Browse > Article
http://dx.doi.org/10.4333/KPS.2010.40.S.103

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process  

Rhee, Yun-Seok (School of Pharmacy, Sungkyunkwan University)
Lee, Jae-Hwi (College of Pharmacy, Chung-Ang University)
Lee, Beom-Jin (Bioavailability Control Laboratory, College of Pharmacy, Kangwon National University)
Park, Eun-Seok (School of Pharmacy, Sungkyunkwan University)
Publication Information
Journal of Pharmaceutical Investigation / v.40, no.spc, 2010 , pp. 103-112 More about this Journal
Abstract
Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.
Keywords
Pellets; Multiparticulates; Modified- release; Pelletization; Solubilization;
Citations & Related Records
연도 인용수 순위
  • Reference
1 Trivedi, N.R., Rajan, M.G., Johnson, J.R., Shukla, A.J., 2007. Pharmaceutical approaches to preparing pelletized dosage forms using the extrusion-spheronization process. Crit. Rev. Ther. Drug Carrier Syst. 24, 1-40.   DOI   ScienceOn
2 Tuleu, C., Newton, M., Rose, J., Euler, D., Saklatvala, R., Clarke, A., Booth, S., 2004. Comparative bioavailability study in dogs of a self-emulsifying formulation of progesterone presented in a pellet and liquid form compared with an aqueous suspension of progesterone. J. Pharm. Sci. 93, 1495-1502.   DOI
3 Vergote, G.J., Kiekens, F., Vervaet, C., Remon, J.P., 2002. Wax beads as cushioning agents during the compression of coated diltiazem pellets. Eur. J. Pharm. Sci. 17, 145-151.   DOI
4 Wagner, K.G., Krumme, M., Schmidt, P.C., 2000. Pellet-containing tablets examination of distribution and deformation behaviour. STP Pharm. Sci. 10, 327-334.
5 Wang, L., Wang, J., Lin, X., Tang, X., 2010a. Preparation and in vitro evaluation of gliclazide sustained-release matrix pellets: formulation and storage stability. Drug Dev. Ind. Pharm. 36, 814-822.   DOI
6 Wang, Z., Sun, J., Wang, Y., Liu, X., Liu, Y., Fu, Q., Meng, P., He, Z., 2010b. Solid self-emulsifying nitrendipine pellets: preparation and in vitro/in vivo evaluation. Int. J. Pharm. 383, 1-6.   DOI   ScienceOn
7 Williams, R.O., 3rd, Liu, J., 2000. Influence of processing and curing conditions on beads coated with an aqueous dispersion of cellulose acetate phthalate. Eur. J. Pharm. Biopharm. 49, 243-252.   DOI
8 Pund, S., Joshi, A., Vasu, K., Nivsarkar, M., Shishoo, C., 2010. Multivariate optimization of formulation and process variables influencing physico-mechanical characteristics of site-specific release isoniazid pellets. Int. J. Pharm. 388, 64-72.   DOI
9 Rahman, M.A., Ahuja, A., Baboota, S., Bhavna, Bali, V., Saigal, N., Ali, J., 2009. Recent advances in pelletization technique for oral drug delivery: a review. Curr. Drug Deliv. 6, 122-129.   DOI
10 Sawicki, W., Lunio, R., 2005. Compressibility of floating pellets with verapamil hydrochloride coated with dispersion Kollicoat SR 30 D. Eur. J. Pharm. Biopharm. 60, 153-158.   DOI
11 Scala-Bertola, J., Gajdziok, J., Rabiskova, M., Bonneaux, F., Lecompte, T., Sapin, A., Maincent, P., 2009. Pellets for oral administration of low-molecular-weight heparin. Drug Dev. Ind. Pharm. 35, 1503-1510.   DOI
12 Serratoni, M., Newton, M., Booth, S., Clarke, A., 2007. Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system. Eur. J. Pharm. Biopharm. 65, 94-98.   DOI
13 Shavi, G.V., Nayak, U., Averineni, R.K., Arumugam, K., Meka, S.R., Nayanabhirama, U., Sureshwar, P., 2009. Multiparticulate drug delivery system of aceclofenac: development and in vitro studies. Drug Dev. Ind. Pharm. 35, 252-258.   DOI   ScienceOn
14 Siepmann, F., Muschert, S., Flament, M.P., Leterme, P., Gayot, A., Siepmann, J., 2006. Controlled drug release from Gelucirebased matrix pellets: experiment and theory. Int. J. Pharm. 317, 136-143.   DOI
15 Sinha, V.R., Agrawal, M.K., Agarwal, A., Singh, G., Ghai, D., 2009. Extrusion-spheronization: process variables and characterization. Crit. Rev. Ther. Drug Carrier Syst. 26, 275-331.   DOI   ScienceOn
16 Sungthongjeen, S., Paeratakul, O., Limmatvapirat, S., Puttipipatkhachorn, S., 2006. Preparation and in vitro evaluation of a multiple-unit floating drug delivery system based on gas formation technique. Int. J. Pharm. 324, 136-143.   DOI   ScienceOn
17 Mezreb, N., Charrueau, C., Boy, P., Allain, P., Chaumeil, J.C., 2004. Production of Carbopol 974P and Carbopol 971P pellets by extrusion-spheronization: optimization of the processing parameters and water content. Drug Dev. Ind. Pharm. 30, 481-490.   DOI
18 Mehta, K.A., Kislalioglu, M.S., Phuapradit, W., Malick, A.W., Shah, N.H., 2000. Effect of formulation and process variables on porosity parameters and release rates from a multi unit erosion matrix of a poorly soluble drug. J. Control. Release 63, 201-211.   DOI   ScienceOn
19 Mehta, K.A., Kislalioglu, M.S., Phuapradit, W., Malick, A.W., Shah, N.H., 2001. Release performance of a poorly soluble drug from a novel, Eudragit-based multi-unit erosion matrix. Int. J. Pharm. 213, 7-12.   DOI
20 Mehta, K.A., Kislalioglu, M.S., Phuapradit, W., Malick, A.W., Shah, N.H., 2002. Multi-unit controlled release systems of nifedipine and nifedipine:pluronic F-68 solid dispersions: characterization of release mechanisms. Drug Dev. Ind. Pharm. 28, 275-285.   DOI
21 Montousse, C., Pruvost, M., Rodriguez, F., Brossard, C., 1999. Extrusion-spheronization manufacture of Gelucire matrix beads. Drug Dev. Ind. Pharm. 25, 75-80.   DOI
22 Newton, M., Petersson, J., Podczeck, F., Clarke, A., Booth, S., 2001. The influence of formulation variables on the properties of pellets containing a self-emulsifying mixture. J. Pharm. Sci. 90, 987-995.   DOI
23 Panchagnula, R., Gupta, A., Kandavilli, S., Varma, M.V., 2006. High-throughput evaluation of non-swellable controlled release matrix tablets. Drug Dev. Ind. Pharm. 32, 669-675.   DOI
24 Pieszczek, B., Jachowicz, R., 2010. The effect of physico-chemical properties of the drug on the pharmaceutical availability of piroxicam from pellets. Pharm. Dev. Technol. 15, 241-248.   DOI
25 Kojima, M., Nakagami, H., 2002. Development of controlled release matrix pellets by annealing with micronized waterinsoluble or enteric polymers. J. Control. Release 82, 335-343.   DOI
26 Karrout, Y., Neut, C., Wils, D., Siepmann, F., Deremaux, L., Flament, M.P., Dubreuil, L., Desreumaux, P., Siepmann, J., 2009. Novel polymeric film coatings for colon targeting: Drug release from coated pellets. Eur. J. Pharm. Sci. 37, 427-433.   DOI
27 Kibria, G., Islam, K.M., Jalil, R.U., 2009. Stability study of ambroxol hydrochloride sustained release pellets coated with acrylic polymer. Pak. J. Pharm. Sci. 22, 36-43.
28 Kilor, V.A., Sapkal, N.P., Awari, J.G., Shewale, B.D., 2010. Development and characterization of enteric-coated immediaterelease pellets of aceclofenac by extrusion/spheronization technique using kappa-carrageenan as a pelletizing agent. AAPS PharmSciTech 11, 336-343.   DOI
29 Krogars, K., Heinamaki, J., Vesalahti, J., Marvola, M., Antikainen, O., Yliruusi, J., 2000. Extrusion-spheronization of pH-sensitive polymeric matrix pellets for possible colonic drug delivery. Int. J. Pharm. 199, 187-194.   DOI
30 Liu, Y., Schwartz, J.B., Schnaare, R.L., 2003. A multimechanistic drug release approach in a bead dosage form and in vitro predictions. Pharm. Dev. Technol. 8, 163-173.   DOI
31 Mallipeddi, R., Saripella, K.K., Neau, S.H., 2010. Use of coarse ethylcellulose and PEO in beads produced by extrusion-spheronization. Int. J. Pharm. 385, 53-65.   DOI
32 Mayo-Pedrosa, M., Alvarez-Lorenzo, C., Lacik, I., Martinez-Pacheco, R., Concheiro, A., 2007. Sustained release pellets based on poly(N-isopropyl acrylamide): matrix and in situ photopolymerization-coated systems. J. Pharm. Sci. 96, 93-105.   DOI
33 Ghosh, P.K., Murthy, R.S., 2006. Microemulsions: a potential drug delivery system. Current Drug Delivery 3, 167-180.   DOI
34 Fekete, R., Zelko, R., Marton, S., Racz, I., 1998. Effect of the formulation parameters on the characteristics of pellets. Drug Dev Ind Pharm 24, 1073-1076.   DOI
35 Freire, C., Podczeck, F., Veiga, F., Sousa, J., 2010. Influence of the coating formulation on enzymatic digestibility and drug release from 5-aminosalicylic acid pellets coated with mixtures of high-amylose starch and Surelease intended for colon-specific drug delivery. Drug Dev. Ind. Pharm. 36, 161-172.   DOI
36 Ghaffari, A., Avadi, M.R., Moghimi, H.R., Oskoui, M., Bayati, K., Rafiee-Tehrani, M., 2008. Mechanistic analysis of drug release from theophylline pellets coated by films containing pectin, chitosan and Eudragit RS. Drug Dev. Ind. Pharm. 34, 390-402.   DOI
37 Gursoy, R.N., Benita, S., 2004. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomedicine & Pharmacotherapy 58, 173-182.   DOI
38 Huang, Y.T., Tsai, T.R., Cheng, C.J., Cham, T.M., Lai, T.F., Chuo, W.H., 2007. Formulation design of a highly hygroscopic drug (pyridostigmine bromide) for its hygroscopic character improvement and investigation of in vitro/in vivo dissolution properties. Drug Dev. Ind. Pharm. 33, 403-416.   DOI
39 Iosio, T., Voinovich, D., Grassi, M., Pinto, J.F., Perissutti, B., Zacchigna, M., Quintavalle, U., Serdoz, F., 2008. Bi-layered selfemulsifying pellets prepared by co-extrusion and spheronization: influence of formulation variables and preliminary study on the in vivo absorption. Eur. J. Pharm. Biopharm. 69, 686-697.   DOI
40 Jachowicz, R., Nurnberg, E., Pieszczek, B., Kluczykowska, B., Maciejewska, A., 2000. Solid dispersion of ketoprofen in pellets. Int. J. Pharm. 206, 13-21.   DOI
41 Chiou, W.L., Riegelman, S., 1971. Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci. 60, 1281-1302.   DOI
42 Brachkova, M.I., Duarte, A., Pinto, J.F., 2009. Evaluation of the viability of Lactobacillus spp. after the production of different solid dosage forms. J. Pharm. Sci. 98, 3329-3339.   DOI
43 Bruce, L.D., Petereit, H.U., Beckert, T., McGinity, J.W., 2003. Properties of enteric coated sodium valproate pellets. Int. J. Pharm. 264, 85-96.   DOI
44 Chi, N., Guo, J.H., Zhang, Y., Zhang, W., Tang, X., 2010. An oral controlled release system for ambroxol hydrochloride containing a wax and a water insoluble polymer. Pharm. Dev. Technol. 15, 97-104.   DOI
45 Chivate, A.A., Poddar, S.S., 2008. Designing, optimisation & characterization of sustained release matrix pellets prepared by extrusion spheronization containing mixture of proteolytic enzymes. Curr. Drug Deliv. 5, 265-274.   DOI
46 Chuong, M.C., Christensen, J.M., Ayres, J.W., 2009. Sustained delivery of intact drug to the colon: mesalamine formulation and temporal gastrointestinal transit analysis. Pharm. Dev. Technol. 14, 116-125.
47 Dashevsky, A., Kolter, K., Bodmeier, R., 2004. Compression of pellets coated with various aqueous polymer dispersions. Int. J. Pharm. 279, 19-26.   DOI
48 Debunne, A., Vervaet, C., Remon, J.P., 2002. Development and in vitro evaluation of an enteric-coated multiparticulate drug delivery system for the administration of piroxicam to dogs. Eur. J. Pharm. Biopharm. 54, 343-348.   DOI
49 el-Mahdi, I.M., Deasy, P.B., 2000. Tableting of coated ketoprofen pellets. J. Microencapsul. 17, 133-144.   DOI
50 Elchidana, P.A., Deshpande, S.G., 1999. Microporous membrane drug delivery system for indomethacin. J. Control. Release 59, 279-285.   DOI
51 Abbaspour, M.R., Sadeghi, F., Afrasiabi Garekani, H., 2007. Thermal treating as a tool to produce plastic pellets based on Eudragit RS PO and RL PO aimed for tableting. Eur. J. Pharm. Biopharm. 67, 260-267.   DOI
52 Abdalla, A., Klein, S., Mader, K., 2008. A new self-emulsifying drug delivery system (SEDDS) for poorly soluble drugs: characterization, dissolution, in vitro digestion and incorporation into solid pellets. Eur. J. Pharm. Sci. 35, 457-464.   DOI
53 Abdalla, A., Mader, K., 2007. Preparation and characterization of a self-emulsifying pellet formulation. Eur. J. Pharm. Biopharm. 66, 220-226.   DOI
54 Awad, G.A.S., Charrueau, C.A.A., Allain, P., Chaumeil, J.C., 2002. Formulation and evaluation of bioadhesive pellets containing different carbomers made by extrusion-spheronization. STP Pharm. Sci. 12, 157-162.
55 Bendas, E.R., Ayres, J.W., 2008. Leaky enteric coating on ranitidine hydrochloride beads: dissolution and prediction of plasma data. Eur. J. Pharm. Biopharm. 69, 977-985.   DOI
56 Bendas, E.R., Christensen, J.M., Ayres, J.W., 2010. Development and in vitro evaluation of mesalamine delayed release pellets and tableted reservoir-type pellets. Drug Dev. Ind. Pharm. 36, 393-404.   DOI
57 Zeeshan, F., Peh, K.K., Tan, Y.T., 2009. Exploring the potential of a highly compressible microcrystalline cellulose as novel tabletting excipient in the compaction of extended-release coated pellets containing an extremely water-soluble model drug. AAPS PharmSciTech 10, 850-857.   DOI
58 Bodmeier, R., 1997. Tableting of coated pellets. Eur. J. Pharm. Biopharm. 43, 1-8.   DOI
59 Wiwattanapatapee, R., Pengnoo, A., Kanjanamaneesathian, M., Matchavanich, W., Nilratana, L., Jantharangsri, A., 2004. Floating pellets containing bacterial antagonist for control sheath blight of rice: formulations, viability and bacterial release studies. J. Control. Release 95, 455-462.   DOI
60 Zeeshan, F., Bukhari, N.I., 2010. Development and evaluation of a novel modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride as model drugs. AAPS PharmSciTech 11, 910-916.   DOI
61 Zhang, X., Tang, X., Yang, R., 2009. Development of a tamsulosin hydrochloride controlled-release capsule consisting of two different coated pellets. Drug Dev. Ind. Pharm. 35, 26-33.   DOI
62 Talegaonkar, S., Azeem, A., Ahmad, F.J., Khar, R.K., Pathan, S.A., Khan, Z.I., 2008. Microemulsions: a novel approach to enhanced drug delivery. Recent Patents on Drug Delivery & Formulation 2, 238-257.   DOI
63 Tian, L., Zhang, Y., Tang, X., 2008. Sustained-release pellets prepared by combination of wax matrices and double-layer coatings for extremely water-soluble drugs. Drug Dev. Ind. Pharm. 34, 569-576.   DOI