Swellable and rigid matrices: Controlled release matrices with cellulose ethers

Pharmaceutical Dosage Forms: Tablets, Third Edition: Volume 2: Rational Design and Formulation

Volumn , Issue , 2008, Pages 433-468

  Colombo, Paolo ^a   Santi, Patrizia ^a   Siepmann, Jürgen ^b   Colombo, Gaia ^c   Sonvico, Fabio ^a   Rossi, Alessandra ^a   Strusi, Orazio Luca ^a  

^a UNIVERSITY OF PARMA   (Italy)

^b UNIV LILLE   (France)

^c UNIVERSITY OF FERRARA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 85056210611     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (108)

1. Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci 1961; 50(10):874–5.
2. Bettini R, Colombo P, Massimo G, et al. Swelling and drug release in hydrogel matrices: Polymer viscosity and matrix porosity effects. Eur J Pharm Sci 1994; 2(3):213–9.
3. Colombo P, Bettini R, Massimo G, et al. Drug diffusion front movement is important in drug release control from swellable matrix tablets. J Pharm Sci 1995; 84(8):991–7.
4. Colombo P, Bettini R Peppas NA. Observation of swelling process and diffusion front position during swelling in hydroxypropyl methyl cellulose (HPMC) matrices containing a soluble drug. J Control Release 1999; 61(1–2):83–91.
5. Colombo P, Bettini R, Catellani PL, et al. Drug volume fraction profile in the gel phase and drug release kinetics in hydroxypropylmethyl cellulose matrices containing a soluble drug. Eur J Pharm Sci 1999; 9(1):33–40.
6. Ju RT, Nixon PR Patel MV. Drug release from hydrophilic matrices. 1. New scaling laws for predicting polymer and drug release based on the polymer disentanglement concentration and the diffusion layer. J Pharm Sci 1995; 84(12):1455–63.
7. Conte U, Colombo P, Gazzaniga A, et al. Swelling-activated drug delivery systems. Biomaterials 1988; 9(6):489–93.
8. Bettini R, Cattellani PL, Santi P, et al. Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate. J Control Release 2001; 70(3): 383–91.
9. Klemm D, Heublein B, Fink HP, et al. Cellulose: fascinating biopolymer and sustainable raw material. Angew Chem Int Ed Engl 2005; 44(22):3358–93.
10. Salsa T, Veiga F, Pina ME. Oral controlled-release dosage forms. I. Cellulose ether polymers in hydrophilic matrices. Drug Dev Ind Pharm 1997; 23(9):929–38.
11. Kidane A, Bhatt PP. Recent advances in small molecules drug delivery. Curr Opin Chem Biol 2005; 9(4):347–51.
12. Davis SS. Formulation strategies for absorption windows. Drug Discov Today 2005; 10(4):249–57.
13. Li CL, Martini LG, Ford JL, et al. The use of hypromellose in oral drug delivery. J Pharm Pharmacol 2005; 57(5):533–46.
14. Nokhodchi A, Rubinstein MH. An overview of the effects of material and process variables on the compaction and compression properties of hydroxypropyl methylcellulose and ethylcellulose. STP Pharma Sci 2001; 11(3):195–202.
15. Rekhi GS, Nellore RV, Hussain AS, et al. Identification of critical formulation and processing variables for metoprolol tartrate extended-release (ER) matrix tablets. J Control Relese 1999; 59(3):327–42.
16. Colombo P, Bettini R, Santi P, et al. Swellable matrices for controlled drug delivery: gel-layer behaviour, mechnisms and optimal performance. Pharm Sci Technol Today 2000; 3(6):198–204.
17. Xu G, Sunada H. Influence of formulation change on drug release kinetics from hydroxypropylmethylcellulose matrix tablets. Chem Pharm Bull 1995; 43(3):483–7.
18. Miranda A, Millan M, Caraballo I. Study of the critical points of HPMC hydrophilic matrices for controlled drug delivery. Int J Pharm 2006; 311(1–2):75–81.
19. Zuelger S, Fassihi R, Lippold BC. Polymer particle erosion controlling drug release. II. Swelling investigations to clarify the release mechanism. Int J Pharm 2002; 247(1–2):23–37.
20. Sung KC, Nixon PR, Skoug JW, et al. Effect of formulation variables on drug and polymer release from HPMC-based matrix tablets. Int J Pharm 1996; 142(1):53–60.
21. McCrystal CB, Ford JL, Rajabi-Siahboomi AR. Water distribution studies within cellulose ethers using differential scanning calorimetry. 2. Effect of polymer substitution type and drug addition. J Pharm Sci 1999; 88(8):797–801.
22. Gustafsson C, Bonferoni MC, Caramella C, et al. Characterization of particle properties and compaction behavior of hydroxypropylmethylcellulose with different degrees of methoxy/hydroxypropyl substitution. Eur J Pharm Sci 1999; 9(2):171–84.
23. Nellore RV, Rekhi GS, Hussain AS, et al. Development of metoprolol tartrate extended release matrix tablet formulations for regulatory policy consideration. J Control Release 1998; 50(1–3):247–56.
24. Gao P, Skoug JW, Nixon PR, et al. Swelling of hydroxypropyl methylcellulose matrix tablets. 2. Mechanistic study of the influence of formulation variables on matrix performance and drug release. J Pharm Sci 1996; 85(7):732–40.
25. Nokhodchi A, Rubinstein MH, Ford JL. The effect of particle size and viscosity grade on the compaction properties of hydroxypropylmethylcellulose 2208. Int J Pharm 1995; 126(1–2):189–97.
26. Salsa T, Veiga F, Texeira-Dias JC, et al. Effect of polymer hydration on the kinetic release of drugs: a study of ibuprofen and ketoprofen in HPMC matrices. Drug Dev Ind Pharm 2003; 29(3):289–97.
27. Nokhodchi A, Ford JL, Rowe PH, et al. The effect of compression rate and force on the compaction properties of different viscosity grades of hydroxypropylmethylcellulose. Int J Pharm 1996; 129(1–2):21–31.
28. Nokhodchi A, Ford JL, Rowe PH, et al. The influence of moisture content on the consolidation properties of hydroxypropylmethylcellulose K4M (HPMC 2208). J Pharm Pharmacol 1996; 48(11):1116–21.
29. Mithchell K, Ford JL, Armstrong DJ, et al. The influence of the particle size of hydroxypropylmethylcellulose K15M on its hydration and performance in matrix tablets. Int J Pharm 1993; 100(1–3):175–9.
30. Campos-Alderte ME, Villafuerte-Robles L. Influence of viscosity grade and particle size of HPMC on metronidazole release from matrix tablets. Eur J Pharm Biopharm 1997; 43(2):173–8.
31. Heng PWS, Chan LW, Easterbrook MG, et al. Investigation of the influence of mean HPMC particle size and number of polymer particle on the release of aspirin from swellable hydrophylic matrix tablets. J Control Release 2001; 76(1–2):39–49.
32. Timmins P, Delargy AM, Minchom CM, et al. Influence of some process variables on product properties for a hydrophilic matrix controlled release tablet. Eur J Pharm Biopharm 1992; 38(3):113–8.
33. Kleinebudde P. Roll compaction/dry granulation: pharmaceutical applications. Eur J Pharm Biopharm 2004; 58(2):317–26.
34. Sheskey PJ, Dasbach TP. Evaluation of various polymers as dry binders in the preparation of an immediate-release tablet formulation by roller compaction. Pharm Technol Eur 1996; 8(2):44–50.
35. Sheskey PJ, Hendren J. The effects of roll compaction equipment variables, granulation technique and HPMC polymer level on a controlled-release matrix model drug formulation. Pharm Technol Eur 1999; 11(11):18–35.
36. Inghelbrecht S, Remon JP. Reducing dust and improving granule and tablet quality in the roller compaction process. Int J Pharm 1998; 171(2):195–206.
37. Liu C, Chen S, Kao Y, et al. Properties of hydroxypropylmethylcellulose granules produced by water spraying. Int J Pharm 1993; 100(1–3):241–8.
38. Huang Y, Khanvilkar KH, Moore A, et al. Effects of manufacturing process variables on in vitro dissolution characteristics of extended-release tablets formulated with hydroxypropyl methylcellulose. Drug Dev Ind Pharm 2003; 29(1):79–88.
39. Herder J, Adolfsson A, Larsson A. Initial studies of water granulation of eight grades of hypromellose (HPMC). Int J Pharm 2006; 313(1–2):57–65.
40. Shah NH, Railkar AS, Phuapradit W, et al. Effect of processing techniques in controlling the release rate and mechanical strength of hydroxypropyl methylcellulose based hydrogel matrix. Eur J Pharm Biopharm 1996; 42(3):183–7.
41. Cobby J, Mayersohn M, Walker GC. Influence of shape factors on kinetics of drug release from matrix tablets I: Theoretical. J Pharm Sci 1974; 63(5):725–37.
42. Ford JL, Rubinstein MH, Caul FM, et al. Importance of drug type, tablet shape and added diluents on drug release kinetics from hydroxypropylmethylcellulose matrix tablets. Int J Pharm 1987; 40(3):223–34.
43. Skoug JW, Borin MT, Fleishaker JC, et al. In vitro and in vivo evaluation of whole and half tablets of sustained-release adinazolam mesylate. Pharm Res 1991; 8(12):1482–8.
44. Reynolds TD, Mitchell SA, Balwinski KM. Investigation of the effect of tablet surface area/volume on drug release from hydroxypropylmethylcellulose controlled-release matrix tablets. Drug Dev Ind Pharm 2002; 28(4):457–66.
45. Siepmann J, Kranz H, Peppas NA, et al. Calculation of the required size and shape of hydroxypropyl methylcellulose matrices to achieve desireddrug release profiles. Int J Pharm 2000; 201(2):151–64.
46. Kim C. Compressed donut-shaped tablets with zero-order release kinetics. Pharm Res 1995; 12(7):1045–8.
47. Sangalli ME, Maroni A, Zema L, et al. A study on the release mechanism of drugs from hydrophilic partially coated perforated matrices. Farmaco 2003; 58(9):971–76.
48. Conte U, Maggi L, Colombo P, et al. Multi-layered hydrophilic matrices as constant release devices (Geomatrix™ system). J Control Release 1993; 26(1):39–47.
49. Conte U, Maggi L. Modulation of the dissolution profiles from Geomatrix multi-layer matrix tablets containing drugs of different solubility. Biomaterials 1996; 17(9):889–96.
50. Krogel I, Bodmeier R. Development of a multifunctional matrix drug delivery system surrounded by an impermeable cylinder. J Control Release 1999; 61(1–2):43–50.
51. Colombo P, Santi P R B, et al. New modules, new assemblage kits and new assemblies for the controlled release of substances. 2006, PCT/EP2006/011661.
52. Losi E, Bettini R, Santi P, et al. Assemblage of novel release modules for the development of adaptable drug delivery systems. J Control Release 2006; 111(1–2):212–8.
53. Follonier N, Doelker E, Cole ET. Various ways of modulating the release of diltiazem hydrochloride from hot-melt extruded sustained release pellets prepared using polymeric materials. J Control Release 1995; 36(3):243–50.
54. Repka MA, Gerding TG, Repka SL, et al. Influence of plastucuzers and drugs on the physical-mechanical properties of hydroxypropylcellulose films prepared by hot melt extrusion. Drug Dev Ind Pharm 1999; 25(5):625–33.
55. Agrawal AM, Neau SH, Bonate PL. Wet granulation fine particle ethylcellulose tablets: Effect of production variables and mathematical modeling of drug release. AAPS PharmSci 2003; 5(2):Article 13.
56. Henrist D, Remon JP. Influence of the process parameters on the characteristics of starch based hot stage extrudates. Int J Pharm 1999; 189(1):7–17.
57. Breitenbach J. Melt extrusion: from process to drug delivery technology. Eur J Pharm Biopharm 2002; 54(2):107–17.
58. Levina M, Rubinstein MH, Rajabi-Siahboomi AR. Principles and application of ultrasound in pharmaceutical powder compression. Pharm Res 2000; 17(3):257–65.
59. Caraballo I, Millan M, Fini A, et al. Percolation thresholds in ultrasound compacted tablets. J Control Release 2000; 69(3):345–55.
60. Rodriguez L, Cini M, Cavallari C, et al. Evaluation of theophylline tablets compacted by means of a novel ultrasound assisted apparatus. Int J Pharm 1998; 170(2):201–8.
61. Sancin P, Caputo O, Cavallari C, et al. Effects of ultrasound-assisted compaction on keto-profen/Eudragit® S100 mixtures. Eur J Pharm Sci 1999; 7(3):207–13.
62. Levina M, Rubinstein MH. The effect of ultrasonic vibration on the compaction characteristics of ibuprofen. Drug Dev Ind Pharm 2002; 28(5):495–514.
63. Motta G. Process for preparing controlled release pharmaceutical forms and the forms thus obtained. 1994.
64. Williams RO, Reynolds TD, Cabelka TD, et al. Investigation of excipient type and level on drug release from controlled release tablets containing HPMC. Pharm Dev Technol 2002; 7(2):181–93.
65. Samani SM, Montaseri H, Kazemi A. The effect of polymer blends on release profiles of diclofenac sodium from matrices. Eur J Pharm Biopharm 2003; 55(3):351–5.
66. Vueba ML, Batista de Carvalho LAE, Veiga F, et al. Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets. Eur J Pharm Biopharm 2004; 58(1):51–9.
67. Vueba ML, Batista de Carvalho LAE, Veiga F, et al. Role of cellulose ether polymers on ibuprofen release from matrix tablets. Drug Dev Ind Pharm 2005; 31(7):653–65.
68. Pina ME, Veiga F. The influence of diluent on the release of theophylline from hydorphilic matrix tablets. Drug Dev Ind Pharm 2000; 26(10):1125–8.
69. Pose-Vilarnovo B, Rodriguez-Tenreiro C, Rosa dos Santos JF, et al. Modulating drug release with cyclodextrins in hydroxypropyl methylcellulose gels and tablets. J Control Release 2004; 94(2–3):351–63.
70. Nerurkar J, Jun HW, Price JC, et al. Controlled-release matrix tablets of ibuprofen using cellulose ethers and carrageenans: effect of formulation factors on dissolution rates. Eur J Pharm Biopharm 2005; 61(1–2):56–68.
71. Madhusudan RY, Krishna VJ, Jayasagar G. Formulation and evaluation of diclofenac sodium using hydrophilic matrices. Drug Dev Ind Pharm 2001; 27(8):759–66.
72. Alderman D. A review of cellulose ethers in hydrophilic matrices. Int J Pharm Technol Prod Manuf 1984; 5:1–9.
73. Hardy IJ, Windberg-Baarup A, Neri C, et al. Modulation of drug release kinetics from hydroxypropyl methyl cellulose matrix tablets using polyvinyl pyrrolidone. Int J Pharm 2007; 337(1–2):246–53.
74. Karavas E, Georgarakis E, Bikiaris D. Application of PVP/HPMC miscible blends with enhanced mucoadhesive properties for adjusting drug release in predictable pulsatile chro-noterapeutics. Eur J Pharm Biopharm 2006; 64(1):115–26.
75. Cao QR, Choi Y, Cui J, et al. Formulation, release characteristics and bioavailability of novel monolithiv hydroxypropylmethylcellulose matrix tablets containing acetaminophen. J Control Release 2005; 108(2–3):351–61.
76. Feely LC, Davis SS. The influence of polymeric excipients on drug release from hydroxypropylmethylcellulose matrices. Int J Pharm 1988; 44(1–3):131–9.
77. Nokhodchi A, Norouzi-Sani S, Siahi-Shadbad M, et al. The effect of various surfactants on the release rate of propanolol hydrochloride from hydroxypropylmethylcellulose (HPMC)-Eudragit matrices. Eur J Pharm Biopharm 2002; 54(3):349–56.
78. Colombo P. Swelling-controlled release in hydrogel matrices for oral route. Adv Drug Deliv Rev 1993; 11(1–2):37–57.
79. Peppas NA. Hydrogels in Medicine and Pharmacy. 1st ed. Boca Raton: CRC Press, 1986.
80. Siepmann J, Peppas NA. Mathematical modeling of controlled drug delivery. Adv Drug Deliv Rev 2001; 48(2–3):137–8.
81. Siepmann J Peppas NA. Hydrophilic matrices for controlled drug delivery: an improved mathematical model to predict the resulting drug release kinetics the “sequential layer” model. Pharm Res 2000; 17(10):1290–8.
82. Noyes AA, Whitney WR. Über die Auflösungsgeschwindigkeit von festen Stoffen in ihren eigenen Lösungen. Z Phys Chem 1897; 23:689–92.
83. Crank J. The Mathematics of Diffusion. 2nd ed. Oxford: Clarendon Press, 1975.
84. Fujita H. Diffusion in polymer-diluent systems. Fortschr Hochpolym Forsch 1961; 3:1–47.
85. Ju RT, Nixon PR, Patel MV, et al. Drug release from hydrophilic matrices. 2. A mathematical model based on the polymer disentanglement concentration and the diffusion layer. J Pharm Sci 1995; 84(12):1464–77.
86. Narasimhan B, Peppas NA. Disentanglement and reptation during dissolution of rubbery polymers. J Polym Sci Part B: Polym Phys 1996; 34(5):947–61.
87. Narasimhan B, Peppas NA. On the importance of chain reptation in models of dissolution of glassy polymers. Macromolecules 1996; 29(9):3283–91.
88. Narasimhan B, Peppas NA. Molecular analysis of drug delivery systems controlled by dissolution of the polymer carrier. J Pharm Sci 1997; 86(3):297–304.
89. Siepmann J, Kranz H, Bodmeier R, et al. HPMC-matrices for controlled drug delivery: A new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res 1999; 16(11):1748–56.
90. Hsieh DST, Rhine WD, Langer R. Zero-order controlled-release polymer matrices for micro-and macro-molcules. J Pharm Sci 1983; 72(1):17–22.
91. Lee PI. Effect of non-uniform initial drug concentration distribution on the kinetics of drug release from glassy hydrogel matrices. Polymer 1984; 25(7):973–8.
92. Swan EA, Peppas NA. Drug release kinetics from hydrophobic porous monolithic devices. Proc Symp Control Release Bioact Mater 1981; 8:18–23.
93. Korsmeyer RW, Gurny R, Doelker R, et al. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983; 15(1):25–35.
94. Colombo P, Conte U, Caramella C, et al. Compressed mini-matrices for drug release control. J Control Release 1985; 1(4):283–9.
95. Colombo P, Gazzaniga A, Caramella C, et al. in vitro programmable zero-order release drug delivery system. Acta Pharm Technol 1987; 33(1):15–20.
96. Colombo P, Catellani PL, Peppas NA, et al. Swelling characteristics of hydrophilic matrices for controlled release. New dimensionless number to describe the swelling and release behavior. Int J Pharm 1992; 88(1–3):99–109.
97. Colombo P, Conte U, Gazzaniga A, et al. Drug release modulation by physical restrictions of matrix swelling. Int J Pharm 1990; 63(1):43–8.
98. Catellani PL, Colombo P, Peppas NA, et al. Partial permeselective coating adds an osmotic contribution to drug release from swellable amtrices. J Pharm Sci 1998; 87(6):726–31.
99. Maggi L, Bruni R, Conte U. High molecular weight polyethylene oxides (PEOs) as an alternative to HPMC in controlled release dosage forms. Int J Pharm 2000; 195(1–2): 229–38.
100. Frishman WH. A new extended-release formulation of diltiazem HCl for the treatment of mild-to-moderate hypertension. J Clin Pharmacol 1993; 33(7):612–22.
101. Bettini R, Acerbi D, Caponetti G, et al. Influence of layer position on in vitro and in vivo release of levodopa methyl ester and carbidopa from three-layer matrix tablets. Eur J Pharm Biopharm 2002; 53(2):227–32.
102. Moustafine RI, Kabanova TV, Kemenova VA, et al. Characteristics of interpolyelectrolyte complexes of Eudragit E100 with sodium alginate. Int J Pharm 2005; 294(1–2):113–20.
103. Orienti I, Cerchiara T, Luppi B, et al. Influence of different chitosan salts on the release of sodium diclofenac in colon specific delivery. Int J Pharm 2002; 238(1–2):51–9.
104. Bonferoni MC, Rossi S, Ferrari F, et al. On the employment of lambda carrageenan in a matrix system. III. Optimization of lamba carageenan-HPMC hydrophilic matrix. J Control Release 1998; 51(2–3):231–9.
105. Jimenez-Kairuz AF, Llabot JM, Allemandi DA, et al. Swellable drug-polyelectrolyte matrices (SDPM). Characterization and delivery properties. Int J Pharm 2005; 288(1):87–99.
106. Rowe RC, Sheskey PJ, Owen SC. Handbook of pharmaceutical excipients. 5th ed. London, Chicago: Pharmaceutical Press, 2006.
107. Siepmann J, Podual K, Sriwongjanya M, et al. A new model describing the swelling and drug release kinetics from hydroxypropyl methylcellulose tablets. J Pharm Sci 1999; 88(1): 65–72.
108. Siepmann J, Streubel A, Peppas NA. Understanding and predicting drug delivery from hydrophilic matrix tablets using the “sequential layer” model. Pharm Res 2002; 19(3): 306–14.