scholarly journals PREPARATION AND IN VITRO EVALUATION OF FAST RELEASE DIAZEPAM SUPPOSITORIES FOR FEBRILE SEIZURES

2017 ◽  
Vol 10 (9) ◽  
pp. 365
Author(s):  
Aseel Alsamman ◽  
Mohammad Othman
Keyword(s):  
Tween 80 ◽  
Febrile Seizures ◽  
Water Soluble ◽  
Infrared Spectrometry ◽  
Ionic Surfactant ◽  
Scanning Calorimetry ◽  
Water Soluble Polymer ◽  
In Vitro Drug Release ◽  
Fast Release

  Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as a water-soluble polymer, and Poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a non-ionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of tween 80 to witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release.Conclusion: Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.

scholarly journals PREPARATION AND IN VITRO EVALUATION OF FAST RELEASE DIAZEPAM SUPPOSITORIES FOR FEBRILE SEIZURES

2017 ◽  
Vol 10 (9) ◽  
pp. 224
Author(s):  
Aseel Alsamman ◽  
Mohammad Othman
Keyword(s):  
Tween 80 ◽  
Febrile Seizures ◽  
Water Soluble ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Water Soluble Polymer ◽  
In Vitro Drug Release ◽  
Fast Release ◽  
Physical Mixtures

  Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as water-soluble polymer and poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a nonionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Fast release of diazepam has been obtained from suppositories containing the effervescent pair. Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and Witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of Tween 80 to Witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release.Conclusion: Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.

Formulation and Evaluation of Lercanidipine Loaded Self-Nanoemulsifying Drug Delivery System

2018 ◽  
Vol 11 (3) ◽  
pp. 4112-4120
Author(s):  
J. Venkateswara Rao ◽  
T. Rama Mohan Reddy
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Droplet Size ◽  
Tween 80 ◽  
Water Soluble ◽  
In Vitro Drug Release ◽  
Ternary Phase Diagrams ◽  
Water Soluble Drug ◽  
Poorly Water Soluble Drug

In the present study, we sought to improve the solubility and bioavailability of lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for FTIR studies, scanning electron microscopy (SEM), solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm and Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. Hence, lercanidipine SNEDDS is an optimum formulation strategy to enhance the solubility and oral bioavailability of this poorly water-soluble drug.

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.

The Potential Migrated Mechanism of Water-Soluble Components in Pellets Prepared by Wet Extrusion/Spheronization: Effect of Drying Rate

2020 ◽  
Vol 17 ◽  
Author(s):  
Bingwei Wang ◽  
Jianping Liu ◽  
Zhenghua Li ◽  
Yulong Xia ◽  
Shuangshuang Zhang ◽  
...  
Keyword(s):  
Relative Humidity ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Drying Rate ◽  
Scanning Calorimetry ◽  
Drying Temperature ◽  
Wet Extrusion ◽  
Extrusion Spheronization ◽  
Soluble Components

Background: At present, there were numerous researches on the migration of components in tablets and granules, the investigation in the pharmaceutical literatrue concerning the effect of drying rate on the migration of water-soluble components of pellets was limited. Temperature and relative humidity (RH) were crucial parameters during the drying process which was an essential step in the preparation of pellets via wet extrusion/spheronization. To quantify these variables, the water loss percentage of pellets per minute was defined as drying rate. Objective: The study aimed to investigate the influence of drying rate on the migration of water-soluble components in wet pellets and the potential migrated mechanism. Methods: The pellets containing tartrazine as a water-soluble model drug and microcrystalline cellulose as a matrix former were prepared by extrusion/spheronization and dried at four different drying temperature and relative humidity. Afterward, the extent of migrated tartrazine was assessed regarding appearance, in-vitro dissolution test, Differential Scanning Calorimetry, X-Ray Powder Diffraction, Attenuated total reflectance Fourier transform infrared spectroscopy and Confocal Raman Mapping. Results: Results demonstrated that red spots of tartrazine appeared on the surface of pellets and more than 40% tartrazine were burst released within 5 minutes when pellets dried at 60℃/RH 10%. While pellets dried at 40℃/RH 80%, none of these aforementioned phenomena was observed. Conclusion: In conclusion, the faster drying rate was, the more tartrazine migrated to the exterior of pellets. Adjusting drying temperature and relative humidity appropriately could inhibit the migration of water-soluble components within wet extrusion/spheronization pellets.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF OROMUCOSAL WAFER OF TRAMADOL HYDROCHLORIDE

2018 ◽  
Vol 11 (8) ◽  
pp. 116
Author(s):  
Rita N Wadetwar ◽  
Tejaswini Charde
Keyword(s):  
Drug Release ◽  
Biodegradable Polymer ◽  
Research Work ◽  
Water Soluble ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Water Soluble Polymer ◽  
Surface Ph ◽  
Folding Endurance

Objective: The objective of the present work was the preparation of fast-dissolving film of tramadol HCl (TMH) using water-soluble polymer, to achieve faster onset of action, to improve patient compliance, ease of dosing, and bypass the first-pass metabolism. Methods: TMH oromucosal wafers were prepared using pullulan as natural, biodegradable polymer, and propylene glycol as plasticizer by solvent casting method. Formulation batches were prepared using 32 full-factorial designs. The prepared TMH oromucosal wafers were characterized for morphology, uniformity of weight, drug content, folding endurance, in vitro disintegration time (DT), % moisture content, surface pH, in vitro % drug release, ex vivo permeation studies, compatibility studies (differential scanning calorimetry, Fourier transform infrared spectroscopy, and X-ray diffraction), and stability studies.Results: Optimized batch of mouth-dissolving film of TMH containing pullulan as polymer showed 98.67±0.11% drug release at 6 min. It showed better folding endurance 88 No. of folds, in vitro DT 5.11 s, surface pH 6.84±0.12 pH, thickness 0.17±0.11 mm, and percentage content uniformity 98.45±0.48%. Stability studies carried out for the best formulation FDF5 revealed that the formulation was stable.Conclusion: The results obtained in this research work clearly indicated a promising potential of fast-dissolving oral films using natural biodegradable polymer, pullulan which gave rapid drug delivery and rapid onset of action of centrally acting drug, TMH for patients suffering from pain.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals IVABRADINE HYDROCHLORIDE DIRECTLY COMPRESSED TABLETS USING NANO-CELLULOSE EXTRACTED FROM ARACHIS HYPOGAEA SHELLS

2019 ◽  
pp. 115-123
Author(s):  
JEEVANA JYOTHI B ◽  
APARNA J
Keyword(s):  
Silicon Dioxide ◽  
Acid Hydrolysis ◽  
Arachis Hypogaea ◽  
Alkali Treatment ◽  
Size Analysis ◽  
Direct Compression ◽  
Dsc Analysis ◽  
Scanning Calorimetry ◽  
Fast Release

Objective: The main objective of this work was the extraction of nanocellulose from Arachis hypogaea shells, characterization of nanocellulose, development, and in vitro evaluation of directly compressed tablets of ivabradine hydrochloride (IVH) using nanocellulose. Methods: IVH and colloidal silicon dioxide are gift samples from Mylan Laboratory, Hyderabad, and Karnataka Antibiotics and Pharmaceuticals Ltd., Bengaluru, respectively. Nanocellulose was extracted from A. hypogaea shells by alkaline treatment followed by acid hydrolysis and it was characterized by particle size analysis by zeta sizer, melting point determination, differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis. Compatibility between IVH and nanocellulose was confirmed by FTIR and DSC analysis. Then, fast-release tablets of containing 5 mg of IVH were prepared by direct compression using various compositions containing nanocellulose, starch, and colloidal silicon dioxide and evaluated. Results: Nanocellulose in the size of 273.4 nm was extracted from A. hypogaea shells to possess its ideal characteristics. IVH and nanocellulose were compatible according to FTIR and DSC analysis. Fast-release tablets of IVH were prepared as directly compressed tablets by direct compression. Tablets made with 5 mg of IVH and nanocellulose, starch, and colloidal silicon dioxide evidenced fast release of 96.37% in 5 min. Conclusion: Nanocellulose from A. hypogaea shells can be produced successfully by alkali treatment followed by acid hydrolysis, ball milling, and lyophilization. This nanocellulose can be exploited successfully for the design of fast-release tablets of IVH.

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