Formulation of pharmaceutical products of Garcinia mangostana Linn. extracts

Abstract

Part I: The purpose of the investigation was to develop the extraction process that was simple, practical and giving high yield. The maceration of dried powder of Garcinia mangostana fruit husk with ethyl acetate gave yellow crystalline powder of mangostin. The yield was calculated as 7.47%. The identification of the Garcinia mangostanahusk extract was carried out by thin-layer chromatography (TLC) and differential scanning calorimetry. The TLC of mangostin was done by using the alumina sheet and ethyl acetate: hexane (3:1) as mobile phase. The Rf value as compared with standard mangostin was 0.60. The DSC thermogram showed the board melting range of the crude extract at 165.04-166.80 °C. The quantitative analyses of mangostin were developed using the high performance liquid chromatography (HPLC) and ultraviolet (UV) spectrophotometry. The HPLC system using methanol: water (87:13) as mobile phase, clotrimazole as internal standard and using UV detector at 243 nm. The UV spectrophotometric method was carried out using the UV spectrophotometer at 243 nm. The validation of both systems gave high specificity, linearity, accuracy and precision. The solubility study of mangostin showed the low water insolubility. The water solubility was improving with increasing ethanol content. The in vitro microbiological activity of mangostin to Staphylococcus aureus ATCC 25923 and Streptococcus mutans ATCC KPSK2 was studied. The minimum inhibitory concentrations of the extract were 3 µg/ml and 1.5 µg/ml, respectively. The minimum bactericidal concentrations of the extract was 4 µg/ml and 3 µg/ml, respectively. Part II: The purpose of this study was to develop fast dissolving oral strips containing Garcinia mangostana husk extract. The films consisted of low viscosity hydrophilic polymers such as hydroxypropyl methylcellulose and hydroxypropylcellulose, acesulfame potassium as sweetener, and menthol and eucalyptus oil as flavoring agents. The physical and mechanical properties and dissolution time of film bases were compared with commercial product strips A. From the dissolution time data, it was found that the film prepared from mixed polymer between HPMC 3 cps and HPC LV at ratios 2:1, 3:1, 4:1 and 5:1 were not significantly different from commercial product strips A (p>0.05). The films containing extract were light yellow and had porous surface based on observation from scanning electron microscopy. The dissolution profiles of all formulations showed the rapid release more than 80 percent of mangostin from films within 3-7 minutes and the fastest release was from formulation of HPMC 3 cps and HPC LV at ratio 5:1. Differential scanning calorimetry results exhibited that the Garcinia mangostana extract and additives were not in crystalline form in the films. The fast dissolving oral strips containing Garcinia mangostana husk extract showed in vitro antimicrobial activity against oro-dental bacteria, namely, Staphylococcus aureus aTCC 25923 and Streptococcus mutans ATCC KPSK2. Unter strese conditions at 40 degree Celcius and 75 percent relative humidity, the strips showed a good stability. The purpose of the study was to develop monoglyceride-based drug delivery systems containing Garcinia Mangostana extract. The system is based on the ability of mixtures of monoglyceride (dlyceryl monooleate) and triglycerides to form liquid crystals upon contact with water. The drug delivery systems can be administered by syringe and transformed into high-viscous liquid crystalline phases at the injection site. Ternary phase diagrams were constructed from various triglycerides: sesame oil, soybean oil and olive oil. In this study, monoglyceride-based drug delivery systems were prepared in the ratio of triglycerides: monoglyceride: water as 8: 62: 30 and 12: 58: 30. These systems could sustain release of Garcinia Mangostana husk extract over a period of 48 hr and followed squared root of time kinetics during the initial 24 hr of the release phase, indicating that the rate of release was diffusion-controlled. The system containing sesame oil showed the highest drug release. The increasing triglyceride content did not affect the release profiles. Differential scanning calorimetry results demonstrated that Garcinia Mangostana husk extract could be incorporated into drug delivery systems without causing phase transition. In the in vitro test, monoglyceride-based drug delivery systems containing Garcinia mangostana husk extract did not show the antimicrobial activity probably due to the high lipophilicity of the extract therefore it did not diffuse into the medium. Additionally, the drug delivery systems containing Garcinia mangostana husk extract showed good stability under the stress condition.