scholarly journals Investigation of Crystallization and Salt Formation of Poorly Water-Soluble Telmisartan for Enhanced Solubility

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 102 ◽  
Author(s):  
Chulhun Park ◽  
Nileshkumar Meghani ◽  
Yongkwan Shin ◽  
Euichaul Oh ◽  
Jun-Bom Park ◽  
...  
Keyword(s):  
Room Temperature ◽  
Gastric Fluid ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Distilled Water ◽  
Salt Formation ◽  
Intestinal Fluid ◽  
Salt Form ◽  
Enhanced Solubility ◽  
Poorly Water Soluble

The crystal changes and salt formation of poorly water-soluble telmisartan (TEL) in various solvents were investigated for enhanced solubility, stability and crystallinity. Polymorphic behaviors of TEL were characterized by dispersing in distilled water, acetone, acetonitrile, DMSO, or ethanol using Method I: without heat and then dried under vacuum at room temperature; and Method II: with heat below boiling temperature, cooled at 5 °C, and then dried under vacuum at 40 °C. For salt formation (Method III), the following four powdered mixtures were prepared by dispersing in solution of hydrochloric acid (HCl) (pH 1.2), TEL/HCl; in simulated gastric fluid (pH 1.2 buffer), TEL/simulated gastric fluid (SGF); in intestinal fluid (pH 6.8 buffer), TEL/simulated intestinal fluid (SIF); or in NaOH (pH 6.8), TEL/NaOH, respectively, and then dried under a vacuum at room temperature. The structures of powdered mixtures were then studied using a field emission scanning electron microscope (FESEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), FTIR, 1H nuclear magnetic resonance (1H-NMR), and LC–MS. The solubility of TEL in powdered forms was performed in pH 6.8, pH 1.2, and distilled water. No polymorphic behaviors of TEL were observed in various solvents as characterized by FESEM, DSC, PXRD, and FTIR. However, the structural changes of powdered mixtures obtained from Method III were observed due to the formation of salt form. Moreover, the solubility of salt form (TEL/HCl) was highly increased as compared with pure TEL. There were no significant changes of TEL/HCl compared with TEL in the content assay, PXRD, DSC, and FTIR during stressed storage conditions at 40 °C/75% relative humidity (RH) for 4 weeks under the closed package condition. Therefore, the present study suggests the new approach for the enhanced stability and solubility of a poorly water-soluble drug via salt form.

scholarly journals Biorelevant dissolution models to assess precipitation of weak base drug

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 2165-2172
Author(s):  
Viviane Annisa ◽  
Teuku Nanda Saifullah Sulaiman ◽  
Agung Endro Nugroho
Keyword(s):  
Small Intestine ◽  
Gastric Fluid ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Weak Base ◽  
Fluid Medium ◽  
Fed State ◽  
Fasted State ◽  
The Impact

The impact of precipitation can affect the amount of drug absorbed, thereby affecting the amount of drug in the systemic body. The precipitation process is preceded by a supersaturation phase, caused by decreased drug solubility in the gastrointestinal tract. This precipitation occurs for weak base drugs with low solubility. When the drug entering the small intestine, the solubility of weak base drugs decrease, then occurs supersaturation, which leads to precipitation, so that drug precipitation is one of a challenge for the pharmaceutical industry in drug development. Precipitation testing of water-soluble weak base drugs can be carried out by the pH shift method to describe the gastrointestinal pH gradient from gastric to small intestine. This pH change can cause supersaturation and then trigger precipitation, especially for weak base drugs. The methods that can used to assess precipitation drug is modification of the USP dissolution which are two compartment and multi compartment model. The choice of dissolution medium play an important role in the test results. The use of bio relevant medium can produce closer in vitro and in vivo correlations than the use of buffers. Generally, the medium used to simulate the weakly condition in the small intestine is FaSSIF (Fasted State Simulated Intestinal Fluid) or FeSSIF (Fed State Stimulate Intestinal Fluid) medium. The medium used to simulate the acidic condition in the stomach is FaSSGF (Fasted state simulated gastric fluid) or FeSSGF (Fed state simulated gastric fluid) medium.

scholarly journals Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics

2021 ◽  
Vol 71 (5) ◽  
pp. 393-409
Author(s):  
Earle Radha-Rani ◽  
Gadela Venkata-Radha
Keyword(s):  
Benzoic Acid ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
X Ray ◽  
Water Soluble Drug ◽  
Novel Approach ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were compared with the products formed by neat grinding (NG) and liquid assisted grinding (LAG) in their enhancement of solubility. The formation of CCs was confirmed by the IR spectroscopy, powder X-ray diffraction and thermal analysis methods. The saturation solubility studies indicate that the aqueous solubility of PPD-BA and PPD-PABA CCs was significantly improved to 1.343±0.162mg/ml and 1.964±0.452mg/ml, respectively, in comparison with the PPD solubility of 0.473mg/ml. This increase in solubility is 2.83-and 3.09-fold, respectively. PPD exhibited a poor dissolution of 37.8% in 60min, while the dissolution of the CCs improved tremendously to 96.07% and 89.65% in 60min. CCs of PPD with BA and PABA present a novel approach to overcome the solubility challenges of poorly water-soluble drug PPD.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

scholarly journals Formulation Optimization and Evaluation of Probiotic Lactobacillus sporogenes-Loaded Sodium Alginate with Carboxymethyl Cellulose Mucoadhesive Beads Using Design Expert Software

2016 ◽  
Vol 2016 ◽  
pp. 1-14 ◽  
Author(s):  
Himanshu K. Solanki ◽  
Dushyant A. Shah
Keyword(s):  
Carboxymethyl Cellulose ◽  
Room Temperature ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Pharmaceutical Products ◽  
Sodium Carboxymethyl Cellulose ◽  
Simulated Gastric Fluid ◽  
Formulation Optimization ◽  
Design Expert ◽  
Alginate Concentration

The present study deals with the formulation optimization of sodium carboxymethyl cellulose-alginate mucoadhesive beads containing probiotic Lactobacillus sporogenes through ionotropic gelation using 32 factorial design. The effect of sodium carboxymethyl cellulose-alginate concentration on the probiotic entrapment efficiency (PEE, %), viability in simulated gastric fluid (log CFU/g), and mucoadhesion over 8 hr (%) was optimized. The optimized beads containing probiotic Lactobacillus sporogenes showed entrapment efficiency of 93.7±1.97%, viability of probiotic in simulated gastric fluid (log CFU/g) of 9.34, mucoadhesion of 71.75±1.38%, and mean diameter of 1.21±0.11 mm. The beads were also characterized by SEM, FTIR, and XRD. The swelling and degradation of these beads were influenced by pH of the test medium. Finally, stability tests performed at room temperature (25~28°C) highlighted a bacterial viability of about 91% and 86% after 1 and 2 months, respectively. The advantageous properties of probiotic Lactobacillus sporogenes-loaded mucoadhesive beads make them suitable for incorporation in functional food and/or pharmaceutical products.

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. 

Design, Optimization and Evaluation of Repaglinide Self-Nanoemulsifying Drug Delivery for Enhanced Solubility

2017 ◽  
Vol 10 (6) ◽  
pp. 3920-3928
Author(s):  
Mahalaxmi K ◽  
Sailu Ch
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Antidiabetic Drug ◽  
Water Soluble Drug ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Capmul Mcm ◽  
Poorly Water Soluble Drug

The aim of study was to develop self-nanoemulsifying systems of poorly water-soluble drug repaglinide, which is an antidiabetic drug in the class of medications known as meglitinides. Solubility of repaglinide in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrysol K 150, Kolliphor EL and Capmul MCM were selected as oil, surfactant and co-surfactant respectively. Formulation F8 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, SNEDDS were found to be influential in improving the release performance of repaglinide, indicating their potential to improve the solubility and oral bioavailability of repaglinide.  

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).

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