scholarly journals Particle design of tolbutamide by the spherical crystallization technique. II. Factors causing polymorphism of tolbutamide spherical agglomerates.

1989 ◽  
Vol 37 (8) ◽  
pp. 2183-2187 ◽  
Author(s):  
Akimitsu SANO ◽  
Takeo KURIKI ◽  
Yoshiaki KAWASHIMA ◽  
Hirofumi TAKEUCHI ◽  
Toshiyuki NIWA
1991 ◽  
Vol 28 (3) ◽  
pp. 172-176
Author(s):  
Akimitsu SANO ◽  
Takeo KURIKI ◽  
Yoshiaki KAWASHIMA ◽  
Hirofumi TAKEUCHI ◽  
Tomoaki HINO ◽  
...  

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 32-39
Author(s):  
D. B Tandel ◽  
◽  
P. A Shah ◽  
K. G. Patel ◽  
M. C Gohel ◽  
...  

The present study was carried out with an aim to improve dissolution rate of febuxostat (FBX, BCSclass II) drug. Spherical agglomerates were prepared by hybrid technique of spherical crystallization and solid dispersion using different ratios of FBX and polymer (PVP K30, HPMC E3LV and chitosan). Drug excipient compatibility study was evaluated by Fourier transform infrared spectroscopy and X-ray diffractometry. Scanning electron microscopy was used for measurement of size of agglomerate. In vitro dissolution study of prepared spherical agglomerates was compared with untreated FBX and marketed formulation in phosphate buffer pH 6.8. The ratio of drug to polymer also affected the drug dissolution results. Drug excipient compatibility study showed no interaction between FBX and PVP K30 (1:5) polymer. The use of PVP K30 (1:5) resulted in partial amorphization and improved drug dissolution. Direct compression method can be adopted in manufacturing to simplify the validation efforts. The performance of the formulated product was superior to the marketed product in the in vitro dissolution test.


RSC Advances ◽  
2016 ◽  
Vol 6 (7) ◽  
pp. 5466-5473 ◽  
Author(s):  
Andrea F. Kardos ◽  
Judit Tóth ◽  
László Trif ◽  
János Gyenis ◽  
Tivadar Feczkó

Spherical crystallization proved to be feasible for the preparation of spherical salt hydrate particles as core material for microencapsulation.


Crystals ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 53 ◽  
Author(s):  
Ji-Hun An ◽  
Alice Nguvoko Kiyonga ◽  
Eun Hee Lee ◽  
Kiwon Jung

Clopidogrel bisulfate (CLP) form-I crystals are irregular, rectangular-shaped crystals. Because of their poor compressibility, flowability and their strong surface tension, manufacturers apply spherical crystallization methods to produce CLP form-I spherical agglomerates with a uniform particle size distribution. Consequently, manufacturers primarily synthesize CLP form-I crystal salts utilizing very complex methods, which produces form-I spherical agglomerates by means of spherical crystallization. In this study, spherical crystals of CLP Form-I were directly prepared from CLP Form-II, the most stable polymorph at room temperature, by using ethanol as solvent and a mixture of isopropyl alcohol (IPA)/n-Hexane (Hex) as an anti-solvent. To provide systematic inputs for the development of spherical agglomerates of optimal morphology, size, particle size distribution (PSD), and polymorphic form, processing parameters such as anti-solvent type, a mixture of IPA/Hex, pure Hex, or pure acetone; stirring speeds of 500, 600, 700, or 800 rpm; and temperatures ranging from 25 to 40 °C were explored. The effects of these parameters on spherical crystallization and polymorphic form were studied in terms of supersaturation, a driving force for polymorphic transformation, and the crystallization solution. Notably, our method does not require a large volume of anti-solvent which is the main complication of conventional anti-solvent crystallization methods.


Author(s):  
N B Bhagat ◽  
A V Yadav ◽  
P R Mastud ◽  
R A Khutale

In this article we describe the optimizing parameters in the process of spherical crystallisation. Particle engineering of active pharmaceutical agents is an innovative area of research in pharmaceutical industry because of several advantages. Spherical crystallization is one of the particle engineering technique in which drug directly gets crystallized and agglomerated into spherical shape. The spherical crystals can be obtained by different methods like solvent change, Quasi-emulsion droplet, ammonia diffusion and neutralisation. The optimization of process of spherical crystallization is important for obtaining the ideal spherical crystal agglomerates. It includes stirring rate, selection of solvent, pH, temperature etc. which affects on the physico-chemical properties of crystals. These optimizing parameters play its specific role in formation of spherical crystals. Stirring rate affects the shape as well as size of the final agglomerates and solvent selection helps in the formation of maximum amount of agglomerates in the system. The factors like pH and temperature should be maintained in case of drugs which show polymorphism. Apart from this, several others physical phenomenon or parameters like interfacial tension and rate of crystallisation are also important for thorough optimization of process.  


2017 ◽  
Vol 17 (9) ◽  
pp. 4776-4784 ◽  
Author(s):  
Ramon Peña ◽  
Joseph A. Oliva ◽  
Christopher L. Burcham ◽  
Daniel J. Jarmer ◽  
Zoltan K. Nagy

Author(s):  
Zhengdong Zhang ◽  
Liping Wang ◽  
Pei Zhao ◽  
Yuntian Xiao ◽  
Hongxun Hao ◽  
...  

Author(s):  
Yousef Javadzadeh ◽  
Zhila Vazifehasl ◽  
Solmaz Maleki Dizaj ◽  
Masumeh Mokhtarpour

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