Cyclodextrins are natural macrocyclic oligosaccharides able to form inclusion complexes with a wide variety of guests, affecting their physicochemical and pharmaceutical properties. The inclusion complexes were prepared by four different methods, namely, physical mixing, kneading, coprecipitation, and solvent. Powder xray diffraction patterns of e microwave method using beta cyclodextrin, f kneading method using alpha cyclodextrin, g kneading method using beta cyclodextrin. Enhancement of dissolution rate of naproxen by solid 11 fig.
Pdf preparation and characterization of etoricoxib. This is the most common and simple method used to prepare the inclusion complexes and it presents very low cost of production. They are used in food, pharmaceutical, drug delivery, and chemical industries, as well as agriculture and environmental engineering. Combine use of pvp k30 and hpb with doe approach was an. The inclusion complex formation of cyclodextrins by kneading method has been reported in the encapsulation of ibuprofen 8, omega3 fatty acids in thymol essential oil 9, thyme essential oil 9 and european anchovy engraulis encrasicolus l. Cyclodextrins are produced from starch by enzymatic conversion. Find patient medical information for cyclodextrin reagent on webmd including its uses, side effects and safety, interactions, pictures, warnings and user ratings. Solubility and dissolution enhancement of domperidone using 2hydroxypropyl. In laboratory scale kneading can be achieved by using a morter and pestle 14,15in large scale the kneading can be done by utilizing the extruders and other machines. A molecular dynamics study of conformations of beta. Each day, i learn more about the amazing benefits of cyclodextrins novel excipients of unexplored potential. For curcumincyclodextrin inclusion complex preparation, two most often used methods are freeze drying and common solvent evaporation.
The phase solubility analysis indicates the formation of 1. In kneading method, the drug and the carrier were dissolved in water. Cd were used for the preparation of inclusion complex by shaking method in aqueous. The dsc curve of silymarin shows one characteristic sharp endothermic peak at around 150c, indicating the melting point of the drug. Cyclodextrins are cyclic oligosaccharides consisting of six, seven or eight glucose molecules looking like a truncated cone or torus. The main advantage is that no water need be added, unless a washing step is used. Beta cyclodextrin is a cyclodextrin composed of seven alpha 14 linked dglucopyranose units. Three cyclodextrins were separated using asahipak nh2p50 4e, a polymerbased amino column. After grinding paste, solvent get evaporated and powder like complex is formed. On laboratory scale kneading can be achieved by using a mortar and pestle11. The effect of parameters such as kneading time and temperature on complexation was also studied.
The potential use of natural cyclodextrins and their synthetic derivatives have been studied extensively in pharmaceutical research and development to modify certain properties of hydrophobic drugs. The freeze dried phenytoin betacyclodextrin complex lacked flowability and compressibility. Improved oral bioavailability of anticancer drug tamoxifen. Jan 05, 2016 this paper describes a new and reliable method for cit enantioseparation by hplc, using sbe. Cetirizine dihydrochloride, betacyclodextrin inclusion.
Inclusion complex formation of cyclodextrin with its guest. There was an increase in the starch crystallinity in all complexed bgn starches figs. Encapsulation of clove essential oil in hydroxypropyl beta. Kneading method the required amounts of aripiprazole and cyclodextrin were accurately weighed, transferred to a mortar and triturated with small volume of ethanolwater 50.
The aim of this research was to formulate and develop an orally disintegrating tablet odt that incorporated a mel. The dried mass was pulverized and sieved through mesh no. Its disadvantages are the risk of caking on scaleup, resulting in mixing not being sufficiently thorough leading to incomplete complexation, and, with many guests. Millingcogrinding technique a solid binary inclusion compounds can be prepared by grinding and milling of the drug and cds with the help of mechanical devices. One way to achieve this is by the use of cyclodextrins, a wellknown group of molecules able to include waterinsoluble molecules. The reason for this lies in the ease of its production and subsequent low price more than 10,000 tons produced annually with an average bulk price of approximately 5 usd per kg. There are different methods to prepare cyclodextrin inclusion complexes. Pdf development and characterization of paracetamol. Subjects were randomly allocated to each preparation and crossed over after. Results from numerous investigations have demonstrated its safety and metabolism. Cyclodextrin alpha and beta were used as initiators for grafting catechin to the bgn starch molecule.
Paracetamol is a sparingly soluble bitter tasting drug. Sulfobutylether beta cyclodextrin was rationally designed to maximize safety and optimize interaction. Dissolution enhancement of clarithromycin using ternary. Hpbcd is used as a dissolution medium for polymer coated drug eluting coronary stent, bt my question is only about beta cyclodextrin. Cd and to study the effect of the preparation method on the in vitro dissolution profile in different media 0. The inclusion complexes were formed by physical mixing, kneading, coevaporation, and lyophilisation methods. The aims of this study were to enhance the solubility and dissolution rate of nimodipine nd by preparing the inclusion complexes of nd with sulfobutyletherbcyclodextrin sbe. Enhancement of dissolution rate of naproxen by solid. The effect of fly ash, betacyclodextrin and fly ashbeta.
Development of orodispersible tablets of candesartan. Black pepper oleoresin bpo is obtained by solvent extraction of black pepper piper nigrum l. They have been applied for delivery of a variety of drugs, including hydrocortisone, prostaglandin, nitroglycerin, itraconazol, chloramphenicol. A comparative analysis of more than 30 currently known cdcontaining pharmaceutical formulations shows that. Enantioseparation of citalopram by rphplc, using sulfobutyl. Caraway, cycloheptaamylose, cyclomaltoheptaose, schardinger. Multiple regression linear analysis was conducted to develop the kneading process and odt formulation. Pdf formulation and evaluation of cyclodextrin inclusion. Enhancement of norfloxacin solubility via inclusion. Seds is novel, single step method, which can produce solid drugcyclodextrin complexes. However, its physicochemical propertiesnamely water solubilityand, consequently, pharmacokinetics and pharmacodynamics could be object of improvement. The coprecipitation technique has previously applied for encapsulation of.
Then it was dried for 24 hours under room temprature. The thick slurry was kneaded for 45 min and then dried at 55 o c until dry. Mishra proceedings of the world congress on engineering and computer science 2016 vol ii wcecs 2016, october 1921, 2016, san francisco, usa isbn. Coprecipitation technique is useful for nonwatersoluble. These methods encompass coprecipitation, kneading, lyophilisation, spray drying, freeze drying and supercritical fluid technology norfloxacin is a fluoroquinolone antibacterial with properties similar to those of ciprofloxacin, but generally less potent in vitro. Dissolution profile of inclusion complex kneading method containing. The aim of this work was to compare the physicochemical characteristics of the solid complexes prepared by traditional methods kneading. Rosuvastatin calcium rst was gifted from astron research limited. We are working in the fields of pharmaceutical, cosmetic and food industry, agrochemical, environmental and analytical applications of cyclodextrins. The ability of these host molecules of including guest molecules within their cavities improves notably the physicochemical properties of poorly soluble drugs, such as albendazole, the first chosen. Alpha, beta, and gamma cyclodextrin are all generally recognized as safe by the u. Analysis of cyclodextrins nh2p50 4e shodex hplc columns.
The aim of this study was to investigate the use of inclusion complexation technique employing. The solid complexes prepared by physical mixtures, kneading methods, and. Acid and alkaline susceptible drugs can undergo degradation during this process is the limitation associated with this method. Dissolution enhancement of poorly soluble drugs by using. Standard solution a dissolve accurately weighed quantities of usp beta cyclodextrin rs and usp propylene glycol rs in water to make a solution having a known concentration of about 15 mg per ml for beta cyclodextrin, calculated on the anhydrous basis, and about 25 mg per ml for propylene glycol. Among all carvedilolcyclodextrin complexes, inclusion complex 1. Aripiprazolecyclodextrin binary systems for dissolution. The research work includes developing a multicomponent system comprising of macrolide. The solid complexes prepared by physical mixtures, kneading methods, and coprecipitation methods were characterized using differential scanning calorimetry and ftir. The slurry obtained was kneaded for 30 min and then dried under vacuum at room temperature in presence of calcium chloride as a dehydrating agent.
Often one would like to combine multiple ingredients. Separation of flavanone7oglycoside diastereomers and analysis in citrus juices by multidimensional liquid chromatography coupled with mass spectrometry. Apparent stability constant for silymarin k c was 722 k1 with. The influence of cyclodextrin and ph on the solubility of. The coprecipitation technique has previously applied for encapsulation of drugs such as oxaprozin 14. Beta cyclodextrin complexation and formulation as an antihiv microbicide by haitao yang b. Clove essential oil was encapsulated by the kneading method with hydroxypropyl beta. The effect of milling process on acyclovir inclution complex with beta cyclodextrin deni noviza, dedi afrianto, erizal and auzal halim department of pharmaceutics, faculty of pharmacy, andalas university, kampus unand limau manis. Phase solubility study and kneading method was employed to develop and formulate solid inclusion complexes. Cicchi, in comprehensive heterocyclic chemistry iii, 2008. Cd was optimized by evaluation of four processing methods autoclave, lyophilization, shaking, and kneading, incorporation of four watersoluble polymers hpmc.
Research studies in both humans and animals have shown that cyclodextrins and their derivatives can be used to improve the drug delivery system for almost any type of drug formulation from anticancer drugs to antiviral drugs. Cyclodextrins are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits joined by. Sulfobutylether beta cyclodextrin, also known as sbe beta cd, is a polyanionic beta cyclodextrin derivative with a sodium sulfonate salt separated from the lipophilic cavity by a butyl ether spacer group, or sulfobutylether sbe. Immobilized betacyclodextrin as a simple and recyclable method for cholesterol removal in milk. Alpha and betacyclodextrin inclusion complexes with 5. The complexation of a drug with cyclodextrins cds is a commonly used method to improve its solubility 3,4. Coprecipitation technique this method involves the coprecipitation of drug and cds in a complex. Molecules free fulltext alpha and betacyclodextrin. Investigations of polyethylene glycol mediated ternary. The content of curcumin in the inclusion complexes study each inclusion complex prepared from different.
The various methods that are used to prepare dcd complexes include. The optimization of processing conditions is essential in order to achieve the optimum complexation efficiency and to compare with drugcyclodextrin complexation methods described earlier in the literature e. Study of inclusion complex of bcyclodextrin and nitrobenzene ming chen, guowang diao, enren zhang college of chemistry and chemical engineering, yangzhou university, yangzhou 225002, peoples republic of china received 23 january 2005. An in vitro study showed that the solubility and dissolution rate of meclizine hcl were significantly improved by complexation with 2hydroxypropyl. Studies on the preparation, characterization, and solubility of 2hp. Preparation of inclusion complex used kneading method in 1. Investigation of various practical techniques to enhance. Bambara groundnut bgn starch extracted from bgn flour was modified through complexation methods using alpha and beta cyclodextrin. Tamoxifen tmx, a class ii antiestrogen drug consistent with the biopharmaceutical classification system, shows low plasma levels leading to therapeutic failure as a result of poor aqueous solubility. A molecular dynamics study of conformations of betacyclodextrin and its eight derivatives in four di. With a hydrophobic interior and hydrophilic exterior, cyclodextrins form complexes with hydrophobic compounds. Cd inclusion complex formation and to evaluate the effect of some parameters.
Paste of cyclodextrin is prepared with small amount of water to which the drug is added without a solvent or in a small amount of ethanol. Improved bioavailability from a spironolactone beta. Betacyclodextrin was gifted from ex laboratory, ap ankleshwar, gujarat, india. Bpo is a source of various biologically active compounds including alkaloids, terpenes, flavones, steroids, among others. In order to obtain an improvement of the bioavailability and solubility of 5fluorouracil, a pyrimidine analogue used as chemotherapeutic agent in the treatment of the colon, liver, and stomac cancers, the. Capsules containing 100 mg micronised spironolactone powder were compared with 100 mg spironolactone beta cyclodextrin complex in 8 healthy volunteers by a single dose, double blind, crossover pharmacokinetic study. These conditions lead to a short elution time with greater resolution compared to the separation using an sec column. Kneading technique is suitable for poorly watersoluble guests, because the guest is dissolved slowly during the formation of complex 6. The effect of milling process on acyclovir inclution. Oct 10, 2015 in this study, the anticancer effect and improved safety for hypesensitivity reactions of docetaxelhydroxypropyl betacyclodextrin complex dcxcd were investigated. Functional characteristics of bambara groundnut starch. Corticosteroids like ciclesonide are used to manage asthma.
Naproxen is a poorly soluble antiinflammatorydrug, the solubility of which canbe enhanced by complexation withbetacyclodextrin. Preliminary phase solubility experiments were conducted to determine drug. Cd complex, using a quality by design qbd approach to enhance solubility and drug release. The aim of this study was to investigate the influence of both cyclodextrin and ph on the overall solubility of ketoprofen. Cheirsilp b 2016 inclusion complex formation of cyclodextrin with its guest and their applications biol eng med, 2016 doi. Characterization of inclusion complexes prepared inclusion complexes were characterized by. The inclusion complexes were prepared by slurry evaporation and kneading method using different proportions of bcds and soluplus. The influence of betacyclodextrin on the solubility and dissolution rate. Cetirizine dihydrochloride has a very unpleasant bitter taste. In aqueous ecd, complexation increased solubility 53. Evaluation of some methods for preparing gliclazide. Hplc method was used to investigate the thermodynamic behavior of the uc781 complex.
A read is counted each time someone views a publication summary such as the title, abstract, and list of authors, clicks on a figure, or views or downloads the fulltext. Complexation with multifunctional excipients cyclodextrins cds is an effective technique to increase the bioavailability of low watersoluble drugs in oral. Cyclodextrin complexation and ph adjustments have been reported as useful tools to increase the solubility of drug. Generally, this method is performed at ambient temperature and is a variation on the paste method. Complexation methods used included the microwave, coevaporation and kneading methods. Cyclodextrin diacerein inclusion complexes nitin maski 1, arulkumaran 1, kundlik girhepunje 2, prashant ghode 1, surajkumar randive 1 and ranju pal2 1 dept. Drug content and yield of kneading process for the binary and ternary. Cyclolab cyclodextrin research and development ltd. Sulfobutylether betacyclodextrin sodium sbebetacd cas. The preparation of dcxcd was confirmed by using differential scanning calorimetry, xray powder diffraction analysis, and scanning electron microscope. Aiming at increasing abz solubility, complexation with beta cyclodextrin ecd using aqueous and acetic acid solutions as abz solubilizer was studied. The main purpose of the liposomal drug delivery is to combine the. The anticancer activity was tested in human lung cancer a549 cell. The inclusion complexloaded fast disintegrating tablet had good taste and good perception in the mouth.
Besides that, the inclusioncomplex reduces the incidence of gastrointestinal side effects of the drug. The relative bioavailability of spironolactone from a complex with beta cyclodextrin has been evaluated. To improve solubility and dissolution rate of zafirlukast via complexation with. The aim of this study was to investigate the physicochemical characteristics, release behavior, and antioxidant activity of clove essential oil. In 2010, yadav et al reported a novel ph shift method for curcumin. There are several methods to obtain cyclodextringuest complexes depending on the properties of the guest and the nature of the chosen cyclodextrin. Study of inclusion complex of cyclodextrin and nitrobenzene. The inclusion complexes were prepared by four different methods, namely, physical mixing, kneading, coprecipitation, and solvent evaporation. The inclusion complexes were prepared in the solid state by kneading method and characterized by fourier transforminfrared ftir spectroscopy and xray powder diffractometry. Cyclodextrins can reduce side effects of cancer drug. The effect of fly ash, betacyclodextrin and fly ashbetacyclodextrin composites on cement pastes viscosity and setting times bolanle d. Betacyclodextrin has been the most studied of the cyclodextrins.
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