Rajalingam, B (2011) Screening of Physicochemical, Pharmacological, Microbiological Properties and Possible Pharmaceutical Applications of Some Selected Plant Constituents. Doctoral thesis, The Tamilnadu Dr.M.G.R. Medical University, Chennai.
Full text not available from this repository.Abstract
The present work entitled “Screening of physicochemical, pharmacological, microbiological properties and possible pharmaceutical applications of some selected plant constituents” was designed and carried out with a broad perspective to achieve the objectives. The objective of the study includes evaluation of the mucilage and resin and their potential as a pharmaceutical excipient. After thorough literature survey, the above plants were selected for study and the plant constituents of interest were separated and were used for developing different types of solid dosage forms. The development of immediate release tablets was to establish the binding and disintegrant effects of the separated plant constituents. The sustained release matrix tablets and pellets (spheroids) were developed to establish the rate controlling effect of the separated plant constituents. The plant constituents, a resinous matter from Ipomoea quamoclit Linn and mucilage from Aegle marmelos Correa, were obtained and purified. The plants and their sources were authenticated, Maximum yield of resin obtained was (5.93 % w/w) and the mucilage was (14.95 % w/w). The identification of the purified resin and mucilage were confirmed by chemical tests. The purity of resin and mucilage were determined by phytochemical tests. A finger print profile for identification of resin was also developed using HPTLC technique. Identification of sugars present in the separated mucilage was also performed using HPTLC technique and found that in the separated mucilage there was 5.85% w/w of sucrose, 6.56% w/w of glucose and 5.13% w/w of fructose. The resin and mucilage were characterized by various organoleptic and physicochemical properties such as colour, odour, shape, taste, touch, texture, surface characters, solubility, pH, swelling index, loss on drying, hygroscopicity, angle of repose, bulk and true densities, porosity, surface tension and different ash values. The microbial load and the presence of specific pathogens were determined and found to be very well within acceptable limits. The rheological studies of resin and mucilage showed that both resin and mucilage separated from the plants followed a nonnewtonian flow, especially pseudoplastic flow. Both resin and mucilage lost the viscosity after heating for different time intervals, but regained to the initial viscosity after 24 h when stored at 25C. Similarly, the pH of the solution did not affect the viscosity of resin and mucilage. The compatibility of resin and mucilage with the selected drugs, diclofenac sodium and paracetamol, were tested by using DSC, IR spectra and HPTLC technique and were found that there was no interactions. The separated plant components, resin and mucilage were selected as binders for developing tablet dosage form. The granules were prepared by wet granulation method using different concentrations of resin and mucilage with diclofenac sodium as model drug. To compare the binding efficacy of the separated plant components, formulations containing standard binders like PVP-K30, corn starch and methyl cellulose were used. The prepared granules were evaluated for percentage of fines, particle size and flow properties. As the concentration of resin /mucilage increased, the fines were decreased. The particle size and flow properties of granules were found to be satisfactory. Tablets were compressed from these granules and were evaluated for content uniformity, hardness, friability, disintegration time and dissolution profiles. All the batches of tablets exhibited good uniformity in content. The hardness, friability and disintegration time were increased with increase in percentage of resin used, but all these properties decreased with increase in percentage of mucilage. Based on physical characters, the tablets prepared with 4, 6, 8 and 10% w/w of resin and 6, 8, and 10% w/w of mucilage were found to be good. The drug release was found to decrease with increase in concentration of resin. In case of mucilage, the drug release was increased with increase in concentration of mucilage. The disintegrating property was evaluated using resin and mucilage as disintegrant. Paracetamol (as model drug) granules were prepared by wet granulation method using different concentrations of resin and mucilage powder as disintegrant (2.5, 5.0, 7.5 and 10% w/w) with other excipients and was compared with standard disintegrants such as sodium starch glycolate, cross carmellose and potato starch. The prepared granules were evaluated for percentage of fines, angle of repose, loose and tapped bulk densities, and compressibility. The results were found to be satisfactory. Tablets were prepared using these granules and were evaluated for content uniformity, hardness, friability, disintegration time and in vitro dissolution profiles. The content uniformity, hardness and friability were found to be comparable to standard disintegrants. The disintegration time was decreased with increase in concentration of mucilage. The drug release was found to increase with increase in concentration of mucilage. The release was found to be more than 90% within 30 min. The ideal batch of tablet was subjected to stability studies according to ICH guidelines and they were found to be stable. These results indicated that the mucilage acts as good disintegrant at 5% w/w concentration. The sustained release matrix tablets were formulated using different concentrations (10, 20 and 30% w/w) of resin by wet granulation technique. The physicochemical parameters of granules were satisfactory. The drug release was found to be sustained from the matrix tablets. An increase in the polymer ratio retarded the drug release to a greater extent. Among the various diluents used, microcrystalline cellulose was found to be an ideal diluent. The wet granulation technique was found to be ideal for formulation of sustained release matrix tablets using resin as the rate controlling polymer. The matrix tablets formulated with resins and mucilages were compared with tablets prepared with HPMC (30% w/w). HPMC tablets also were evaluated for physicochemical and in vitro drug release behavior. The drug release behavior was sustained for both HPMC and resin as evident by the T50 values. The drug release behavior of developed matrix tablets was similar to that of marketed formulation. The ideal batch of matrix tablets were subjected to stability studies according to ICH guidelines and they were found to be physically and chemically stable. Controlled release pellets are manufactured either to deliver the bioactive agents at specific site within gastrointestinal tract or to sustain the action of drugs over an extended period of time. As synthetic pelletizing agents have certain disadvantages such as high cost , toxicity, environmental pollution, non-renewable sources and more side effects, this project was taken up to explore the sustaining and pelletizing property of resin and mucilage, since natural components are preferred to synthetic materials due to their non toxicity, low cost and ease of availability. Spheroids of diclofenac sodium were prepared using resin and mucilage. The pelletization process was optimized for the selection of suitable diluent, proportion of diluent, spheronization speed and spheronization time. The prepared spheroids were characterized for particle size and size distribution, shape, surface characters, porosity, density, friability, and flow properties. The spheroids equivalent to 100 mg of diclofenac sodium was filled in capsules and in-vitro release profile of drug was studied. The spheroids were able to sustain the drug release. CONCLUSION: The present study “Screening of physicochemical, pharmacological, microbiological properties and possible pharmaceutical applications of some selected plant constituents”, may be concluded as the application of separated plant components i.e. resin from Ipomoea quamoclit and mucilage from Aegle marmelos can be used as a good pharmaceutical excipient, especially as a binding agent in the formulation of granules and tablets. As a disintegrating agent, for tablets and granules, the separated mucilage performs better than the resin and is comparable to the existing standard disintegrants used (sodium starch glycolate, cross carmellose and potato starch) in the study. As an agent for sustaining the drug release, separated resin was found to be better than the mucilage, as it did not perform well in sustaining the release but, only more or less equivalent to the standard polymer (HPMC) used in the study for comparison. The selected natural resin and mucilage are low cost alternatives to their synthetic counterparts which may be due to their versatile properties, biocompatible nature, physicochemical and microbiological stability. Hence, the selected resin and mucilage can be used as natural excipients for development of different dosage forms.
| Item Type: | Thesis (Doctoral) |
|---|---|
| Uncontrolled Keywords: | Screening, Physicochemical, Pharmacological, Microbiological Properties, Possible Pharmaceutical Applications, Some Selected Plant Constituents. |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Subramani R |
| Date Deposited: | 11 Jan 2022 02:12 |
| Last Modified: | 11 Jan 2022 02:12 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/13198 |
Actions (login required)
 |
View Item |
