Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: In vitro evaluation and in vivo bioavailability test

Acta Pharmacologica Sinica

Volumn 32, Issue 10, 2011, Pages 1294-1302

  Wang, Yan Ping ^a   Gan, Yong ^a   Zhang, Xin Xin ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

bioavailability; gastroretentive sustained release tablet; immunosuppressants; self microemulsifying lipid mixture; tacrolimus

Indexed keywords

CHITOSAN; CREMOPHOR; GLYCERIC ACID; MACROGOL; MANNITOL; POVIDONE; TACROLIMUS;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; DRUG SYNTHESIS; FEMALE; GASTRORETENTIVE SUSTAINED RELEASE; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RABBIT; SELF MICROEMULSIFYING MIXTURE; TABLET; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; BIOLOGICAL AVAILABILITY; DELAYED-ACTION PREPARATIONS; DOGS; EMULSIONS; FEMALE; GASTROINTESTINAL TRACT; GLYCERIDES; IMMUNOSUPPRESSIVE AGENTS; MALE; OCTANOIC ACIDS; POLYETHYLENE GLYCOLS; RABBITS; TABLETS; TACROLIMUS;

EID: 80053906378     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1038/aps.2011.90     Document Type: Article

References (37)

1. Yamashita K, Nakate T, Okimoto K, Ohike A, Tokunaga Y, Ibuki R, et al. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm 2003; 267: 79-91. (Pubitemid 37352952)
2. Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, et al. FK 506, a novel immunosuppressant isolated from a Streptomyces I. Fermentation, isolation and physico-chemical and bio logical characteristics. J Antibiot 1987; 42: 1249-55. (Pubitemid 17138109)
3. Plosker GL, Foster RH. Tacrolimus - a further update of its pharmacology and therapeutic use in the management of organ transplantation. Drugs 2000; 59: 323-89. (Pubitemid 30168519)
4. Borhade V, Nair H, Hegde D. Design and evaluation of self-micro- emulsifying drug delivery system (SMEDDS) of tacrolimus. AAPS PharmSciTech 2008; 9: 13-21.
5. Abdalla A, Klein S, Mader K. 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 2008; 35: 457-64.
6. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004; 58: 173-82. (Pubitemid 38479922)
7. Abdalla A, Mader K. Preparation and characterization of a self-emulsifying pellet formulation. Eur J Pharm Biopharm 2007; 66: 220-6. (Pubitemid 46654779)
8. Nazzal S, Khan MA. Controlled release of a self-emulsifying formulation from a tablet dosage form: stability assessment and optimization of some processing parameters. Int J Pharm 2006; 315: 110-21. (Pubitemid 43674113)
9. Patil P, Joshi P, Paradkar A. Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen. AAPS PharmSciTech 2004; 5: e42.
10. Joseph S, inventors; AluhaRx Inc., assignee. Solid self-emulsifying dosage form for improved delivery of poorly soluble hydrophobic com pounds and the process for preparation there of. US Patent 10252158. 2002 Sep 23.
11. Tang B, Cheng G, Gu JC, Xu CH. Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms. Drug Discovery Today 2008; 13: 606-12.
12. Serratoni M, Newton M, Booth S, Clarke A. Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system. Eur J Pharm Biopharm 2007; 65: 94-8. (Pubitemid 44834468)
13. Balakrishnan P, Lee BJ, Oh DH, Kim JO, Hong MJ, Jee JP, et al. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS). Eur J Pharm Biopharm 2009; 72: 539-45.
14. Nazzal S, Nutan M, Palamakula A, Shah R, Zaghloul AA, Khan MA. Optimization of a self-nanoemulsified tablet dosage form of ubiquinone using response surface methodology: effect of formulation ingredients. Int J Pharm 2002; 240: 103-14. (Pubitemid 34607707)
15. Tuleu C, Newton M, Rose J, Euler D, Saklatvala R, Clarke A, et al. 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 2004; 93: 1495-502. (Pubitemid 38725021)
16. Tamura S, Tokunaga Y, Ibuki R, Amidon GL, Sezaki H, Yamashita S. The site-specific transport and metabolism of tacrolimus in rat small intestine. J Pharmacol Exp Ther 2003; 306: 310-6. (Pubitemid 36734386)
17. Venkataramanan R, Swaminathan A, Prasad T, Jain A, Zuckerman S, Warty V, et al. Clinical pharmacokinetics of tacrolimus. Clin Pharmacokinet 1995; 29: 404-30. (Pubitemid 26004179)
18. Holm P, Norling T, Lademann AM, inventors; LIFECYCLE PHARMA A/S, assignee. Once daily oral dosage form comprising tacrolimus. Patent WO2008/145143. 2008 May 30.
19. Kagayama A, Tanimoto S, Fujisaki J, Kaibara A, Ohara K, Iwasaki K, et al. Oral absorption of FK506 in rats. Pharm Res 1993; 10: 1446-50. (Pubitemid 23302660)
20. Shigeki T, Atsuo O, Rinta I, Gordon L, Shinji Y. Tacrolimus is a class II low-solubility high-permeability drug: the effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats. J Pharm Sci 2002; 91: 719-29.
21. Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin Drug Deliv 2006; 3: 217-33. (Pubitemid 43338093)
22. 2 generation by benchtop MRI and its relation to drug release and floating strength. Eur J Pharm Biopharm 2008; 69: 708-17.
23. Ramji AKA, Chandra SRG, Prabhakar RV. Formulation and evaluation of swellable and floating gastroretentive ciprofloxacin hydrochloride tablets. AAPS PharmSciTech 2009; 10: 220-6.
24. Parikh DC, Amin AF. In vitro and in vivo techniques to assess the performance of gastro-retentive drug delivery systems: a review. Expert Opin Drug Deliv 2008; 5: 951-65.
25. Gusler G, Berner B, Chau M, Berner B, inventors; Depomed, Inc, assignee. Optimal polymer mixtures for gastric. Patent AU2002337974. 2002 Oct 22.
26. Wu N, Wang LS, Tan DCW, Moochhala SM, Yang YY. Mathematical modeling and in vitro study of controlled drug release via a highly swellable and dissoluble polymer matrix: polyethylene oxide with high molecular weights. J Control Release 2005; 102: 569-81. (Pubitemid 40170201)
27. Mahalingam R, Jasti B, Birudaraj R, Stefanidis D, Killion R, Alfredson T, et al. Evaluation of polyethylene oxide compacts as gastroretentive delivery systems. AAPS PharmSciTech 2009; 10: 98-103.
28. Waterman KC. A critical review of gastric retentive controlled drug delivery. Pharm Dev Technol 2007; 12: 1-10. (Pubitemid 46902611)
29. Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastro-retentive dosage forms. J Control Release 2003; 90: 143-62.
30. Werle M, Bernkop SA. Thiolated chitosans: useful excipients for oral drug delivery. J Pharm Pharmacol 2008; 60: 273-81. (Pubitemid 351269813)
31. Chambin O, Jannin V, Champion D, Chevalier C, Rochat-Gonthier MH, Pourcelot Y. Influence of cryogenic grinding on properties of a self-emulsifying formulation. Int J Pharm 2004; 278: 79-89. (Pubitemid 38670439)
32. Constantinides PP. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm Res 1995; 12: 1561-72. (Pubitemid 26005509)
33. Li HT, Hardy RJ, Gu XC. Effect of drug solubility on polymer hydration and drug dissolution from polyethylene oxide (PEO) matrix tablets. AAPS PharmSciTech 2008; 9: 437-43.
34. Kim CJ. Effects of drug solubility, drug loading, and polymer molecular weight on drug release from Polyox® tablets. Drug Dev Ind Pharm 1998; 24: 645-51.
35. Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Self-emulsifying drug delivery systems (SEDDS) with polyglycolized glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm 1994; 106: 15-23. (Pubitemid 24110060)
36. Hauss DJ, Fogal SE, Ficorilli JV, Price CA, Roy T, Jayaraj AA, et al. Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor. J Pharm Sci 1998; 87: 164-9. (Pubitemid 28081323)
37. Fischl MA, Richman DD, Flexner C, Para MF, Jaubrich R, Karim A, et al. Phase I/II study of the toxicity, pharmacokinetics, and activity of the HIV protease inhibitor SC-52151. J Acquir Immune Defic Syndr Hum Retrovirol 1997; 15: 28-34.