Formulation and Process Optimization of Solid Dispersion of Meloxicam and PEG8000 Prepared by Spray Drying

Author(s):  
Patel R.P. ◽  
Patel M. P. ◽  
Suthar A. M. ◽  
Baria A.H.

The poor solubility and wettability of meloxicam leads to poor dissolution and hence shows poor bioavailability. The present study is aimed at increasing solubility of drug using solid dispersion technique. The solid binary systems were prepared using different drug: polymer ratio (1:1, 1:5 and 1:10) with polyethylene glycol 8000 by different techniques like physical mixing, melting method and spray drying method. The formulations were characterized by differential scanning colorimetry, scanning electron microscopy and in vitro dissolution rate studies. The solubility of drug increased linearly with the increase in polymer concentration. The solid dispersion of drug prepared by spray drying method demonstrated higher drug dissolution rates in comparison to solid dispersion prepared by physical mixtures, melting method and pure meloxicam. Moreover, spray drying process parameters inlet air temperature and feed rate were also optimized to obtain maximum powder yield and satisfactory particle size and compressibility. The outcome indicated that with the increase in feed rate, the powder yield and Carr’s index decreases but particle size increases. On the other hand, as the inlet temperature increases, powder yield and Carr’s index increases.

2019 ◽  
Vol 9 (2) ◽  
pp. 228 ◽  
Author(s):  
Pingxu Chen ◽  
Nanbiao Ye ◽  
Chaoxiong He ◽  
Lei Tang ◽  
Shuliang Li ◽  
...  

Polyacrylate microspheres with a hollow structure were prepared by a facile spray drying method. The effects of spray drying process parameters, including inlet temperature, atomizer rotational speed, and feed speed, on the particle size, bulk density, and morphology of the resultant polyacrylate hollow microspheres were investigated and discussed. The mechanism for the formation of the polyacrylate hollow microspheres was proposed. This facile and scalable method for preparing hollow polymer microspheres is expected to be valuable to prepare various polymer hollow structures for widespread application.


Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Eun-Sol Ha ◽  
Du Hyung Choi ◽  
In-hwan Baek ◽  
Heejun Park ◽  
Min-Soo Kim

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.


2004 ◽  
Vol 141 (3) ◽  
pp. 187-195 ◽  
Author(s):  
Hirofumi Takeuchi ◽  
Shinsuke Nagira ◽  
Hiromitsu Yamamoto ◽  
Yoshiaki Kawashima

2021 ◽  
Vol 02 ◽  
Author(s):  
Thanh V. Ngo ◽  
Christopher J. Scarlett ◽  
Michael C. Bowyer ◽  
Rebecca McCullum ◽  
Quan V. Vuong

Background: S. chinensis extract contains bioactive compounds, which exhibit high antioxidant activities. However, for commercial uses, it is necessary to encapsulate the extract to protect it from degradation. Objective: This study aimed to optimise spray-drying conditions and then compare with freeze-drying to identify the most suitable conditions for encapsulation of Salacia chinensis L. root extract. Method: Three factors of spray-drying encapsulation, including maltodextrin concentration, inlet temperature and feed rate, have been tested for the impacts on the physical and phytochemical properties of S. chinensis root extract. Based on the optimal conditions, the spray-drying was then compared with freeze-drying. Results: The results showed that maltodextrin concentration, inlet temperature and feed rate had significant impacts on recovery yield, phenolics, mangiferin and antioxidant activity of the spray-dried extract. The optimal spray-drying encapsulation conditions were maltodextrin concentration of 20 %, inlet temperature of 130ºC and feed rate of 9 mL/min. Under these optimal conditions, the encapsulated extract had comparable solubility, total phenolics, mangiferin, and antioxidant activity, lower bulk density, moisture content, and water activity as compared to encapsulated extract made using the freeze-drying technique. These optimal spray-drying conditions are recommended to encapsulate the extract of S. chinensis root. Conclusion: Spray-drying was found to be more effective for encapsulation of S. chinensis root extract than freeze-drying. Therefore, spray-drying is recommended for further applications.


Author(s):  
Sejal Patel ◽  
Anita P. Patel

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.


Author(s):  
Amir A. Shaikh ◽  
Praveen D. Chaudhari ◽  
Sagar S. Holkar

<p><strong>Objective: </strong>The objective of the present investigation was to prepare and characterize Etodolac (ETO), Polyvinyl pyrrolidone K30 (PVP K30) and Hydroxypropyl β-cyclodextrin (HPB) ternary system in order to study the effect of complexation on solubility of ETO.</p><p><strong>Methods: </strong>Physical mixtures of a drug and polymers in different weight ratios (1:1, 1:2, 1:4) were prepared to study the effect of individual polymers on solubility of ETO. Spray drying method was used to investigate the combined effect of PVP K30 and HPB on saturation solubility (SS), Dissolution efficiency (DE) and mean dissolution time (MDT) of ETO. Design of experiment (DoE) was used for preparation and optimization of ternary system. Drug polymer interactions were analyzed with Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), Xray diffraction (XRD) and particle size analysis.<strong></strong></p><p><strong>Results: </strong>Results of solubility study suggested that there was significant increase in solubility of ETO with increase in the concentration of PVP K30, Polyvinyl pyrrolidone K 90 (PVP K90) and HPB (*p&lt;0.05). This might be due to the solubilizing effect of PVP K30, PVPK90 and complex formation of ETO with HPB. Various combinations of PVP K30 and HPB prepared using DoE approach by spray drying method showed greater solubility of ETO than its physical mixtures (*p&lt;0.05). Results of FTIR, DSC, SEM, XRD and particle size analysis revealed the interaction between ETO, PVP K30 and HPB. This suggested formation of amorphous ternary system with mean particle diameter in the range of 763±1.35 nm.</p><p><strong>Conclusion: </strong>Combine use of PVP K30 and HPB with DoE approach was an effective tool for formulating ternary system of ETO.</p>


2007 ◽  
Vol 544-545 ◽  
pp. 733-736
Author(s):  
Moon Kwan Choi ◽  
Jin Sang Cho ◽  
Sung Min Joo ◽  
Jin Koo Park ◽  
Ji Whan Ahn ◽  
...  

The purpose of this work is to influence of CaO concentrations of 5.0 wt.% and 10.0 wt.%, slurry feeding rate of 200~400 /min, rotating rate of drum of 5,000 and 10,000 rpm, inlet and outlet temperature on the synthesis of Ca(OH)2 powder, and the synthesis of precipitated calcium carbonate by carbonation process using Ca(OH)2 prepared by spray drying method. As the feeding rate of slurry was increased, the particle size of Ca(OH)2 was decreased. Regardless of rotating rate of drum, when the concentration of CaO was 5.0 wt.% and 10.0 wt.%, the morphology of Ca(OH)2 showed spherical shape of 10~30 μm and 20~60 μm, respectively. The specific surface area of synthesized Ca(OH)2 was 27~30 m2/g. When the initial reaction temperature was 11 °C and 30 °C, the shape and particle size of precipitated calcium carbonate synthesized in the carbonation process showed the rectangular shape of 0.1~0.4 μm and the spindle shape of 0.5~1.0 μm, respectively.


Author(s):  
Pavani S ◽  
Mounika K ◽  
Naresh K

The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.


2013 ◽  
Vol 16 (1) ◽  
pp. 15-25
Author(s):  
Tuyen Thi Phuong Dao ◽  
Nhan Ngoc Thanh Le ◽  
Anh Tuan Nguyen ◽  
Khai Tan Tran ◽  
Dam Duy Le ◽  
...  

The purpose of this study is to i) fabricate a biodegradable nanoparticle formulation of Ketoprofen, ii) evaluate its characteristics, iii) investigate its in vitro dissolution and in vivo pharmaceutical property. The nanoparticle formulation was prepared by spray drying method using Eudragit L100 as the matrix polymer. Size and morphology of drug-loaded nanoparticles were characterized with the electron microscopes (TEM, SEM). These successfully prepared nanoparticles by spray drying method are spherical in shape and quite homologous with diameter size of 100 – 200 nm. The in vitro dissolution studies were conducted at pH 1.2 and 7.4. The results indicated that there is a significant increase in Keto concentration at pH 7.4 compared to pH 1.2. For the in vivo assessment, our Keto-loaded nanoparticles and referential Profenid were administered by oral gavages to rabbits. The results implied that Keto-loadednanoparticles remarkably increased AUC compared to Profenid.


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