Experimental Work On Norfloxacin Biology Essay

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Accurately weighed 100 mg of norfloxacin was dissolved in 100 ml of distilled water/phosphate buffer pH 6.7/0.1 N Hcl. The solution was suitably diluted to prepare solutions of strengths ranging from 2, 4, 6, 8, 10 µg / ml. These solutions were scanned by UV spectrophotometer at 274 nm and the calibration curve was plotted.

The resin was accurately weighed and placed on a Whatman filter paper in a funnel and washed several times with distilled water and then with 1N HCl solution followed by washing with 1N NaOH solution, finally the resins were again washed with distilled water.

Preparation of complex

Drug resin complex was prepared by batch process, 100 mg of activated Indion 234 was taken in a beaker. A volume of 25 ml of distilled water was added. The resin was allowed to swell in water for 30 min and 100 mg of norfloxacin was added. The contents of the beaker were stirred on a magnetic stirrer for 30 min. The complex was filtered using a Whatman filter paper.After that the complex is plased overnight in hot air oven.

Detection of unbound drug

The residue from above process was further washed with 75 ml of distilled water to remove any unbound drug. The filtrate was collected and diluted 10 times with distilled water and then subjected to analysis at 274 nm on UV spectrophotometer to determine any unbound drug. By subtracting the quantity of unbound drug from the concentration of the drug added, the amount of bound drug was calculated. Similarly, study was carried out for other drug resin ratios.

Optimization of drug resin complex 15

Optimization of the Drug-Resin Ratio

Six drug-resin ratios were studied, namely, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:2, 1:3.

Optimization of Drug loading time

Complexes were stirred on a magnetic stirrer, and the percent drug loading obtained at different time periods was calculated. Formation of drug resin complexes for Norfloxacin-Indion 234 was studied at 5 min, 10 min, 15 min, 20 min, 30 min, and 240min.

Study of molecular properties of drug-resin complexes 15

X-ray powder diffraction of norfloxacin

Samples were irradiated with monochromatized Cu Kα radiation (1.542 A0) and analysed between 2-50 (2θ). The voltage and current were used 30 KV and 30mA respectively. The range was 5x10 3 cycles /sec.

Infrared spectroscopic analysis

Infrared spectra of norfloxacin pure drug, Indion 234 resin and norfloxacin - Indion 234 complex were obtained using Fourier transform infrared (FTIR) spectroscopy. The pellets were prepared on KBr press and the spectras were recorded over the wave number range of 4000-400 cm-1.

Drug release kinetics for norfloxacin complex 12,16,29

Drug release of optimized drug resin complex in plain distilled water was determined using a USP type II dissolution apparatus at 370C, at 50 r.p.m. for 30 min.

Similarly the release of norfloxacin from the resinates was determined in 0.1 N HCl, 900 ml, 370C and 50 r.p.m. for 120 min.

Drug release from the optimized drug complex was also studied in Phosphate buffer pH 6.7 at 370C and 50 r.p.m. for 60 min.

Formulation of dispersible tablet 13

Tablets containing 100 mg of norfloxacin were prepared by direct compression method and the various formulae used in study are shown in Table . The drug, dry binder, diluents, superdisintegrant and flavor were passed through sieve #40 then all ingredients were properly mixed together in a polybag. Talc and Magnesium stearate were passed through sieve #80 and mixed and blended with initial mixture in a polybag.

Table

Formulation of dispersible tablet

Ingredients(mg)

DT 1

DT 2

DT 3

DT 4

DT 5

DT 6

DT 7

DT 8

DT 9

Drug resin complex

325

325

325

325

325

325

325

325

325

Microcrystalline cellulose

30

30

30

30

30

30

30

30

30

Mannitol

19

14

9

19

14

9

19

14

9

Crosscarmellose sodium

10

15

20

-

-

-

-

-

-

Crospovidone

-

-

-

10

15

20

-

-

-

Sodium starch glycolate

-

-

-

-

-

-

10

15

20

Magnesium stearate

2

2

2

2

2

2

2

2

2

Talc

4

4

4

4

4

4

4

4

4

Aspartame

10

10

10

10

10

10

10

10

10

Total

400

400

400

400

400

400

400

400

400

Evaluation of powder blend

Angle of repose 2

Angle of repose was determined by using fixed funnel method. It is the maximum angle that can be obtained between the free flowing surface of lubricated blend of matrix tablets heap and the horizontal plane. Accurately weighed lubricated blends were allowed to fall freely through a funnel until apex of conical pile just touched the tip of the funnel. The angle of repose θ was determined according to the following formula:

θ = tan-1 (h/r)

Where,

h = height of the pile

r = radius of the pile

θ = angle of repose

Hausner's ratio 32

A similar index has been defined by Hausner

Tapped Density

Hauser's ratio =

Bulk density

It indicates that the flow properties of the powder and is measured by the ratio of tapped density to bulk density.

Value less than 1.25 (= 25% Carr's index) indicates good flow while greater than 1.25 indicate poor flow (= 33% Carr's index). Between 1.25 and 1.5 added Glidants normally improves flow.

Bulk density 12,25

Ten grams of DRCs were placed into 100 ml measuring cylinder and volume noted. The bulk density was calculated by the following equation

ρo = M/Vb

Where,

ρo =bulk density,

M =mass of the DRC and

Vb= Volume of DRC

Tap density 12

10 gm of DRCs were taken in measuring cylinder. The cylinder was then subjected to a fixed number of taps (100). The final volume was recorded and the tap density was calculated by the following equation

ρt =M/V

Where,

ρt=tapped density,

M= mass of the DRC and

Vt =Volume of DRC on tapping.

Compressibility5

Compressibility of the drug was determined using the following equation

% compressibility= (ρt- ρo/ ρt) 100

Where,

ρt is the tapped density and

ρo is the bulk density.

EVALUATION OF TABLETS

Hardness 17,25

Hardness of the tablets has been defined as the force required for breaking a tablet in diametric compression. The resistance of the tablets to chipping, abrasion or breakage under the conditions of storage, transportation and handling before usage depends in its hardness. For each formulation, the hardness of 3 tablets was determined using the Monsanto hardness tester. The tablet was held along its oblong axis in between the two jaws of the tester. At this point, reading should be zero kg/cm2. Then constant force was applied by rotating the knob until the tablet fractured. The value at this point was noted in kg/cm2.

Friability 5,29

Friability was measured to find the strength of tablet by Roche Friabilator. This test subjects a number of tablets to the combined effect of shock abrasion by utilizing a plastic chamber which revolves at a speed of 25 rpm, dropping the tablets to a distance of 6 inches in each revolution. A sample of preweighed 10 tablets was placed in Roche friabilator which was then operated for 100 revolutions i.e. 4 minutes. The tablets were then dusted and reweighed. A loss of less than 1 % in weight is generally considered acceptable. Percent friability was calculated as follows,

Percentage friability = (Initial weight - Final weight / Initial weigh) x 100

Weight variation29

Twenty tablets were selected randomly and average weight was determined. Then individual tablets were weighed and was compared with average weight.

Table

Weight variation test USP

Average weight of Tablets (mg.)

Maximum percentage deviation

130 or less

130 - 324

324 mg or more

10

7.5

5

Not more than two of the individual weights deviate from the average weight by more than the percentage shown in above table and none deviates by more than twice of that percentage.

Drug content uniformity15

The drug content was determined by eluting the crushed tablet with continuous stirring in 100 ml 1N Hcl for 4 hour to ensure complete elution. The solution was filtered. After suitable dilution the drug content was determined at 274 nm by UV/VIS spectrophotometer. According to USP acceptable limit is ± 10%.

Uniformity of dispersion15

This test is applicable only to dispersible tablets. In the method, 2 tablets are placed in 100 ml of water and stirred gently until completely dispersed. A smooth dispersion must be obtained which passes through a sieve screen with a nominal mesh aperture of 710µm (sieve no.22).

Disintegration time29

Disintegration time was determined using USP tablet disintegration test apparatus using 900ml of distilled water without disk at room temperature (300C). If 1 or 2 tablets fail to disintegrate completely, repeat the test on additional 12 numbers. Not less than 16 of the total of 18 numbers tested disintegrate completely.

In vitro Dissolution Study15,29

Dissolution profiles of norfloxacin dispersible tablets were determined using the USP 24 Method II with paddle speed 50 rpm. Dissolution was performed in 900 ml of 0.1N Hcl maintained at 37 ± 0.5°C. 5 ml of samples were withdrawn at specified time intervals. The volume of dissolution fluid was adjusted to 900 ml, by replacing each 5 ml aliquot withdrawn with 5 ml of 0.1N Hcl, pre-warmed at 37± 0.5°C. Samples withdrawn were filtered through whatmann filter paper, suitably diluted with 0.1N Hcl and analyzed at 274 nm.

Stability study8,35

Stability of a pharmaceutical preparation can be defined as "the capability of a particular formulation in a specific container/closure system to remain within its physical, chemical, microbiological, therapeutic and toxicological specifications throughout its shelf life."

The purpose of stability testing is to provide evidence on how the quality of a drug substance or drug product varies with time under influence of a variety of environmental factors such as temperature, humidity and light, and enables recommended storage conditions,test periods and shelf-lives to be established.

ICH specifications for stability study:

Long term testing: 250C ± 20C /60% RH ± 5% RH for 12 months.

Accelerated testing: 400C ± 20C /75% RH ± 5% RH for 6 months.

Procedure

In the present study, stability studies were carried out at 40 0C and 75% RH for a specific time period up to 90 days for all formulations. For stability study, the tablets were sealed in aluminium packaging coated inside with polyethylene. These sample containers were placed in oven.

Evaluation of samples

The samples were analyzed for the following parameters

Evaluation:

Appearance: The samples were checked for any change in colour at every week

Hardness: The samples were tested for hardness at every week.

Drug content: The samples were checked for drug content.

Disintegration time: The samples were subjected to disintegration time studies.

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