Enhancing In Vitro Bioavailability of Berberine by Incorporation of Beta–Cyclodextrin Complex into Solid Dispersion System

2021 ◽  
pp. 301-314
Author(s):  
Hang Thu Than ◽  
Thuy Phan-Quoc Nguyen ◽  
Phat Dong Le ◽  
Phi Hong Tran ◽  
Van Hong Nguyen
Keyword(s):  
Solid Dispersion ◽  
Cyclodextrin Complex ◽  
Dispersion System ◽  
Beta Cyclodextrin

scholarly journals In Vitro Stability and in Vivo Absorption Studies of Colloidal Particles Formed from a Solid Dispersion System.

1996 ◽  
Vol 44 (12) ◽  
pp. 2309-2313 ◽  
Author(s):  
Katsuhiko YANO ◽  
Atsushi KAJIYAMA ◽  
Shigeru YAMAZAKI ◽  
Yoshisuke MATSUMURA ◽  
Kouji WATANABE ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Colloidal Particles ◽  
Dispersion System ◽  
Absorption Studies ◽  
In Vivo Absorption ◽  
In Vitro Stability

Beta-Cyclodextrin and Maltodextrin Based Solid Dispersion of Meloxicam to Enhance the Solubility of Meloxicam; Formulation and In-vitro Evaluation

2019 ◽  
Vol 41 (1) ◽  
pp. 133-133
Author(s):  
Muhammad Zaman Muhammad Zaman ◽  
Muhammad Hanif Muhammad Hanif ◽  
Syed Saeed Ul Hassan Syed Saeed Ul Hassan ◽  
Javed Iqbal and Muhammad Ahmad Shehzad Javed Iqbal and Muhammad Ahmad Shehzad
Keyword(s):  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
X Ray ◽  
Beta Cyclodextrin ◽  
Release Studies ◽  
Pure Drug

The purpose of the current study was to enhance the solubility of the meloxicam (MLX) by preparing complex with β-Cyclodextrin (CD) and maltodextrin (MD). Dextrins have the ability to capture the drug inside their cavities without forming any chemical bonding. Three (3) formulations, each of solid dispersion (SD) and physical mixture (PM) were prepared by using different drug to polymer ratios (1:4, 1:6 and 1:8) followed by evaluation for micromeritic properties, drug contents, and in vitro drug release studies, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and x-ray diffraction (XRD) studies. Chemical compatibility of the ingredients was evaluated by using Fourier transform infrared spectroscopy (FTIR). Results of conducted studies exposed excellent flow properties of SDs as well as prepared PMs, with reasonable amount of loaded drug, i.e. andgt;90%. SEM showed a bit irregular surface while XRD suggested crystalline behavior of pure drug, which was masked after its conversion into SDs and PMs based on dextrins. Solubility of the MLX was increased significantly form its initial extent of solubility i.e. 12.5 and#181;g/ml in pure form to 786.72 and#181;g/ml in the form of SD (pandlt;0.05), advocating suitability of materials and methods for solubility enhancement of MLX.

scholarly journals IMPROVEMENT OF DISSOLUTION RATE OF VALSARTAN BY SOLID DISPERSION SYSTEM USING D(−) MANNITOL

2017 ◽  
Vol 10 (3) ◽  
pp. 288 ◽  
Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Type I ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Dispersion System ◽  
Grinding Technique

ABSTRACTObjective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach.Methods: Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid statecharacterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior(differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USPdissolution apparatus type I at a temperature of 37±0.5°C.Results: Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan.Conclusion: Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.

scholarly journals Preparation and Physicochemical Characterization of Solid Dispersion of Irbesartan with Poloxamer 188

2020 ◽  
Vol 8 (A) ◽  
pp. 16-19
Author(s):  
Fifi Harmely ◽  
Salman Umar ◽  
Yufri Aldi ◽  
Ellyza Nasrul ◽  
Erizal Zaini
Keyword(s):  
Dissolution Rate ◽  
Powder Diffraction ◽  
Solid Dispersion ◽  
Degree Of Crystallinity ◽  
In Vitro Dissolution ◽  
Poloxamer 188 ◽  
X Ray ◽  
Dispersion System ◽  
Ft Ir

AIM: The aim of the present study was to prepare and characterize the solid dispersion of poorly soluble drugs irbesartan with hydrophilic polymer poloxamer 188 by solvent co-evaporation technique. METHODS: The ratio of irbesartan to poloxamer 188 in solid dispersion system was 1:0.5; 1:1; and 1:3. Physicochemical properties characterization was analyzed by X-ray powder diffraction, Fourier-transform infrared (FT-IR) spectroscopy, differential thermal analysis, and scanning electron microscopy (SEM). The in vitro dissolution rate profile of solid dispersion was performed by Type II United States Pharmacopeia dissolution testing apparatus. RESULTS: The results of the X-ray powder diffraction pattern showed that the degree of crystallinity of irbesartan crystalline phase reduced in a solid dispersion system. FT-IR spectra indicate that there is no chemical interaction between irbesartan and poloxamer 188 in a solid dispersion system. SEM microscopy demonstrated a homogenous phase of a solid dispersion system with distinct crystal habit. In general, in vitro dissolution rate of all solid dispersions was higher than intact irbesartan. The highest percentage of dissolved irbesartan was the solid dispersion of irbesartan-poloxamer 188 (1:0.5 w/w). CONCLUSIONS: The study concludes that the solid dispersion can be applied to improve the dissolution rate of irbesartan.

scholarly journals In Vitro Evaluation of Cholesterol-Reducing Ability of Chitosan from Mangrove Crab (Scylla serrata) Shell Solid Dispersion using PVP K-30 as a Carrier

2021 ◽  
Vol 7 (2) ◽  
pp. 99-109
Author(s):  
Hilya Nur Imtihani ◽  
Silfiana Nisa Permatasari ◽  
Rahmad Aji Prasetya
Keyword(s):  
Solid Dispersion ◽  
Positive Control ◽  
Scylla Serrata ◽  
Total Serum ◽  
In Vitro Evaluation ◽  
Dispersion System ◽  
Cholesterol Levels ◽  
Mangrove Crab ◽  
Reducing Ability

Background: Chitosan is a compound that can be synthesized from nature which can reduce the total serum cholesterol levels between 5.8−42.6% and decrease LDL (Low-Density Lipoprotein) between 15.1-35.1%. One of the natural resources containing chitosan derivative compounds is the shell of mud crab. Chitosan is insoluble in water but soluble in acidic solutions such as acetic acid. With such chitosan solubility, it is necessary to increase the solubility by making a solid dispersion system so that drug absorption can be faster. Objectives: The aims of this study is to determine the potential of chitosan solid dispersion system for reducing cholesterol. Material and Methods: The reduction of cholesterol levels was carried out by in vitro tests using UV-Vis spectrophotometer at a wavelength of 405 nm with Lieberman-Burchad reagent. The positive control used was simvastatin. There are 4 formulas, namely SD1, PM1, SD2, and PM2. This solid dispersion system uses polyvinyl pyrrolidone K-30 (PVP K-30) as carrier. Results: The characterization of chitosan has fulfilled all the characterization requirements that is organoleptic (shape and color) was creamy white, moisture content was 2.15%, ash content was 1.14%, ninhydrin test was positive purple, and deacetylation degree was 70.57%. The results of in vitro evaluation were obtained a dark green solution. The reducing percentage in cholesterol levels are SD1: 18.44%; PM1 : 18.11%; SD2 : 29.57%; and PM2 :12.01%. Simvastatin as a positive control has a percentage reduction in cholesterol levels of 30.07%.  Conclusion: Chitosan has an activity as anticholesterol agent. SD2 (Solid Dispersion Chitosan: PVP K-30 = 1:2) has the higher percentage than other formulas for reducing cholesterol level comparable with the positive control.

Injectable in-situ Forming Depot Of Doxycycline Hyclate/α-Cyclodextrin Complex using PLGA for Periodontitis Treatment: Preparation, Charac-terization, and In-Vitro Evaluation

2020 ◽  
Vol 17 ◽  
Author(s):  
Elham Khodaverdi ◽  
Farhad Eisvand ◽  
Mohammad Sina Nezami ◽  
Seyedeh Nesa Rezaeian Shiadeh ◽  
Hossein Kamali ◽  
...  
Keyword(s):  
Complex Form ◽  
Docking Studies ◽  
Morphological Properties ◽  
Burst Release ◽  
Cyclodextrin Complex ◽  
Doxycycline Hyclate ◽  
Scanning Calorimetry ◽  
In Situ Forming

Background:: Doxycycline (DOX) is used in treating a bacterial infection, especially for periodontitis treatment. Objective: To reduce irritation of DOX for subgingival administration and increase the chemical stability and against enzy-matic, the complex of α-cyclodextrin with DOX was prepared and loaded into injectable in situ forming implant based on PLGA. Methods:: FTIR, molecular docking studies, X-ray diffraction, and differential scanning calorimetry was performed to char-acterize the DOX/α-cyclodextrin complex. Finally, the in-vitro drug release and modeling, morphological properties, and cellular cytotoxic effects were also evaluated. Results:: The stability of DOX was improved with complex than pure DOX. The main advantage of the complex is the al-most complete release (96.31 ± 2.56 %) of the drug within 14 days of the implant, whereas in the formulation containing the pure DOX and the physical mixture the DOX with α-cyclodextrin release is reached to 70.18 ± 3.61 % and 77.03 ± 3.56 %, respectively. This trend is due to elevate of DOX stability in the DOX/ α-cyclodextrin complex form within PLGA implant that confirmed by the results of stability. Conclusion:: Our results were indicative that the formulation containing DOX/α-cyclodextrin complex was biocompatible and sustained-release with minimum initial burst release.

Sign in / Sign up

Export Citation Format

Share Document