scholarly journals Physical Characteristics of Cilostazol–Hydroxybenzoic Acid Cocrystals Prepared Using a Spray Drying Method

Crystals ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 313
Author(s):  
Maho Urano ◽  
Megumi Kitahara ◽  
Kae Kishi ◽  
Eiichi Goto ◽  
Tatsuaki Tagami ◽  
...  

The cocrystal formation of pharmaceuticals can improve the various physical properties of drugs, such as solubility, without the need for chemical modification of the drug substances. In the present study, we prepared cocrystals of cilostazol and additive coformers (derivatives of hydroxybenzoic acid) using a spray drying method. Based on the preparation of the cocrystals of cilostazol and the coformers as reported previously, the characteristics of the cilostazol cocrystals prepared using solvent evaporation, slurry, and spray drying methods were compared. The physical characterization revealed that the spray drying method successfully produced cilostazol–4-hydroxybenzoic acid and cilostazol–2,4-dihydroxybenzoic acid cocrystals, whereas samples of cocrystals of cilostazol and 2,5-dihydroxybenzoic acid produced via the spray drying process appeared to contain coformer polymorphs. The dissolution of cilostazol was improved using the spray-dried cocrystal samples composed of coformers compared to samples prepared using cilostazol alone or a physical mixture. The present results provide useful information regarding the manufacture of cilostazol cocrystals and pharmaceutical cocrystals via spray drying in large-batch production.

2020 ◽  
Vol 37 (8) ◽  
Author(s):  
Kimberly B. Shepard ◽  
April M. Dower ◽  
Alyssa M. Ekdahl ◽  
Michael M. Morgen ◽  
John M. Baumann ◽  
...  

Abstract Purpose The purpose of this work is to introduce solvent-assisted secondary drying, a method used to accelerate the residual solvent removal from spray dried materials. Spray-drying is used to manufacture amorphous solid dispersions, which enhance the bioavailability of active pharmaceutical ingredients (APIs) with low aqueous solubility. In the spray-drying process, API and excipients are co-dissolved in a volatile organic solvent, atomized into droplets through a nozzle, and introduced to a drying chamber containing heated nitrogen gas. The product dries rapidly to form a powder, but small amounts of residual solvent (typically, 1 to 10 wt%) remain in the product and must be removed in a secondary-drying process. For some spray-dried materials, secondary drying by traditional techniques can take days and requires balancing stability risks with process time. Methods Spray-dried polymers were secondary dried, comparing the results for three state-of-the-art methods that employed a jacketed, agitated-vessel dryer: (1) vacuum-only drying, (2) water-assisted drying, or (3) methanol-assisted drying. Samples of material were pulled at various time points and analyzed by gas chromatography (GC) and Karl Fischer (KF) titration to track the drying process. Results Model systems were chosen for which secondary drying is slow. For all cases studied, methanol-assisted drying outperformed the vacuum-only and water-assisted drying methods. Conclusions The observation that methanol-assisted drying is more effective than the other drying techniques is consistent with the free-volume theory of solvent diffusion in polymers.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Wasim Akram ◽  
Navneet Garud

Abstract Background Chicory is one of the major source of inulin. In our study, Box–Behnken model/response surface analysis (RSM) was used for the optimization of spray drying process variables to get the maximum inulin yield from chicory (Cichorium intybus L.). For this investigation, the investigational plan utilized three process variables drying temperature (115–125 °C), creep speed (20–24 rpm), and pressure (0.02–0.04 MPa). Result The optimal variables established by applying the Box–Behnken model were as follows: drying temperature 119.20 °C, creep speed 21.64 rpm, and pressure 0.03 MPa. The obtained powdered inulin by spray drying was investigated for the yield value, identification, size, and surface morphology of the particle. The inulin obtained from the spray drying process consists of a fine molecule-sized white powder. Instead, the drying methods shows a significant effect on the morphology and internal configuration of the powdered inulin, as the inulin obtained from spray drying was of a widespread and uniform size and shape, with a rough surface on increase in temperature and smoother surface while increasing the creep speed. The findings indicate that the spray drying with optimum parameters resulted in maximum product yield. Conclusion The outcomes of the study concluded that the product yield through spray drying technique under optimized condition is optimal as compared to other drying technique. Hence, this technique may be applied at commercial scale for the production of inulin.


Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4153
Author(s):  
Doaa Abouelenein ◽  
Ahmed M. Mustafa ◽  
Simone Angeloni ◽  
Germana Borsetta ◽  
Sauro Vittori ◽  
...  

Strawberry is the most consumed berry fruit worldwide due to its unique aroma and flavor. Drying fruits to produce a powder represents one of the possible conservation methods to extend their shelf-life. The aim of the present study was to compare the influence of freezing and different drying methods on the volatile profile of strawberry using the HS-SPME/GC–MS method, in addition to analysis of strawberry jam volatiles. A total of 165 compounds were identified, accounting for 85.03–96.88% of the total volatile compositions. Results and PCA showed that freezing and each drying process affected the volatile profile in a different way, and the most remarkable representative differential volatiles were ethyl hexanoate, hexyl acetate, (E)-2-hexenyl acetate, mesifurane, (E)-nerolidol, γ-decalactone, 1-hexanol, and acetoin. Shade air-dried, frozen, freeze-dried, and oven-dried 45 °C samples retained more of the fruity and sweet aromas of strawberry, representing more than 68% of the total aroma intensity according to the literature. In contrast, the microwave-drying method showed drastic loss of fruity esters. Strawberry jams demonstrated complete destruction of esters and alcohols in most jams, while terpenes were significantly increased. These findings help better understand the aroma of strawberry and provide a guide for the effects of drying, freezing, and jam processing.


Author(s):  
Aliasgar J Kundawala ◽  
Khushbu S Chauhan ◽  
Harsha V Patel ◽  
Swati K Kurtkoti

Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.


Author(s):  
Aleksandra A. Jovanović ◽  
Steva M. Lević ◽  
Vladimir B. Pavlovic ◽  
Smilja B. Markovic ◽  
Rada V. Pjanovic ◽  
...  

Freeze drying was compared with spray drying regarding feasibility to process wild thyme drug in order to obtain dry formulations at laboratory scale starting from liquid extracts produced by different extraction methods: maceration, heat-, ultrasound-, and microwave-assisted extractions. Higher powder yield (based on the dry weight prior to extraction) was achieved by freeze than spray drying and lower loss of total polyphenol content (TPC) and total flavonoid content (TFC) due to the drying process. Gelatin as a coating agent (5% w/w) provided better TPC recovery by 70% in case of lyophilization and higher powder yield in case of spray drying by diminishing material deposition on the wall of the drying chamber. The resulting gelatin-free and gelatin-containing powders carried polyphenols in amount ~190 and 53-75 mg gallic acid equivalents GAE/g of powder, respectively. Microwave-assisted extract formulation distinguished from others by higher content of polyphenols, proteins and sugars, higher bulk density and lower solubility. The type of the drying process affected mainly position of the gelatin-derived -OH and amide bands in FTIR spectra. Spray dried formulations compared to freeze dried expressed higher thermal stability as confirmed by differential scanning calorimetry analysis and higher diffusion coefficient; the last feature can be associated with the lower specific surface area of irregularly shaped freeze-dried particles (151-223 µm) compared to small microspheres (~8 µm) in spray-dried powder.


2020 ◽  
Vol 7 (2) ◽  
pp. 75-83
Author(s):  
Tulsi Gurung ◽  
Karma Wangchuk ◽  
Bishal Sitaula

Farmers in Bhutan practice hot water blanching and sun drying of green chillies as one of the preservation measures. The blanched dried chilli is known as ema shukam locally and is used in preparing various traditional cuisines. Blanching is done for 2-3 minutes by immersing in boiling water and drying in open sun. However, blanching and drying process lead to quality changes such as texture, colour, flavour, and nutritional value. Therefore, this study aimed to determine the proximate compositions of sun dried and oven dried green-blanched chillies. An experiment with two drying methods and two levels of blanching durations with three replications for each treatment were conducted to examine the proximate compositions of the dried and blanched chillies. Blanching duration of two minutes retained higher carbohydrates (x͂ = 31.78) than three minutes (x͂ = 26.08). However, the Mann-Whitney U test showed no significant effect of blanching duration on carbohydrate (U = 7.5, z = - .690, p > .05). Drying methods had significant effect only on fat content with oven drying retaining higher fat content (x͂ = 4) compared to sun drying method (x͂ = 2); (U = 2, z = -2.713, p < .01). Blanching for three minutes resulted in higher loss of Vitamin C content. The colour of oven dried chilli was dark brownish green even at lower temperature of 37 oC. Hot water blanching of green chillies for two minutes followed by sun drying produced desired colour of dried chillies.


Author(s):  
Tran Thi Hai Yen ◽  
Tran Thi Nhu Quynh ◽  
Duong Thi Thuan ◽  
Pham Thi Minh Hue

The aims of study was formulation and evaluation of berberin (BBR) loaded proliposomes by spray-drying method. BBR proliposomes were evaluated for appearance, spray-drying efficiency, morphology and differential scanning calorimetry (DSC). Liposomes, obtained after hydration, were evaluated for particle size, size distribution, morphology and entrapment efficiency. The results showed that BBR proliposomes were prepared by spray-drying method with molar ratio of Hydrogenated soy phosphatidyl choline (HSPC): Sodium deoxycholat (NaDC): vitamin E (vtE): BBR = 7: 1: 6: 6. Mixture of manitol and Aerosil at weight ratio of 97:3 was used as carrier. Results of DSC showed that berberin was dispersed molecularly into proliposomes powder. BBR liposomes, obtained after hydration, had average particle diameter of about 29 μm and entrapment efficiency was 22.23%. Keywords Proliposomes, liposomes, berberin, sodium deoxycholate, spray-dried. References [1] W. Kong, J. Wei, A. Parrveen et al., Berberine is A Novel Cholesterol-Lowering Drug Working Through A Unique Mechanism Distinct From Statins, Nature Medicine, Vol. 10, No. 12, 2004, pp. 1344-1351, https://doi.org/10.1038/nm1135.[2] S. K. Kulkarni, A. Dhir, on The Mechanism of Antidepressant-Like Action of Berberine Chloride, European Journal of Pharmacology, Vol. 589, No. 1-3, 2008, pp. 163-172, https://doi.org/ 10.1016/j.ejphar.2008.05.043.[3] Y. T. Ho, J. S. Yang, T. C. Li et al., Berberine Suppresses in Vitro Migration and Invasion of Human SCC-4 Tongue Squamous Cancer Cells Through the Inhibitions of FAK, IKK, NF-Κb, U-PA and MMP-2 and-9, Cancer Letters, Vol. 279, No. 2, 2009, pp. 155-162, https://doi.org/10.1016/j.canlet.2009.01.033.[4] S. Muneer, Z. Masood, S. Butt et al., Proliposomes as Pharmaceutical Drug Delivery System: A Brief Review, Journal of Nanomedicine and Nanotechnology, Vol. 8, No. 3, 2017, pp. 448-450, https://doi.org/10.4172/2157-7439.1000448.[5] H. K. Omer, N. R. Hussein, A. Ferraz et al., Spray-Dried Proliposome Microparticles for High-Performance Aerosol Delivery Using a Monodose Powder Inhaler, AAPS PharmSciTech, Vol. 19, No. 5, 2018, pp. 2434-2448, https://doi.org/10.1208/s12249-018-1058-4.[6] T. T. H. Yen, T. T. N. Quynh, D. T. Thuan, P. T. M. Hue, Preparation of Berberin Liposomes, Contained Sodium Deoxycholate by Ethanol Injection Method, Journal of Pharmaceutical Research and Drug information, Vol. 11, No. 4, 2020, pp. 11-17 (in Vietnamese). [7] T. T. H. Yen, T. T. Hue, P. T. M. Hue et al., Preparation of Berberin Proliposomes by Film Deposition on Carrier Surface Method, VNU Journal of Science: Medical and Pharmaceutical Sciences, Vol. 36, No. 2, 2020, pp. 9-15, https://doi.org/10.25073/2588-1132/vnumps.4204.[8] R. G. Ahmed, S. Sherif, Z. Zainab et al., Silymarin Spray-Dried Proliposomes: Preparation, Characterization and Cytotoxic Evaluation, Drug Delivery Letters, Vol. 10, No. 1, 2020, pp. 14-23, https://doi.org/10.2174/2210303109666190722114211.[9] A. Bangham, M. M. Standish, J. C. Watkins Diffusion of Univalent Ions Across the Lamellae of Swollen Phospholipids, Journal of Molecular Biology, Vol. 13, No. 1, 1965, pp. 238-252.    


2019 ◽  
Vol 966 ◽  
pp. 19-24
Author(s):  
Srie Muljani ◽  
Heru Setyawan ◽  
Ketut Sumada

The silica potassium humic substance (Si-K-HAs) composite have been produce by spray drying successfully. In the previous study the preparation of Si-K-HAs gel by precipitation method required the addition of acid so that Si-K-HAs gel product contains acid salts. This study was develope spray drying method in order to eliminate the use of acid. The mixture of potassium silicate, cellulose and humic potassium solution was mixed with varying volume ratios and flowed into a spray dryer to produce Si-K-HAs powder. The used of cellulose (CMC) in this study acts as a homogeneous agent so that silica and humic substance can be completely mixed at controlled viscosity. Si-K-HAs products were characterized by Scanning electron microscopy (SEM), X-ray fluorescence (XRF), X-ray diffraction (XRD), Fourier transform infrared spectrometry (FTIR), and Surface area analytical (SAA). The result showed that the Si-K-HAs composite prepared by spray dryers have spherical particles, SiO2 in the range of 48-50%, K2O in the range of 49-50%. The present of cellulose caused the increasing of Si-K-HAs particle size e.g 17.30 μm prepared without CMC to 41.11 μm prepared with addition of 100g of CMC. The presence of cellulose can also increase the surface area of the spray-dried Si-K-HAs particles from 111.92 m2g-1; 163.241 m2g-1.


Foods ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 669
Author(s):  
Karolina Östbring ◽  
Ingegerd Sjöholm ◽  
Marilyn Rayner ◽  
Charlotte Erlanson-Albertsson

Thylakoid membranes isolated from spinach have previously been shown to inhibit lipase/co-lipase and prolong satiety in vivo. There is a need to develop thylakoid products that not only have the desired characteristics and functionality after processing, but also are stable and provide equivalent effect on appetite over the promised shelf life. The aim of the present study was therefore to evaluate how the thylakoid powders’ characteristics and functionality were affected by moisture during storage. Thylakoids produced by drum-drying, spray-drying, and freeze-drying were incubated in controlled atmosphere with different relative humidity (10 RH%, 32 RH%, 48 RH% and 61 RH%) for 8 months. The water content in all powders was increased during storage. The water absorption was moisture-dependent, and the powders were considered hygroscopic. Relative humidity showed a definite influence on the rate of chlorophyll degradation and loss of green color in thylakoid powders after storage which correlated with impaired emulsifying capacity. Spray-dried powder had the overall highest chlorophyll content and emulsifying capacity at all RH-levels investigated. Spray drying was therefore considered the most suitable drying method yielding a powder with best-maintained functionality after storage. The results can be applied towards quality control of high-quality functional foods with appetite suppressing abilities.


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.


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