scholarly journals Penetration Driving Force of Metformin Hydrochloride via Paracellular Pathway in Relation to its Pharmacodynamic Effect

2021 ◽  
Author(s):  
Omar Y. Mady ◽  
Adam A. Al-Shoubki ◽  
Ahmed A. Donia ◽  
Waseem Qasim
Keyword(s):  
Driving Force ◽  
Paracellular Pathway ◽  
Sorbitan Monostearate ◽  
Absorption Enhancement ◽  
Metformin Hydrochloride ◽  
Total Drug ◽  
Pharmacodynamic Effect ◽  
Drug Permeation ◽  
Drug Products ◽  
The Matrix

Abstract Background: Penetration enhancement of metformin hydrochloride via its molecular dispersion in sorbitan monostearate microparticles is reported. Metformin dispersion in sorbitan monostearate as a carrier was thought to be the basic philosophy to maximize its entrapment in the matrix for maximum penetration effect.Methods: Drug dispersion in sorbitan monostearate with different theoretical drug contents (TDC) were prepared. Results: All products showed excellent micromeritics and actual drug content (ADC) increased by increasing TDC. These two features are essential for industry concerning processing and cost. The partition coefficient of the drug products showed huge improvement. This indicates the drug entrapment should be in the polar part of sorbitan monostearate as a special image. The drug entrapment process was also reflected in the drug release process due to the insolubility of the matrix in the dissolution medium. The drug permeation profiles from the different drug-sorbitan monostearate products are overlapped and its permeation parameters (permeation coefficient, total drug permeation percent & drug absorption enhancement percent) are nearly equal. The results of the permeation study by using modified non-everted sac suggested the main driving force for 11 improving the drug paracellular pathway is its dispersion in sorbitan monostearate (special image) and is independent of ADC. Pharmacodynamic of the drug products showed a significant improvement than that from the drug alone at p ˂ 0.05. ANOVA test indicated the insignificant pharmacodynamic difference between the low, middle, and high ADC of the products. There is an excellent point-to-point correlation between the drug permeation percent and the drug pharmacodynamic percent. The total amount of the drug permeation percent is equal to the mean of the total drug pharmacodynamic percent. Conclusion: The results concluded that the drug permeation driving force via the paracellular pathway is its entrapment in sorbitan monostearate as a special image and it does not depend on ADC. This entrapment mechanism improved the drug pharmacodynamic effect. The technique is simple and the products are easy to process due to having an excellent micromeritics property.

scholarly journals Metformin hydrochloride entrapment in sorbitan monostearate for intestinal permeability enhancement and pharmacodynamics

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Omar Y. Mady ◽  
Adam A. Al-Shoubki ◽  
Ahmed A. Donia ◽  
Waseem Qasim
Keyword(s):  
Driving Force ◽  
Paracellular Pathway ◽  
Sorbitan Monostearate ◽  
Metformin Hydrochloride ◽  
Drug Permeation ◽  
Drug Products ◽  
Penetration Effect ◽  
Permeability Enhancement ◽  
Drug Dispersion ◽  
Maximum Penetration

AbstractPenetration enhancement of metformin hydrochloride via its molecular dispersion in sorbitan monostearate microparticles is reported. This represents basic philosophy to maximize its entrapment for maximum penetration effect. Drug dispersion in sorbitan monostearate with different theoretical drug contents (TDC) were prepared. Products showed excellent micromeritics and actual drug content (ADC) increased by increasing TDC. The partition coefficient of the drug products showed huge improvement. This indicates the drug entrapped in the polar part of sorbitan monostearate as a special image which effects on the drug release. The drug permeation profiles from the different products are overlapped with nearly equal permeation parameters. The permeation results suggested the main driving force for improving the drug paracellular pathway is its dispersion in sorbitan monostearate and is independent of ADC. Pharmacodynamic of the products showed a significant improvement than the drug alone at p ˂ 0.05. ANOVA test indicated the insignificant pharmacodynamic difference between the low, middle, and high ADC of the products. An excellent correlation founded between the drug permeation and pharmacodynamic precents. Drug permeation driving force via the paracellular pathway is its entrapment in sorbitan monostearate and independent on ADC. The technique is simple and the products had excellent micromeritics.

scholarly journals Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 174
Author(s):  
Rebeca Simancas-Herbada ◽  
Ana Fernández-Carballido ◽  
Juan Aparicio-Blanco ◽  
Karla Slowing ◽  
Jorge Rubio-Retama ◽  
...  
Keyword(s):  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Metformin Hydrochloride ◽  
Oral Toxicity ◽  
Crosslinking Degree ◽  
Polymer Swelling ◽  
Hydrophilic Drugs ◽  
Swelling Capacity ◽  
The Matrix ◽  
Model Drug

The potential of a new poly(magnesium acrylate) hydrogel (PAMgA) as a pharmaceutical excipient for the elaboration of matrix tablets for the extended release of highly hydrophilic drugs was evaluated. The polymer was synthetized with two different crosslinking degrees that were characterized by FTIR and DSC. Their acute oral toxicity was determined in a mouse model, showing no toxicity at doses up to 10 g/kg. Matrix tablets were prepared using metformin hydrochloride as a model drug and the mechanisms involved in drug release (swelling and/or erosion) were investigated using biorrelevant media. This new hydrogel effectively controlled the release of small and highly hydrophilic molecules as metformin, when formulated in matrix tablets for oral administration. The rate of metformin release from PAMgA matrices was mainly controlled by its diffusion through the gel layer (Fickian diffusion). The swelling capacity and the erosion of the matrix tablets influenced the metformin release rate, that was slower at pH 6.8, where polymer swelling is more intensive, than in gastric medium, where matrix erosion is slightly more rapid. The crosslinking degree of the polymer significantly influenced its swelling capacity in acid pH, where swelling is moderate, but not in intestinal fluid, where swelling is more intense.

Electrochemical Corrosion Behavior of Different Graphite Shapes Cast Irons in Acidic Solution

2014 ◽  
Vol 906 ◽  
pp. 275-282
Author(s):  
Zhu Huan Yu ◽  
Jun Feng Qiang ◽  
Hui Lu Li
Keyword(s):  
Electron Microscopy ◽  
Corrosion Resistance ◽  
Corrosion Behavior ◽  
Driving Force ◽  
Acidic Solution ◽  
Electrochemical Corrosion ◽  
White Iron ◽  
Cast Irons ◽  
The Matrix ◽  
Electrochemical Corrosion Behavior

The effect of graphite shapes on the electrochemical corrosion behavior of cast iron was studied by means of weight loss tests, electrochemical measurements and electron microscopy. It was found that the electrochemical corrosion behavior of graphite is significantly different from one other, and the corrosive potential difference between carbide ad the matrix is the main driving force of the different phase corrosions. Among them, the center A type and edge D type graphite exhibited the highest corrosion resistance. The corrosion of white iron is worst, because there are so many type carbides in white iron and so there is an obvious tendency to produce micro-cell in white iron.

Embrittlement of Cracks at Interfaces

1995 ◽  
Vol 408 ◽  
Author(s):  
Robb Thomson ◽  
Emeritus ◽  
A. E. Carlsson
Keyword(s):  
Chemical Bonding ◽  
Driving Force ◽  
Driving Forces ◽  
Interface Analysis ◽  
Analytic Approximations ◽  
The Matrix ◽  
Block Construction ◽  
Lattice Resistance

AbstractThis paper presents a synopsis of already published work for cracks on interfaces and new results on the effect of changing the chemistry of the atoms at the interface. Once the appropriate cut-off for the oscillatory singularity in the interface analysis is determined, the physics of the crack is determined in terms of an appropriate driving force for a particular event of interest, and a lattice resistance to the event. Analytic approximations are available for the driving forces, and the lattice resistance is determined on the basis of a block construction for the lattice. We show that for the case where the chemical bonding at the interface is different from that in the matrix, the same ideas are applicable, provided the different chemistry is incorporated correctly in the lattice resistance construction.

Embrittlement of Cracks at Interfaces.

1995 ◽  
Vol 409 ◽  
Author(s):  
Robb Thomson Emeritus ◽  
A. E. Carlsson
Keyword(s):  
Chemical Bonding ◽  
Driving Force ◽  
Driving Forces ◽  
Interface Analysis ◽  
Analytic Approximations ◽  
The Matrix ◽  
Block Construction ◽  
Lattice Resistance

AbstractThis paper presents a synopsis of already published work for cracks on interfaces and new results on the effect of changing the chemistry of the atoms at the interface. Once the appropriate cut-off for the oscillatory singularity in the interface analysis is determined, the physics of the crack is determined in terms of an appropriate driving force for a particular event of interest, and a lattice resistance to the event. Analytic approximations are available for the driving forces, and the lattice resistance is determined on the basis of a block construction for the lattice. We show that for the case where the chemical bonding at the interface is different from that in the matrix, the same ideas are applicable, provided the different chemistry is incorporated correctly in the lattice resistance construction.

Influence of Cr Content on Cellular Precipitation Behaviour of Ni-38Cr-3.8Al Alloy with Lamellar Structure

2018 ◽  
Vol 941 ◽  
pp. 1203-1209 ◽  
Author(s):  
Yoshihiko Koyanagi ◽  
Hiroyuki Takabayashi ◽  
Hiroyuki Y. Yasuda
Keyword(s):  
Driving Force ◽  
Lamellar Structure ◽  
Annealing Treatment ◽  
Al Alloy ◽  
Precipitation Reaction ◽  
Cellular Precipitation ◽  
Gamma Prime ◽  
Precipitation Behaviour ◽  
The Matrix ◽  
Cr Concentration

Ni-Cr binary alloys containing high amount of Cr demonstrate gamma/alpha-Cr lamellar structure by discontinuous precipitation (DP) reaction from grain boundary. The mechanism of DP reaction is caused by supersaturated Cr in the gamma phase. Supersaturated Cr concentration influences the driving force for the DP reaction and the lamellar spacing. Moreover, the Ni-based alloys with high Cr, containing Al, significantly increase the hardness and strength due to the very narrow lamellar structure. Al addition brings on Ni consumption in the matrix by precipitation of the gamma prime phase. Therefore, Cr supersaturates dramatically in the matrix. The wrought Ni-Cr-Al alloy, Ni-38Cr-3.8Al (mass%) , reaches extremely high tensile strength, which is over 2 GPa, after annealing treatment. Even though chemical composition of Ni-38Cr-3.8Al is simple, the microstructure is complex because it consists of the gamma/alpha Cr lamellar structure with the fine gamma prime particles. Therefore, in this study, we investigated the influence of Cr concentration on the cellular precipitation behaviour. In order to understand the influence of Cr concentration, Ni-34, 36 and 38Cr-3.8Al alloys were prepared. Forged bars were subjected to solution treatment in the gamma single phase region. Subsequently, the alloys were aged from 873K to 1073 K for various times. The cellular precipitation reaction is suppressed by a decrease in Cr concentration, particularly at low temperature annealing treatment condition. The hardness is low in lower Cr concentration alloys in all range of annealing treatment temperature. These results indicate that Cr concentration remarkably affects the driving force for the DP reaction.

scholarly journals Development and Validation of an HPLC Stability-Indicating Method for Identification and Assay of Elemental Iron(II) in Pharmaceutical Drug Products Using Reversed-Phase HPLC

2011 ◽  
Vol 94 (4) ◽  
pp. 1233-1239
Author(s):  
Neil C Dias ◽  
Abu M Rustum
Keyword(s):  
Ferrous Sulfate ◽  
Methanesulfonic Acid ◽  
Reversed Phase ◽  
Hplc Method ◽  
Elemental Iron ◽  
Stability Indicating ◽  
Drug Products ◽  
Stability Indicating Method ◽  
The Matrix ◽  
Development And Validation

Abstract Ferrous sulfate tablets are a supplementary iron source for people who suffer from iron defciency anemia. A simple, fast, and QCfriendly HPLC method was developed and validated to determine elemental iron in ferrous sulfate drug products. A TSK-GEL Super octadecylsilyl column (50 × 4.6 mm id, 2 µm particle size) with a mobile phase consisting of 0.06 M methanesulfonic acid in water–acetonitrile (40 + 60, v/v) and UV detection at 282 nm were used for this method. Separation of the elemental iron peak from the matrix was achieved within 5 min. This method was successfully validated according to International Conference on Harmonization guidelines, and shown to be stability-indicating for the shelf-life samples of ferrous sulfate tablets, as well as selective for the analyte of interest.

scholarly journals Stability Matrix Designs: A Boon For Stability Testing of Pharmaceutical Drug Products.

2019 ◽  
Vol 9 (4-s) ◽  
pp. 839-843
Author(s):  
Rada Santosh Kumar ◽  
P. Swetha
Keyword(s):  
Search Algorithm ◽  
Storage Condition ◽  
Storage Conditions ◽  
Dose Inhaler ◽  
Matrix Approach ◽  
Meter Dose Inhaler ◽  
Drug Products ◽  
The Matrix ◽  
The Stability ◽  
Expiration Dating

Long term stability is done in a matrix approach after manufacturing of drug for ensuring the stability of drugs. Using the matrix basic design which is useful for testing 3 lots under one storage condition can be expanded to multiple presentation of products or multiple storage conditions. The design shows full testing at the end points (0 and 36 months) and shows partial testing at the interim time points (3, 6, 9, 12, 18 &24 min). With the assistance of a statistical search algorithm, the test points are selected . 37.5%  reduction in analytical testing, while permitting a reliable interim expiry estimate. Based on 12 months stability data it is provided by the proposed matrix design. The matrix approach obtained by expiration dating periods is typically more conservative than the approaches derived from the full testing estimate. The comparison of expiration dating estimate for meter dose inhaler and capsules is presented using the matrixed and full testing approaches.

scholarly journals Quality assessment of nine brands of metformin hydrochloride tablets marketed in Abuja, Nigeria

2021 ◽  
Vol 18 (3) ◽  
pp. 216-222
Author(s):  
Olubukola A. Odeniran1, ◽  
Olubunmi J. Olayemi ◽  
Isa H. Galadima, ◽  
Rukaiyatu A. Kirim ◽  
Christianah Y. Isimi ◽  
...  
Keyword(s):  
Active Ingredient ◽  
Type Ii Diabetes ◽  
Type Ii Diabetes Mellitus ◽  
In Vitro Dissolution ◽  
Metformin Hydrochloride ◽  
Disintegration Time ◽  
Drug Products ◽  
First Choice

Metformin is a drug of first choice in management of type II diabetes mellitus and the Nigerian market is flooded with many brands of metformin tablets. The aim of this study is to assess the pharmaceutical quality of nine brands of metformin tablets circulating in pharmacy outlets in Abuja. The brands were assessed for uniformity in weight, hardness, friability, disintegration time and in vitro dissolution using official methods. The content of active ingredient was also determined spectrophotometrically. All the brands had weights within the official limits, hardness was found to differ across the brands with values ranging between 1.20 and 11.50 kgF. Friability values were between 0.00 and 2.25%, disintegration time was between 2.06 and 10.36 min and within official specifications for film-coated tablets. Drug release within 60 min was between 93 and 103%, however, one of the brands fell outside the lower limit of the official specification and therefore, failed the dissolution test. Similarly, all but one of the brands were within the official specification of the percent content of active ingredient. The results highlight the need to routinely carry out market surveillance on drug products so as to safeguard the health of patients.

scholarly journals Calorimetric Investigation of the Relaxation Phenomena in Amorphous Lyophilized Solids

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1735
Author(s):  
Sebastian Groёl ◽  
Tim Menzen ◽  
Gerhard Winter
Keyword(s):  
Thermal History ◽  
Drug Product ◽  
Scanning Calorimetry ◽  
Calorimetric Methods ◽  
Drug Products ◽  
Relevant Today ◽  
Freeze Dried ◽  
The Matrix ◽  
Amorphous Drug ◽  
Calorimetric Investigations

Studying the thermal history and relaxation of solid amorphous drug product matrices by calorimetry is a well-known approach, particularly in the context of correlating the matrix parameters with the long-term stability of freeze-dried protein drug products. Such calorimetric investigations are even more relevant today, as the application of new process techniques in freeze-drying (which strongly influence the thermal history of the products) has recently gained more interest. To revive the application of calorimetric methods, the widely scattered knowledge on this matter is condensed into a review and completed with new experimental data. The calorimetric methods are applied to recent techniques in lyophilization, such as controlled nucleation and aggressive/collapse drying. Phenomena such as pre-Tg events in differential scanning calorimetry and aging shoulders in isothermal microcalorimetry are critically reviewed and supplemented with data of freeze-dried products that have not been characterized with these methods before.

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