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ISSN: 2357-0539 (Online) Osman and Shatla, 2018, 2 (3), 191-200

Preparation and Evaluation of Rapidly Dissolving Tablet of Telmisartan

Mohamed A. Osman and Ali A. Shatla*

Department of Pharmaceutical Technology, College of Pharmacy, Tanta University, Tanta, Egypt.

*Corresponding author: Ali A. Shatla, Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta
University, Tanta, Egypt. Tel.: (+2)01001768769
E-mail address: Alishatla59@[Link]

Submitted on: 06-02-2018; Revised on: 16-03-2018; Accepted on: 21-03-2018

ABSTRACT
Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast
disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid
dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A),
polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC
E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio
(formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug
utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium
bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of
polymers. The order of enhanced dissolution of the drug in the first 5 min Q 5 (%) was: formula E > F > D5, where the %
drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was
selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the
drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a
solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of
telmisartan FDT with fast dissolution rate.

Keywords: Fast release tablets; Sodium bicarbonate; Solid dispersion; Sublingual tablet; Telmisartan

INTRODUCTION soluble2,3. According to Biopharmaceutical

Classification System (BCS), telmisartan is classified as
Telmisartan is 2-(4-{[4-methyl-6-(1-methyl- class II drug, meaning that the drug is highly permeable
1H-1, 3 benzodiazol-2-yl) -2-propyl-1H-1, 3- but poorly soluble4. The poor solubility of telmisartan
benzodiazol-1-yl methyl} phenyl) benzoic acid (Figure in biological fluids is one of its major problems which
1), approved as antihypertensive agent1. It exerts its accounts for low bioavailability that reaches 42 % after
action via competitive inhibition of the angiotensin- oral administration. It also shows high first-pass
converting enzyme (ACE) with higher selectivity for metabolism, which further reduces the oral
(AT1) than (AT2) receptor. Telmisartan shows a long bioavailability 5. Rapid dissolution in the oral cavity
duration of action with the elimination half-life provides a chance for mucosal absorption of the drug
approaching 24 h. The pharmacokinetics pattern of and avoiding presystemic disposition. The development
telmisartan after oral administration follows nonlinear of rapidly disintegrating and dissolving oral tablets has
kinetics over the dose range 20-160 mg. Telmisartan is gained interest recently. The main problem of such
readily ionizable and subsequently, the solubility is pH dosage form is the need for fast disintegration and rapid
dependent with maximum solubility observed at high drug dissolution in small volumes of saliva. The
and low pH, but in the range of pH 3-9, it is only poorly Optimizing drug dissolution rate is thus the main
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limiting factor in the formulation of these systems6. Methods

FDTs are intended for administration to patients who Calibration curve
cannot swallow, such as the elderly patients, stroke A Known amount of telmisartan (10 mg) was
victims, bedridden patients, patients affected by a renal accurately weighed, dissolved in 1.0 M NaOH and the
failure, and patients who refuse to swallow, such as volume was adjusted to 100 ml in order to obtain a
pediatric, geriatric, and psychiatric patients 7. Numerous stock solution (100 μg/ml). Different aliquots of this
studies had been carried out in order to modify the solution were diluted with 1.0 M NaOH to produce
dissolution kinetics of poorly soluble drugs to improve solutions containing 5, 7, 8, 10, 12, 15, 18 μg/ml of
their bioavailability. A common method used to telmisartan. The absorbance of these solutions was
improve the dissolution rate of a poorly water-soluble measured at 297 nm on UV-Visible spectrophotometer
drug is the formation of a solid dispersion (SD) with (Thermo Fisher Scientific, USA) against 1.0 M NaOH
hydrophilic polymers. It has also been reported that the as a blank. The calibration curve was linear as shown in
modulation of pH in dosage forms is a promising way Figure 2.
to modify the release rate of several pH-dependent and
ionizable drugs4. Accordingly, the aim of this work was
to enhance the dissolution rate of telmisartan with the
goal of formulating rapidly disintegrating oral tablets
with subsequent fast dissolution. To achieve this
objective, (SDS) of the drug was prepared using
different types of polymers and sodium bicarbonate
either alone or in combination to select the best formula
which provides higher dissolution rate of telmisartan.

Figure 2. Calibration curve of Telmisartan in water at

pH 7.5.

Preparation of solid dispersion systems (SDS)

Binary SDS of the drug with various polymers,
sodium bicarbonate or combination of polymer and
sodium bicarbonate were prepared by solvent
evaporation technique according to the composition
presented in Table 1. The drug and the polymers and/or
Figure 1. Chemical structure of Telmisartan. sodium bicarbonate were dissolved in a mixture of
(Adopted from Chivate et al., 2013) dichloromethane with methanol (20:80). The organic
solvent was removed by evaporation over a water bath
at 50 °C with continuous stirring until complete
MATERIALS AND METHODS evaporation. The residue was stored in desiccators at
room temperature for 2 days until complete drying. The
Materials dry product was ground and sieved through a 300 µm
Telmisartan was supplied from Biopharm sieve and stored in a tightly closed container.
pharmaceutical industries 6th of October city, Cairo,
Egypt. PluronicF68, Mannogem 2000USP/EP (Granular Physical characterization of the prepared
mannitol), AvicelPH102, croscarmellose sodium, formulations
crospovidone sodium, polyethylene glycol Determination of dissolution rate
4000(PEG4000), Hydroxypropyl methylcellulose The dissolution rate of telmisartan from
(HPMC E5), Gelucire 44/14, magnesium stearate and different formulations was determined using the USP II
aerosil were supplied from Sigma pharmaceutical dissolution apparatus (Coply, NG 42JY, Nottingham,
industries, Quesna, Egypt. Methyl alcohol, UK). Telmisartan (40 mg) or equivalent formulations
dichloromethane, and all other materials were obtained were exposed for 1.0 hr dissolution testing in phosphate
from EL Nasr pharmaceutical chemicals Company, buffer (pH 6.8). The dissolution medium (900 ml) was
Cairo, Egypt. maintained at 37 ± 0.5 °C and the paddle speed was
adjusted to 75 rpm. Samples were withdrawn from the
dissolution medium at predetermined intervals
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Table 1. The composition of the solid dispersion systems (SDS) and the amount of the drug dissolved in the first
five min Q5 (%)

Pluronic
Formulation Telmisartan Gelucire PEG4000 HPMC E5 NaHCO3 Aerosil **Q5 (%) + S.D
F68
Control 1 0 0 0 0 0 0 6.41 + 0.28
A1 1 1 0 0 0 0 0 8.37 + 0.89
A2 1 2 0 0 0 0 0 14.79 + 1.80
A3 1 3 0 0 0 0 0 13.05 + 1.19
B1 1 0 1 0 0 0 0 7.83 + 1.50
B2 1 0 2 0 0 0 0 9.01 + 0.74
B3 1 0 3 0 0 0 0 13.81 + 0.87
C1 1 0 0 1 0 0 0 27.05 + 2.06
C2 1 0 0 2 0 0 0 24.6 + 1.52
C3 1 0 0 3 0 0 0 24.92 + 3.60
C4 1 0 0 2 0 2 0 33.03 + 0.80
D1 1 0 0 0 1 0 0 13.90 + 1.56
D2 1 0 0 0 2 0 0 22.72 + 1.72
D3 1 0 0 0 3 0 0 21.69 + 2.53
D4 1 0 0 0 2 2 0 45.33 + 5.60
D5 1 0 0 0 2 2 1 *72.66 + 0.81
E 1 0 0 0 0 0.5 0 *88.94 + 1.31
F 1 0 0 0 0 1 0 *84.77 + 1.10

* statistically different (p-value < 0.01).

** Q5 (%) values are expressed as mean + SD. (n=3)

(5, 10, 15, 30, 45 and 60 min) and then drug recorded using FTIR spectrophotometer. Samples were
concentration was determined using UV-VIS mixed with potassium bromide (spectroscopic grade)
spectrophotometer at 297 nm using dissolution medium and compressed into disks using hydraulic press before
as a blank. An equivalent amount of fresh medium was scanning from 4000 to 400 cm-1.
added to maintain a constant dissolution volume. The
dissolution profiles were obtained as the plots of the Powder X ray diffraction (XRD)
cumulative amounts of drug dissolved as a function of The XRD patterns of the pure drug, pure
time. These were used to calculate the dissolution sodium bicarbonate, pure HPMC and their formulations
parameters which included the amount of drug were collected using a X-ray diffractometer (GNR APD
dissolved after 5 min (Q5)8. 2000 pro-X-ray diffractometer, Novara, Italy). Data
collection was performed at ambient temperature, using
Differential thermal analysis (DTA) 2θ scan axis with continuous scan mode. The scanning
Thermograms of different samples step size was adjusted to 0.03 and scan range of 3–65.
(telmisartan, polymers and the prepared formulations)
were recorded using DTA (PerkinElmer STA6000 Preparation of fast disintegrating tablets (FDTs)
module, Ohio, USA). Samples equivalent to 2.4 mg of The formulation showed the best release
the drug were loaded into aluminum pans and the lids pattern was used to prepare the FDTs which contained
were crimped using a Shimadzu crimper. The thermal an amount equivalent to 40 mg of the drug per tablet.
behavior of each sample was investigated under The composition of the prepared tablet formulation is
nitrogen at a heating rate of 10 °C/min, covering depicted in Table 2. The drug or its equivalent
temperature ranges of 25-400 °C. formulation was mixed with the excipients for 10 min
using the bottle method, before compression into tablets
Fourier-transform infrared spectroscopy (FTIR) using 8 mm die and the tablet weight was adjusted to
The FTIR was used to investigate any 220mg. This process employed single punch tablet
interaction between the drug and polymers9. This machine (Royal Artist, Kapadia Industrial Estate,
employed FTIR spectrophotometer (Bruker Tensor 27, BLDG, Mumbai, India) and the compression force were
Germany). FTIR spectra of Telmisartan, Sodium adjusted to produce tablets having a hardness of 4-5
bicarbonate, HPMC E5, and their binary SDS were kg/inch2.

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Table 2. Master formula for preparation of 40mg must be assayed individually and all of them should be
telmisartan tablets within the limit 6.
Formula of
Control tablet Disintegration test
Ingredients NaHCO3
(mg/tablet) The test was carried out on six tablets using
(mg/tablet)
tablet disintegration tester (Copley Scientific, Model:
Telmisartan - 40
NE4-COP, UK) using 900ml of phosphate buffer pH
Drug-Sodium
60 - 6.8 as a disintegration media and the time taken for the
bicarbonate SDS complete disintegration of the tablet was recorded 6.
Mannitol (granular) 70 70
Wetting time
Avicel PH102 48 68 The wetting time of the tablets was monitored
Croscarmellose
10 10 using the procedures developed previously11. A filter
sodium paper is placed in a petri dish containing 6 ml of
Crospovidone 10 10 distilled water. A small amount of allura red powder
was placed on the surface of the tablet before placing
Magnesium stearate 2 2 the tablet on the wet filter paper. The time required for
Aerosil 20 20 developing a red color on the surface of the tablet was
recorded and taken as the wetting time.
Total weight 220 220
Statistical analysis
*Q5 (%) 64.89% + 0.91 5.40% + 0.34
The Student`s t-test was used for statistical
* Q5 (%) values are expressed as mean + SD. (n=3) analysis to probe the significance of the difference
between different formulations.

RESULTS AND DISCUSSION

Evaluation of fast disintegrating tablets
Uniformity of weight Solid state characterization of the prepared
Twenty tablets were selected and weighed on formulations
digital weighing balance, and average weight was The drug content of the prepared formulations
determined. Then individual tablets were weighed, and was in the acceptable range. The drug content values
the individual weight was compared with an average were in the range of 93.45-110. 4 % w/w, excluding any
weight. The allowed percentage deviation is 7.5 %. The segregation of the drug during SD formation. The solid-
tablets meet the USP test if no more than two tablets are state characterization involved DTA, FTIR, X-ray
outside the limit and no tablet differs by more than diffraction and dissolution studies.
twice the limit10 .
Differential thermal analysis (DTA)
Tablet friability Figure 3 presents an example of the DTA
Ten tablets were weighed and placed in the traces of telmisartan, HPMC E5, sodium bicarbonate
friabilator (Erweka - Apparatebau- G.M.B.H, Western and binary SDS. The Pure drug produced a
Germany) and the equipment was rotated at 25 rpm for characteristic endothermic peak with aTm being
4 min. The tablets were taken out, de-dusted, and recorded at 268.89 °C indicating that the pure
reweighed. The friability was calculated as the unprocessed telmisartan present in the crystalline form.
percentage loss which should not exceed 1 % 6. The recorded endothermic peak correlates with the
specifications of the supplier which indicated that the
Drug content melting point of the drug is in the range of 266.37-
To ensure uniform potency, a content 273.37 °C. The recorded thermal behavior is similar to
uniformity test was applied by random selection of 30 that recorded by other investigators12. The pure HPMC
tablets. At least 10 tablets of them were individually E5 thermogram showed the melting point in the range
subjected to drug content determination. The tablets of 313.71-373.93 °C (Figure 3A). This is similar to that
were considered acceptable if the content of each of at recorded by other investigators6,13 but it is important to
least 9 tablets was in the range of 85–115 % of the note that the recorded thermograms of HPMC did not
labeled amount of telmisartan. The tenth tablet should show the endothermic peak of the bound moisture
not contain < 75 % or > 125 % of the labeled content. If indicating the dryness of the polymer. Preparation of
these conditions were not met, the remaining 20 tablets SDS of the drug with increasing concentrations of
HPMC E5 resulted in initial broadening

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Table 3. The characteristic absorption bands of FTIR spectra of the pure drug and the prepared formulations
Solid dispersion of Formula prepared using
Absorption band Pure drug
telmisartan with HPMC E5 NaHCO3
O-H hydrogen bond 3428 cm-1 3443 cm-1 3428 cm-1
C-H aromatic 3060 cm-1 3061 cm-1 3060 cm-1
C-H aliphatic 2961 cm-1 2927 cm-1 2966 cm-1
C=O stretching 1384 cm-1 1329 cm-1 1329 cm-1
C=C stretching 1600 cm-1 1616 cm-1 1557 cm-1
C-N stretching 1696 cm-1 1695 cm-1 1693 cm-1
C=N stretching 1459 cm-1 1461cm-1 1557 cm-1

and decrease in the Tm of the main endothermic peak of stretching peak was shifted from 1459 cm-1 in pure drug
the drug without complete disappearance even at the to 1557 cm-1 in the prepared formulation. This indicates
higher polymer ratio (Figure 3B). This change in the hydrogen bond formation between sodium bicarbonate
melting transition was accompanied by a gradual and a lone pair of an electron on the nitrogen atom,
reduction in the enthalpy. This effect indicates a therefore, making a dipolar molecule and subsequently
possible partial transformation of the drug from increased the solubility of the molecule.
crystalline to amorphous form. Similar effects have
been recorded after formulation of SDS of HPMC with X-ray Diffraction
other drugs13. For pure sodium bicarbonate, the Figure 5 shows the XRD pattern for pure
thermogram showed endothermic peak starting at 85.72 telmisartan, pure HPMC E5, pure sodium bicarbonate
°C and ending at 98.92 °C. This was attributed to the and SDS. Characteristic peaks appeared in the XRD for
release of the adsorbed moisture from the sodium telmisartan showed high-intensity peaks at 2θ values of
bicarbonate. Another broad peak was recorded in the 6.856, 14.253, 15.082, 19.065 and 22.35. This complies
range of 130.68-187.9 °C which corresponding to the with the published data15. The XRD pattern of HPMC
melting and decomposition of sodium bicarbonate. The E5 did not show any distinct peak reflecting the
formulation prepared from the drug with sodium amorphous nature of the polymer. This correlates with
bicarbonate had resulted in complete disappearance of the published data on the polymer16. The XRD pattern
the endothermic peak of the drug in 1: 0.5 (drug: of unprocessed sodium bicarbonate reflected its
sodium bicarbonate) weight ratio (Figure 3B). This crystalline nature with the diffraction pattern showing
effect indicates the possible transformation of the drug distinct peaks. In case of SD of the drug with HPMC
from crystalline to amorphous form. E5, sodium bicarbonate and aerosil respectively in a
ratio (1: 2: 2: 1) the diffraction peaks disappeared
FTIR spectroscopy suggesting the transformation of telmisartan from
Figure 4 shows the FTIR spectra of crystalline to amorphous form (Figure 5 (A)). The same
telmisartan, sodium bicarbonate, HPMC E5 and the was recorded in case of the formulation of the drug with
prepared SDS formulations. The FTIR spectrum of pure sodium bicarbonate at the weight ratio of 1: 0.5 (Figure
telmisartan and the prepared SDS with HPMC E5 5B) suggesting the transformation of the drug to the
showed the characteristic peaks of the drug at the amorphous form. This result confirms the data obtained
specified wave number (cm)-1 corresponding to each after thermal analysis of the same formulations.
functional group as indicated in Table 3. This is similar
to that reported by other workers14. This revealed Drug dissolution
absence of interaction between the drug and HPMC E5. Figure 6 shows the dissolution profile of the
The FTIR spectrum of the prepared formulation of the drug powder in a pure state or as binary SD with
drug with sodium bicarbonate showed alterations in the different polymers or with sodium bicarbonate. The
main absorption bands of pure drug reflecting a dissolution parameters are presented in Table1. The
significant interaction between the drug and sodium dissolution profile of pure drug indicated slow
bicarbonate. These alterations were manifested as a dissolution with only 6.41 % + 0.28 being released in
shift in the position of C-N stretching peak from 1669 the first 5 min This correlates with the published work
cm-1 in pure drug to 1693 cm-1 in the prepared of the same drug17. Preparation of the binary SD of the
formulation. In addition, the position of a C=N drug with Gelucire 44/14 or PEG4000 resulted in
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Figure 3. Panel A: Thermograms of unprocessed telmisartan (control), pure HPMC E5 and solid dispersions of telmisartan
with increasing concentrations of HPMC E5 (D1, D2, D3 andD5). Panel B: Thermograms of telmisartan (control), pure
sodium bicarbonate, and solid dispersion of telmisartan with sodium bicarbonate 1:0.5 (E) respectively. Formulation details
are in Table 1.

compared with formula C1, with the amount dissolved

in the first 5 min being 24.6 + 1.52 and 24.92 + 3.6 for
the formula C2 and C3 respectively (Figure 6C) and
Table 1). In case of HPMC E5 the binary solid
dispersions resulted in an increase in the dissolution rate
in 1:1 drug: polymer, The weight ratio (D1). At this
ratio, the formulation liberated 13.9% + 1.56 of the drug
in the first 5 min. There was a slight increase in the %
dissolved of the drug upon increasing the polymer
concentration to 2 in the formulation D2, but further
increase in the polymer concentration slightly decreased
the dissolution rate (Figure 6D and Table 1). The
enhanced dissolution rate after solid dispersion
formation of the drug with HPMC E5 can be attributed
to crystalline structure modification and partial or
Figure 4: FTIR spectra of telmisartan (control), sodium complete amorphousization as revealed from the
bicarbonate, HPMC E5, and their solid dispersions. The thermal analysis and X-Ray diffraction data. Similar
traces from bottom to top are pure telmisartan (control),
explanation was used to describe the dissolution
pure sodium bicarbonate, pure HPMC E5, drug-HPMC
E5 solid dispersion (D2) and solid dispersion of enhancement of other drugs after solid dispersion
telmisartan with sodium bicarbonate 1:0.5 (E) formation with the same polymer6. Sodium bicarbonate
respectively. was added as a second excipient to solid dispersion
showing a potential for enhanced drug dissolution.
When sodium bicarbonate was added to a solid
a slight increase in the dissolution rate of the drug even dispersion of the drug with Pluronic F68 in the ratio of
at the highest polymer concentration (Figure 6 A, B) (1: 2: 2) drug: excipient: sodium bicarbonate
and Table 1). The binary SD of the drug with Pluronic respectively (formula C4) the dissolution rate was
F68 and HPMC E5 resulted in an increase in the increased to 33.025% + 0.8 of the dose in the first 5
dissolution rate compared to the pure unprocessed drug. minutes. Incorporation of sodium bicarbonate with
Formulation of the binary SD of the drug with Pluronic HPMC E5 in solid dispersion system (formula D4)
F68 at a weight ratio of 1:1 (C1) resulted in a significantly enhanced the dissolution rate of the drug
significant increase in drug dissolution compared with with the % dissolved in the first 5 min reaching 45.3 %
the unprocessed dug (p < 0.05) with 27.05% + 2.06 of + 5.6 in (Figure 6E and Table 1). The addition of
the dose being dissolved in the first 5 min. Increasing aerosil to this formulation (formula D5) increased the %
the polymer concentration (formula C2 and C3) resulted Q5 to reach 72.6.%. + 0.81 in (Figure 6F and Table1)
in a slight reduction in the dissolution rate of the drug This increase in the dissolution rate can be

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Figure 5. X-ray diffraction pattern of pure telmisartan (control), pure HPMC E5, pure sodium bicarbonate and their solid
dispersions D5 (panel A) and E (panel B). Formulation details are in Table 1.

explained based on the adsorption of the prepared solid Based on these results formula E which
dispersion on the surface of aerosil which increases the composed of telmisartan with sodium bicarbonate in a
surface area with a consequent increase in the ratio (1: 0.5) was selected for the preparation of rapidly
dissolution rate of the drug. The presence of a drug in dissolving tablet of telmisartan. This selection was
the amorphous state in this formulation can contribute based on the enhanced dissolution rate, more palatable
further to the enhanced dissolution of the drug. taste in the buccal cavity and relatively inexpensive
Dissolution enhancement was recorded for drug material which is more economical for the
adsorbed on the solid surfaces and the results were pharmaceutical industry and easier in processing
similarly explained18. compared with the solid dispersions prepared using
When sodium bicarbonate was employed alone in the polymers.
preparation of solid dispersion system instead of the
polymer at the weight ratio of 1:1 and 1:0.5 drug: Characterization of fast disintegrating tablets
sodium bicarbonate (formula F and E) the dissolution (FDTs)
rate was enhanced significantly. The recorded % Q5 The prepared tablets were found to be of
values were 88.94% + 1.31 and 84.77 % + 1.1 for both uniform weight with the recorded deviation from the
formula E and F respectively (Figure 6F and Table 1). average weight being < 4.5 %. The recorded friability
This increase in the dissolution rate can be attributed to values were in the range of 0.85 %. This is acceptable
the nature of the drug which is readily ionizable and its based on the acceptance criteria of the USP (USP
solubility is pH dependent. Hence, the drug solubility 2009). The drug content was in the range 93.45 % –
increased upon the addition of sodium bicarbonate due 110.4 %. Dissolution profiles of the prepared tablets are
to the increase in the pH of the diffusion layer. Another shown in (Figure 7), which indicates that the percent
explanation for the enhanced dissolution rate was based drug release after 5 min (Q5) in control tablet reached
on the results of powder X-ray diffractometry and only 5.4 % ± 0.34 compared with 64.89% + 0.91
thermal analysis, which indicated the transformation of (Figure 7 and Table 2) in case of tablets sodium
the drug from crystalline to amorphous form. bicarbonate. The unpaired t-test for the effect of sodium
The formula which produced the highest percentage of bicarbonate on the % release of telmisartan for the test
the drug dissolved in first 5 min Q5 (%) was in the order: tablets compared with control indicated a highly
E > F > D5 where the % drug dissolved was 88.94 + significant effect of sodium bicarbonate (p < 0.01).
1.31, 84.77 + 1.1 and 72.6 + 0.81 (mean + SD) for each Development of fast disintegrating tablets with
formula respectively. However, there was no statistical subsequent rapid dissolution was employed to enhance
difference between formulae E and F (P > 0.05). dissolution rate of drugs including those which have
Meanwhile, the statistical analysis showed highly dose of 100 mg19. The developed formulation can be
significant difference between formulae E and D5 (p < considered promising for enhancing the dissolution rate
0.01). of telmisartan.

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100 100

A1
80 A2 80
B1
A3 B2

% Drug relaesed
% Drug released

60 Control 60 B3
Control

40 40

20 20

0 0
0 10 20 30 40 50 60 70 0 10 20 30 40 50 60 70
A) B)
Time (min) Time (min)

100
100
C1 D1
80 C2 D2
80
%Drug released

C3 D3
60
%Drug released

60
control control
40
40

20
20

0
0
0 10 20 30 40 50 60 70
0 10 20 30 40 50 60 70
C) Tim(min) D)
Tim(min)

100 120

80 100
D4
%Drug released

% Drug release

80
60 C4 E
60
40 D5
control
40
F
20
20 Control
0 0
0 10 20 30 40 50 60 70 0 10 20 30 40 50 60 70
E) Tim(min) F) Tim(mint)

Figure 6. Dissolution profiles of telmisartan from its unprocessed powder and from solid dispersions with different
additives. Formulation details are in Table1. Mean + SD, n=3.

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antihypertensive agent. Int. J. Curr. Pharm. Res.

100 2012, 2 (4), 37-41.
4. Kausalya, J.; Suresh, K.; Padmapriya, S.;
80 Rupenagunta, A.; Senthilnathan, B. Solubility and
Dissolution Enhancement Profile of Telmisartan
%Drug released

60 using various techniques. Int. J. Pharm. Tech. Res.

2011, 3 (3), 1737-1749.
Control tablet
40
tablet formula
5. Patel, B.; Parikh, R. H.; Swarnkar, D. Enhancement
of dissolution of Telmisartan through use of solid
20 dispersion technique - surface dispersion. J Pharm
Bioallied. Sci. 2012, 4, suppl S1: 64-68.
0 6. El Maghraby, G. M.; Elsergany, R. N. Fast
0 10 20 30 40 50 60 70
disintegrating tablets of nisoldipine for intra-oral
Tim(min)
administration. Pharm. Dev. Technol. 2014, 19 ( 6),
641-650.
Figure 7. Dissolution profile of the selected fast 7. Parkash, V.; Maan, S.; Deepika.; Yadav, S. K.;
dissolving tablet (FDT) compared with the control.
Hemlata.; Jogpal, V. Fast disintegrating tablets:
Mean + SD, n=3.
Opportunity in drug delivery system. J. Adv.
Pharm. Technol. Res. 2011, 2 (4), 223-235.
8. Arafa, M. F.; El-Gizawy, S. A.; Osman, M. A.; El
CONCLUSION Maghraby, G. M. Sucralose as co-crystal co-former
for hydrochlorothiazide: development of oral
SD with a polymer or with sodium bicarbonate disintegrating tablets. Drug Dev. Ind .Pharm. 2016,
was able to enhance the dissolution rate of telmisartan 42 ( 8), 1225-1233.
depending on the presence of the pH modifying agent 9. El Maghraby, G. M.; Elgohary, A. Y.; Osman, M.
(sodium bicarbonate) and concentration of the polymer.
A. Enhancement dissolution rate of
The formula prepared using sodium bicarbonate with
hydrochlorothiazide. Int. J. Pharm. Pharm. Sci.
the drug in (0.5: 1) ratio was selected for preparation of
2016, 7 (8), 427- 433.
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