7801antacids Evaluation
7801antacids Evaluation
7801antacids Evaluation
College of pharmacy.
Department of pharmaceutics.
Supervised by
Dr. Ouday Sajjad
Submitted by:
Ali Jamhour Thani.
Fatima Raad Qasim.
Aetebar Hadeer Adbullwahab.
1
DEDICATION
First of all, we would like to express our gratitude to the
Presidency of Al-Basra Pharmacy college for their support
and encouragement.
2
ACKNOWLEDGMENT
• Firstly, we would like to thank our parents, who
support us during our journey in life, studying,
and working hard to become what we are now
and to achieve our goals and wishes.
• In addition, we would like to express our sincere
gratitude And our greatest appreciation to our
supervisor Dr. Ouday Sajjad for his patience,
guidance, Enthusiastic encouragement, valuable,
constructive, useful Critiques of this research
work.
3
Content
1 Introduction 6
5. Conclusion. 28
6. Discussion. 29
7. References. 37
4
Abstract
5
1.Introdution
Different brands of antacids are available to relieve heartburn and peptic ulcer
pain in Basra pharmacies. These commercial brands of antacids come in
various dosage forms, as either liquids or solids. Magnesium and aluminum as
hydroxides alone or in combination form the principal composition of most
antacids. Some also contain salts of calcium, sodium, alginate, carbon or
bismuth in their formulations, in vivo experiment were carried out to find if
these antacid brands are within the standards of antacids according USP
(United states pharmacopeia).
7
2.Tests carried out in this experiment for antacids:
8
2.1.Tests to be performed:
Ph Meter
9
• 3.Preliminary antacid test: The preliminary antacid test measured
the final pH of a 10-mL solution of 0.5 N HCl 10 minutes after
addition of the minimum recommended dose of an antacid, while
the neutralizing capacity test measured the amount (mEq) of HCl
neutralized by the minimum recommended dose in 15 minutes.(5)
• Procedure:
• An accurate amount of a well-mixed antacid product equivalent to
the minimum labeled dosage; (5 mL) was weighed into a 100 ml
beaker., Sufficient distilled water was added to obtain a total volume
of about 40 ml and mixed on a Hotplate magnetic stirrer at 300
r.p.m for a minute.
• 10 mL of 0.5 N HCl was added to the test solution while stirring on
the magnetic stirrer at 300 r.p.m for exactly 10 min after addition of
acid.
• The pH was read and recorded with PH meter to ascertain label
claim as an antacid if pH is 3.5 or greater.(5)
10
• 4.The acid neutralizing capacity : is often defined as a measure of
the amount of base present that can accept hydrogen ions from a
strong acid.(6)
• Procedure
• The ANC was determined for all the brands since each had a pH of
3.5 or greater from the PAT. An accurate volume (5 mL) of the
antacid suspension was measured into a 25 ml beaker and weighed.
The suspension was then transferred into a 250 ml beaker and made
up to 70 ml with distilled water and stirred for one minute and the
pH is measured. An accurate volume of 30 ml of 1.0 N HCl was
pipetted into the suspension whiles stirring for 15 mins. The excess
HCl was titrated with 0.5 N NaOH to attain a threshold pH of 3.5.
The experiment was carried out for the different brands and their
respective batches at a temperature of 37 °C on a magnetic stirrer.
The number of milliequivalent (mEq) of acid consumed per gram of
antacid was calculated.
• The acid neutralizing capacity (ANC) was calculated using the
Equation below:
• Total mEq = (30 x NHCl) – (VNaOH x NNaOH)……………….Equation.
• Where NHCl and NNaOH are the normality of HCl and NaOH,
respectively, and VNaOH is the volume of NaOH used for the back
titration.(6)
11
• 5.Buffering capacity: (β) is defined as the moles of an acid or
base necessary to change the pH of a solution by 1, divided by the
pH change and the volume of buffer in liters; it is a unitless
number.(8)
• Procedure:
• An accurate volume of 5 mL each of the antacid samples were
measured and transferred into a 250 mL beaker and 50 mL of
distilled water added and heated to 37 °C. The suspension was
stirred for one minute and the initial pH recorded with pH meter. An
accurate volume of 100 mL of 0.1 N HCl previously heated to 37°C
was added to the suspension with continuous stirring. The rate of
pH change of the resulting solution was measured 10 times at an
interval of 5 mins, at ambient temperature.
• During this process, a quantity of 20 mL of the suspension was
removed by means of a pipette and replaced with 20 mL of fresh
0.1 N HCl. This process was repeated at 5.0 min interval until a pH
below 2.75 was observed for the different brand.
• The rate of pH change with time representing the Buffering capacity
for each antacid was determined and compared . All the brands had
their initial pH ranging from 7.91 – 8.91.(10)
12
• 6.Viscosity: Viscosity is a measurment of a fluid's resistance to flow
i.e. the measure of a substance's resistance to motion under an
applied force. Viscosity checks should ensure the correct
consistency of the end product to meet customers’ expectations. We
can measure the viscosity by using Viscometer.
• Proceedure:
• Prepare the samples by placing a proper amount of each brand of
each Antacid in a clean beaker.
• Set up the viscometer, and choose a suitable spindle to use,
according to the sample to be evaluated.( For the sample with high
viscosity, you should choose the small size spindle ( Code L3 and
L4) and slow rotating speed, for the sample with low viscosity you
should choose the larger spindle (code L1 and L2) and fast rotating
speed.)
• Switch on the viscometer by the left side button, the screen will
flash and left on standby.
• Input the spindle code, the input id over when the selected spindle is
displayed.
• Select the rotating speed.
• Immerses the spindle into the liquid (the mark of the spindle should
be on the same level as the liquid) then adjust the device to
horizontal level.
• Press "run"
• Record the readings displayed on the screen.
viscometer
13
Sampling and composition of samples:
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3.Antacids containing Magnesium hydroxide, Aluminum
hydroxide and (simethicone or dimethicone as antiflatulence)
simethicone dimethicone 15
3.1.MAALOX PLUS.
Composition:
• Magnesium hydroxide 4g.
• Aluminum hydroxide 3.5g.
• Simethicone 0.50g.
Appearance: elegant, uniform, becomes two phases upon standing
and the particles are well distributed upon shaking.
• Color: white.
• Odor: lemon.
• Teste: lemon with a little bitterness and dusty feeling upon tasting.
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3.2.EPICOGEL.
Composition:
• Dried aluminum hydroxide gel 8.1gm
• Magnesium hydroxide 2gm
• Dimethicone 2.5gm
Appearance: elegant, uniform, becomes two phases upon standing
and the particles are well distributed upon shaking.
• Color: white.
• Odor: mint.
• Taste: unpleasant minty teste.
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3.3.ACILOX PLUS.
Composition:
• Aluminum hydroxide 225mg.
• Magnesium hydroxide 200mg.
• Simethicone 25mg.
Appearance: elegant, uniform, becomes two phases upon standing
and the particles are well distributed upon shaking.
• Color: white.
• Odor: mint, acceptable.
• Taste: mint like taste.
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3.4.MOXAL PLUS
Composition:
• Aluminum hydroxide 215mg.
• Magnesium hydroxide 80mg.
• Simethicone 25mg.
Appearance: elegant, uniform, becomes two phases upon standing
and the particles are well distributed upon shaking.
• Color: white.
• Odor: mint.
• Taste: mint.
19
3.5.DIGEL.
Composition:
• Aluminum hydroxide gel 215mg.
• Magnesium hydroxide 80mg.
• Simethicone 25mg.
Appearance: uniform, becomes two phases upon standing and the
particles are well distributed upon shaking.
• Color: greenish white.
• Odor: Fennel.
• Taste: unpleasant fennel taste.
20
3.6.Testing
S2 1.03 8.45
S3 0.85 8.09
S4 1.03 8.85
S5 0.85 7.91
21
Buffering Capacity (Rate of pH change of antacid suspension
with time)for (S1,S2,S3,S4,S5):
min
ND=Not determined.
22
Viscosity Values:
S1
Speed (RPM) Viscosity mPa.s Percentage %
0.3 5714.7 28.6%
0.6 3424.2 34.2%
1.5 1499.5 37.5%
3 800.9 40%
6 459.3 45.9%
12 200.9 52.2%
30 141 67%
S2
23
s3
Speed (RPM) Viscosity mPa.s Percentage %
S4
24
S5
Speed (RPM) Viscosity mPa.s Percentage %
0.3 4212.8 15.1%*
0.6 3312.5 22.5%
1.5 2411.5 27.4%
3 773.1 36.6%
6 532.3 46.1%
12 199.9 54.9%
30 ND ND
P.S/
All the samples viscosities where measured at the same conditions.
Spindle used for all the samples was (L1).
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4.Alginate antacid.
One of the primary treatments for gastroesophageal reflux disease
(GERD) is the administration of alginate/antacid anti-reflux
preparations. These provide a physical barrier on contact with the
stomach contents in the form of a neutral floating gel or raft. This
physical mode of action is quite distinct from the chemical
neutralization of the bulk gastric contents provided by antacids
alone, although alginate raft forming Preparations. The advantage
of alginate/antacid combinations over antacids alone is that they
provide longer lasting symptom relief, even though relief is rapid
in both cases. Their rapid onset of action makes them more
suitable for self-medication than pharmacologically acting acid
suppressants such as H2-receptor antagonists or proton pump
inhibitors This has also led to their successful use as a well
tolerated non-systemic treatment for prevention of relapse in
healed reflux esophagitis and for the treatment of heartburn in
pregnancy. Alginate rafts may be formed in liquid products by the
action of gastric fluid on a soluble alginate to form an insoluble gel
of alginic acid. They may also be formed by the interaction of
soluble alginate with metal ions released by acid from an insoluble
antacid such as calcium carbonate. The simultaneous action of
Gastric acid on a bicarbonate salt produces carbon dioxide, which
should ideally be trapped inside the alginate gel to aid buoyancy of
the raft. Several features of rafts formed by alginate/antacid anti-
reflux preparations are useful in forming an effective long lasting
barrier between corrosive gastric fluid and the esophageal mucosa.
Such rafts would be expected to be cohesive, buoyant, voluminous,
resistant to reflux into the esophagus and not easily broken up by
movement in the stomach.(12)
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4.1.GAVISCON
Composition:
• Each 10 ml contain:
• Sodium alginate 500mg.
• Sodium bicarbonate 267mg.
• Calcium carbonate 160mg.
Appearance: elegant, uniform, becomes two phases upon standing
and the particles are well distributed upon shaking.
• Color: light pink.
• Odor: Aniseed.
• Taste: aniseed taste, sweet with a little pungent effect upon tasting.
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4.2.PYROSIX.
Composition:
• Sodium alginate 5000g .
• Sodium bicarbonate 2670 g.
Appearance : elegant, uniform, becomes two phases upon
standing and the particles are well distributed upon shaking.
Color: milky white.
Odor: Aniseed- like smell.
Taste: Aniseed with mild sweet taste.
28
4.3.Testing.
S7 0.96 8.91
0
min min
29
Viscosity Values:
S6
S7
P.S/
All the samples viscosities where measured at the same conditions.
Spindle used for all the samples was (L1).
30
5.Conclusion
• Buffering capacity:
• The rate of pH change with time representing the Buffering capacity for
each antacid was determined and compared. All the brands had their
initial pH ranging from 7.91 – 8.91. Based on the data from the
buffering capacity of the antacids analyzed, it is observed that brand
“S6” had buffering capacity being maintained for 35minutes whilst
product “S7”, had buffering capacity maintained for 40 min. Product
“S7” had the highest initial pH of 8.91 and showed a consistently
resilient change to pH with time followed by brand “S6”. The consistent
data obtained indicates the superior stability of brand “S7”, followed by
brands “S1”, “S2”, and “S6”. A demonstration of a high ANC and a
longer buffering capacity by an antacid indicates its efficacy and quality.
31
5.Conclusion
• The study has shown that all the antacid brands analyzed (n = 7) had
aluminum hydroxide and magnesium hydroxide as active acid
neutralizing agents, and some of them containing simethicone or
dimethicone as antifoam. All the brands qualified as antacids with
each having PAT pH greater than 3.5. In addition, they all recorded
ANC values above the acceptable limit of 5 mEq/g. The buffering
capacities observed were however not consistent with the ANC
except for brands “S2” and “S7” that demonstrated consistent ANC
and buffering capacity to assure quality and efficacy in vitro. The
current work has further shown that cost does not translate to quality
as both expensive and low cost brands were found within the
acceptable limits of antacid action. Antacids exert their effects by
the combined action of their acid neutralization and buffering
capacities. Therefore to improve human acceptance to the use of
antacids, it is highly recommended for manufacturers to state ANC
and BC values on labels or in drug information leaflets to assure
medicine quality, efficacy and value for money.
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6.Discussion.
consumption
• First of all, We can notice that Gaviscon has the upper hand among
the Seven samples, and this can be attributed to many reason like
Advertising: Gaviscon has a very strong advertising base. For
examples in T.V commercials, YouTube advertising, Facebook and
Instagram commercials.
From the previous study of Gaviscon sample we noticed that it has
a high Acid neutralizing capacity (20.49) as well as it has a
buffering capacity that maintained for 35 minutes, these two
parameters indicates the good quality and effectiveness of
Gaviscon as an antacid.
Gaviscon contains Sodium Alginate which gives it an additional
property by forming a floating raft on the top of the stomach to
prevent the stomach content from backing up into the esophagus.
33
• Secondly we have Acilox plus , it is highly consumed by patient in
Basra and this is basically due to its low price (2500 IQD), so its
affordable for all patients and they can get back to buy it again with no
compliance.
• Also its manufactured by pioneer company in Iraq which has a
popularity in Basra.
• thirdly, Moxal plus, and its popularity is basically due to its low cost.
And also Jolphar company has agood reputation among consumers in
Basra.
• fourth of all, we have Maalox plus, It’s the most expensive one but it’s
also consumed by a good average in Basra because of its effectiveness
and also because its produced by Sanofi French company that has a
good reputation in the pharmaceutical industry and it’s trusted by
physicians.
• The rest of the antacids (Pyrosix, Epicogel and Digel) are not highly
consumed in Basra according to our study.
Q/ through out our experiment, we noticed that Pyrosix was the best
antacid among the seven samples, but why its not so popular in Basra?
34
The seven samples were personally tested on 4 people for two weeks ,
The following results were determined.
o Pt.1/ 63 Y.O man with stomach ulcer.
o Pt.2/ 32 Y.O female with H.Pylori.
o Pt.3/ 26 Y.O female with GERD.
o Pt.4/35 Y.O female Dyspepsia.
Pt. S1 S2 S3 S4 S5 S6 S7
Pt.1 ✔️ X X X X ✔️ ✔️
Pt.2 ✔️ X ✔️ ✔️ ✔️ ✔️ ✔️
Pt.3 ✔️ ✔️ ✔️ ✔️ ✔️ ✔️ ✔️
Pt.4 ✔️ X X X X ✔️ ✔️
Note/ Both Digel and Acilox did not have a rapid onset of action
when administered (Digel delayed for 50 minutes and Acilox for 1
hour). That’s why they are not considered as a first line treatment
to relief hurt burn symptoms.
35
• These seven samples were also subjected to different circumstances in
order to test their stability.
• For example they were left outdoors for 20 days and the following was
noticed:
Maalox No change.
Digel No change.
Epicogel Epicogel
After 17 days In normal
outdoors condition
36
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