Modification & Characterization of Natural Polymer for Development of Dosage Forms (original) (raw)
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The aim of this work was the chemical modification of pectin by limited acetylation of their free hydroxyl groups to yield high ester pectin and to investigate its swelling and erosion behavior along with the effect on the release pattern of drugs. Propranolol as an antihypertensive drug was formulated as tablet using chemically modified pectin and pure pectin by using wet granulation method and its collision on drug release was studied. Physicochemical characterization of chemically modified pectin, the solubility, gelling or swelling factor was studied. Optimum concentrations of the modified pectin in such a system protect the tablet throughout the gastrointestinal tract. The pectin modified with acetylating agent was found to be promising to modify the release of drugs which are to be delivered throughout GIT. Drug dissolution studies were carried out in buffers of pH 1.2 and 6.8 and the system was designed based on the total GIT transit time concept. The matrix tablet of modified pectin show more release retardant action as compared to pure pectin. Modified dosage form subject to sintering technique it show fast disintegration and dissolution.
Chemical modification of pectins, characterization and evaluation for drug delivery
2008
The aim of this work was the chemical modification of pectins by limited acetylation of their free hydroxyl groups to yield high ester pectins and to investigate its swelling and erosion behavior along with the effect on the release pattern of drugs. Ibuprofen as a weakly acidic drug was formulated as tablets using chemically modified pectin and its impact on drug release was studied. Optimum concentrations of the modified pectin in such a system protect the tablet throughout the gastrointestinal tract (GIT) for 10-12 hrs. The pectin modified with acetylating agent was found to be promising to modify the release of drugs which are to be delivered throughout GIT. Drug dissolution studies were carried out in buffers of pH 1.2 and 6.8 and the system was designed based on the total GIT transit time concept. This article reviews physicochemical characterization of chemically modified pectins, correlation of the physicochemical characteristics with the drug release pattern of ibuprofen and the potential use of chemically modified pectin for modified release dosage forms.
Swelling and erosion of pectin matrix tablets and their impact on drug release behavior
European Journal of Pharmaceutics and Biopharmaceutics, 2007
The aim of this study was to investigate swelling and erosion behaviors of hydrophilic matrix tablets using pectin and their impact on drug release. The matrix tablets were prepared by direct compression using different types of pectin. Swelling and erosion studies of pectin matrix tablets were carried out in various media. The pectin matrix tablets formed a continuous gel layer while in contact with the aqueous medium undergoing a combination of swelling and erosion. The swelling action of pectin matrices was controlled by the rate of its hydration in the medium. Release studies showed that the swelling and erosion of matrices influenced the drug release. The extent of matrix swelling, erosion and diffusion of drug determined the kinetics as well as mechanism of drug release from pectin-based matrix tablets. The release data showed a good fit into the power law or the Korsmeyer-Peppas equation indicating the combined effect of diffusion and erosion mechanisms of drug release.
AAPS PharmSciTech, 2004
The aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T 50 ). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T 50 . When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.
Chandra Kumar Chanchal*, Dr. Ishab Kumar** Universe International Journal of Interdisciplinary Research, 2020
Physico-chemical characteristics of pectin and guar gum were found to be within the specified limits. The guar gum showed passable compressibility index, high % of swelling and passable angle of repose as compared to pectin. Swelling and erosion experiment were carried out with tablets containing different ratios of guar to pectin using USP 24 Type II apparatus. From the result it was observed that guar gum has greater swelling capacity and pectin has high erosion rate. In-vitro drug release from the formulation batch F 3 and F 4s was found to be most promising and show optimum release in a controlled manner for 10 h. The formulation batch F 4 shows the zero-order release. At the same polymer level (pectin and guar gum). The effect of different filler excipients were studied (batch F 3). It was observed that tablets prepared with lactose shows faster release and recompress decrease the drug release from diltiazem HCl matrix tablets. All the formulation batches tested for physical parameters like weight variation, hardness, friability and drug content, all were found to be within the I. P. limits. The in-vitro drug release data showed that the optimized formulation batch F 3 follows the Korsmeyer-peppas model, indicating that the possible mechanism of drug release was by non-Fickian diffusion. The optimized formulation batch F 4 follows the zero order release. The drug-excipient interaction studies were carried out by FTIR and DSC. No significant interaction of drug with polymer was observed. During stability studies, no significant variation (1 to 3%) in drug release was observed, indicating that formulation batch F 3 and F 4 were stable over the chosen condition for 2 months. The optimized formulation batch F 3 and F 4 showed better drug release profile with Dilzem SR (diltiazem HCL , Torrent) and Voveran SR (diclofenac sodium ,Novartis) respectively. This was concluded from the similarity factor (f 2), which was found to be 53.53 and 52.40 respectively.
OVERVIEW OF PECTIN AS AN EXCIPIENT AND ITS USE IN THE PHARMACEUTICAL DOSAGE FORM Review Article
International Journal of Applied Pharmaceutics, 2022
Pectin is a polysaccharide that is abundant in nature and has promising uses in the pharmaceutical field. Pectin is resistant to digestive enzymes but pectin gel can swell in aqueous media and small amounts of compounds can be released into the gastrointestinal tract. This problem can be solved by developing pectin composites obtained from the incorporation of pectin polymers with other polymers. This article discusses the interaction of pectin with other polymers in various drug delivery systems. The method used in review articles is to review nationally and internationally published scientific journals obtained from Google, Google Scholar, Pubmed and Science Direct. From several related studies, delivery systems that have been developed and reported in the form of films, hydrogels, particulate systems and tablets. Other polymers such as Alginatee, protein, chitosan, gelatin and starch are known to improve the properties of pectin so that pectin composites can be used as controlled drug delivery. Thus, the development of other drug delivery systems with pectin composites becomes an opportunity and challenge in the future.
Studies on pectin formulations for colonic drug delivery
Journal of Controlled Release, 1994
An investigation has been undertaken to assess, in vitro, the potential of several pectin formulations as colonic drug delivery systems. Experiments were conducted on the release of model compounds from matrix tablets under conditions pertaining to those in vivo. The monitoring of release gives a sensitive indication of the behaviour of the pectin under the different conditions. The type of pectin, the presence of calcium and the solubility of the calcium salt all influence release. Additionally, pectins with a low degree of methoxylation were more susceptible to enzymic breakdown. Calcium enhanced the enzymic activity. Rheological studies indicated that gel strength was a factor in determining release. These findings suggest that either a high methoxy pectin formulation or a low methoxy pectin with a carefully controlled amount of calcium should maximise colonic specificity by providing optimal protection of a drug during its transit to the colon and a high susceptibility to enzymic attack.
SELECTION OF PECTIN AS PHARMACEUTICAL EXCEPIENT ON THE BASIS OF RHEOLOGICAL BEHAVIOR
ijppsjournal.com
The aim of this study was to evaluate rheological properties of pectin solutions to determine the influence of polymer concentration, pH, preservatives and heating duration on viscosity, using Brookfield R/S Plus Rheometer. The results shows that dilute pectin solutions are showing Newtonian, but at a moderate concentration they exhibit the non‐Newtonian behavior, and the psudoplastic nature was found to increase with concentration. As the pH of the polymer solution lowered there was increase in viscosity of the system observed, this may be due do the carboxyl acid groups on the pectin chains are neutralize i.e. reduction in ionization, and leads to reduction in hydration of the carboxylic acid groups. As a result of reduced ionisation, the polysaccharide molecules do not repel each other over their entire length. The result shows that pectin solutions are stable at broad range of pH. It was observed that as the temperature or pH of the system increases there was decrease in viscosity.
Overview on Pectin and its Pharmaceutical uses
International journal of innovative research in engineering and management, 2022
Pectin, a spontaneously occurring carbohydrate, has grown in importance in previous decades. Because of its biodegradability, scientists and consumers are increasingly appreciating the advantages of natural pectin. The dimethyl ester of polygalacturonic acids is pectin. Dried fruits and apple pomace are commercially extracted under moderately acidic circumstances. On the grounds of the degree of esterification, pectins are classified into two main categories. The development of three-dimensional networks, or gels, is caused by the connection of pectin chains. Pectin was used in the pharmaceutical business, as well as health promotion and treatment, because of its gelling characteristics. Tablets, gel beads, and film-coated dosage forms have all been explored as possible carriers for drug administration to the gastrointestinal system. The essential chemistry and general characteristics of pectin, as well as its gel formation process and properties, will be discussed in this study. Pectin will be used as an example in the pharmaceutical industry.
Pectin as a Versatile Biodegradable Polymer
2019
An investigation has been undertaken to assess, in vitro, the potential of several pectin formulations as a versatile polymer in various drug delivery systems. Literature review was studied on the release of model compounds from various drug delivery systems under conditions pertaining to those in vivo. The monitoring of release gives a sensitive indication of the behavior of the pectin under the different conditions. The type of pectin, the presence of calcium and the solubility of the calcium salt all influence release. Additionally, pectins with a low degree of methoxylation were more susceptible to enzymatic breakdown. Calcium enhanced the enzymatic activity. Rheological studies indicate that gel strength was a factor in determining release. This suggested that either a high methoxy pectin formulation or a low methoxy pectin with a carefully controlled amount of calcium should maximize colonies specificity by providing optimal protection of a drug during its transit to the colon and a high susceptibility to enzymic attack. On the other hand, this may also enhance mucoadhesive contributing in favor of other oral dosage forms.