PREPARATION AND EVALUATION OF COMPRESSION-COATED TABLETS FOR CHRONOPHARMACEUTICAL DRUG DELIVERY

Öz

Objective: This study aims to prepare and evaluate time-controlled drug delivery system of telmisartan. Telmisartan has low aqueous solubility, which is its major drawback. The solubility of the drug enhanced by using solid dispersion method and compression coated chronotherapeutic tablets were formulated. Material and Method: Solid dispersion of telmisartan was prepared by melting method. Direct compression method was used to prepare telmisartan containing core tablets and tablets were coated by compression-coating method. Prepared tablets were characterized in terms of hardness, diameter, and thickness. In order to demonstrate the pulsatile release, the tablets were subjected to USP Apparatus II dissolution test. Result and Discussion: Solid dispersion of telmisartan increased the solubility of telmisartan significantly (p<0.05). Compression-coated tablets were obtained with suitable hardness values (149.833±5.862-205.367±3.955 N) and telmisartan was released with lag times of 120-540 min which are suitable for chronopharmaceutic application.

Anahtar Kelimeler

• Chronopharmaceutical
• compression-coated
• pulsatile release
• solid dispersions
• telmisartan

KRONOFARMASÖTİK İLAÇ TAŞIYICI BASINÇLA KAPLANMIŞ TABLETLERİN HAZIRLANMASI VE DEĞERLENDİRİLMESİ

Öz

Amaç: Bu çalışmada telmisartanın çözünürlüğünün artırılması için katı dispersiyonlarının hazırlanması amaçlanmıştır. Telmisartanın en önemli sorunu olan düşük çözünürlüğe sahip olmasıdır. Telmisartanın çözünürlüğü katı dispersiyon yöntemi kullanılarak artırılmış ve basınçla kaplanmış kronoterapötik tabletler formüle edilmiştir. Gereç ve Yöntem: Telmisartanın katı dispersiyonları eritme yöntemi ile hazırlanmıştır. Telmisartan katı dispersiyonlarını içeren çekirdek tabletler doğrudan basım yöntemi ile hazırlanmış ve basınçla kaplama yöntemi ile kaplanmıştır. Hazırlanan tabletler sertlik, çap ve kalınlık açısından karakterize edilmiştir. Tabletlerde pulsatil ilaç salımını göstermek amacıyla USP aparat II çözünme hızı testi yapılmıştır. Sonuç ve Tartışma: Telmisartan katı dispersiyonları telmisartanın çözünürlüğünü önemli ölçüde artırmıştır (p<0,05). Basınçla kaplanmış tabletler uygun sertlik değerleri (149,833±5,862-205,367±3,955 N) ve elde edilmiştir. Telmisartan, kronofarmasötik uygulamalara uygun şekilde 120-540 dk arasında değişen gecikme sürelerinden sonra hızla salınmıştır.

Anahtar Kelimeler

• Basınçla kaplama
• katı dispersiyon
• kronofarmasötik
• pulsatil salım
• telmisartan

Kaynakça

1. 1. Lin, S.Y., Kawashima, Y. (2012). Current status and approaches to developing press-coated chronodelivery drug systems. Journal of Controlled Release, 157(3), 331-353. [CrossRef]
2. 2. Mandal, A.S., Biswas, N., Karim, K.M., Guha, A., Chatterjee, S., Behera, M., Kuotsu, K. (2010). Drug delivery system based on chronobiology-A review. Journal of Controlled Release, 147(3), 314-325. [CrossRef]
3. 3. Shah, S., Patel, R., Soniwala, M., Chavda, J. (2015). Development and optimization of press coated tablets of release engineered valsartan for pulsatile delivery. Drug Development and Industrial Pharmacy, 41(11), 1835-1846. [CrossRef]
4. 4. Sharma, G.S., Srikanth, M.V., Uhumwangho, M.U., Phani, K.K.S., Ramana, M.K.V. (2010). Recent trends in pulsatile drug delivery systems - A review. International Journal of Drug Delivery, 2(3), 200-212.
5. 5. Hermida, R.C., Ayala, D.E., Portaluppi, F. (2007). Circadian variation of blood pressure: The basis for the chronotherapy of hypertension. Advanced Drug Delivery Reviews, 59(9-10), 904-922. [CrossRef]
6. 6. Marzouk, M.A.H., Darwish, M.K., Yassin, G.E., El-Fattah, M.A.A. (2022). Pulsatile chronotherapeutic drug delivery for controlling early morning surge in blood pressure; Effect of coating on eplerenone in-vitro, in-vivo release and urinary Na/K ratio. Brazilian Journal of Pharmaceutical Sciences, 58. [CrossRef]
7. 7. Sungthongjeen, S., Puttipipatkhachorn, S., Paeratakul, O., Dashevsky, A., Bodmeier, R. (2004). Development of pulsatile release tablets with swelling and rupturable layers. Journal of Controlled Release, 95(2), 147-159. [CrossRef]
8. 8. Maroni, A., Zema, L., Del Curto, M.D., Loreti, G., Gazzaniga, A. (2010). Oral pulsatile delivery: rationale and chronopharmaceutical formulations. International Journal of Pharmaceutics, 398(1-2), 1-8. [CrossRef]

9. 9. Patel, B., Parikh, R., Swarnkar, D. (2012). Enhancement of dissolution of telmisartan through use of solid dispersion technique-surface solid dispersion. Journal of Pharmacy & Bioallied Sciences, 4(Suppl 1), S64-68. [CrossRef]
10. 10. Tran, P., Pyo, Y.-C., Kim, D.-H., Lee, S.-E., Kim, J.-K., Park, J.-S. (2019). Overview of the manufacturing methods of solid dispersion technology for improving the solubility of poorly water-soluble drugs and application to anticancer drugs. Pharmaceutics, 11(3), 132. [CrossRef]
11. 11. Huang, S., Williams, R.O. (2018). Effects of the preparation process on the properties of amorphous solid dispersions. AAPS PharmSciTech, 19(5), 1971-1984. [CrossRef]
12. 12. Schittny, A., Huwyler, J., Puchkov, M. (2020). Mechanisms of increased bioavailability through amorphous solid dispersions: a review. Drug Delivery, 27(1), 110-127. [CrossRef]
13. 13. Pandi, P., Bulusu, R., Kommineni, N., Khan, W., Singh, M. (2020). Amorphous solid dispersions: An update for preparation, characterization, mechanism on bioavailability, stability, regulatory considerations and marketed products. International Journal of Pharmaceutics, 586, 119560. [CrossRef]
14. 14. Van den Mooter, G. (2012). The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate. Drug Discovery Today: Technologies, 9(2), e79-e85. [CrossRef]
15. 15. Huang, Y., Dai, W.G. (2014). Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharmaceutica Sinica B, 4(1), 18-25. [CrossRef]
16. 16. Vo, C.L., Park, C., Lee, B.J. (2013). Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. European Journal of Pharmaceutics and Biopharmaceutics, 85(3 Pt B), 799-813. [CrossRef]
17. 17. Phuong, H.L.T., Tran, T.T., Lee, S.A., Nho, V.H., Chi, S.C., Lee, B.J. (2011). Roles of MgO release from polyethylene glycol 6000-based solid dispersions on microenvironmental pH, enhanced dissolution and reduced gastrointestinal damage of telmisartan. Archives of Pharmcal Research, 34(5), 747-755. [CrossRef]
18. 18. Borba, P.A., Pinotti, M., de Campos, C.E., Pezzini, B.R., Stulzer, H.K. (2016). Sodium alginate as a potential carrier in solid dispersion formulations to enhance dissolution rate and apparent water solubility of BCS II drugs. Carbohydrate Polymers, 137, 350-359. [CrossRef]
19. 19. Dukeck, R., Sieger, P., Karmwar, P. (2013). Investigation and correlation of physical stability, dissolution behaviour and interaction parameter of amorphous solid dispersions of telmisartan: a drug development perspective. European Journal of Pharmaceutical Sciences, 49(4), 723-731. [CrossRef]
20. 20. Marasini, N., Tran, T.H., Poudel, B.K., Cho, H.J., Choi, Y.K., Chi, S.C., Choi, H.G., Yong, C.S., Kim, J.O. (2013). Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. International Journal of Pharmaceutics, 441(1-2), 424-432. [CrossRef]
21. 21. Zhong, L., Zhu, X., Yu, B., Su, W. (2014). Influence of alkalizers on dissolution properties of telmisartan in solid dispersions prepared by cogrinding. Drug Development Industrial Pharmacy, 40(12), 1660-1669. [CrossRef]
22. 22. Higuchi, T. (1965). A phase solubility technique. Advances in Analytical Chemistry and Instrumentation, 4, 117-211.
23. 23. Aldawsari, H.M., Naveen, N.R., Alhakamy, N.A., Goudanavar, P.S., Rao, G.K., Budha, R.R., Nair, A.B., Badr-Eldin, S.M. (2022). Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization. Drug Delivery, 29(1), 2258-2268. [CrossRef]
24. 24. Rashid, R., Zaman, M., Ahmad, M., Khan, M.A., Butt, M.H., Salawi, A., Almoshari, Y., Alshamrani, M., Sarfraz, R.M. (2022). Press-coated aceclofenac tablets for pulsatile drug delivery: Formulation and in vitro evaluations. Pharmaceuticals, 15(3), 326. [CrossRef]
25. 25. Sawada, T., Kondo, H., Nakashima, H., Sako, K., Hayashi, M. (2004). Time-release compression-coated core tablet containing nifedipine for chronopharmacotherapy. International Journal of Pharmaceutics, 280(1-2), 103-111. [CrossRef]
26. 26. Gazzaniga, A., Palugan, L., Foppoli, A., Sangalli, M.E. (2008). Oral pulsatile delivery systems based on swellable hydrophilic polymers. European Journal of Pharmaceutics and Biopharmaceutics, 68(1), 11-18. [CrossRef]
27. 27. Edgar, K.J. (2007). Cellulose esters in drug delivery. Cellulose, 14(1), 49-64. [CrossRef]
28. 28. Obeidat, W.M., Alzoubi, N.M. (2014). Controlled-release cellulose esters matrices for water-soluble diclofenac sodium: compression and dissolution studies. Pharmazie, 69(2), 96-103.
29. 29. Praveen Kumar, B., Ramanaiah, S., Madhusudana Reddy, T., Reddy, K.S. (2014). Surface characterization of cellulose acetate propionate by inverse gas chromatography. Polymer Bulletin, 71(1), 125-132. [CrossRef]
30. 30. Wu, B., Shun, N., Wei, X., Wu, W. (2007). Characterization of 5-fluorouracil release from hydroxypropyl- methylcellulose compression-coated tablets. Pharmaceutical Development and Technology, 12(2), 203-210. [CrossRef]
31. 31. Rane, A.B., Gattani, S.G., Kadam, V.D., Tekade, A.R. (2009). Formulation and evaluation of press coated tablets for pulsatile drug delivery using hydrophilic and hydrophobic polymers. Chemical and Pharmaceutical Bulletin, 57(11), 1213-1217. [CrossRef]
32. 32. Dineshmohan, S., Gupta, V.R.M., Ramesh, A., Harika, V., Sravani, T. (2015). Effect of HPMC and ethyl cellulose polymeric granules and its combinations in press coated tablets of lornoxicam: fabrication and in vitro characterization. International Current Pharmaceutical Journal, 4(10), 447-452. [CrossRef]
33. 33. Pamu, S., Benazir, F., Rao Patnaik, K.S.K., Subrahmanyam, C. V. S. (2014). Design and evaluation of pulsatile drug delivery system for chronotherapeutic release of metprolol tartrate. International Journal of Biological & Pharmaceutical Research, 5(1), 83-88.
34. 34. Popova, T., Petkova, V., Dimitrov, M. (2016). Formulation approaches to pulsatile-release chronotherapeutical drug delivery system with montelukast sodium. World Journal of Pharmacy and Pharmaceutical Sciences, 5(6), 217-225.
35. 35. Patadia, R., Vora, C., Mittal, K., Mashru, R. (2016). Investigating effects of hydroxypropyl methylcellulose (HPMC) molecular weight grades on lag time of press-coated ethylcellulose tablets. Pharmaceutical Development and Technology, 21(7), 794–802. [CrossRef]
36. 36. Patil, S., Rakshe, A., Jagtap, R., Jagtap, S. (2022). Press coated bioadhesive pulsatile tablet of lisinopril for chronotherapy of cardiac disorders: In-vitro evaluation. Research Journal of Pharmacy and Technology, 15(7), 3057-3062. [CrossRef]
37. 37. Raina, B., Sharma, S., Bajwa, P. s., Sharma, A.R. (2022). Design development and optimization of chronotherapeutic delivery system of deflazacort. Journal of Pharmaceutical Innovation, 1-11. [CrossRef]
38. 38. Colorcon. The influence of hydro-alcoholic media on hypromellose matrix systems. https://www.colorcon.com/markets/pharmaceuticals/polymers-controlled-release/hydrophilic-matrix-tablets/methocel-cr/item/499-aaps-2006-influence-of-hydro-alcoholic-media-on-hypromellose-matrix-systems-499. Accessed date: 30.01.2023.
39. 39. Gill, P., Moghadam, T.T., Ranjbar, B. (2010). Differential scanning calorimetry techniques: Applications in biology and nanoscience. Journal of Biomolecular Techniques : JBT, 21(4), 167-193.
40. 40. Ha, N.S., Tran, T.T.-D., Tran, P. H.-L., Park, J.-B., Lee, B.-J. (2011). Dissolution-enhancing mechanism of alkalizers in poloxamer-based solid dispersions and physical mixtures containing poorly water-soluble valsartan. Chemical and Pharmaceutical Bulletin, 59(7), 844-850. [CrossRef]
41. 41. Fule, R., Amin, P. (2014). Development and evaluation of lafutidine solid dispersion via hot melt extrusion: Investigating drug-polymer miscibility with advanced characterisation. Asian Journal of Pharmaceutical Sciences, 9(2), 92-106. [CrossRef]
42. 42. Kim, E.J., Chun, M.K., Jang, J.S., Lee, I.H., Lee, K.R., Choi, H.K. (2006). Preparation of a solid dispersion of felodipine using a solvent wetting method. European Journal of Pharmaceutics and Biopharmaceutics, 64(2), 200-205. [CrossRef]