Dissertation > Excellent graduate degree dissertation topics show

Study on the Manufacture and Vitro Release of Oral Colon-specific Ketoprofen Pellets

Author: JinLei
Tutor: DingHong；LiangGuiXian
School: Shanxi Medical
Course: Pharmacy
Keywords: Colon targeted drug delivery Film test Ketoprofen Colon targeted release pellets In vitro release
CLC: R944.9
Type: Master's thesis
Year: 2010
Downloads: 150
Quote: 0
Read: Download Dissertation

Abstract

Project selection insoluble drugs ketoprofen as a model drug use of pectin with metal ions to form a gel and form a polyelectrolyte complex reaction with cationic polysaccharide preparation flora triggered colon targeted release pellets, to improve drug colonic targeting, to increase the local concentration of the colon of drugs and topical bioavailability, lower drug gastrointestinal adverse reactions, to improve patient compliance purposes. Established ketoprofen pellets Determination by high performance liquid chromatography and ultraviolet spectrophotometry pellets drug loading, encapsulation efficiency and release determination and precision, stability and recovery methodological study, the results of the various analytical methods are accurate and reliable, suitable for the analysis of samples of ketoprofen pellets in vitro. 2 chitosan, pectin, calcium and pectin as a membrane, were prepared using the electrostatic interaction between the poly-anion and a polycation to form a polyelectrolyte principle and pectin with calcium ions, the principle of formation of insoluble calcium pectinate kinds of free film (chitosan - free film of pectin, pectin calcium free film, chitosan - pectin calcium free film), by examining prescription and media environment free film, physical and chemical properties (Appearance, expansion, permeability, water vapor permeability) of a preliminary evaluation of the different composition of polysaccharide carrier material barrier function of drug release segment of the gastrointestinal tract and colon targeted release characteristics. The results show that: obtained free film deposition effects and good permeability the free chitosan - pectin calcium degree of swelling of the membrane permeability coefficient than chitosan - free film of pectin and pectin calcium-free film for small in the enzyme buffer, the examined the free membrane permeation coefficient are less plus enzyme medium CUHK. This film carrier material screening test for colon targeting provides a user-friendly way. 3 to calcium chloride as the crosslinking agent, the use of pectin and calcium ions may be the formation of insoluble calcium pectinate, pectin calcium colonic release pellets for preparation of ketoprofen, composed of pellets formability, drug prescription by examining The amount and encapsulation efficiency to optimize their prescription, and the determination of gastrointestinal pH environment by simulating the in vitro release of optimized prescription. The results show that the obtained pellets of good formability, 2h, less than 10% of the cumulative release in artificial gastric juice, and in artificial intestinal juice 4h the cumulative release is near 90%, improve its strength, the control in the small intestine The release of the segment is expected to reach the colon targeted drug delivery purposes. 4 In order to improve the strength of the pellets, to control its release in the small intestine segment, zinc acetate replace calcium chloride as the crosslinking agent, like calcium ion, zinc ion, with the pectin may also be the formation of insoluble pectin zinc gel can used to control the release of drugs in the colon before the preparation of ketoprofen release pellets of the pectin zinc colon formability of pellets composed by examining prescription drug loading and encapsulation efficiency, optimize their prescription, and simulated gastrointestinal pH environment optimized prescription vitro release test. The results show that the ketoprofen pectin zinc pellets formability superior to the calcium pectinate, 2h, less than 10% of the cumulative release in artificial gastric juice, 4h, over 80% of the cumulative release in artificial intestinal juice, but in artificial intestinal fluid two hours before the cumulative release is less than the pectin calcium pellets. The prepared pellets can be controlled to a certain extent the release of the drug in the upper end of the gastrointestinal tract, compared with calcium pectinate pellets, have significantly improved in the moldability of the pectin zinc pellets, I want to achieve colon-targeted drug delivery purposes its release in the small intestine segment control still needs further improvement. The colon targeting improve pellets introduction of this study chitosan, the use of polyelectrolyte reaction between chitosan and pectin, so that it jointly with the free carboxyl groups of pectin is crosslinked with zinc ions to form the strength a higher gel network structure to control drug release before it reaches the colon, the preparation of ketoprofen dose of chitosan - pectin zinc colon release pellets by examining prescription formability of pellets, containing and entrapment rate to optimize their prescription, and the determination of gastrointestinal pH environment by simulating the in vitro release of optimized prescription. And formed the basis of the pellets to the in vitro release indicators pellets in vitro release factors examined further. The results show that the ketoprofen chitosan - Pectin zinc pellets formability, chitosan introduction of effectively reducing the sensitivity of the pH of the pellets, increasing the strength of the pellets, the release of the pellets in the artificial intestinal juice has been effectively controlled, 8h cumulative release does not exceed 40%.

Study on the Manufacture and Vitro Release of Oral Colon-specific Ketoprofen Pellets

Abstract

Related Dissertations