Co-surfactant effect of polyethylene glycol 400 on microemulsion using BCS class II model drug

The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. Phenytoin is taking as a model drug; the present study adopted an innovative solid phospholipid nanoparticle (SPLN) line of attack, and it is parallelly equated with the industrialized methods (freeze-drying) which are used for the boosting of solubility and dissolution of Phenytoin. Phenytoin was articulated along with phospholipid and mannitol at a diverse ratio of phenytoin, PL, mannitol, in which 1:12:18 was the correct ratio for ideal preparation. Freeze-drying helps to prepare SPLNs in orbicular shape, which is amorphous in nature with ≤ 1µm diameter on average. While the amorphous matrix-like structure of solid phospholipid dispersion with larger particle size is obtained by freeze-drying technique. Formulating the formulation from this method improved the dissolution rate in a remarkable way. Tris buffer with pH 7.4acts as an apparent solubility dissolved concentration of phenytoin. The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. The decrease in the particle size or cumulating the drug surface area is the widely used practices to proliferate the solubility. The target of the present work was improvisation in solubility, dissolution of a poorly water-soluble drug, and its release by using solid phospholipid nanoparticles. Phenytoin is taking as a model drug. The solid phospholipid nanoparticles were primed by freeze-drying technique along with phospholipid and mannitol in diverse drug to excipients ratios (1:1, 1:2w: w). These preparations were assessed for compatibility study using FTIR, solubility enhancement study by XRD, entrapment efficiency, surface morphology by SEM, and in-vitro release study. As per the results, there is no influence of the excipients on the drug used. The solubility was increased by folds compared to in house prepared formulation.

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Enhanced Dissolution Performance of BCS Class II Compound

10.26226/morressier.57d6b2bbd462b8028d88d2dd ◽

2016 ◽

Author(s):

Saujanya Gosangari

Keyword(s):

Class Ii ◽

Bcs Class Ii ◽

Enhanced Dissolution

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Flame retardancy of Scots pine (Pinus sylvestris) by using polyethylene glycol 400 and phosphoric acid

International Journal of Psychosocial Rehabilitation ◽

10.37200/ijpr/v24i4/pr201029 ◽

2020 ◽

Vol 24 (04) ◽

pp. 507-515

Author(s):

Fatima Zohra Brahmia ◽

Tibor Alpár ◽

Péter Horváth György

Keyword(s):

Polyethylene Glycol ◽

Phosphoric Acid ◽

Pinus Sylvestris ◽

Scots Pine ◽

Flame Retardancy ◽

Polyethylene Glycol 400

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Development, Evaluation and Optimization of Osmotic Controlled Tablets of Aceclofenac for Rheumatoid Arthritis Management

Drug Delivery Letters ◽

10.2174/2210303109666181203150830 ◽

2019 ◽

Vol 9 (1) ◽

pp. 29-36

Author(s):

Bijaya Ghosh ◽

Niraj Mishra ◽

Preeta Bose ◽

Moumita D. Kirtania

Keyword(s):

Rheumatoid Arthritis ◽

Polyethylene Glycol ◽

Sodium Chloride ◽

Cellulose Acetate ◽

Hydroxypropyl Methylcellulose ◽

Release Profile ◽

Polyethylene Glycol 400 ◽

Permeable Membrane ◽

Cumulative Release ◽

The Core

Objective: Rheumatoid arthritis is a dreaded disease, characterized by pain, inflammation and stiffness of joints, leading to severe immobility problems. The disease shows circadian variation and usually gets aggravated in early morning hours. Aceclofenac, a BCS Class II compound is routinely used in the treatment of pain and inflammation associated with rheumatoid arthritis. The objective of this study was to develop an osmotic delivery system of Aceclofenac that after administration at bedtime would deliver the drug in the morning hours. </P><P> Methods: A series of osmotically controlled systems of aceclofenac was developed by using lactose, sodium chloride and hydroxypropyl methylcellulose K100M as osmogens. Cellulose acetate (2% w/v in acetone) with varying concentrations of polyethylene glycol-400 was used as the coating polymer to create semi permeable membrane and dissolution was carried out in 290 mOsm phosphate buffer. Formulation optimization was done from four considerations: cumulative release at the end of 6 hours (lag time), cumulative release at the end of 7 hours (burst time), steady state release rate and completeness of drug release. </P><P> Results: A formulation having swelling polymer hydroxypropyl methylcellulose in the core and lactose and sodium chloride as osmogens, polyethylene glycol-400 (16.39 %) as pore former, with a coating weight of 5% was a close fit to the target release profile and was chosen as the optimum formulation. Conclusion: Aceclofenac tablets containing lactose, HPMC and sodium chloride in the core, given a coating of cellulose acetate and PEG-400 (5% wt gain), generated a release profile for optimum management of rheumatoid arthritic pain.

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Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190422160115 ◽

2020 ◽

Vol 10 (5) ◽

pp. 649-663

Author(s):

Reena Siwach ◽

Parijat Pandey ◽

Harish Dureja

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Oral Absorption ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Class Ii ◽

Dissolution Enhancement ◽

In Vitro Drug Release ◽

Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

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Improved Bioavailability of Oxcarbazepine, a BCS class II drug by Centrifugal Melt Spinning: In-vitro and in-vivo Implications

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2021.120775 ◽

2021 ◽

pp. 120775

Author(s):

Sidra Nasir ◽

Amjad Hussain ◽

Nasir Abbas ◽

Nadeem Irfan Bukhari ◽

Fahad Hussain ◽

...

Keyword(s):

Melt Spinning ◽

Class Ii ◽

Bcs Class Ii

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The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxib

Molecules ◽

10.3390/molecules26010110 ◽

2020 ◽

Vol 26 (1) ◽

pp. 110

Author(s):

Nele-Johanna Hempel ◽

Tra Dao ◽

Matthias M. Knopp ◽

Ragna Berthelsen ◽

Korbinian Löbmann

Keyword(s):

Polyethylene Glycol ◽

Microwave Radiation ◽

Magnesium Stearate ◽

Einstein Equations ◽

Dissolution Process ◽

Target Temperature ◽

Peg 4000 ◽

Lower Viscosity ◽

Model Drug

Microwaved-induced in situ amorphization of a drug in a polymer has been suggested to follow a dissolution process, with the drug dissolving into the mobile polymer at temperatures above the glass transition temperature (Tg) of the polymer. Thus, based on the Noyes–Whitney and the Stoke–Einstein equations, the temperature and the viscosity are expected to directly impact the rate and degree of drug amorphization. By investigating two different viscosity grades of polyethylene glycol (PEG), i.e., PEG 3000 and PEG 4000, and controlling the temperature of the microwave oven, it was possible to study the influence of both, temperature and viscosity, on the in situ amorphization of the model drug celecoxib (CCX) during exposure to microwave radiation. In this study, compacts containing 30 wt% CCX, 69 wt% PEG 3000 or PEG 4000 and 1 wt% lubricant (magnesium stearate) were exposed to microwave radiation at (i) a target temperature, or (ii) a target viscosity. It was found that at the target temperature, compacts containing PEG 3000 displayed a faster rate of amorphization as compared to compacts containing PEG 4000, due to the lower viscosity of PEG 3000 compared to PEG 4000. Furthermore, at the target viscosity, which was achieved by setting different temperatures for compacts containing PEG 3000 and PEG 4000, respectively, the compacts containing PEG 3000 displayed a slower rate of amorphization, due to a lower target temperature, than compacts containing PEG 4000. In conclusion, with lower viscosity of the polymer, at temperatures above its Tg, and with higher temperatures, both increasing the diffusion coefficient of the drug into the polymer, the rate of amorphization was increased allowing a faster in situ amorphization during exposure to microwave radiation. Hereby, the theory that the microwave-induced in situ amorphization process can be described as a dissolution process of the drug into the polymer, at temperatures above the Tg, is further strengthened.

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