The purpose of this research was to design CPOP tablets to achieve controlled delivery of diltiazem hydrochloride (DH) up to 12 hours, which is a water-soluble calcium channel blocker with a short biological half-life. Two batches of osmotic tablet cores were prepared, containing DH with mannitol as an osmotic agent (1: 1.5 ratio). The tablet cores formulation with 10 mm diameter achieved the required technical and mechanical specifications. Direct compression technique was used to prepare the tablet cores which were evaluated in terms of mechanical resistance and uniformity of dosage units, followed by spray film coating using cellulose acetate as a former polymer of the semipermeable membrane and polyethylene glycol (PEG) as a pore forming agent. Several molecular weights of PEG (6000, 1500 and 400) were used and coating thickness levels were obtained. In vitro drug release, morphology of coating surface and the effect of pH change on release rate were investigated. Most of the prepared formulations demonstrated a burst release at the initial stage, which could be controlled by increasing the coating thickness. Formulations with PEG400 as a pore former presented better controlled and less burst release than those containing PEG6000, PEG1500, or a mixture of PEG6000: PEG400 (1: 1), and the pH change did not affect the drug release except in the initial stage.
Cite this article:
Lomass Soliman, Wehad Ibrahim. Effect of Coating Thickness and Polyethylene Glycol’s Molecular Weight on Diltiazem Hydrochloride Release from Controlled Porosity Osmotic Pump Tablets. Research Journal of Pharmacy and Technology. 2022; 15(9):4043-7. doi: 10.52711/0974-360X.2022.00678
Lomass Soliman, Wehad Ibrahim. Effect of Coating Thickness and Polyethylene Glycol’s Molecular Weight on Diltiazem Hydrochloride Release from Controlled Porosity Osmotic Pump Tablets. Research Journal of Pharmacy and Technology. 2022; 15(9):4043-7. doi: 10.52711/0974-360X.2022.00678 Available on: https://rjptonline.org/AbstractView.aspx?PID=2022-15-9-38
1. Théroux P. Taeymans Y. Morissette D. Bosch X. Pelletier G. Waters D. A Randomized Study Comparing Propranolol and Diltiazem in the Treatment of Unstable Angina. J. Am. Coll. Cardiol. 1985, 5(3), 717-22. Doi: 10.1016/s0735-1097(85)80400-9
2. Talreja O. Cassagnol M. Diltiazem. 4 Nov 2020. In: StatPearls [https://pubmed.ncbi.nlm.nih.gov/30422532/]. Treasure Island (FL): StatPearls Publishing; (Jan 2021 date last accessed). PMID: 30422532.
3. McKeever RG. Hamilton RJ. Calcium Channel Blockers. 25 Jul 2021. In: StatPearls [https://pubmed.ncbi.nlm.nih.gov/29494080/]. Treasure Island (FL): StatPearls Publishing; (Jan 2021 date last accessed). PMID: 29494080.
4. Adibkia K. Shokri J. Barzegar-Jalali M. Solduzian M. Javadzadeh Y. Effect of Solvent Type on Retardation Properties of Diltiazem HCl form Liquisolid Tablets. Colloids Surf. B. 2014, 113, 10-14. https://doi.org/10.1016/j.colsurfb.2013.08.017
5. Hammad T. Ibrahim W. Mhanna Z. The Influence of Type and Concentration of Polymer on Furosemide Release from Extended Hard Capsules. Tuj-hlth. 2016, 37(6). Tuj-hlth [Internet]. 2016Oct.18 [cited 2022Jan.25];37(6). Available from: http://journal.tishreen.edu.sy/index.php/hlthscnc/article/view/2077
6. Ummadi S. Shravani B. Raghavendra Rao NG. Srikanth Reddy M. Sanjeev Nayak B. Overview on Controlled Release Dosage Form. Int J Pharm Sci Res. 2013, 7(8), 51-60. http://ijps.aizeonpublishers.net/content/2013/4/ijps258-269.pdf
7. Wankhade VP. Sridhar E. Ingole SD. Sheaikh S. Kawtikwar PS. To Evaluate the Effect of Food and other GI Factors on Osmotic Tablet of Aceclofenac. Research J. Pharm. and Tech. 2010, 3(4), 1053-57. Doi: 10.5958/0974-360X
8. Ibrahim W. Haroun M. Saker R. Preparation and Evaluation of Sustained Release Tablets of Nifedipine Solid Dispersions. Tuj-hlth. 2020, Vol. (42) No. (3). Tuj-hlth [Internet]. 2020Aug.1 [cited 2022Jan.25];42(3). Available from: http://journal.tishreen.edu.sy/index.php/hlthscnc/article/view/9760
9. Stillhart C. Vučićević K. Augustijns P. Basit AW. Batchelor H. Flanagan TR. Gesquiere I. et al Impact of Gastrointestinal Physiology on Drug Absorption in Special Populations––An UNGAP Review. Eur J Pharm Sci. 2020, 147, 105280. https://doi.org/10.1016/j.ejps.2020.105280
10. Murkute RS. Wanare RS. Dongre KJ. A Review: Recent Scenario on Osmotic Controlled Drug Delivery System. Research J. Pharm. and Tech. 2012, 5(5), 580-91. Doi: 10.5958/0974-360X
11. Verma RK. Mishra B. Garg S. Osmotically Controlled Oral Drug Delivery. Drug Dev Ind Pharm. 2000, 26(7), 695-708. https://doi.org/10.1081/DDC-100101287
12. Umaretiya GM. Chavda JR. Patel JK. Fabrication and Characterization of Single Layer Osmotic Pump (SCOP) by Solubility Modulation Approach for Fluvoxamine Maleate. Research J. Pharm. and Tech. 2020, 13(8), 3817-24. Doi: 10.5958/0974-360X.2020.00676.9
13. Mahalpure NP. Gondkar SB. Saudagar RB. A Review on-Controlled-Porosity Osmotic Pump Tablet. Asian J. Res. Pharm. Sci. 2016, 6(2), 101-06. Doi: 10.5958/2231-5659.2016.00014.X
14. Malaterre V. Ogorka J. Loggia N. Gurny R. Oral Osmotically Driven Systems: 30 Years of Development and Clinical Use. Eur. J. Pharm. Biopharm. 2009, 73(3), 311-23. https://doi.org/10.1016/j.ejpb.2009.07.002
15. Zentner GM. Rork GS. Himmelstein KJ. The Controlled Porosity Osmotic Pump. J. Control. Release. 1985, 1(4), 269-82. https://doi.org/10.1016/0168-3659(85)90003-3
16. Sahoo CK. Rao SRM. Sudhakar M. Evaluation of Controlled Porosity Osmotic Pump Tablets: A Review. Research J. Pharm. and Tech. 2015, 8(12), 1340-46. Doi: 10.5958/0974-360X.2015.00312.1
17. Farheen F. Elango K. Devi Damayanthi R. Santhanalakshmi G. Formulation and Evaluation of Controlled Porosity Prednisolone Osmotic Tablets for Colon Targeting. Research J. Pharm. and Tech. 2011, 4(7), 1106-10. Doi: 10.5958/0974-360X
18. Hemlata T. Amit A. Tripti B. Palak A. Akansha B. Aditi B. Swapnil G. et al Formulation and Evaluation of Self-Poring Osmotic Tablet of Diltiazem HCl for the Treatment of Hypertension. Research J. Pharm. and Tech. 2018, 11(5), 1768-73. Doi: 10.5958/0974-360X.2018.00328.1
19. Prabakaran D. Singh P. Kanaujia P. Vyas SP. Effect of Hydrophilic Polymers on the Release of Diltiazem Hydrochloride from Elementary Osmotic Pumps. Int. J. Pharm. 2003, 259(1-2), 173-79. https://doi.org/10.1016/S0378-5173(03)00230-8
20. Prasad MB. Vidyadhara S. Sasidhar RLC. Balakrishna T. Trilochani P. Development and Evaluation of Diltiazem Hydrochloride Controlled-Release Pellets by Fluid Bed Coating Process. J Adv Pharm Technol Res. 2013, 4(2), 101. Doi: 10.4103/2231-4040.111526
21. Ismail R. Hammad T. Madani F. Formulation and in Vitro Evaluation of Once-Daily Methyldopa Sustained Release Matrix Tablets. Research J. Pharm. and Tech. 2015, 8(2), 161-66. Doi : 10.5958/0974-360X.2015.00029.3
22. United States Pharmacopeial, convention. The United States pharmacopeia. the national formulary. 36th revision 31st edition. 2013, Rockville, United States Pharmacopeial Convention.
23. European Pharmacopoeia 5th edition. 2007, Strasbourg: Council of Europe.
24. Prabu SL. Shirwaikar AA. Shirwaikar A. Ravikumar G. Kumar A. Jacob A. Formulation and Evaluation of Oral Sustained Release of Diltiazem Hydrochloride Using Rosin as Matrix Forming Material. Ars Pharm 2009, 50(1), 32-42. https://www.scopus.com/inward/record.uri?eid=2-s2.0-70349666783&partnerID=40&md5=04e41443d7abfd7125c307-979b98b947
25. Banerjee A. Verma PRP. Gore S. Controlled Porosity Solubility Modulated Osmotic Pump Tablets of Gliclazide. AAPS PharmSciTech 2015, 16(3), 554-68. https://doi.org/10.1208/s12249-014-0246-0
26. Li G. Wang Y. Chen H. Leng D. Ma P. Dong Y. Gao L. et al Can Semipermeable Membranes Coating Materials Influence in Vivo Performance for Paliperidone Tri-Layer Ascending Release Osmotic Pump Tablet: in Vitro Evaluation and in Vivo Pharmacokinetics Study. Asian J. Pharm. Sci. 2015, 10(2), 128-37. https://doi.org/10.1016/j.ajps.2014.12.002
27. Bonferoni MC. Rossi S. Ferrari F. Stavik E. Pena-Romero A. Caramella C. Factorial Analysis of the Influence of Dissolution Medium on Drug Release from Carrageenan-Diltiazem Complexes. AAPS Pharmscitech 2000, 1(2), 72-9. https://doi.org/10.1208/pt010215