10mg concentrations were prepared (shown in Table) and

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10mg concentrations were prepared (shown in Table) and

10mg
of pure drug was dissolved in 10ml methanol (primary stock solution – 1000
µg/ml). From this primary stock solution 1 ml was pipette out into 10 ml
volumetric flask and made it up to 10ml with the media (Secondary stock
solution – 100µg/ml). From secondary stock solution again 1ml was taken it in
to another volumetric flask and made it up to 10 ml with media (working
solution – 10µg/ml). The working solution was taken for determining the
wavelength.

 b) Determination of Calibration Curve:

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10mg of pure drug was dissolved in 10ml methanol
(primary stock solution – 1000 µg/ml). From this primary stock solution 1 ml
was pipette out into 10 ml volumetric flask and made it up to 10ml with the
media (Secondary stock solution – 100µg/ml). From secondary stock solution
required concentrations were prepared (shown in Table) and those concentrations
absorbance was found out at required wavelength.

 

2.5. Evaluation of
Nanosuspension:

2.5.1. Drug Content: Accurately
weighed amount of each preparation dissolved in required amount of methanol and
diluted suitably in pH 6.8 phosphate buffer. The drug content was determined
spectrophotometrically at required wavelength. Calculation was done using
following formula

2.5.2. Determination of
Nanosuspension Percentage Yield:

The
Nanosuspension production yield was calculated by gravimetry. Fixed volumes of
nanoparticles suspension were centrifuged (15,000×g, 30 min, 15ºC) and
sediments were dried.

The
percentage yield was calculated as follows:

 

 

 

 

2.6.
In Vitro
Drug Release Studies:

Dissolution
test was carried out in USP rotating basket dissolution apparatus. Employing
the stirrer speed at 100 rpm and Phosphate buffer pH 6.8 as dissolution medium
(900ml), at fixed time intervals 5 ml of the aliquot was withdrawn and same
quantity was replaced by fresh buffer. The withdrawn samples were
spectrophotometrically analyzed at respective wavelength on Lab India UV3000+.

2.7. Drug and Excipient Compatability
studies by FTIR:     

The compatibility between the pure drug and excipients was
detected by FTIR spectra obtained on Bruker FTIR Germany(Alpha T).The solid
powder sample directly place on yellow crystal which was made  up of ZnSe. The spectra were recorded over
the wave number of 4000 to 400cm-1.

2.8. Differential
Scanning Calorimetry:

DSC
scans of prepared dried powdered drug sample, pure drug and physical mixture
were recorded using DSC–Hitachi 7020 with muse software. All samples were
weighed (8-10mg) and heated at scanning rate of 10oC/min under dry
nitrogen flow (50ml/min). Aluminium pans and lids were used for all samples.

2.9. Scanning Electron
Microscopy:

The
shape and surface morphology of Nanoparticle were investigated using Scanning
Electron Microscopy (SEM). The samples for SEM study were prepared by lightly
sprinkling the formulation on a double-adhesive tape stuck to an aluminium
stub. The stubs were then coated with gold to a thickness of ~300 Å under an
argon atmosphere using a gold sputter module in a high vacuum evaporator. The
coated samples were then randomly scanned and photomicrographs were taken with
a scanning electron microscope.

2.10. In VivoStudies:

2.10.1. Bioavailability
studies in Wistar rats:

Male
Wistar rats (body weight 200 ± 20 g) were supplied by the Experimental Animal
Center of Local Vendor and the animal experiment was evaluated and approved by
the Animal Ethics Committee. All rats were divided randomly into two groups of
?ve animals each and were housed in cages for at least three days prior to the
beginning of the study and had free access to food and water. Food was with-
drawn 12 hr prior to the beginning of the study. Nano Suspension Optimised
Formulation was orally administrated to group of rats.

 

GLYBURIDE

 In the
present work Glyburide is an antidiabetic drug in a class of medications known
as sulfonylureas.It is an
oral diabetes medicine that helps control blood sugar levels. Drug used in
treatment of type 2 diabetes. Glyburide belongs to class II of the
BCS.Class II drugs having High Permeability, Low Solubility Means Class II
drugs have a high absorption number but a low dissolution number. An attempt
has been made to improve the bioavailability Present it is in the form of Nano
Suspension.

3. Results and
discussion:

3.1. Physical Properties

                                                Table 3: Physical
Properties of drug

S. No

Parameter

Drug(Glyburide)

1.

Colour

White

2.

Appearance

Solid
Powder

 

2. Melting Point

 

Melting point was determined by
capillary tube method and it was found to be 169°C, Glyburide. This value is
same as that of the literature citation shown in Table.

 

Table: Melting
Point determination of drug

 

Drug Name

Reported melting point

Observed Melting point

Glyburide

170 °C

169 °C

 

 

 

3. Solubility studies

According to
pharmacopoeias limits it is insoluble in water, 6.8 phosphate buffer. The results were shown in Table.

 

                                                            Table
4: Solubility Studies

Medium

mg/100ml

Water

Insoluble

Phosphate buffer pH(6.8)

Very
slightly soluble

Methanol

Soluble

Chloroform (CHCL3)

Soluble

 

 

Analytical Method for Glyburide:

It was found that the estimation of Glyburide using UV spectrophotometric method
at ?max242 nm in pH 6.8 phosphate buffer. It had good
reproducibility and this method was used in the study.

 

 

 

 

                        Figure: Wave scan of Glyburide in 6.8 Phosphate buffer

Glyburide Standard graph in 6.8 Phosphate buffer
(? max 242 nm)

S.No

Concentration (µg/mL)

Absorbance

1

0

0

2

5

0.148

3

10

0.334

4

15

0.497

5

20

0.679

6

25

0.856

Table 5: Standard graph
values of Glyburide in 6.8
Phosphate buffer

 

 

 

 

 

Fig1  :
Standard graph of Glyburide in 6.8 Phosphate Buffer

Evaluation of Nanosuspension:

Table 6: Drug
content and % Yield of Nanosuspension

Formulation
Code

Drug
content

% Yield

F1

78.62±0.24

75.69±1.29
 

F2

96.38±0.84

95.45±0.32
 

F3

87.47±1.41

90.11±1.63

F4

75.23±0.59

80.32±0.90
 

F5

79.66±0.45

84.13±0.34
 

F6

92.84±0.57

89.42±0.91
 

 

 

Figure2
:Drug content of Nanosuspension

                                                                                                  

Figure3 :Percentage Yield of Nanosuspension

Drug
content: From the Table,
All the formulations drug content was found to be in the
range of 75.23±0.59 
to 96.38±0.84.

Percentage
Yield: From the Table,
The entire formulations percentage yield was found to be in the range of 75.69±1.29 to 95.45±0.32.

In
vitro
drug release studies :

Table 7: Dissolution
data of Nanosuspension

Time (Min)

F1

F2

F3

F4

F5

F6

0

0

0

0

0

0

0

5

11.26±0.49

33.42±0.76

26.75±0.12

19.67±0.62

25.68±0.65

30.45±0.26

10

24.41±1.28

45.78±0.61

30.20±1.13

29.89±0.39

34.11±0.81

38.33±0.56

15

32.56±0.91

59.42±1.28

54.12±0.79

41.1±0.48

47.1±0.65

53.35±0.41

20

49.20±0.73

66.49±0.83

60.26±1.18

54.35±0.14

58.4±0.23

69.33±0.54

30

59.46±0.54

82.75±1.08

78.24±0.82

62.4±0.26

64.23±0.71

74.51±0.4

45

71.21±0.41

90.84±0.99

88.56±0.62

68.66±0.72

77.59±0.74

85.02±0.81

60

88.78±0.72

97.31±0.44

91.56±0.13

72.28±1.49

84.67±0.68

90.62±0.34

 

Figure 4: 
Dissolution of Nanosuspension Formulations F1-F3 having PVA as a
Stabilizer

Figure
5:  Dissolution of Nanosuspension
Formulations F4-F6 having HPMC as a Stabilizer

 

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