Effect of Granulation Methods on Drug Release Studies in Sustained Release Matrix Tablets of a Poorly Soluble Drug prepared using Synthetic Polymers
Vomiting or emesis is the abnormal emptying of stomach and upper part of intestine through esophagus and mouth. It occurs due to stimulation of the emetic (vomiting) centre situated in the medulla oblongata. Domperidone, a D2 receptor antagonist has antiemetic and prokinetic action is used as a model drug in the present work to prepare Sustained release matrix tablets using various synthetic polymers like Eudragit and HPMC K15 M. The tablets are designed to have a pH dependent release profile in order to prevent initial drug release in the stomach to reduce the possible gastro-irritant and ulcerogenic effects of the drug. Different polymer and diluent concentrations and various compression techniques like wet granulation technique and direct compression techniques were used in order to release the contents of the tablets in a sustained manner over a certain period of time. Domperidone is BCS Class II drug and its solubility was enhanced by preparing solid dispersions using solvent evaporation technique. In the present work solid dispersions containing drug and polymer mixture in the ratio 1:1 was further formulated into tablets by incorporating various synthetic polymers in three different concentrations. The tablets were prepared using different granulating techniques. Formulation (F3) containing drug and polymers in the ratio 1:1 prepared by wet granulation technique could sustain the drug release over a period of 12h and hence considering all the post compression parameters it was optimized as the better formulation. FTIR, DSC, X-Ray Diffraction, SEM studies were performed for optimized solid dispersion mixture and also the optimized formulation.
Keywords: Solubility enhancement, Solid dispersions, Solvent Evaporation, Wet granulation, Direct Compression.
2. Ratnaparkhi M.P, Gupta Jyothi P. Sustained release Oral drug delivery system- An Overview. International Journal of Pharma Research & Review, March 2013; 2(3):11-21.
3. Smith HS, Smith EJ, Smith AR. Pathophysiology of nausea and vomiting in palliative medicine. Ann Palliat Med. 2012; 1(1):87-93.
4. Andrew PLR, Horn CC. Signals for nausea and vomiting: Implications for model of upper gastrointestinal diseases. Auton Neurosci. 2006: 125(1-2):100-115.
5. Navin D, Sheodutt M, Bhanu PS, Sustained release drug delivery system. Ind J Res Pharma Biotech `2013; 1(3):301-10.
6. Chauhan MJ, Patel SA. A concise review on sustained drug delivery system and its opportunities. Am J Pharmtech Res 2012; 2(2):227-38.
7. Syed IA, Rao YM. A modified release drug delivery device: multilayerd matrix tablets. Am J Pharmtech Res 2012; 2(3):206-25.
8. Shanmugam SB, Ayyappan TS, Vetrichelvan T. Formulation and evaluation of sustained release matrix tablet of Zidovudine using different polymers. Res J Pharma Dosage Form Tech 2011; 3(1):17-23.
9. Rahmad MD, Ashan MD, Jha MK, Ahmed I, Rahman MD. Effect of mannitol on release of lamivudine sustained release matrix tablets using methocel K 15M co polymer. Invention Impact & Pharm Tech 2011; 1:58-62.
10. Madgulkar AR, Bhalekar MR, Warghade NS, Chavan NS. Preparation and evaluation of sustained release matrix tablet of nateglinide - effect of variables. Invention Rapid 2011; 2(1):14-19.
11. Jain D, Shukla SB. Formulation and evaluation of sustained release matrix tablets if isoniazid. A comparative aspect based on polymer. Invention Rapid: NDDS 2011; 2(1):14-19
12. Haresh M, Thimmasetty J, Ratan GN. Formulation development and in vitro evaluation of sustained release matrix tablet of risperidone. Invention Impact Pharmatech 2013; 1(1):28-34
13. Chithirra A, Mohamed S, Pillai k, Abirami A, Aruna A. Formulation and evaluation of controlled release frusemide tablets by bilayer technology. Journal of drug delivery and research 2013; 3(2):37-44.
14. Sanjay D, Bhaskar M, Sankha C, Das MK, Samrendu S, Ganguly S, Kakali D, Mridula M. Polymers derived from xanthomonas compesteries and retardant materials for the formulation of sustained release floating matrix tablet of atenolol. Int J BioL Macromol 2014; 651:345-56.
15. Praveen S, Ranendra N. Controlled release hydrophilic matrix tablet formulations of isoniazid: design and in vitro studies. AAPS PharmSciTech 2008; 9(4):1171-8.
16. Pranati S, Ranendra N. Formulation and evaluation of paracetamol tablets to access binding property of orange peel pectin. International journal of research and review 2010; (1):30-4.
17. Kamlesh JW, Arvind B, Shailesh A, Milind JU. Formulation and evaluation of sustained release gastroretentive dosage form of metformin Hcl. Der pharmacia letter 2013; 3(1):264-71.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
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 3.0 Unported License. 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).