6,220 results match your criteria Aaps Journal[Journal]


Development, Characterization, and Optimization of a Novel Abiraterone Acetate Formulation to Improve Biopharmaceutical Attributes Aided by Pharmacokinetic Modelling.

AAPS PharmSciTech 2021 Nov 22;23(1). Epub 2021 Nov 22.

Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, 382481, India.

Abiraterone acetate has very low bioavailability and drastic food effect to warrant a dosing regimen under fasting state only. Therefore, we aimed to develop and optimize a liquisolid compact formulation of abiraterone acetate to improve biopharmaceutical attributes aided by pharmacokinetic modelling and achieve dose reduction with no food effect on the formulation. Preliminary studies highlighted the importance of the selection of olive oil as a compatible vehicle. Read More

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November 2021

Navigating Through Cell-Based In vitro Models Available for Prediction of Intestinal Permeability and Metabolism: Are We Ready for 3D?

AAPS J 2021 Nov 22;24(1). Epub 2021 Nov 22.

Center for Pharmacometrics and Systems Pharmacology, Department of Pharmaceutics, College of Pharmacy, University of Florida, Orlando, Florida, USA.

Traditionally, in vitro studies to quantify the intestinal permeability of drugs have relied on two-dimensional cell culture models using human colorectal carcinoma cell lines, namely Caco-2, HT 29 and T84 cells. Although these models have been commonly used for high-throughput screening of xenobiotics in preclinical studies, they do not fully recapitulate the morphology and functionality of enterocytes found in the human intestine in vivo. Efforts to improve the physiological and functional relevance of in vitro intestinal models have led to the development of enteroids/intestinal organoids and microphysiological systems. Read More

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November 2021

Electrochemical detection of alkaline phosphatase activity via atom transfer radical polymerization.

Bioelectrochemistry 2021 Nov 16;144:107998. Epub 2021 Nov 16.

Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, PR China. Electronic address:

Alkaline phosphatase (ALP) activity is a diagnostic indicator for a variety of clinical diseases. In this study, an electrochemical method for detecting ALP activity through activators regenerated by electron transfer atom transfer radical polymerization (ARGET ATRP) was developed. Specifically, 3-mercaptopropionic (MPA) was firstly fixed on the electrode through sulfur-gold bonding. Read More

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November 2021

Quantification of Compatibility Between Polymeric Excipients and Atenolol Using Principal Component Analysis and Hierarchical Cluster Analysis.

AAPS PharmSciTech 2021 Nov 19;23(1). Epub 2021 Nov 19.

Department of Analytical Chemistry, Medical University of Gdansk, Gen. Hallera 107, 80-416, Gdansk, Poland.

An important challenge to overcome in the solid dosage forms technology is the selection of the most biopharmaceutically efficient polymeric excipients. The excipients can be selected, among others, by compatibility studies since incompatibilities between ingredients of the drug formulations adversely affect their bioavailability, stability, efficacy, and safety. Therefore, new, fast, and reliable methods for detecting incompatibility are constantly being sought. Read More

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November 2021

Inclusion Complexes of Daidzein with Cyclodextrin-Based Metal-Organic Framework-1 Enhance Its Solubility and Antioxidant Capacity.

AAPS PharmSciTech 2021 Nov 18;23(1). Epub 2021 Nov 18.

Graduate School of Medicine, University of Yamanashi, 1110 Shimokato, Chuo, Yamanashi, 4093898, Japan.

Daidzein, an aglycone-type isoflavone, is useful in the prevention of atherosclerotic cardiovascular diseases. However, the solubility of daidzein remains relatively low even with pharmaceutical interventions (e.g. Read More

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November 2021

The Influence of Relative Humidity and Storage Conditions on the Physico-chemical Properties of Inhalation Grade Fine Lactose.

AAPS PharmSciTech 2021 Nov 17;23(1). Epub 2021 Nov 17.

Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, 8010, Graz, Austria.

Dry powder inhalers (DPIs) are favorable devices for the delivery of dry formulations to the lungs; still, they largely fail to deliver higher doses of active pharmaceutical ingredient (API) to the lower airways. Addition of fine particles of excipient (fines) to the blend of API and carrier was shown to improve aerosolization performance. Lactose monohydrate is ubiquitous excipient used for this purpose. Read More

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November 2021

Auricularia auricula-judae (Bull.) polysaccharides improve type 2 diabetes in HFD/STZ-induced mice by regulating the AKT/AMPK signaling pathways and the gut microbiota.

J Food Sci 2021 Nov 17. Epub 2021 Nov 17.

The State Key Laboratory of Bioreactor Engineering, School of Bioengineering, East China University of Science and Technology, No. 130 Meilong Road, Shanghai, Xuhui District, 200237, P. R. China.

Auricularia auricula-judae is an edible fungus with high nutritional value due to abundant polysaccharides, and is acknowledged as traditional food and medicine in Asia. Polysaccharides from A. auricula (AAPs) are typically fungal polysaccharides and have a wide range of biological activities. Read More

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November 2021

To blind or not to blind first in human and exploratory clinical trials - acceleration of development vs. risk of bias.

Clin Transl Sci 2021 Nov 16. Epub 2021 Nov 16.

Quantitative Pharmacology, EMD Serono Research and Development Institute, Inc, Billerica, MA, USA.

An IQ consortium (IQ) working group (WG) conducted a survey across multiple biopharmaceutical companies to gain information about the level of blinding commonly utilized for early clinical development trials. The main objectives were: 1. To understand blinding practices between healthy volunteer (HV) and early explorative patient trials in all therapeutic areas except oncology where early clinical trials are commonly open-label 2. Read More

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November 2021

Correction to: Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles Modified with Transferrin for Antitumor.

AAPS PharmSciTech 2021 Nov 15;22(8):276. Epub 2021 Nov 15.

Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, No. 1160 Shengli South Street, Yinchuan, 750004, China.

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November 2021

A Software Tool for Lyophilization Primary Drying Process Development and Scale-up Including Process Heterogeneity, I: Laboratory-Scale Model Testing.

AAPS PharmSciTech 2021 Nov 12;22(8):274. Epub 2021 Nov 12.

Davidson School of Chemical Engineering, Purdue University, West Lafayette, Indiana, USA.

Freeze-drying is a deceptively complex operation requiring sophisticated design of a robust and efficient process that includes understanding and planning for heterogeneity across the batch and shifts in parameters due to vial or lyophilizer changes. A software tool has been designed to assist in process development and scale-up based on a model that includes consideration of the process heterogeneity. Two drug formulations were used to test the ability of the new tool to develop a freeze-drying cycle and correctly predict product temperatures and drying times. Read More

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November 2021

ICH Q10 Pharmaceutical Quality System Guidance: Understanding Its Impact on Pharmaceutical Quality.

AAPS J 2021 11 12;23(6):117. Epub 2021 Nov 12.

College of Pharmacy, University of Georgia, Athens, Georgia, 30602, USA.

The International Council for Harmonization (ICH) "Q10 Pharmaceutical Quality Systems" (ICH Q10) guidance was introduced to address the growing gap between current good manufacturing practices and pharmaceutical manufacturing quality systems. This study evaluated the impact of the ICH Q10 guidance on the PQS of pharmaceutical manufacturers. Data were obtained from the enabler questionnaire from pharmaceutical manufacturers surveyed by the St. Read More

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November 2021

Preparation and Characterization of pH-Independent Sustained-Release Tablets Containing Hot Melt Extruded Solid Dispersions of Clarithromycin : Tablets Containing Solid Dispersions of Clarithromycin.

AAPS PharmSciTech 2021 Nov 12;22(8):275. Epub 2021 Nov 12.

Punjab University College of Pharmacy, University of the Punjab Lahore, Lahore, Pakistan.

The limited solubility of clarithromycin (CAM), coupled with low bioavailability and rapid elimination, are major shortcomings, needed to be addressed to achieve optimum therapeutic goals. Therefore, sustained-release (SR) tablets containing solid dispersion (SD) granules of CAM were prepared in this study. Initially, SD granules of CAM were prepared by hot melt extrusion (HME) technique using Kollidon VA64 as a hydrophilic carrier. Read More

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November 2021

A Practical Discussion on Estimating Shelf Life Through Tolerance Intervals.

AAPS PharmSciTech 2021 Nov 12;22(8):273. Epub 2021 Nov 12.

Early Development Biostatistics, Novartis, East Hanover, NJ, USA.

This paper is a companion article to the research originally presented in "Estimating Shelf Life through Tolerance Intervals" (Schwenke et al., 21:290, 2020) published in AAPS PharmSciTech where tolerance intervals are introduced as an alternative methodology for estimating pharmaceutical shelf life. An industry stability shelf life example data set was used to demonstrate the proposed methods. Read More

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November 2021

Development and Optimization of Microballoons Assisted Floating Tablets of Baclofen.

AAPS PharmSciTech 2021 Nov 11;22(8):272. Epub 2021 Nov 11.

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Elite Status and Centre of Excellence (Maharashtra), Deemed University, N.P. Marg, Matunga East, Mumbai, Maharashtra, 400019, India.

The objective of the present study was to develop microballoons aided gastro-retentive floating tablets of baclofen, a skeletal muscle relaxant with a low elimination half-life of ~ 3.5 h. Baclofen floating tablet was prepared to offer convenience by designing a tablet that would float in the stomach for a prolonged period and allow controlled drug release to enable once-a-day administration. Read More

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November 2021

Highlighting DEM's Potential to Gauge Mechanistic Attributes of MUPS Tablet and Capsule Formulations.

AAPS PharmSciTech 2021 Nov 11;22(8):271. Epub 2021 Nov 11.

Operations Science & Technology, AbbVie Deutschland GmbH & Co. KG, 67061, Ludwigshafen, Germany.

Simulation of pharmaceutical unit operations by the discrete element method (DEM) has elevated our understanding of the impact of single-particle interactions on themselves, and on the entire tablets/powder. Studies in the past have shown how this knowledge helps to mitigate/solve multiple challenges during conventional formulation and process development/modernization/troubleshooting, with minimal use of active drug material. This communication adds to this- highlighting the tool's potential for a rapid preliminary assessment of the mechanistic attributes of multiple unit particle system (MUPS) based tablet and capsule drug products. Read More

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November 2021

AddaVax Formulated with PolyI:C as a Potential Adjuvant of MDCK-based Influenza Vaccine Enhances Local, Cellular, and Antibody Protective Immune Response in Mice.

AAPS PharmSciTech 2021 Nov 11;22(8):270. Epub 2021 Nov 11.

National Engineering Technology Research Center for Combined Vaccines, Wuhan, 430207, China.

Poor immune responses to inactivated influenza vaccine can be improved by effective and safe adjuvants to increase antibody titers and cellular protective response. In our study, AddaVax and PolyI:C combined adjuvant (AP adjuvant) were used for influenza vaccine development. After immunizing BALB/c mice and Wistar rats intramuscularly, Split inactivated H3N2 vaccine adjuvanted with AP elicited higher serum hemagglutination-inhibition antibodies and IgG titers. Read More

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November 2021

Brucine-Loaded Ethosomal Gel: Design, Optimization, and Anti-inflammatory Activity.

AAPS PharmSciTech 2021 Nov 11;22(8):269. Epub 2021 Nov 11.

Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Hail, Saudi Arabia.

Brucine, one of the natural medications obtained from Nux vomica seeds, is used as an anti-inflammatory drug. Several investigations were performed to overcome its drawbacks, which will affect significantly its pharmaceutical formulation. The goal of the current investigation was to design, optimize, and evaluate the anti-inflammatory performance of BRU ethosomal gel. Read More

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November 2021

A Novel Method for Rapid Particle Size Analysis of Ibuprofen Using Near-infrared Spectroscopy.

AAPS PharmSciTech 2021 Nov 8;22(8):268. Epub 2021 Nov 8.

Institute of Chemistry, Faculty of Natural Sciences and Mathematics, Ss. Cyril and Methodius University in Skopje, Arhimedova 5, 1000, Skopje, Republic of North Macedonia.

Particle size distribution (PSD) is often considered as critical material attribute for active pharmaceutical ingredients (APIs), and the need for regular evaluation stands as an important quality control parameter in the pharmaceutical industry. Near-infrared (NIR) spectroscopy, used routinely for API identification, was introduced as analytical tool for simultaneous determination of particle size of ibuprofen. The demonstrated potential was highlighted by the development of rapid, robust, and noninvasive method coupled with multivariate data analysis (MVA), which can be easily transferred in QC laboratories for routine analysis. Read More

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November 2021

Recommended Best Practices for Lyophilization Validation 2021 Part II: Process Qualification and Continued Process Verification.

AAPS PharmSciTech 2021 Nov 8;22(8):266. Epub 2021 Nov 8.

Birck Nanotechnology Center, Purdue University, 1205 W State St., West Lafayette, IN, 47907, USA.

This work describes the lyophilization process validation and consists of two parts. Part one (Part I: Process Design and Modeling) focuses on the process design and is described in the previous paper, while the current paper is devoted to process qualification and continued process verification. The goal of the study is to show the cutting edge of lyophilization validation based on the integrated community-based opinion and the industrial perspective. Read More

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November 2021

Pharmacokinetics of Monoclonal Antibody and Antibody Fragments in the Mouse Eye Following Systemic Administration.

AAPS J 2021 11 8;23(6):116. Epub 2021 Nov 8.

Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, The State University of New York at Buffalo, 455 Pharmacy Building, Buffalo, New York, 14214-8033, USA.

The ocular pharmacokinetics (PK) of antibody-based therapies are infrequently studied in mice due to the technical difficulties in working with the small murine eye. This study is the first of its kind to quantitatively measure the PK of variously sized proteins in the plasma, cornea/ICB, vitreous humor, retina, and posterior cup (including choroid) of the mouse and to evaluate the relationship between molecular weight (MW) and antibody biodistribution coefficient (BC) to the eye. Proteins analyzed include trastuzumab (150 kDa), trastuzumab-vc-MMAE (T-vc-MMAE, 155 kDa), F(ab) (100 kDa), Fab (50 kDa), and scFv (27 kDa). Read More

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November 2021

Design and Characterization of HY-038 Solid Dispersions via Spray Drying Technology: In Vitro and In Vivo Evaluations.

AAPS PharmSciTech 2021 Nov 8;22(8):267. Epub 2021 Nov 8.

Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai, 201203, People's Republic of China.

The aim of this study was to prepare HY-038 solid dispersions (SDs) with single carrier at high drug loading and then forming a tablet to enhance solubility, dissolution, and bioavailability via spray drying technology. At the same time, we hope to develop a more convenient in vitro method to predict the absorption behavior of different formulations in vivo. Different solid dispersions, varying in drug/polymer ratios, were prepared. Read More

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November 2021

Immunogenicity Risk Assessment for Multi-specific Therapeutics.

AAPS J 2021 11 5;23(6):115. Epub 2021 Nov 5.

Bill & Melinda Gates Medical Research Institute, One Kendall Square, Building 600, Suite 6-301, Cambridge, Massachusetts, 02139, USA.

The objective of this manuscript is to provide the reader with a hypothetical case study to present an immunogenicity risk assessment for a multi-specific therapeutic as part of Investigational New Drug (IND) application. In order to provide context for the bioanalytical strategies used to support the multi-specific therapeutic presented herein, the introduction focuses on known immunogenicity risk factors. The subsequent hypothetical case study applies these principles to a specific example HC-12, based loosely on anti-TNFα and anti-IL-17A bispecific molecules previously in development, structured as an example immunogenicity risk assessment for submission to health authorities. Read More

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November 2021

Interrelationships Between Coating Uniformity and Efficiency in Pan Coating Processes.

AAPS PharmSciTech 2021 Nov 4;22(8):265. Epub 2021 Nov 4.

The University of British Columbia, Vancouver, British Columbia, Canada.

The relationships between coating uniformity and efficiency were explored for tablet coating processes in pan coaters. The factors affecting the size of the spray zone were modeled using one-dimensional deposition analysis of spray droplets. This model was incorporated into the analytical model developed for coating uniformity by Choi et al. Read More

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November 2021

Budding Multi-matrix Technology-a Retrospective Approach, Deep Insights, and Future Perspectives.

AAPS PharmSciTech 2021 Nov 3;22(8):264. Epub 2021 Nov 3.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500037, India.

The human race is consistently striving for achieving good health and eliminate disease-causing factors. For the last few decades, scientists have been endeavoring to invent and innovate technologies that can substitute the conventional dosage forms and enable targeted and prolonged drug release at a particular site. The novel multi-matrix technology is a type of matrix formulation where the formulation is embraced to have a matrix system with multiple number of matrices. Read More

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November 2021

Preformulation Studies to Guide the Production of Medicines by Fused Deposition Modeling 3D Printing.

AAPS PharmSciTech 2021 Nov 2;22(8):263. Epub 2021 Nov 2.

Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasilia, Brasília, DF, 70910-900, Brazil.

Fused deposition modeling (FDM) 3D printing has demonstrated high potential for the production of personalized medicines. However, the heating at high temperatures inherent to this process causes unknown risks to the drug product's stability. The present study aimed to assess the use of a tailored preformulation protocol involving physicochemical assessments, including the rheological profiles of the samples, to guide the development of medicines by FDM 3D printing. Read More

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November 2021

Quick and Simultaneous Analysis of Dissolved Active Pharmaceutical Ingredients and Formulation Excipients from the Dissolution Test Utilizing UHPLC and Charged Aerosol Detector.

AAPS PharmSciTech 2021 Nov 1;22(8):262. Epub 2021 Nov 1.

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Kyoto, Japan.

The objective of the study is to develop a quick and simultaneous analysis system for the dissolution of the active pharmaceutical ingredient (API) and the formulation excipient in samples from the dissolution test by UHPLC using the charged aerosol and PDA detectors. The combination of two columns for size-exclusion chromatography (SEC) and the equipment of the charged aerosol detector allowed the quick determination of various water-soluble polymers. Three model sustained-release tablets, each containing a different API of different water solubility (propranolol (soluble), ranitidine (very soluble), and cilostazol (practically insoluble)), were prepared from polyethylene oxide (PEO) matrix to verify the applicability and utility of the analysis system. Read More

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November 2021

Understanding Drug Delivery to the Brain Using Liposome-Based Strategies: Studies that Provide Mechanistic Insights Are Essential.

AAPS J 2021 10 28;23(6):114. Epub 2021 Oct 28.

Research Division of Systems Biomedicine and Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC, Leiden, The Netherlands.

Brain drug delivery may be restricted by the blood-brain barrier (BBB), and enhancement by liposome-based drug delivery strategies has been investigated. As access to the human brain is limited, many studies have been performed in experimental animals. Whereas providing interesting data, such studies have room for improvement to provide mechanistic insight into the rate and extent of specifically BBB transport and intrabrain distribution processes that all together govern CNS target delivery of the free drug. Read More

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October 2021

Enhancing Biopharmaceutical Attributes of Khellin by Amorphous Binary Solid Dispersions.

Authors:
Sonali S Bharate

AAPS PharmSciTech 2021 Oct 27;22(8):260. Epub 2021 Oct 27.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, 400056, India.

Khellin, a furanochromone isolated from fruits and seeds of Ammi visnaga, is traditionally used in many eastern Mediterranean countries. The plant decoction and the crystalline substance khellin have many pharmacological activities. For instance, it acts as a bronchodilator and also relieves renal colic and urethral stones, etc. Read More

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October 2021