You are hereDESIGN AND DEVELOPMENT OF SUSTAINED RELEASE MATRIX TABLETS OF FUROSEMIDE

DESIGN AND DEVELOPMENT OF SUSTAINED RELEASE MATRIX TABLETS OF FUROSEMIDE


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ABOUT AUTHORS:
Dr. D. Nagendrakumar, Reddy VM, Keshavshetti G G, Shardor A G*
Department of Pharmaceutics, SVET’s College of Pharmacy,
Humnabad- 585 330 (Karnataka).
ambarish.pharma@gmail.com

ABSTRACT
Sustained release matrix system are favored because of their simplicity, patient compliance etc, than traditional drug delivery which have many drawbacks like repeated administration, fluctuation in blood concentration level etc. For the purpose of enhancement the bioavailability of furosemide, a dosage form with sustained release of furosemide was designed in this study.
Sustained release tablets of furosemide were fabricated using xanthan gum(13.33 % to 66.67 %). Thepreparedtablets were evaluated for pre compression and post compression studies likeangle of repose, bulk density, tapped density, hardness, weight variation, fraibilty, drug content, in-vitro releaseof drugetc. among the five formulations A better controlled drug release (85 %) was obtained with the matrix tablet SX5 containingxanthan gum66.67%. Short-term stability studies of all formulations indicates that there were no significant changes in drug content and dissolution parameter values after 3 month storage at 40° ± 2°C/75 ± 5% RH.

REFERENCE ID: PHARMATUTOR-ART-2064

PharmaTutor (ISSN: 2347 - 7881)

Volume 1, Issue 2

Received On: 30/10/2013; Accepted On: 24/11/2013; Published On: 20/12/2013

How to cite this article: Kumar DN, Reddy VM, Keshavshetti GG, Shardor AG, Design and Development of Sustained Release Matrix Tablets of Furosemide, PharmaTutor, 2013, 1(2), 99-105

INTRODUCTION
Matrix tablets composed of drug and polymer as release retarding material offer the simplest approach in developing a sustained-release drug delivery system. Recent trend in development of sustained-release drug delivery systems was the use of gums of plant origin to fulfill the aim of retarding the drug release1,2,3,4. Natural gums are biodegradable, non-toxic and have capability to swell on contact with aqueous media. The natural polymers used do hold advantages over the synthetic polymers generally because they are non toxic, less expensive and freely available. Most common examples of natural gums are Guargum, Xanthan gum, Pectin and GumTragacanth.

Xanthan gum is a high molecular weight extracellular polysaccharide, produced on commercial scale by the viscous fermentation of gram negative bacterium Xanthomonas campesteris. The molecule consists of a backbone identical to that of cellulose, with side chains attached to alternate glucose residues. It is a hydrophilic polymer, which until recently had been limited for use in thickening, suspending and emulsifying water based systems.5

Furosemide (4-chloro-2- furfurylamino-5-sulphamoyl benzoic acid) is a drug with a diuretic action which acts at the renal level on the ascending limb of the loop of Henle.6 Furosemide is absorbed mostly in the stomach and upper small intestine, possibly due to its weak acidic properties, Furosemide undergoes first pass metabolism resulting in a narrow absorption window, leads to its low bioavailability (43-69 %). The biological half life of furosemide is 100 minutes.

MATERIALS AND METHODS
Furosemide was obtained as a gift sample from Wokhardth Aurangabad. Xanthan gum was obtained from Bangalore fine chem, Bangalore. Other materials like MCC, PVP K-30, Magnesium stearate, talc were obtained from SD fine chem, Mimbai.

PREPATION OF SUSTAINED RELEASE MATRIX TABLETS
Sustained release matrix tablets of furosemide were prepared by using different drug: polymer ratios viz. 1:1, 1:2, 1:3, 1:4 and 1:5 for SX1, SX2, SX3, SX4 and SX5 respectively for all formulations as per the composition given in Tabl-1. The lubricated formulations were compressed by a direct compression technique.

Table 1: Composition of matrix tablets of furosemide.

Ingredients

mg/tablet

Formulation code

SF0

SX1

SX2

SX3

SX4

SX5

 

Furosemide

20

20

20

20

20

20

 

Xanthan gum

---

20

40

60

80

100

 

Microcrystalline cellulose

113

93

73

53

33

13

 

Talc

2.0

2.0

2.0

2.0

2.0

2.0

 

Magnesium stearate

2.0

2.0

2.0

2.0

2.0

2.0

 

PVP K 30

3.0

3.0

3.0

3.0

3.0

3.0

 

Lactose

10

10

10

10

10

10

 

Total weight

150

150

150

150

150

150

 

SF   = Sustained formulation not containing any polymer.SXF   = Sustained formulation containing Xanthan Gum.

EVALUATION OF MATRIX TABLETS OF FUROSEMIDE
All the prepared matrix tablets were evaluated for uniformity of weight and drug content as per IP method. The friability of tablets was determined using Roche Friabilator. It is expressed in percentage (%). Hardness was measured by using Pfizer hardness tester. Thickness was measered by Vernier caliper.

In vitro drug release studies
The in vitro dissolution studies of sustained release matrix tablets of furosemide were carried out using USP XXIII tablet dissolution test apparatus (Electrolab TDT-08L), employing a paddle stirrer at 50 rpm in 900 ml of pH 6.8 phosphate buffer at 37.0° ± 0.5°C. Then 5 ml of samples were collected and replaced with the same amount of dissolution medium at 1hr time intervals for 12 hr. The samples withdrawn were analyzed spectrophotometrically at 276.0 nm using UV-visible double-beam spectrophotometer (Shimadzu UV-1800 spectrophotometer).

RESULTS

Hardness test
The hardness of tablets was found to be in range of 4.86±0.11 to 5.08 ±0.82 kg/cm2.

Friability test
The % weight loss in friability test of all the formulations was found to be less than 1%, indicating that the can withstand the mechanical shock or during handling.

Weight Variation Test
The average weight of tablets was found to be 149-152 mg for all formulations. Overall the all prepared formulations were good quality with regard to weight uniformity. The standard deviation values were within the acceptable limits.

Table 2:Results of physical characteristics of Matrix tablets with Xanthan gum

Formulation

Code

Hardness

(kg/cm2)

Mean ± SD (n=3)

Thickness

(mm)

Mean ± SD (n=3)

Average weight

(mg)

Mean ± SD (n=10)

Friability

(%)

Drug content

(%)

Mean ± SD (n=3)

SX1

4.86 ± 0.11

3.22 ± 0.11

150.4 ± 0.9

0.19

97.49 ± 1.08

SX2

4.87 ± 0.06

3.31 ± 0.06

151.7 ± 0.8

0.12

99.78 ± 0.96

SX3

4.91 ± 0.18

3.21 ± 0.18

149.3 ± 1.1

0.70

98.22 ± 0.69

SX4

5.08 ± 0.12

3.16 ± 0.12

149.2 ± 0.9

0.75

97.75 ± 0.38

SX5

4.93 ± 0.11

3.25 ± 0.11

152.4 ± 0.8

0.86

101.21 ± 1.07

Drug Content Uniformity

Uniformity in drug content was found according to I.P specifications and percentage of

drug content was more than 95% . All the formulations comply with official standards.

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