A Prospective
Validation of Hydrocholorothiazide and Bisoprolol Fumerate in its Pure and Bulk
Dosage Forms by using RP- HPLC Technique
S. Janet Beula1*, Dr. R. Suthakaran1,
Prem Kumar Bichala1, CH. Shankar1, Syed Ghouse1,
K. Suneetha2
1Vijaya College of
Pharmacy, Munuganoor, RR District, India.
2 SSJ College of
Pharmacy, Gandipet, RR
District, India.
*Corresponding Author E-mail: Pharmjanet123@gmail.com
ABSTRACT:
A simple, specific and
accurate RP-HPLC method was developed for the simultaneous estimation of
Bisoprolol fumerate and Hydrochlorothiazide in bulk dosage forms. The
chromatographic conditions were successfully developed for the separation of
Bisoprolol fumerate and Hydrochlorothiazide by using ACE C18 column
(4.6×150mm) 5µ,
flow rate was 1.2ml/min mobile phase ratio was (70:30 v/v) methanol: Phosphate
buffer pH 3 (pH was adjusted with orthophosphoric acid), detection wavelength
was 240nm. The method was validated according to ICH guidelines for specificity,
LOD, LOQ, Precision, Accuracy and Linearity. The method showed good
reproducibility and recovery with % RSD less than 2.
KEYWORDS: ACE C18
column, Hydrochlorothiazide and Bisoprolol, RP HPLC.
INTRODUCTION:
Combination therapy or poly
therapy is therapy that uses more than one medication. Typically, these terms
refer to using multiple therapies to treat a single disease. Poly therapy is a
related term, referring to the use of multiple medications1.
Hydrochlorothiazide one of the oldest thiazide diuretics and is used in the
treatment of hypertension patients either alone or with other antihypertensive
drugs such as angiotensin converting enzyme inhibitors and beta blockers2-4.
It is a modestly intense diuretic and applies its diuretic impact by lessening
the reabsorption of electrolytes from the renal tubules along these lines
expanding the discharge of sodium and chloride particles and consequently of
water.
Bisoprolol is a cardio
selective beta blocker used in the treatment of hypertension and angina
pectoris. But the combination of Hydrochlorothiazide and Bisoprolol RP-HPLC
method validation was still now not et al performed.5-8 This method
was validated according to ICH guidelines for specificity, LOD, LOQ, Precision,
Accuracy, and Linearity.9,10 The method showed good reproducibility
and recovery with % RSD less than 2. Hence we had made an attempt to develop a
simple accurate and precise RP-HPLC method for the simultaneous estimation of
Hydrochlorothiazide and Bisoprolol in bulk and in tablet dosage form.
DRUG PROFILE:
Hydrochlorothiazide:
Structure:
IUPAC name:
6-chloro-1,
1-dioxo-3, 4-dihydro-2H-1, 2, 4-benzothiadiazine-7-sulfonamide.
Category:
Antihypertensive
Agents, Diuretics, Sodium Chloride Symporter Inhibitors.
Bisoprolol Structure:
IUPAC name:
[2-hydroxy-3-(4-{[2-(propan-2yloxy)
ethoxy] methyl} phenoxy) propyl] (propan-2-yl) amine.
Category:
Antihypertensive Agents,
Adrenergic beta-1 Receptor Antagonists, Sympatholytics.
Pharmaceutically pure
sample of Hydrochlorothiazide and Bisoprolol drug was obtained from Awamedica
Company (in Erbil city, Kurdistan region of Iraq). Commercial tablet of
Hydrochlorothiazide and Bisoprolol (100mg) was procured from the local drug
market. Acetonitrile and water, Methanol, Ortho phosphoric acid, KH2PO4,,
K2HPO4 were HPLC from merck KGaA, 64271 Darmstadt,
Germany.
Analytical HPLC-auto
sampler –UV detector Separation module 2695, UV. Detector 2487
Empower-software version-2 Waters, U.V double beam spectrometer UV 3000+,
Digital weighing balance(sensitivity 5mg), pH meter, Sonicator.
Accurately weigh and transfer
59.8mg of Hydrochlorothiazide and Bisoprolol Tablet powder into a 10mL clean
dry volumetric flask add about 7mL of diluent and sonicate to dissolve it
completely and make volume up to the mark with the same solvent. (Stock
solution). Further pipette 0.6ml of Hydrochlorothiazide and Bisoprolol the
above stock solution into a 10ml volumetric flask and dilute up to the mark
with diluent.
Standard solution preparation:
Accurately weigh and transfer
12.5mg & 8mg of Hydrochlorothiazide and Bisoprolol working standard into a
10mL clean dry volumetric flask add about 7mL of diluent and sonicate to
dissolve it completely and make volume up to the mark with the same solvent.
(Stock solution) Further pipette 0.6ml of Hydrochlorothiazide and Bisoprolol
the above stock solution into a 10ml volumetric flask and dilute up to the mark
with diluent.
Procedure:
10mL of the blank, standard
and sample were injected into the chromatographic system and areas for the
Hydrochlorothiazide and Bisoprolol the peaks were used for calculating the %
assay by using the formula.
Optimized chromatographic
conditions:
By performing the
trails the chromatographic conditions were optimized as follows
|
Column |
: |
“ACE C18 (4.6×150 mm) 5.0µm” |
|
Mobile phase |
: |
“Methnol: Pb (70: 30 % v/v)” |
|
Wavelength |
: |
240 nm |
|
Flow rate |
: |
1.2 ml/min |
|
Injection volume |
: |
10µl |
|
Column Temperature |
: |
Ambient |
|
Rt |
: |
2.449 & 3.191 mins |
Fig.No.1 Optimized
chromatographic conditions
The detection wavelength was
hand-picked by”. “The ensuing resolution was scanned in U.V vary from
200-400nm”. “The overlay and Hydrochlorothiazide and Bisoprolol showed at 240
nm”.
Fig.No.2 The scan
spectrums
Fig.No.3. Chromatogram showing
blank preparation (mobile phase)
Fig.No.4. Chromatogram showing
standard injection
Fig.No.5.
Chromatogram showing sample injection.
The specificity check was
performed for Hydrochlorothiazide and Bisoprolol. It had been found that there
was no interference of impurities in retention time of analytical peak.
Assay calculation for
Hydrochlorothiazide and Bisoprolol:
Fig.No.6. Chromatogram showing
assay of sample injection-1, 2
The specificity check was
performed for Hydrochlorothiazide and Bisoprolol. It had been found that there
was no interference of impurities in retention time of analytical peak.
Table.No.1. Showing assay
results:
|
S. No |
“Name of compound” |
“Amount taken” |
“%purity” |
|
1 |
“Hydrochlorothiazide” |
754.7 |
99.24 |
|
2 |
“Bisoprolol” |
735.6 |
101.04 |
Linearity:
The one-dimensionality study
was performed for the concentration of 50 ppm to 250 ppm for
Hydrochlorothiazide” and 10ppm to 50ppm for Bisoprolol”. Every level was
injected into activity system. The world of every level was used for
calculation of correlation. The results area unit tabulated in Table. No.2-3.
Standardization graph area unit shown in Fig.No.7- 8.
Table No.2 Linearity
Results for Hydrochlorothiazide
|
S. No |
Linearity Level |
Concentration |
Area |
|
1 |
I |
50 ppm |
471543 |
|
2 |
II |
100 ppm |
656277 |
|
3 |
III |
150 ppm |
794999 |
|
4 |
IV |
200 ppm |
946124 |
|
5 |
V |
250 ppm |
1002139 |
|
Correlation Coefficient |
0.999 |
||
Fig.No.7. Showing
calibration graph for Hydrochlorothiazide
Fig.No.7. Showing calibration
graph for Bisoprolol
Table No.3. Linearity Results
for Bisoprolol
|
S. No |
Linearity Level |
Concentration |
Area |
|
1 |
I |
10 ppm |
220102 |
|
2 |
II |
20 ppm |
258503 |
|
3 |
III |
30 ppm |
299655 |
|
4 |
IV |
40ppm |
344622 |
|
5 |
V |
50 ppm |
389792 |
|
|
Correlation Coefficient |
0.999 |
|
The linearity range of
50.µg-250µg and 10µg-50µg of Hydrochlorothiazide and Bisoprolol and the
correlation coefficient was found to be 0.999 and 0.999. (NLT 0.999)”.
Accuracy:
|
%Concentration (at specification level) |
Average area |
Amount added (mg) |
Amount found (mg) |
% Recovery |
Mean recovery |
|
50% |
656659 |
5 |
4.96 |
99.91% |
99.56% |
|
100% |
1304258 |
10 |
9.98 |
99.18% |
|
|
150% |
1854608 |
15 |
15.02 |
99.60% |
Table.No.5. Showing accuracy
results for Bisoprolol:
|
%Concentration (at specification level) |
Average area |
Amount added (mg) |
Amount found (mg) |
% Recovery |
Mean recovery |
|
50% |
65312 |
0.5 |
0.99 |
99.53% |
99.47% |
|
100% |
124509 |
1.0 |
1.05 |
99.38% |
|
|
150% |
178517 |
1.5 |
1.495 |
99.52% |
For teenagers recovery of
Hydrochlorothiazide and Bisoprolol. The be 99.56% and 99.47% severally (NLT
ninety eight and NMT 102%).
Precision:
The standard resolution was
injected for 5 times and measured the world for all 5 injections in HPLC”. The
% RSD is among the desired limits”. The % RSD and results area unit tabulated
in Table.6-7.
Intermediate
precision:
The intermediate
exactitude study was performed for 5 injections of Hydrochlorothiazide and
Bisoprolol”. The result area unit tabulated in table 7-8.
Table.No.6. Showing%
RSD results for Hydrochlorothiazide Peak Name: Hydroclorothaizide
|
|
Peak Name |
RT |
Area (µV*Sec) |
Height (µV) |
|
1 |
Hctz |
2.343 |
1302729 |
248455 |
|
2 |
Hctz |
2.344 |
1302729 |
248699 |
|
3 |
Hctz |
2.344 |
1302947 |
249526 |
|
4 |
Hctz |
2.345 |
1303977 |
246695 |
|
5 |
Hctz |
2.345 |
1303236 |
250012 |
|
Mean |
|
|
1304529.8 |
|
|
Std. Dev. |
|
|
2361.1 |
|
|
% RSD |
|
|
0.2 |
|
Table.No.7. Showing
%RSD results for Bisoprolol
Peak Name:
Bisoprolol
|
|
Peak Name |
RT |
Area (µV*Sec) |
Height (µV) |
|
1 |
Bisoprolol |
3.285 |
124263 |
19458 |
|
2 |
Bisoprolol |
3.287 |
124487 |
19634 |
|
3 |
Bisoprolol |
3.287 |
124175 |
19600 |
|
4 |
Bisoprolol |
3.288 |
124894 |
19327 |
|
5 |
Bisoprolol |
3.288 |
124495 |
19540 |
|
Mean |
|
|
124462.7 |
|
|
Std. Dev. |
|
|
278.6 |
|
|
% RSD |
|
|
0.2 |
|
Table.No.7. Showing
results for intermediate precision of Hydrochlorothiazide
Peak Name:
Hydroclorothaizide
|
|
Peak Name |
RT |
Area (µV*Sec) |
Height (µV) |
|
1 |
Hctz |
2.342 |
1305937 |
247870 |
|
2 |
Hctz |
2.343 |
1306476 |
246764 |
|
3 |
Hctz |
2.344 |
1304520 |
245696 |
|
4 |
Hctz |
2.344 |
1300148 |
247140 |
|
5 |
Hctz |
2.345 |
1308271 |
247280 |
|
Mean |
|
|
1305070.2 |
|
|
Std. Dev. |
|
|
3061.8 |
|
|
% RSD |
|
|
0.2 |
|
Table.No.8. Showing
results for intermediate precision of Bisoprolol
Peak Name:
Bisoprolol
|
|
Peak Name |
RT |
Area (µV*Sec) |
Height (µV) |
|
1 |
Bisoprolol |
3.278 |
122962 |
19165 |
|
2 |
Bisoprolol |
3.281 |
122487 |
19115 |
|
3 |
Bisoprolol |
3.281 |
122632 |
19073 |
|
4 |
Bisoprolol |
3.281 |
122626 |
19003 |
|
5 |
Bisoprolol |
3.283 |
122702 |
19123 |
|
Mean |
|
|
122681.8 |
|
|
Std. Dev. |
|
|
174.8 |
|
|
% RSD |
|
|
0.1 |
|
The intermediate
precision was performed for % RSD of Hydrochlorothiazide and Bisoprolol was
found to be 0.2 and 0.1. From the system precisions studies it is observed that
all parameters like %RSD of retention time and peak areas are within limits.
Detection limit:
LOD’s will be calculated
supported the quality deviation of the response (SD) and also the slope of the
standardization curve (S) at levels approximating the LOD consistent with the
formula. The quality deviation of the response will be determined supported the
quality deviation of y-intercepts of regression lines.
Formula
LOD = 3.3 X σ/S
Where
σ - Standard deviation
(SD)
S – Slope
Fig.No.8. Showing Results of
LOD
The LOD was performed for
Hydrochlorothiazide and Bisoprolol was found to be 3.17and 0.0172 respectively.
LOQ’s may be calculated
supported the quality deviation of the response (SD) and also the slope of the
activity curve (S) in line with the formula. Again, the quality deviation of
the response may be determined supported the quality deviation of y-intercepts
of regression lines.
LOQ = 10 X σ/S
Whereσ -
Standard deviation
S - Slope
Fig.No.9. Showing
Results of LOQ
The LOQ was performed for
Hydrochlorothiazide and Bisoprolol was found to be 5.80 and 0.212 severally.
The developed method was
successfully applied for simultaneous estimation of Hydrochlorothiazide and
Bisoprolol in compound tablet formulation. The proposed method was found to be
simple, accurate and precise. There is no analytical method available to
determine the same combination of drugs. Therefore, this method may be useful
for routine analysis of Hydrochlorothiazide and Bisoprolol in API drugs and
pharmaceutical dosage forms.
ACKNOWLEDGEMENT:
I express my sincere thanks to
Dr. Suthakaran and Management of Vijaya College of Pharmacy for encouragement
throughout my research work. And also thankful to Awamedica Company providing
the Reserpine and Hydrochlorothiazide pure drugs.
REFERENCE:
7.
Arjun G, Sathis KD, Bindu MB, Naga MM, Ramalingam R, Nath AR. Asimple
HPLC Method for Quantitation of Bisoprolol Fumarate in Tablet Dosage Form.
Indian Drugs, 2009; 46:39-42. 7.
8.
Yadav SS, Rao JR. Simultaneous HPTLC analysis of Bisoprolol Fumarate
and Hydrochlorothiazide in Pharmaceutical Dosage Form. Int J Pharm Sci, 2013;
5:286-90.
9.
International Conference on Harmonization. Draft Guideline on
Validation of Analytical Procedures: Definitions and Terminology, Federal
Register. 60, 1995, 11260.
10. Global Quality
Guideline.
Validation of Analytical Procedures. Number: G-6.9, 2002 Version: 1.0.
Received on 09.01.2019
Modified on 22.01.2020
Accepted on 18.02.2020 ©Asian Pharma
Press All Right Reserved
Asian J. Pharm. Ana. 2020; 10(1):01-06.
DOI: 10.5958/2231-5675.2020.00001.0