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Advanced Drug Delivery Reviews Oct 2021Evaluation of orally ingestible devices is critical to optimize their performance early in development. Using animals as a pre-clinical tool can provide useful... (Review)
Review
Evaluation of orally ingestible devices is critical to optimize their performance early in development. Using animals as a pre-clinical tool can provide useful information on functionality, yet it is important to recognize that animal gastrointestinal physiology, pathophysiology and anatomy can differ to that in humans and that the most suitable species needs to be selected to inform the evaluation. There has been a move towards in vitro and in silico models rather than animal models in line with the 3Rs (Replacement, Reduction and Refinement) as well as the better control and reproducibility associated with these systems. However, there are still instances where animal models provide the greatest understanding. This paper provides an overview of key aspects of human gastrointestinal anatomy and physiology and compares parameters to those reported in animal species. The value of each species can be determined based upon the parameter of interest from the ingested device when considering the use of pre-clinical animal testing.
Topics: Administration, Oral; Animals; Dosage Forms; Drug Delivery Systems; Drug Evaluation, Preclinical; Gastrointestinal Tract; Humans; Models, Animal
PubMed: 34371085
DOI: 10.1016/j.addr.2021.113915 -
International Journal of Pharmaceutics Feb 2022The present paper reports the powder filling of milled electrospun materials in vials, which contained voriconazole and sulfobutylether-β-cyclodextrin. High-speed...
The present paper reports the powder filling of milled electrospun materials in vials, which contained voriconazole and sulfobutylether-β-cyclodextrin. High-speed electrospinning was used for the production of the fibrous sample, which was divided into 6 parts. Each portion was milled using different milling methods and sizes of sieves to investigate whether the milling influences the powder and filling properties. Bulk and tapped density tests, laser diffraction and angle of repose measurements were applied to characterize the milled powders, while a vibratory feeder was used for the feeding experiments. The correlation between the material property descriptors and the feeding responses was investigated by multivariate data analysis. Based on the results, three samples were chosen for the vial filling, which was accomplished with 3400 mg electrospun material containing 200 mg voriconazole, representative of the commercial product. The feed rate was set to fit the 240 g/h production rate of the electrospinning and the relative standard deviation of three repeated vial filling was determined to see the accuracy of the process. This research shows that by applying a suitable milling method it is possible to process electrospun fibers to a powder, which can be filled into vials and used as reconstitution dosage forms.
Topics: Emollients; Powders; Proof of Concept Study; Technology, Pharmaceutical; Voriconazole
PubMed: 34954004
DOI: 10.1016/j.ijpharm.2021.121413 -
Journal of Colloid and Interface Science Nov 2023Pharmaceutical formulation of oral dosage forms is continuously challenged by the low solubility of new drug candidates. Pickering emulsions, emulsions stabilized with...
Pharmaceutical formulation of oral dosage forms is continuously challenged by the low solubility of new drug candidates. Pickering emulsions, emulsions stabilized with solid particles, are a promising alternative to surfactants for developing long-term stable emulsions that can be tailored for controlled release of lipophilic drugs. In this work, a non-emulsifying lipid-based formulation (LBF) loaded with fenofibrate was formulated into an oil-in-water (O/W) emulsion synergistically stabilized by stearic acid and silica (SiO) nanoparticles. The emulsion had a droplet size of 341 nm with SiO particles partially covering the oil-water interface. In vitro lipid digestion was faster for the emulsion compared to the corresponding LBF due to the larger total surface area available for digestion. Cellulose biopolymers were added to the emulsion to produce a gel for semi-solid extrusion (SSE) 3D printing into tablets. The emulsion gel showed suitable rheological attributes for SSE, with a trend of higher viscosity, yield stress, and storage modulus (G'), compared to a conventional self-emulsifying lipid-based emulsion gel. The developed emulsion gel allows for a non-emulsifying LBF to be transformed into solid dosage forms for rapid lipid digestion and drug release of a poorly water-soluble drug in the small intestine.
Topics: Surface-Active Agents; Emulsions; Silicon Dioxide; Lipids; Nanoparticles; Water
PubMed: 37478742
DOI: 10.1016/j.jcis.2023.07.055 -
Clinical Pharmacology and Therapeutics Nov 2013Both researchers and practitioners have reached an influential period in the new era of developing pediatric medicines. Evolving regulatory reforms and guidance continue... (Review)
Review
Both researchers and practitioners have reached an influential period in the new era of developing pediatric medicines. Evolving regulatory reforms and guidance continue to serve as platforms steering research and development while distinctive opportunities and challenges in the field emerge. An advancing research need involves gaining a better understanding of end-user requirements and acceptability of formulations. This review considers solid oral forms to demonstrate the importance of such research to stakeholders in policy and practice.
Topics: Administration, Oral; Age Factors; Capsules; Child; Dosage Forms; Drug Evaluation; Humans; Tablets
PubMed: 23892403
DOI: 10.1038/clpt.2013.154 -
International Journal of Pharmaceutics Mar 2021Interest in 3D-printing technologies for pharmaceutical manufacturing of oral dosage forms is driven by the need for personalized medicines. Most research to date has...
Interest in 3D-printing technologies for pharmaceutical manufacturing of oral dosage forms is driven by the need for personalized medicines. Most research to date has focused on printing of polymeric-based drug delivery systems at high temperatures. Furthermore, oral formulation development is continuously challenged by the large number of poorly water-soluble drugs, which require more advanced enabling formulations to improve oral bioavailability. In this work, we used semi-solid extrusion (SSE) printing of emulsion gels with three types of emulsified lipid-based formulations (LBFs) to produce solid lipid tablets incorporating the poorly water-soluble drug, fenofibrate. Tablets were successfully 3D-printed from emulsion gels using SSE at room temperature, making the methodology particularly useful for thermolabile compounds. The tablets were well-defined in mass and disintegrated rapidly (<15 min). Importantly, the oil droplet size reconstituted after dispersion of the tablets and subsequent lipid digestion was similar to traditional liquid LBFs. This work demonstrates the successful use of SSE for fabricating solid lipid tablets based on emulsion gels. The method is further promising for on demand production of personalized dosage forms, necessary for flexible dosage adjustment in e.g., pediatric patients, when poorly water-soluble compounds constitute the core of the therapy.
Topics: Child; Drug Liberation; Emulsions; Gels; Humans; Lipids; Printing, Three-Dimensional; Tablets; Technology, Pharmaceutical
PubMed: 33540029
DOI: 10.1016/j.ijpharm.2021.120304 -
Acta Pharmaceutica (Zagreb, Croatia) Jun 2010Reversed-phase high-performance liquid chromatography (RP-HPLC) and thin-layer chromatography (TLC) methods have been developed and validated for simultaneous estimation...
Reversed-phase high-performance liquid chromatography (RP-HPLC) and thin-layer chromatography (TLC) methods have been developed and validated for simultaneous estimation of tamsulosin hydrochloride and finasteride in bulk drug and in combined dosage forms. RP-HPLC separation was achieved on a Phenomenex C18 column using methanol/0.02 mol L-1 ammonium acetate buffer/triethylamine (79.9 + 20 + 0.1, V/V/V) (pH 9.2) as mobile phase. TLC separation was achieved on an aluminium-backed layer of silica gel 60 F254 using toluene/methanol/triethylamine (9 + 1.5 + 1, V/V/V) as eluent. Quantification was achieved with photodiode array (PDA) detection at 235 nm over the concentration range 0.5-16 and 1-50 μg mL-1 with mean recovery of 99.8 ± 0.9 and 100.0 ± 0.8% for tamsulosin hydrochloride and finasteride, respectively, by the RP-HPLC method. Quantification was achieved with UV detection at 270 nm over the concentration range 100-2000 ng per spot and 250-5000 ng per spot with mean recovery of 98.9 ± 0.9 and 99.6 ± 0.7 % for tamsulosin hydrochloride and finasteride, respectively, by the TLC method. Both methods are simple, precise, accurate and sensitive and are applicable to the simultaneous determination of tamsulosin hydrochloride and finasteride in bulk drug and in combined dosage forms.
Topics: Chromatography, High Pressure Liquid; Chromatography, Reverse-Phase; Chromatography, Thin Layer; Dosage Forms; Finasteride; Pharmaceutical Preparations; Reproducibility of Results; Sulfonamides; Tablets; Tamsulosin
PubMed: 21134856
DOI: 10.2478/v10007-010-0013-z -
World Journal of Gastroenterology Jul 2014Helicobacter pylori (H. pylori) is one of the most common pathogenic bacterial infections and is found in the stomachs of approximately half of the world's population.... (Review)
Review
Helicobacter pylori (H. pylori) is one of the most common pathogenic bacterial infections and is found in the stomachs of approximately half of the world's population. It is the primary known cause of gastritis, gastroduodenal ulcer disease and gastric cancer. However, combined drug therapy as the general treatment in the clinic, the rise of antibiotic-resistant bacteria, adverse reactions and poor patient compliance are major obstacles to the eradication of H. pylori. Oral site-specific drug delivery systems that could increase the longevity of the treatment agent at the target site might improve the therapeutic effect and avoid side effects. Gastroretentive drug delivery systems potentially prolong the gastric retention time and controlled/sustained release of a drug, thereby increasing the concentration of the drug at the application site, potentially improving its bioavailability and reducing the necessary dosage. Recommended gastroretentive drug delivery systems for enhancing local drug delivery include floating systems, bioadhesive systems and expandable systems. In this review, we summarize the important physiological parameters of the gastrointestinal tract that affect the gastric residence time. We then focus on various aspects useful in the development of gastroretentive drug delivery systems, including current trends and the progress of novel forms, especially with respect to their application for the treatment of H. pylori infections.
Topics: Administration, Oral; Animals; Anti-Bacterial Agents; Chemistry, Pharmaceutical; Dosage Forms; Drug Carriers; Drug Therapy, Combination; Helicobacter Infections; Helicobacter pylori; Humans; Proton Pump Inhibitors; Technology, Pharmaceutical; Treatment Outcome
PubMed: 25071326
DOI: 10.3748/wjg.v20.i28.9321 -
Farmacia Hospitalaria : Organo Oficial... 2013The aims of this paper are to review the pharmaceutical guide in order to include suitable dosage forms for patients with dysphagia and to establish specific... (Review)
Review
PURPOSE
The aims of this paper are to review the pharmaceutical guide in order to include suitable dosage forms for patients with dysphagia and to establish specific recommendations for the drug administration.
METHODS
A comprehensive literature review was performed to develop general recommendations. Three topics were checked for every drug: a) alternative dosage forms suitable to patients with dysphagia; b) appropriateness of crushing tablets and opening capsules; and c) are these drugs suitable be mixed with food?
RESULTS
An algorithm was designed in order to help clinicians to select the best pharmaceutical form and its optimal administration method. The former pharmaceutical guide was modified and handling recommendations were made for each drug. Eleven dispersable, 26 liquid and 8 powder new forms were included.
CONCLUSIONS
This work has turned the pharmaceutical guide of the hospital in a useful tool for the prescription, validation and administration of medicines to patients with dysphagia.
Topics: Administration, Oral; Administration, Topical; Adult; Airway Obstruction; Algorithms; Deglutition Disorders; Dosage Forms; Drug Prescriptions; Food-Drug Interactions; Guideline Adherence; Hospitals, Urban; Humans; Pharmaceutical Preparations; Pharmacy Service, Hospital; Powders; Practice Guidelines as Topic
PubMed: 23789798
DOI: 10.7399/FH.2013.37.3.577 -
Acta Pharmaceutica (Zagreb, Croatia) Mar 2016A novel, simple and robust high-performance liquid chromatography (HPLC) method was developed and validated for simultaneous determination of xipamide (XIP), triamterene...
A novel, simple and robust high-performance liquid chromatography (HPLC) method was developed and validated for simultaneous determination of xipamide (XIP), triamterene (TRI) and hydrochlorothiazide (HCT) in their bulk powders and dosage forms. Chromatographic separation was carried out in less than two minutes. The separation was performed on a RP C-18 stationary phase with an isocratic elution system consisting of 0.03 mol L(-1) orthophosphoric acid (pH 2.3) and acetonitrile (ACN) as the mobile phase in the ratio of 50:50, at 2.0 mL min(-1) flow rate at room temperature. Detection was performed at 220 nm. Validation was performed concerning system suitability, limits of detection and quantitation, accuracy, precision, linearity and robustness. Calibration curves were rectilinear over the range of 0.195-100 μg mL(-1) for all the drugs studied. Recovery values were 99.9, 99.6 and 99.0 % for XIP, TRI and HCT, respectively. The method was applied to simultaneous determination of the studied analytes in their pharmaceutical dosage forms.
Topics: Calibration; Chromatography, High Pressure Liquid; Hydrochlorothiazide; Powders; Reproducibility of Results; Triamterene; Xipamide
PubMed: 26959547
DOI: 10.1515/acph-2016-0022 -
Acta Poloniae Pharmaceutica 2013Solid-phase extraction method followed by direct UV spectrophotometry at 264 nm was developed and applied for the selective ibuprofen determination in two-component...
Solid-phase extraction method followed by direct UV spectrophotometry at 264 nm was developed and applied for the selective ibuprofen determination in two-component formulation of ibuprofen and pseudoephedrine-HCl, combined powder which contains ibuprofen in the form of salt with L-arginine and 10% ibuprofen cream. Procedures for ibuprofen determination in complex pharmaceutical preparations by direct UV spectrophotometry lack selectivity because of interferences of other active substances and fat components. A limited number of spectrophotometric methods applicable to these samples are based on derivative (first and second-order) UV spectroscopy. Common HPLC procedures are more selective but more expensive and for creams also require some type of extraction because the large amount of oily excipients would clog up the column. The proposed solid-phase extraction method proved to be suitable for analysis of ibuprofen in combined tablets, powders and creams by direct UV spectrophotometry. Also the method provides an effective clean-up of the cream and allows ibuprofen determination by HPLC analysis. For the extraction three different commercial sorbents were tested: anion exchange Oasis MAX, hydrophilic-lipophilic balanced Oasis HLB and reverse-phase Chromabond C18ec. The optimization of the SPE method was first done on standard ibuprofen solutions and then the suitability of the method was checked on solutions of commercial pharmaceutical samples. The method yields good results for all three types of commercial preparations on the anion-exchange Oasis MAX cartridges, with recoveries of 90-100.2%. The interferences in UV analysis were not registered and good precision (RSD < 6%) was obtained. The present method has been verified as accurate as the reference HPLC with the great advantage of less expensive instrumentation. For this reason, the method would be suitable for a routine and rapid drug quality control.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Ibuprofen; Ointments; Powders; Solid Phase Extraction; Spectrophotometry, Ultraviolet; Tablets
PubMed: 23757930
DOI: No ID Found