scholarly journals DRUG RELEASE CONTROL AND ENHANCEMENT USING CARRIERS WITH DIFFERENT CONCENTRATIONS OF CAPMUL® MCM C8

2021 ◽  
pp. 249-252
Author(s):  
MOHAMMAD F. BAYAN
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Swelling Behavior ◽  
Release Formulation ◽  
Poorly Soluble ◽  
Model Drug

Objective: The main aim of this study was to design a drug carrier capable to control and enhance the release of poorly water soluble drugs. Methods: Three polymeric formulations, based on poly (2-hydroxyethyl methacrylate) and loaded with different Capmul® MCM C8 concentrations (0, 10 and 20 % w/w), were prepared. Felodipine, which is a poorly soluble substance, was selected as a model drug. The effect of Capmul® MCM C8 on swelling behavior and in vitro release profile of the prepared polymer was investigated in PBS. Results: The swelling profiles of allformulationswere statistically similar, which indicated the non-significant effect of added Capmul® MCM C8 on polymer's swelling behavior. All formulations showed a delayed drug release. Formulation-F3, which is loaded with 20% w/wCapmul® MCM C8 displayed a significant higher release compared to the other formulations. Conclusion: Capmul® MCM products, which are widely used in food industries, can be used to improve the oral delivery of poorly soluble substances. The optimized formulation exhibited the ability to control and enhance the release of the model drug.

scholarly journals Mechanical characterization of calcium pectinate hydrogel for controlled drug delivery

2003 ◽  
Vol 57 (12) ◽  
pp. 611-616 ◽  
Author(s):  
Jin Chung ◽  
Zhang Zhibing
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Release Profile ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Force Relaxation ◽  
Calcium Pectinate ◽  
Model Drug

Calcium pectinate beads, a paniculate hydrogel system, is an attractive drug carrier for oral delivery. In this study, a poorly water-soluble model drug indomethacin was incorporated into calcium pectinate beads made of different pectin concentrations, which were produced by an extrusion method. The effect of pectin concentration on bead size, circularity, swelling behavior, and mechanical properties, as well as in vitro drug release profile was investigated. The mechanical properties of calcium pectinate beads were determined by a micromanipulation technique. The drug release profile was measured using a standard British Pharmacopoeia method. It was found that the beads made of higher pectin concentration in general had a less permeable matrix structure and greater mechanical rigidity, although they swelled more after hydration. However, such an effect was not significant when the pectin concentration was increased to above 8%. Micromanipulation measurements showed that there was significant relaxation of the force being imposed on single hydrated beads when they were held, but this phenomenon did not occur on dry beads, which means that the force relaxation was dominated by liquid loss from the beads. The rate of the force relaxation was determined, and has been related to the release rate of the model drug entrapped in the calcium pectinate beads.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability

2020 ◽  
Vol 88 (4) ◽  
pp. 52
Author(s):  
Mona Qushawy ◽  
Ali Nasr ◽  
Shady Swidan ◽  
Yasmin Mortagi
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Production Yield ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Drug Content ◽  
Vitro Release

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial design. The prepared formulations were evaluated for production yield, drug content, micromeritic properties, thermal analysis, in-vitro release, and in-vivo hypoglycemic effect. All prepared formulations showed high production yield ranged from 98.4 ± 2.8 to 99.8 ± 2.2% and high drug content in the range of 97.2 ± 3.2 to 99.6 ± 2.1%. The micromeritic properties revealed that all prepared glimepiride formulations showed good flowability. The differential scanning calorimetry study revealed the presence of the drug in the more soluble amorphous form. In accordance with the results of in vitro release study, it was found that the solubility of glimepiride was increased by increasing the drug carrier ratio, compared with the pure form of the drug. It was found that F9 showed a high and rapid reduction in blood glucose levels in diabetic rats, which indicated the success of a solid dispersion technique in improving the solubility and hence the bioavailability of glimepiride.

scholarly journals Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis

2010 ◽  
Vol 60 (3) ◽  
pp. 255-266 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Nazia Khanam ◽  
Ch. Patra ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Polymer Concentration ◽  
Multiple Comparison ◽  
Prolonged Release ◽  
Comparison Analysis ◽  
Significant Difference

Preparation,in vitroandin vivoevaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysisIonotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigatedin vitrofor possible sustained drug release and their usein vivoas a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.

scholarly journals Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
V. J. Kapure ◽  
V. V. Pande ◽  
P. K. Deshmukh
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Weight Variation ◽  
Liquisolid Compacts ◽  
Rosuvastatin Calcium

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

scholarly journals Hydroxyapatite/nifuroxazide conjugate: Characterization, drug release and antimicrobial activity

2021 ◽  
pp. 40-40
Author(s):  
Zeljko Radovanovic ◽  
Katarina Mihajlovski ◽  
Lidija Radovanovic ◽  
Djordje Janackovic ◽  
Rada Petrovic
Keyword(s):  
Drug Release ◽  
Raw Materials ◽  
Drug Carrier ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Antibacterial Drug ◽  
Stomach Acid ◽  
Poorly Soluble ◽  
Good Biocompatibility

Synthetic hydroxyapatite (Ca10(PO4)6(OH)2, HAp) is very similar to the inorganic part of the bones and teeth of mammals. It is a well-known biomaterial with good biocompatibility, osteoconductivity and bioactivity. Nifuroxazide (C12H9N3O5, NFX) is a broad-spectrum antibacterial drug and poorly soluble in water. In order to increase the solubility of NFX, nanosized HAp powder and raw NFX drug were mixed giving, as a result, HAp/NFX conjugate. Characterization of the raw materials and the obtained conjugate confirmed the integration of NFX on the HAp surface. The in vitro study of drug release in simulated stomach acid and intestinal fluid showed a much faster release of NFX from HAp surface than those of raw drug. HAp/NFX conjugate showed an excellent inhibitory effect against Gram-positive bacterium Staphylococcus aureus, Gram-negative bacterium Escherichia coli and yeast Candida albicans, proving the nanosized HAp powder as a promising drug carrier.

scholarly journals Preparation and in vitro release kinetics of nitrendipine-loaded PLLA–PEG–PLLA microparticles by supercritical solution impregnation process

RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16167-16175 ◽  
Author(s):  
Shiping Zhan ◽  
Jingchang Wang ◽  
Weijing Wang ◽  
Liyun Cui ◽  
Qicheng Zhao
Keyword(s):  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Impregnation Process ◽  
Supercritical Solution ◽  
Model Drug ◽  
Polymer Microparticles ◽  
Kinetics Of ◽  
Vitro Release

In this work, drug-loaded polymer microparticles were prepared by a supercritical solution impregnation (SSI) process with nitrendipine as the model drug and PLLA–PEG–PLLA as the drug carrier.

Sign in / Sign up

Export Citation Format

Share Document