Development and Evaluation of Solid Dispersion Formulations of Olanzepine
Abstract
The purpose of present study was to enhance the aqueous solubility of olanzapine by using the Solid dispersion technique. Solid dispersions of olanzapine were prepared by the dispersion method using PGS and SSG as carriers. Drug-carrier ratios such as 1 : 1, 1 : 2, 1 : 4, 1 : 6, 1: 8 and 1 : 10 were tried for optimization. Characterization was done by phase solubility, in-vitro release, saturation solubility, permeation, wettability, XRD and FTIR analysis. Solid dispersions showed higher solubility and an improved drug release profile than the pure drug. Solid dispersion and physical mixture with a drug-polymer ratio of 1 : 10 showed the best release profile in comparison with the other samples. Phase solubility results verified the solubilization effect of the carrier. XRD and NIR analysis confirmed the reduction of crystallinity in the samples. The release study findings were well supported by the results of wettability, saturation solubility and permeability studies. IR analysis substantiated the inertness of the carrier. It was concluded that pregelatinised starch (PGS) and sodium starch glycollate (SSG) could be utilized as effective carriers to improve the aqueous solubility of poorly soluble drugs.
Keywords: Olanzapine, solid dispersion, solubility, evaluation.
Keywords:
Olanzapine, solid dispersion, solubility, evaluationDOI
https://doi.org/10.22270/jddt.v13i10.5985References
Sarkar B, et al. Effect of sustained release solid dispersions on dissolution of poorly soluble drug. Asian J Biomed Pharm Sci 2011; 1(2):08-10.
Kumar A, Kumar K. Solid dispersion-strategy to enhance solubility and dissolution of poorly water soluble drugs. Universal Journal of Pharmaceutical Research2017; 2(5):50-54. https://doi.org/10.22270/ujpr.v2i5.RW4
K R Bobe, et al. Formulation and evaluation of solid dispersion of atorvatstatin with various carriers. Pharmacie Globale (IJCP) 2011, 1 (02).
Mahmoud A. Younis. Solid dispersion technology, a contemporary overview on a well established technique. Universal Journal of Pharmaceutical Research2017; 2(3):14-18. https://doi.org/10.22270/ujpr.v2i3.RW1
Tandale P, et al. Formulation and evaluation of extended release solid dispersions conatining simvastatin. Asian J Biomed Pharm Sci 2011; 1 (3):13-19.
Md. Shahidul Islam, Rasheda Akter Lucky. Development and in vitro dissolution study of binary and ternary solid dispersions of aceclofenac. Universal Journal of Pharmaceutical Research2019;4(1):29-34.
Wang Y, Bao Y, Liu J, Duan L, Cui Y. Olanzepine 5 mg Once Daily Improves Lower Urinary Tract Symptoms and Erectile Dysfunction: A Systematic Review and Meta-analysis. Low Urin Tract Symptoms 2018; 10 (1):84-92. https://doi.org/10.1111/luts.12144 PMid:29341503
Jajere UM, Achadu AE. Fabrication and characterization of ezetimibe solid dispersion for solubility enhancement. Universal Journal of Pharmaceutical Research2017; 2(1):11-14. https://doi.org/10.22270/ujpr.v2i1.R3
Daugan A, et al. The discovery of Olanzepine: A novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo1',5':1,6pyrido3,4-bindole-1,3(2H)-dione analogues. J Med Chem 2003; 46 (21):4525-32. https://doi.org/10.1021/jm030056e PMid:14521414
Akhter S, Hossen MS, Salahuddin M, Sunny MA, Sathi FA, Islam MS. In vitro dissolution study of glimepiride from binary and ternary solid dispersion formulation. Universal Journal of Pharmaceutical Research 2019; 4(5):7-11. https://doi.org/10.22270/ujpr.v4i5.310
Mahajan HS, Kokate VB. Development and characterization of oral dissolving films of Olanzepine based on pregelatinized hydroxypropyl pea starch. Indian J Novel Drug Deliv. 2015; 7(3):100- 107.
Anwar W, Dawaba HM, Afouna MI, SamyAM. Screening study for formulation variables in preparation and characterization of candesartan cilexetil loaded nanostructured lipid carriers. Universal Journal of Pharmaceutical Research 2019; 4(6):8-19. https://doi.org/10.22270/ujpr.v4i6.330
Haaf F, Sanner A, Straub F. Polymers of N-Vinylpyrrolidone: Synthesis, Characterization and Uses. Polymer J 1985; 17:143-152. https://doi.org/10.1295/polymj.17.143
Magdum SS. Liquisolid technique for dissolution and bioavailability enhancement of poorly soluble drugs. Universal Journal of Pharmaceutical Research2017; 2(5):42-48. https://doi.org/10.22270/ujpr.v2i5.RW3
Yoshida K, Sakurai Y, Kawahara S, et al. Anaphylaxis to polyvinylpyrrolidone in povidone-iodine for impetigo contagiosum in a boy with atopic dermatitis. International Archives of Allergy and Immunology 2008; 146 (2):169-73. https://doi.org/10.1159/000113522
PMid:18204285
Singh S, Virmani T, Virmani R, Kumar P, Mahlawat G. Fast dissolving drug delivery systems: formulation, preparation techniques and evaluation. Universal Journal of Pharmaceutical Research2018;3(4):56-64. https://doi.org/10.22270/ujpr.v3i4.185
Verma BK, Pandey S, Arya P. Tablet granulation: current scenario and recent advances. Universal Journal of Pharmaceutical Research2017; 2(5): 30-35. https://doi.org/10.22270/ujpr.v2i5.RW1
Mahaparale PR, Gudsoorkar VR, et al. Studies on solid dispersions of meloxicam. Ind J Pharm Educ Res 2006; 40(4):241- 244.
ALGIN YAPAR E, BESKAN U, KARAVANA SY. A recent overview of locally administered topical otic dosage forms. Universal Journal of Pharmaceutical Research 2019; 4(4):39-42. https://doi.org/10.22270/ujpr.v4i4.299
Published
Abstract Display: 475 
PDF Downloads: 484 PDF Downloads: 27 How to Cite
Issue
Section
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.