DEPARTMENT OF PHARMACEUTICS AND PHARMACEUTICAL TECHNOLOGY

STABILITY STUDIES OF METRONIDAZOLE SUSPENSION UNDER VARYING ENVIRONMENTAL AND STORAGE CONDITIONS USING PET BOTTLES

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Background: Metronidazole, a widely used antimicrobial agent, is susceptible to environmental factors that may compromise its stability and efficacy. This study investigates the stability of metronidazole suspension stored in polyethylene terephthalate (PET) bottles under different environmental conditions. Given the potential interaction between PET packaging and liquid pharmaceuticals, it is crucial to assess how temperature, light exposure, and pH affect drug degradation.
Aim: The purpose of this study is to evaluate the stability of metronidazole suspension under various environmental conditions to determine the optimal storage practices and highlight the impact of temperature, light exposure, and packaging materials on drug degradation and drug concentrations.
Method: Metronidazole suspensions were formulated and stored under various conditions, including refrigerator (4°C), room temperature (25°C), elevated temperature (55°C), sunlight exposure (38°C), and acidic and basic pH environments. Spectrophotometric analysis at 277 nm was conducted weekly for 10 weeks to determine the concentration of metronidazole remaining in each sample. The percentage of the drug remaining was calculated for each condition to evaluate the extent of degradation.
Result: By week 10, samples stored under elevated temperature (55°C) and sunlight exposure (38°C) showed significant degradation, with metronidazole content reduced to 27.33% and 41.90%, respectively. At room temperature (RT) it reduced to 76.34%, at acidic pH (AP) to 69.04%, and basic pH (BP) to 58.62%. Refrigerated storage (4°C) and dark storage provided optimal stability, maintaining over 94% of the initial drug concentration.
Discussion: The results indicate that temperature and light are critical factors affecting the stability of metronidazole in suspension. Elevated temperatures accelerate degradation, likely due to increased hydrolysis and photodegradation. In contrast, refrigeration effectively preserves the drug’s stability, reducing the risk of degradation. These findings emphasize the importance of storage conditions for maintaining the efficacy of metronidazole.
Conclusion:
Refrigeration and storage in light-protected environments are recommended for main taining the stability of metronidazole suspension. Further studies on alternative packaging materials and the long-term effects of extreme pH conditions could provide additional insights into improving drug formulation and packaging
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THE EFFECT OF RELATIVE HUMIDITY ON THE DISSOLUTION PROFILES OF CERTAIN BRANDS OF ASPIRIN TABLETS IN THE NIGERIAN MARKET

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Ensuring that medications are effective is crucial for the pharmaceutical industry. Factors like humidity can have undesirable impact on the Dissolution Profiles of these drugs, which could affect their therapeutic efficacy. This study explores the frequently disregarded connection between humidity and the Dissolution Profiles of aspirin tablet for five popular brands in the
Nigerian market. It is essential to understand this relationship to guarantee both patient safety and standard drug performance. Aim and objectives: the aim of this study was to investigate how varying relative humidity affects the dissolution profiles of the various brands aspirin tablets after prolonged storage under these conditions. Methods: The dissolution profiles of five well-known brands of aspirin tablets available in Nigeria were investigated using standard pharmacopeial methods. Two humidity levels, 0% and 70%, were used for the dissolution studies to replicate typical Nigerian ambient conditions. Dissolution Profiles were produced, and the rates and extents of dissolution under various humidity levels were compared. Results : the results from the experiment showed that Elevated relative humidity seems to quicken the process of dissolution for the five brands of aspirin used in the study which could result in quicker drug release and absorption. On the other hand, reduced humidity can hinder drug disintegration and cause a delayed release of the medication. Conclusion : This study confirmed that changes in the dissolution profiles occur when Aspirin tablets are stored under varying relative humidity conditions of 0% Relative humidity and 70%Relative humidity. This study revealed that there is an undesired reduction in the percentage of the drug released when stored at 0% relative humidity and also an undesired increase in the percentage of drug released when stored at 70% relative humidity as seen from the results over the 10 week period. It is imperative that patients, caregivers and even manufacturers are educated on the need to store tablets in facilities and areas of optimum relative humidity in order to preserve the efficacy of these drugs.
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PREPARATION AND EVALUATION OF AMLODIPINE SOLID DISPERSION USING POLYVINYLPYRROLIDONE K30

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Background: Amlodipine is a third-generation dihydropyridine antihypertensive that blocks calcium on calcium channels used frequently in hypertension and angina. It has even been listed by WHO as an Essential Medicine. Although very practical, it belongs to the Biopharmaceutical Classification System (BCS Class) II - the drug is very permeable across the intestinal wall but very low water solubility. Even the low solubility is the slowest step in absorption which may lead to the release of tablets being not fully done, inconsistent bioavailability between different patients and reliance on food. Consequently, by enhancing solubility of amlodipine we desire to make the administration of amlodipine more effective orally.
Purpose: The purpose of this work was the development, characterization, and testing of solid dispersions (SDs) of amlodipine with Polyvinylpyrrolidone (PVP K30). We thought that the method would help us to change the drug which is not soluble in large quantities but exists as crystals to a high- energy, highly soluble amorphous one. The research rigorously investigated system of varying drug- polymer ratios and characterized the optimally dispersed system completely, as a solubility was demonstrated and the in-vitro rate of solubility was significantly increased.
Material and Methods: Amlodipine solid dispersions through solvent evaporation method were prepared by us. A common organic solvent (ethanol) was used to dissolve the drug as well as the hydrophilic carrier, PVP K30. A rotary evaporator was then used to remove the solvent under reduced pressure leaving a mass of solid. This mass was dried, ground and sieved. Five ratios of drug-polymer weight were made: 1:1, 1: 2, 1:3, 1:4 and 1:5. Lastly, all Solid dispersion had their apparent aqueous solubility determined. And lastly we pressed this optimized powder into tablet form and compared the drug release of this tablet in in-vitro with that of a normal tablet in a dissolution experiment. Results: There was distinct polymer-dose-dependent increase in aqueous solubility of Mamlodipine in the solid dispersions relative to pure, unprocessed amlodipine drug. This ratio was the best solubility enhancer with the highest level of 1:5 (drug: polymer), and it was determined to completely analyze. FTIR of 1:5 Solid dispersion showed the typical peaks of the amlodipine and PVP K30, and no new peak or significant change, meaning strong chemical interaction. The most important was the Differentiated Scanning Calorimetry (DSC) thermogram, which indicated the total loss of the sharp endothermic melting point of crystalline amlodipine, which confirmed the drug had been transformed to a molecularly dispersed or amorphous form. Most importantly, the 1:5 solid dispersion to tablets discharged the drug far quicker and more certainly in-vitro when compared to the control tablets to the pure drug.
Conclusion: This experiment proves the application of PVP30 as a hydrophilic carrier in a solvent evaporation solid-dispersion method is an efficient approach to increase the solubility and dissolution rate of the poorly water-soluble amlodipine drug. The 1:4 optimization resulted in the drug being altered to a stable and amorphous form, thus a significantly better release profile. This method presents a good avenue towards the generation of novel oral dosage shapes of amlodipine that may confer improved bioavailability and dependable therapeutic results
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PRELIMINARY ANALYSIS IN TO THE FORMULATION OF PROMPT DISINTEGRATINGCIPROFLOXACINTABLETSUSINGPECTIN EXTRACTED FROM CITRUS SINENSIS PEEL AS A DISINTEGRANT

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Introduction: Disintegrating agents are used to speed up the breakdown of solid dosage forms, such as tablets and capsules, after administration. Pectin is a complex polysaccharide composed of galacturonic acid units commonly used in the pharmaceutical industry as a disintegrant due to its ability to absorb water and swell leading to the disruption of tablet structure and promoting
rapid disintegration.
Objective: To investigate the feasibility of incorporating pectin obtained from citrus sinensis peel as a fast acting disintegrant and assessing its impact on tablet disintegration and dissolution profile and to compare the performance of the locally obtained pectin based-formulations with
other disintegrants.
Method: Pectin was extracted using the hot acid extraction method and various batches of ciprofloxacin tablets (F1-F7) were prepared by wet granulation technique. The granules
produced were subjected to pre-compression (bulk and tapped densities, angle of repose, Hausner’s ratio and Carr’s index) and post compression (hardness, friability, weight uniformity and dissolution) evaluations respectively.
Results: The granular mixtures of the various batches had angle of repose between 22.53° to 28.60° indicating excellent flow. The Hausner’s ratio ranged from 1.12 to 1.22 while the Carr’s index was between 11.69% and 17.20%. The bulk and tapped densities were found to be between 0.41gm/cm3 to 0.58gm/cm3 and 0.42gm/cm3 to 0.60gm/cm3 respectively. The seven batches had uniform weight with low standard deviation values of less than ±5% which are within the
B.P limits. The hardness values ranged from 7.2 to 10.0 kg/cm2 while the friability values of 0.60- 0.98% were found to be less than 1%. The disintegration time of the pectin formulation F2-F6 ranged from 11.5-26.4min as compared with those of the standards F1 and F7 whose disintegration time value were 8.2 and 13.5 respectively. The in vitro dissolution result showed that F6 had the best dissolution profile among the formulations containing pectin.
Conclusion: Pectin obtained from Citrus sinensis at a concentration of 15% showed excellent disintegrating property when compared with sodium starch glycolate and maize starch which are super disintegrants and conventional disintegrants respectively.
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PREPARATION AND CHARACTERIZATION OF A CO- PROCESSED EXCIPIENT FOR FAST TABLET DISINTEGRATION

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Introduction: Excipients play a crucial role in pharmaceutical tablet formulation, influencing drug stability,bioavailabilty,and mechanical properties.Traditional excipients often present challenges such as poor flowability,inadequate compressibility and inconsistent drug release to address these limitations,co-processed excipients,which combine multiple excipients to enhance functionality,have gained attention.
Purpose: The primary aim of this study is to prepare and characterize a co-processed excipient for direct compression and fast tablet disintegration.
Method: The novel excipient was prepared through milling and co-processing of the selected excipient.The excipients physical and flow properties were characterized by measuring bulk density, tapped density,car’s index, hausner’s ratio, moisture content, swelling index and hydration capacity.Paracetamol tablets were formulated using the excipient in different concentrations an evaluated for weight uniformity,hardness,friability,disintegration time and dissolution rate.
Results: The co-processed excipient exhibited improved physiochemical properties with hardness(6.6-7),Disintegration time(1.45secs) and drug release profile of above 80% within 50mins in two separate batches.It showed poor flow properties with carr’s index of 60% and hydration capacity of 1.18
Conclusion: The result from the disintegration time of the different batches of tablet
formulation with the co-processed excipient showed signs of a fast disintergratig tablet with a disintegration time of 1.45secs.
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FORMULATION AND EVALUATION OF A CO-PROCESSED EXCIPIENT FOR DIRECT COMPRESSION OF GLIMEPIRIDE TABLETS.

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Co-processed excipients have been developed to enhance the performance of poorly soluble drugs like Glimepiride. Varying ratios of the API (Glimepiride) was mixed with the co-processed excipients and from the results, there was improved flowability, compressibility and disintegration properties, optimizing tablet formulation and bioavailability. Studies have demonstrated reduced lubricant sensitivity and enhanced drug release profiles. Co-processed excipients offer improved dilution potential, mechanical strength and faster manufacturing processes making co-procession a valuable advancement in pharmaceutical technology
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INVESTIGATION OF THE DISINTEGRATION BEHAVIOUR AND DISSOLUTION PROFILE OF OMEPRAZOLE IN DIFFERENT BEVERAGES

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Variable drug release from solid dosage forms has been a major cause of bioavailability problems. The two main processes by which they release drugs are disintegration and dissolution. The objective of the present study was to assess the disintegration and dissolution of Omeprazole in different beverages like Coca-Cola, Chivita juice, Hollandia yoghurt and Malta Guinness. The test was carried out per the US Pharmacopoeia standard for delayedrelease drugs. A hybrid medium of different beverages and pH 6.8 phosphate buffer (250ml) was prepared to mimic in-vivo conditions. The result showed that the disintegration time increased in Hollandia yoghurt, while it decreased in Coca-Cola, Malta Guinness and Chivita juice. As the viscosity of fluid increases, the disintegration time was also increased. Coco- cola which contains Carbon Dioxide is implicated in reducing the disintegration time of omeprazole. Since the dissolution profile phase of the study, the results reflected that the drug release was retarded in Hollandia yoghurt and it was sufficiently released in Coca-Cola, Malta Guinness and Chivita juice. From the above study, it can be concluded that there is variation in the disintegration time and dissolution profile of the studied drug in different beverages. Hollandia yoghurt had poor disintegration and dissolution quality compared to other dissolution media used.
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GREEN SYNTHESIS OF COPPER NANOPARTICLES USING VERNONIA AMYGDALINA LEAF EXTRACT AND ITS ANTIMICROBIAL ACTIVITY

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Pharmaceutical nanotechnology deals with the formation and development of substances of molecules and atoms ranging from size 0.1 – 100nm which can be further developed into special structures and devices with desired characteristics. This study employed green chemistry to synthesize copper nanoparticles (CuNPs) using fresh leaf extract of Vernonia amygdalina. The resultant CuNPs were investigated by UV-Vis spectroscopy. Fresh leaves were collected and identified, aqueous extraction was then carried out on the washed leaves using water at 60°C. The existence of flavonoids, tannins, glycosides and alkaloids in the plant extract actas reducing, stabilizing and capping agents that reduces the metal ion to form metal nanomaterials. The UV-Vis absorption spectra show maximum absorption at 543nm. The synthesized nanoparticles (NPs) were tested for their in vitro antimicrobial activity against the bacterial strain Staphylococcus aureus using the agar well diffusion method and compared with the following test samples (copper salt solution, plant extract alone, mixture of copper salt solution and plant extract). From the result of the antimicrobial evaluation of the copper nanoparticles, the copper nanoparticles showed the highest zone of inhibition
when compared to the other test samples. This is possible due to the nano-dimension of nanoparticles which increases the surface area of the particles, hence leading to increased antimicrobial activity
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A COMPARATIVE EVALUATION OF THE EMULSIFYING PROPERTIES OF THE STARCH EXTRACTED FROM THE CERTAIN SPECIES OF MUSA SAPIENTUM AND MUSA ACUMINATA

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Emulsions are generally unstable formulations, hence the need for an emulsifying agent to be incorporated into the preparation.Emulsifying agents can be obtained from natural sources which are readily available, cheap and biodegradable. AIM of the study-This study investigated starches obtained from two banana species i.e Musa acuminata and Musa sapientum as naturally occurring emulsifying agents that can be used in the formulation of pharmaceutical emulsions. SPECIFIC OBJECTIVE OF THE STUDY-The specific objective of the study was to extract and evaluate the emulsifying properties of starch obtained from certain banana species. Method:Starches were isolated from ground unripe banana fruit species using already established method.The unripe banana fruit were peeled, washed, milled and the slurry was passed through a mesh seive.The filtrate was allowed to settle and water was decanted to obtain the starch. Varying concentrations (5-30%w/v) of the starches obtained from the banana species were employed in the preparation of the emulsion.Physicochemical characterization of the starches obtained from the banana species were carried out and compared with maize starch as standard.Parameters evaluated included viscosity and the effect of age on globule size and size distribution and the globule structure. Results:The result showed the yield of Musa acuminata and Musa sapientum was 10.17%w/w and 14.21%w/w respectively. It also showed an increase in viscosity(rate of flow)with an increase in the concentration of the emulsifying agent (5-30%w/v ) with the range 760- 10728±171.06(sec) for maize starch,466-7204.8±82.12(sec) for Musa acuminata and 114- 5618±299.83(sec)for Musa sapientum.It also showed that there was a decrease in the globule number of the emulsion and an increase in the globule size after 7days which showed 1.75- 3.94±1.37(mm) for Musa acuminata ,1.57 -3.0±0.71(mm)for Musa sapientum and 2.25- 3.0±0.71(mm) for maize starch which is the standard.The study showed that Musa acuminata is more favorable as an emulsifying agent than Musa sapientum when compared to maize starch.The study also showed cracking and phase separation in the emulsion from the 7th day and it was observed that there was a reduction in the viscosity of the preparation with time . Conclusion: The study showed that the yield obtained from Musa sapientum and Musa acuminata were 14.21% and 10.17% respectively. However the yields are poor and not economical.This calls for improvement in the methods for extraction of the starch from the unripe fruit .Musa acuminata compared more favorably with maize starch than Musa acuminata and hence can be used as emulsifying agents in the formulation of pharmaceutical emulsions and hence they can be used as an emulsifying agent in pharmaceutical emulsions
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COMPARATIVE STUDY OF THE DISINTEGRANT PROPERTIES OF MAIZE STARCH AND BAMBARA NUT STARCH ON METRONIDAZOLE TABLETS

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Disintegrants expand and dissolve when wet causing the tablet to break apart in the digestive tract, releasing the active ingredients for absorption. They can be added extra-granularly, intra-granularly or both during tablet formation. A standard disintegrant used extensively for tablet formation is maize starch. There is a growing interest in locally sourced tablet excipients, hence the disintegrant property of indigenously sourced Bambara nut (Vigna subterranea) starch and its effect on metronidazole tablets is evaluated in this study The purpose of the study is to compare the effect of the disintegrant properties of various concentrations of Bambara nut starch (Vigna subterranea) and maize starch BP on metronidazole tablets. The starch from Vigna subterranea seeds was extracted and its disintegrant ability was compared to that of maize starch BP at concentrations of 10%, 15%, 20%, 25% in metronidazole-based tablets. All other parameters were kept constant during the formulation process. The organoleptic properties, bulk and tapped density and the chemical properties of the starch of Vigna subterranea was determined. The flow properties of the granules formed with both starches were determined and the metronidazole tablets were evaluated for weight uniformity, dimensions, tablet hardness, friability, disintegration and dissolution rates. The metronidazole granules and tablets formulated with the starch from Vigna subterranea were comparable in granule flow properties, tablet weight, variation, hardness, friability. The study revealed that Vigna subterranea starch used as a disintegrant performed better with a shorter disintegration time than tablets formulated with the different concentrations of maize starch BP. It was discovered that 20% and 25% of the starches were not adequate for tablet formation due to their friability values of above 1%. This study revealed that Vigna subterranea starch can be used as a disintegrant in the production of tablets of adequate pharmaceutical quality. It serves as an adequate disintegrant for metronidazole tabletskey words
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