AN INVESTIGATION OF THE IMPACT OF STORAGE CONDITIONS ON SOME PHARMACOLOGICAL CHARACTERISTICS OF POWDERS AND TABLETS

AN INVESTIGATION OF THE IMPACT OF STORAGE CONDITIONS ON SOME PHARMACOLOGICAL CHARACTERISTICS OF POWDERS AND TABLETS

ABSTRACT

The storage conditions of pharmaceutical products can significantly affect their pharmacological characteristics, potentially compromising their efficacy and safety. This research study aims to explore the influence of storage conditions on the properties and performance of powders and tablets, shedding light on their stability, dissolution rates, bioavailability, and other relevant pharmacological attributes.The investigation will involve subjecting samples of powders and tablets to varying storage conditions, including temperature, humidity, light exposure, and other environmental factors. Comprehensive analyses will be conducted to assess changes in physicochemical properties, drug release profiles, and potential alterations in pharmacokinetic behavior and pharmacokinetic profiles of exposed samples of ciprofloxacin marketed by hawkers in the three senatorial areas of Gombe State. Sample A represents non-exposed and control while samples B, C, and D represent exposure to different environmental conditions in the Gombe state for three months. The in vitro quality control of the drug sample was carried out using 2002 and 2009 B.P. standards. The parameters determined were identification, assay, disintegration, dissolution, and friability tests. The method used was adopted and validated by U.V spectrophotometry and a wavelength (λmax) of 271 nm was measured which served as our working wavelength. The validation parameters used were: Precision (within a day and between days), percentage extraction recovery, and linearity.  In the pharmacokinetics studies, six healthy volunteers were enrolled and were administered 500 mg of ciprofloxacin each non-exposed, and the exposed samples of the ciprofloxacin and saliva samples were collected before and after administration with a washout period of one week-intervals between studies.  The results indicated that all the samples showed identification tests. Friability and disintegration values were within the acceptable limits ( ≤ 1% and ≤ 30 min respectively). The dissolution and assay parameters of the exposed sample D were 66% and 82.9% which were less than the accepted limits of ≥ 70% and

95-105% respectively indicating low quality compared to others. The within-day and between-day precision were 1.1 and 1.5 % RSD respectively and within the acceptable limit of ≤ 2%. The percentage extraction recovery was 98.8% which was within the acceptable range of 95-105%. The calibration curve that was constructed was found to be linear within 1-6 μg/ml with a correlation coefficient of 0.998. When sample A was compared with each of samples B, C, and D, there was no significant difference except between sample A and D which showed a significant (p ≤ 0.05) change in elimination half-life (t1/2β), 3.03 h for A and 1.63 h for D; and elimination rate constant (Kβ), 0.28 h^-1 for A, and 0.638 h^-1 for D. Elimination half-life and elimination rate constant are parameters that determine how drugs are removed from the body. The shorter half-life shown for sample D means the exposed drug will be easily removed from the body. This may give a sub-therapeutic drug level and loss of antibacterial activity. It can be concluded that the environmental conditions of the senatorial area where ciprofloxacin tablet sample D was exposed affected its assay, dissolution, elimination half-life, and elimination rate constant profiles thereby affecting its quality and pharmacokinetics.

 

CHAPTER ONE

INTRODUCTION

1.1 Background

Pharmaceutical powders and tablets are widely used dosage forms for the delivery of medications due to their convenience, stability, and ease of administration. The quality, safety, and efficacy of these dosage forms are of utmost importance to ensure optimal patient outcomes. However, the storage conditions to which pharmaceutical powders and tablets are exposed can have a significant impact on their stability and pharmacological characteristics. Ensuring the safety and effectiveness of drug products relies on their consistent quality and reproducibility across different batches. To maintain this quality, drug manufacturers are responsible for testing their products during and after manufacturing, as well as at regular intervals throughout the product’s shelf life. The quality of medicines plays a vital role in ensuring that pharmaceutical products are suitable for their intended use, meet the requirements of marketing authorization, and do not pose risks to consumers (Jackson et al., 2011). A drug product refers to the final form of medication, such as tablets, capsules, or injectables, containing active pharmaceutical ingredients (API) in combination with inactive ingredients known as excipients (Shargel et al., 2010).

To meet the criteria for good quality, a product must adhere to the established standards outlined in official monographs, both at the national and international levels. These monographs provide detailed procedures for manufacturing specific items, along with specifications for expected quality. For example, tablets from the same batch should exhibit consistent physicochemical properties, such as uniform weight, weight variation within ±5%, consistent levels of the active ingredient, appropriate hardness for handling and disintegration in the gastrointestinal tract, and a minimum release of 70% of the active ingredient into a dissolution medium within 45 minutes (Yabo, 1996; Ogar et al., 2015). However, even when tablets from all batches comply with these standards, they may not be stored properly from the time of manufacture to the point of dispensing to patients. During transportation between these two points, drugs are exposed to various environmental conditions. Environmental factors such as light, heat, humidity, and stress can alter the physicochemical properties of drug products, leading to changes in stability, solubility, membrane permeability, and drug interactions with different tissues (Bajaj et al., 2012; Hedaya, 2007). These changes can ultimately impact the pharmacokinetic profile of the drug product (Yabo, 1996), which is particularly crucial for antibiotics like ciprofloxacin, whose bactericidal activity depends on concentration (Jacobs, 2001).

Numerous factors can influence the stability of pharmaceutical products during storage, including temperature, humidity, light exposure, and packaging materials (Smith et al., 2018). Temperature variations can accelerate chemical reactions, leading to the degradation of active pharmaceutical ingredients (APIs) and the formation of impurities or degradation products (Dahl et al., 2016). High humidity levels can promote moisture uptake by powders and tablets, potentially causing changes in their physicochemical properties, such as altered dissolution rates or physical instability (USP, 2020). Light exposure, especially to ultraviolet (UV) radiation, can induce photochemical reactions in certain APIs, resulting in reduced potency or the generation of harmful photoproducts (Zhang et al., 2017). Additionally, the selection of appropriate packaging materials is crucial to protect pharmaceutical products from external factors and maintain their stability throughout their shelf life (Patel et al., 2019).

Understanding the impact of storage conditions on the pharmacological characteristics of powders and tablets is vital for ensuring the safety and effectiveness of pharmaceutical products. By investigating the effects of temperature, humidity, light exposure, and packaging materials on pharmaceutical formulations, potential risks, and challenges associated with storage can be identified and addressed. This knowledge can assist pharmaceutical manufacturers, regulatory authorities, and healthcare professionals in establishing appropriate storage guidelines and recommendations to maintain the quality and efficacy of pharmaceutical products.

Furthermore, with advancements in pharmaceutical technology and the increasing complexity of drug formulations, evaluating the impact of storage conditions specific to each formulation becomes essential. Different APIs and excipients may exhibit varying sensitivities to environmental factors, necessitating formulation-specific storage conditions to ensure product stability. Hence, researching the impact of storage conditions on powders and tablets will contribute to the existing knowledge base, providing valuable insights for the development of robust storage strategies and guidelines tailored to different pharmaceutical formulations.

1.2 Statement of Research Problem

The storage conditions of pharmaceutical powders and tablets play a critical role in their stability and pharmacological characteristics. However, in Nigeria, there are significant challenges in maintaining appropriate storage conditions for pharmaceutical products, which can have a detrimental impact on drug availability, suitability for consumption, and overall burden on the populace and the health sector.

Nigeria faces various storage challenges that compromise the integrity of pharmaceutical products. Firstly, inadequate infrastructure and unreliable power supply contribute to inconsistent temperature control, exposing drugs to unfavorable conditions such as high temperatures, which can accelerate degradation and reduce efficacy. Secondly, the lack of proper humidity control in storage facilities leads to increased moisture uptake by powders and tablets, resulting in physical and chemical instability. Additionally, inadequate protection against light exposure, particularly UV radiation, can lead to the degradation of active ingredients, rendering drugs less potent or potentially generating harmful by-products.

These storage challenges have significant implications for drug availability and suitability for consumption. Pharmaceutical products that are improperly stored may experience reduced potency, altered dissolution rates, or physical deterioration, making them less effective or potentially harmful when consumed by patients. This not only compromises the therapeutic outcomes for individuals but also poses risks to public health. It further exacerbates the burden on the populace and the healthcare sector by necessitating the need for additional medications or treatments due to the diminished efficacy of improperly stored drugs.

Therefore, there is a pressing need for research to investigate the impact of storage conditions on the pharmacological characteristics of powders and tablets in Nigeria. By understanding the specific storage challenges faced in the country and their consequences on drug availability and suitability for consumption, this research can provide valuable insights for the development of strategies to overcome these challenges. Implementing appropriate storage guidelines and recommendations tailored to the Nigerian context can help improve the overall quality, safety, and efficacy of pharmaceutical products, benefiting the populace and alleviating the burden on the healthcare sector.

1.3 Research Aim and Objectives

This research aims to investigate the impact of storage conditions on the pharmacological characteristics of powders and tablets. The specific objectives of this study are as follows:

1. To evaluate the influence of temperature variations on the stability of pharmaceutical powders and tablets.
2. To assess the effect of humidity levels on the physicochemical properties of powders and tablets.
3. To examine the impact of light exposure on the degradation of active pharmaceutical ingredients (APIs) in powders and tablets.
4. To compare the stability and dissolution profiles of powders and tablets stored under different packaging materials.
5. To provide recommendations for optimal storage conditions to maintain the quality and efficacy of pharmaceutical powders and tablets.

1.4 Significance of the Study

Understanding the impact of storage conditions on the pharmacological characteristics of powders and tablets is crucial for ensuring the safety and efficacy of pharmaceutical products. This research will contribute to the existing knowledge by providing valuable insights into the factors that influence the stability and quality of powders and tablets during storage. The findings of this study can aid pharmaceutical manufacturers, regulatory authorities, and healthcare professionals in establishing appropriate storage guidelines and recommendations for pharmaceutical products, ultimately benefiting patients and improving the overall quality of healthcare.

1.5 Research Methodology

This research will employ a combination of experimental and analytical approaches to investigate the impact of storage conditions on the pharmacological characteristics of powders and tablets. Pharmaceutical formulations will be prepared, and representative APIs will be selected for inclusion in the powders and tablets. The formulations will be subjected to controlled storage conditions, including temperature variations, humidity levels, light exposure, and different packaging materials. The stability of the formulations will be assessed using various analytical techniques, including spectroscopy, chromatography, and dissolution testing. Statistical analysis will be performed to analyze the data obtained from the experiments.

1.6 Organisation of the Thesis

This thesis will be organised into five chapters. Chapter One provides an introduction to the research topic, including the background, aim, objectives, significance, and methodology. Chapter Two presents a comprehensive review of the relevant literature on the impact of storage conditions on pharmaceutical powders and tablets. Chapter Three describes the materials and methods used in the research, including the selection of APIs, formulation preparation, storage conditions, and analytical techniques. Chapter Four presents the results and data analysis, followed by a discussion of the findings. Finally, Chapter Five provides the conclusion, summarises the key findings, and proposes recommendations for future research.

AN INVESTIGATION OF THE IMPACT OF STORAGE CONDITIONS ON SOME PHARMACOLOGICAL CHARACTERISTICS OF POWDERS AND TABLETS, PHARMACEUTICAL SCIENCES  FAULTY PROJECT TOPICS AND MATERIALS

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