The Study and Application of Film Coated Pellets in the Prep aratio n of Pharmaceutic s

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1 , Vol. 32, No. 2,, 3 (, ) [ ],, [ ] ; ; ; [ ] R94419 [ ] A [ ] (2008) The Study and Application of Film Coated Pellets in the Prep aratio n of Pharmaceutic s J IANG Shao2ping, HAN Ke, WU Chuan2bin ( Lab of Pharmaceutics, School of Pharmacy, Sun Yat2Sen University, Guangzhou , China) [ Abstract] In this paper, the development and application of film coated pellets were reviewed. Pellets,as one of the multiple2unit drug delivery systems, are characteristic of their numerous advantages. By combining the technique of pellets manufacturing with film coating, the film coated pellets with the unique drug release properties have been developed and become the most popular direction in the field of sustained and controlled release preparations. [ Key words] Pellets ; Film coating ; Sustained release ; Controlled release ( multiple2unit drug delivery system),, [1,2 ], mm,,,, 1,, [ ] :, ; : ; Tel : ; E2mail

2 2008, Vol. 32, No ,, ph,,, [3 ] ( HPMC) ( PVP) ; ( EC) ; ( Eudragit ) (CAP),,,, [4 ] EC CAP (HPMCAS) [1,5 ],, ;,,, Wurster,, ;,,, ;,,, :, ; ;,,, EC HPMC Eudragit L Eudragit S100 Lecomte [6 ] EC Eudragit L,, ph,, EC Eudragit L 2,,,, 211,, [7 ] Badve [7 ] -, 7 12, 5

3 , Vol. 32, No. 2, ph,, - Sawicki [8 ], (MCC) PVP,, Kollicoat SR 30 D,,,,, Kollicoate,, Kollidone CL, 50 m, Avicel PH 102 Kollidone CL,, Sungthongjeen [9 ],, Eudragit RL 30D, 3, 24 ; ; 212,,, Dashevsky [10 ] Aqua2 coat ECD, 3 : EC,,,(AcDiSol), (L2HPC) ( Explotab),,, 26 %AcDiSol, 48 %AcDiSol, Aquacoat ECD EC,,,, 213, ph, ph, ph ;, ph, Akhgari [11 ] ph 3,,, Eudragit RS100 Eudragit S100 Eudragit L100, , 10 %, Siepmann [12 ] HPMCAS,, HPMCAS, :,

4 2008, Vol. 32, No ;,,,,,Basit [13 ],,,, ph (ph 5), ; EC, 2 2,, EC,, Huyghebaert [14 ] 210 ( IL210) Lactococcus lactis MCC,15 % Eudragit FS30D, Lactococcus lactis, 85 %, , 80 % IL molπl,2 2 %, 214,,, OΠW,, Serratoni [15 ] 80, MCC,, HPMC, EC,Abdalla [16 ], MCC Solutol HS 15 Cithrol GMS, Franceschinis [17 ] Cithrol GMO 80,, MCC,,, 215,,,, Mgschwitzer [18 ], ph Eudragit L 30255, 20,, Ho [19 ], EC Pluronic F268,, Pluronic F268 EC Kim [20 ],, 1

5 , Vol. 32, No. 2 80, PVP PEG6000 ; 2 Eudragit RS 30D Eudragit L 30D, Eudragit L 30 D ph > 5. 5, 3,,,,, [21 ] 6 MCC 4 1, 3 %HPMC,,, Eudragit L30D255 Eudragit L1002S100 GS2H(HPMC) 3, ph ph,,, Song [22 ] ph, 7, HPMC, Eudragit L30D255 Eudragit L1002Eudragit S100 (1 5), ph ph, 12 1 ph, [23 ], 3, MCC,,, 1 L2HPC, 2 EC, [24 ], Eudragit NE30D,,,, % [25 ],, Eudragit NE30D,,,,,12, 4,, 24,,, [ ] [1 ]. [J ].,2005,36 (2) : [2 ],,. [J ].,2001,16 (2) : [3 ],. [J ].,2004,31 (3) :

6 2008, Vol. 32, No [4 ]. [M]. :,2003 : [5 ],,. [J ]., 2004,15 (3) : [6 ] Lecomte F, Siepmann J, Walther M, et al. Blends of enteric and GIT2insoluble polymers used for film coating : physico2 chemical characterization and drug release patterns [ J ]. Controlled Release, 2003, 89 (3) : [7 ] Badve S S, Sher P, Korde A, et al. Development of hollowπ porous calcium pectinate beads for floating2pulsatile drug delivery[j ]. Eur J Pharm Biopharm, 2007,65 (1) : [8 ] Sawicki W, Lunio R. Compressibility of floating pellets with verapamil hydrochloride coated with dispersion Kollicoat SR 30 D[J ]. Eur J Pharm Biopharm, 2005, 60 (1) : [9 ] Sungthongjeen S, Paeratakul O, Limmatvapirat S, et al. Preparation and in vitro evaluation of a multiple2unit floating drug delivery system based on gas formation technique [J ]. Int J Pharm, 2006, 32 (2) : [10 ] Dashevsky A, Mohamad A. Development of pulsatile multi2 particulate drug delivery system coated with aqueous dispersion Aquacoat R ECD[J ]. Int J Pharm, 2006,318 (12 2) : [11 ] Akhgari A, Sadeghi F, Garekani H A. Combination of time2 dependent and ph2dependent polymethacrylates as a single coating formulation for colonic delivery of indomethacin pellets [J ]. Int J Pharm, 2006, 320 (122) : [12 ] Siepmann F, Siepmann J, Walther M, et al. Aqueous HPMCAS coatings : effects of formulation and processing parameters on drug release and mass transport mechanisms [J ]. Eur J Pharm Biopharm, 2006, 63 (3) : [13 ] Basit A W, Podczeck F, Newton J M, et al. The use of formulation technology to assess regional gastrointestinal drug absorption in humans[j ]. Eur J Pharm Sci, 2004, 21 (22 3) : [14 ] Huyghebaert N, Vermeire A, Rottiers P, et al. Development of an enteric2coated, layered multi2particulate formulation for ileal delivery of viable recombinant Lactococcus lactis [ J ]. J Eur J Pharm Biopharm, 2005, 61 (3) : [15 ] Serratoni M, Newton M, Booth S, et al. Controlled drug release from pellets containing water2insoluble drugs dissolved in a self2emulsifying system [J ]. Eur J Pharm Biopharm, 2007,65 (1) : [16 ] Abdalla A, Mgder K. Preparation and characterization of a self2emulsifying pellet formulation [ J ]. Eur J Pharm Bio2 pharm, 2007, 66 (2) : [17 ] Franceschinis E, Voinovich D, Grassi M, et al. Self2emulsi2 fying pellets prepared by wet granulation in high2shear mixer : influence of formulation variables and preliminary study on the in vitro absorption[j ]. Int J Pharm, 2005, 291 (122) : [18 ] Mgschwitzer J, M ller R H. Spray coated pellets as carrier system for mucoadhesive drug nanocrystals[j ]. Biopharm, 2006, 62 (3) : Eur J Pharm [19 ] Ho H O, Chen C N, Sheu M T. Influence of pluronic F268 on dissolution and bioavailability characteristics of multiple2 layer pellets of nifedipine for controlled release delivery[j ]. J Controlled Release, 2000, 68 (3) : [20 ] Kim T W, Sah H, Lee B J. Characterization of dual layered pellets for sustained release of poorly water2soluble drug[j ]. Chem Pharm Bull, 2007,55 (7) : [21 ],,. ph [J ].,2004, 35 (4) : [22 ] Song H, Guo T, Zhang R, et al. Preparation of the tradi2 tional Chinese medicine compound recipe heart2protecting musk ph2dependent gradient2release pellets [ J ]. Ind Pharm, 2002,28 (10) : Drug Dev [23 ],,,. [J ]., 2005,12 (425) : [24 ]. [D]. :,20031 [25 ]. [D]. :,20011

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