Development and characterization of solid dispersion-microsphere controlled release system for poorly water-soluble drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

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NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

Journal of Medicine and Pharmacy ◽

10.34071/jmp.2012.5.4 ◽

2012 ◽

pp. 31-35

Author(s):

Truong Dinh Thao Tran ◽

Ha Lien Phuong Tran ◽

Nghia Khanh Tran ◽

Van Toi Vo

Keyword(s):

Drug Release ◽

Droplet Size ◽

Solid Dispersion ◽

Water Soluble ◽

Drug Dissolution ◽

Dissolution Enhancement ◽

Particle Size Reduction ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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Loading and Controlled Release of Poorly Water-Soluble Drug Telmisartan from Porous Silicon Microparticles

Silicon ◽

10.1007/s12633-020-00465-7 ◽

2020 ◽

Author(s):

Chetan Sharma ◽

Nalin H. Maniya ◽

Meghal A. Desai ◽

Sanjaykumar R. Patel

Keyword(s):

Controlled Release ◽

Porous Silicon ◽

Water Soluble ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

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Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

Advances in Polymer Technology ◽

10.1155/2020/4239207 ◽

2020 ◽

Vol 2020 ◽

pp. 1-7

Author(s):

Qingyun Zeng ◽

Liquan Ou ◽

Guowei Zhao ◽

Ping Cai ◽

Zhenggen Liao ◽

...

Keyword(s):

Thermal Stability ◽

Molecular Weight ◽

Dissolution Rate ◽

Solid Dispersion ◽

Water Solubility ◽

Water Soluble ◽

Carrier Material ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

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