Effervescent Method Research Articles

Design and evaluation of cost-effective oro-dispersible tablets of venlafaxine hydrochloride by effervescent method

Design and evaluation of cost-effective oro-dispersible tablets of venlafaxine hydrochloride by effervescent method

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLET OF PROCHLORPERAZINE MALEATE

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. Prochlorperazine Maleate, a potent antipsychotic medication with antiemetic properties, holds significance in treating various conditions such as nausea, vomiting, and vertigo. The decision to formulate it into orodispersible tablets aimed to address issues related to patient compliance and convenience, particularly for individuals who experience difficulty swallowing conventional tablets. Formulation F10, enriched with 10% Croscarmellose sodium as a superdisintegrant and an effervescent mixture for taste masking, exhibited remarkable characteristics. Croscarmellose sodium, chosen for its exceptional disintegration properties, ensures rapid breakdown upon contact with saliva, facilitating swift drug release and subsequent onset of action. Moreover, the incorporation of an effervescent mixture not only aids in masking the potentially unpleasant taste of Prochlorperazine Maleate but also holds the potential to enhance palatability and overall patient acceptance. Physicochemical characterization of Prochlorperazine Maleate unveiled favorable attributes, including a loss on drying of 0.413±0.002%, a melting point range of 234-236°C, and a moisture content of 0.0354%, affirming its suitability for formulation into orodispersible tablets. Through dissolution profile comparisons, formulation F10 demonstrated superior drug release kinetics compared to the commercial formulation, underscoring its potential therapeutic advantages.

A REVIEW ON ORODISPERSIBLE TABLET

The most common and preferred route of drug administration is through the oral route. Orodispersible tablets are gaining importance among novel oral drug-delivery system as they have improved patient compliance and have some additional advantages compared to other oral formulation. They are also solid unit dosage forms, which disintegrate in the mouth within a minute in the presence of saliva due to super disintegrants in the formulation. Thus this type of drug delivery helps a proper peroral administration in pediatric and geriatric population where swallowing is a matter of trouble. Various scientists have prepared orodispersible tablets by following various methods. However, the most common method of preparation is the compression method. Other special methods are molding, melt granulation, phase-transition process, sublimation, freeze-drying, spray-drying, and effervescent method. Since these tablets dissolve directly in the mouth, so, their taste is also an important factor. Various approaches have been taken in order to mask the bitter taste of the drug. A number of scientists have explored several drugs in this field. Like all other solid dosage forms, they are also evaluated in the field of hardness, friability, wetting time, moisture uptake, disintegration test, and dissolution test.

FORMULATION AND EVALUATION OF FENOVERINE FLOATING TABLETS

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile.
 Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations.
 Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism.
 Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.

Formulation and Taste Masking of Metronidazole Oral Disintegrating Tablets by a Novel Approach

The anti-protozoal drug, metronidazole, is developed as an oral disintegrating tablet (ODT) to treat amoebiasis and to bypass hepatic metabolism. The work aimed to prepare, taste-masking oral disintegrating tablets of metronidazole using different proportions of the drug and disintegrants in various ratios by an effervescent method. The ODT was developed by direct compression with various concentrations of super disintegrating agents (1-7%). In this technique, sodium bicarbonate and tartaric acid were used to generate effervescence. The formulated tablets were assessed for physicochemical characteristics. The results of FTIR spectroscopy indicated the stable character of metronidazole. In vitro studies revealed that batch F6 was having a 97.65% cumulative amount of drug release at 20th minute compared to other formulations. Due to the effervescent method, there was a significant increase in drug release, seen at the 1:1.5 ratio. Taste evaluation studies were conducted on healthy human volunteers.

Effect of directly compressible excipient and treated agar on drug release of clopidogrel oral disintegrating tablets.

In the present investigation, oral dissolving/dispersible/disintegrating tablets (ODTs) of clopidogrel were designed with a view to enhance the bioavailability and patient compliance by two different methods, namely, direct compression and effervescent methods using directly compressible excipient and treated agar (TAG). In the direct compression method, TAG was used as a disintegrant and another method used a mixture of sodium bicarbonate and tartaric acid along with TAG as disintegrants. Among the directly compressed tablets, treated agar formulation 3 and among the effervescent tablets, treated agar and effervescent formulation 4 was found to be promising. Treated agar formulation 3 prepared by direct compression method emerged as an overall best formulation based on the in vitro drug release characteristics.

Docetaxel-Loaded Lecithoid Nanoparticles with Enhanced Lung Targeting Efficiency and Reduced Systemic Toxicity: Developed by Solid Dispersion and Effervescent Techniques.

The application of chemotherapeutics with chemical drugs is always challenged by their high toxicities throughout the body in clinical trials. Here, we reported a smart formulation of docetaxel developed by solid dispersion and effervescent techniques for efficient and safe delivery of chemical drug to lung tissue. To achieve a high delivery to lung with reduced systemic toxicity, docetaxel was loaded into a kind of lecithoid nanoparticles (DTX-LN) which were prepared by a solid dispersion and effervescent method. After intravenous administration of DTX-LN to rabbit, the docetaxel level in lung was approximately 37-fold higher than that of docetaxel injection (DTX-INJ, a commercial injection preparation of DTX/polysorbate 80 micelles) group at 0.5 h and showed the highest tissue distribution among all the organs. Besides, the targeting parameter Re value of total increased amount of DTX in lung (AUC0-t) ratio (DTX-LN to DTX-INJ) is about 16.69, indicating a significantly enhanced lung targeting ability of DTX-LN. In subacute toxicity study, DTX-LN displayed a reduced hematotoxicity, especially for the negative impacts on white blood cells, lymphocyte and granulocyte when compared with DTX-INJ during both weekly and 3-weekly schedules administration. In addition, histopathological analysis demonstrated that DTX-LN showed less tissue damages on rabbit heart and kidney compared to DTX-INJ. Hence, this work would provide an insight for improving lung delivery efficacy of drugs with reduced systemic toxicity.

Formulation and Evaluation of Fast Dissolving Tablets of Doxazosin Mesylate

The objective of this research was to formulate fast dissolving tablets of Doxazosin mesylate that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Doxazosin mesylate is used for the treatment of the signs and symptoms of benign Prostatic Hyperplasia. Fast dissolving tablets of Doxazosin mesylate were prepared by direct compression method using superdisintegrant addition method, by using sublimation method and effervescent method. Thirty two formulations were prepared and evaluated for hardness, thickness, friability, weight variation, drug content, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio and in vitr o dissolution studies. FTIR and DSC studies revealed that there was no chemical interaction between the drug and the excipients. Formulation S8 was found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. The formulation S8 containing camphor (8%) as subliming agent was found to be the optimized combinations. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for formulation S8 for 60 days. The results of stability studies indicated no significant changes with respect to physicochemical properties, in vitro disintegration time, wetting time and in vitro drug release.

Formulation and in vitro comparative evaluation of orodispersible tablets of Pantoprazole

In the present work, an attempt has been made to formulate oral dispersible tablets of pantoprazole by three different methods. Conventional tabletting procedure was followed for the preparation of tablets. Nine batches of tablets were prepared and evaluated for general appearance and physical parameters, drug content, in vitro disintegration, in vitro dispersion, in vitro drug release, kinetic and stability studies. Formulations prepared by superdisintegrants addition method emerged as the best formulations, as they showed rapid in vitro disintegration time, in vitro dispersion time and drug release at the end of 5 min, apart from taste and excellent mouth feel compared to formulations prepared by sublimation and effervescent methods. It was concluded that oral dispersible tablets of pantoprazole can be successfully formulated and will be used as a novel drug dosage form for pediatrics and geriatrics with improved patient compliance.

Floating Drug Delivery Systems Using Metronidazole as a Model Drug Part I: By Effervescent Method

Gastric retentive dosage forms are highly useful for the delivery of many kinds of drugs.The use of floating dosage forms (FDFs) is one of the methods used to achieve prolonged gastric residence time (GRT). Formulation of Metronidazole (MDZ) as FDF provides an opportunity for both local and systemic drug action for eradication of Helicobacter pylori which is a gram-negative bacterium that is associated with gastric inflammation, peptic ulcer, and gastric cancer.This study was undertaken in order to formulate effervescent single-unit floating drug delivery system (FDDS) for MDZ.In the effervescent method, a carbon dioxide generating agent, e.g. sodium bicarbonate, was incorporated in hydrophilic polymer matrix together with MDZ.Different formulation parameters were studied and their effects on the floatation and in vitro drug release profiles were investigated.Polyvinyl pyrrolidone (PVP) provided rapid hydration of matrix, and this influence was decreased with time.Pectin was found to meet the requirements needed from a matrix for drug delivery applications including suitable mechanical properties to confine the gas, and to sustain MDZ release.The optimal amount of polymer and effervescent agent, lubricant agent concentration, and compression force were also demonstrated.The stability of the selected floating MDZ tablet formula (6) was also studied at different temperatures for three months and the calculated expiration date was found to be more than 4 years

FORMULATION AND EVALUATION ORAL DISPERSIBLE TABLET OF CINNARIZINE

Oral Dispersible tablets (ODTs) constitute an innovative dosage form, which overcomes the problem of swallowing and provides a quick onset of action. The aim of the proposed work is to formulate fast dissolving tablets of Cinnarizine for rapid dissolution of drug and absorption, which may produce rapid onset of action in the treatment of motion sickness. For this purpose the tablets of Cinnarizine were prepared by Effervescent method, Super disintegrants addition method and Sublimation method. Cinnarizine is an Antihistamines drug has been used for the treatment of motion sickness. Cinnarizine is poorly soluble in water making it a potent candidate fast-dissolving drug delivery system. Key word: ODT, Cinnarizine, Granules, Superdisintegrants,

Formulation Design and Optimization of Fast Dissolving Effervescent Tablets of Clonazepam

A B S T R A C T Fast dissolving tablets of clonazepam were prepared by effervescent method with a view to enhance patient compliance. A 3² full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and 1:1 mixture of sodium bicarbonate and anhydrous citric acid. Crospovidone (2-8% w/w) was used as superdisintegrant and mixture of sodium bicarbonate and anhydrous citric acid (16-48% w/w) as effervescent material, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 10 sec); the formulation containing 8% w/w crospovidone and 48% w/w effervescent material was found to be promising and tested for in vitro drug release pattern (in pH 6.8 phosphate buffer),accelerated stability (at 40oC/75% relative humidity for 6 months) and drug-excipient interaction (FT-IR analysis). Surface response plots are presented to graphically represent the effect of independent variables on the in vitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design check point formulations. The optimized tablet formulation was compared with conventional commercial tablet for drug release profiles. This formulation showed nearly nine-fold faster drug release (t 1.9 min) compared to the conventional commercial 50%

Formulation design and optimization of fast disintegrating lorazepam tablets by effervescent method

Fast disintegrating tablets of lorazepam were prepared by effervescent method with a view to enhance patient compliance. A 32 full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and mixture of sodium bicarbonate, citric acid and tartaric acid (effervescent material) on in vitro dispersion time. Crospovidone (2-8% w/w) was used as superdisintegrant and mixture of sodium bicarbonate, citric acid and tartaric acid (6-18% w/w) was used as effervescent material, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13 s); the formulation containing 8% w/w crospovidone and 18% w/w mixture of sodium bicarbonate, citric acid and tartaric acid was found to be promising and tested for in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables (concentrations of crospovidone and effervescent material) on the in vitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design check point formulations. The optimized tablet formulation was compared with conventional marketed tablet for drug release profiles. This formulation showed nearly eleven-fold faster drug release (t50% 2.8 min) compared to the conventional commercial tablet formulation (t50% >30 min). Short-term stability studies on the formulation indicated that there were no significant changes in drug content and in vitro dispersion time (P<0.05).

Orodispersible tablets: A new trend in drug delivery.

The most common and preferred route of drug administration is through the oral route. Orodispersible tablets are gaining importance among novel oral drug-delivery system as they have improved patient compliance and have some additional advantages compared to other oral formulation. They are also solid unit dosage forms, which disintegrate in the mouth within a minute in the presence of saliva due to super disintegrants in the formulation. Thus this type of drug delivery helps a proper peroral administration in pediatric and geriatric population where swallowing is a matter of trouble. Various scientists have prepared orodispersible tablets by following various methods. However, the most common method of preparation is the compression method. Other special methods are molding, melt granulation, phase-transition process, sublimation, freeze-drying, spray-drying, and effervescent method. Since these tablets dissolve directly in the mouth, so, their taste is also an important factor. Various approaches have been taken in order to mask the bitter taste of the drug. A number of scientists have explored several drugs in this field. Like all other solid dosage forms, they are also evaluated in the field of hardness, friability, wetting time, moisture uptake, disintegration test, and dissolution test.

Preparation and evaluation of orodispersible tablets of pheniramine maleate by effervescent method

In the present work, orodispersible tablets of pheniramine maleate were designed with a view to enhance patient compliance by effervescent method. In the effervescent method, mixture of sodium bicarbonate and tartaric acid (each of 12% w/w concentration) were used along with super disintegrants, i.e., pregelatinized starch, sodium starch glycolate, croscarmellose sodium and crospovidone. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 60 s), three formulations were tested for in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40±2°/75±5% RH for 3 mo) and drug-excipient interaction (IR spectroscopy). Among three promising formulations, formulation ECP4 containing 4% w/w crospovidone and mixture of sodium bicarbonate and tartaric acid (each of 12% w/w) emerged as the overall best formulation (t70% = 1.65 min) based on the in vitro drug release characteristics compared to commercial conventional tablet formulation. Short-term stability studies on the formulations indicated no significant changes in the drug content and in vitro dispersion time (P < 0.05).

Fast dissolving tablets of fexofenadine HCl by effervescent method

In the present work, fast dissolving tablets of fexofenadine HCl were prepared by effervescent method with a view to enhance patient compliance. Three super-disintegrants viz., crospovidone, croscarmellose sodium and sodium starch glycolate along with sodium bicarbonate and anhydrous citric acid in different ratios were used and directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on the in vitro dispersion time (approximately 20 s), three formulations were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability at 40°/75% RH for 3 mo and drug-excipient interaction (IR spectroscopy). Among the three promising formulations, the formulation ECP3 containing 8% w/w of crospovidone and mixture of 24% w/w sodium bicarbonate 18% w/w of anhydrous citric acid emerged as the best (t50% 4 min) based on the in vitro drug release characteristics compared to conventional commercial tablet formulation (t50% 15 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (P<0.05).

Design of fast disintegrating tablets of prochlorperazine maleate by effervescence method

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5 nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13-21 s), two promising formulations (one from each super-disintegrant) were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability (at 40°/75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t50% 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 17.4 min). Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

Supersonic Combustion of Kerosene/H2-Mixtures in a Model Scramjet Combustor

Liquid hydrocarbon supersonic combustion has been experimentally investigated. Kerosene was burnt in a steady. vitiated Mach 2.15 - air flow of a model scramjet combustor. The fuel is injected into the supersonic air stream by means of pylons. The effervescent atomisation method has been employed such that the liquid fuel is injected as a spray. By means of the Mie scattering technique the fuel jet structure was visualised and the evaporation rate estimated. The mechanisms of ignition and combustion of the kerosene/H2-mixture were studied and compared with the case of hydrogen combustion. Combustor ignition limits have been determined. Fuel-specific combustion phenomena are discussed. It was found that for the kerosene combustion a gas dynamic feedback mechanism strongly affects the supersonic combustion process.

Scanning electron microscopic examination of ultrasonic and effervescent methods of surface contaminant removal from complete dentures

Dentures were examined by scanning electron microscopy to evaluate removal of surface contaminants such as plaque, calculus, microflora, and cigarette smoke. Ten complete dentures were obtained during patient appointments and prepared for SEM examination. Samples from 10 control surfaces, 10 surfaces cleaned with effervescent cleansers, and 10 surfaces ultrasonically cleaned were photographed at ×5000. One photograph of each sample was evaluated in random order by five judges for a total of 150 observations. Photographs were compared with one of a clean denture sample. Statistical analysis of the results validated the superiority of the ultrasonic method for cleaning dentures.

Formulation Development of Verapamil Hydrochloride Tablet by Effervescent Method

Fast disintegrating tablets of Verapamil Hydrochloride were designed to achieve increased absorption as well as quick onset of pharmacological action of the active ingredient with a view to enhance patient compliance by effervescent method. Different combinations and ratios of sodium bicarbonate, anhydrous citric acid, sodium starch glycolate, Micro-crystalline cellulose (MCC) and lactose were used in order to get optimum result. The prepared formulations were evaluated for hardness, friability, thickness, diameter, taste of the solution to be administered and in-vitro dispersion time. The acceptable dispersion time was achieved by using a combination of citric acid and sodium bi carbonate in the same amount along with sodium starch glycolate, micro-crystalline cellulose (MCC) &amp; lactose. Acceptable taste of the solution to be administered was obtained with a combination of sucrose, aspartame and sodium saccharine. Key words: Effervescent method; Verapamil Hydrochloride; Dispersion time DOI: 10.3329/sjps.v3i1.6795S. J. Pharm. Sci. 3(1): 34-37