Sunitha HS. et al. / International Journal of Research in Pharmaceutical and Nano Sciences. 4(2), 2015, 72 - 84.

Research Article CODEN: IJRPJK ISSN: 2319 – 9563

International Journal of Research

in
Pharmaceutical and Nano Sciences
Journal homepage: www.ijrpns.com

DEVELOPMENT AND EVALUATION OF CAPTOPRIL FAST DISINTEGRATING

OR DISSOLVING TABLETS BY COMPLEXATION TECHNIQUES USING GUAR
GUM AS A SUPERDISINTEGRANT

Sunitha H S1*, S. Parthiban1, A. Vikneshwiri2, G.P. Senthil kumar3, T. Tamiz Mani4

1
*Department of Pharmaceutics, Bharathi College of Pharmacy, Bharathinagara, Mandya, Karnataka-571422, India.
2
Department of Pharmacy Practice, Bharathi College of Pharmacy, Bharathinagara, Mandya, Karnataka-571422, India.
3
Department of Pharmaceutical Chemistry, Bharathi College of Pharmacy, Bharathinagara, Karnataka-571422, India.
4
Department of Pharmacognosy, Bharathi College of Pharmacy, Bharathinagara, Mandya, Karnataka-571422, India.

ABSTRACT
The aim of the present study was an attempt to formulate and evaluate taste masked fast disintegrating tablets
of Captopril to increase the palatability and bioavailability of the drug. Fast disintegrating tablets of Captopril were
prepared by direct compression method using β-cyclodextrin as a complexing agent to mask the bitter taste of
Captopril. Guar gum as natural super disintegrants was used in different concentration 2.5 mg, 5 mg, 7.5 mg, 10 mg
respectively. The Captopril - β-cyclodextrin complex were characterized by FT-IR, DSC and XRD. Compatibility
studies by FT-IR showed no significant interactions between drug and excipients. DSC and XRD analysis
confirmed the formation of complex for taste masking. The developed tablet formulations were evaluated for pre
compression and post compression parameters which complied official limits. Among all the formulations,
formulation F4 containing guar gum 10 mg gives best disintegration and dissolution profile compared with other
formulations, showed drug release of 99.86±0.54 % with 12 min and disintegration time 50.16±1.32 sec. From this
study we concluded that the formulated tablets of Captopril containing guar gum of concentration 10 mg was better
and effective than conventional tablets to meet patient compliance along with fast relief from hypertension.

KEY WORDS
Captopril, β-cyclodextrin, Fast disintegrating tablets and Superdisintegrants.

INTRODUCTION
Author of correspondence:
The major problem faced by the patients with
Sunitha H S,
conventional tablet dosage form is difficult in
Department of Pharmaceutics,
taking medicine; hence patients may not comply
Bharathi College of Pharmacy, Bharathinagara,
with prescription, which results in high incidence of
Mandya, Karnataka-571422, India.
ineffective therapy. With the advancement in
technology and experience, pharmaceuticals are
Email: [email protected]
prepared and administered to patients in more
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 Sunitha HS. et al. / International Journal of Research in Pharmaceutical and Nano Sciences. 4(2), 2015, 72 - 84.

compliant and efficient manner. Rapid specialities Pvt, Mumbai), microcrystalline

disintegrating tablets are the new improved dosage cellulose, magnesium stearate, mannitol (S D fine
form developed especially for the young and elderly chemical Ltd, Mumbai), aspartame (Shreeji
patients who find inability to swallow tablets and chemicals, Mumbai), talc (Loba chemical Pvt. Ltd.
capsules due to under developed muscular, nervous Mumbai). All the other solvents, reagents and
system and dysphagia. This solid dosage forms chemicals used were of either pharamcopoeial or
dissolves or disintegrate rapidly in oral cavity, analytical grade.
resulting in solution and suspension that can be Methods
swallowed without need of water .When this type of Compatibility studies4
tablet is placed in mouth, the saliva serves to Compatibility studies by Fourier transformer
rapidly dissolve the tablet usually in about 30 sec. infra-red spectroscopy (FTIR)
The critical formulation problem in making such Infra-red spectra of drug and inclusion complexes
type of dosage form is the taste masking of bitter were recorded by KBr method using Fourier
taste associated with most of the drugs and this can transformer infra-red spectrophotometer (IR-
be overcome by taste masking technique such as Affinity-1, Shimadzu, Japan). A base line
polymer coating, complex formation, granulation, correction was made using dried potassium bromide
microencapsulation and use of ion exchange resins1. and then spectra of dried mixtures of drug and
Captopril is widely used antihypertensive drug but inclusion complexes with potassium bromide were
it is very bitter. Captopril is poorly absorbed recorded.
followed an oral dose leads to poor bioavailability. Preparation of inclusion complexes by physical
Therefore, to provide this drug in a more accessible mixture method5, 6
and patient compliant form and to overcome such Inclusion complexes were prepared by physical
problems, in the present study we plan to mask the mixture method, in this method Captopril and β-
bitter taste by complexation technique and Cyclodextrin were accurately weighed in different
formulate into a rapid disintegrating tablet using molar ratios viz. 1:1 and 1:3 separately and blended
natural superdisintegrant. The physicochemical thoroughly by triturating in a mortar at 20 °C for
properties of Captopril are water soluble drug about 30 min. The powder mixtures were then
having plasma half-life of 2 hrs, make it suitable pulverized through sieve no.80 and stored in
candidate to formulate buccal disintegrating desiccator till further use.
tablets2. Characterization of Captopril inclusion
On the basis of these considerations, in this study, complexes7
we aim to formulate rapidly disintegrating tablets of Inclusion complexes of Captopril were
Captopril using natural superdisintegrant, since characterized by following analytical techniques.
synthetic superdisintegrants are expensive, have Estimation of drug content
environment related issues, need long development The quantities of inclusion complexes equivalent to
time for synthesis. However, the use of natural 25 mg of Captopril were dissolved in water.
superdisintegrants in pharmaceutical application is Appropriate dilutions were made and filtered. The
attractive because they are economic, readily drug content of each complex was calculated.
available, non-toxic and potentially degradable3. Differential Scanning Calorimetric analysis
(DSC)
MATERIALS AND METHODS The study was performed using DSC model
Materials (Mettler DSC 823, Germany). For this study, the
Captopril (Micro labs, Bangalore), β-cyclodextrin samples were placed in a platinum crucible and the
(Rolex chemical industries, Mumbai), Psyllium thermograms were recorded at a heating rate of 10
husk (Abbott Pvt, Ltd), guar gum (Merck °C/min in the range of 20 °C to 310 °C. Inert

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atmosphere was maintained by purging nitrogen gas varying the weight of MCC. The prepared tablets
at a flow rate of 10 ml/min. were evaluated for various parameters.
X-Ray diffraction (XRD) study Pre-compression parameters9-11
The X-Ray diffraction pattern of the selected The flow properties of the powder are vital for the
inclusion complexes was compared with that of the performance of the tablet. Hence, the flow
pure Captopril. This was done by measuring 2ϕ in properties of the powder were analyzed before
the range of 4 to 50° with reproducibility of compression to tablets. The powder mixture of
±0.001° on a diffractometer (Rigaku Co. Tokyo, different formulation were evaluated for angle of
Japan). The XRD patterns were recorded repose, bulk density, tapped density,
automatically using rate meter with constant of 2 × compressibility index, hausner’s ratio, and obtained
102 pulse /sec and with the scanning speed of 2° values were within the prescribed limits of IP.
(2ϕ)/min. Post-compression parameters12- 15
Dissolution studies of Captopril and its inclusion After tablet compression, all the tablets were
complexes evaluated for different parameters as follows.
The Dissolution study of inclusion complex Hardness and Thickness
(equivalent to 25 mg Captopril) and pure drug was The hardness was tested using Monsanto hardness
performed using USP dissolution test apparatus tester. The force was measured in kilograms per
type II with 900 ml of phosphate buffer pH 7.4. The centimeter square (kg/cm2). Thickness of tablets
stirring speed employed was 50 rpm, and the was measured by digital caliper.
temperature was maintained at 37 ± 0.5 °C. 5 ml Friability Test
aliquots of dissolution medium was withdrawn at The friability of the tablets was determined using
predetermined time intervals and replaced by same Roche friabilator. The % friability was then
volume of fresh dissolution medium. The filtrates of calculated using the formula:
the samples were analyzed for the content of drug Initial weight − final weight
by UV spectrophotometer at 205 nm. Cumulative % Friability = -------------------------------------×100
percent drug released was determined at each time Initial weight
point. Weight variation test
Formulation development of fast dissolving Twenty tablets were randomly selected from each
tablets by direct compression method8 formulation, individually weighed, the average
Fast disintegrating tablets were prepared using β- weight and standard deviation was calculated. The
CD inclusion complex of Captopril by direct percentage difference in the weight variation should
compression method. Captopril: β-CD were taken be within the permissible limits (±7.5%). The total
and mixed with directly compressible diluent, weight of tablets formulated was 200 mg.
super-disintegrants and other excipients in a plastic % Drug content determination
container. The formula included variable amount of Twenty tablets were powdered; 25 mg equivalent
superdisintegrants and other excipients. The weight of Captopril in tablet powder was accurately
resulting powder blends were evaluated for flow weighed and transferred into a 100 ml volumetric
parameters. The powder blends equivalent to 25 mg flask. Initially, 50 ml of phosphate buffer (pH 7.4)
of drug were directly compressed into tablets using was added and shaken for 10 min. Then, the volume
8 mm flat- faced round punches of 8 station was made up to 100 ml with phosphate buffer. The
compression machine. The natural superdisintegrant solution in the volumetric flask was filtered, diluted
used was guar gum in concentration range of 2.5 suitably and analyzed spectrophotometrically at 205
mg, 5.0 mg, 7.5 mg and 10 mg. Table No.1 gives nm. The drug content in each tablet was calculated
composition of these tablet formulation. Final using the standard calibration curve of Captopril in
weight of each tablet was kept constant (200 mg) by phosphate buffer pH 7.4 solution.

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In-vitro dispersion Time RESULTS AND DISCUSSION

Tablet was added to 10 ml of phosphate buffer Drug -polymer compatibility by FTIR studies
solution pH 7.4 (pH of saliva) in a petridish at The IR spectral analysis of Captopril and the
37±0.5°C. Time required for complete dispersion of physical mixture of Captopril and other excipients
tablet was measured. are presented in Figure No.1, 2 respectively. Pure
Wetting time and Water absorption ratio Captopril spectra showed principal peaks at
Wetting time of dosage form is related to the different wave numbers corresponding to its
contact angle. It needs to be assessed to give an functional groups, confirming the purity of the drug
insight into the disintegration properties of the as per established standards. The IR spectra of
tablets; a lower wetting time implies a quicker Captopril exhibited peak at 3000 cm–1 1747 cm–1,
disintegration of the tablet. For this purpose, a piece 1041 cm–1, 2877 cm–1 (O-H Stretching, C=O
of tissue paper folded twice is placed in a small Stretching, C−N Stretching, C−H Stretching). The
petridish containing 6 ml of water. Eosin, a water IR spectra of β-CD showed prominent absorption
soluble dye, is added to petridish. A tablet is kept bands at 3377 cm–1 (O-H stretching). The FTIR
on the paper and the time for complete wetting is spectra of inclusion complexes seemed to be only
measured. Water absorption ratio, R is then summation of drug and β-CD spectra. This result
determined according to the following equation. suggested that there was no chemical interaction
R = 100 × (wa - wb) / wb between drug and β-CD in their combination. All
Where, the above characteristic peaks appear in the spectra
wb and wa are tablet weights before and after water of physical mixture of inclusion complex of
absorption. Captopril and other excipients, indicating no
In-vitro drug release modification or interaction between the drug and
The in-vitro dissolution study was carried out using excipients.
USP dissolution test apparatus type II. The Characterization of Captopril inclusion
dissolution medium consisted of 900 ml of pH 7.4 complexes
phosphate buffer solution maintained at 37 ± 0.5 °C Estimation of drug content
and stirred at 50 rpm. Aliquot samples (5 ml) were The drug content of Captopril inclusion complex
withdrawn every minute, filtered through a 0.45 µm with different ratio (1:1, 1:3) was found to be 99.54
membrane filter and replaced by an equivalent ± 0.56 % to 99.97 ± 1.09 % respectively. The drug
volume of fresh dissolution medium. The samples content of Captopril inclusion complexes was
were suitably diluted with phosphate buffer pH shown in Table No.2.
(7.4) and the amount of the drug dissolved was Differential Scanning Calorimetric analysis
analyzed spectrophotometrically at 205 nm. The (DSC)
cumulative percentage drug release was calculated. The DSC thermogram of pure Captopril showed
Stability Studies16, 17 sharp endothermic peaks at 109°C (Figure No.3).
Accelerated stability studies were performed for 6 The absence of sharp endothermic peak in
months as per ICH guidelines. The optimized Captopril-β-CD inclusion complexes (Figure No.4)
formulation (F4) was kept at 40 ± 2 °C and 75 ± 5 suggesting complete complex formation.
% RH. Physical appearance, hardness, % drug X-Ray diffraction (XRD) study
content, In-vitro dispersion time and In-vitro drug Captopril in pure form and inclusion complex of
release were fixed as parameters for stability drugs with β-CD prepared by physical mixture was
testing. subjected to XRD analysis and the results were
depicted in Figure No.5 and 6. From the figure, it
was evident that diffraction pattern of the pure drug
shows its highly crystalline nature indicated by

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numerous distinctive peak. On the other hand XRD friability of all the formulated tablets of Captopril
of inclusion complex showed significant decrease in was found to be in the range 0.42 to 0.58 %. The
degree of crystallinity as evident from weight variation and percentage deviation from the
disappearance of sharp distinctive peaks, suggesting average weight were found to be within (±7.5) the
probable transformation of crystalline form into an prescribed official limits.
amorphous state. % Drug content
Dissolution The drug content of all the formulations of
The Captopril and inclusion complex of different Captopril fast disintegrating tablets were found to
ratio (1:1, 1:3) were evaluated for in-vitro be within the range of 99.95 ± 0.7 to 100.30 ± 1.01
dissolution studies in pH 7.4 buffer and the results % which were within the limits of IP specifications.
were shown in the Table No.3. The release of The drug content of all the formulations of
Captopril was increased with increasing Captopril tablets was shown in Table No.6.
concentration of β-CD with pure drug as standard. In-vitro dispersion time
Formulation developments The in-vitro dispersion time of all the formulation
Fast disintegrating tablets of Captopril were prepared were found to be 50.16 ± 1.32 to 56.0 ± 2.28 sec.
by complexation technique using direct compression The results were showed in Table No.6.
method and by using an 8 mm flat- faced punch of 8 Photographs of in-vitro dispersion time were shown
station compression machine. Guar gum was used as in Figure No.7.
superdisintegrants. MCC and mannitol was used as Wetting time
diluent. Magnesium stearate and talc were added to The wetting time of all the formulations (F1-F4)
the above blend as flow promoters. were found to be within 3.27 ± 2.26 to 3.54 ± 1.47
Evaluation of Captopril fast dissolving tablets mins, which complies with the official
Pre-compression parameters specifications. The results were showed in Table
The powder blends were also evaluated for various No. 6. Photographs of wetting time of formulation
pre-compression parameters. The results were F4 was shown in Figure No.8.
shown in Table No.4. Bulk densities of powder Water absorption ratio
blends were found between 0.43 ± 0.01 to 0.44 ± The water absorption ratio of all the formulated
0.01 gm/ml. Tapped densities of powder blends batches was found to be in the range 55.81 ± 1.47 to
were found between 0.51 ± 0.01 to 0.52 ± 0.00 68.50 ± 2.24 which was satisfactory in giving
gm/ml. The angle of repose values varied from effective and better formulations of fast
26.84 ± 0.48 to 28.93 ± 0.59. Carr’s index values disintegrating tablets. The results were shown in
were found to be in the range of 13.46 ± 1.0 to Table No.6.
15.38 ± 0.29 %. Haunser’s ratio values were found In-vitro dissolution study
to be in the range of 1.16 ± 0.01 to 1.17 ± 0.005. The tablets were evaluated for in vitro dissolution
From these values it was evident that all these studies in pH 7.4 buffer and the results were shown
blends had excellent flow properties. in the Table No.7 and in the Figure No.9. The
Post-compression parameters formulations F1-F4 were formulated with the help
The formulated tablets were evaluated for various of guar gum in concentration 2.5 mg, 5.0 mg, 7.5
post-compression parameters. The results were mg, 10 mg respectively. The in-vitro release of
shown in Table No.5. The thickness of the batch Captopril from fast disintegrating tablets was found
from F1-F4 was found to be in the range of 3.67 ± to vary according to the type and ratio of
0.045 to 3.74 ± 0.09 mm. The hardness was superdisintegrants used. The release of Captopril was
uniformly maintained for all formulation and it was increased with increasing concentration of guar gum
found to be 3.83±0.258 to 4.0±0.0 kg/cm2. Thus, and guar gum.
tablets were having good mechanical strength. The

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The percentage of the drug released from the concentration of superdisintegrant and t50, t70, t90
formulations F1, F2, F3, F4 were found to be 94.94 ± values decreased with increase in the concentration
0.028 %, 97.66 ± 0.64 %, 100.17 ± 1.14 %, 99.86 ± of gaur gum. From the dissolution parameter it was
0.54 % respectively. More than 90% of the drug was evident that the formulation F4 achieved maximum
released from F1-F4 formulations in between 8 - 12 dissolution efficiency of 75.72 % for D5 and 97.8 %
mins. for D10 and lowest t50, t70, t90 values of 3.10 min,
Among the different formulation the F4 which 4.30 min and 5.0 min respectively.
contain the 10 mg guar gum achieved more than 90 Stability studies16, 17
% drug release within 8 min. These results Accelerated Stability studies were carried out at 40
suggested that formulation containing 10 mg guar ± 2 °C and 75 ± 5 % RH for the optimized
gum have faster disintegrating effect. formulation F4 and monitored for physical
Various dissolution parameters values viz., Percent appearance, hardness, drug content, in-vitro
drug dissolved in 5 and 10 min (D5 and D10), Time dispersion time and dissolution profile study and
taken to dissolve the 50%, 70% and 90% drug (t50, found to stable for all the different parameters. The
t70, t90 respectively) were given in the Table No.8. results are shown in Table No.9.
From the results it was observed that percent drug
dissolves was increased by increasing the
Table No.1: Formulation design of Captopril fast disintegrating tablets
S.No Ingredients (mg) F1 F2 F3 F4
1 Captopril and β – cyclodextrin (1:3) equivalent to 25 mg Captopril 100 100 100 100
2 Guar gum 2.5 5.0 7.5 10
3 MCC 57.5 55 52.5 50
4 Mannitol 30 30 30 30
5 Aspartame 10 10 10 10
6 Magnesium stearate 2 2 2 2
7 Talc 2 2 2 2
8 Total weight 200 200 200 200

Table No.2: % Drug content of inclusion complex

S.No Ratio of drug and β-cyclodextrin % drug content
1 1:1 99.54±0.56
2 1:3 99.97±1.09

Table No.3: In-vitro dissolution study of inclusion complex and pure drug
% Cumulative drug release
S.No Time (min) Pure drug %
1:1 1:3
1 0 0 0 0
2 0.5 1.28±1.42 1.51±1.11 2.53±0.67
3 1 5.32±1.08 7.82±1.25 12.87±0.85
4 2 12.2±0.78 14.57±1.02 20.55±1.19
5 4 27.55±1.18 28.64±0.90 35.53±1.68
6 6 44.88±0.91 49.25±0.76 54.21±1.05
7 8 52.44±0.56 54.56±0.81 61.47±0.64
8 10 66.79±1.19 69.12±0.89 74.16±0.94

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Table No.4: Pre compression parameters of Captopril tablets

Formulation Bulk density Tapped Angle of Carr’s index Haunser’s
S.No
Code (g/cc) Density (g/cc) repose (ө) % ratio
1 F1 0.44±0.01 0.52±0.01 28.93±0.59 15.38±0.29 1.17±0.005
2 F2 0.44±0.01 0.52±0.01 27.15±0.52 13.46±0.26 1.16±0.01
3 F3 0.43±0.01 0.51±0.01 27.77±0.45 14.92±0.85 1.17±0.01
4 F4 0.44±0.00 0.52±0.00 26.84±0.48 15.28±0.16 1.17±0.005
Value expressed as mean ±SD, n=3
Table No.5: Post compression parameters of Captopril tablets
*Hardness *Thickness Friability **Weight
S.No Formulation Code
(kg/cm2) (mm) (%) Variation (%)
1 F1 4.0±0.0 3.67±0.045 0.42 0.019±0.69
2 F2 3.91±0.204 3.75±0.065 0.49 0.102±0.83
3 F3 3.83±0.258 3.72±0.048 0.58 0.064±0.80
4 F4 3.91±0.204 3.74±0.09 0.55 0.161±0.78
Value expressed as mean ±SD,* n=6, **n=20
Table No.6: Results of % drug content In vitro dispersion time, wetting time and water absorption ratio
of Captopril tablets
In vitro dispersion Wetting Water absorption
S.No Formulation Code % Drug content
time (sec) time (min) ratio (%)
1 F1 99.95±0.70 56.0±2.28 3.53±2.59 55.81±1.47
2 F2 100.03±1.14 54.33±2.73 3.48±2.42 59.93±1.90
3 F3 99.96±1.18 52.83±2.56 3.54±1.47 62.22±1.35
4 F4 100.43±0.90 50.16±1.32 3.27±2.26 68.50±2.24
Value expressed as mean ±SD, n=3
Table No.7: In-vitro release study of formulations F1-F4
% Cumulative drug release
S.No Time (min)
F1 F2 F3 F4
1 0 0 0 0 0
2 0.5 2.55±0.14 5.32±0.66 9.84±0.36 15.32±0.38
3 1 9.82±0.25 12.87±0.24 22.06±0.51 29.05±0.53
4 2 14.15±0.73 18.21±0.67 38.34±1.26 43.96±0.73
5 4 35.53±0.32 37.85±0.31 53.08±0.32 66.14±0.39
6 6 67.79±0.96 70.93±0.49 72.7±0.77 80.71±0.50
7 8 77.09±0.73 82.24±0.31 84.05±0.95 91.64±0.57
8 10 85.74±0.44 88.8±0.81 95.25±0.50 97.80±0.37
9 12 94.94±0.69 97.66±0.47 100.17±1.14 99.86±0.54
Table No.8: In-vitro dissolution parameters of different formulations
S.No Formulation DE5 (%) DE10 (%) T50 (min) T70 (min) T90 (min)
1 F1 50.91 85.74 6 8 11
2 F2 55.2 88.8 4.42 5.54 10.30
3 F3 60.9 95.25 3.42 5.48 6.0
4 F4 75.72 97.8 3.10 4.30 5.0
DE5= Percent drug dissolved in 5 min, DE10= Percent drug dissolved in 10 min, t50 = Time taken to dissolve 50% of the drug, t70 =
Time taken to dissolve 70% of the drug and t90 =Time taken to dissolve 90% of the drug.
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Table No.9: Stability studies for the formulation F4

Time (months)
S.No Specification Parameters
0 3 6
Hardness* (kg/cm2) 3.91±0.204 3.91±0.35 3.94±0.28
40±2 °C and 75±5% Drug content** (%) 100.12±1.21 100.09±0.12 100.07±0.16
1
RH Dispersion**time(sec) 50.33±0.97 51.29±1.12 50.48±1.16
Cumulative % drug release** 99.84±0.18 99.81±0.24 99.78±0.31
Value expressed as mean ±SD, *n=6, **n=3

Figure No.1: IR spectra of Captopril

Figure No.2: IR spectra of physical mixture of Captopril, β-cyclodextrin and guar gum
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DSC Thermal Analysis Result

mW

0.00
Captopril.Drug.tad DSC

-10.00
Peak 109.79 C
Onset 105.46 C
File Name: Captopril.Drug.tad
Detector: DSC-60 Endset 116.25 C
Acquisition Date 15/03/06
-20.00 Heat -781.09 mJ
Acquisition Time 12:32:40(+0530)
Sample Name: Captopril.Drug -260.36 J/g
Sample Weight: 3.000[mg]
Annotation:

-30.00

-40.00
50 100 150
Temp [C]

Figure No.3: DSC thermo graph of pure drug Captopril

DSC Thermal Analysis Result

mW

0.00 Captopril + B Cyclodextrin.tad DSC

-5.00 File Name: Captopril + B Cyclodextrin.tad

Detector: DSC-60
Acquisition Date 15/03/06
Acquisition Time 12:46:17(+0530)
Sample Name: Captopril + B Cyclodextrin
Sample Weight: 3.000[mg] Peak 128.03 C
Annotation:
Onset 120.69 C
Peak 110.25 C Endset 136.17 C
-10.00
Onset 99.96 C Heat -141.54 mJ
Endset 116.61 C -47.18 J/g

Heat -51.20 mJ
-17.07 J/g

50 100 150
Temp [C]

Figure No.4: DSC thermo graph of pure drug and β-cyclodextrin

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Figure No.5: X-Ray diffraction pattern study of Captopril

Figure No.6: X-Ray diffraction pattern study of Captopril and β-cyclodextrin

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 Sunitha HS. et al. / International Journal of Research in Pharmaceutical and Nano Sciences. 4(2), 2015, 72 - 84.

at 5 sec at 50.16 sec

Figure No.7: In-vitro dispersion of F4

at 0 min at 3.27 min

Figure No.8: Wetting of formulation F4
100
% Cumulative drug release

80

60

40

20

0
0 2 4
Time6(min) 8 10 12

Figure No.9: In-vitro release profile of formulation F1-F4

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CONCLUSION of BCS class II pharmaceuticals by non-aqueous

The tablets were evaluated for various parameters granulation technique, IJPRD, 1(12), 2012, 1-
like hardness, thickness, friability, weight variation, 12.
% of drug content, wetting time, water absorption 5. Gawali V U, Patilp B, Chede S M, Jagdale S C.
ratio, in-vitro dispersion time, in-vitro dissolution Studies on Cilostazol and β-cyclodextrin
studies confirmed that the results were within the inclusion complexes, IJPRIF, 1(4), 2009, 1073-
specified limits. The in-vitro release of Captopril 1078.
from fast disintegrating tablets was found to vary 6. Mukesh Chandra Sharma, Smita Sharma.
according to the type and concentration of Preparation, physicochemical characterization,
disintegrants used. The drug release was increased dissolution, formulation and spectroscopic
with increasing disintegrants concentration. Among studies of β-cyclodextrins inclusion complex,
all the formulation, the formulation F4 was showed Int J Chem Tech Res, 3(1), 2011, 104-111.
99.86 ± 0.54 % drug release within 12 min and it 7. Kolhe S R, Chaudhari P D, More D M.
showed dispersion time 50.16 ± 1.32 sec. Stability Development and evaluation of melt-in-mouth
studies of selected formulation F4 showed that, tablets by sublimation technique, IJPSR, 2(1),
negligible changes in hardness, % drug content, in- 2011, 65-76.
vitro dispersion time and in-vitro drug release 8. Venkateswarlu B S, Margret Chandira R, Talele
revealed that the tablets were stable on storage Ajay, Debjit Bhowmik. Formulation
condition. From the present study, it can be development and evaluation of fast dissolving
concluded that natural superdisintegrants like guar tablets of Carvedilol, J Chem Pharm Res, 2(1),
gum showed better disintegrating property. 2010, 196-210.
9. Sunil Kumar Reddy B, Shubhrajit Mantry, Anil
ACKNOWLEDGEM ENT Kumar S, Satheesh Kumar E. Development and
The authors wish to express their sincere gratitude evaluation of fast disintegrating tablets of
to Department of Pharmaceutics, Bharathi College Granisetron hydrochloride with natural and
of Pharmacy, Bharathinagara, Mandya, Karnataka, synthetic polymers, AJPTS, 3(1), 2013, 8-18.
India for providing necessary facilities to carry out 10. Narasimha Rao N, Radian Krishna Murthy B,
this research work. Rajasekhar D, Suri Babu P, Phaneendra Babu
K, Srinivasa Babu P. Design and development
CONFLICT OF INTEREST of Amlodipine besylate fast dissolving tablets
We declare that we have no conflict of interest. by using natural superdisintegrants, IJRPB,
1(2), 2013, 175-179.
REFERENCES 11. Dineshmohan S, Vanitha K, Ramesh A,
1. Shishu, Bhatti A. Fast disintegrating tablets of Srikanth G. Formulation and evaluation of
Diazepam, Indian drugs, 43(8), 2006, 643-648. Salbutamol sulphate fast dissolving tablet,
2. Dumbare A S, Shelke P V, Gadhave M V, IJRPBS, 1(2), 2010, 105-118.
Gaikwad D D. Formulation and evaluation of 12. Hindustan Abdul Ahad, Anuradha C M, Chitta
mouth dissolving tablets of Captopril, Suresh Kumar, Kishore Kumar Reddy B. Novel
International Journal of Universal Pharmacy approach in formulation and evaluation of
and Life Science, 3, 2012, 748-759. mouth dissolving tablets of Ondansetron
3. Dourroumis D. Practical approaches of taste hydrochloride, IJABPT, (2), 2010, 582-588.
masking technologies in oral solid forms, 13. Lavande J P, Ade R N, Jaiswal S B, Chandewar
Expert Opin Drug Deliv, 4(4), 2007, 417-426. A V. Evaluation and optimization of
4. Venkat B. Yadav, Adhikrao V. Yadav. Olmesartan medoxomil tablet using synthetic
Enhancement of solubility and dissolution rate

Available online: www.uptodateresearchpublication.com March – April 83

 Sunitha HS. et al. / International Journal of Research in Pharmaceutical and Nano Sciences. 4(2), 2015, 72 - 84.

and natural superdisintegrants, Int J Pure App Hydrochlorothiazide as a model drug, RJPT,
Biosci, 1(5), 2013, 19-29. 1(4), 2008, 349-352.
14. Basawaraj S Patil, Upendra Kulkarni, Parik 16. Deshmukh V N, Zade N H, Sakarkar D M.
bhavik, Srinivas R Soodam. Formulation and Development and evaluation of orally
evaluation of mouth dissolving tablets of disintegrating tablet by direct compression
Nimesulide by new compressed technique, method, Int J Pharm Tech Res, 4(4), 2012,
RJPBCS, 1(4), 2010, 587-592. 1351-1357.
15. Uday S Rangole, Kawtikwar P S and Sakarkar 17. Sanjay Bajaj, Dinesh Singla and Neha Sakhuja.
D M. Formulation and in-vitro evaluation of Stability test of pharmaceutical products, JAPS,
rapidly disintegrating tablets using 2(3), 2012, 129-138.

Please cite this article in press as: Sunitha H S et al. Development and Evaluation of Captopril Fast
Disintegrating or Dissolving Tablets by Complexation Techniques using Guar Gum as a Superdisintegrant,
International Journal of Research in Pharmaceutical and Nano Sciences, 4(2), 2015, 72 - 84.
Available online: www.uptodateresearchpublication.com March – April 84