Solid Dispersion Method Research Articles

Solubilty Enhancement of Naproxen Sodium Using Different Carriers by Solid Dispersion

In the existing study an attempt has been made to increase the in vitro dissolution rate of poorly water-soluble drug naproxen, by utilizing novel solid dispersion methods are one of the most auspicious methods to enhance the oral bioavailability of poorly water soluble drug. naproxen sodium formulations were planned out by using melting method or fusion method, and using carrier like PVP-K30 and PEG4000. the formulation were planned out with the above-mentioned carriers in three different drug-carrier (w/w) ratios of 1:1, 1:2 and 1:3. the prepared solid dispersion was subjected for percentage practical yield, drug content, and FTIR studies. absence of significant drug-carrier interaction was confirmed by FTIR data. in-vitro release profiles of all solid dispersions (SD1 to SD6) were analogously evaluated and also studied against pure naproxen sodium. solid dispersion of formulation (SD6) naproxen sodium and PVP-K30 combination planned out in (1:3) ratio showed excellent solubility and the dissolution rate was found to be 98.97% drug release at 24 min was chosen as the absolute best formulation in this study. solubility of naproxen sodium was increased as the concentration of carriers increased.

Development of Effervescent Granules with Solid Dispersion of Furazolidone

Introduction. Treatment of infectious and inflammatory diseases demands active substances (AS), characterized by low resistance of microorganisms, high specificity of the mechanism of action and a wide range of antimicrobial activity. Though furazolidone (FZ) – AS meets these criteria, however, practically insolubility in water significantly limits its use. Use of the solid dispersion method (SD) could increase the solubility and dissolution rate of AS with low water solubility. revious studies indicate an increase in the solubility and dissolution rate of FZ in water from SD with polyvinylpyrrolidone-24 000 (PVP-24 000) in a ratio with AS > 6 : 1 by weight. As a result, it becomes possible to introduce SD FZ into the composition of rapidly dissolving effervescent dosage forms, for example, granules for obtaining solutions for external use for the treatment of infectious and inflammatory diseases.Aim. Development of the composition and technology for producing effervescent granules based on solid dispersions of FZ for obtaining a solution for external use.Materials and methods. FZ substance, polyvinylpyrrolidone-24 000 ± 2000 (PVP-24 000 ± 2000), tartaric acid, malic acid, sodium carbonate anhydrous, ethyl alcohol 96 %, purified water. We provided the granules through fluidized bed granulation. The analysis of the obtained granules included the following parameters: description, granule size, loss in mass on drying, disintegration, uniformity of dosage according to GPМ 1.4.1.0004.15 "Granules". Then followed a qualitative and quantitative determination of AS and analysis of the pH of the aqueous solution of the granules. To study the stability and shelf life of the samples of granules, we laid them to the storage in accordance with GPМ 1.10009.15 "Stability and shelf life of drugs".Results and discussion. We developed he composition and technology of FZ effervescent granules for obtaining a solution for external use. Granules are obtained by separate granulation of the main (containing a SD AS) and acid components, followed by mixing in ratios that provide a solution of FZ with a concentration of 0.004 % in water at room temperature. Later we assessed the quality of the obtained compositions and determined, the shelf life (2 years) and storage conditions (in a dry, dark place at a temperature of 25 °C) of the developed compositions of granules.Conclusion. As a result of technological and chemical-pharmaceutical research using the SD method, we developed a new FZ dosage form – effervescent granules, which makes it possible to obtain an aqueous solution with a concentration of FZ 0.004 % in less than 5 minutes without heating. Based on the results of the work, an application was filed with Rospatent No. 2021105988 dated 10.03.2021, "Fast-dissolving dosage form of furazolidone and a method for its production".

Intranasal delivery of insulin by self-emulsified nanoemulsion system: In vitro and in vivo studies

The main objective of this research was to develop a self-emulsified nanoemulsion (SEN) dosage form of insulin where insulin is loaded into the lipid phase of the nanoemulsion for enhanced absorption through intranasal delivery. When loaded into the lipid droplets (oil phase), insulin can be protected from enzymatic degradation, can penetrate through the mucus gel barrier in a comparatively effective manner and can be absorbed through transcellular permeation along with paracellular route. To incorporate lipophilicity to insulin molecule, Ins-SPC (Soy-L-α-phosphatidylcholine) complex was prepared by solid dispersion method to load insulin into the oil phase. The cytotoxicity of SPC and the developed nanoemulsions was tested on the human nasal epithelial cells in vitro. An optimized formulation with high loading of insulin and low in vitro cytotoxicity was developed and characterized. To predict the absorption of insulin through nasal mucosa in vivo by the nanoemulsion system, the insulin-loaded SEN along with controls was tested for the transport through human nasal epithelial cell monolayer in vitro. The insulin-loaded SEN significantly (p < 0.01) enhanced the permeation of insulin by three times as compared to the insulin solution. The in vivo absorption of insulin after intranasal delivery of the insulin-loaded SEN was evaluated in anesthetized rats. The results show that the Cmax (maximum plasma concentration) and the bioavailability (relative to the subcutaneous delivery) of the insulin-loaded SEN was 255.9 µU/ml and 68 %, respectively, while the intranasal delivery of the insulin solution resulted in only 5.8 µU/ml of Cmax and 5% of relative bioavailability. Intranasal delivery of 3.6 IU/kg insulin-loaded SEN decreased the plasma glucose level remarkably, achieving a maximum reduction of 70%, and the glucose reduction activity lasted for the whole experimental period of 4 h. Histological examination of the nasal mucosa showed no apparent signs of toxicity at the site of administration after single dose of the insulin-loaded SEN. These results demonstrate that the insulin-loaded SEN significantly enhanced insulin absorption through intranasal delivery, indicating that the developed nanoemulsion system offers a favorable approach for intranasal delivery of insulin.

Capsanthin-Loaded Micelles: Preparation, Characterization and in vitro Evaluation of Cytotoxicity Using MDA-MB-231 Breast Cancer Cell Line.

Breast cancer is one of the most common cancers and remains a major cause of morbidity and mortality among women worldwide. In developed countries, breast cancer as a multifactorial disease is a major health concern, and its incidence is constantly rising in low and middle-income countries. Numerous studies have demonstrated that phytochemicals such as carotenoids inhibit breast cancer growth and induce apoptosis. We recently enhanced the solubility of capsanthin in water by encapsulating it in diosgenin polyethylene glycol succinate, a novel non-ionic surfactant. Thus, this study aims to evaluate the cytotoxicity of water-soluble capsanthin-loaded micelles in MDA-MB-231 cells in vitro through tetrazolium dye MTT assay. In the current study, capsanthin, a hydrophobic carotenoid, is extracted from sweet red pepper (Capsicum annuum). Capsanthin-loaded diosgenin polyethylene glycol succinate 1000 (cap-DPGS-1000) micelles were prepared from capsanthin extract (cap) and diosgenin polyethylene glycol succinate 1000 (DPGS-1000) using the solid dispersion method. The capsanthin extract and cap-DPGS-1000 micelles were characterized by UV-visible spectroscopy, high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), particle size distribution, polydispersity, and scanning electron microscopy (SEM). The effects of capsanthin extract and cap-DPGS-1000 micelles on a human triple-negative breast cancer cell line (MDA-MB-231) were tested to check the cell viability, proliferation and cytotoxicity of the micelles. The solubility of encapsulated cap-DPGS-1000 micelles in water is greatly enhanced and leads to an increased scope for localized drug delivery, a better delivery option for treating residual cancerous tumours. The encapsulated capsanthin showed a sustained release in simulated intestinal fluid (pH=6.8). Our research proposes a sustained drug delivery system that ensures effective and controlled release to the affected site. The characterization data revealed no change in the structure and functional groups in the encapsulated capsanthin. The IC50 value of the cap-DPGS-1000 micelles against MDA-MB-231 breast cancer cells was (3.10±1.09) μg/mL, which is much lower than of capsanthin extract ((81.1±1.5) μg/mL). Capsanthin extract and capsanthin-loaded micelles are promising drug candidates to induce apoptosis and increase reactive oxygen species (ROS) in cancer cells. The result shows the cytotoxic effect of capsanthin and capsanthin-loaded micelles on MDA-MB-231 cell line for the first time. Capsanthin from sweet red pepper (Capsicum annuum) showed remarkable cytotoxic effect on the triple-negative MDA-MB-231 cell line.

Solubility enhancement of curcumin, quercetin and rutin by solid dispersion method

Solubility enhancement of curcumin, quercetin and rutin by solid dispersion method

Study on preparation of CuCl/REY adsorbent with high CO adsorption and selectivity

In this paper, rare earth elements are used to modify Y zeolite, and CuCl-loaded rare earth Y zeolite adsorbents (CuCl/REY) were prepared by solid monolayer dispersion method. The adsorption performance of CuCl/REY on CO was studied, and the adsorbents were characterized via nitrogen adsorption/desorption at 77 K, X-ray fluorescence (XRF), X-ray diffraction (XRD) and scanning electron microscopy (SEM). We also characterize the state of Cu through temperature-programmed reduction using hydrogen (H2-TPR). The results show that rare earth can slightly increase the pore size, while maintaining the stability of the zeolite framework structure. Also, it can inhibit the production of copper oxide (CuO) to increase the CO capacity, and reduce the adsorption of N2 to increase the CO/N2 selectivity. Under the condition of 298 K and 1 bar, CuCl/REY showed a high CO adsorption capacity of 2.64 mmol/g, and the selectivity of CO/N2 reached 53, which was nearly double the performance of the adsorbent prepared with NaY zeolite.

“FORMULATION DEVELOPMENT AND SOLUBILITY ENHANCEMENT OF ROSUVASTATIN CALCIUM BY USING HYDROPHILIC POLYMERS AND SOLID DISPERSION METHOD”

Objective: Preparation of Rosuvastatin Calcium by Using Hydrophilic Polymers and Solid Dispersion Method, Rosuvastatin calcium is a Dyslipidaemic agent, which act as a selective competitive inhibitor of HMG CoA educates enzyme and is used in the treatment of hyperlipidemia.&#x0D; Methods: In the present work, Solid Dispersion was prepared by kneading method to increase the solubility of Rosuvastatin Calcium.&#x0D; Results: Solid dispersions were evaluated by determining percentage yield, drug content, solubility, Scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), DSC and in vitro dissolution profile. The prepared solid dispersion are formulated into capsule dosage form and characterized by various parameters i.e. weight variation, content uniformity, disintegration and dissolution. The evaluated parameters of capsule dosage form increase in solubility and dissolution rate of the pure drug.&#x0D; Conclusion: These are various techniques to enhance the solubility of the drug, such as particle size reduction, use of surfactants, solid dispersion etc. Carriers are the major players in these formulations, e. g. Hydroxypropylmethylcellulose, ethylcellulose, Carbopol, Acacia Gum etc. Carbopol and Acacia Gum is one of the most efficient polymers work as a carrier for these drugs to enhance solubility.

Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

PREDICTION OF PROCESS VARIABLES IN INDOMETHACIN TERNARY SYSTEM USING EXPERIMENTAL DESIGN SOLID STATE CHARACTERIZATION AND IN-VIVO STUDIES

The aim of the present investigation is (i) to apply and analyze response surface methodology to optimize the preparation method of indomethacin solid dispersion which involves three significant independent variables: amounts of each carrier β-Cyclodextrin (βCD), Polyvinyl pyrrolidone (PVP K30), and solvent mixture (ethanol-water), (ii) to characterize by solid state analysis, and evaluate by in vivo study. A 3-factor, 3- level ‘Central Composite Face Centered design’ was used to explore the quadratic and linear response surfaces and to construct a second order polynomial models which can predict responses ‘aqueous solubility’, and ‘% release’ with minimum % error. In addition, the desirability function approach was applied to obtain the best compromise among the multiple responses. It was found that both the independent variables played a significant role on the solubility and percentage drug release. The solid state studies enable the phase (crystalline) transform of drug which influences its solubility and drug release. The enhancement of Cmax and AUC0-24 of indomethacin (in solid dispersion)with that of pure drug imply the increase in bioavailability of drug.

High diversity of natural Dalmatian pyrethrum based on pyrethrin composition at intra- and interpopulation level

Seeds collected from 10 Dalmatian pyrethrum (Tanacetum cinerariifolium /Trevir./ Sch. Bip. Asteraceae) populations naturally occurring along the Adriatic coast and islands, were used to establish a common garden with the aim of estimating the variation of pyrethrin compounds between and within populations. A recently optimized matrix solid phase dispersion (MSPD) method was used for the extraction of six pyrethrin compounds from dry flower heads of 200 Dalmatian pyrethrum individuals. Separation and quantification of pyrethrin compounds were performed by high performance liquid chromatography with diode array detector (HPLC-DAD). High variability in pyrethrin content and composition was observed within and between populations. Total pyrethrin content in individual samples varied from 0.10% to 1.35% of flower dry weight. On average, the lowest total pyrethrin content was observed in the population of Pelješac (0.22%) and the highest in the island populations of Mali Lošinj and Zlarin (0.87%). The population of Mali Lošinj had the most favourable pyrethrin profile, including the lowest variability in total pyrethrin content, the highest pyrethrin I (PI) content (up to 60.47%) and PI/PII ratio (up to 5.88), as well as the lowest pyrethrin II (PII) content. In contrast, the populations from Biokovo and Pelješac represented pyrethrin profiles with the lowest content of total pyrethrin, PI and PI/PII ratio. The Biokovo population also had the highest PII content (43.18% on average), while the Pelješac population had the highest jasmolin I (JI) and jasmolin II (JII) content. Four different chemotypes were determined by cluster analysis. Chemotype P1 is the most promising for future breeding programs and is characterized by the highest total pyrethrin content, PI content and PI/PII ratio, as important measures of insecticidal activity. Correlation analysis of each pyrethrin compound with 25 environmental variables and Principal Component Analysis (PCA) were carried out and the importance of optimum temperature and precipitation on pyrethrin quantity and quality was suggested. Total pyrethrin content was significantly correlated with six temperature and five precipitation parameters. Pyrethrin I, PII and cinerin II (CII) were significantly correlated mainly with temperature parameters; JII and cinerin I (CI) with precipitation parameters, while JI was correlated with temperature range and precipitation parameters. The mountainous Biokovo population was an outlier in the PCA analysis, mainly due to the extremely low values of temperature parameters at a higher altitude. Precipitation variables separated the central Adriatic islands inhabiting drier habitats from populations inhabiting habitats with greater precipitation. The high-resolution data from this study provide the opportunity for individual-based selection for breeding plants with the best pyrethrin profiles, as well as for increased adaptation to broader climatic conditions.

Aluminum phthalocyanine hydroxide-loaded thermoresponsive biomedical hydrogel: A design for targeted photosensitizing drug delivery

Dermatological formulations can enable a more efficient therapy by directly delivering the active ingredient to the action site. Photodynamic therapy is a promising technique to eliminate the microorganism in wounds. The present work aims to obtention a dermatological bioadhesive and stimuli-responsive platform that efficiently solubilizes aluminum phthalocyanine hydroxide (AlPcOH) photosensitizer. A better formulation for dermatological application was obtained after evaluation of the formulation polymeric composition and mechanical characterization. Ex-vivo permeation and complete rheological assays were carried out. The photodynamic potential of AlPcOH was evaluated quantitatively and qualitatively. AlPcOH was shown to be incorporated mostly in monomeric form when subjected to the solid dispersion method. Satisfactory results were achieved for the formulation composed of 0.05, 20, and 0.20 % w/w of AlPcOH, F127 and Carbopol. This formulation was easily administered and presented adequate retention at the application site. Furthermore, the system showed a gelation temperature of 29.1 °C, ensuring the preparation, filling, and administration in the bodýs temperature. The nanostructured thermo-responsive platform promoted AlPcOH skin permeation effects and demonstrated a high capacity to generate reactive oxygen species (ФΔ1O2 for AlPcOH of 0.68 in ethanol). All the information provided in this study supports the potential of the AlPcOH-containing platform designed to treat wounds aggravated by microbial infections. It suggests future in vitro and in vivo applications of the platform developed.

EFFECT OF SOLID DISPERSIONS ON THE SOLUBILITY OF METRONIDAZOLE

The aim of the work is to study the effect of solid dispersions using polyethylene glycols of various molecular weights on the solubility of metronidazole in water. Metronidazole is an antimicrobial and antiprotozoal drug. Its low solubility in water limits the use of metronidazole, causing technological difficulties and reducing its bioavailability. The solubility and release of the active substance from dosage forms can be increased using the solid dispersion methods. Solid dispersions are bi- or multicomponent systems consisting of an active substance and a carrier (a highly dispersed solid phase of the active substance or molecular-dispersed solid solutions) with a partial formation of complexes of variable compositions with the carrier material.Materials and methods. The substance of metronidazole used in the experiment, was manufactured by Hubei Hongyuan Pharmaceutical Technology Co., Ltd. (China). To obtain solid dispersions, polyethylene glycols of various molar masses – 1500, 2000 and 3000 g/mol – were used. The solid dispersions were prepared by “the solvent removal method”: metronidazole and the polymer were dissolved in a minimum volume of 96% ethyl alcohol (puriss. p.a./analytical grade) at 65±2°C, and then the solvent was evaporated under vacuum to the constant weight. A vacuum pump and a water bath were used at the temperature of 40±2°C. The dissolution of the samples was studied using a magnetic stirrer with heating, and a thermostatting device. The concentration of metronidazole was determined on a spectrophotometer using quartz cuvettes at the wavelength of 318±2 nm. To filter the solutions, syringe nozzles were used, the pores were 0.45 μm, the filter was nylon. Microcrystalloscopy was performed using a microscope with a digital camera. The optical properties of the solutions were investigated using a quartz cuvette and a mirror camera (the image exposure – 20 sec).Results. Obtaining solid dispersions increases the completeness and rate of the metronidazole dissolution. The solubility of metronidazole from solid dispersions increases by 14–17% in comparison with the original substance. The complex of physical-chemical methods of the analysis, including UV spectrophotometry, microcrystalloscopy and the study of the optical properties of the obtained solutions, makes it possible to suggest the following. The increase in the solubility of metronidazole from solid dispersions is explained by the loss of crystallinity and the formation of a solid solution of the active substance and the solubilizing effect of the polymer with the formation of colloidal solutions of metronidazole at subsequent dissolution of the solid dispersion in water.Conclusion. The preparation of solid dispersions with polyethylene glycols improves the dissolution of metronidazole in water. The results obtained are planned to be used in the development of rapidly dissolving solid dosage forms of metronidazole with an accelerated release and an increased bioavailability.

Solubility Enhancement of Diclofenac Using Solid Dispersions

Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

Enhancement of Solubility and Dissolution Rate of BCS Class-II Fluvoxamine Tablets using Solvent Evaporation Solid Dispersion Technique

Aim: This research work was aimed to formulate Enhancing the solubility of Poorly soluble drug i.e. Fluvoxamine tablets by the solvent evaporation method, Fluvoxamine medicament is a selective serotonin reuptake inhibitor (SSRI) antidepressant agent.&#x0D; Purpose: The BCS class II drug Fluvoxamine consist low aqueous solubility and low oral bioavailability, for this reason to improve the biological performance of Fluvoxamine drug by solid dispersion mechanism.&#x0D; Methodolgy: The drug Fluvoxamine was formulated by using solvent evaporation technique, solid dispersions of Fluvoxamine were prepared with different carriers in different ratios of PEG 6000 &amp; Mannitol (1:1, 1:2 and 1:3).&#x0D; Results: Results of prepared solid dispersions of Fluvoxamine by solid dispersion method Finally by comparing all the formulations, formulation (SF3) containing Fluvoxamine and PEG 6000 (1:3) shows better results.&#x0D; Conclusion: Here we concluded that the poorly soluble drug solubility improving by solvent evaporation solid dispersion mechanism, and also developed six Fluvovamine formulations (FDF1-FDF6) during this FDF4 shows maximum (98.9±0.8%) drug release at the end of time.

Water Solubility and Dissolution Enhancement of Fisetin by Spherical Amorphous Solid Dispersion in Polymer of Cyclodextrin

Fisetin (3, 7, 3', 4'-tetrahydroxyflavone) is an active ingredient characterized by a large spectrum of biological activities with a wide range of nutraceutical properties, including neuroprotecting, antidiabetic and suppression or prevention of tumors. The only drawback limiting its use is its low water solubility. The present work was focused on the solubility improvement of fisetin using spray-drying solid dispersion method, using also cyclodextrin polymers and which is extensively employed as technique to enhance poorly-water soluble compounds. Fisetin solubility was evaluated in the presence of poly-aβ-CD, poly-aγ-CD, poly-aβγ-CD and poly-methyl-β-CD by Higuchi solubility study. Spherical Amorphous solid dispersion formulations were prepared using polymethyl- β-CD (choice of the polymer was based on the better results of solubility study) at different ratios drug: polymer (1:1) and (1:3). In addition, different formulations were investigated using several techniques such as: Fourier Transformed Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), NMR and Scanning Electron Microscopy (SEM). The in vitro dissolution was performed in water at 37°C. The results of dissolution studies showed a complete dissolution observed with the formulation ratio 1:3 while the formulation ratio 1:1 showed a maximum dissolution rate about 59%. This difference is due to the formation of watersoluble inclusion complex and on the other hand to the high hydrophilicity of the cyclodextrin polymer.

Enhanced Solubility and Bioavailability of Dolutegravir by Solid Dispersion Method: In Vitro and In Vivo Evaluation-a Potential Approach for HIV Therapy.

Being a candidate of BCS class II, dolutegravir (DTG), a recently approved antiretroviral drug, possesses solubility issues. The current research was aimed to improve the solubility of the DTG and thereby enhance its efficacy using the solid dispersion technique. In due course, the miscibility study of the drug was performed with different polymers, where Poloxamer 407 (P407) was found suitable to move forward. The solid dispersion of DTG and P407 was formulated using solvent evaporation technique with a 1:1 proportion of drug and polymer, where the solid-state characterization was performed using differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffraction. No physicochemical interaction was found between the DTG and P407 in the fabricated solid dispersion; however, crystalline state of the drug was changed to amorphous as evident from the X-ray diffractogram. A rapid release of DTG was observed from the solid dispersion (>95%), which is highly significant (p<0.05) as compared to pure drug (11.40%), physical mixture (20.07%) and marketed preparation of DTG (35.30%). The drug release from the formulated solid dispersion followed Weibull model kinetics. Finally, the rapid drug release from the solid dispersion formulation revealed increased Cmax (14.56 μg/mL) when compared to the physical mixture (4.12 μg/mL) and pure drug (3.45 μg/mL). This was further reflected by improved bioavailability of DTG (AUC: 105.99±10.07 μg/h/mL) in the experimental Wistar rats when compared to the AUC of animals administered with physical mixture (54.45±6.58 μg/h/mL) and pure drug (49.27±6.16 μg/h/mL). Therefore, it could be concluded that the dissolution profile and simultaneously the bioavailability of DTG could be enhanced by means of the solid dispersion platform using the hydrophilic polymer, P407, which could be projected towards improved efficacy of the drug in HIV/AIDS.

Facile preparation of solid dispersions by dissolving drugs in N-vinyl-2-pyrrolidone and photopolymerization

Drug solid dispersions improve the dissolution of drugs in aqueous media for enhancement of oral bioavailability. The current preparation methods of drug solid dispersions mainly involve the evaporation of solvents or the melting of drugs and matrix. Here, we create a new and simple method for the preparation of drug solid dispersions by dissolving drugs in N-vinyl-2-pyrrolidone (NVP) and then NVP photopolymerization. A variety of drugs were explored to find whether they were suitable for this method and only some of them were soluble in NVP and formed transparent and hard solid dispersions, including fluconazole, ketoconazole, bifonazole, miconazole nitrate, sulfamethoxazole, aspirin, ibuprofen and artesunate. The formation of photocuring solid dispersions was highly related to the free radical scavenging function of drugs. Those drugs with strong free radical scavenging capability, including curcumin, resveratrol, quercetin, genistein, puerarin, nicergoline, olanzapine, indomethacin, did not form solid dispersions. They scavenged 2,2-diphenyl-1-picrylhydrazyl free radicals, which was demonstrated by ultraviolet spectrometry and electron spin resonance. The scavenging of free radicals stopped the chain polymerization of NVP. The Fourier transform infrared spectra, X-ray diffraction and differential scanning calorimetry of ibuprofen solid dispersions and artesunate solid dispersions showed the molecularly miscible state of the drugs and the hydrogen bonding between the drugs and polyvinyl pyrrolidone. The NVP-based solid dispersions of the two drugs had faster and more complete dissolution than their traditional solid dispersions. The NVP photopolymerization-based solid dispersion method provides a new choice for the production of solid dispersions in the research and industrial fields.

Preparation and Characterization of Artemether Solid Dispersion by Spray Drying Technique

Introduction: Artemether, a BCS class IV drug (poorly water soluble and poorly permeable, less bioavailability) but is found to be effective against falciparum malaria. Preparation of water soluble formulation could be the technique to improve bioavailability of such drug. The most ideally used technique to enhance the solubility and dissolution of poorly water soluble drugs is Solid dispersion method.&#x0D; Method: The objective of the study was to enhance the solubility and dissolution rate of Artemether by preparing solid dispersions using Soluplus, at different ration of 1:1, 1:2, 1:3 and 1:4 using spray drying technology. Prepared Solid dispersions were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry.&#x0D; Results: The spray-dried solid dispersions found to be having less crystallinity and showed higher dissolution rates. Solubility study data showed the optimum drug/Soluplus ratio to be 1:3. The dissolution studies of Solid dispersions in 1.2 pH and 6.8 pH buffer showed higher drug release as compared to pure drug.&#x0D; Conclusion: Thus we conclude that an amorphous solid dispersion of Artemether could be a better option for enhancing the dissolution rate of drug&#x0D; Keywords: solid dispersion, artemether, soluplus, solubility enhancement

Synthesis of ZnO/FA composite for methylene blue decolorization

In this research, a ZnO/FA composite was successfully synthesized for the photocatalytic treatment of methylene blue. ZnO was obtained from Zn-C battery waste by precipitation method. Zinc metal from battery waste was separated, cleaned, and dissolve in hydrochloric acid to get the ZnCl2 solution. After adding some base until pH = 10, white precipitation was formed. This precipitate was filtered out and calcinated at 400 °C for 4 hours to obtained ZnO. Fly Ash (FA) was obtained from coal combustion waste. Fly ash was cleaned and drying at 105 °C for 3 hours. Synthesis of ZnO/FA composite was synthesized by a solid dispersion method using acetone as a medium with a various composition of ZnO: FA = 20:80; 40:60; 60:40; 80,20 in percentage. The XRD data show that the ZnO/FA composite was successfully synthesized. The SEM photo’s show that different morphology where more ZnO in the composite, the FA particles will be increasingly encased with ZnO particles. Photocatalytic performance studies of ZnO/FA composites for decolorization of methylene blue were carried out in various compositions, exposure times, substrate concentrations, and mass composites. The optimum decolorization was found in 40:60 composition, 3 hours irradiation time, 5 ppm concentration of methylene blue, and 150 mg of photocatalyst mass.

Proximate analysis and nutrient content estimation of marine fish species of saint martin’s island in Bangladesh

Saint Martin’s Island is a unique coral island in Bangladesh. Locally available fish species (both fresh and dry fish) were collected from the island to study moisture, ash, fat, protein content, fatty acid compositions and heavy metals. Fish oil was extracted from samples by solid phase dispersion method and fatty acid compositions were analyzed by GC-FID. Protein content in fresh fish samples was determined by the micro-Kjeldahl method. Homogenized samples were digested, filtered and analyzed by AAS for determining toxic heavy metals in the fish samples. The fresh fishes appear to be a good source of dietary protein.&#x0D; Journal of Bangladesh Academy of Sciences, Vol. 44, No. 2, 191-195, 2020