Facile Preparation of Polylactic Acid/Ketoconazole Composite Microspheres by Oil/Water Solvent Evaporation Method

2013 ◽  
Vol 652-654 ◽  
pp. 335-338 ◽  
Author(s):  
Yan Hong Zhang ◽  
Yan Wang ◽  
Xian Chao Kong ◽  
Qian Ke Cheng ◽  
Xi Yuan Yang ◽  
...  

In this study, polylactic acid(PLA)/ketoconazole(KCZ) composite microspheres were prepared by oil/water solvent evaporation method. Those drug-loaded microspheres were characterized in morphology using the scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FT-IR) was used to determine the chemical functional groups in the sample and to analysis whether a chemical reaction occured between PLA and KCZ. The thermogravimetric spectra of PLA and PLA/KCZ microspheres were used to analyse the influence of KCZ on the thermal decomposition mechanism of PLA. Crystallinities of the KCZ and PLA/KCZ were analyzed by X-ray diffraction analysis (XRD).

2019 ◽  
Vol 9 (01) ◽  
pp. 21-26
Author(s):  
Arif Budiman ◽  
Ayu Apriliani ◽  
Tazyinul Qoriah ◽  
Sandra Megantara

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture


2011 ◽  
Vol 236-238 ◽  
pp. 2264-2272
Author(s):  
Guang Fa Wang ◽  
Chun Lan Dai ◽  
Zheng Gen Liao ◽  
Guo Wei Zhao ◽  
Xin Li Liang ◽  
...  

Solid dispersions (SD) were prepared with naringenin and mannitol by the solvent evaporation method with three drying methods (vacuum drying, VD; microwave-vacuum drying, MVD; and spray drying, SPD). The SD was characterized by Differential Scanning Calorimetry (DSC), Powder X-ray Diffractometry (PXRD), Scanning Electronic Microscope (SEM), and Fourier Transform Infrared Spectroscopy (FT-IR).In vitrodissolution of naringenin and physical stability was investigated, and the energy consumption of different processing methods was measured. The results showed that the vitro dissolution rate and extent of naringenin was significantly improved by SD prepared with different drying methods compared to that of the pure drug and physical mixture (PM), and the dissolution rate of SD-SPD and SD-MVD was much higher than the SD-VD. The results of FT-IR showed that naringenin is possibly interacted with mannitol via intermolecular hydrogen bond; The PXRD showed that the crystallinity of the SD prepared with three drying methods was reduced sharply as compared with pure naringenin and PM. There results showed that the physical state of SD-MVD was more stable than SD-SPD and SD-VD that stored in the 40 °C/75% RH chamber in three month. Compared with other drying methods, the MVD method can save time and energy. These results suggest that MVD is feasible to replace the traditional time-consuming and low efficiency drying procedure for preparation of solid dispersions.


2014 ◽  
Vol 70 (a1) ◽  
pp. C658-C658
Author(s):  
Hong-Liang Lin ◽  
Tieh-Kang Wu ◽  
Yu-Ting Huang ◽  
Shan-Yang Lin

A possible cocrystal formation between metaxalone and short-chain dicarboxylic acids (HOOC-(CH2)n-COOH, n=0-3) was quickly investigated using a solvent-assisted grinding approach. Differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) microspectroscopy, and powder X-ray diffraction (PXRD) were used to verify the cocrystal formation between metaxalone and each dicarboxylic acid. A solvent evaporation method was used to prepare the standard cocrystal. The cocrystal formation was also estimated by using a one-step simultaneous DSC-FTIR microspectroscopy. The present study indicates that only n=2 of short-chain dicarboxylic acids such as succinic acid, fumaric acid and maleic acid could form a cocrystal with metaxalone. Both solvent-assisted grinding technique and solvent evaporation method were successfully applied to prepare the metaxalone cocrystal with n=2 of short-chain dicarboxylic acids. Moreover, this cocrystal formation was also easily screened and estimated using a unique DSC-FTIR microspectroscopy in real time. Acknowledgement This work was supported by National Science Council, Taipei, Taiwan, ROC (NSC 100-2320-B- 264-001-MY3).


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 54-60
Author(s):  
L Adhikari ◽  
M. Semalty ◽  
P. S Naruka ◽  
V. K Aswal ◽  
A Semalty ◽  
...  

Cyclodextrin complexation is a one of the most investigated techniques of solubility and dissolution enhancement of drugs. In the present study, a poorly water soluble drug glimepiride, was complexed with β-cyclodextrin (βCD) with the aim of improving water solubility and drug dissolution. The complexes were prepared using two different methods (solvent evaporation and kneading) and then characterized by Fourier-transform infrared spectroscopy (FT-IR), powder x-ray diffractometry (X-RD), thermal analysis (DSC),scanning electron microscopy and in-vitro dissolution study. The phase solubility study revealed the most suitable ratio of drug to β CD (1:4 molar ratio). Analysis of various physical and pharmacokinetic parameters for the complex prepared by solvent evaporation method showed better drug content, solubility and drug release profile in comparison to the complex prepared by the kneading method. The complex prepared with solvent evaporation method showed better drug release as compared with that of kneading method and the pure drug. The FT-IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:βCD molar ratio) using solvent evaporation method showed the better improvement in solubility and drug dissolution.


2020 ◽  
Vol 21 (3) ◽  
pp. 109
Author(s):  
Agnes Nuniek Winantari ◽  
Roisah Nawatila ◽  
Cecilia Jocelyn

PREPARATION OF ACYCLOVIR-ISONICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION METHOD WITH METHANOL AND ISOPROPANOL. Acyclovir is a nucleoside synthetic analog antiviral group used in the treatment of Herpes simplex virus (HSV-1 & HSV-2) and Varicella zoster virus (VZV). Acyclovir has low water solubility, so it needs to be modified in the form of cocrystal with isonicotinamide. This study aims to obtain the physical characteristics produced by acyclovir-isonicotinamide cocrystal (1:1) made through the solvent evaporation method with methanol and isopropanol. The crystalline formed is characterized by DSC, PXRD, FT-IR and SEM. The characterization results showed the presence of new crystals that formed between acyclovir-isonicotinamide in methanol and isopropanol solvents. Thermograms showed sharp exothermic peaks at 183.31°C and 186.24°C. The diffractogram showed a new peak at 2θ = 5.19 and 5.82. The spectrum showed a shift in wavelength in the cocrystal formed. The cocrystal has a different morphology compared with parent drug and coformer on analysis using SEM. This research shows that acyclovir can form cocrystal with isonicotinamide by solvent evaporation method with methanol and isopropanol.


Author(s):  
Taha A. Basher ◽  
Entidhar J. Muhammad

Itraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients. The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles. Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of   ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula  with composition of  ITZ(200mg), a first coat of HPMC15cps (200mg), a second coat of EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) which prepared by a dual coating solvent evaporation method using a first coat which provides relatively pH-independent solubility, while the second coat applied as a bouncy producing agents. Polyvinyl alcohol (PVA) was used as a surfactant in both cases. The prepared floating microparticles were subjected to various evaluation parameters such as yield percent, drug loading and drug entrapment efficiency (EE), particle size analysis, in- vitro bouncy, drug release, Fourier Transforms Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD) studies.


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