Rice granules with improved solubility prepared via fluidised-bed granulation

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Hye-Mi Park ◽  
Dae-Hoon Lee ◽  
Jung-Min Kim ◽  
Joo-Heon Hong ◽  
Jun-Hyeon Cho ◽  
...  

AbstractThe purpose of this study was to improve the processability of rice powder using fluidised-bed granulation technology. Bukkyungmi-rice granules were prepared by fluidised-bed granulation for 1 and 2 h using water, 5% lactose (w/v) and 5% dextrin (w/v) solutions as dispersants. The particle size of Bukkyungmi-rice granules increased from 574.83 to 728.07 μm. Granules were produced due to pore formation, and the produced particles could be dispersed easily without any entanglement. The water solubility of the produced rice granules is 1.91–6.74%, which reflects the improvement in their quality with increased treatment time. In particular, Bukkyungmi-rice granules processed in 5% dextrin showed excellent settleability. The enthalpy (ΔH) was found to be the highest for Bukkyungmi-rice granules processed in 5% dextrin for 2 h by differential scanning calorimetry. The results indicated that rice granules obtained by fluidised-bed granulation could be used in various types of rice-based foods.

Author(s):  
Hariyanti Hariyanti ◽  
Sophi Damayanti ◽  
Sasanti Tarini

Sinkonin praktis tidak larut dalam air, sedikit larut dalam kloroform dan alkohol. Hal ini berdampak pada rendahnya penetrasi transfollicular sinkonin, karena hanya bahan aktif hidrofilik yang mampu melewati hair follicle. Dengan demikian dibutuhkan satu sistem penghantaran yang mampu menurunkan hidrofobisitas sinkonin untuk meningkatkan penetrasi sinkonin ke follicle. Niosom merupakan vesikel ampifilik dengan struktur lapisan rangkap yang terbentuk dari hidrasi kombinasi surfaktan nonionik dan kolesterol yang mampu menurunkan hidrofobisitas sinkonin. Penelitian ini bertujuan untuk menentukan proses pembuatan niosom sinkonin yang optimum. Pembuatan niosom sinkonin diawali dengan menentukan temperatur gelasi (Tg) dari span 60 dengan Differential Scanning Calorimetry (DSC), kemudian dilanjutkan dengan optimasi proses meliputi: optimasi kecepatan rotavapor pembentukan film lapis tipis, temperatur hidrasi, kecepatan rotavapor hidrasi, waktu hidrasi, dan waktu sonikasi. Karakteristik vesikel niosom yang optimal meliputi: ukuran partikel dan indeks polidispersitas dengan menggunakan Particle Size Analized (PSA) serta efisiensi penjeratan sinkonin dengan menggunakan KCKT. Temperatur gelasi (Tg) span 60 45±2 oC, kecepatan rotavapor pembentukan film lapis tipis niosom 210 rpm, temperatur hidrasi 55±2 oC, kecepatan rotavapor hidrasi 210 rpm, waktu hidrasi 20 menit, waktu sonikasi suspensi niosom 1 menit. Ukuran vesikel yang diperoleh adalah 100–200 nm, indeks polidispersitas 0,2–0,4 dan efisiensi penjeratan niosom sinkonin 84,49±0,0025%. Proses pembuatan niosom sinkonin memiliki pengaruh besar terhadap hasil ukuran vesikel dan efisiensi penjeratan niosom sinkonin.


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.


Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 421
Author(s):  
Yao Yu ◽  
Yang Tian ◽  
Hui Zhang ◽  
Qingxian Jia ◽  
Xuejun Chen ◽  
...  

Meloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals with three different particle sizes to improve solubility and compare the differences between various particle sizes. The nanocrystal particle sizes were studied through dynamic light scattering (DLS) and laser scattering (LS). Transmission electron microscopy (TEM) was used to characterize the morphology of nanocrystals. The sizes of meloxicam-nanocrystals-A (MLX-NCs-A), meloxicam-nanocrystals-B (MLX-NCs-B), and meloxicam-nanocrystals-C (MLX-NCs-C) were 3.262 ± 0.016 μm, 460.2 ± 9.5 nm, and 204.9 ± 2.8 nm, respectively. Molecular simulation was used to explore the distribution and interaction energy of MLX molecules and stabilizer molecules in water. The results of differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) proved that the crystalline state did not change in the preparation process. Transport studies of the Caco-2 cell model indicated that the cumulative degree of transport would increase as the particle size decreased. Additionally, plasma concentration–time curves showed that the AUC0–∞ of MLX-NCs-C were 3.58- and 2.92-fold greater than those of MLX-NCs-A and MLX-NCs-B, respectively. These results indicate that preparing MLX in nanocrystals can effectively improve the bioavailability, and the particle size of nanocrystals is an important factor in transmission and absorption.


Author(s):  
S. Princely ◽  
Saleem Basha N ◽  
Saleem Basha N ◽  
Nandhakumar S ◽  
Dhanaraju Md

ABSTRACTObjective: Lamivudine (LVD) is a nucleoside reverse transcriptase inhibitor originally developed as an antiretroviral drug and primarily used in thetreatment of most common chronic disease of the planet, acquired immune deficiency syndrome and hepatitis B. The main objective of the study is todevelop controlled drug delivery system to increase the efficacy of antiretroviral drug, LVD against human immunodeficiency virus infections.Methods: The microencapsulation of LVD in gelatin microspheres was carried out by cross-linking process with glutaraldehyde saturated tolueneusing ionic-gelation method. The prepared microspheres were evaluated for particle size analysis, % yield value, % drug content, drug entrapmentefficiency, scanning electron microscopy for surface morphology, swelling index, accelerated stability studies, Fourier transform infrared radiationspectroscopy (FT-IR) and differential scanning calorimetry (DSC) for polymer drug compatibility, in vitro dissolution efficiency and release kineticstudies.Results: The obtained microspheres showed very smooth surface and exhibited regular spherical geometry due to higher crosslinking density. FT-IRand DSC revealed the absence of drug polymer interactions. The percentage yield, entrapment efficiency and drug content for F6 LVD microsphereswas found to be 79.31%, 65.55% and 96.25% respectively. The particle size was ranged from 34.61% to 51.45 µm sizes and in vitro release profileshowed that cross-linking density of gelatin microspheres effectively controlled the release of LVD.Conclusion: The findings of our investigation demonstrated that F6 of gelatin-LVD microspheres had good controlled release profile with maximumentrapment efficiency and prolonged drug release for 24 hrs or longer and this formulation would be capable of overcoming the drawbacks andlimitations of LVD conventional dosage forms.Keywords: Lamivudine, Microspheres, Controlled release, Gelatin, Fourier transform infrared, Differential scanning calorimetry, In vitro releasekinetics.


Author(s):  
Amruta Papdiwal ◽  
Kishor Sagar ◽  
Vishal Pande

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.


Author(s):  
Jaya Prakash Alla ◽  
Nishad Fathima Nishter ◽  
Jonnalagadda Raghava Rao

In the present study we have synthesised thermoresponsive syntan using phase changing material (PCM) encapsulated into a replacement syntan. Syntan was analysed for their particle size, thermal response was verified using Differential scanning calorimetry (DSC) and surface morphology was analysed using scanning electron microscopy (SEM). These syntans were applied to leathers for making leather thermoresponsive. The thermal comfort range achieved on leathers prepared using the experimental syntan was about 2.5℃, compared to control of about 0.5℃ with an error of ±0.5℃. The physical and strength properties of experimental leathers were superior compared to control.


2018 ◽  
Vol 10 (4) ◽  
pp. 133 ◽  
Author(s):  
Shweta Gedam ◽  
Pritee Jadhav ◽  
Swati Talele ◽  
Anil Jadhav

Objective: The present investigation was undertaken to develop and evaluate a gastroretentive mucoadhesive microspheres of anti-osteoporosis drug risedronate sodium to enhance the residence time and drug release by studying the effect of the crosslinking agent to obtain the best formulation with reduced particle size and good in vitro mucoadhesion strength.Methods: Selected drug risedronate sodium is a potent pyridinyl bisphosphonate used for the treatment of osteoporosis, and other bone disorders. Microspheres using sodium alginate as a polymer and calcium chloride solution as a cross-linker were prepared successfully by the emulsification crosslinking method. The 23 factorial design was used to study the effects of various variables like a drug: polymer ratio, crosslinking agent concentration and crosslinking time on the particle size and in vitro mucoadhesion strength. All these formulations were evaluated for entrapment efficiency, percentage yield and cumulative drug release. F1 batch was selected as best formulation and evaluated for scanning electron microscopy, fourier transforms infrared spectroscopy, differential scanning calorimetry, stability study.Results: Design batches were evaluated for percent yield (61.29-89.33%), % entrapment efficiency (42.25±0.620-62.58±0.330), mucoadhesion strength (68.15±0.37-82.24±0.72%) and drug release at 12 h (67-84%). Among the microspheres formulation, an F1 batch of (0.5:1) drug: polymer concentration and at 4% concentration of calcium chloride as a crosslinker was considered best formulation with reduced particle size 32.85±0.774μm, % intro mucoadhesion. 82.24±0.72. In vitro mucoadhesion strength was increased with the increasing crosslinking time from 5 min to 10 min. The fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) study showed no interaction between drug and polymer. X-ray diffraction (XRD) spectrum of microspheres indicates that drug particles are dispersed at the molecular level in the polymer matrices so no indication of the crystalline nature of the drug nature. Scanning electron microscopic (SEM) study showed that microspheres were spherical in shape with a smooth surface. F1 batch shows percentage cumulative drug release 84.07%. In vitro dissolution studies indicates that percent cumulative drug release from microspheres follows zero order kinetics plot which indicates controlled-release drug-delivery for 12 h which leads to control of plasma concentration.Conclusion: The results show that the formulation that contains (0.5:1) drug: polymer ratio, calcium chloride in 4% concentration and crosslinking time 10 min is the best one and can be utilized to formulate risedronate sodium mucoadhesive microspheres to enhance gastric residence time, improved patient compliance and reduction in the frequency of drug administration.


e-Polymers ◽  
2014 ◽  
Vol 14 (5) ◽  
pp. 363-372 ◽  
Author(s):  
Shamim Zargham ◽  
Saeed Bazgir ◽  
Ali Asghar Katbab ◽  
Abosaeed Rashidi

AbstractElectrospun polyacrylonitrile (PAN) nanofibers were impregnated with KMnO4 under varying conditions of concentration and time. The morphological structures, chemical and thermal properties were studied by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The original and preoxidized samples were stabilized and carbonized for characterization with SEM and FTIR. The coloration, weight gain and solubility in N,N-dimethylformamide were also evaluated. A clear peak at 2340 cm-1 corresponding to MnO4–C=N conjugation, together with a wide peak at 1650 cm-1, was revealed in the FTIR spectrum of the preoxidized samples. Based on the DSC results, the cyclization reactions in the preoxidized samples were accelerated by initiating the exothermic reaction at lower temperatures. The modified samples had higher reaction times and ΔH values, broad exotherms, lower initial induction time and lower Ti values than the untreated ones.


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