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PubMed Journals Articles About "Comparison Of Two Formulations Of Proellex For Oral Administration" RSS

21:33 EST 15th January 2019 | BioPortfolio

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Showing "Comparison Formulations Proellex Oral Administration" PubMed Articles 1–25 of 10,000+

Age Impacts Olanzapine Exposure Differently During Use of Oral Versus Long-Acting Injectable Formulations: An Observational Study Including 8,288 Patients.

Olanzapine is a commonly prescribed antipsychotic available as oral and long-acting injectable (LAI) formulations. Data are lacking on the use and safety of olanzapine-LAI in older patients. The aim of this study was to investigate the effect of increasing age on olanzapine exposure during oral versus LAI administration in a real-life setting.


Pediatric Oral Formulations: An Updated Review of Commercially Available Pediatric Oral Formulations Since 2007.

Oral pediatric formulations are either ready-to-use or require manipulation, and multi-use or single-use. Strong encouragement for preservative-free pediatric formulations has resulted in fewer multi-use solutions or suspensions in favor of single-use solid oral dosage forms. This updated review covering new pediatric formulations marketed in the United States of America, Europe, and Japan spanning the years 2007 to mid-2018 identified 16 types of pediatric oral formulations of which 7 are ready-to-use and ...

Relative Oral Bioavailability of Two Amoxicillin-Clavulanic Acid Formulations in Healthy Dogs: A Pilot Study.

The use of human generic amoxicillin-clavulanic acid formulations in veterinary medicine is currently lacking supportive evidence. This pilot study was conducted to determine preliminary pharmacokinetic parameters and relative oral bioavailability of a human generic and veterinary proprietary 4:1 amoxicillin-clavulanic acid formulation in healthy dogs to evaluate whether drug exposure was similar and to determine if further comparative investigation is warranted. Each dog received a single oral dose of each...


The effect of administration media on palatability and ease of swallowing of multiparticulate formulations.

Multiparticulate formulations based on pellets, granules or beads, could be advantageous for paediatrics, geriatrics and patients with swallowing difficulties. However, these formulations may require suitable administration media to facilitate administration. The aim of this work was to investigate the effect of administration media properties on palatability and ease of swallowing of multiparticulates. A range of vehicles were developed using xanthan gum (XG) and carboxymethyl cellulose (CMC) as model hydr...

Recent advancements in oral administration of insulin-loaded liposomal drug delivery systems for diabetes mellitus.

Diabetes is a chronic medical condition, which is characterised by high blood sugar level. Exogenous insulin is commonly administered subcutaneously for the management of diabetes. However, daily injections of insulin could result in poor patient compliance and various side-effects. Although oral administration offers benefits, insulin is vulnerable to enzymatic degradation, chemical instability and poor gastrointestinal absorption. There is an absence of reviews on insulin-loaded liposomal drug carriers, d...

Stimulant Formulations for the Treatment of Attention-Deficit/Hyperactivity Disorder.

Clinicians have access to a variety of formulations of methylphenidate and amphetamine to treat attention-deficit/hyperactivity disorder (ADHD). However, due to new emerging formulations, clinicians may lack up-to-date knowledge about all available stimulant formulations. Presented here is a comprehensive guide to13 formulations of methylphenidate and 10 formulations of amphetamine that have US Food and Drug Administration approval to treat ADHD.

Abuse of immediate-release opioids and current approaches to reduce misuse, abuse, and diversion.

Deaths from opioid overdoses have increased dramatically over the past few years. Given that immediate-release (IR) opioids account for most of the US market share, and that abusers generally prefer IR opioids over extended-release (ER) opioids, it is not surprising that rates of abuse are higher for IR than ER opioids. IR opioids are widely prescribed, often without consideration for risks of abuse, misuse, and diversion. Prescription opioid abuse and misuse often begins through oral administration and pro...

Pharmacokinetic properties of a novel inosine analog, 4'-cyano-2'-deoxyinosine, after oral administration in rats.

4'-cyano-2'-deoxyinosine (SK14-061a), a novel nucleoside analog based on inosine, has antiviral activity against the human immunodeficiency virus type 1 that has the ability to acquire resistance against many types of reverse transcriptase inhibitors based on nucleosides. The aim of this study was to investigate the pharmacokinetics studies after its oral administration to rats. For this purpose, we first developed and validated an analytical method for quantitatively determining SK14-061a levels in biologi...

Impact on intestinal permeability of pediatric hyperosmolar formulations after dilution: studies with rat perfusion method.

There is no consensus on administering hyperosmolar formulations by mouth to neonates. In 1976, the Committee on Nutrition of the American Academy of Pediatrics published a recommendation of not administer formulations with an osmolarity higher than 400mOsm/L due to the possible damage to intestine and relationship with necrotizing enterocolitis. Since this recommendation, exists a general trend of reducing osmolality of oral formulations without considering the pharmacokinetics of absorption of the drugs. ...

Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid Based Formulations.

The absolute bioavailability of many small molecule kinase inhibitors (smKIs) is low. The reasons for low bioavailability are multifaceted and include constraints due to first pass metabolism and poor absorption. For smKIs where absorption limits oral bioavailability, low aqueous solubility and high lipophilicity, often in combination with high-dose requirements have been implicated in low and variable absorption, food-effects and absorption-related drug-drug interactions. The current study has evaluated wh...

Oral co-administration of a bacterial protease inhibitor in the vaccine formulation increases antigen delivery at the intestinal epithelial barrier.

The study of capture and processing of antigens (Ags) by intestinal epithelial cells is very important for development of new oral administration systems. Efficient oral Ag delivery systems must resist enzymatic degradation by gastric and intestinal proteases and deliver the Ag across biological barriers. The recombinant unlipidated outer membrane protein from Brucella spp. (U-Omp19) is a protease inhibitor with immunostimulatory properties used as adjuvant in oral vaccine formulations. In the present work ...

Mechanisms of poor oral bioavailability of flavonoid Morin in rats: From physicochemical to biopharmaceutical evaluations.

We recently reported that the absolute oral bioavailability of flavonoid Morin was extremely low at 0.45%, resulting in unsatisfied therapeutic efficacy in vivo. The present study was aimed to systemically assess the pre-absorption risks of Morin for rationale formulation design. Physicochemical properties of Morin were evaluated using in vitro assays including water solubility and stability in simulated gastric, intestinal fluids, followed by permeability tests in Caco-2 cells. The results suggested that b...

Pharmacokinetics and pharmacodynamics of intranasally administered selegiline nanoparticles with improved brain delivery in Parkinson's disease.

Selegiline, a well-known anti-Parkinson agent, is reported to be associated with poor oral bioavailability and safety. Therefore, we formulated selegiline as chitosan nanoparticles and evaluated its pharmacokinetics and pharmacodynamics after intranasal administration to rats relative to those after oral administration. The optimized formulation exhibited spherical nanoparticles with more than 90% drug loading and steady in vitro and ex vivo drug release. Selegiline concentrations in the brain and plasma we...

Updating formulations for compounded oral liquid medications in a university health system.

The development of a compounded oral liquid medication formulary and subsequent implementation of revised standard formulations in a university health system are described.

Microfabricated devices for oral drug delivery.

Oral administration of drugs is most convenient for patients and therefore the ultimate goal when developing new medication. The physical barriers in the body, low pH of the stomach and degradation by enzymes in the gastrointestinal tract are a few of the obstacles to succeeding with oral drug delivery. Microfabricated devices show promise to overcome some of these hindrances and thereby improve the bioavailability of drugs after oral administration. There is an increasing focus on microfabricated oral drug...

Oral Propranolol in a Child with Infantile Hemangioma of the Urethra.

Infantile hemangiomas (IH) are the most common in the head and neck region. They can occur anywhere in the skin, however, urethral hemangiomas are very rare. We describe a case report of a three years old boy with extensive lesions of IH in the anterior urethra. Urethral IH were disappeared during one year of oral administration of propranolol though it brought on urinary retention. This is the first report about oral propranolol treatment in a child with urethral IH. Oral administration of propranolol may ...

Biopolymer-Based Minimal Formulations Boost Viability and Metabolic Functionality of Probiotics Lactobacillus Rhamnosus GG through Gastrointestinal Passage.

The delivery of probiotic microorganisms as food additives via oral administration is a straightforward strategy to improve the intestinal microbiota. To protect probiotics from the harsh environments in stomach and small intestine, it is necessary to formulate them in biocompatible carriers, which finally release them in ileum and colon without losing their viability and functions. Despite of a major progress in various polymer-based formulations, many of them are highly heterogeneous and too large in size...

Quantitative prediction of oral bioavailability of a lipophilic antineoplastic drug bexarotene administered in lipidic formulation using a combined in vitro lipolysis/microsomal metabolism approach.

For performance assessment of the lipid-based drug delivery systems (LBDDS), in vitro lipolysis is commonly applied because traditional dissolution tests do not reflect the complicated in vivo micellar formation and solubilisation processes. Much of previous research on in vitro lipolysis have mostly focused on rank-ordering formulations for their predicted performances. In this study, we have incorporated in vitro lipolysis with microsomal stability to quantitatively predict the oral bioavailability of a l...

Optimization of nanostructured lipid carriers for Zidovudine delivery using a microwave-assisted production method.

An adapted methodology for obtaining lipid nanoparticles that only uses the microwave reactor in the synthesis process was developed. The method has the following features: one-pot, one-step, fast, practical, economical, safe, readiness of scaling-up, lack of organic solvents and production of nanoparticles with low polydispersity index (PDI) (below 0.3). This new method was applied for the development of nanostructured lipid carriers (NLC) loaded with a hydrophilic drug, the antiretroviral agent zidovudine...

Assessment of the preparation and administration of oral medications to institutionalized children.

to evaluate the preparation and administration of oral medications to institutionalized children by nursing professionals.

Safety and efficacy of intravenous ferric carboxymaltose in Japanese patients with iron-deficiency anemia caused by digestive diseases: an open-label, single-arm study.

Iron-deficiency anemia (IDA) accounts for majority of anemia. Although iron replacement therapy is effective, in Japan, conventional iron formulations have disadvantages such as gastrointestinal side effects for oral formulations and issues of frequent administration for intravenous (IV) formulations. Ferric carboxymaltose (FCM), which overcomes these limitations, is widely used as an IV iron source overseas. In this multi-center, open-label, single-arm study, we investigated the safety and efficacy of FCM ...

Long-term oral administration of Exendin-4 to control type 2 diabetes in a rat model.

Exendin-4 is a glucagon-like peptide-1 (GLP-1) receptor agonist and potent insulinotropic agent for type 2 diabetes patients; however, its therapeutic utility is limited due to the frequent injections required. Long-acting agonists reduce the number of injections, but they can compromise potency. In this study, chondroitin sulfate-g-glycocholic acid-coated and Exendin-4 (Ex-4)-loaded liposomes (EL-CSG) were prepared for oral administration of Ex-4. The Ex-4 loading efficiency was 77% and the loading content...

Drug-Lipid Conjugates for Enhanced Oral Drug Delivery.

Oral drug delivery route is one of the most convenient and extensively utilised routes for drug administration. But there exists class of drugs which exhibit poor bioavailability on oral drug administration. Designing of drug-lipid conjugates (DLCs) is one of the rationale strategy utilised in overcoming this challenge. This review extensively covers the various dimensions of drug modification using lipids to attain improved oral drug delivery. DLCs help in improving oral delivery by providing benefits like...

Alternative Pharmaceutical Formulation for Oral Administration of Rifampicin.

Tuberculosis (TB) is considered an emergency global public health, mainly due to the TB-HIV co-infection, bacillus dormancy stage, and emergence of resistant strains. In addition, the therapeutic toxicity and its pharmacokinetic interactions with other drugs may influence treatment non-compliance, low serum concentration of drugs, and, consequently, treatment failure. Strategies using nanotechnology represent a new tool for the therapy, since they are effective delivery systems due to the possibility of sol...

Pharmacokinetics and Comparative Bioavailability of a Levothyroxine Sodium Oral Solution and Soft Capsule.

A new formulation of levothyroxine sodium has been developed in the form of an oral solution contained in unit-dose ampules. A study has been conducted to compare the bioavailability of levothyroxine sodium oral solution and levothyroxine sodium soft capsule in healthy volunteers under fasting conditions. The rate and extent of absorption of the new levothyroxine solution were also evaluated when administered on dilution in water or directly into the mouth without water. In each period, according to the ran...


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