scholarly journals Taste Masking of Nizatidine Using Ion-Exchange Resins

Processes ◽  
2019 ◽  
Vol 7 (11) ◽  
pp. 779 ◽  
Author(s):  
Pattaraporn Panraksa ◽  
Kasidech Boonsermsukcharoen ◽  
Kyu-Mok Hwang ◽  
Eun-Seok Park ◽  
Pensak Jantrawut
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Drug Loading ◽  
Electronic Tongue ◽  
Spherical Shape ◽  
Batch Process ◽  
Taste Masking ◽  
Simulated Gastric Fluid ◽  
Exchange Resins

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, and 1:5. The optimum drug: resin ratio and the time required for maximum percentage drug loading into the complexes were determined. The selected drug-resin complexes were evaluated for morphology, drug release, and taste. The NZD-Dowex complex was obtained at a drug: resin ratio of 1:5 using a stirring time of 1 h in order to get 100% loading of NZD. The NZD-Dowex complex had a spherical shape and smooth texture similar to Dowex resin. The NZD-Dowex complex with a ratio of 1:5 showed that in vitro drug release of 4.27% at 5 min in simulated salivary fluid of pH 6.8 and 99.67% at 1 h in simulated gastric fluid of pH 1.2. NZD’s bitter taste was effectively masked when it formed a complex with Dowex at a ratio of 1:5. This was proved by an electronic tongue and human test panel.

scholarly journals DESIGN, OPTIMIZATION, AND STATISTICAL EVALUATION OF ORAL RECONSTITUTED SUSPENSION OF CLARITHROMYCIN USING ION-EXCHANGE RESINS

2020 ◽  
pp. 53-60
Author(s):  
KOMAL S ◽  
HARIKRISHNAN N
Keyword(s):  
Complex Formation ◽  
Ion Exchange ◽  
Drug Release ◽  
Bitter Taste ◽  
Drug Loading ◽  
Taste Masking ◽  
Ion Exchange Resins ◽  
Comparison Test ◽  
Multiple Comparison Test ◽  
Exchange Resins

Objectives: The objective of the present study is taste masking of bitter clarithromycin using Indion 204, Indion 234, and Tulsion 335 as ion-exchange resins, which forms insoluble complexes, inhibiting the drug release in saliva as ion-exchange resins are cross-linked polymers, water-insoluble that contains salt-forming groups in repeating positions on the polymer chain. Drugs that are bitter and cationic get adsorbed onto weak cationic exchange resins of carboxylic acid functionality such as Indion 204, Indion 234, and Tulsion 335 to form non-bitter complexes. Methods: The drug-resin complex loading process was optimized for the resin content, activation, swelling time, stirring time, influence of pH, and temperature for maximum drug loading and the formed complex was evaluated by differential scanning calorimetry (DSC) to confirm complex formation. The drug-resin complex was also characterized by their micromeritic and rheological properties. These complexes were used to prepare oral reconstituted suspensions and the taste was evaluated. The formulation was evaluated for various parameters such as sedimentation volume, pH, redispersibility, viscosity, drug content, and in vitro drug release. Results: Acid-activated resins comprising Indion 204, Indion 234, and Tulsion 335 with the drug:resin ratio of 1:2, stirred in a solution of pH 7–8 at 70° for 6 h had a maximum drug loading and masked the bitter taste of clarithromycin. DSC of the drug-resin complex (DRC) revealed that there was interaction leading to complex formation. The drug-resin complex was formulated into suspension formulations (S1-S9) and evaluated. Various parameters were found to be within permissible limits. Formulations S3, S6, and S9 containing 1:2 ratios of the drug-resin complex of Indion 204, Indion 234, and Tulsion 335 revealed maximum taste masking. This was further confirmed by treatment of taste evaluation scores obtained from the volunteers by ANOVA, Dunnett’s multiple comparison test, and Tukey’s multiple comparison test. All the three optimized formulations had a significant difference of p<0.001 when compared to control S10. S6 formulation was widely accepted. Conclusion: Ion-exchange complexation could efficiently mask the bitter taste of clarithromycin and achieve palatable taste suitable for pediatric use.

scholarly journals Fixed Dose Oral Dispersible Tablet of Bitter Drug Using Okra Mucilage: Formulation and Evaluation

2020 ◽  
Vol 10 (5) ◽  
pp. 149-158
Author(s):  
Pintu Dhar ◽  
Himangshu Sarma ◽  
Hemanta Kumar Sharma
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Oral Dosage ◽  
Taste Masking ◽  
Fixed Dose ◽  
Wet Granulation ◽  
Formulation Development ◽  
Dispersible Tablet ◽  
Promethazine Hydrochloride

Background: The solid oral dosage forms containing bitter drugs need improved palatability for administration. Formulation scientists have given attention to the improvement of taste masking technologies and utilised various strategies. Objective: The present work aimed to mask the bitter taste of Promethazine Hydrochloride by formulating Oral Dispersible Tablets using Okra mucilage as a taste-masking agent.  Methods: The Okra mucilage was extracted from Okra by the aqueous extraction process. An emulsion solvent diffusion technique was used for masking the bitter taste of Promethazine Hydrochloride by using Okra mucilage. The Oral Dispersible Tablet was prepared by the wet granulation method. The mucilage and the formulation were characterized and evaluated by standard methods and protocols. Results: Taste masking of the bitter drug was successfully achieved by Okra mucilage. The DSC and FTIR study revealed that the drug molecule was compatible with okra mucilage and drug entrapment efficacy was found to be 94.76%. The palatability test asserted that masking of the bitter taste of the drug.  The In vitro drug release study showed that the F7 tablet batch has a better drug release rate and followed non- fickian mechanism of drug release. Conclusion: Thus, taste masking with Okra mucilage was successful and this opens opportunities for application of common edible substances in formulation development. Keywords: Fast disintegrating tablet; Natural polymer; Mouth dissolving tablet; Promethazine Hydrochloride; Taste masking

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

scholarly journals Development and evaluation of ofloxacin orally disintegrating tablets

2012 ◽  
Vol 48 (2) ◽  
pp. 217-225 ◽  
Author(s):  
Badrinath Pralhadrao Mohite ◽  
Sandip Annaji Chafle ◽  
Jayaprakash Somasundaram ◽  
Jasmine Gev Avari
Keyword(s):  
Bitter Taste ◽  
Drug Loading ◽  
Masking Effect ◽  
Taste Masking ◽  
Physical Parameters ◽  
Effect Of Ph ◽  
Orally Disintegrating Tablets ◽  
Cation Exchange Resins ◽  
Weak Cation Exchange ◽  
Exchange Resins

Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204.

scholarly journals Preparation and Evaluation of Gastroretentive Floating Pellets of Metronidazole

2013 ◽  
Vol 16 (1) ◽  
pp. 107-115 ◽  
Author(s):  
Shahriar Nowshad ◽  
Md Saiful Islam Pathan
Keyword(s):  
Drug Release ◽  
Bulk Density ◽  
Sodium Alginate ◽  
Drug Loading ◽  
Simulated Gastric Fluid ◽  
Gi Tract ◽  
Enhanced Absorption ◽  
Psyllium Husk ◽  
Alginate Concentration

Traditionally metronidazole is used in the treatment of bacterial vaginosis, trichomoniasis, amoebiasis and is also used in combination with other drugs to treat Helicobacter pylori (H. pylori) that causes stomach or intestinal ulcers. The main aim of this study was to develop a gastroretentive floating pellets for the treatment of above pathological conditions. Such kind of dosage form may provide an extension of drug presence in the upper GI tract resulting enhanced absorption and improved bioavailability for the treatment against protozoa and bacteria. Nine formulations of metronidazole floating pellets such as F1, F2, F3, F4, F5, F6, F7, F8 and F9 were prepared by ionic gelation method using different quantities of sodium alginate and psyllium husk. The drug and polymer ratio were 1:1.4, 1:1.5, 1:1.6, 1:1.6; 1:1.7, 1:1.8, 1:1.8, 1:1.9 and 1:2.0, respectively. The in vitro drug release study was carried out in 900 ml phosphate buffer (pH 7.4) at 37±0.50C and 50 rpm for 12 hours using USP XXIV paddle method and the content of drug release was determined by UV spectrometer at 277nm. Maximum and minimum drug release were found in F1 (88.63%) and in F6 (73.21%), respectively. It indicates that increase in sodium alginate concentration decreases drug release. All the formulations were buoyant for more than 12 hours in simulated gastric fluid at 370C. The maximum and minimum bulk density tapped were 0.57 and 0.52 in F1 and F9, respectively where drug loading were 14.07% in F1 and 12.56% in F9 which indicates that bulk density of the pellets is directly proportional to drug loading. The maximum and minimum swelling were in F3 (75%) and F7 (59%), respectively which demonstrate that swelling of pellets were inversely proportional to the sodium alginate concentration but it is directly proportional to psyllium husk content. In addition, the psyllium husk keeps the GI tract healthy by scavenging toxins and residues of digestive systems. Therefore, it can be concluded that combination of sodium alginate and biodegradable psyllium husk can be prospectively used for the preparation of gastroretentive floating pellets. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14504 Bangladesh Pharmaceutical Journal 16(1): 107-115, 2013

scholarly journals Taste Masking Study Based on an Electronic Tongue: the Formulation Design of 3D Printed Levetiracetam Instant-Dissolving Tablets

2021 ◽  
Author(s):  
Zengming Wang ◽  
Jingru Li ◽  
Xiaoxuan Hong ◽  
Xiaolu Han ◽  
Boshi Liu ◽  
...  
Keyword(s):  
Drug Release ◽  
Electronic Tongue ◽  
Principal Component ◽  
Partial Least Square ◽  
Least Square ◽  
Partial Least Square Regression ◽  
Taste Masking ◽  
Formulation Design ◽  
3D Printed

Abstract Purpose Proper taste-masking formulation design is a critical issue for instant-dissolving tablets (IDTs). The purpose of this study is to use the electronic tongue to design the additives of the 3D printed IDTs to improve palatability. Methods A binder jet 3D printer was used to prepare IDTs of levetiracetam. A texture analyzer and dissolution apparatus were used to predict the oral dispersion time and in vitro drug release of IDTs, respectively. The palatability of different formulations was investigated using the ASTREE electronic tongue in combination with the design of experiment and a model for masking bitter taste. Human gustatory sensation tests were conducted to further evaluate the credibility of the results. Results The 3D printed tablets exhibited rapid dispersion (<30 s) and drug release (2.5 min > 90%). The electronic tongue had an excellent ability of taste discrimination, and levetiracetam had a good linear sensing performance based on a partial least square regression analysis. The principal component analysis was used to analyze the signal intensities of different formulations and showed that 2% sucralose and 0.5% spearmint flavoring masked the bitterness well and resembled the taste of corresponding placebo. The results of human gustatory sensation test were consistent with the trend of the electronic tongue evaluation. Conclusions Owing to its objectivity and reproducibility, this technique is suitable for the design and evaluation of palatability in 3D printed IDT development.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

scholarly journals Cholesterol Levels Affect the Performance of AuNPs-Decorated Thermo-Sensitive Liposomes as Nanocarriers for Controlled Doxorubicin Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 973
Author(s):  
Mónica C. García ◽  
Nabila Naitlho ◽  
José Manuel Calderón-Montaño ◽  
Estrella Drago ◽  
Manuela Rueda ◽  
...  
Keyword(s):  
Drug Release ◽  
Cancer Cells ◽  
Electrostatic Interactions ◽  
Drug Loading ◽  
Gradient Methods ◽  
Spherical Shape ◽  
Morphological Properties ◽  
Ovarian Cancer Cells ◽  
Cholesterol Levels ◽  
L1 And L2

Stimulus-responsive liposomes (L) for triggering drug release to the target site are particularly useful in cancer therapy. This research was focused on the evaluation of the effects of cholesterol levels in the performance of gold nanoparticles (AuNPs)-functionalized L for controlled doxorubicin (D) delivery. Their interfacial and morphological properties, drug release behavior against temperature changes and cytotoxic activity against breast and ovarian cancer cells were studied. Langmuir isotherms were performed to identify the most stable combination of lipid components. Two mole fractions of cholesterol (3.35 mol% and 40 mol%, L1 and L2 series, respectively) were evaluated. Thin-film hydration and transmembrane pH-gradient methods were used for preparing the L and for D loading, respectively. The cationic surface of L allowed the anchoring of negatively charged AuNPs by electrostatic interactions, even inducing a shift in the zeta potential of the L2 series. L exhibited nanometric sizes and spherical shape. The higher the proportion of cholesterol, the higher the drug loading. D was released in a controlled manner by diffusion-controlled mechanisms, and the proportions of cholesterol and temperature of release media influenced its release profiles. D-encapsulated L preserved its antiproliferative activity against cancer cells. The developed liposomal formulations exhibit promising properties for cancer treatment and potential for hyperthermia therapy.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

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