Inclusion Complexation in Sulfobutyl Ether Beta Cyclodextrin and Dispersion in Gelucire for Sustained Release of Nifedipine Employing Almond Gum
Abstract
In the present research investigation, the utility of employing high dissolving forms of nifedipine for sustained release from matrix tablets with almond gum as major release retardant is explored. A poorly soluble BCS class II drug nifedipine is chosen as a model drug. Efforts were made to alter the dissolution characteristics of the drug before it is entrapped in the polymer matrix of almond gum. Inclusion complexation in sulfobutyl ether beta cyclodextrin or solid dispersion in gelucire (50/13) resulted in enhanced dissolution of nifedipine. The high dissolving forms are characterized by x-ray diffraction, differential scanning calorimetry and infra-red spectroscopy. The matrix tablets prepared employing the high dissolving forms exhibited satisfactory characteristics such as hardness, friability, swelling index. The drug release is found to be slow and spread over a period of 12 hours and the release could be modified with changes in nature of high dissolving form and the proportion of almond gum as the major release retardant. Employing high dissolving forms in matrix tablets of almond gum is found to be a novel approach in obtaining slow and complete release of poorly soluble drug such as nifedipine.
Keywords: sulfobutyl ether beta cyclodextrin, solid dispersion, nifedipine
DOI
https://doi.org/10.22270/jddt.v9i6.3681References
Nowsheen G, Archana B. Naltrexone: A review of existing sustained drug delivery systems and emerging nano-based systems. J Control Release. 2014; 183:154-166.
Varaporn B, Junyapraserta G. Release profile comparison and stability of diltiazem–resin microcapsules in sustained release suspensions. Int J Pharm. 2008; 352(1):81-91.
Amidon GL, Lennerlas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995; 12:413-20.
Nixon, J.R., 1983. Release characterization of microcapsules. In: Lim, F. (Ed.), Biomedical Applications of Microcapsulation. CRC Press, Boca Raton, FL, p. 19. Peppas NA., Sahlin,
Benita S, Barkai A, Pathak YV. 1990. Effect of drug loading extent on the in vitro release kinetic behavior of nifedipine from polyacrylate microspheres. J. Control. Rel. 1990; 12:213.
AHFS Drug Information. 2018 published by American Society of Health System Pharmacists, p.2005-2012
Okimoto K, Rajewski RA, Uekama K, Jona JA, Stella VJ. The interaction of charged and uncharged drugs with neutral (HP-beta-CD) and anionically charged (SBE7-beta-CD) beta-cyclodextrins. Pharm Res. 1996; 13:256–1264
Sheng QI, Delphine M, Duncan QM. An Investigation into the Mechanism of Dissolution Rate Enhancement of Poorly Water-Soluble Drugs from Spray Chilled Gelucire 50/13 Microspheres J Pharm Sci 2010; 99(1):262-274
Dordunoo SK, Ford JL, Rubinstein MH. Solidification studies of polyethylene glycols, gelucire 44/14 or their dispersions with triamterene or temazepam. J Pharm Pharmacol 1996; 48:782–9
Bouaziz, F, Ben Romdhane, M et al. Healing efficiency of oligosaccharides generated from almond gum (Amygdalus communis) on dermal wounds of adult rats. J Tissue Viability. 2014; 23(3):98–108.
Sarojini A, Kunam DS, Manavalan R, Jayanthi B. Effect of natural almond gum as a binder in the formulation of diclofenac sodium tablets Int J Pharm Sci Res. 2010; 1(3):55-60.
Syed AH, Jaisankar V. An eco-friendly synthesis, characterization and antibacterial applications of novel almond gum – poly(acrylamide) based hydrogel silver nanocomposite Polym Test. 2017; 62 (10):1016 -1029.
Higuchi T, Connors A. Phase-solubility techniques. In: Advances in analytical chemistry instrumentation. New York, NY: Wiley Interscience; 1965; 117–211.
Carrier RL, Miller LA, Ahmed I. The utility of cyclodextrins for enhancing oral bioavailability. J Control Release. 2007; 123:78–99.
Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol. 1975; 27:48–9.
Moore JW and Flanner HH. Mathematical comparison of dissolution profiles. Pharm. Tech. 1996; 20(6):64–75.
Ali SL, In Analytical Profiles of Drug Substances, K. Florey, Ed., Academic Press Inc., New York 1989, p. 221.
Mielcarek J, Sadaj A. Inclusion compounds of nifedipine and other 1, 4-dihydropyridine derivatives with cyclodextrins I. Complexation of nifedipine with –cyclodextrins Acta. Pol. Pharm 1994; 51:15.
Ghori, M.U, Conway, B.R. Hydrophilic matrices for oral control drug delivery. Am. J. Pharmacol. Sci. 2015; 3:103–109
Higuchi T. Mechanism of sustained action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963; 52(12):1145-1149.
Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983; 15:25-35.
Published
Abstract Display: 680
PDF Downloads: 814 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).

.