Effervescent Systems Research Articles

Fingerprinting of physical manufacturing properties of different acids for effervescent systems

The study aimed to fingerprint the physical manufacturing properties of five commonly used acid sources in effervescent systems for designing the formulation and process of such systems. The hygroscopicity, texture properties, rheological torque, compressibility, tabletability, etc., were investigated to inspect ‘powder direct compression (DC)’ and ‘wet granulation and compression’ properties of citric (CA), tartaric (TA), malic (MA), fumaric (FA), and adipic acid (AA). The DC ability was evaluated by the SeDeM expert system. The results indicated that all acid powders failed to meet flowability requirements for DC, and plastic deformation dominated during compression. Furthermore, CA exhibited strong hygroscopicity and punch sticking, while MA demonstrated the best tabletability. TA had a large wet granulation space and was relatively the most suitable for DC. AA was extremely hygroscopic, and its flowability improved significantly as particle size increased. Finally, FA displayed the lowest hygroscopicity and ejection force as well as great compressibility and wet granulation space, and did not exhibit punch sticking, while the granule fragments dissolved slowly during disintegration. Generally speaking, the formulation or granulation affected the tabletability, indicating that pairing with other acids or suitable fillers could potentially improve its disadvantages. These multidimensional assessments effectively reduce the pre-exploration and enhance the efficiency of the development of effervescent systems.

Design, Development and Physicochemical Evaluation of Effervescent Tablets of Antihistamine Drug

Purpose: Effervescent bilastine tablets were the focus of this investigation because of their ease of administration and the fact that some patients, especially younger ones or those with impaired swallowing abilities, have trouble ingesting oral dosage forms. Methods: Using the wet granulation process, 20 mg of effervescent bilastine tablets were produced. Pre-compression properties assessed for powder blend and granule combination. Here are some post-compression properties of the tablets that were examined: friability, hardness, drug content, pH, dissolution time, content uniformity, water content, X-ray, and Differential scanning calorimetry (DSC). We also measured carbon dioxide content and effervescence duration. To get the greatest results, we looked for effervescent systems that dissolved quickly in water and had the right properties before and after compression. Results: Based on their physicochemical properties, F2 formulations were determined to be best formulations, and the results demonstrated that the wet granulation process had greater flowability. Conclusion: Sweeteners such as mannitol, sodium saccharine, methylparaben, and citric acid were chosen for this investigation, along with sodium bicarbonate. If you want to hide the bitter flavor of bilastine, sodium saccharine is your best bet. From a physicochemical and physical property standpoint, the wet granulation process outshines the alternatives.

Novel approaches of gastro retentive drug delivery system

Oral route of drug administration is the most convenient route and accepted route of drug delivery. It is probable that at least 90% of all the drugs given by oral route. There are different drug deliveries to cure the diseases through oral route. Among them Gastroretentive drug delivery system plays an important and significant role in novel drug delivery systems. The floating systems, bioadhesive drug delivery system, expandable drug delivery system, high density systems, effervescent systems (Gas Generating systems), non-effervescent systems etc are various approaches. The wide applications can be achieved through this delivery system are enhanced bioavailability, sustained drug delivery, site-specific drug delivery, absorption enhancement, mitigating adversity at colon etc. In addition to specified above, the advantages and disadvantages, drugs and polymers used and the method of evaluation is also summarized in this review.

Novel Strategies and Model Studies for Colon Targeted Drug Delivery

: Targeting drugs with controlled release characteristics to the colon is gaining importance for localized action as well as to improve the systemic availability of peptides and proteins. : The present manuscript aims to describe the various approaches and model study for colon targeted drug delivery. : Drugs that have low absorption window are targeted into in the colonic regions using different novel technologies such as microparticulate system, prodrugs, pH and time dependent polymeric, effervescent and noneffervescent systems etc. Along with this it manuscript also describes the model study for colon targeting. : Colon targeted drug delivery system offers the potential therapeutic benefits to patients in terms of both local and systemic treatment. These drugs can be directly targeted in the colon which helps in the reducing systemic side effects.

Improvements in sticking, hygroscopicity, and compactibility of effervescent systems by fluid-bed coating.

Recently, effervescent tablets (ETs) have become increasingly popular with patients in clinics due to their fast disintegration by acid–alkali reactions in water. However, certain undesirable properties of ETs (e.g., sticking and high hygroscopicity) can limit their production and application. In particular, frequent sticking always severely decreases the tablet quality and productivity. Therefore, in this study, polyvinylpyrrolidone (PVP) at different usage levels, grades, or spray solution concentrations was coated onto the surfaces of both acidic and alkaline granules of ETs by means of the fluid-bed coating technique. In terms of fully characterized powder, tableting, and tablet properties, the following points were concluded: (i) a uniform coating of PVP onto the surfaces of these two granules not only resolved the sticking problem, but also effectively decreased the hygroscopicity and enhanced the compactibility; (ii) the improvements increased with an increase in the PVP content or PVP molecular weight and a decrease in the PVP spray solution concentration owing to the formation of an increasingly even and cohesive coating layer; (iii) the process of fluid-bed coating was not the simple superposition or simple mixing of two different materials' properties; (iv) the coating process did not cause significant influences on the disintegration time of ETs. Overall, it is fairly meaningful to further promote the development of ETs in practice since these problems have been overcome.

Formulation, characterization and physicochemical evaluation of ranitidine effervescent tablets.

The aim of this study was to design, formulate and physicochemically evaluate effervescent ranitidine hydrochloride (HCl) tablets since they are easily administered while the elderly and children sometimes have difficulties in swallowing oral dosage forms. Effervescent ranitidine HCl tablets were prepared in a dosage of 300 mg by fusion and direct compression methods. The powder blend and granule mixture were evaluated for various pre-compression characteristics, such as angle of repose, compressibility index, mean particle size and Hausner's ratio. The tablets were evaluated for post-compression features including weight variation, hardness, friability, drug content, dissolution time, carbon dioxide content, effervescence time, pH, content uniformity and water content. Effervescent systems with appropriate pre and post-compression qualities dissolved rapidly in water were selected as the best formulations. The results showed that the flowability of fusion method is more than that of direct compression and the F5 and F6 formulations of 300 mg tablets were selected as the best formulations because of their physicochemical characteristics. In this study, citric acid, sodium bicarbonate and sweeteners (including mannitol, sucrose and aspartame) were selected. Aspartame, mint and orange flavors were more effective for masking the bitter taste of ranitidine. The fusion method is the best alternative in terms of physicochemical and physical properties.

EFFERVESCENT ATOMIZATION FOR INDUSTRIAL ENERGY-TECHNOLOGY REVIEW

Effervescent atomization technology is a process employing the creation of a two-phase flow between a liquid fuel and an aerating gas. This technology is receiving renewed interest in the industrial energy field due to its applicability to alternative fuels. This paper presents a review of the principal governing parameters controlling the atomization characteristics of effervescent systems. Previous research in this field has developed a number of systematic parameters relating to the operation of effervescent atomizers but none are universally applicable, i.e., a thorough first-principles-based understanding of effervescent atomization has not yet been achieved. This paper reviews initial operating conditions (gas-to-liquid ratio, pressure drop), fluid properties (liquid viscosity, liquid surface tension, fuel type, atomizing gas molecular weight, non-Newtonian fluids), and geometric constraints (atomizer geometry, exit orifice geometry). There is considerable agreement among researchers with regard to most of these parameters. By contrast, geometric constraints have not been satisfactorily optimized. Recommendations based on experimental work do exist for most geometric constraints. These could, however, almost certainly be further optimized. Also included in this work is a thorough review of the experimental correlations required to develop effervescent atomization systems, including resultant spray characteristics, injector internal flow, and bubble energy.

Preparation and Evaluation of Fast-Disintegrating Effervescent Tablets of Glibenclamide

Fast-dissolving effervescent tablets (FETs) were prepared by the modification of nonreactive liquid-based wet granulation technique. Effervescent systems are not stable in the presence of trace amount of moisture, and elimination or inactivation of free water is the key to stability apart from manufacturing in controlled humidity environment. Our main objective of the project was to develop FETs of glibenclamide based on highly plastic granules that can be compressed at low pressure to form fast-melting pharmaceutical tablets. In this study, we have screened various acid and carbonate sources for the effervescent system. Citric acid was coated with plastic materials such as polyethylene glycol (PEG), which provide a physical barrier to the reaction. The inherent hygroscopic nature of PEG could decrease the affinity for moisture of effervescent mixtures and can provide a stabilizing effect. Sodium bicarbonate was blended with sugar alcohol like mannitol, which would give a protective coating. PEG 1000 melts at body temperature (∼37°C) and thereby does not delay the reaction between the acid source and base. The present formulation using citric acid–sodium bicarbonate and citric acid–sodium glycine carbonate tablet with PEG and mannitol was found to have better reaction properties and reaction stability than does the standard citric acid–sodium bicarbonate tablet. FETs of glibenclamide might aid in dissolution due to increase in microenvironmental pH around the granules and saliva. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness, and overall preference as best.

Sistemas farmacêuticos gastrorretentivos flutuantes

Gastro-retentive systems are often produced in order to modulate drugs release from pharmaceutical forms and in this way to increase drug residence time in the gastrointestinal tract. One of the most interesting strategies consists in the preparation of floating devices. These can be classified into two groups: effervescent systems and non-effervescent systems. A review of what has been done in the last years is presented in this article.

A Process to Produce Effervescent Tablets: Fluidized Bed Dryer Melt Granulation

The purpose of the present study was to apply melt granulation in a fluidized bed dryer (fluidized bed dryer melt granulation) to manufacture one-step effervescent granules composed of anhydrous citric acid and sodium bicarbonate to make tablets. This study permitted us to establish that such process parameters as concentrations of polyethylene glycol (PEG) 6000, residence times in the fluidized bed dryer, fineness of PEG6000, fineness of initial mixture effervescent systems, and efficiency of two lubricants markedly affect some granule and tablet characteristics. It is a dry process that is simple, rapid, effective, economical, reproducible, and particularly adapted to produce effervescent granules that are easily compressed into effervescent tablets.

Methods for the Determination of the Carbon Dioxide Evolved from Effervescent Systems

AbstractDifferent methods for determining the carbon dioxide evolved from effervescent systems are described. In addition, a comparison between some of them is carried out when a stoechiometric mixture of L-tartaric acid and sodium bicarbonate reacts.The methods compared are: gravimetric, volumetric and gasometric.The gravimetric methods can be direct or indirect. The direct ones are based on taking in the carbon dioxide by a sorbent substance. The increase of weight after the absorption represents the CO2 evolved. In the indirect gravimetric methods the amount of carbon dioxide is determined by substraction of the weight of the sample after and before the effervescent reaction.The volumetric methods are based on an acid-base titration. In the method used, the carbon dioxide released reacts with barium hydroxide. The excess of barium hydroxide is titrated with oxalic acid. It is possible to calculate then the carbon dioxide produced in the reaction from the volume of oxalic acid used.In the gasometric met...

Quantitative evaluation of pharmaceutical effervescent systems I: Design of testing apparatus

Two new devices were developed to monitor the reactivity of pharmaceutical effervescent systems. The first method monitored carbon dioxide pressure generation during the effervescent reaction in a plastic pressure vessel fitted with a pressure gauge. The second method monitored weight loss, attributed to carbon dioxide loss to the atmosphere, by means of a double cantilever beam and an electromagnetic proximity transducer. In the pressure device, the quantification of an effervescent reaction was accomplished by measuring the dissolution time of the effervescent system and the pressure generated. Quantification of an effervescent reaction using the beam device utilized the total carbon dioxide weight loss, the rate of weight loss, and the effervescent reaction lag time.

Quantitative Evaluation of Pharmaceutical Effervescent Systems II: Stability Monitoring by Reactivity and Porosity Measurements

The stability of selected effervescent tablet systems was monitored by means of mercury intrusion porosimetry and by a cantilever beam/proximity transducer balance. The porosity measurements proved to be useful in elucidating tablet pore structure changes over time. The measured parameter, percent pores greater than the experimental range, was a useful measure of porosity for statistical evaluations. The study showed that compression pressure and manufacturing conditions are not significant factors in the stability of an effervescent tablet system when nonhygroscopic materials are used.