Development and evaluation of Metronidazole containing topical gel using different gelling agents (original) (raw)
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Asian Journal of Pharmaceutical and Clinical Research
Objective: Emulgels as topical dosage form recently gains an interest represent a combination of gels and emulsions in united form. Metronidazole is an antimicrobial and anti-inflammatory drug, as the first topical therapy approved for rosacea; metronidazole has remained a cornerstone of rosacea management. Methods: Emulgel formulations of metronidazole benzoate were prepared using two types of gelling agents, Carbopol 940 and hydroxypropyl methylcellulose, the influence of type and concentration of them on the release of metronidazole benzoate was investigated. The prepared formulations were evaluated on the basis of pH, spreadability, viscosity, drug content, in vitro release, and compatibility studies. Results: All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and pH value. Conclusion: The best formulation (F4) prepared using Carbopol 940 as gelling agent showed the highest drug release through 5 h.
Aim of present research work was to develop polycarbophil based mucoadhesive vaginal gel comprising of novel combination of Miconazole nitrate (MIZ) & Metronidazole (MNZ) for the treatment of vaginitis. FT-IR studies revealed no interactions. Gel formulations were characterized for pH, spreadability, viscosity, rheological properties, mucoadhesive force, drug content, in vitro drug release study, drug release kinetics studies & antimicrobial efficacy studies. The pH & spreadability was found to be 4.19 & 5.5 to 8.1 cm, which is compatible with vaginal pH & indicates easy spreadability. F5 & F8 were selected as the best formulations with optimum gel viscosity of 22480 & 24800 cps respectively. The detachment stress of the optimized batch was found to be 81.06 & 88.11 respectively. Drug release was non-diffusion controlled. Microbiological studies revealed faster release of drugs than the commercial markets product of Metronidazole & Miconazole nitrate, expressed as inhibition zone. The stability study as per ICH guidelines revealed that the optimized batch holds promise for a high stability. It can be concluded that formulation batch F5 & F8 was considered optimized since it showed better release pattern of both drugs along with other parameters such as viscosity & mucoadhesive properties.
Formulation and Characterization of Micro Sponge Loaded Topical Gel Preparation of Metronidazole
2017
Key Words Metronidazole topical gel, Micro sponge formulation, Over-the-counter (OTC) Permeation enhancer Micro-sponge containing Metronidazole as active constituent with four different formulations by changing the proportions of drug (Metronidazole), polymer (ethyl cellulose), emulsifier (Poly vinyl alcohol) were obtained successfully using emulsion solvent diffusion method. Metronidazole topical gel is used in the treatment of fungating tumours, rosacea. The drug was chosen because unavailable micro sponge dosage forms in the market in order to decrease the skin irritation by preventing excess accumulation of drug on epidermis. The size of the micro sponges can be varied, usually from 5-300 μm in diameter, depending upon the degree of smoothness or after-feel required for the end formula. The micro sponge system can also avoid unnecessary accumulation of ingredients within the epidermis and the dermis. Potentially, they can reduce considerably the irritation of effective drugs wit...
Design and Evaluation Of Metronidazole Vaginal Tablet For Once Daily Administration
International Journal of ChemTech Research
In this study bioadhesive sustained release tablets of metronidazole for once daily administration were formulated. This formulation helps to increase the localized effect of metronidazole by formulating the vaginal bioadhesive tablet and to increase the ease of application when compared to various types of vaginal gels and creams that are available in the market.Metronidazole is a nitro imidazole derivative class of anti-protozoal drug used to treat amoebiasis, vaginitis, trichomonal infections, trepenomal infections and giardisis. The objective of the present study is to formulate the bioadhesive controlled release drug delivery system which would remain in contact with the vaginal tissue for prolonged period of time in view to maximize the bioavailability and therapeutic efficacy of the drug.Bioadhesive tablets were prepared using metronidazole and sodium alginate in different proportions by wet granulation method. The prepared tablets were evaluated for weight variation, hardness, friability, dissolution and swelling studies.The release of drug from various vaginal bioadhesive tablets exhibited the following order F4>F1>F3, but F2 exhibited faster drug release compared to other formulations, which is not a desired characteristic for the treatment of vaginosis. By observing the above results, more ca +2 ions became available to bind with sodium alginate during the wet granulation stage of the preparation. As a result better and stronger gel was formed when high amount of calcium carbonate was used. As the concentration of ca +2 ions increases, stronger gel of calcium alginate is formed that delay the influx of the dissolution medium and efflux of the dissolved drug out the matrix. As a result drug is released in amore sustained manner.
Different Types of Gel Carriers as Metronidazole Delivery Systems to the Oral Mucosa
Polymers, 2020
Periodontal diseases are some of the most widespread oral afflictions, and they are labeled as chronic infections caused by the accumulation of bacteria in dental plaque that produces localized inflammation of the periodontium. The use of local drug delivery systems to treat periodontal diseases has received greater attention, because the active substance is targeted directly to the affected area, which minimizes its systemic side effects. Therefore, the purpose of the investigation was to develop and characterize different types of gel formulations—bigel, hydrogel and oleogel—as local delivery systems containing metronidazole (MET), which can be applied to the oral mucosa. The influence of the formulation type on the mechanical, rheological and mucoadhesive properties were examined. Moreover, in vitro release of metronidazole, its ex vivo permeation through buccal porcine mucosa and antimicrobial activity measured by the plate diffusion method were estimated. It was found that the ...
Formulation and Evaluation of Metronidazole Microspheres-Loaded Bioadhesive Vaginal Gel
Asian Journal of Pharmaceutical and Clinical Research, 2017
ABSTRACTObjectives: The objective of the present work is to develop and characterize metronidazole microsphere-loaded bioadhesive vaginal gel to ensurelonger residence time at the infection site, providing a favorable release profile for the drug.Methods: Microsphere was prepared by solvent evaporation method in various ratios of metronidazole to poly-ε-caprolactone (PCL). Physicochemicalevaluation of microspheres includes determination of solubility in simulated vaginal fluid, partition coefficient (n-octanol/citrate phosphatebuffer pH 4.5), particle size distribution, entrapment efficiency, X-ray diffraction, and surface morphology by scanning electron microscopy (SEM).Drug excipient compatibility was established by Fourier transform infrared and differential scanning calorimetry studies. Bioadhesive gel wasprepared using Carbopol 934P and HPMC K4M in various concentrations, and methyl paraben was used as a preservative. The pH was adjustedwith triethanolamine which resulted in a ...
2017
Quality of pharmaceutical products is very important because drugs must be marketed as safe and therapeutically active formulations whose performance is consistent and predictable. The evaluation of the physical characteristics of the pharmaceutical products can ensure their quality as well as bioavailability and impart optimum therapeutic activity. Metronidazole was chosen for this comparative study because this drug is widely used worldwide in the treatment of amoebiasis and other microbial diseases. Studies on metronidazole revealed that it is a recommended treatment during pregnancy for infections with bacterial vaginitis and Trichomonas vaginalis. The purpose of this study was to compare the quality of metronidazole tablets of some brands and to evaluate whether all brands obey the USP protocols. There are many different brands and different types of dosage forms of metronidazole under various trade names manufactured by different pharmaceutical companies available in the marke...
Iranian Journal of Pharmaceutical Sciences
Hydrogel-Based Metronidazole Bioadhesive Tablet (HMBT) was prepared as a novel vaginal delivery system to achieve Controlled release of drug from the tablet for vaginal candidiasis. The highly swollen hydrogel were prepared by dissolving chitosan in acetic acid solution containing drug, followed by neutralisation with sodium hydroxide and characterized by SEM, DSC and FT-IR and evaluated for % swelling. The drug loaded hydrogels were incorporated into tablet formulation by dry granulation method using bioadhesive polymers such as HPMC, sodium CMC and guar gum in different ratios. HMBT was tested for drug content, hardness, friability, weight variation, thickness, swelling studies, in vitro drug release, bioadhesive strength, in vivo studies and antifungal activity. The FT-IR and DSC spectra's revealed that there was no chemical interaction between drug and polymers used. SEM revealed that particles of hydrogels appeared small and irregular shaped with large numbers of pores. F3 formulation shows good in vitro release profile with highest bioadhesive strength. From the in vivo study in rabbit it was found that the HMBT hold the tablet for more than 12 hours inside the vaginal tube. It may be concluded from present study that HMBT can be used as a novel delivery system for local therapy of vaginal candidiasis which can controlled the release of drug for prolong period of time.
Formulation, development and optimization of metronidazolecompression coated tablets
2011
The aim of present work was to develop colon-specific drug delivery systems based on polysaccharide chitosan, were evaluated using in-vitro method. Metronidazole is choice of drug for intestinal amoebiasis. These drugs are to be delivered to the colon for their effective action against E. histolytica wherein the trophozoites reside in the lumen of the caecum and large intestine and adhere to the colonic mucus and epithelial layers. But the pharmacokinetic profile of metronidazole indicates that the drug is completely and promptly absorbed after oral administration reaching a concentration in plasma of about 10 mg/ml approximately 1 hr after a single 500 mg dose. The administration of this drug in conventional tablet dosage form provides minimal amount of metronidazole for local action in the colon, still resulting in the relief of amoebiasis, but with unwanted systemic effects.4,5The factors Amount of chitosan (X1), amount of carbopol 934P (X2) showed significant effect on the relea...