scholarly journals Dissolution Testing of Single- and Dual-Component Thyroid Hormone Supplements

Separations ◽  
2019 ◽  
Vol 6 (1) ◽  
pp. 18
Author(s):  
Samantha Bowerbank ◽  
Michelle Carlin ◽  
John Dean
Keyword(s):  
Thyroid Hormone ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Testing ◽  
Liquid Chromatography Mass Spectrometry ◽  
Intestinal Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Biorelevant Dissolution ◽  
Fasted State

A method for the analysis of thyroid hormones by liquid chromatography-mass spectrometry was used for the dissolution testing of single- and dual-component thyroid hormone supplements via a two-stage biorelevant dissolution procedure. The biorelevant media consisted of fasted-state simulated gastric fluid and fasted state simulated intestinal fluid at 37 °C, and was investigated using an internationally recognized protocol. The dissolution profiles showed consistent solubilization for both single- and dual-component batches at pH 6.5 in the fasted-state simulated intestinal fluid.

scholarly journals Interpolymer Complexes of Eudragit® Copolymers as Novel Carriers for Colon-Specific Drug Delivery

Polymers ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 1459
Author(s):  
Aleksandra V. Bukhovets ◽  
Nikoletta Fotaki ◽  
Vitaliy V. Khutoryanskiy ◽  
Rouslan I. Moustafine
Keyword(s):  
Drug Delivery ◽  
Photoelectron Spectroscopy ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Swelling Properties ◽  
Interpolymer Complexes ◽  
Fasted State ◽  
The Media

Interpolymer complexes (IPC) based on Eudragit® EPO and Eudragit® S100 were investigated as potential carriers for oral controlled drug delivery to the colon. IPC samples were prepared by mixing copolymer solutions in organic solvents (ethanol, isopropanol:acetone mixture (60:40, % v/v) and tetrahydrofuran). According to the data of elemental analysis, FTIR-spectroscopy, X-ray photoelectron spectroscopy and thermal analysis these IPCs have excess of anionic copolymer (Eudragit® S100) in their structure; they are stabilized by hydrogen and ionic intermacromolecular bonds and do not include free copolymer domains. IPC have pH-independent swelling properties in the media mimicking gastrointestinal tract (GIT) conditions and provide colon-specific delivery of indomethacin in buffer solutions (pH 1.2; 5.8; 6.8; 7.4) and in biorelevant media (fasted state simulated gastric fluid, fasted state simulated intestinal fluid—version 2 and fasted stated simulated colonic fluid).

scholarly journals Release Activity of Encapsulated Lactobacillus plantarum NBRC 3070 in Optimum Alginate - Aloe vera Matrices during Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF) Exposure

2017 ◽  
Vol 5 (2) ◽  
Author(s):  
Nur Syahirah Sallehudin ◽  
Khalilah Abdul Khalil ◽  
Maslinda Musa ◽  
Hifa Nazirah Mohd Yazid ◽  
Anida Yusof
Keyword(s):  
Aloe Vera ◽  
Clinical Results ◽  
Gastric Fluid ◽  
Alginate Beads ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Encapsulated Cells ◽  
Aloe Vera Gel ◽  
Encapsulation Process

Probiotic encapsulation approach has the potential to protect microorganisms and to deliver them into the gut. Because of the promising preclinical and clinical results, probiotics have been incorporated into a range of products. However, there are still many challenges to overcome with respect to the encapsulation process and the conditions prevailing in the gut. Thus in this study, the release activity of encapsulated L. plantarum NBRC 3070 and Aloe vera gel within alginate coated chitosan matrices during simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) exposure were investigated. There were four groups of beads prepared in this study: 1) Encapsulated probiotic and Aloe vera within alginate beads (chitosan coated), 2) Encapsulated probiotic within alginate beads (chitosan coated), 3) Encapsulated probiotic and Aloe vera within alginate beads (uncoated) and 4) Encapsulated probiotic alone within alginate beads (uncoated). Encapsulation process was carried out using extrusion method. The optimized composition of alginate matrix (1.34% w/v) and Aloe vera gel (1.99% w/v) were used.  In order to investigate their release activity, all beads were exposed in Simulated Gastric (SGF) at pH 2.5 and Simulated Intestinal Fluids (SIF) at pH 6.5 for 120 min and 270 min, respectively. Based on the findings, alginate-Aloe vera beads with chitosan coated was able to protect L. plantarum NBRC 3070 during SGF exposure with only 1 log10 cfu/mL reduction. The presence of Aloe vera gel in the beads improved the survivability of the cells. Encapsulated cells were observed successfully slow released of cells from the beads after exposure in SIF. Scan Electron Microscope (SEM) result had shown that cross link activity of the optimum alginate-Aloe vera with chitosan coating resulted in better survival of cells after simulated gastro and able to deliver sufficient probiotic dose to intestinal region. The combinations were able to improve encapsulated cells survivability during low acidic environment passage and release activity into the intestinal target region.   

scholarly journals Survival Survey of Lactobacillus acidophilus In Additional Probiotic Bread

2019 ◽  
Vol 7 (4) ◽  
pp. 588
Author(s):  
Truong Duc Thang ◽  
Le Thi Hanh Quyen ◽  
Hoang Thi Thuy Hang ◽  
Nguyen Thien Luan ◽  
Dang Thi KimThuy ◽  
...  
Keyword(s):  
Lactobacillus Acidophilus ◽  
Xanthan Gum ◽  
Gastric Fluid ◽  
Probiotic Bacteria ◽  
Simulated Gastric Fluid ◽  
Protective Agent ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
The World ◽  
Alginate Matrix

Bread is a popular food in the world because of its variety and convenience. Currently, studies on the adding probiotics to bread are limited due to the adverse effects of processing, such as baking temperature, aerobic environment to the probiotic bacteria. The objective of this study was to produce probiotic cream bread, in which Lactobacillus acidophilus was microencapsulated with Alginate 2% (A); Alginate 2% + maltodextrin 1% (AM); Alginate 2% + xanthan gum 0.1% (AX); and Alginate 2% + maltodextrin 1% + xanthan gum 0.1% (AMX). Microcapsules were added to the kernel, conducting encapsulation yield investigations, survival in baking, preservation of bread, and in simulated gastric fluid and simulated intestinal fluid conditions after 8 days of storage. The results showed that the addition of xanthan gum enhanced the encapsulation yield, it reached 92.9% and 92.37% in AMX and AX samples, respectively. The viability of L. acidophilus during baking was decreased by 3.64 and 3.75 Log (CFU/bread) in AMX and AM samples, compared to A and AX which were decreased by 4.75 and 4.44 Log (CFU/ bread). In SGF (Simulated Gastric Fluid) and SIF (Simulated Intestinal Fluid) conditions, the AMX microcapsules provide the best probiotic protection among the four tested carriers. The combination of xanthan gum and maltodextrin in alginate matrix, eventually leading to having dual efficiency: First, xanthan gum would act as buffers that reduce acid activity; Second, maltodextrin acting as a protective agent of L. acidophilus against high temperature as well as potential prebiotic that improve the viability of probiotic.

scholarly journals IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
Author(s):  
Jose Raul Medina ◽  
Jonathan Hernandez ◽  
Marcela Hurtado
Keyword(s):  
In Vitro Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Time ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Release Studies ◽  
Flow Through ◽  
Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance. 

Role of Biorelevant Media in Estimation of in vitro Lipolysis and Food Impact on Self-emulsifying Drug Delivery Systems.

2020 ◽  
Vol 15 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery Systems ◽  
Food Effect ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Biorelevant Media ◽  
In Vitro Lipolysis ◽  
Fasted State

: Self-emulsifying drug delivery systems (SEDDS) includes self-micro emulsifying drug delivery system (SMEDDS) and self-nano emulsifying drug delivery system (SNEDDS) whose major benefits is reduction of inter/intra subject variability and food effect which may alter the pharmacological response of the drug. Oral intake of these formulations triggers the digestion process because of pancreatic lipase which emulsify/digest the lipidic ingredients of the formulation resulting into precipitation of the drug. As a tool to foresee in vivo medicament precipitation, in vitro lipolysis models are established. Biorelevant media play an important role to study the effect of in vitro lipolysis and food impact on the bioavailability of SEDDS formulations. It is vital to generate composition of fluids for both fed and fasting conditions of gastric, small intestine and colon to investigate the impact of in vitro lipolysis and food effect on the release behavior of drug from SEDDS. Fed/Fasted state simulated gastric fluid (Fe/FaSSGF), Fed/Fasted state simulated gastric fluid (Fe/FaSSIF) (Phosphate buffers) are first generation while Fa/FeSSIF-V2 (maleate) are second generation biorelevant media utilized for these studies. FaSSIF-V3 belongs to third generation which differs from other generations in the composition and source of bile salts. With updates in physiological data, it is vital to incorporate changes in the dissolution media to make it more biorelevant. This review paper mainly laid emphasis on the compositions of biorelevant media of gastric and small intestine for both fed and fasting conditions. In addition to these, applications of biorelevant to investigate effect of in vitro lipolysis and food on SEDDS are discussed with some recent research reports.

scholarly journals Directly Compressed Tablets of Free Acid Ibuprofen with Nanocellulose Featuring Enhanced Dissolution: A Side-by-Side Comparison with Commercial Oral Dosage Forms

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 71 ◽  
Author(s):  
Athanasios Mantas ◽  
Marie-Amélie Petit ◽  
Albert Mihranyan
Keyword(s):  
Surface Area ◽  
Free Acid ◽  
High Surface ◽  
High Surface Area ◽  
Oral Dosage ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid ◽  
Enhanced Dissolution

We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization. The goal of the present work was to further elaborate the concept and conduct side-by-side in vitro drug release comparisons with commercial formulations, including film-coated tablets, soft gel liquid capsules, and IBU-lysine conjugate tablets, in biorelevant media. Directly compressed tablets were produced from heated mixtures of 20% w/w IBU and high surface area Cladophora cellulose (CLAD), with 5% w/w sodium croscarmelose (AcDiSol) as superdisintegrant. The side-by side studies in simulated gastric fluid, fasted-state simulated intestinal fluid, and fed-state simulated intestinal fluid corroborate that the IBU-CLAD tablets show more rapid and less variable release in various media compared to three commercial IBU formulations. On the sidelines of the main work, a possibility of the presence of a new meta-crystalline form of IBU in mixture with nanocellulose is discussed.

scholarly journals Metabolic Stability of D-Allulose in Biorelevant Media and Hepatocytes: Comparison with Fructose and Erythritol

Foods ◽  
2019 ◽  
Vol 8 (10) ◽  
pp. 448 ◽  
Author(s):  
Maeng ◽  
Yoon ◽  
Chun ◽  
Kim ◽  
Jang ◽  
...  
Keyword(s):  
Calorific Value ◽  
Rat Hepatocytes ◽  
Gastric Fluid ◽  
Metabolic Stability ◽  
Simulated Gastric Fluid ◽  
Pharmacokinetic Studies ◽  
Food Ingredient ◽  
Biorelevant Media ◽  
Simulated Intestinal Fluid

D-allulose, a C-3 epimer of D-fructose, is a rare monosaccharide used as a food ingredient or a sweetener. In the present study, the in vitro metabolic stability of D-allulose was examined in biorelevant media, that is, simulated gastric fluid (SGF) and fasted state simulated intestinal fluid (FaSSIF) containing digestive enzymes, and in cryopreserved human and rat hepatocytes. The hepatocyte metabolic stabilities of D-allulose were also investigated and compared with those of fructose and erythritol (a sugar-alcohol with no calorific value). D-allulose was highly stable in SGF (97.8% remained after 60 min) and in FaSSIF (101.3% remained after 240 min), indicating it is neither pH-labile nor degraded in the gastrointestinal tract. D-allulose also exhibited high levels of stability in human and rat hepatocytes (94.5–96.8% remained after 240 min), whereas fructose was rapidly metabolized (43.1–52.6% remained), which suggested these two epimers are metabolized in completely different ways in the liver. The effects of D-allulose on glucose and fructose levels were negligible in hepatocytes. Erythritol was stable in human and rat hepatocytes (102.1–102.9% remained after 240 min). Intravenous pharmacokinetic studies in rats showed D-allulose was eliminated with a mean half-life of 72.2 min and a systemic clearance of 15.8 mL/min/kg. Taken together, our results indicate that D-allulose is not metabolized in the liver, and thus, unlikely to contribute to hepatic energy production.

scholarly journals Production, Properties and Swelling of Copper-Pectic Gel Particles in an Artificial Gastroenteric Environment

2021 ◽  
Vol 11 (1) ◽  
pp. 50-52
Author(s):  
Anatoly Shubakov ◽  
Elena Mikhailova
Keyword(s):  
Aqueous Solutions ◽  
Copper Ions ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Apple Pectin ◽  
Simulated Intestinal Fluid ◽  
Ionotropic Gelation ◽  
Gel Particles

The purpose of the this research was to obtain and study the properties of copper-pectic gel particles (CuPGPs) obtained from aqueous solutions of apple pectin (AP) in the concentration range of 1%-5% in the presence of Cu2+ ions. Methods and Results: We used commercial AP AU701 (Herbstreith & Fox KG, Germany). CuPGPs were obtained from aqueous solutions of AP (1%, 3%, 5%) in the presence of Cu2+ ions (1%-10%) by the method of ionotropic gelation, The diameter and density of the CuPGPs were determined. Dry CuPGPs formed from 5% AP with all tested concentrations of copper ions have the largest diameter (0.96-1.15mm), and gel particles formed on the basis of 1% AP have the smallest diameter (0.42-0.74mm). CuPGPs formed from 5% AP have the highest density (1.43-1.65 mg/mm3), and CuPGPs formed on the basis of 1% AP have the lowest density (0.65-0.92 mg/mm3). Gel particles obtained from 1% AP swelled in simulated gastric fluid (SGF) by 161% and then completely degraded immediately upon entering in simulated intestinal fluid (SIF). CuPGPs obtained from 3% AP swelled by 166% in simulated gastric fluid (SGF) and 148% in SIF, and completely degraded in SIF after 2.5 hours of incubation in it. Gel particles obtained from 5% AP in the presence of 10% Cu2+ swelled most strongly – by 173% in SGF and by 208% in SIF. And then, they degraded after 8 hours of incubation in simulated colonic fluid (SCF).

scholarly journals Stability of Principal Hydrolysable Tannins from Trapa taiwanensis Hulls

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 365 ◽  
Author(s):  
Ching-Chiung Wang ◽  
Hsyeh-Fang Chen ◽  
Jin-Yi Wu ◽  
Lih-Geeng Chen
Keyword(s):  
Protective Effect ◽  
Water Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Buffer Solution ◽  
Simulated Intestinal Fluid ◽  
Hydrolysable Tannins ◽  
The Stability ◽  
Tellimagrandin Ii

The fruit and hulls of the water caltrop (Trapa taiwanensis Nakai) are used as hepatoprotective herbal tea ingredients in Taiwan. The stability of hydrolysable tannins in herbal drinks has rarely been reported. In the present study, two hydrolysable tannins, tellimagrandin II (TGII) and 1,2,3,4,6-pentagalloylglucopyranose (PGG), were isolated from water caltrop hulls. The stability of the two compounds was evaluated by treatment with various pH buffer solutions, simulated gastric fluid and intestinal fluid, different temperatures, and photo-irradiation at 352 nm in different solvents. Results showed that TGII and PGG were more stable in a pH 2.0 buffer solution (with 91.88% remaining) and in a water solution with 352 nm irradiation (with 95% remaining). TGII and PGG were more stable in methanol or ethanol solutions (with >93.69% remaining) than in an aqueous solution (with <43.52% remaining) at 100 °C. In simulated gastric fluid, more than 96% of the hydrolysable tannins remained after incubation at 37 °C for 4 h. However, these hydrolysable tannins were unstable in simulated intestinal fluid, as after incubation at 37 °C for 9 h, the content of TGII had decreased to 31.40% and of PGG to 12.46%. The synthetic antioxidants, butyl hydroxy anisole (BHA), di-butyl hydroxy toluene (BHT), and propyl gallate, did not exhibit photoprotective effects on these hydrolysable tannins. However, catechin, a natural antioxidant, displayed a weak photoprotective effect. Ascorbic acid had a short-term thermal-protective effect but not a long-term protective effect. The different stability properties of hydrolysable tannins in solutions can be used in the development of related herbal teas in the future.

Modifying release of poorly soluble active pharmaceutical ingredients with the amine functionalized SBA-16 type mesoporous materials

2019 ◽  
Vol 33 (9) ◽  
pp. 1214-1231 ◽  
Author(s):  
Barbara Jadach ◽  
Agnieszka Feliczak-Guzik ◽  
Izabela Nowak ◽  
Bartłomiej Milanowski ◽  
Hanna Piotrowska-Kempisty ◽  
...  
Keyword(s):  
Mesoporous Materials ◽  
Gastric Fluid ◽  
Bet Surface Area ◽  
Simulated Gastric Fluid ◽  
Active Pharmaceutical Ingredients ◽  
Intestinal Fluid ◽  
Pharmaceutical Ingredients ◽  
Fasted State ◽  
Small Intestinal ◽  
Release Profiles

SBA-16 and two modified SBA-16 type ordered mesoporous silica were used as the carriers for ibuprofen (anti-inflammatory drug) and furosemide (loop diuretic drug). Modification of the solid carrier was prepared with chitosan or N-3[(amino(poly-propylenoxy)]aminopropyltrimethoxysilane. The samples of carriers and carrier-drug loaded materials were characterized by X-ray diffraction, N2 adsorption, Fourier-transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. The release profiles of active pharmaceutical ingredients were performed in media with different pH in the USP 2 apparatus as well as in two biorelevant media (fasted state simulated gastric fluid and fasted state small intestinal fluid) in USP 4 apparatus. The loading of active substances into mesoporous materials was performed with modified immersion method. The maximum content of deposited drug in mesoporous material was close to 12.0 and 2.2 wt.% for ibuprofen and furosemide, respectively. After drug adsorption, the reduction of BET surface area, pore volume and pore diameter of non-modified and modified SBA-16 was observed, while the cubic arrays of siliceous matrix were well preserved. The release profiles of ibuprofen and furosemide loaded in mesoporous materials in media with different pH and biorelevant fasted state simulated gastric fluid and fasted state small intestinal fluid showed that the new SBA-16 type materials modify the release profiles of furosemide, increasing the dissolution rate of these substances in the medium at pH 1.2. The cytotoxicity of the materials and permeability of drugs after their loading on SBA-16 materials were evaluated on Caco-2 model. The results of our study showed that mesoporous materials did not exert cytotoxic effects and did not influence on the permeability of both active pharmaceutical ingredients in relation to pure substances.

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