A toxicological review of lactose to support clinical administration by inhalation

Baldrick, Paul; Bamford, D. G.

doi:10.1016/s0278-6915(97)00041-0

Cited by 41 publications

(21 citation statements)

References 48 publications

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“…It is also easily available in different grades and inexpensive [179]. Published inhalation studies in humans have shown no local effects of lactose exposure by inhalation [180]. Because the particles of lactose in these preparations are generally larger than the respirable range, the bulk of lactose will be deposited mostly in the mouth and throat where it is either hydrolysed by bacterial enzymes present in normal saliva or swallowed and subsequently metabolised by intestinal enzymes.…”

Section: Use Of Lactose As a "Carrier"mentioning

confidence: 99%

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Lactose characteristics and the generation of the aerosol

Pilcer¹,

Wauthoz²,

Amighi³

2012

Advanced Drug Delivery Reviews

178

113

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Section: Use Of Lactose As a "Carrier"mentioning

confidence: 99%

“…Furthermore, in contrast to oral administration, lactose swallowed at the levels present in inhaled preparations (i.e., up to 25 mg) is unlikely to present problems, even in patients with lactose intolerance [180].…”

Section: Use Of Lactose As a "Carrier"mentioning

confidence: 99%

Lactose characteristics and the generation of the aerosol

Pilcer¹,

Wauthoz²,

Amighi³

2012

Advanced Drug Delivery Reviews

178

113

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“…[16] In the pharmaceutical industry, α-lactose monohydrate is widely used as a filler or diluent in capsules and tablets. [17] Maltitol is made from maltose, is almost as sweet as sucrose and can, therefore, be used as its replacement. Sucrose is obtained from sugar cane, sugar beet or other sources and is widely used in oral pharmaceutical formulations.…”

Section: Mono-and Disaccharidesmentioning

confidence: 99%

“…[16,18,19] Differences between the spectra can also be seen in the region between 1200 and 1460 cm −1 which contains δ(CH) deformations and in the region between 1430 and 1480 cm −1 (plus Raman bands around 830 cm −1 ) which contains δ(CH 2 ) deformations. [17,19] Since these monomers and dimers lack any C O or C C bonds in their structures (see www.interscience.wiley.com/journal/jrs a Handbook of Pharmaceutical Excipients. [11] b Article by Pyne et al [14] Supporting Information), there are no Raman bands present above 1500 cm −1 .…”

Section: Mono-and Disaccharidesmentioning

confidence: 99%

Reference database of Raman spectra of pharmaceutical excipients

Veij

Vandenabeele

Beer

et al. 2008

J Raman Spectroscopy

197

100

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Raman spectroscopy has evolved into an important fast, direct and nondestructive technique in pharmaceutical analysis. Usually, the focus in this field is mainly on the active ingredients and not on the excipients present in the drugs. A collection of Raman spectra of widely used pharmaceutical excipients is presented in this article, which can serve as a reference for the interpretation of Raman spectra during drug analysis (including classical qualitative and quantitative pharmaceutical analysis, counterfeit tracing and process analytical technology (PAT) applications). The 43 analyzed excipients can be classified into seven categories: mono-and disaccharides (dextrose, lactitol, maltitol, lactose and sucrose), polysaccharides (microcrystalline cellulose, methylcellulose (MC), carboxymethylcellulose (CMC), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), wheat starch, maltodextrin, primojel, tragacanth and pectin), polyalcohols (propylene glycol, erythritol, xylitol, mannitol and sorbitol), carboxylic acids and salts (alginic acid, glycine, magnesium stearate, sodium acetate and sodium benzoate), esters (arachis oil, lubritab, dibutyl sebacate, triacetin, Eudragit E100 and Eudragit RL100), inorganic compounds (calcium phosphate, talc, anatase and rutile (TiO 2 ), calcium carbonate, magnesium carbonate, sodium bicarbonate and calcium sulfate) and some unclassified products [gelatin, macrogol 4000 (polyethylene glycol (PEG), polyvinyl pyrrolidone and sodium lauryl sulfate].

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“…Notwithstanding, the literature is devoid of comprehensive reviews of lactose safety when aimed at pulmonary delivery and most available data come from studies performed to assess the potential toxicity of formulations containing an active drug in the presence of lactose instead of evaluating lactose per se. Most results from these inhalation studies revealed no finding of toxicological significance with lactose although some of them comprised cases of minimal peribronchiolar lymphoid hyperplasia in the lungs and carina and also lymph node lymphocyte depletion together with alveolar macrophage infiltration in the lungs [7]. However, a causal relationship between lactose and these effects is yet to be disclosed.…”

Section: Introductionmentioning

confidence: 98%

Toxicological evaluation of lactose and chitosan delivered by inhalation

Valle

Dinis-Oliveira

Carvalho

et al. 2008

Journal of Biomaterials Science, Polymer Edition

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Abstract-These days, inhalation constitutes a promising administration route for many drugs. However, this route exhibits unique limitations, and formulations aimed at pulmonary delivery should include as few as possible additives in order to maintain lung functionality. The purpose of this work was to investigate the safety of lactose and chitosan to the pulmonary tissue when delivered by inhalation. The study was carried out with 18 Wistar rats divided in three groups receiving distilled water, lactose or chitosan. A solution of each excipient was administered by inhalation at a dose of 20 mg. The lungs were excised and processed to determine several biochemical parameters used as toxicity biomarkers. Protein and carbonyl group content, lipid peroxidation, reduced and oxidized glutathione (GSSG), myeloperoxidase (MPO), cooper/zinc and manganese superoxide dismutase, catalase, glutathione S-transferase and glutathione peroxidase were determined. Results of myeloperoxidase activity and glutathione disulfide lung concentrations showed a relevant decrease for chitosan group compared to control: 4.67 ± 2.27 versus 15.10 ± 7.27 (P = 0.011) for MPO and 0.89 ± 0.68 versus 2.02 ± 0.22 (P = 0.014) for GSSG. The other parameters did not vary significantly among groups. Lactose and chitosan administered by inhalation failed to show toxic effects to the pulmonary tissue. A protective effect against oxidative stress might even be attributed to chitosan, since some biomarkers had values significantly lower than those observed in the control group when this product was inhaled. Nevertheless, caution must be taken regarding chemical composition and technological processes applied to incorporate these products during drug formulation, in particular for dry powder inhalators.

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A toxicological review of lactose to support clinical administration by inhalation

Cited by 41 publications

References 48 publications

Lactose characteristics and the generation of the aerosol

Lactose characteristics and the generation of the aerosol

Reference database of Raman spectra of pharmaceutical excipients

Toxicological evaluation of lactose and chitosan delivered by inhalation

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