Pectin As a Natural Excipient in Tablet Formulations - Essay Example

? Pectin As a Natural Excipient in Tablet Formulations Pectin As a Natural Excipient in Tablet Formulations Background Aim of the study Pectin is arguably the most complex polysaccharide that is found in plant cell walls when talking in terms of structure and functions (Willats, Knox and Mikkelsen, 2006). This is because as an element of pectic substances, pectin can be identified to belong to a group of polysaccharides that are in both plant cell walls, and a number of mucilages can play multifunctional roles because they possess multi-diversifying properties (Rehman and Salariya, 2005). Using a typical plant cell wall as an example, pectin has both in-muro and out-of-muro properties that make it possible to control cell wall integrity and porosity and give plants protection against phytopathogens (Bhattacharjee and Timell, 2005). Moreover, apart from the fact that pectin has functional roles in plant morphology, growth and general development, it also has been found to be highly defensive for the plant cell wall as it acts as a gelling and stabilising polymer agent (Aspinall and Fanous, 1984). Indeed, the aim of the proposed project is directly related to the property of pectin that makes it act as a gelling and stabilising polymer in a number of food and specialty products (Vincken et al., 2003; Mohnen, 2008). It is the aim of the project to investigate how this property of pectin can make it act as a natural excipient in tablet formulations. Using dried mango fruit peels as sources of extracted pectin, the researcher seeks to investigate the binding property in such pectin and how it would aid in tablet formulation, by use of sodium salicylate as a drug model. On the whole, the research will be carried out in a manner that formulates four major different batches of tablets using different weights of pectins such as 10, 20 30 and 40 mg. The binding property of pectin that will be recorded in the sodium salicylate will then be compared to other models of binding agents, particularly starch. Eventually, testing of the binding property will be done with pectin as an experimental agent and starch as a control agent (Malviya, Srivastava, Bansal and Sharma, 2010). Background literature The research problem being identified is not the first of its kind in the field of pharmacological studies. There have been a number of researchers who have had similar projects related directly to the proposed study. Yapo (2011) focused on the different co-polymer blocks available in complex pectin. In the study, it was found that there are four main co-polymer blocks, which are: unsubstituted homogalacturonan (HGs), otherwise known as linear galacturonan, which has been found to come in two major forms, i.e. low methyl-esterified HG and high methyl-esterified HG (Steffe, 1996); rhamnogalacturonan-I (RG-I), which has been found to be branched and compositionally heterogeneous and having ?-D-GalpA, NS residues such as ?-L-Rhap, ?-L-Araf and ?-D-Galp (Willats et al. 2001); rhamnogalacturonan-II (RG-II), which happens to be the most widespread form of SGs in plant cell walls (Beldman et al., 2001); and xylogalacturonan XGA), which can be isolated using chemical processes that include mild alkaline hydrolysis (Matsunaga et al., 2004). Generally, the study by Yapo (2011) is relevant to this research because it will help in knowing the various size-exclusion chromatography (SEC) elution profiles of the co-polymers that exist in the cell walls of pectin (Le Goff et al., 2001; O’Donoghue and Somerfield, 2008). In the diagram below, there is an example of a pectin source, such as mango, manifested when deesterified through endo-PG-digested acid extraction. Source: Yapo (2011). In another related study, Fissore, Rojas, Gerschenson and Williams (2012) looked into the characterisation and functional properties of pectin. Their study is relevant to the proposed project in appreciating various ways in which the characteristics and properties of specific sources of pectin can lead to a successful role playing as a natural excipient in sodium salicylate (Tang, Yong and Woo, 2011). Fissore et al. (2012) actually found that pectin has rheological characterisation that varies from one source of pectin to another. For example in butternut pectin, there was found to be high DM, which meant that the gelling capacity of butternut pectin had to be assessed using sugar that is low at pH (Baker, 1997; Ovodova et al., 2006). For beetroot pectin, there was identified that DM is low, making it necessary to assess the beetroot pectin using calcium ions (Pellerin et al. 2006; Reuman, Salariya, Habib and Shah, 2004). As with mango, which is the focus of the proposed study, the nature of DM, whether is it high or low, would therefore determine the pectin systems that should be used in the pectin extraction process. Fissore et al. (2012), however, found that the common forms of variables that will be presented in the pectin system include 1% (w/w) pectin, 70°C temperature, and the additional dissolving agent, be it sugar or calcium ions. Due to differences in DM levels, when FTIR spectra recordings are done, there are different readings for butternut and beetroot pectin as showed in the diagram below. Source: Fissore et al. (2011) Going directly into the formulation of tablets and the role of pectin in doing this, Menon et al. (2011) conducted a study that focused on formulation and evaluation of ibuprofen tablets using orange peel pectin as a binding agent. As the proposed study focuses on another form of tablet, which is sodium salicylate, and a different form of pectin, which is mango, it is important to review their work to identify possible effects and outcomes (Seixas et al., 2011). Generally, Menon et al. (2011) found that microwave assisted extraction is one of the best techniques that make the extraction of pectin possible in a shorter time frame and by use of fewer solvents. Moreover, the microwave assisted extraction guarantees 740 mg of pectin, which is of refined quality, and a higher extraction rate (Mohamed and Hasan, 1995; Van der Vlugt-Bergmans et al., 2000). In the study of drug-excipient interaction, Menon et al. (2011) found that when FTIR spectroscopy is used, it will be revealed that there exists no interaction between the drug and the pectin derived from the plant source. This relationship is showed in the diagram below, where it will be noted that the interaction produced no significant shift in the principal peaks of ibuprofen. Source: Mennon et al. (2011). Outline Plan of Work Generally, the analysis of the project will be undertaken with consideration of two major data analysis methods, which are chromatography and statistical methods. Below is a brief description of processes that are going to be followed in the experimentation that seeks to use mango sourced pectin as a natural excipient in the formation of sodium salycilate. PROCESSES Extraction of pectin from mango Characterisation of pectin Tablet formulation Statistical analysis In-vitro drug release Factorial design Identification of degree of esterification First formulation using 10 mg of pectin Analysis of test friability Determination of wavelength Re. timing Measurement of galacturonic acid content Second formulation using 20 mg of pectin Testing of hardness Pre-analysis calibration curve construction pH identification Third formulation using 30 mg of pectin Measurement of drug content Fine tuning Fourth formulation of pectin Identification of weight variation Comparison with British pharmacopoeia standards References Aspinall, G. O. and Fanous, H. K., 1984. Structural investigations on the non-starchy polysaccharides of apples. Carbohydrate Polymers, 4, pp. 193–214. Baker R. A., 1997. Reassessment of some fruit and vegetable pectin levels. Journal of Food Science, 62(2), pp. 190–225. Beldman, G., Vincken, J.-P., Schols, H. A., Meeuwsen, P. J. 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D., 2006. Pectin: new insights into an old polymer are starting to gel. Trends in Food Science & Technology, 173, pp. 97–104. Yapo, B. M., 2011. Pectic substances: from simple pectic polysaccharides to complex pectins—a new hypothetical model. Carbohydrate Polymers, 86, 373–385. Read More