Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design
DOI:
https://doi.org/10.37285/ijpsn.2018.11.6.7Abstract
Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.
Downloads
Download data is not yet available.
Metrics
Metrics Loading ...
Keywords:
Repaglinide, Diabetes, Solid dispersion, Central composite design.
Downloads
Published
2018-11-30
How to Cite
1.
D. V. R. N. B, I S. Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design. Scopus Indexed [Internet]. 2018 Nov. 30 [cited 2024 Dec. 30];11(6):4337-48. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/403
Issue
Section
Research Articles
References
Ahuja N, Katare OP and Singh B (2007). Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur. J. Pharm. Biopharm 65: 26–38.
Bayomi M A (1994). Geometric approach for zero-order release of drugs dispersed in an inert matrix. Pharm Res 11PP: 914-916.
Culy C and Jarvis B (2001). Repaglinide a review of its therapeutic use in type 2 diabetes mellitus. Drugs 61: 1625–1660
Guyot M, Fawaz F, Bildet J, Bonini F and Lagueny AM (1995). Bioavailability of Norfloxacin from PEG 6000 solid dispersion and cyclodextrin inclusion complexes in rabbits Int. J. Pharm 123: 53-63.
Ha ES, Choo GH, Baek IH, Min-Soo and Kim (2014). Formulation, Characterization and In Vivo Evaluation of Celecoxib-PVP Solid Dispersion Nano particles Using Supercritical Antisolvent Process Molecules 19: 20325-20339.
Kim EJ, Chun MK, Jang JS, Lee IH, Lee KR and Choi HK (2006). Preparation of a solid dispersion of Felodipine using a solvent wetting method. Eur. J. Pharm. Biopharm 64: 200-205.
Koh PT, Chuah JN, Talekar M, Gorajana A and Garg S (2013). Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems. Indian. J. Pharm. Sci 75(3): 291-301.
Landgraf W, Li N and Benson JBR (2005). New polymer enables near zero order release of drugs. Drug Deliv. Technol 5PP: 48-55.
Leuner C and Dressman J (2000). Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm 50 (1): 47 – 60.
Malaisse W (1999). Repaglinide a new oral anti-diabetic agent a review of recent preclinical studies. Eur J Clin Invest 29:21–29.
Manvi P, Narendra P and Bhaskar VH (2011). Preparation Characterization and In Vitro Evaluation of Repaglinide Binary Solid Dispersions with Hydrophilic Polymers. Int. J. Drug. Devel. Res 3 (2):111-121.
Martinez-Oharriz MC, Martin C, Goni MM, Rodriguez-Espinosa C, Tros-Ilarduya MC and Zornoza A (1999). Influence of polyethylene glycol 4000 on the polymorphic forms of diflunisal. Eur. J. Pharm. Sci 127-132.
Mooter GV, Augustijns P, Blaton N and Kinget R (1998). Solid Dispersion an Alternative Technique for Bioavailability Enhancement of Poorly Soluble Drugs. Int. J. Pharm 164: 67- 80.
Nauna Kettanech-Wold (1991). Use of Experimental Design in the Pharmaceutical Industry. Journal of Pharmaceutical and Biomedical Analysis 9(8): PP: 605-610.
Nayak AK, Laha B and Sen KK (2011). Development of hydroxyapatite-ciprofloxacin bone-implants using Quality by design. Acta Pharm 61:25-36.
Panneerselvam R (2012). Design and Analysis of Experiments. Eastern Economy Edition. PHI Learning Pvt. Ltd., New Delhi PP: 201-213.
Patel MM and Patel DM (2006). Fast dissolving valdecoxib tablets containing solid dispersion of valdecoxib. Int. J. Pharm. Sci 12: 222-226.
Pouton CW (2006). Formulation of Poorly water-soluble drugs for oral administration Physicochemical and physiological issues and the lipid formulation classification systems. Eur. J. Pharm. Sci 29: 278-87.
Purvis T, Mattucci ME, Crisp MT, Johnston KP and Williams RO (2007). Rapidly dissolving Repaglinide powders produced by the ultra-rapid freezing process. AAPS Pharm Sci Tech 8(3): E1 - E9.
Ravi K, Patel MJ, Dr. Rakesh P, Patel and Bhatt TV (2010). Modern Optimization Techniques in Field of Pharmacy. RJPBCS 1(2) PP: 148-157.
Ruan LP, Yu BY, Fu GM and Zhu D (2005). Improving the solubility of ampelopsis by solid dispersions and inclusion complexes. J. Pharm. Biomed. Analysis 38: 457 - 464.
Serajuddin A T M (1999). Solid Dispersion of Poorly Water-Soluble Drugs Early Promises Subsequent Problems and Recent Breakthroughs. J. Pharm. Sci 88 (10): 1058-1066.
Suvakanda D, Narasimha Murthy P, Lilakanta N and Prasanta Chowdhary (2010). Kinetic Modeling on drug release from controlled drug delivery systems. Acta Poloniae Pharmaceutical Drug research 67(3): 217-23.
Vande Waterbeemd H (1998). The fundamental variables of the bio pharmaceutics classification system a commentary. Eur J Pharm Sci 7:1–3.
Verma S, Rawat A, Kaul M and Saini S (2011). Solid dispersion a strategy for solubility enhancement. Int J Pharm Tech 3: 1062–99.
Vippagunta SR, Maul KA, Tallavajhala S and Grant DJW (2002). Solid-state characterization of nifedipine solid dispersions. Int. J. Pharm 236: 111–123.
Wagh VT, Jagtap VA, Shaikh TJ and Nandedkar SY (2012). Formulation and Evaluation of Glimepiride Solid Dispersion Tablets for Their Solubility Enhancement. J. Adv. Sci. Res 3(4): 36-41.
Yang D, Kulkarni R, Behme RJ and Kotiyan PN (2007). Effect of the melt granulation technique on the dissolution characteristics of griseofulvin. Int. J. Pharm 329:72-80.
Bayomi M A (1994). Geometric approach for zero-order release of drugs dispersed in an inert matrix. Pharm Res 11PP: 914-916.
Culy C and Jarvis B (2001). Repaglinide a review of its therapeutic use in type 2 diabetes mellitus. Drugs 61: 1625–1660
Guyot M, Fawaz F, Bildet J, Bonini F and Lagueny AM (1995). Bioavailability of Norfloxacin from PEG 6000 solid dispersion and cyclodextrin inclusion complexes in rabbits Int. J. Pharm 123: 53-63.
Ha ES, Choo GH, Baek IH, Min-Soo and Kim (2014). Formulation, Characterization and In Vivo Evaluation of Celecoxib-PVP Solid Dispersion Nano particles Using Supercritical Antisolvent Process Molecules 19: 20325-20339.
Kim EJ, Chun MK, Jang JS, Lee IH, Lee KR and Choi HK (2006). Preparation of a solid dispersion of Felodipine using a solvent wetting method. Eur. J. Pharm. Biopharm 64: 200-205.
Koh PT, Chuah JN, Talekar M, Gorajana A and Garg S (2013). Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems. Indian. J. Pharm. Sci 75(3): 291-301.
Landgraf W, Li N and Benson JBR (2005). New polymer enables near zero order release of drugs. Drug Deliv. Technol 5PP: 48-55.
Leuner C and Dressman J (2000). Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm 50 (1): 47 – 60.
Malaisse W (1999). Repaglinide a new oral anti-diabetic agent a review of recent preclinical studies. Eur J Clin Invest 29:21–29.
Manvi P, Narendra P and Bhaskar VH (2011). Preparation Characterization and In Vitro Evaluation of Repaglinide Binary Solid Dispersions with Hydrophilic Polymers. Int. J. Drug. Devel. Res 3 (2):111-121.
Martinez-Oharriz MC, Martin C, Goni MM, Rodriguez-Espinosa C, Tros-Ilarduya MC and Zornoza A (1999). Influence of polyethylene glycol 4000 on the polymorphic forms of diflunisal. Eur. J. Pharm. Sci 127-132.
Mooter GV, Augustijns P, Blaton N and Kinget R (1998). Solid Dispersion an Alternative Technique for Bioavailability Enhancement of Poorly Soluble Drugs. Int. J. Pharm 164: 67- 80.
Nauna Kettanech-Wold (1991). Use of Experimental Design in the Pharmaceutical Industry. Journal of Pharmaceutical and Biomedical Analysis 9(8): PP: 605-610.
Nayak AK, Laha B and Sen KK (2011). Development of hydroxyapatite-ciprofloxacin bone-implants using Quality by design. Acta Pharm 61:25-36.
Panneerselvam R (2012). Design and Analysis of Experiments. Eastern Economy Edition. PHI Learning Pvt. Ltd., New Delhi PP: 201-213.
Patel MM and Patel DM (2006). Fast dissolving valdecoxib tablets containing solid dispersion of valdecoxib. Int. J. Pharm. Sci 12: 222-226.
Pouton CW (2006). Formulation of Poorly water-soluble drugs for oral administration Physicochemical and physiological issues and the lipid formulation classification systems. Eur. J. Pharm. Sci 29: 278-87.
Purvis T, Mattucci ME, Crisp MT, Johnston KP and Williams RO (2007). Rapidly dissolving Repaglinide powders produced by the ultra-rapid freezing process. AAPS Pharm Sci Tech 8(3): E1 - E9.
Ravi K, Patel MJ, Dr. Rakesh P, Patel and Bhatt TV (2010). Modern Optimization Techniques in Field of Pharmacy. RJPBCS 1(2) PP: 148-157.
Ruan LP, Yu BY, Fu GM and Zhu D (2005). Improving the solubility of ampelopsis by solid dispersions and inclusion complexes. J. Pharm. Biomed. Analysis 38: 457 - 464.
Serajuddin A T M (1999). Solid Dispersion of Poorly Water-Soluble Drugs Early Promises Subsequent Problems and Recent Breakthroughs. J. Pharm. Sci 88 (10): 1058-1066.
Suvakanda D, Narasimha Murthy P, Lilakanta N and Prasanta Chowdhary (2010). Kinetic Modeling on drug release from controlled drug delivery systems. Acta Poloniae Pharmaceutical Drug research 67(3): 217-23.
Vande Waterbeemd H (1998). The fundamental variables of the bio pharmaceutics classification system a commentary. Eur J Pharm Sci 7:1–3.
Verma S, Rawat A, Kaul M and Saini S (2011). Solid dispersion a strategy for solubility enhancement. Int J Pharm Tech 3: 1062–99.
Vippagunta SR, Maul KA, Tallavajhala S and Grant DJW (2002). Solid-state characterization of nifedipine solid dispersions. Int. J. Pharm 236: 111–123.
Wagh VT, Jagtap VA, Shaikh TJ and Nandedkar SY (2012). Formulation and Evaluation of Glimepiride Solid Dispersion Tablets for Their Solubility Enhancement. J. Adv. Sci. Res 3(4): 36-41.
Yang D, Kulkarni R, Behme RJ and Kotiyan PN (2007). Effect of the melt granulation technique on the dissolution characteristics of griseofulvin. Int. J. Pharm 329:72-80.
