Yıl: 2016 Cilt: 13 Sayı: 1 Sayfa Aralığı: 91 - 102 Metin Dili: Türkçe İndeks Tarihi: 29-07-2022

Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery

Öz:
Bu çalışmanın amacı, kronofarmakoterapiye yönelik olarak ofloksasinin yüzen-pulsatil salımı için içi boş kalsiyum pektinat boncuklarını geliştirmekti. Yüzen pulsatil kavramı, ani salımı takiben ilaç şeklinin gastrik kalış süresinin artırılması için kullanıldı. Mukoza ile temas etmeden midede kalış süresini artırmak üzere tasarlanmış kontrollü salım sistemi, hız kontrollü ilaç salımı yaklaşımıyla yüzen ilaç salım sisteminin hazırlanmasıyla elde edildi. Yüzebilmesi için çeşitli yaklaşımların kısıtlamalarının üstesinden gelmek üzere, iyonotropik çapraz bağlama sırasındaki basit asit-baz reaksiyonuyla içi boş/poröz boncuklar hazırlandı. Yüzen boncuklar, beklendiği şekilde asidik ortamdaki şişme sırasında ilk gecikme süresini takiben fosfat tamponda hızlı pulse salım sağladı. Elde edilen yüzen boncuklar, poröz (%38 porozite), <1 dansite ile içi boş ve 16-22 saatlik Ft50% ye sahipti. Bu yaklaşım, hastalıkların kronofarmakoterapiyle tedavisi için yüzen-pulsatil ilaç şekillerinin kullanımını kontrollü salım yapan ilaç salım sistemleri olarak kullanım potansiyellerinden dolayı önerir.
Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık

Yüzen-Pulsatil İlaç Salımı İçin İçi Boş Kalsiyum Pektinat Boncuklarının Hazırlanması ve Değerlendirilmesi

Öz:
The purpose of this work was to develop hollow calcium pectinate beads for floating-pulsatile release of ofloxacin intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. A controlled release system designed to increase its residence time in the stomach without contact with the mucosa was achieved through the preparation of floating drug delivery system by rate controlled drug delivery approach. To overcome limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic crosslinking. The floating beads provided expected two-phase release pattern with initial lag time during floating in acidic medium followed by rapid pulse release in phosphate buffer. The floating beads obtained were porous (38% porosity), hollow with bulk density <1 and had Ft50% of 16-22 h. This approach suggested the use of floating pulsatile dosage forms due to their potential as controlled-release drug delivery systems for treatment with chronopharmacotherapy of diseases.
Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık
Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
  • Bussemer T, Otto I, Bodmeier R, Pulsatile drug- delivery systems, Crit Rev Ther Drug Carrier Syst 18 (5) 433-458, 2001.
  • Lemmer B, Circadian rhythms and drug delivery, J Control Release 16, 63-74 1991.
  • Kulkarni AR, Soppimath KS, Aminabhavi TM, Rudzinski, WE, In vitro release kinetics of cefadroxil, loaded sodium alginate interpenetrating network beads, Eur J Pharm Biopharm 51, 127-133, 2001.
  • Soppimth KS, Kulkarni AR, Aminabhavi TM, Controlled release of antihypertensive drug from the interpenetrating network poly (vinyl) alcohol, guar gum hydrogel microspheres, J Biomater Sci Polym Ed. 11, 27-43, 2000.
  • Hwagno J, Skinner GW, Harcu WW, Barnum PE, Pharmaceutical application of naturally occurring water soluble polymer, Pharm Sci Technol Today 1, 254-261, 1998.
  • Aydin Z, Akbuga J, Preparation and evaluation of pectin beads, Int J Pharm 137, 133-136, 1996.
  • Kedziereuciz K, Lemory C, Effect of the formulation on the in vitro release of propranolol from gellan beads, Int J Pharm 178, 129-136, 1999.
  • Whithead L, Collete JH, Fell JT, Amoxicillin release from a floating dosage form based on alginates, Int J Pharm 2, 45-49, 2000.
  • Iannuccelli V, Coppi G, Bernber MT, Cameroni R, Air compartment multiple unit system for prolonged gastric residence. Part I, Formulation study, Int J Pharm 174, 47-54, 1998.
  • Sriamornsak P, Thirawong N, Putkhachorn S, Morphology and buoyancy of oil entrapped calcium pectinate gel beads, AAPS J 6 (3) article 24, 2004.
  • Murata Y, Sasaki N, Miyamoto E, Kawashima S, Use of floating alginate gel beads for stomach specific drug delivery, Eur J Pharm Biopharm 50, 221-226, 2000.
  • Bussmer T, Dashevsky A, Bodmeier R, A pulsatile drug delivery system based on rupturable coated hard gelatin capsule, J Control Release 93, 331-339, 2003.
  • Bulgarelli E, Forni, F, Bernaber MT, Effect of matrix composition and process condition on casein gelatin beads floating properties, Int J Pharm 198, 279-292 2002.
  • Stockwell,AF, Davis SS, In vitro evaluation of alginate gel system as sustained release drug delivery systems, J Control Release 3, 167-175, 1986.
  • Fatmanur TD et al. Evaluation of alginate based mesalazine tabletsfor intestinal drug delivery, Eur J Pharm Biopharm 67, 491-497, 2007.
  • Sungthongjeen S, Sriamornsak P, Puttipipatkhachorn S, Design and evaluation of floating multi-layer coated tabletsbased on gas formation,European J Pharm Biopharm 69, 255- 263,2008.
  • Choi BV, Park JB, Hwang SJ, Preparation of alginate beads for floating drug delivery system: effects of CO2 gas forming agent, Int J Pharm 239, 81-92, 2002.
  • Talukder R, Fassihi R, Gastroretentive delivery systems: hollowbeads, Drug Dev Ind Pharm 30, 4, 405-412, 2004.
  • Sriamornsak P, Thirawong N, Puttipipatkhachorn S, Emulsion gel beads of calcium pectinate capable of floating on the gastric fluid: effect of some additives, hardening agent or coating on release behavior of metronidazole, Eur J Pharm Sci, 24, 363-373, 2005.
  • Smolensky MH, Chronobiology and chronotherapeutics, applications to cardiovascular medicine, Am J Hypertens 9 (4 Pt 3) 11S-21S, 1996.
  • Lemmer B, Circadian rhythms and drug delivery, J Control Release 16, 63-74, 1991.
  • Rubinstein A, Approaches and opportunities in colon-specific drugdelivery, Crit Rev Ther Drug Carrier Syst 12, 101-149, 1995.
  • Mustofa M, Suryawati S, Dwiprahasto I, Santoso B, The relative bioavailability of diclofenac with respect to time of administration, Br J Clin Pharmacol 32, 246-247, 1991.
  • Gonza´lez-Rodr´y´guez ML, Holgado MA, C Sa´nchez-Lafuente, Rabasco AM, Fini A, Alginate/chitosan particulate systems forsodium diclofenac release, Int J Pharm 232, 225-234, 2002.
  • Ferna´ndez-Herva´s MJ, Holgadoa MA, Fini A, Fell JT, In vitro evaluation of alginate beads of a diclofenac salt, Int J Pharm 163, 23-34, 1998.
  • El-Gibaly I, Development and in vitro evaluation of novel floating chitosan microcapsules for oral use: comparison with non-floating chitosan microspheres, Int J Pharm 249, 7-21, 2002.
  • Srimornsak P, Prakongpan S, Puttipipatkhachorn S, Calcium pectinate gel coated pellets as an alternative carrier to calcium pectinate beads, Int J Pharm 156, 189-194, 1997.
  • Sriamornsak P, Nunthanid J, Calcium pectinate gel beads for controlled release drug delivery: I. Preparation and in vitro release studies, Int J Pharm 160, 207-212, 1998.
  • Wong TW, Lee HY, Chan LW, Heng PWS, Drug release properties of pectinate microspheres prepared by emulsification method, Int J Pharm 242, 233-237, 2002.
  • Pillay V, Fassihi R, In vitro release modulation from crosslinked pellets for site-specific drug delivery to the gastrointestinal tract I. Comparison of pH responsive drug release and associated kinetics, J Control Release 59, 229- 242, 1999.
  • Sharma GS, Srikanth MV, Uhumwangho MU, Phani Kumar KS, Ramana Murthy KV, Recent trends in pulsatile drug delivery systems - A review, Int J Drug Del 2, 200-212, 2010.
  • Godge GR, Misal AV, Pawar PY, Formulation and evaluation of mouth dissolving tablet with taste masking resin, Int J Life Sci Rev (IJLSR) 1(7), 253-263, 2015.
  • Godge G, Labade S, Misal A, Oral bioavailability improvement using solid dispersion techniques: A review, Int J Life Sci Rev, (IJLSR) 1 (7), 243- 252, 2015.
  • Hiremath S, Godge G, Sonawale B, Shirsath R, Pharmaceutical advances in cyclodextrin inclusion complexes for improved bioavailability of poorly-soluble drugs, Int J Pharm Sci Nanotechnol, Volume 8 Issue 3 July- September, 2894-2905, 2015.
  • Godge GR, Labade SP, Preparation of solid dispersion of poorly water soluble drug formulation and consideration, Int J Pharm Sci Res (IJPSR), 6 (5) May, 897-903, 2015.
  • Godge GR, Hiremath SN, An investigation into the characteristics of natural polysaccharide: polymer metoprolol succinate tablets for colonic drug delivery, Mahidol University J Pharm Sci 41 (2), 7-21, 2014.
  • Godge GR, Hiremath SN, Colon targeted drug delivery system: A Review, Int J Pharm Drug Anal. [ISSN: 2348 - 8948 ], 2 (1), 35- 48, 2014.
  • Godge GR, Hiremath SN, Development and evaluation of colon targeted drug delivery system by using natural polysaccharides/polymers. Dhaka Univ J Pharm Sci, 13(1), 105-113, 2014.
  • Hiremath S, Godge G, Preparation and in vitro evaluation of inclusion complexes of nelfinavir with chemically modified ?-cyclodextrins, Dhaka Univ J Pharm Sci, 11(2), 107-116, 107-116, 2012.
  • Godge G, Hiremath S, Colonic delivery of film coated meloxicam tablets using natural polysaccharide polymer mixture, Int Curr Pharm J,1(9), 264-271, 2012.
  • Kharia AA, Hiremath SN, Omray LK, Yadav R Godge GR, Gastro retentive drug delivery system, Indian Drugs, 48 (5), 7-15, 2011.
  • Hiremath SN, Godge GR, Kharia AA, Vaidya VR, Studies on the preparation, characterization and solubility of ?-cyclodextrin-nelfinavir inclusion complexes, JPRHC, 2 (3), 279-284, 2010.
  • Vaidya VR, Karodi RS, ,Mohite MT, Hiremath SN, Godge GR, Formulation optimization of mucoadhesive buccal tablets of carvedilol using 32 full factorial design. Deccan J Pharm Cosmetol, [ISSN: 0976-1403], 1(2), 7-20, 2010.
  • Hiremath SN, Kharia AA, Godge GR, Formulation strategiesfFor low absorption window antihypertensive agents, Res J Pharmacy Technol, 3 (1), 2010.
APA S. Z C, G. R G, K.K P, K.A R (2016). Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. , 91 - 102.
Chicago S. Z Chemate,G. R Godge,K.K Pawa,K.A Rupnar Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. (2016): 91 - 102.
MLA S. Z Chemate,G. R Godge,K.K Pawa,K.A Rupnar Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. , 2016, ss.91 - 102.
AMA S. Z C,G. R G,K.K P,K.A R Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. . 2016; 91 - 102.
Vancouver S. Z C,G. R G,K.K P,K.A R Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. . 2016; 91 - 102.
IEEE S. Z C,G. R G,K.K P,K.A R "Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery." , ss.91 - 102, 2016.
ISNAD S. Z, Chemate vd. "Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery". (2016), 91-102.
APA S. Z C, G. R G, K.K P, K.A R (2016). Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. Turkish Journal of Pharmaceutical Sciences, 13(1), 91 - 102.
Chicago S. Z Chemate,G. R Godge,K.K Pawa,K.A Rupnar Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. Turkish Journal of Pharmaceutical Sciences 13, no.1 (2016): 91 - 102.
MLA S. Z Chemate,G. R Godge,K.K Pawa,K.A Rupnar Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. Turkish Journal of Pharmaceutical Sciences, vol.13, no.1, 2016, ss.91 - 102.
AMA S. Z C,G. R G,K.K P,K.A R Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. Turkish Journal of Pharmaceutical Sciences. 2016; 13(1): 91 - 102.
Vancouver S. Z C,G. R G,K.K P,K.A R Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery. Turkish Journal of Pharmaceutical Sciences. 2016; 13(1): 91 - 102.
IEEE S. Z C,G. R G,K.K P,K.A R "Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery." Turkish Journal of Pharmaceutical Sciences, 13, ss.91 - 102, 2016.
ISNAD S. Z, Chemate vd. "Preparation and Evaluation of Hollow Calcium Pectinate Beads for Floating-Pulsatile Drug Delivery". Turkish Journal of Pharmaceutical Sciences 13/1 (2016), 91-102.