scholarly journals Design of Catalase Monolithic Tablets for Intestinal Targeted Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 69
Author(s):  
Mirna Alothman ◽  
Pompilia Ispas-Szabo ◽  
Mircea Alexandru Mateescu
Keyword(s):  
Targeted Delivery ◽  
Intestinal Inflammation ◽  
Gastric Fluid ◽  
Oral Dosage ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
Negative Effects ◽  
Simulated Intestinal Fluid

Several studies confirmed a correlation between elevated hydrogen peroxide (H2O2) levels in patients with intestinal bowel diseases (IBD) and the negative effects caused by its presence. The objective of this study was to explore the potential use of catalase (CAT) to diminish the level of H2O2 and its deleterious action on intestinal mucosa. Oral dosage forms of a CAT bioactive agent targeted to the intestines were designed and tested in various simulated gastric and intestinal media. Monolithic tablets (30% loading) were prepared using commercial CarboxyMethylCellulose (CMC) or synthesized CarboxyMethylStarch (CMS) and TriMethylAmineCarboxyMethylStarch (TMACMS) as matrix-forming excipients. For starch derivatives, the presence of the ionic groups (carboxymethyl and trimethylamine) was validated by spectral analysis. In vitro studies have shown that tablets formulated with TMACMS and 30% CAT resisted the acidity of the simulated gastric fluid and gradually released the enzyme into the simulated intestinal fluid. The investigation of the CAT release mechanism revealed the role of anionic and cationic groups of polymeric excipients and their involvement in the modulation of the CAT dissolution profile. The proposed drug delivery system can be considered an efficient solution to target CAT release in the intestine and contribute to the reduction of H2O2 associated with intestinal inflammation.

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

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. 

scholarly journals INCORPORATION OF VITAMIN E ONTO CROSS-LINKED GALACTOMANNAN PHOSPHATE MATRIX AND IN VITRO STUDY

2018 ◽  
Vol 11 (5) ◽  
pp. 355 ◽  
Author(s):  
Juliati Br Tarigan ◽  
Djendakita Purba ◽  
Cut Fatimah Zuhra
Keyword(s):  
Vitamin E ◽  
In Vitro Study ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Crosslinking Reaction ◽  
Reliability Study ◽  
Simulated Intestinal Fluid ◽  
Palm Fatty Acid Distillate ◽  
The Fourier Transform

 Objective: This study demonstrated the incorporation of Vitamin E from palm fatty acid distillate onto crosslinked galactomannan phosphate (CGP) matrix.Methods: CGP was obtained from the crosslinking reaction of galactomannan from Arenga pinnata (GAP) with tri-sodium metaphosphate (TMF) ranging from 1:1 to 4:3 while incorporation of Vitamin E was conducted in two steps to form films. The reliability study of Vitamin E in CGPVE was conducted using a solution of pepsin and sodium chloride and also in solution of pancreatin and buffer phosphate.Results: The Fourier-transform infrared spectrum indicated the presence of phosphate in CGP while the scanning electron microscope images depicted the changes of surface morphology from smooth (GAP) to rough and hollow (CGP) which confirmed that crosslink had occurred. The swelling study of CGP showed that the swelling indexes were similar and decreased with the increase of TMF. The efficiency of CGP to absorb Vitamin E ranged from 89.66% to 91.09%. The in vitro releasing study of Vitamin E in simulated gastric fluid and simulated intestinal fluid showed that only a small amount of Vitamin E was released.Conclusions: This study demonstrated that CGP can be prepared and is potentially useful for drug delivery to the colon.

Naturally Derived Matrix for Controlled Selenium Nanoparticles Delivery

2016 ◽  
Vol 695 ◽  
pp. 284-288 ◽  
Author(s):  
Simona Cavalu ◽  
Vasile Laslo ◽  
Florin Banica ◽  
Simona Ioana Vicas
Keyword(s):  
Gastric Fluid ◽  
Point Of View ◽  
Matrix Composition ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Elemental Selenium ◽  
Simulated Intestinal Fluid ◽  
Advantages And Disadvantages ◽  
Probiotic Lactic Acid Bacteria

The aim of this study is to develop a lyophilized matrix (microspheres) as a controlled delivery system for nanoselenium particles, using different formulation based on alginate or agar. Elemental selenium is considered as the least toxic of all selenium forms and in the same time supplementation with its nanosize particles has the same or better bioavailability compared to its salts. In our study, nanosized elemental selenium was obtained by fermentation technology using probiotic lactic acid bacteria (Lactobacillus casei). The microspheres have been characterized from structural point of view by using different techniques: FTIR spectroscopy, X-ray Diffraction and SEM. Each individual natural polymer has its own characteristic advantages and disadvantages; it is commonly accepted that naturally derived matrix often show an excellent balance between the mechanical properties, swelling and dissolution capacity. The optimized formulation was proposed upon in vitro dissolution study using Diferential Pulsed Voltammetry in order to measure the concentration of selenium released in simulated gastric fluid (pH=1.2) and simulated intestinal fluid (pH=8.1). The cumulative release of selenium from different formulations showed large differences with respect to matrix composition. We demonstrated that both alginate and agarose-based formulations are suitable to be used in basic environment such as small or large intestine. The results might be of high importance as absorption of selenium occurs mainly in the duodenum, caecum and colon (more than 85%).

Evaluation of Ibuprofen/Montmorillonite Nano-Clay Composites as an Oral Drug Delivery System and In-Vitro Drug Release Performance

2021 ◽  
Vol 21 (7) ◽  
pp. 3651-3655
Author(s):  
Woo Chang Kwon ◽  
Moonhee Choi ◽  
Kyung Chan Kang ◽  
Dong Hyun Kim
Keyword(s):  
Oral Drug Delivery ◽  
Gastric Fluid ◽  
Controlled Delivery ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Simulated Intestinal Fluid ◽  
Oral Drug Delivery System ◽  
Nano Clay ◽  
Best Fitting

A formulation for controlled delivery of ibuprofen (IBU) involving montmorillonite (MMT) nanoclays has been proposed. The present work has investigated the beneficial effect of MMT in improving controlled delivery of IBU. The intercalation of IBU into the interlayer of MMT was studied under different processing conditions such as reaction time and initial concentration of IBU. To characterize the IBU/MMT composites, X-ray diffraction (XRD) and Fourier transform infrared spectra (FTIR) were performed. The release behavior of IBU from IBU/MMT composites have been investigated under vitro conditions using buffer media of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37 °C. Controlled release of IBU from IBU/MMT composite has been observed during in vitro release experiments. Different mathematical models were used for fitting our experimental results, among them the best fitting was found for Higuchi equation based on the parabolic diffusion process.

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 In Vitro Dissolution Profile of Dapagliflozin: Development, Method Validation, and Analysis of Commercial Tablets

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Rafaela Zielinski Cavalheiro de Meira ◽  
Aline Biggi Maciel ◽  
Fabio Seigi Murakami ◽  
Paulo Renato de Oliveira ◽  
Larissa Sakis Bernardi
Keyword(s):  
Quality Evaluation ◽  
Systematic Approach ◽  
Gastric Fluid ◽  
Scientific Basis ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Dissolution Profile ◽  
Sodium Glucose Cotransporter ◽  
Dissolution Efficiency

Dapagliflozin was the first of its class (inhibitors of sodium-glucose cotransporter) to be approved in Europe, USA, and Brazil. As the drug was recently approved, there is the need for research on analytical methods, including dissolution studies for the quality evaluation and assurance of tablets. The dissolution methodology was developed with apparatus II (paddle) in 900 mL of medium (simulated gastric fluid, pH 1.2), temperature set at 37±0.5°C, and stirring speed of 50 rpm. For the quantification, a spectrophotometric (λ=224 nm) method was developed and validated. In validation studies, the method proved to be specific and linear in the range from 0.5 to 15 μg·mL−1 (r2=0.998). The precision showed results with RSD values lower than 2%. The recovery of 80.72, 98.47, and 119.41% proved the accuracy of the method. Through a systematic approach by applying Factorial 23, the robustness of the method was confirmed (p>0.05). The studies of commercial tablets containing 5 or 10 mg demonstrated that they could be considered similar through f1, f2, and dissolution efficiency analyses. Also, the developed method can be used for the quality evaluation of dapagliflozin tablets and can be considered as a scientific basis for future official pharmacopoeial methods.

scholarly journals Improvement in Entrapment Efficiency and In Vitro Digestion Stability of Lutein by Zein Nanocarriers with Pepsin Hydrolysis

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Yan Jiao ◽  
He Han ◽  
Ying Chang ◽  
Dajing Li ◽  
Asad Riaz
Keyword(s):  
Structural Characteristics ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
In Vitro Digestion ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Bioactive Ingredients

Zein is one of the popular bioactive carriers and play critical roles in the promotion of stability, absorption, and utilization of the nutrients and bioactive ingredients. The application of zein delivery systems for the encapsulation of bioactive ingredients has recently gained increasing interest. The aim of this work was to modify zein by pepsin and prepare the lutein-loaded zein nanoparticle (LZN) and the lutein-loaded zein hydrolysate nanoparticle (LZHN), respectively. The effects of zein hydrolysation on entrapment efficiency and in vitro digestion stability of lutein were also evaluated in this study. Hydrolysation of zein by the pepsin has important effects on lutein embedding. The optimal hydrolysis conditions, including the pepsin concentration (1.5%), temperature (55°C), and time (4 h), enhanced the entrapment efficiency (EE) of lutein by 93.82 ± 2.82% as compared to 85.18 ± 3.28% of the untreated zein, respectively. In contrast to LZN, LZHN had better structural characteristics, the average particle size decreases from 158.40 ± 3.22 nm to 112.2 ± 1.56 nm, and LZHN showed better dispersivity and zeta potential. The stability and release assays in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed that hydrolyzed zein nanocarriers by pepsin improved the digestion stability and promoted the release of lutein under gastrointestinal digestive conditions. These results suggest that hydrolyzed zein with pepsin may act as an effective carrier for lutein delivery and shows many potential advantages compared with the zein.

scholarly journals In Vitro Dissolution Evidence for Delivering Multiple Vitamin-Mineral Ingredients past the Stomach by Novel Capsule Delivery System (P24-009-19)

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Luke Bucci ◽  
Mastaneh Sharafi ◽  
Nima Alamdari
Keyword(s):  
Absorption Spectrometry ◽  
Gastric Fluid ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Magnesium Concentration ◽  
Simulated Gastric Fluid ◽  
Lauryl Sulfate ◽  
Simulated Intestinal Fluid ◽  
Tablet Disintegration

Abstract Objectives The ability of a novel beadlet-in-oil, gastric-resistant, vegetarian capsule containing a multiple vitamin-mineral (MVM) composition to deliver capsule contents past the stomach was tested by standard in vitro tablet disintegration procedures using magnesium as the marker of capsule contents dissolution. Methods A novel capsule design using a gastric-resistant vegetarian hypromellose/gellan gum capsule (DRcaps®, Capsugel®) was tested for disintegration in a standard tablet disintegration apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. The MVM ingredients were encapsulated into size 0 Vcaps® (hypromellose with no gastric acid resistance) and DRcaps®. Individual capsules were placed into chambers containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.0) for an additional 300 minutes. Aliquots were tested for magnesium concentration at ten time points by atomic absorption spectrometry. Results Magnesium was contained inside coated beadlets along with ferrous bisglycinate, methylcobalamin, 5-methyltetrahydrofolate, calcium fructoborate and cellulose. Vcaps® released 50% of the magnesium between 30–45 minutes and all by 60 minutes in the acid phase. DRcaps® released 25% of the magnesium at 45 minutes, and 43% at 120 minutes, followed by slow, steady release of the remaining magnesium by 420 minutes. Conclusions These dissolution profiles reproduce the known, rapid disintegration profile of Vcaps® when wetted. DRcaps® released the majority of their contents after the pH was changed to intestinal conditions, and then the beadlets released the water-soluble ingredients (magnesium) in a linear manner over a two hour period. Since normal stomach emptying of DRcaps® without a meal is less than 20–30 minutes (previously shown), DRcap® MVMs bypass the stomach almost completely to release ingredients in the small intestine. Thus, a novel, beadlet-in-oil, gastric-resistant capsule delivered its contents past the stomach. These properties have the ability to improve tolerability and thus, compliance with users. Funding Sources Capsugel®, Greenwood, SC, conducted this study for Ritual. Supporting Tables, Images and/or Graphs

Alginate-Inulin Hydrogel: Synthesis and Development for Targeted Delivery of Protein

2019 ◽  
Vol 16 (12) ◽  
pp. 4954-4959
Author(s):  
Norsyazwani Solehah Norudin ◽  
Hajaratul Najwa Mohamed ◽  
Nor Aisyah Mat Yahya
Keyword(s):  
Targeted Delivery ◽  
Protein Delivery ◽  
Drug Carrier ◽  
Physiological Saline ◽  
Gastric Fluid ◽  
Alginate Beads ◽  
Simulated Gastric Fluid ◽  
Simulated Intestinal Fluid ◽  
Good Efficiency ◽  
Ft Ir

Recently, a lot of strategies have been developed to enhance oral protein delivery. The combination of biodegradable polymer which is alginate-inulin as the material for hydrogel matrices was studied as a carrier of BSA which was used as a model protein. The effects of different formulations on the BSA release profile in physiological saline was investigated. Meanwhile, the compatibility of protein and polymer was characterized by FT-IR spectroscopy. High BSA encapsulation efficiency was found with the increase of inulin amount in the hydrogel matrices. The BSA release pattern showed that the minor released of BSA in simulated gastric fluid, SGF pH (1.2) throughout 2 hours’ incubation and after changing the solution into simulated intestinal fluid, SIF pH (7.4) the protein release started to increase gradually up to 100% within 90 minutes. Incorporation of inulin in the alginate beads also resulted in improved BSA release in physiological saline solution. In addition, swelling behavior revealed that highest swelling rate of hydrogel was in alkali solution indicating that alginate-inulin hydrogels were influenced by the pH of test medium. The FT-IR results show that encapsulating matrices are compatible with protein and can be used as drug carrier. Therefore, the alginate-inulin hydrogel showing a good efficiency in oral administration of protein drug.

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