Preparation and Evaluation of Fast Dissolving Tablet Tramadol Hydrochloride

 

Rohan Patil, Neha Patil, Aniket Patil , S. J. Shid, V.N. Dange, C.S. Magdum, S.K. Mohite

Department of Pharmaceutics, Rajarambapu College of  Pharmacy, Kasegaon, Tal- Walwa, Dist- Satara

 

ABSTRACT:

Novel drug delivery system assists to achieve better patient compliance. Fast dissolving tablets are one of them. FDT have benefits such as accurate dosing, easy portability and manufacturing, good physical and chemical stability and an ideal alternative for pediatric and geriatric patients. FDDT formulation combines the advantage of both liquid and conventional tablet formulation while also offering advantage over both traditional dosage forms. This review gives a view of advantages, limitations, need for formulating FDTS, Formulation factors, excipients used, and methodology and evaluation parameters.

 

Fast dissolving tablets (FDTs) can be prepared by different methods, such as direct compression, freeze-drying, spray drying, sublimation, wet granulation method4. The basic approach for the development of FDTs is the use of superdisintegrants.  The aim of this study was to formulate FDTs with sufficient mechanical integrity and to achieve faster disintegration in the oral cavity without water. To achieve this goal, mannitol used as diluent as well as sweetening agent for the formulation of tablets. Attempts were made to enhance dissolution rate along with faster disintegration using superdisintegrants, like microcrystalline cellulose. Tramadol hydrochloride, a centrally acting synthetic opioid analgesic, was selected as the active pharmaceutical ingredient in the study.

 

 

 

INTRODUCTION:

Recent advance in novel drug delivery system aims to enhance the safety and efficacy of the drug molecule by formulating a dosage form being for the administration. Difficulty in swallowing is experienced by patient such as pediatric, geriatric, bedridden, disabled and mentally ill, including motion sickness and sudden episodes of allergic attacks, hence resulting in higher incidence of non-compliance and ineffective therapy. To improve the quality of life and treatment compliances of such patients fast dissolving tablets dosage form is a better alternative for oral medication.

Orally disintegrating tablets are solid dosage form containing medical substances which disintegrate rapidly, usually within few seconds when placed upon tongue requiring no additional water to facilate swallowing. It is suited for tablets undergoing high first pass metabolism and is improving bioavailability with reducing dosing frequency to minimize side effect. Tramadol hydrochloride is a synthetic opioid analgesic used for moderate to severe pain like labor pain, postoperative surgeical pain, traumatic pain and cancer pain. Tramadol hydrochloride can be administered orally, intravenously or rectally. Tramadol hydrochloride is rapidly absorbed orally. It is bitter in taste. Taste masking is an essential requirement for fast dissolving tablets for commercial success. Taste masking of the active ingredients can be achieved by various techniques. Two approaches are commonly utilized to overcome bad taste of the drug. The first includes reduction of drug solubility in saliva, where a balance between reduced solubility and bioavailability must be achieved. Another approach is to alter the ability of the drug to interact with taste receptor. In present study an attempt has been made to prepare the Fast dissolving tablet Tramadol hydrochloride. Taste masking of Tramadol hydro chloride was carried out by using mannitol.

 

Microcrystalline cellulose and guar gum are the superdisintegrants used for rapid dissolution of drug and absorption, which may produce the rapid onset of action in the treatment of analgesic for postoperative pain.

 

MATERIALS AND METHODS:

Materials:

Tramadol hydrochloride is used as a main ingredient. The excipients are used which having a property like superdisintegrants (microcrystalline cellulose), Diluents as well as sweetening agent (Mannitol), and other excipients like Magnesium stearate, Guar Gum, Talc.  

 

Methods:

Preparation of Tramadol Hydrochloride Fast Dissolving Tablet by Direct compression Firstly fixed amount of Tramadol Hydrochloride is mixed in an appropriate manner by using the mortar and pastle. and Then the mixed ingredients are then directly use for the formulation of the tablet using the direct compression technique with the help of the tablet punching machine.

 

Formulation table:

Ingredients  (mg)	Batches For Formulation
	F1	F2	F3	F4
Tramadol Hydrochloride	50	50	50	50
Microcrystalline Cellulose	2.5	5	-	-
Guar Gum	-	-	2.5	5
Magnesium stearate	0.25	0.25	0.25	0.25
Talc	0.25	0.25	0.25	0.25
Mannitol	47	44.5	47	44.5

 

Evaluation tests:

Weight variation test:

Twenty tablets were taken and their weight was determined individually and collectively on a digital weighting balance. The average weight of one tablet was determined from the collective weight.

 

Hardness test:

The hardness of the tablet was determined using Monsanto Hardness Tester.

 

Friability test:

Six tablets from each batch were examined for friability using Roche Fribilator   and the equipment was run for 4min at 25 revolutions per minute. The tablets were taken out, dedusted and reweighted and % friability was calculated.

%Friability = (Loss in weight/Initial weight) x 100

 

In vitro disintegration time:

The disintegration test was performed using an USP disintegration apparatus, with distilled water at 24±0.5⁰C. The time reported to obtain complete disintegration of six tablets were recorded and average was reported

 

In vitro dissolution testing:

Dissolution study was conducted for all the formulation using USP Type-II apparatus. The dissolution test was performed using 500 ml of phosphate buffer (PH 6.8) was taken as the dissolution medium at 50 rpm and 370C±0.5⁰C. Five millilitres of aliquots were periodically withdrawn and the sample volume was replaced with an equal volume of fresh dissolution medium. The samples were analyzed spectrophotometrically at 270 nm.

 

Table no. 2:- Evaluation Table for Fast Dissolving Tablet Tramadol Hydrochloride

Evaluation Parameters	Batches For Evaluations
	F1	F2	F3	F4
Thickness(mm)	1.96	2.02	1.98	2.24
Hardness(Kg/cm2)	3.5	4	3	2.5
Weight variation	±7.1	±7.35	±6.9	±7.05
Friability (%)	0.94	0.78	0.95	0.97
Disintegration Time (sec)	23± 1.25	20±1.15	25±1.10	28±1.18
% Drug Release	97.5	99.85	95.35	96.40

 

RESULT AND CONCLUSION:

All the prepared batches of tablets were within the range. Using Monsanto hardness tester, the strength of the tablets was tested. All the tablets showed good hardness. Batch ‘F4’ had minimum hardness (2.5±0.10) while ‘F2’ had maximum hardness (4.0±0.09). The friability was carried out for all the batches of tablets. The friability was less than 0.99% for all the blends and was satisfactory. From the data obtained it was found that 99.85% of drug was released from the batch ‘F2’ at 20 min while other batches ‘F1’ , ‘F3’and ‘F4’ had shown  97.5% , 95.35%, and 96.40% drug re-lease at 20 min respectively. The variation in the dissolution rate of Tramadol hydrochloride tablets was in the following order F2›F1›F4 ›F3. The dissolution profile of batches of tablets prepared by direct compression method has shown better results which is shown in the fig.2

 

CONCLUSION:

All the tablets showed satisfactory results with respect to hardness, friability, wt. variation, Disintegration studies and in- vitro dissolution studies. The Batch ‘F2’ had the better dissolution rate as compared to batch ‘F1’ ‘F3’ and ‘F4’.

 

So it is concluded that the formulated batch F2 shows the better results in all the tests performed during formulation and evaluation and it is the good batch among all the batches.

 

REFERENCE:

1.     Sonali J. Shah, Rupa Mazumder, Formulation Development and Evaluation of Mouth Dissolving Tablet of Tramadol Hydrochloride. Asian Journal of Pharmaceutical and Clinical Research, Vol 6, Suppl 3, 2013, ISSN-0974-2441. 

2.     Lachman L., Liberman H.A, Kanig J.L., the Theory and Practice of Industrial Pharmacy. 3^rdedition. Varghese Publication House, Mumbai. (2003) 293-294.

3.     Raja Sridhar Rao. Ponugoti  and Chandrasekara Rao Gonugunta.  Formulation and Evaluation of Mouth Dissolving Tablet of Tramadol Hydrochloride. Tropical Journal of Pharmaceutical Research, May 2014; 13 (5); 669-675.

4.     Shubhangi J. Shid, Chandrakant. S. Magdum, Shrinivas. K. Mohite, Manoj M. Nitalikar, Vidya N. Dange.  Formulation and Evaluation of Sustained Release Microspheres. 3(6), 2014,177-186

5.     Raut Indrayani D. Mane Pallavi, Mane Dipak, Mohite S. K. Magdum C.S. Design And Characterization Of Fast Dissolving Tablet Valsartan Using Synthetic And Natural Super Disintegrants. International Journal of Advanced Research (2015), Vol 3 Issue 3,1207-1212

6.     Vidya. N. Dange, Chandrakant. S. Magdum, Shrinivas K. Mohite, Manoj M. Nitalikar, Shubhangi J. Shid. Formulation and Evaluation of Cetylpyridinium Chloride Toothpaste. 3 (6). 2014, 68-78

 

 

 

Received on 11.05.2016       Accepted on 30.06.2016     

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