scholarly journals Polymorphism in Commercial Sources of Fusidic Acid: A Comparative Study of the In Vitro Release Characteristics of Forms I and III from a Marketed Pharmaceutical Cream

2017 ◽  
Vol 2017 ◽  
pp. 1-7
Author(s):  
Jonathan Byrne ◽  
Robert Reinhardt ◽  
Trinidad Velasco-Torrijos
Keyword(s):  
Fusidic Acid ◽  
Drug Product ◽  
In Vitro Release ◽  
Inert Atmosphere ◽  
Drug Substance ◽  
Intrinsic Dissolution ◽  
Polymorphic Forms ◽  
Commercial Sources ◽  
The Stability

A comparison of the polymorphic forms of 3 commercial sources of fusidic acid using FTIR and XRPD techniques has been performed in this study. It has been demonstrated that polymorphic Forms I and III are currently available on the commercial market. The influence of the observed polymorphism on the stability of the drug substance in bulk form has been investigated through stability and stress testing according to current ICH guidelines. Significant differences were detected between commercial sources with regard to the stability of the bulk substance under photolytic and humidity stress conditions. When properly packaged in an inert atmosphere, fusidic acid from all 3 manufacturers showed a comparable stability. The effects of the observed polymorphic differences on the intrinsic dissolution rate of the drug substance and its in vitro release from the marketed drug product Fusicutan® plus Betamethasone cream have been investigated. Results indicated that the release rate of the drug substance is similar for polymorphic Forms I and III, allowing both forms to be used during manufacture without affecting the safety or efficacy of the drug product.

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

scholarly journals 75 Evaluating the in vitro release of essential oils from microparticles in simulated swine gastric and intestinal fluids and the essential oil stability in microparticles during feed pelleting process

2019 ◽  
Vol 97 (Supplement_3) ◽  
pp. 70-70
Author(s):  
Janghan Choi ◽  
Lucy Wang ◽  
Joshua Gong ◽  
Ludovic Lahaye ◽  
Song Liu ◽  
...  
Keyword(s):  
Essential Oil ◽  
Essential Oils ◽  
In Vitro Release ◽  
Oil Stability ◽  
Positive Effects ◽  
Intestinal Fluids ◽  
Gastric Fluids ◽  
The Stability ◽  
Vitro Release

Abstract Essential oils are defined as plant-derived natural bioactive compounds with positive effects on animal growth and health due to their antimicrobial and antioxidative properties. However, essential oils are very volatile, can evaporate rapidly and be rapidly absorbed in the upper gastrointestinal tract. In addition, due to their labile nature, the stability of essential oils during feed processing is often questionable, leading to variable final concentrations in feeds. Micro-encapsulation has become one of the most popular methods to deliver essential oils into the lower gut. The objective of the present study was double: 1) to validate and demonstrate the slow release of essential oils, such as thymol, micro-encapsulated in combination with organic acids in a matrix of triglycerides, in simulated swine gastric and intestinal fluids and 2) to evaluate the essential oil stability in the microparticles during feed pelleting process. In the in vitro release experiments, the microparticles were incubated in simulated gastric fluids for 2 hours and then the samples were incubated in simulated intestinal fluids for 0, 1, 2, 3, 4, 6, 8, 10, and 24 hours at 39°C. In the pelleting experiment, a wheat-corn basal diet with 2 kg of micro-encapsulated product was formulated and pelleted. The thymol content in the samples was analyzed by gas chromatography with flame-ionization detection. The results showed that 27.65% thymol was released in simulated gastric fluids and the rest of thymol was progressively released in intestinal fluids until completion, which was achieved by 24 hours. The thymol concentration was not significantly different between the mash feeds and pelleted feeds (P > 0.05). In conclusion, the micro-encapsulated organic acid and essential oil product was able to maintain the stability of thymol under a commercial pelleting process and allow a slow and progressive release of its active ingredients as thymol in simulated digestive fluids.

scholarly journals Pre-Formulation Studies: Physicochemical Characteristics and In Vitro Release Kinetics of Insulin from Selected Hydrogels

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1215
Author(s):  
Aneta Ostróżka-Cieślik ◽  
Małgorzata Maciążek-Jurczyk ◽  
Jadwiga Pożycka ◽  
Barbara Dolińska
Keyword(s):  
Release Kinetics ◽  
Polymer Network ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Diabetic Patients ◽  
Tertiary Structures ◽  
Duration Of Action ◽  
The Stability

Insulin loaded to the polymer network of hydrogels may affect the speed and the quality of wound healing in diabetic patients. The aim of our research was to develop a formulation of insulin that could be applied to the skin. We chose hydrogels commonly used for pharmaceutical compounding, which can provide a form of therapy available to every patient. We prepared different gel formulations using Carbopol® UltrezTM 10, Carbopol® UltrezTM 30, methyl cellulose, and glycerin ointment. The hormone concentration was 1 mg/g of the hydrogel. We assessed the influence of model hydrogels on the pharmaceutical availability of insulin in vitro, and we examined the rheological and the texture parameters of the prepared formulations. Based on spectroscopic methods, we evaluated the influence of model hydrogels on secondary and tertiary structures of insulin. The analysis of rheograms showed that hydrogels are typical of shear-thinning non-Newtonian thixotropic fluids. Insulin release from the formulations occurs in a prolonged manner, providing a longer duration of action of the hormone. The stability of insulin in hydrogels was confirmed. The presence of model hydrogel carriers affects the secondary and the tertiary structures of insulin. The obtained results indicate that hydrogels are promising carriers in the treatment of diabetic foot ulcers. The most effective treatment can be achieved with a methyl cellulose-based insulin preparation.

scholarly journals Effect of Doxycycline Microencapsulation on Buccal Films: Stability, Mucoadhesion and In Vitro Drug Release

Gels ◽  
2021 ◽  
Vol 7 (2) ◽  
pp. 51
Author(s):  
Venu Gopal Reddy Patlolla ◽  
Nikolina Popovic ◽  
William Peter Holbrook ◽  
Thordis Kristmundsdottir ◽  
Sveinbjörn Gizurarson
Keyword(s):  
Tensile Strength ◽  
Room Temperature ◽  
In Vitro Release ◽  
Sodium Thiosulfate ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Metalloproteinase Inhibitors ◽  
The Stability ◽  
Buccal Films

The aim of this work was to stabilize doxycycline in mucoadhesive buccal films at room temperature (25 °C). Since doxycycline is susceptible to degradation such as oxidation and epimerization, tablets are currently the only formulation that can keep the drug fully stable at room temperature, while liquid formulations are limited to refrigerated conditions (4 °C). In this study, the aim was to make formulations containing subclinical (antibiotic) doxycycline concentration that can act as matrix metalloproteinase inhibitors (MMPI) and can be stored at temperatures such as 25 °C. Here, doxycycline was complexed with excipients using three techniques and entrapped into microparticles that were stored at 4 °C, 25 °C and 40 °C. Effect of addition of precomplexed doxycycline microparticles on films: stability mucoadhesion capacity, tensile strength, swelling index and in vitro release was studied. The complexation efficiency between drug-excipients, microparticles and films was studied using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Two of the films were found to be stable at 4 °C but the film containing microparticle composed of precomplexed doxycycline with β-cyclodextrin, MgCl2, sodium thiosulfate, HPMC and Eudragit® RS 12.5 was found to be stable at 25 °C until 26 weeks. The addition of microparticles to the films was found to reduce the mucoadhesive capacity, peak detachment force, tensile strength and elasticity, but improved the stability at room temperature.

scholarly journals Consequence of ANASTROZOLE on Chemo therapy

2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Saritha Garrepalli
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Scanning Calorimetry ◽  
Ir Studies ◽  
Release Studies ◽  
Ft Ir ◽  
The Mean ◽  
Pure Drug ◽  
The Stability

Prepared nanoparticles were characterized in terms of particle size, scanning electron microscope (SEM), fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In-vitro release studies were performed in phosphate buffer saline pH 7.4 at 37˚±0.5˚C for 1month. The mean particle size of obtained nanoparticles was 150-400 nm and was apparently spherical in shape, with smooth surface. DSC is done for the stability test for pure drug and sample. The thermogram of drug has not shifted for in the formulation compare to pure drug thermogram hence, the stability of formulation is not changed. FT-IR studies demonstrated that the drug was not changed in the formulation during the fabrication process.The encapsulation efficiency was about 48%. The Anastrozole-BSA nanoparticles exhibit a most interesting release profile with small initial burst followed by slower and controlled release.

scholarly journals The investigation of polymorph transition of erlotinib salts

2016 ◽  
Author(s):  
Wioleta Maruszak ◽  
Marta Łaszcz ◽  
Kinga Trzcińska ◽  
Wojciech Łuniewski ◽  
Krzysztof Bańkowski ◽  
...  
Keyword(s):  
Solid State ◽  
Kinase Inhibitor ◽  
Drug Product ◽  
Variable Temperature ◽  
Drug Substance ◽  
Crystalline Solid ◽  
Scanning Calorimetry ◽  
Thermal Methods ◽  
Polymorphic Transitions ◽  
Polymorphic Forms

Erlotinib is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR) and is used to treat non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer [1]. It is known that erlotinib forms different salts which can exist in multiple crystalline solid forms. This important property known as a polymorphism may have an impact on physical and chemical stability of the drug substance (API), processability during manufacturing in the final drug product and bioavailability of the drug to the patient. Changes in the crystal structure of API can lead to the undesired changes in properties. Hence, the control of the polymorphic form is essential during the drug substance manufacture and requires a thorough understanding of solid-state changes that may occur in pharmaceutical materials. To achieve a comprehensive understanding of solid-state transformations different analytical techniques are applied. In our studies the variable–temperature powder X-ray diffraction (VT–PXRD), differential scanning calorimetry (DSC), thermogravimetry (TGA), Fourier transformed infrared (FTIR), attenuated total reflectance (ATR) and Raman spectroscopy were used to investigate the correlation between the thermal behavior and structural transformations of polymorphic forms of erlotinib salts. VT-PXRD method has detected the temperature range of the existence of polymorphic transitions, spectroscopy methods have characterized intramolecular vibrations and thermal methods have provided information on the transition and melting temperature and relationships between polymorphic forms.

scholarly journals Formulation and Evaluation of Mucoadhesive Buccal Tablet of Repaglinide

2019 ◽  
Vol 9 (4-A) ◽  
pp. 415-424
Author(s):  
Eknath B Thakare ◽  
Prashant S. Malpure ◽  
Avish D. Maru ◽  
Yashpal M. More
Keyword(s):  
In Vitro Release ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
Powder Bed ◽  
Weight Variation ◽  
Compressibility Index ◽  
Buccal Tablet ◽  
The Stability ◽  
Buccal Tablets

The aim of present investigation was formulation and evaluation of mucoadhesive buccal tablet of Repaglinide to study the effect of different polymers on release profile of drug for prolonged release. In this study mucoadhesive buccal tablet were prepared by direct compression method. Various rheological characteristics of the powder bed like bulk density, compressibility index, and angle of repose were evaluated and studied. Mucoadhesive buccal tablets were compressed on a 8 station mini press using 10 mm flat faced punches and were all assessed for weight variation, hardness, thickness, percent swelling index, mucoadhesive strength and in vitro release of the drug by using USP TDT 08L dissolution testing apparatus method II using a paddle at 50 rpm. Data was optimized by using 32 full factorial design by using software named as design expert and with the help of kinetic study. The stability studies showed that there is no decrease in the drug content of all formulations for the period of 2 months. Keywords: Buccal tablet, Repaglinide, HPMC K100M, Xanthan gum.

scholarly journals Host-guest interaction and properties of cucurbit[8]uril with chloramphenicol

2021 ◽  
Author(s):  
Lin Zhang ◽  
Jun Zheng ◽  
Guangyan Luo ◽  
Xiaoyue Li ◽  
Yunqian Zhang ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Slow Release ◽  
In Vitro Release ◽  
Titration Calorimetry ◽  
X Ray Diffraction ◽  
X Ray ◽  
E Coli ◽  
The Stability ◽  
Vitro Release

The interaction between cucurbit[8]uril (Q[8]) and chloramphenicol (CPE) was investigated using single-crystal X-ray diffraction, spectroscopy, isothermal titration calorimetry (ITC) and UV-Vis, NMR and IR spectroscopy. The effects of Q[8] on the stability, in vitro release performance and antibacterial activity of CPE were also studied. The results showed that CPE and Q[8] formed a 1:1 inclusion complex (CPE@Q[8]) with an inclusion constant of 5.4736 × 105 L/mol. The intervention of Q[8] did not affect the stability of CPE, but obviously reduced the release rate of CPE in artificial gastric and intestinal juice; Q[8] has a slow-release effect on CPE. The antibacterial results showed that the minimum inhibitory concentration (MIC) of CPE and CPE@Q[8] toward Escherichia coli (E. coli) was 1.5 × 10–3 and 1.0 × 10–3 mol/L, respectively, and toward Staphylococcus aureus (SA), the MIC was 2.0 × 10–3 mol/L for both CPE and CPE@Q[8]. Therefore, Q[8] enhanced the inhibitory activity of CPE against E. coli.

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