Araştırma Makalesi
Yıl 2020,
Cilt: 24 Sayı: 1, 56 - 70, 27.06.2025
Öz
Kaynakça
- [1] Reppas C, Kalantzi L. Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen. J Pharm Sci. 2006; 95(1): 4-14. [CrossRef]
- [2] Alleso M, Chieng N, Rehder S, Rantanen J, Rades T, Aaltonen J. Enhanced dissolution rate and synchronized Release of drugs in binary systems through formulation: Amorphous naproxen–cimetidine mixtures prepared by mechanical activation. J Control Rel. 2009; 136: 45–53. [CrossRef]
- [3] Hancock B, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci.1997; 86: 1–12. [Cross Ref]
- [4] Kaushal A, Bansal K. Thermodynamic behavior of glassy state of structurally related compounds. Eur J Pharm Biopharm. 2008; 69: 1067–1076. [CrossRef]
- [5] Bodmeier R, Wang J, Bhagwatwar H. Process and formulation variables in the preparation of wax microparticles by melt dispersion technique for water insoluble drugs. J Microcapsulation.1992; 9: 89-98. [CrossRef]
- [6] Ambike A, Mahadik K, Paradkar A. Stability study of amorphous valdecoxib. Int J Pharm.2004; 282: 151-162. [CrossRef]
- [7] Shinde R, Shelake M, Shetty S, Chavan Patil A, Pore Y, Late S. Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique. J Pharm Pharmacol. 2008; 60(9): 1121-1129. [CrossRef]
- [8] Baird J. Evaluation of amorphous solid dispersion properties using thermal analysis techniques. Adv Drug Deli Rev. 2012; 64: 396-421. [CrossRef]
- [9] Sanghvi R, Evans D, Yalkowsky S. Stacking complexation by nicotinamide: A useful way of enhancing drug solubility. Int J Pharm. 2007; 336(1): 35-41. [CrossRef]
- [10] Carstensen J. Advanced pharmaceutical solids. Marcel Dekker, New York, 2001; 117-227.
- [11] Hecq J, Deleers M, Fanara D, Vranckx H, Amighi K. Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine. Int J Pharm. 2005; 299(1-2): 167-177. [CrossRef]
- [12] Balania P, Wonga S. Influence of polymer content on stabilizing milled amorphous salbutamol sulphate. Int J Pharm. 2010; 391: 125–136. [CrossRef]
- [13] Amina M, Myasar M, khayrallah A. Preparation and evaluation of meloxicam solid dispersion by solvent evaporation method. Int Res J Pharm. 2014; 5: 838-845.
- [14] Bhende S, Jadhav N. Moringa coagulant as a stabilizer for amorphous solid AAPS PharmSciTech.2012; 13(2): 400- 410. [CrossRef]
- [15] Amidon G, Lennernas H, Shah V, Crison J. A theoretical base for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995; 12(3): 413-420. [CrossRef]
- [16] Branham M, Moyo T, Govender T. Preparation and solid-state characterization of ball milled saquinavir mesylate for solubility enhancement. Eur J Pharma and Biopharm. 2012; 80: 194-202. [CrossRef]
- [17] Chieng N, Aaltonen J, Saville D, Rades T. Physical characterization and stability of amorphous indomethacin and ranitidine hydrochloride binary systems prepared by mechanical activation. Eur J Pharm Biopharm.2009; 71: 47–54. [CrossRef]
- [18] Hancock B, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. Pharm Sci.1997; 86: 1–12. [CrossRef]
- [19] Hassan M, Najib N, Suleiman M. Characterization of glibenclamide glassy state. Int J Pharm.1991; 67(2):131–137. [CrossRef]
- [20] Hilden L, Morris K. Physics of amorphous solids. J Pharm Sci. 2004; 93: 3–12. [CrossRef]
- [21] Jacob S, Nair A, Patil N, Panda P. Solid state crystallinity, amorphous state, and it implications in the pharmaceutical process. Int J Pharm Sci Res. 2011; 2(3): 472-482.
- [22] Karmwar P, Graeser K, Gordon K, Strachan C, Rades T. Investigation of properties and recrystallization behavior of amorphous indomethacin samples prepared by different methods. Int J Pharm.2011; 417(1–2):94–100. [CrossRef]
- 23] Jadhav N, Gaikwad V, Nair K. Glass transition temperature: Basics and application in pharmaceutical sector. Asian J Pharm. 2010; 3: 83-88.
- [24] Kulkarni P, Dixit, Kumar S, Johri A. Preparation and evaluation of ketoprofen beads by melt solidification technique. Pelagia Res Lib. 2010; 1(2): 31-43.
- [25] Paradkar A, Maheshwari M, Ketkar A. Chouhan, B. Preparation and evaluation of ketoprofen beads by melt solidification technique. Int J Pharm. 2003; 33-42.
- [26] Pokharkar V, Mandpe L, Padamwar M, Ambike A, Mahadik K, Paradkar A. Development, characterization and stabilization of amorphous form of a low Tg drug. Powder Techno. 2006; 167: 20–25.
- [27] Paradkar A, Kamble R, Kadam S. Melt solidification technique: Incorporation of higher wax content in ibuprofen beads. AAPS Pharmtech Sci. 2004; 4: 325-329. [CrossRef]
Design and development of melt solidification of meloxicam for enhancement of solubility and dissolution
Öz
The objective of the present study was to prepare an amorphous system of BCS Class 2 drug meloxicam (MLX) to improve its solubility and dissolution by using the melt solidification techniques. About 40% of new chemical entities do not reach to market due to its poor aqueous solubility. Melt solidification technique is an important process to control the transition from liquid in to solid phase to obtain product in an amorphous form. During the process of heating, some solid gets melted and if quench cooled, instead of crystallizing gets converted to amorphous solid form appearing as that of glass, which improve dissolution and bioavailability of drugs. Physical mixtures of MLX were prepared by melt solidification technique using polymer (soluplus). The solubility and dissolution studies for the meloxicam and batches were conducted in a phosphate buffer (pH 6.8). The fourier transform infrared(FTIR) spectrophotometry, X-ray diffraction microscopy(XDM) and Differential scanning calorimetry(DSC) studies were conducted to evaluated pure drug and optimized batch(MS7). Saturation solubility and % drug release showed the improve solubility and dissolution, results suggest that optimized batch (MS7) containing drug and polymer in proportion of 1:4 (MLX:soluplus) was a successful enhancing the solubility and dissolution of MLX. The % crystallinity of MLX in amorphous sample was 18.60%, which indicates significant decrease in crystallinity of MLX in an amorphous system. The best fit model of optimized batch (MS7) was zero order model, showing the %drug release 96.83% and R2 0.9904. The present investigation, successfully enhancement solubility and dissolution of MLX by using melt solidification technique.
Anahtar Kelimeler
Meloxicam melt solidification dissolution solubility soluplus
Kaynakça
- [1] Reppas C, Kalantzi L. Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen. J Pharm Sci. 2006; 95(1): 4-14. [CrossRef]
- [2] Alleso M, Chieng N, Rehder S, Rantanen J, Rades T, Aaltonen J. Enhanced dissolution rate and synchronized Release of drugs in binary systems through formulation: Amorphous naproxen–cimetidine mixtures prepared by mechanical activation. J Control Rel. 2009; 136: 45–53. [CrossRef]
- [3] Hancock B, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci.1997; 86: 1–12. [Cross Ref]
- [4] Kaushal A, Bansal K. Thermodynamic behavior of glassy state of structurally related compounds. Eur J Pharm Biopharm. 2008; 69: 1067–1076. [CrossRef]
- [5] Bodmeier R, Wang J, Bhagwatwar H. Process and formulation variables in the preparation of wax microparticles by melt dispersion technique for water insoluble drugs. J Microcapsulation.1992; 9: 89-98. [CrossRef]
- [6] Ambike A, Mahadik K, Paradkar A. Stability study of amorphous valdecoxib. Int J Pharm.2004; 282: 151-162. [CrossRef]
- [7] Shinde R, Shelake M, Shetty S, Chavan Patil A, Pore Y, Late S. Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique. J Pharm Pharmacol. 2008; 60(9): 1121-1129. [CrossRef]
- [8] Baird J. Evaluation of amorphous solid dispersion properties using thermal analysis techniques. Adv Drug Deli Rev. 2012; 64: 396-421. [CrossRef]
- [9] Sanghvi R, Evans D, Yalkowsky S. Stacking complexation by nicotinamide: A useful way of enhancing drug solubility. Int J Pharm. 2007; 336(1): 35-41. [CrossRef]
- [10] Carstensen J. Advanced pharmaceutical solids. Marcel Dekker, New York, 2001; 117-227.
- [11] Hecq J, Deleers M, Fanara D, Vranckx H, Amighi K. Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine. Int J Pharm. 2005; 299(1-2): 167-177. [CrossRef]
- [12] Balania P, Wonga S. Influence of polymer content on stabilizing milled amorphous salbutamol sulphate. Int J Pharm. 2010; 391: 125–136. [CrossRef]
- [13] Amina M, Myasar M, khayrallah A. Preparation and evaluation of meloxicam solid dispersion by solvent evaporation method. Int Res J Pharm. 2014; 5: 838-845.
- [14] Bhende S, Jadhav N. Moringa coagulant as a stabilizer for amorphous solid AAPS PharmSciTech.2012; 13(2): 400- 410. [CrossRef]
- [15] Amidon G, Lennernas H, Shah V, Crison J. A theoretical base for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995; 12(3): 413-420. [CrossRef]
- [16] Branham M, Moyo T, Govender T. Preparation and solid-state characterization of ball milled saquinavir mesylate for solubility enhancement. Eur J Pharma and Biopharm. 2012; 80: 194-202. [CrossRef]
- [17] Chieng N, Aaltonen J, Saville D, Rades T. Physical characterization and stability of amorphous indomethacin and ranitidine hydrochloride binary systems prepared by mechanical activation. Eur J Pharm Biopharm.2009; 71: 47–54. [CrossRef]
- [18] Hancock B, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. Pharm Sci.1997; 86: 1–12. [CrossRef]
- [19] Hassan M, Najib N, Suleiman M. Characterization of glibenclamide glassy state. Int J Pharm.1991; 67(2):131–137. [CrossRef]
- [20] Hilden L, Morris K. Physics of amorphous solids. J Pharm Sci. 2004; 93: 3–12. [CrossRef]
- [21] Jacob S, Nair A, Patil N, Panda P. Solid state crystallinity, amorphous state, and it implications in the pharmaceutical process. Int J Pharm Sci Res. 2011; 2(3): 472-482.
- [22] Karmwar P, Graeser K, Gordon K, Strachan C, Rades T. Investigation of properties and recrystallization behavior of amorphous indomethacin samples prepared by different methods. Int J Pharm.2011; 417(1–2):94–100. [CrossRef]
- 23] Jadhav N, Gaikwad V, Nair K. Glass transition temperature: Basics and application in pharmaceutical sector. Asian J Pharm. 2010; 3: 83-88.
- [24] Kulkarni P, Dixit, Kumar S, Johri A. Preparation and evaluation of ketoprofen beads by melt solidification technique. Pelagia Res Lib. 2010; 1(2): 31-43.
- [25] Paradkar A, Maheshwari M, Ketkar A. Chouhan, B. Preparation and evaluation of ketoprofen beads by melt solidification technique. Int J Pharm. 2003; 33-42.
- [26] Pokharkar V, Mandpe L, Padamwar M, Ambike A, Mahadik K, Paradkar A. Development, characterization and stabilization of amorphous form of a low Tg drug. Powder Techno. 2006; 167: 20–25.
- [27] Paradkar A, Kamble R, Kadam S. Melt solidification technique: Incorporation of higher wax content in ibuprofen beads. AAPS Pharmtech Sci. 2004; 4: 325-329. [CrossRef]
Toplam 27 adet kaynakça vardır.
Ayrıntılar
| Birincil Dil | İngilizce |
|---|---|
| Konular | Eczacılık ve İlaç Bilimleri (Diğer) |
| Bölüm | Articles |
| Yazarlar | |
| Yayımlanma Tarihi | 27 Haziran 2025 |
| Yayımlandığı Sayı | Yıl 2020 Cilt: 24 Sayı: 1 |