An approach for solubility enhancement: solid dispersion
Keywords:
Aceclofenac, hydrophilic carrier, Aerosil 200, solvent evaporation methodAbstract
The solubility behavior of drug is one of most challenging aspect in formulation development. Thus a greater understanding of dissolution & absorption behavior of drug with low aqueous solubility is required to successfully formulate them into more soluble and hence bioavailable drug product. Therefore different approaches are being explored to enhance the solubility of poorly water soluble drugs, one of such approach is using solid dispersion by solvent evaporation method. In this study, we are trying to increase the solubility of aceclofenac, poorly water soluble drug with low bioavailability. Objective of this work is to improve the solubility and dissolution rate of poorly water soluble Aceclofenac by solid dispersion method followed by solvent evaporation method. And to compare effectiveness of hydrophilic polymer PVP-k30, HPMC E-5, using porous carrier Aerosil 200. , resultant complexes were evaluated for drug content, infrared spectroscopy, and XRD and dissolution study. The present study successfully utilized the solvent evaporation method for preparation of stable, amorphous solid dispersions of Aceclofenac by encapsulation with hydrophilic carrier with adsorbents agent (Batch 4, 1:1:2) drug: PVPK30: aerosil, showed maximum release in phosphate buffer pH 6.8 The present study demonstrates high potential of solvent evaporation method for obtaining large surface area and amorphicity of drug using hydrophilic carrier
References
obtained by spray drying. Int J Pharm.
;271:281-286.
Van den Mooter G, Wuyts M, Blaton
, Yoo S, Lee S, Kim K, Yoon D,
ageri GV.
S, Yamamoto H,
KA,
E. Solid dispersion
Ambike,1 K. R.
gira, H. Yamamoto,
N, et al. Physical stabilization of
amorphous ketoconazole in solid
dispersions with polyvinylpyrrolidone
K25. Eur J Pharm Sci. 2001;12:261-
Jung J
Lee K. Enhanced solubility and
dissolution rate of itraconazole by a
solid dispersion technique. Int J
Pharm. 1999;187:209-218.
Doshi DH, Ravis WR, Bet
Carbamazepine and polyethylene
glycol solid dispersion preparation,
invitro dissolution, and
characterization. Drug Dev Ind Pharm.
;23:1167-1176.
Takeuchi H, Nagira
Kawashima Y. Solid dispersion
particles of tolbutamide prepared with
fine silica particles by the spray-drying
method. Powder
Technology.2004;141:1187-1195.
Vippagunta SR, Maul
Tallavajhala S, Grant DJW. Solid-state
characterization of nifedipine solid
dispersions. Int J Pharm.
;236:111-123.
Sethia S, Squillante
of carbamazepine in PVP K30 by
conventional solvent evaporation and
supercritical methods. Int J Pharm.
;272:1-10
Anshuman A.
Mahadik,1 and Anant Paradkar, SprayDried Amorphous Solid Dispersions of
Simvastatin, a Low Tg Drug: In Vitro
and in Vivo Evaluations,
Pharmaceutical Research, Vol. 22,
No6,2005,99-998
H. Takeuchi, S. Na
and Y. Kawashima. Solid dispersion
particles of tolbutamide with fine silica
particles by the spray-drying method.
Powder Technol. 141:187-195 (2004).
E. Morefield. Colloidal silicon dioxide.
In A. H. Kibbe (ed.), Handbook of
Pharmaceutical Excipients, 3rd ed. The
Pharma- ceutical Press, London, 2000,
pp. 143-145.
M.monehigini,A.carcano;Studies in
dissolution enhancement of atenolol.Part
I, International Journal of Pharmaceutics
(1998) 177 183
M. M. Patel , D. M. Patel,Fast
Dissolving Valdecoxib Tablets
Containing Solid Dispersion of
Valdecoxib , Indian Journal of
Pharmaceutical Sciences 222
M. V. Margarit, M. T. Marý´n, and M.
D. Contreras, et al; Solubility of Solid
Dispersions of Pizotifen Malate and
Povidone, Drug Development and
Industrial Pharmacy, 27(6), 517–522
(2001)
Dong-Han Won, Min-Soo Kim, Sibeum
Lee, Jeong-Sook Park;et al; Improved
physicochemical characteristics of
felodipine solid dispersion particles by
supercritical anti-solvent precipitation
process, International Journal of
Pharmaceutics 301 (2005) 199–208.
Omaima A. Sammour, Mohammed A.
Hammad, Nagia A.Megrab, et al
;Formulation and Optimization of Mouth
Dissolve Tablets Containing Rofecoxib
Solid Dispersion, AAPS PharmSciTech
; 7 (2),E1-E9.
B N. SUHAGIA ,H M. Patete.,
Preparation and characterization of
etoricoxib-polyethylene glycol 4000 plus
polyvinylpyrrolidone K30 solid
dispersions, Acta Pharm. 56 (2006) 285–
G. P. Bettinetti and P. Mura, Dissolution
properties of naproxen in combinations
with polyvinylpyrrolidone,Drug Dev.
Ind. Pharm. 20 (1994) 1353–1366.