMC, Guar gum, Gelatin, Moringa Oleifera, as binding agents. The Compression process was performed by using twelth station rotary tablet punching machine (punch size 12/32). Various formulations are mentioned in Table 1.

 

Post formulation study of Paracetamol formulations:

The formulated tablets were evaluated for the following    parameter such as % fines, hardness test, friability, weight variation, thickness, disintegration, and dissolution studies and results were recorded. ^{2, 3, 4}

 

Characterization of Paracetamol formulation by Fourier transfer Infrared spectroscopy (FTIR):

Fourier transform IR spectra were recorded on FT/IR-4100 type A for Paracetamol, Paracetamol formulation with C.rox gum and Paracetamol formulation with M.oleifera gum and results were recorded.

 

RESULTS AND DISCUSSION:

The pre-compression parameters like Bulk density, Tapped density, Angle of repose and Carr’s index were performed and results were recorded in the  Table 2 which showed that all the formulations were well with in the official limits. Tablets prepared were evaluated for % of fines, weight variation, hardness, friability, thickness, disintegration time and the results were given in the Table 3. The % deviation of all the formulations for all the parameters was found to be within the prescribed official limit. It has been observed that increase in the concentration of binders from 2% to 6% effectively changes the binding characteristic of the tablets.

Table-2

Parameters	Binding  Concentration
	2%						4%			6%			2% (1%C.Fil+ 1% C. Mor)
Formulation	F1	F2	F3	F4	F5	F6	F7	F8	F9	F10	F11	F12	F13
Bulk Density (g/cc)	0.43	0.44	0.44	0.47	0.46	0.47	0.47	0.42	0.46	0.48	0.46	0.48	0.47
Tapped Density (g/cc)	0.48	0.52	0.49	0.57	0.54	0.56	0.52	0.53	0.52	0.53	0.52	0.52	0.49
Angle of Repose (θ)	20.22	25.10	21.89	23.79	23.52	24.90	22.86	26.22	23.7	24.0	27.1	25.34	19.57
Carr’s Index	10.41	15.38	10.20	17.54	14.89	16.07	9.615	13.20	10.04	9.43	11.53	7.69	4.08

 

Table-3

Parameters	F1	F2	F3	F4	F5	F6	F7	F8	F9	F10	F11	F12	F13
% of Fines	6.12	6.22	6.18	6.54	6.43	6.7	5.82	6.10	5.92	5.62	5.99	5.63	5.32
Hardness (kg/cm2)	5.98	5.73	5.92	5.16	5.3	4.9	6.53	6.0	6.23	6.82	6.43	6.80	7.20
Friability %	0.66	0.82	0.71	0.91	0.96	1.2	0.57	0.72	0.60	0.50	0.67	0.53	0.44
Weight variation(mg)	604± 3.89	607± 4.76	608± 3.10	607± 2.67	605± 3.56	607± 3.99	510± 5.76	507± 4.76	515± 3.76	508± 3.91	518± 2.34	511± 3.45	510± 6.89
Thickness (mm)	4.2	4.3	4.1	4.2	4.4	4.2	4.2	4.2	4.1	4.2	4.1	4.21	4.10
Disintegr- ations (min.)	12.20	11.98	12.08	9.34	9.02	7.92	13.05	12.45	13.00	14.12	13.42	13.40	12.42

 

 

Results obtained from the dissolution study of Paracetamol  tablets using 2% of all binders like C. roxburghii filtered gum, Moringa oleifera, defatted C. roxburghii gum, gelatin, SCMC, and guar gum,  drug release post 2 hour were found to be 70.65  %,73.32 %, 75.22%  , 78.66% , 79.43 %  82.80% respectively and shown in the Fig 1.  Filtered C. roxburghii gum, Moringa oleifera as a binder shows less release as compared to the other binders. Increase in the concentration from 2% to 6% of C.rox filtered M.oleifera gum, defatted C. roxburghii gum, decreases the drug release. Combination of 2% binders( 1% filtered C. roxburghii gum +1% Moringa oleifera) shows increase in hardness, decrease in % fines, decrease in friability , decrease in release, and decrease in disintegration time,  when it is compared with the individual 2%  filtered C. roxburghii gum and  2% Moringa oleifera which is shown  in the Fig 2. Fourier transform IR spectra were recorded on FT/IR-4100 type A for Paracetamol, Paracetamol formulation with C.rox gum and Paracetamol formulation with  M. oleifera gum. There was no observation of extra peak (Fig 3). It showed that there was no physical interaction of the excipients with active ingredient.

 

SUMMARY AND CONCLUSION:

From the present study it can be concluded that Cassia roxburghii seed gum and Moringa oleifera gum (2%) may be used as a binding agent in the tablet formulation when high mechanical strength is more essential. Tablets prepared with 2 %( 1% C. rox filtered gum+1% M. oleifera) gum were found to be ideal for the preparation of uncoated tablets. Since they both displayed good tabletting characteristics and have high potentials for substitution for other more expensive binders. Further studies shown that Cassia roxburghii gum, Moringa oleifera gum have greater potentialities to become the new source of gums and could also be exploited for the commercial production of gums.

 

REFERENCES:

1.        Mahesh V.Chaubal, Excipient development for Pharmaceutical, Biotechnology and Drug delivery system, Edited by Ashok Katdare, 2006, p. 109-124

2.        Mehta, R.M., Text book of Pharmaceutics. P.226-253.

3.        Leon, L., Liberman, H. A., and Kanig, J.L., The Theory and Practice of Industrial Pharmacy. 3^rd Edition:  p.293-345.

4.        Liberman, H. A., Leon, L., and Joseph, B. S., Text book of Pharmaceutical Dosage forms : Tablets., 2^nd Edition., Vol. 1,  p. 75-130

5.        Wade, A., and Walker, P.J., Handbook of Pharmaceutical excipient, 2^nd Edition. London.,  1994:  p. 51-72

6.        Tausif M., Malhotra, A.K., and Kapoor, V.P., I  J Pharma sci.,  1992; 54(6): p. 234-240

7.        Kulkarni, G.T., Gowthamarajan, K.,  Brahmaji, G.,  and Suresh, B., Evaluation of binding properties of selected natural macilages., J. scientific  and industrial research.,  ISSN  0022-4456  CODEN JSIRAC: 2002, vol. 61:   p. 529-532

8.        Kohli, D.P.S., and Shah, D.H., 3^rd Edition. Drug formulations manual. p. 78.

9.        Indian Pharmacopoeia 1985., Vol II., 734-736.,  A 80-82

10.     Areevath, J., Munday, L.D., Cox, J.P., and Khan. A.K., Release characteristic of Diclofenac sodium  from encapsulated natural gum mini matrix formulation; Int J Pharmaceutics., 1996: Vol.139: (1-2),  p. 53-62

 

 

 

 

Received on 15.10.2009          Modified on 18.11.2009

Accepted on 10.12.2009         © RJPT All right reserved