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Interaction of pharmaceutical excipients with organic cation transporters.

Increasing evidences have shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on several transport function of uptake and efflux drug transporters. Herein, we investigated whether the excipients frequently used in many drug formulations affect transport function of organic cation transporters (OCTs) that are responsible for elimination of cationic drugs. Our finding revealed that solubilizing agents, Tweens, showed the most significant effect rbOCT1/2-mediated [3H]-MPP+ uptake in heterologous expressing cells. The haft inhibitory concentration (IC…

Excipients with specialized functions for effective drug delivery.

INTRODUCTION: There is a growing need for the development of pharmaceutical excipients that could improve product performance and overcome the shortcomings of new drug moieties, such as their poor solubility and membrane permeability, as well as to aid with modern manufacturing processes. AREAS COVERED: Different types of functional excipients are discussed in this paper, in terms of their roles in modern dosage forms to optimize drug delivery and manufacturability. Functions of specialized excipients that are covered in this article include the enhancement of drug membrane permeability, the …

Lumichrome complexation by cyclodextrins: influence of pharmaceutical excipients.

Complexation of the model drug lumichrome by 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD), the most widely used cyclodextrin derivative in pharmaceutical preparations, was investigated in this study. The influence of frequently used pharmaceutical excipients, i.e. alcohols (ethanol, glycerol, propylene glycol), buffers (phosphate, citrate) and tonicity modulators (NaCl, MgCl2) was evaluated by phase solubility, absorption and fluorescence emission spectra and fluorescence lifetime studies. Further, complex formation constants and fluorescence quantum yields were calculated. The formation of a …

Adverse effects of pharmaceutical excipients in drug therapy.

Everyone who prescribes a modern formulated drug is aware of the risks of adverse reactions due to the properties inherent in the active ingredients, but not all are aware of the latent risks due to the excipients. The latter risks are compounded when inappropriate and inferior quality excipients are used. When investigating reports of adverse drug reactions, the possibilities of excipient-contributed reactions must not be overlooked, though such possibilities may appear to be remote. Tragic accidents attributable to excipients have occurred and are on record. Preventive measures include frequ…

Sex-Dependence in the Effect of Pharmaceutical Excipients: Polyoxyethylated Solubilising Excipients Increase Oral Drug Bioavailability in Male but not Female Rats.

It is known that males and females respond differently to medicines and that differences in drug behaviour are due to inter-individual variability and sex specificity. In this work, we have examined the influence of pharmaceutical excipients on drug bioavailability in males and females. Using a rat model, we report that a portfolio of polyoxyethylated solubilising excipients (polyethylene glycol 2000, Cremophor RH 40, Poloxamer 188 and Tween 80) increase ranitidine bioavailability in males but not in females. The in vivo sex and excipient effects were reflected in vitro in intestinal permeabil…

Influence of temperature on the compression behavior of pharmaceutical excipients.

Tableting on an industrial scale is characterized by an increase in temperature, which is dependent on numerous factors. The aim of this study was to examine the glass transition temperature of frequently used polymers as a critical parameter on tablet properties. Tablets were produced in a tablet press equipped with a temperature-controlled die at four different temperatures ranging from 22 to 70 °C. While pure polymers were characterized for their temperature-dependent compressibility behavior using Heckel analysis, tableting was performed from binary blends containing lactose as a filler an

Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

Cyclodextrins (CDs) are oligosaccharides widely used in the pharmaceutical field. In this review, a detailed examination of the literature of the last two decades has been made to understand the role of CDs in nasal drug delivery systems. In nasal formulations, CDs are used as pharmaceutical excipients, as solubilizers and absorption promoters, and as active ingredients due to their several biological activities (antiviral, antiparasitic, anti-atherosclerotic, and neuroprotective). The use of CDs in nasal formulations allowed obtaining versatile drug delivery systems intended for local and sys…

Идентификация исследователей для стабилизации бескостного Аденовируса в качестве биофармацевтики.

Снижение беспорядочного тропизма местных аденовирусов с помощью бескостного аденовируса выгодно для его использования в качестве вектора генной терапии или компонента вакцины. Удаление белка волокна на местном аденовирусе отменяет несколько нежелательных взаимодействий; однако этот подход снижает физическую стабильность частиц. Для создания стабильного волокнистого аденовируса для использования в фармацевтических целях необходимо учитывать воздействие температуры и pH на характеристику устойчивости частиц. Наши результаты свидетельствуют о том, что стабильность аденовируса без волокна повышает

Совпадение в аннотации оригинала
Reducing the promiscuous tropism of native adenovirus by using fiberless adenovirus is advantageous toward its use as a gene therapy vector … idic conditions around pH 6. The stability of fiberless adenovirus can be further enhanced by using excipients. Excipient screening results indicate that the nonionic surfactant Pluronic F-68 and the amino acid glycine are potential stabilizers because of their ability to increase the thermal transition temperature of the virus particle and promote retention …

Use of Natural Gums and Mucilages as Pharmaceutical Excipients.

Polysaccharide rich gums and mucilages are produced by different natural sources such as plants, animals and microbial organisms to fulfil structural and physiological functions. Their diverse structural compositions with a broad range of physicochemical properties make them useful for inclusion in dosage forms for different purposes such as to improve manufacturing processes and/or to facilitate drug delivery. A number of natural gums and mucilages have been investigated for inclusion in pharmaceutical formulations for a variety of reasons. The search for new excipients continues to be an act…

The use of natural and synthetic phospholipids as pharmaceutical excipients.

In pharmaceutical formulations, phospholipids obtained from plant or animal sources and synthetic phospholipids are used. Natural phospholip … osomes. Natural phospholipids instead of synthetic phospholipids should be selected as phospholipid excipients for formulation development, whenever possible, because natural phospholipids are derived from renewable sources and produced with more ecologically friendly processes and are available in larger scale at relatively low costs compared to synthetic p …

Selection of solubility parameters for characterization of pharmaceutical excipients.

The solubility parameter (delta(2)), corrected solubility parameter (delta(T)) and its components (delta(d), delta(p), delta(h)) were determined for series of pharmaceutical excipients by using inverse gas chromatography (IGC). Principal component analysis (PCA) was applied for the selection of the solubility parameters which assure the complete characterization of examined materials. Application of PCA suggests that complete description of examined materials is achieved with four solubility parameters, i.e. delta(2) and Hansen solubility parameters (delta(d), delta(p), delta(h)). Selection of…

Toxicity of excipients--a Food and Drug Administration perspective.

Excipients are essential components of drug products. They are also potential toxicants. Examples of known excipient-induced toxicities include renal failure and death from diethylene glycol, osmotic diarrhea caused by ingested mannitol, hypersensitivity reactions from lanolin, and cardiotoxicity induced by propylene glycol. Proposals to test or market new drug products in the United States should adequately address the safety of the proposed exposure to the excipients in those products. The specific safety data that may be needed will vary depending upon the clinical situation, including such…

Pharmaceutical excipient development: the need for preclinical guidance.

Pharmaceutical excipients have a vital role in drug formulations, a role that has tended to be neglected as evidenced by the lack of mechanisms to assess excipient safety outside a new drug application process. Currently, it is assumed that an excipient is "Проверено" when the new drug formulation, of which it is a constituent, receives regulatory acceptance. Existing regulations and guidelines indicate that new (novel) excipients should be treated as new chemical entities with full toxicological evaluation. No guidance is available for potentially useful materials (essentially new excipients) …

Design expert analysis of tacrolimus compatibility with common excipients.

OBJECTIVE: Tacrolimus is a potent macrolide immunosuppressant widely utilized in solid organ transplantation and the management of autoimmune disorders. The current study aimed to investigate the compatibility of tacrolimus with four commonly used excipients, including sodium croscarmellose, hydroxypropyl methylcellulose (HPMC), magnesium stearate, and lactose monohydrate. SIGNIFICANCE: The design of Experiments transforms drug-excipient compatibility studies by allowing for a precise, data-driven evaluation of multiple key factors with minimal experimental runs, ensuring reliable formulation…

Exploration of surface tension measurement methods for pharmaceutical excipients.

Surface tension is a crucial functional indicator for various classes of pharmaceutical excipients, as highlighted in both the Pharmacopoeia of the People's Republic of China (ChP) < 9601 Guidelines for Functionality-related Characteristics of Pharmaceutical Excipients > and the United States Pharmacopoeia (USP) < 1059 Excipient Performance >. However, there are few systematic studies on surface tension measurement of pharmaceutical excipients, resulting in a lack of stable parameter support in practical applications. In this study, we aim to fill this gap by exploring three different methods …

Sex-specific effects of excipients on oral drug bioavailability.

The mechanism of action of excipients eliciting sex differences in drug bioavailability is poorly understood. In this study, the excipients Cremophor RH 40 (PEG 40 hydrogenated castor oil), Poloxamer 188 (2-methyloxirane) and Tween 80 (polyoxyethylene (80) sorbitan monooleate) were screened at 0.07 - 5% concentrations for their effect on ranitidine bioavailability in male and female Wistar rats. We show that all excipient concentrations significantly increased ranitidine bioavailability in male, but not female, rats. The effect of these excipients on the intestinal efflux transporters P-glycop…

Cucurbit[7]uril: an emerging candidate for pharmaceutical excipients.

Cucurbit[7]uril (CB[7]), belonging to the cucurbit[n]uril family (CB[n], n = 5-8, 10, or 13-15), may form host-guest complexes with a variety of small molecules of biomedical interest. The physical and chemical properties of the complexed drugs are often improved as a result of this complexation, suggesting the potential application of CB[7] as a pharmaceutical excipient. This review has summarized the most recent research progress reported between 2011 and early 2017 regarding the biocompatibility of CB[7] and the influence of CB[7] on the stability, solubility, biouptake, and biological acti

Excipients in Oral Antihistamines Can Perpetuate Allergic Contact Dermatitis.

Propylene glycol is a well-documented causative agent of allergic contact dermatitis (ACD). It is also reported to cause systemic dermatitis after ingestion of foods or medicines containing it and after intravenous injection of a medicine with propylene glycol in its base. We describe two adolescents with sensitivity to propylene glycol confirmed by patch testing whose dermatitis improved dramatically after cessation of oral antihistamines containing propylene glycol. We report these cases to alert providers to the potential for worsening of ACD due to systemic exposure to propylene glycol in

Vendor qualification for pharmaceutical excipients--GMP requirements and approach.

Excipients are, in the large majority of cases, not made specifically for pharmaceutical use. Most pharmaceutical excipient manufacturers supply less than 10% of the total production of that particular material for pharmaceutical use. Excipient product portfolio consists of hundreds of products differing in chemistry, origin and functionality and they are used in many different applications. The days of treating excipients like commodities and buying them without fully qualifying the source and the entire distribution chain have gone by as GMP regulations demands to ensure quality of other mat…

Inverse gas chromatographic determination of solubility parameters of excipients.

The principle aim of this work was an application of inverse gas chromatography (IGC) for the estimation of solubility parameter for pharmaceutical excipients. The retention data of number of test solutes were used to calculate Flory-Huggins interaction parameter (chi1,2infinity) and than solubility parameter (delta2), corrected solubility parameter (deltaT) and its components (deltad, deltap, deltah) by using different procedures. The influence of different values of test solutes solubility parameter (delta1) over calculated values was estimated. The solubility parameter values obtained for a…