Effect of Fast-Disintegrating Tablets' Characteristics on the Sublingual Permeability of Atropine Sulfate for the Potential Treatment of Organophosphates Toxicity.

Abstract:

:Atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs) were tested for AS sublingual permeation's feasibility as a potential alternative dosage form to treat organophosphates (OP) toxicity. More than 12,000 OP pesticide toxicity cases were reported in the USA from 2011 to 2014. AS is the recommended antidote for OP toxicity; however, it is only available as an ATROPEN® auto-injector, an IM injection, for self-administration, which is associated with several drawbacks and limitations. Six AS FDST batches were formulated and characterized. Two tablet sizes, group A weighing 150 mg and group B weighing 50 mg, were formulated with three different AS doses: 2 mg (A1 and B1), 4 mg (A2 and B2), and 8 mg (A3 and B3). AS in vitro diffusion and sublingual permeation were investigated in Franz cells using a cellulose membrane and an excised porcine sublingual membrane. The effect of AS load and tablet size on sublingual permeation was also evaluated. All batches passed quality control tests. AS FDSTs' size and AS load had a significant effect on tablet disintegration time and drug dissolution, which significantly impacted AS concentration gradient across the diffusional membrane. Group B FDSTs (smaller tablets) resulted in a significantly higher initial permeation (JAUC0-15) compared to group A FDSTs. Also, the cumulative AS (JAUC0-90) and AS influx (J) increased linearly with increasing AS dose. These AS FDSTs have the potential to be explored in vivo to determine the required bioequivalent sublingual AS dose as an alternative dosage form for the treatment of OP toxicity.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Aodah A,Rawas-Qalaji M,Bafail R,Rawas-Qalaji M

doi

10.1208/s12249-019-1420-1

subject

Has Abstract

pub_date

2019-06-21 00:00:00

pages

229

issue

6

issn

1530-9932

pii

10.1208/s12249-019-1420-1

journal_volume

20

pub_type

杂志文章
  • Development of Orodispersible Films Containing Benzydamine Hydrochloride Using a Modified Solvent Casting Method.

    abstract::The aim of this study was to develop benzydamine hydrochloride-loaded orodispersible films using the modification of a solvent casting method. An innovative approach was developed when the drying process of a small-scale production was used based on a heated inert base for casting the film. During this process, two ty...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1088-y

    authors: Pechová V,Gajdziok J,Muselík J,Vetchý D

    更新日期:2018-08-01 00:00:00

  • Preparation and Evaluation of Skin Wound Healing Chitosan-Based Hydrogel Membranes.

    abstract::The purpose of the study was to synthesize and characterize a new form of topical membranes as chitosan-based hydrogel membranes for bacterial skin infections. The polymeric membranes were synthesized by modification in free radical solution polymerization technique. High molecular weight (HMW) chitosan polymer was cr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1131-z

    authors: Ahmad S,Minhas MU,Ahmad M,Sohail M,Abdullah O,Badshah SF

    更新日期:2018-10-01 00:00:00

  • Self-microemulsifying Drug Delivery System for Improved Oral Delivery of Limonene: Preparation, Characterization, in vitro and in vivo Evaluation.

    abstract::The current investigation aimed at formulating self-microemulsifying drug delivery system (SMEDDS) to ameliorate oral bioavailability of a hydrophobic functional ingredient, limonene. Solubility test, compatibility test, and pseudo-ternary phase diagrams (PTPD) were adopted to screen the optimal compositions of limone...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1361-8

    authors: Zhu Y,Xu W,Zhang J,Liao Y,Firempong CK,Adu-Frimpong M,Deng W,Zhang H,Yu J,Xu X

    更新日期:2019-03-26 00:00:00

  • Development and evaluation of a floating multiparticulate gastroretentive system for modified release of AZT.

    abstract::The aim of this study was to develop and evaluate a floating multiparticulate gastroretentive system for the modified release of zidovudine (AZT). AZT was used as a model drug water-soluble at therapeutic doses. The floating gastroretentive system was obtained by co-precipitation, after solvent diffusion and evaporati...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9627-9

    authors: Yoshida VM,de Oliveira Junior JM,Gonçalves MM,Vila MM,Chaud MV

    更新日期:2011-06-01 00:00:00

  • A mucoadhesive in situ gel delivery system for paclitaxel.

    abstract::MUC1 gene encodes a transmembrane mucin glycoprotein that is overexpressed in human breast cancer and colon cancer. The objective of this study was to develop an in situ gel delivery system containing paclitaxel (PTX) and mucoadhesives for sustained and targeted delivery of anticancer drugs. The delivery system consis...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070253

    authors: Jauhari S,Dash AK

    更新日期:2006-06-02 00:00:00

  • Advances in metered dose inhaler technology: hardware development.

    abstract::Pressurized metered dose inhalers (MDIs) were first introduced in the 1950s and they are currently widely prescribed as portable systems to treat pulmonary conditions. MDIs consist of a formulation containing dissolved or suspended drug and hardware needed to contain the formulation and enable efficient and consistent...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-013-0062-y

    authors: Stein SW,Sheth P,Hodson PD,Myrdal PB

    更新日期:2014-04-01 00:00:00

  • Evaluation of polymer mucoadhesiveness by the use of acoustic spectroscopy.

    abstract::An innovative and simple methodology has been developed and used for the evaluation of mucoadhesive properties of several polymers by means of sound speed measurements using high-resolution acoustic spectroscopy. In systems made of polymers in water, variations in hydration shell of polymeric chains determine changes ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9490-0

    authors: Cespi M,Bonacucina G,Mencarelli G,Giorgioni G,Palmieri GF

    更新日期:2010-09-01 00:00:00

  • In vitro permeability enhancement in intestinal epithelial cells (Caco-2) monolayer of water soluble quaternary ammonium chitosan derivatives.

    abstract::The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the m...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9399-7

    authors: Kowapradit J,Opanasopit P,Ngawhirunpat T,Apirakaramwong A,Rojanarata T,Ruktanonchai U,Sajomsang W

    更新日期:2010-06-01 00:00:00

  • A comprehensive development strategy in buccal drug delivery.

    abstract::This work combines several methods in an integrated strategy to develop a matrix for buccal administration. For this purpose, tablets containing selected mucoadhesive polymers loaded with a model drug (omeprazole), free or in a complexed form with cyclodextrins, and in the absence and presence of alkali agents were su...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9546-1

    authors: Figueiras A,Pais AA,Veiga FJ

    更新日期:2010-12-01 00:00:00

  • Effect of Carbopol and polyvinylpyrrolidone on the mechanical, rheological, and release properties of bioadhesive polyethylene glycol gels.

    abstract::This study examined the mechanical (hardness, compressibility, adhesiveness, and cohesiveness) and rheological (zero-rate viscosity and thixotropy) properties of polyethylene glycol (PEG) gels that contain different ratios of Carbopol 934P (CP) and polyvinylpyrrolidone K90 (PVP). Mechanical properties were examined us...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt010324

    authors: Tan YT,Peh KK,Al-Hanbali O

    更新日期:2000-08-17 00:00:00

  • Microemulsion-based oxyresveratrol for topical treatment of herpes simplex virus (HSV) infection: physicochemical properties and efficacy in cutaneous HSV-1 infection in mice.

    abstract::The physicochemical properties of the optimized microemulsion and the permeating ability of oxyresveratrol in microemulsion were evaluated, and the efficacy of oxyresveratrol microemulsion in cutaneous herpes simplex virus type 1 (HSV-1) infection in mice was examined. The optimized microemulsion was composed of 10% w...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9828-x

    authors: Sasivimolphan P,Lipipun V,Ritthidej G,Chitphet K,Yoshida Y,Daikoku T,Sritularak B,Likhitwitayawuid K,Pramyothin P,Hattori M,Shiraki K

    更新日期:2012-12-01 00:00:00

  • Percutaneous Delivery of Antihypertensive Agents: Advances and Challenges.

    abstract::Hypertension remains a significant risk factor for several cardiovascular disorders including coronary artery disease and heart failure. Despite the large armamentarium of drugs available for the management of high blood pressure, low oral availability is an ongoing challenge. Researchers are constantly developing alt...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-019-1583-9

    authors: Ita K,Ashong S

    更新日期:2020-01-06 00:00:00

  • Trans-ungual Delivery of AR-12, a Novel Antifungal Drug.

    abstract::AR-12 is a novel small molecule with broad spectrum antifungal activity. Recently, AR-12 was found to be highly active against Trichophyton rubrum, one of the predominantly responsible organisms that cause onychomycosis. The primary objective of this project was to investigate the ability of AR-12 to penetrate into an...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0752-y

    authors: Kushwaha AS,Sharma P,Shivakumar HN,Rappleye C,Zukiwski A,Proniuk S,Murthy SN

    更新日期:2017-10-01 00:00:00

  • Proliposome Powders for the Generation of Liposomes: the Influence of Carbohydrate Carrier and Separation Conditions on Crystallinity and Entrapment of a Model Antiasthma Steroid.

    abstract::Formulation effects on the entrapment of beclometasone dipropionate (BDP) in liposomes generated by hydration of proliposomes were studied, using the high-density dispersion medium deuterium oxide in comparison to deionized water (DW). Proliposomes incorporating BDP (2 mol% of the lipid phase consisting of soya phosph...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0793-2

    authors: Khan I,Yousaf S,Subramanian S,Alhnan MA,Ahmed W,Elhissi A

    更新日期:2018-01-01 00:00:00

  • Fast tablet tensile strength prediction based on non-invasive analytics.

    abstract::In this paper, linkages between tablet surface roughness, tablet compression forces, material properties, and the tensile strength of tablets were studied. Pure sodium halides (NaF, NaBr, NaCl, and NaI) were chosen as model substances because of their simple and similar structure. Based on the data available in the li...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0104-0

    authors: Halenius A,Lakio S,Antikainen O,Hatara J,Yliruusi J

    更新日期:2014-06-01 00:00:00

  • Improved Vemurafenib Dissolution and Pharmacokinetics as an Amorphous Solid Dispersion Produced by KinetiSol® Processing.

    abstract::Vemurafenib is a poorly soluble, low permeability drug that has a demonstrated need for a solubility-enhanced formulation. However, conventional approaches for amorphous solid dispersion production are challenging due to the physiochemical properties of the compound. A suitable and novel method for creating an amorpho...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-0988-1

    authors: Ellenberger DJ,Miller DA,Kucera SU,Williams RO 3rd

    更新日期:2018-07-01 00:00:00

  • Formulation Optimization of Selective Laser Sintering 3D-Printed Tablets of Clindamycin Palmitate Hydrochloride by Response Surface Methodology.

    abstract::The aims of the current study were to develop and evaluate clindamycin palmitate hydrochloride (CPH) 3D-printed tablets (printlets) manufactured by selective laser sintering (SLS). Optimization of the formulation was performed by studying the effect of formulation and process factors on critical quality attributes of ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01775-0

    authors: Mohamed EM,Barakh Ali SF,Rahman Z,Dharani S,Ozkan T,Kuttolamadom MA,Khan MA

    更新日期:2020-08-13 00:00:00

  • Preparation and characterization of polyvinyl alcohol-gelatin hydrogel membranes for biomedical applications.

    abstract::The purpose of this research was to design and develop hydrogels by esterification of polyvinyl alcohol (PVA) with gelatin. The membranes were characterized by Fourier Transform Infrared (FTIR) spectroscopy, x-ray diffraction (XRD), and differential scanning calorimetry. The viscosity of the esterified product (as sol...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt080121

    authors: Pal K,Banthia AK,Majumdar DK

    更新日期:2007-03-16 00:00:00

  • Development and Optimization of an Ex Vivo Colloidal Stability Model for Nanoformulations.

    abstract::Nanotechnology is having a significant impact in the drug delivery systems and diagnostic devices. As most of the nanosystems are intended to be administered in vivo, there is a need for stability models, which could simulate the biological environment. Instability issues could lead to particle aggregation and in turn...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0597-9

    authors: Shaikh MV,Kala M,Nivsarkar M

    更新日期:2017-05-01 00:00:00

  • Acoustic-resonance spectrometry as a process analytical technology for the quantification of active pharmaceutical ingredient in semi-solids.

    abstract::The purpose of this study was to demonstrate acoustic resonance spectrometry (ARS) as an alternative process analytical technology to near infrared (NIR) spectroscopy for the quantification of active pharmaceutical ingredient (API) in semi-solids such as creams, gels, ointments, and lotions. The ARS used for this rese...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070359

    authors: Medendorp J,Buice RG Jr,Lodder RA

    更新日期:2006-07-14 00:00:00

  • DEM Modelling of Granule Rearrangement and Fracture Behaviours During a Closed-Die Compaction.

    abstract::The closed-die compaction behaviour of D-mannitol granules has been simulated by the discrete element method (DEM) to investigate the granule rearrangement and fracture behaviour during compaction which affects the compactibility of the tablet. The D-mannitol granules produced in a fluidized bed were modelled as agglo...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0719-z

    authors: Furukawa R,Kadota K,Noguchi T,Shimosaka A,Shirakawa Y

    更新日期:2017-08-01 00:00:00

  • Process optimization of a novel immediate release film coating system using QbD principles.

    abstract::This work describes a quality-by-design (QbD) approach to determine the optimal coating process conditions and robust process operating space for an immediate release aqueous film coating system (Opadry® 200). Critical quality attributes (CQAs) or associated performance indicators of the coated tablets were measured w...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9935-3

    authors: Teckoe J,Mascaro T,Farrell TP,Rajabi-Siahboomi AR

    更新日期:2013-06-01 00:00:00

  • Co-Processed Excipients for Dispersible Tablets-Part 2: Patient Acceptability.

    abstract::Palatability and patient acceptability are critical attributes of dispersible tablet formulation. Co-processed excipients could provide improved organoleptic profile due to rational choice of excipients and manufacturing techniques. The aim of this study was to identify the most suitable co-processed excipient to use ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1104-2

    authors: Dziemidowicz K,Lopez FL,Bowles BJ,Edwards AJ,Ernest TB,Orlu M,Tuleu C

    更新日期:2018-08-01 00:00:00

  • Kinetics of pramlintide degradation in aqueous solution as a function of temperature and pH.

    abstract::The stability of the 37-amino acid peptide pramlintide, in aqueous solution, was studied as a function of pH and temperature. Samples of pramlintide formulated as a parenteral product were exposed to elevated temperatures and to realistic storage conditions for as long as 30 months. Pramlintide degradation was monitor...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt010207

    authors: Kenley RA,Tracht S,Stepanenko A,Townsend M,L'Italien J

    更新日期:2000-03-18 00:00:00

  • A Novel Eutectic-Based Transdermal Delivery System for Risperidone.

    abstract::This paper reports for the first time the possible formation of a novel room temperature therapeutic deep eutectic solvent (THEDES) of risperidone (RIS) with some fatty acids, namely capric acid (C10; CA), lauric acid (C12; LA), and myristic acid (C14; MA). All mixtures of RIS and MA yielded a solid or pasty-like soli...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01844-4

    authors: Al-Akayleh F,Adwan S,Khanfar M,Idkaidek N,Al-Remawi M

    更新日期:2020-11-22 00:00:00

  • Multimodal particle size distributions emitted from HFA-134a solution pressurized metered-dose inhalers.

    abstract::The purpose of this research was to investigate the measurement and in vitro delivery implications of multimodal distributions, occurring near or in the respirable range, emitted from pressurized metered-dose inhalers (pMDIs). Particle size distributions of solution pMDIs containing hydrofluoroalkane-134a (HFA-134a) a...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt040338

    authors: Smyth HD,Hickey AJ

    更新日期:2003-01-01 00:00:00

  • Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum).

    abstract::The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosag...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9873-5

    authors: Meka VS,Nali SR,Songa AS,Kolapalli VR

    更新日期:2012-12-01 00:00:00

  • Particle size and temperature effect on the physical stability of PLGA nanospheres and microspheres containing Bodipy.

    abstract::The purpose of this study was to investigate the effect of particle size, storage temperature, and duration of storage on the physical stability and morphology of polylactic-co-glycolic acid (PLGA) nanospheres and microspheres. PLGA nanospheres and microspheres containing the fluorescent dye, Bodipy, were prepared in ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050453

    authors: De S,Robinson DH

    更新日期:2004-09-13 00:00:00

  • Development and characterization of siRNA lipoplexes: Effect of different lipids, in vitro evaluation in cancerous cell lines and in vivo toxicity study.

    abstract::Cationic liposomes have long been used as non-viral vectors for small interfering RNA (siRNA) delivery but are associated with high toxicity, less transfection efficiency, and in vivo instability. In this investigation, we have developed siRNA targeted to RRM1 that is responsible for development of resistance to gemci...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0193-9

    authors: Khatri N,Baradia D,Vhora I,Rathi M,Misra A

    更新日期:2014-12-01 00:00:00

  • Formulation Optimization and Ex Vivo and In Vivo Evaluation of Celecoxib Microemulsion-Based Gel for Transdermal Delivery.

    abstract::Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Tran...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0667-z

    authors: Cao M,Ren L,Chen G

    更新日期:2017-08-01 00:00:00