A Comparative Study on the Effect of Hydroxypropyl Methylcellulose F4M and Eudragit® E PO on the Physicochemical Properties of Taste-Masking Microparticles

2020 ◽  
Vol 859 ◽  
pp. 15-20
Author(s):  
Kanokporn Burapapadh ◽  
Napat Wattanakhejorn ◽  
Panitsupa Sukpipat ◽  
Sirapa Promchuay ◽  
Thicha Phengpinit ◽  
...  
Keyword(s):  
Bitter Taste ◽  
Diclofenac Sodium ◽  
Hydroxypropyl Methylcellulose ◽  
Taste Masking ◽  
Loading Capacity ◽  
Type Ii ◽  
Ph Responsive ◽  
Dissolution Apparatus ◽  
Model Drug ◽  
Spray Dried

The objective of this study was to investigate the effect of polymers and their content level on the taste-masking efficiency of spray-dried microparticles. Diclofenac sodium (DS) was used as a model drug, owing to its bitter taste. Hydroxypropyl methylcellulose F4M (HPMC F4M) and Eudragit® E PO were involved in the study as a hydrophilic and a pH-responsive polymer, respectively. The taste-masked DS microparticles with the drug:polymer ratios of 1:1, 1:2 and 1:4 were prepared by the spray-drying technique. The collapsed hollow sphere HPMC F4M based-microparticles was observed meanwhile spray-dried Eudragit® E PO based-microparticles were spherical. Loading capacity of both polymer based-microparticles decreased regarding to the increment of drug:polymer ratio. The Eudragit® E PO based-microparticle in the ratio of 1:4 provided the highest loading efficiency as 91.97%. According to the simplified dissolution testing, the taste-masking ability of HPMC F4M and Eudragit® E PO based-microparticles increased upon the increase of drug:polymer ratio. Drug release at the first 5 minutes from dissolution profiles, tested by type II dissolution apparatus, of the Eudragit® E PO based-microparticles was delayed compared to HPMC F4M based-microparticles. Therefore, it could be assumed that Eudragit® E PO was a promising taste-masking polymer for DS with a pleasant taste.

scholarly journals Experimental and Modeling Study of Drug Release from HPMC-Based Erodible Oral Thin Films

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 222 ◽  
Author(s):  
Alessandra Adrover ◽  
Gabriele Varani ◽  
Patrizia Paolicelli ◽  
Stefania Petralito ◽  
Laura Di Muzio ◽  
...  
Keyword(s):  
Thin Films ◽  
Drug Transport ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Franz Cell ◽  
Flow Through ◽  
Dissolution Apparatus ◽  
Model Drug ◽  
Drug Incorporation

In this work hydroxypropyl methylcellulose (HPMC) fast-dissolving thin films for oral administration are investigated. Furosemide (Class IV of the Biopharmaceutical Classification System) has been used as a model drug for in vitro release tests using three different set-ups: the Franz cell, the millifluidic flow-through device, and the paddle type dissolution apparatus (USP II). In order to enable drug incorporation within HPMC films, a multifunctional excipient, hydroxypropyl- β -cyclodextrin (HP- β -CD) has been included in the formulation, and the influence of HP- β -CD on film swelling, erosion, and release properties has been investigated. Mathematical models capable of describing the swelling and release processes from HPMC erodible thin films in different apparatuses have been developed. In particular, we propose a new model for the description of drug transport and release in a Franz cell that accounts for the effect of the unavoidable imperfect mixing of the receptor chamber.

Principles of masking organoleptic properties of bitter tasting medicines

2020 ◽  
pp. 25-32
Author(s):  
Mariya Anurova ◽  
Elena Bakhrushina ◽  
Anna Moiseyeva ◽  
Ivan Krasnyuk
Keyword(s):  
Nervous System ◽  
Patient Compliance ◽  
Dosage Form ◽  
Bitter Taste ◽  
Drug Uptake ◽  
Taste Masking ◽  
Pure Substance ◽  
High Concentration ◽  
Organoleptic Properties ◽  
Gel Composition

Patient compliance of drug therapy is the key factor in achieving the pharmaceutical effect. Taste masking is particularly important in pediatrics and geriatrics because the unpleasant taste negatively affects drug uptake. Patient compliance can be improved through balanced organoleptic properties of medicines. It is particularly important to choose optimal correction method for medicines with high concentration of the active substance. Hopantenic acid has been chosen as a model drug due to its bitter taste. Taste masking technologies for creating a new dosage form with optimal organoleptic properties are proposed in the article. The objective is to achieve an experimentally justified choice of technological approach to masking bitter taste of a substance and to create a new dosage form on its basis. Materials and methods. Alternative technologies were considered to solve this problem: granulation, creation of complexes with ion-exchange resins, introduction of a gel composition and taste-masking using sweeteners. Organoleptic properties in dry compositions (pure substance of hopantenic acid, granulate and resinate based on it), and also after preparation of liquid dosage forms and incorporation them into gel, were evaluated by A. I. Tentsova method. Choice of sweetener and its concentration to achieve an optimally balanced taste took place at the final stage. Hopantenic acid was chosen as a model substance. Hopantenic acid is a nootropic drug stimulating cognitive functions, nervous system, enhancing intellectual functioning, decreasing nervous system activity, with anticonvulsant action. The main therapeutic indications are mental retardation, dementia, epilepsy. Results and discussion. The study has shown that optimal technology for masking unpleasant taste of hopantenic acid is its introduction into a gel composition, and a promising dosage form is an oral gel. Compri-Zucker G sweetener (Südzucker АG, Germany) in concentration of 5 % has been chosen to create pleasant taste due to its highest taste rating. Conclusion. It has been determined as a result of the study that oral gel with active drug concentration of 5 % and sweetener concentration of 5 % has optimal organoleptic properties. Thus, this combination of active and additional substances can be considered the most perspective for developing a new dosage form of a medicine.

Exploration of Neem Gum, Acrylamide Grafted Neem Gum and Carboxymethylated Neem Gum as Retardant in Tablet Formulation

2020 ◽  
Vol 16 (9) ◽  
pp. 1404-1410
Author(s):  
Rishabha Malviya
Keyword(s):  
Diclofenac Sodium ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Binding Agent ◽  
Grafted Polymer ◽  
Model Drug ◽  
Tablet Dosage ◽  
Tapped Density ◽  
Derivatives Of

Background: In the previous study, investigators have synthesized acrylamide grafted and carboxymethylated derivatives of neem gum and evaluated their potential in the formulation of nanoparticles. In continuation of previous work, authors have evaluated neem gum polysaccharide (NGP), acrylamide grafted neem gum polysaccharide (NGP-g-Am) and carboxymethylated neem gum polysaccharide (CMNGP) as binding agent in the tablet dosage form. Methods: Diclofenac sodium was used as a model drug while microcrystalline cellulose and talc were used as excipient in the preparation of granules employing wet granulation technique. NGP, NGP-g-Am and CMNGP were utilized as binding agent in the preparation of granules. Prepared granules were characterized for various pre-compression and post-compression parameters. Results and Discussion: Binding agents were used in the concentration of 4-24%w/w. NGP incorporated granules showed more bulk density and lower values of tapped density, Carr’s index, bulkiness, Hausner’s ratio and angle of repose as compared to NGP-g-Am consisting granules. NGP-g-Am consisting tablets showed more hardness and zero friability as compared to NGP based tablets. Drug content was found lower for the tablets having grafted polymer in place of NGP. CMNGP were also utilized to prepare granules but granules were not be able to compress keeping all the compacting parameters same as used in the case of NGP and NGP-g-Am consisting granules. NGP and NGP-g-Am were able to sustain drug release up to 6 and 8 h, respectively. Conclusion: It can be concluded that NGP-g-Am induces better properties when used as a binder in the tablet formulation than native polymer, while CMNGP cannot be utilized as a binding agent in the preparation of a tablet.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

Yolk–shell magnetic composite Fe3O4@Co/Zn-ZIF for MR imaging-guided chemotherapy of tumors in vivo

2021 ◽  
Author(s):  
Ying Li ◽  
Lu-Lu Jiang ◽  
Ya-Xian Qiao ◽  
Dong Wan ◽  
Yan-Feng Huang
Keyword(s):  
Mr Imaging ◽  
Contrast Enhancement ◽  
Magnetic Composite ◽  
Loading Capacity ◽  
Ph Responsive

The yolk–shell composites Fe3O4@Co/Zn-ZIF exhibited high doxorubicin loading capacity, pH-responsive release characteristics, and strong T2-weighted MR imaging contrast enhancement, and were used for MR imaging-guided chemotherapy of tumors in vivo.

Real time monitoring of peptide delivery in vitro using high payload pH responsive nanogels

2020 ◽  
Vol 11 (2) ◽  
pp. 425-432 ◽  
Author(s):  
Shegufta Farazi ◽  
Fan Chen ◽  
Henry Foster ◽  
Raelene Boquiren ◽  
Shelli R. McAlpine ◽  
...  
Keyword(s):  
Real Time ◽  
Intracellular Delivery ◽  
Peptide Delivery ◽  
High Loading ◽  
Loading Capacity ◽  
Ph Responsive ◽  
Real Time Monitoring ◽  
High Payload

A pH responsive pMAA nanogel that demonstrates high loading capacity and rapid intracellular delivery of hydrophilic peptides.

scholarly journals Synthesis and Characterization of Stearic Acid-Beclomethasone Dipropionate Conjugates with the Potential for Improving Loading Capacity in Lipid-based Nanoparticles

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Pulmonary Delivery ◽  
Dynamics Simulation ◽  
Loading Capacity ◽  
Technology Platform ◽  
New Type ◽  
Model Drug

<p>Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.</p>

Synthesis and Self-Assembly of the pH-Responsive Anionic Copolymers for Enhanced Doxorubicin-Loading Capacity

Langmuir ◽  
2018 ◽  
Vol 34 (26) ◽  
pp. 7877-7886 ◽  
Author(s):  
Meijun Yi ◽  
Qian Lu ◽  
Yuping Zhao ◽  
Chenqian Cheng ◽  
Shiping Zhang
Keyword(s):  
Self Assembly ◽  
Loading Capacity ◽  
Ph Responsive
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