ABSTRACT

 

The active drug content and weight uniformity of five brands (A – E) of Amoxicillin Trihydrate
capsules in Nsukka open drug market were evaluated to ascertain their quality assurance
using UV visible spectroscopy and gravimetry. This study has shown that all the brands
analyzed showed significant variations with respect to active drug content determination for the
three brands B, D and E. Using United State Pharmacopoeia (USP) and British Pharmacopoeia
(BP) specifications of 90 – 110 %, the values obtained were B – (413.525 mg), D – (440.325
mg), E – (414.100 mg). These values were within the general drug acceptance limit of 80 – 110
% but failed the antibiotic amoxicillin trihydrates USP and BP specifications with acceptable
limit of 90 – 110 % determined at 266 nm. The percentage mean content of all the brands (A –
E) were 77.64, 82.80, 74.24, 88.07 and 82.82. All the brands passed the weight uniformity test
with coefficient of variation CV value range of ± 0 – 5 % for capsules more than 250 mg
according to USP and BP specifications. However, with the result obtained, the
consequences are that it poses a serious threat to the health of the entire people of West
Africa sub regions that depend on these drugs for therapeutical response. As all the drugs
assayed were below the acceptance limit requirement of antibiotic amoxicillin trihydrate
and thus, can lead to serious health implications such as drug resistance, cardiac failure,
etc. Drug regulatory bodies should be at alert and they should conduct strict routine check
on all the NAFDAC satisfied companies as all the drugs analyzed compromise their
quality because of profit reasons.

 

TABLE OF CONTENTS

 

Title Page – – – – – – – – – – – i
Certification Page – – – – – – – – – – ii
Dedication – – – – – – – – – – – iii
Acknowledgement – – – – – – – – – – iv
Table of Contents – – – – – – – – – – v
Abstract – – – – – – – – – – – vi
CHAPTER ONE
1.0 Introduction – – – – – – – – – – 1
1.1 Antibiotics – – – – – – – – – – 1
1.2 Modern Antibiotics – – – – – – – – – 1
1.3 Fake Drug – – – – – – – – – – 2
1.4 Drug regulatory And Enforcement Agent – – – – – – 3
1.5 Drug Professionals – – – – – – – – – 4
1.6 Informal Drug Sellers – – – – – – – – – 5
1.7 Dangers Associated With Purchasing from informal drug sellers – – 6
1.8 Aims and Objectives – – – – – – – – – 7
CHAPTER TWO
2.0 Literature review – – – – – – – – – 8
2.1 Amoxicillin Trihydrate – – – – – – – – – 8
2.2 Properties of Amoxicillin Trihydrate – – – – – – – 8
2.3 β- Lactam Antibiotics – – – – – – – – 10
2.4 Amoxicillin Capsule – – – – – – – – 11
2.5 Medical Uses of Amoxicillin Trihydrate – – – – – – 17
2.6 Side Effect of Amoxicillin Trihydrate – – – – – – – 18
2.7 Instrumentation Method of Analysis – – – – – – 18
2.7. 1 High Performance Liquid Chromatography – – – – – – 18
2.7.2 Operation – – – – – – – – – – 19
2.7.3 Partition Chromatography – – – – – – – – 20
vi
2.7.4 Normal-Phase Chromatography – – – – – – – 21
2.7.5 Displacement Chromatography – – – – – – – 22
2.7.6 Reversed – Phase Chromatography – – – – – – – 23
2.7.7 Sized- Exclusive Chromatography – – – – – – – 25
2.7.8 Ion – Exchange Chromatography – – – – – – – 26
2.8 Voltammetry – – – – – – – – – – 27
2.8.1 Theory – – – – – – – – – – – 28
2.9 Liquid Chromatography – Mass Spectrometry – – – – – – 29
2.9.1 Liquid Chromatography – – – – – – – – 29
2.9.2 Flow Splitting – – – – – – – – – – 30
2.10 Electrospray Ionization — – – – – – – – 31
2.10.1 Ionization Mechanism – – – – – – – – 31
2.10.2 Variants – – – – – – – – – – 31
2.10.3 Applications – – – – – – – – – 32
2.10.4 Noncovalent Gas Phase Interations – – – – – – – 32
2.11 Diferential scanning Calorimetry – – – – – – – 33
2.11.1 Detection Phase Transition – – – – – – – – 33
2.11.2 DTA – – – – – – – – – – – 34
2.11.3 DSC Curves – – – – – – – – – – 34
2.11.4 Applications – – – – – – – – – – 34
2.11.5 Polymers – – – – – – – – – – 35
2.11.6 Liquid Crystals – – – – – – – – – 36
2.11.7 Oxidative Stability – – – – – – – – – 36
2.11.8 Safety Screening – – – – – – – – – 36
2.11.9 DSC in Drug Analysis – – – – – – – – 37
2.11.10 General chemical analysis – – – – – – – 37
2.12 Review of Some of the Works Assayed On Drug Analysis – – – 37
2.13 Ultraviolet Spectroscopy – – – – – – – – 39
2.13.1 Physical Methods of Analysis – – – – – – – 39
2.13.2 Spectrophotometry – – – – – – – – – 41
2.13.3 Terms Used In UV Spectroscopy – – – – – – – 42
vii
2.14 Absorption Laws – – – – – – – – – 45
2.14.1 Instrumentation – – – – – – – – – 46
2.14.2 Light Sources — – – – – – – – – 48
2.14.3 Cells – – – – – – – – – – – 48
2.14.4 Routine Methodology in Spectrophotometric Analysis – – – – 48
CHAPTER THREE
3.0 Materials and Methods – – – – – – – – – 49
3.1 Materials – – – – – – – – – – – 49
3.2 Methods – – – – – – – – – – – 49
3.2.2 Active Drug Content Determination – – – – – – – 49
3.3 Weight Uniformity Test — – – – – – – – 50
CHAPTER FOUR
4.0 Results and Discussion – – – – – – – – – 51
4.1 Results – – – – – – – – – – – 51
4.2 Discussion – – – – – – – – – – 63
CHAPTER FIVE
5.0 Conclusion – – – – – – – – – – 64
References – – – – – – – – – – – 74

 

CHAPTER ONE

1.0 INTRODUCTION
1.1 ANTIBIOTICS
An antibiotic is a compound or substance that kills or slows down the growth of
bacteria [1]. The term is often used synonymously with the term antibacterial; however,
with increased knowledge of the causative agents of various infectious diseases,
antibiotic(s) has come to denote a broader range of antimicrobial compounds, including
antifungal and other compounds [2]. It can be loosely defined as the variety of substances
derived from bacterial sources (microorganisms) that control the growth of or kill other
bacteria. However, synthetic antibiotics, usually chemically related to natural antibiotics,
have since been produced that accomplish comparable tasks.
1.2 Modern antibiotics
The term “antibiotics” was coined by Selman Waksman in 1942 to describe any
substance produced by a micro-organism that is antagonistic to the growth of other
micro-organism in high dilution [3]. This definition excluded substances that kill bacteria,
but are not produced by microorganisms (such as gastric juices and hydrogen peroxide).
It also excluded synthetic antibacterial compounds such as the sulphonamides. Many
antibiotics are relatively small molecules with a molecular weight less than 2000 atomic
mass units [3].With advances in medicinal chemistry, most antibiotics are now semi
synthetic modified chemically form of the original compounds found in nature,[4] as is the
case with beta-Lactams (which include the penicillins, produced by fungi in the genus
penicillium, the cephalosporins, and carbapenems). Some antibiotics are still produced
and isolated from living organisms, such as the amino glycosides and others have been
created through purely synthetic means, the sulphonamides, the quinolones, and the
oxazolidinones[4]. In addition to this origin-based classification into natural, semi
synthetic, and synthetic, antibiotics may be divided into two broad groups according to
2
their effect on micro-organisms. Those that kill bacteria are bactericidal agents, whereas
antibiotics are commonly classified based on their mechanism of action, chemical
structure, or spectrum of activity [4]. Most antibiotics target bacterial functions or growth
processes. Antibiotics that target the bacterial cell wall (penicillin, cephalosporins), or
cell membrane (polymixins), or interfere with essential bacterial enzymes (quinolones,
sulphonamides) are usually bactericidal in nature. Those that target protein synthesis,
such as the amino glycosides, macrolides and tetracyclines are usually bacteriostatic.
Further categorisation is based on their target specificity.
Narrow spectrum” antibiotics target particular types of bacteria, such as Gramnegative
or Gram-positive bacteria, where as broad spectrum antibiotics affects a wide
range of bacteria. In the last few years, three new classes of antibiotics have been brought
into clinical use. This follows a 40-year hiatus in discovering new classes of antibiotics
compounds. These new antibiotics are of the following three classes; cyclic lipopeptides
(daptomycin), glyclycyclines (tigecyclines), and oxazolidinones (linezolid).Tigecyclines
is a broad spectrum antibiotics, where as the other two are used for Gram-positive
infections. These developments show promise as a means to counteract the bacterial
resistance to existing antibiotics.
1.3 FAKE DRUGS
Fake drugs otherwise called ‘counterfeit drugs’ can be defined as drug that are unfit for
usage and human consumption and therefore constitute hazard to good and sound health.
Considering the above definition, the evil effect of fake drugs can be better understood by
looking back to what the situation was several years back, before the country got to her
present situation. The situation could be said to have gone bad many years back when our
hospitals changed from health institutions of excellence to mere consulting clinics
occasioned by non-availability of drugs. As a result of this problem, dubious and
unpatriotic persons came in with fake drugs which they supplied to the hospitals. Added
to these problems are the activities of smugglers who perhaps because of the porous
3
nature of the Nigerian boarders and the connivance of some law enforcement agents,
bring fake drugs into the country [5].
Faking of drugs is a global public health problem, because the effects can be felt
from both the country of manufacture to the recipient countries. Hence, national measures
for combating fake drugs in a country might be insufficient because of the advanced
sophistications of those who manufacture and sell them [5]. Nigeria is not an exception in
the problems of fake drugs till date. Some people still prefer to self medicate when they
are ill, and often time the drugs are bought from unlicensed drug vendors, whose drug
quality is not sure. Through the past two decades in Nigeria, the problem of fake drugs
has been a very big issue. In addition, fake drugs proved a major factor in contributing to
high death rates. Over 50 children died in 1989 as a result of a formulation error in a drug
[5]. Such problems led to the establishment of National Agency for Food Drug
Administration and Control (NAFDAC), which would help create a fake-drug-free
environment [5]. The intent was to ensure effective registration of good quality drugs that
are inexpensive in Nigeria. Since the inception of NAFDAC in April 2001, the
commission has worked hard in combating the problems of sale of fake drugs, but yet to
no avail [5]. Questions are, ‘why does Nigeria still have in existence open drug markets?
Why do Nigerians in drug business breech the stipulated drug laws and still get
away with it and continue with their business, committing mass murder and smiling to
their banks? How long do we fight the battle of fake drug even with the threats on our
lives who want to preserve the health of the Nation? The consistent raids by NAFDAC on
fake drug dealers who contravene the applicable laws and regulations, have helped in
clamping down on the illegal drug traders but when things seem as if it’s getting better,
these illegal drug sellers begin to emerge from their hideouts [5]. I continue to wonder,
why? Could it be that the agency is not doing enough to stop the evil activities, or could
the problem be from the drug sellers themselves? The tragic irony is that the problems of
fake drug have refused to go away from the shores of Nigeria.
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1.4 DRUG REGULATORY AND ENFORCEMENT AGENCY
The role of any drug regulatory agency is the protection and promotion of public health.
The enforcement directorate arm of NAFDAC established under the provisions of the
counterfeit and fake drugs (miscellaneous provision) act is charged with the
responsibility of enforcing the provisions of the counterfeit and fake drug decree, which
includes:
Ø Conducting surveillance on companies and persons suspected to be violating
NAFDAC regulations and carrying out investigations on such persons and
companies.
Ø Paying unscheduled visits to all ports of entry and border posts and
interrogation of suspects.
Ø Sampling of NAFDAC regulated products for laboratory analysis and
compilation of case files.
Ø Raiding of drug hawkers and destruction of fake and spurious regulated
products.
Ø Coordination of activities of state task force.
Ø The establishment of the task force in Nigeria was seen as a welcome
development for the fight against fake drugs.
1.5 DRUG PROFESSIONALS
The main professional organization of pharmacist in Nigeria is the Pharmaceutical
Society of Nigeria (PSN). The organization was established in 1927, with membership
over 7000 pharmacists [6]. Its main functions are to determine the skill and knowledge
that is required of anyone who seeks to be registered as a member of the pharmacy
profession, preparation and review of the code of conduct, regulate and control the
practice of the pharmacy profession. PSN also has a panel that investigates and
disciplines erring pharmacists.
According to the PSN president, the main sources of fake drugs in Nigeria are
India, China, Pakistan, Egypt and Indonesia [7]. The influx of fake drugs is quite
5
worrisome to the health experts. It is difficult to get reliable data on mortality or
morbidity caused due to the consumption of fake drug in Nigeria. In 1987, an increased
number of fake drugs were noticed in some market places, even in some pharmacy
outlets [7]. Chemical test showed that they contain smaller amount of the active ingredient
of the drugs. Some pharmaceutical companies felt it was due to laxity of inspection that
contributes to the successful faking. On 31 October 1987, the Pharmaceutical Society of
Nigeria (PSN) discussed the implication of fake drug manufacturing, marketing as well
as possible remedies; they identified some major drugs that are often faked viz;
antibiotics, antifungal agents, antihypertensive, malaria medicines, bronchodilators and
hormonal preparations. They related the problem of drug faking to exchange control
situation that causes scarcity and high price for drugs and that government can help
reduce the problems through provision of essential drugs at reasonable price to the people
which will in turn make fake drugs low priced and less attractive [8].The effect from fake
drug consumption usually goes unnoticed, except in cases where it results to mass death.
These problems made the PSN as a body to pressure Nigerian government in taking
definite step towards the control of fake drug. Hence, the promulgating of the counterfeit
and fake drug decree No. 21 of 1988 that prohibits the sale and distribution of fake drugs
in open markets and created penalties for anyone who breaches the law [6]. In United
States of America, pharmacists are allowed to work with foreign governments,
international regulatory bodies as well as law enforcement agencies. This collaboration
enables them to detect and combat counterfeiting [9]. In Cuba, almost all pharmaceutical
operations are owned and managed by the government who determines how drugs are
regulated and the members of their drug professional groups can get involved in drug
regulation by joining the advisory committee [10].
1.6 INFORMAL DRUG SELLERS
Informal drug sellers are people that sell drugs in an unregulated manner without
professional consultation and with limited knowledge of pharmacy. Their main aim in
drug business is the profit they make even when they are aware of fake drug proliferation.
6
They can store and handle drugs in inappropriate ways that can endanger the drug
potency [11].
Informal drug sellers can be found in shops, kiosks, open markets, general stores
etc, and can operate as itinerant hawkers. Just like any other business, their existence is
maintained in accordance to consumer demands for easy accessibility, convenience and
affordable supplies. They can be very friendly, approachable and promising to their
customers. Their attraction to those that patronizes them is that they have cheaper
products when compared to the formal Outlets and their products can be given on credit
because they source their products from cheaper sources. Most of these drug sellers are
less knowledgeable about the doses of drug appropriate for a particular illness; their
prescription could be higher or lower than the correct dosage because their major aim is
more on profit making and meeting up with competition from other sellers [11].
1.7 Dangers associated with purchasing from informal drug sellers
Consumers/buyers are exposed to dangers from hazardous drugs because they are
entrapped in the web of fake drugs without respite and any one can be a victim. Many
drugs are offered for sale in Nigeria without expiration dates and can be bought and sold
over the counter or by hawkers selling alongside newspaper vendors (personal
observation). A man who is sick can walk to any drug store and come out with
prescriptions loaded with drugs. In some cases, smooth talking drug peddlers in public
buses save such a man the walk to a drug outlet. Consumers on the other hand may not
know the quality of products they are purchasing [11]. The reasons why consumers prefer
to patronize such outlets include geographical accessibility,
Shorter waiting times, longer opening hours, greater confidentiality, more personable
social interaction, ease of seeking advice, lower cost, flexible pricing policies and no
separate fee charged for advice. However, one of the problems associated with selfmedication
with drugs from these sellers is that in most cases, neither the drug seller nor
the consumer is aware of the correct dosage and duration of treatment [12].
7
1.8 AIMS AND OBJECTIVES
(a.) To assay some brands of amoxicillin trihydrate in the Nigerian market with a view
to ascertain the quality assurance using official standards for quality drug samples.
(b.) To determine the drug claim of active ingredient of the brands of amoxicillin
trihydrate with strength 500 mg.
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