Araştırma Makalesi
Employment of liquisolid approach in the development optimization and evaluation of an oral disintegrating tablet of aripiprazole
Öz
The major problems associated with the oral route of administration are low solubility, low permeability,
and hepatic degradation of drugs, leading to low bioavailability issues. Therefore, in this study, a biopharmaceutics
classification systems (BCS) class II drug aripiprazole was chosen to develop an oral disintegrating tablet using liquisolid
technology to enhance the solubility and dissolution rate of the drug. Liquisolid compact of aripiprazole was prepared
using polyethylene glycol (PEG 400) as a nonvolatile solvent, microcrystalline cellulose (MCC) as a carrier, and Aerosil
200 as a coating material. The formulations were optimized via the 23-factorial design. The optimum formulation was
further converted to oral disintegrating tablets with the help of the super disintegrant, cross povidone, and the produced
tablets were evaluated. The water solubility of aripiprazole was observed to have increased from 4.5µg/ml to 0.13mg/ml
in the liquisolid form and angle of repose was found to be reasonably passable. As was observed from the experimental
design, the solvent, solvent: carrier, and carrier were seen to have a significant influence on the selected responses. The
X-ray diffraction pattern of the optimized formula indicated a reduction in the peak number and the peak intensities
compared to the pure drug. The tablets prepared of liquisolid compacts displayed good tableting properties. The
disintegration time was found to be 40 seconds. The stability studies indicated no apparent changes in the properties
after a storage period of 3 months. The liquisolid compacts are an inexpensive method of preparing oral disintegrating
tablets of Aripiprazole with an assurance of suitable dissolution property of the drug.
Anahtar Kelimeler
Aripiprazole liquisolid compacts oral disintegrating tablets solubility bioavailability
Kaynakça
- Bary A-E, Louis A. Polmesartan medoxomil surface solid dispersion-based orodispersible tablets: formulation and in vitro characterization. Journal of Drug Delivery Science and Technology [Internet]. 2014;24(6):665– 72.http://dx.doi.org/10.1016/s1773-2247(14)50134-7
- Amidon GL, Lennernäs 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 [Internet]. 1995;12(3):413–20. http://dx.doi.org/10.1023/a:1016212804288
- Douroumis DD, Gryczke A, Schminke S. Development and evaluation of cetirizine hcl taste masked oral disintegrating tablets. AAPS PharmSciTech. 2011;(1).https://doi.org/10.1208/s12249-010-9569-7
- Hirani JJ, Rathod DA, Vadalia KR. Orally disintegrating tablets: A review. Trop J Pharm Res [Internet]. 2009;8(2). http://dx.doi.org/10.4314/tjpr.v8i2.44525
- Olmez SS, Vural I. Advantages and quality control of disintegrating tablets. Fabad J Pharm Sci. 2009;34(1).
- Spireas S. Liquisolid system and method of preparing same. U S Patent. 2002;6423339B – 6423340.
- Spireas, Spiridon, Bolton, Sanford M. Liquisolid systems and methods of preparing same. U S Patent.1999;5,968,550.
- Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm [Internet]. 2009;73(3):373–84. http://dx.doi.org/10.1016/j.ejpb.2009.08.002
- Sanjay PD, Deepak M. Liquisolid technology: Technique for formulation with enhanced bioavailability. World J Pharma Pharma Sci. 2013;3(1).
- Vranikova B, Pavlokova S, Gajdziok J. Experimental design for determination of effect of Super disintegrant combination on liquisolid system properties. J Pharm Sci. 2016;13:1–1.
- Vacheron-Trystram M-N, Braitman A, Cheref S, Auffray L. Antipsychotics in bipolar disorders. Encephale [Internet]. 2004;30(5):417–24. http://dx.doi.org/10.1016/s0013-7006(04)95456-5
- Tripathi KD. Essentials of medical pharmacology. New Delhi, India: Jaypee Brothers Medical; 2018.
- Ritter J, Flower R, Henderson G, Loke YK, Macewan D, Rang H. Rang and Dale’s. Pharmacology. 2007;
- Barmpalexis P, Grypioti A, Eleftheriadis GK, Fatouros DG. Development of a new aprepitant liquisolid formulation with the aid of artificial neural networks and genetic programming. AAPS PharmSciTech [Internet]. 2018;19(2):741– 52. http://dx.doi.org/10.1208/s12249-017-0893-z
- Chella N, Shastri N, Tadikonda RR. Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan. Acta Pharm Sin B [Internet]. 2012;2(5):502–8. http://dx.doi.org/10.1016/j.apsb.2012.07.005
- Gubbi S, Jarag R. Liquisolid, technology for enhancement of dissolution property of Bromhexine hydrochloride. Res J Pharm Tech. 2009;2(2).
- Baranauskaite J, Kopustinskiene DM, Masteikova R, Gajdziok J, Baranauskas A, Bernatoniene J. Effect of liquid vehicles on the enhancement of rosmarinic acid and carvacrol release from oregano extract liquisolid compacts. Colloids Surf A Physicochem Eng Asp [Internet]. 2018;539:280–90. http://dx.doi.org/10.1016/j.colsurfa.2017.12.034
- Vraníková B, Pavloková S, Gajdziok J. Experimental design for determination of effects of superdisintegrant combinations on liquisolid system properties. J Pharm Sci [Internet]. 2017;106(3):817–25. http://dx.doi.org/10.1016/j.xphs.2016.11.002
- Elkordy AA, Essa EA, Dhuppad S, Jammigumpula P. Liquisolid technique to enhance and to sustain griseofulvin dissolution: effect of choice of non-volatile liquid vehicles. Int J Pharm [Internet]. 2012;434(1–2):122–32. http://dx.doi.org/10.1016/j.ijpharm.2012.05.072
- Kamalakanan V, Karthikraja M, Karthikeyan M, Arul K, Pushpalatha R. Page 73 Bibliography [12:11 AM, 4/23/2020] @appi #VSR: Formulation of tinidazole liquisolid tablets and invitro evaluation. (4AD). Int J Bio Pham Res. 2012;3(4):597–604.
- Narasimha RJV. Formulation and evaluation of nicardipine liquisolid compacts tablets. Formulation and Evaluation of Nicardipine Liquisolid Compacts Tablets. 2016;7:186–93.
- Chamsai B, Sriamornsak P. Novel disintegrating microcrystalline cellulose pellets with improved drug dissolution performance. Powder Technol [Internet]. 2013;233:278–85. http://dx.doi.org/10.1016/j.powtec.2012.08.019
- Elsay KM, Fetouh SA. Formulation and evaluation of rofecoxib liquisolid tablet. Int J Pharm Sci Rev Res. 2010;28(1).
- Sabale PM, Grampurohit ND, Gaikawad DD, Gadhave MV, Shingade GM, Shaik G. Liquisolid technique for enhancement of dissolution properties of fenofibrate. Int JPharm Sci Res. 2015;(5).
- Barzegar-Jalali M, Valizadeh H, Shadbad M-RS, Adibkia K, Mohammadi G, Farahani A, et al. Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide). Powder Technol [Internet]. 2010;197(3):150–8. http://dx.doi.org/10.1016/j.powtec.2009.09.008
Yıl 2023,
Cilt: 27 Sayı: 2, 811 - 824, 27.06.2025
Öz
Kaynakça
- Bary A-E, Louis A. Polmesartan medoxomil surface solid dispersion-based orodispersible tablets: formulation and in vitro characterization. Journal of Drug Delivery Science and Technology [Internet]. 2014;24(6):665– 72.http://dx.doi.org/10.1016/s1773-2247(14)50134-7
- Amidon GL, Lennernäs 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 [Internet]. 1995;12(3):413–20. http://dx.doi.org/10.1023/a:1016212804288
- Douroumis DD, Gryczke A, Schminke S. Development and evaluation of cetirizine hcl taste masked oral disintegrating tablets. AAPS PharmSciTech. 2011;(1).https://doi.org/10.1208/s12249-010-9569-7
- Hirani JJ, Rathod DA, Vadalia KR. Orally disintegrating tablets: A review. Trop J Pharm Res [Internet]. 2009;8(2). http://dx.doi.org/10.4314/tjpr.v8i2.44525
- Olmez SS, Vural I. Advantages and quality control of disintegrating tablets. Fabad J Pharm Sci. 2009;34(1).
- Spireas S. Liquisolid system and method of preparing same. U S Patent. 2002;6423339B – 6423340.
- Spireas, Spiridon, Bolton, Sanford M. Liquisolid systems and methods of preparing same. U S Patent.1999;5,968,550.
- Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm [Internet]. 2009;73(3):373–84. http://dx.doi.org/10.1016/j.ejpb.2009.08.002
- Sanjay PD, Deepak M. Liquisolid technology: Technique for formulation with enhanced bioavailability. World J Pharma Pharma Sci. 2013;3(1).
- Vranikova B, Pavlokova S, Gajdziok J. Experimental design for determination of effect of Super disintegrant combination on liquisolid system properties. J Pharm Sci. 2016;13:1–1.
- Vacheron-Trystram M-N, Braitman A, Cheref S, Auffray L. Antipsychotics in bipolar disorders. Encephale [Internet]. 2004;30(5):417–24. http://dx.doi.org/10.1016/s0013-7006(04)95456-5
- Tripathi KD. Essentials of medical pharmacology. New Delhi, India: Jaypee Brothers Medical; 2018.
- Ritter J, Flower R, Henderson G, Loke YK, Macewan D, Rang H. Rang and Dale’s. Pharmacology. 2007;
- Barmpalexis P, Grypioti A, Eleftheriadis GK, Fatouros DG. Development of a new aprepitant liquisolid formulation with the aid of artificial neural networks and genetic programming. AAPS PharmSciTech [Internet]. 2018;19(2):741– 52. http://dx.doi.org/10.1208/s12249-017-0893-z
- Chella N, Shastri N, Tadikonda RR. Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan. Acta Pharm Sin B [Internet]. 2012;2(5):502–8. http://dx.doi.org/10.1016/j.apsb.2012.07.005
- Gubbi S, Jarag R. Liquisolid, technology for enhancement of dissolution property of Bromhexine hydrochloride. Res J Pharm Tech. 2009;2(2).
- Baranauskaite J, Kopustinskiene DM, Masteikova R, Gajdziok J, Baranauskas A, Bernatoniene J. Effect of liquid vehicles on the enhancement of rosmarinic acid and carvacrol release from oregano extract liquisolid compacts. Colloids Surf A Physicochem Eng Asp [Internet]. 2018;539:280–90. http://dx.doi.org/10.1016/j.colsurfa.2017.12.034
- Vraníková B, Pavloková S, Gajdziok J. Experimental design for determination of effects of superdisintegrant combinations on liquisolid system properties. J Pharm Sci [Internet]. 2017;106(3):817–25. http://dx.doi.org/10.1016/j.xphs.2016.11.002
- Elkordy AA, Essa EA, Dhuppad S, Jammigumpula P. Liquisolid technique to enhance and to sustain griseofulvin dissolution: effect of choice of non-volatile liquid vehicles. Int J Pharm [Internet]. 2012;434(1–2):122–32. http://dx.doi.org/10.1016/j.ijpharm.2012.05.072
- Kamalakanan V, Karthikraja M, Karthikeyan M, Arul K, Pushpalatha R. Page 73 Bibliography [12:11 AM, 4/23/2020] @appi #VSR: Formulation of tinidazole liquisolid tablets and invitro evaluation. (4AD). Int J Bio Pham Res. 2012;3(4):597–604.
- Narasimha RJV. Formulation and evaluation of nicardipine liquisolid compacts tablets. Formulation and Evaluation of Nicardipine Liquisolid Compacts Tablets. 2016;7:186–93.
- Chamsai B, Sriamornsak P. Novel disintegrating microcrystalline cellulose pellets with improved drug dissolution performance. Powder Technol [Internet]. 2013;233:278–85. http://dx.doi.org/10.1016/j.powtec.2012.08.019
- Elsay KM, Fetouh SA. Formulation and evaluation of rofecoxib liquisolid tablet. Int J Pharm Sci Rev Res. 2010;28(1).
- Sabale PM, Grampurohit ND, Gaikawad DD, Gadhave MV, Shingade GM, Shaik G. Liquisolid technique for enhancement of dissolution properties of fenofibrate. Int JPharm Sci Res. 2015;(5).
- Barzegar-Jalali M, Valizadeh H, Shadbad M-RS, Adibkia K, Mohammadi G, Farahani A, et al. Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide). Powder Technol [Internet]. 2010;197(3):150–8. http://dx.doi.org/10.1016/j.powtec.2009.09.008
Toplam 25 adet kaynakça vardır.
Ayrıntılar
| Birincil Dil | İngilizce |
|---|---|
| Konular | Eczacılık ve İlaç Bilimleri (Diğer) |
| Bölüm | Articles |
| Yazarlar | |
| Yayımlanma Tarihi | 27 Haziran 2025 |
| Yayımlandığı Sayı | Yıl 2023 Cilt: 27 Sayı: 2 |