Implications of In-Use Photostability: Proposed Guidance for Photostability Testing and Labeling to Support the Administration of Photosensitive Pharmaceutical Products, Part 2: Topical Drug Product

Baertschi, Steven W.; Clapham, David; Foti, Chris; Kleinman, Mark H.; Kristensen, Solveig; Reed, Robert A.; Templeton, Allen C.; Tønnesen, Hanne

doi:10.1002/jps.24396

Cited by 27 publications

(18 citation statements)

References 40 publications

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“…In 2010, Baertschi et al discussed the application of ICH Guideline to conduct drug stability tests [27]. After that, other papers from the same Authors were published, detailing the conduction of the tests on various pharmaceutical forms [28,29].…”

Section: Photodegradation Testingmentioning

confidence: 99%

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

Luca

Ioele

Spatari

et al. 2018

Int J Pharm Pharm Sci

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ABSTRACT1, 4-dihydropyridine calcium channels blockers (DHPs) are the most commonly used antihypertensive drugs. Unfortunately, these compounds have a significant degradability to light. The oxidation to the pyridine derivative represents the first, and in many cases the only, step of the degradation mechanism. The photodegradation process causes the complete loss of pharmacological activity and may trigger the formation of single and superoxide oxygen species, potentially responsible for phototoxic reactions. Several analytical techniques have been proposed for DHP determination in the presence of their photoproducts. Nowadays, DHPs are all marketed in solid formulations, especially tablets, because photodegradation is particularly fast in solution. Various approaches aimed to protect molecular integrity and therapeutic activity of these drugs from the effects of light are currently studied. This review covers the studies over the last years about photodegradation of the DHPs and the approaches to obtain photostable formulations of these drugs.

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Section: Photodegradation Testingmentioning

confidence: 99%

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

Luca

Ioele

Spatari

et al. 2018

Int J Pharm Pharm Sci

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“…On the other hand, it should be stressed that following topical administration several papers discussed the lack of photostability testing of pharmaceutical drug substances during or after administration. It is therefore necessary to examine how the existing instruments and existing guidelines aid the understanding of the photostability of topical drugs, which could be exposed to a significant amount of light after application to the skin [10,[17][18][19][20][21].…”

Section: Introductionmentioning

confidence: 99%

“…In addition a very thin layer (about 1 mm) of the drug products are often applied directly to the skin. Therefore, it is necessary to specify the photostability of API alone, as well as in the presence of other substances, including excipients or cosmetic ingredients [10].Ultraviolet radiation (UVR) is divided into the following bands: UVA (315-400 nm), UVB (280-315 nm), and UVC (100-280 nm). All UVC and 95% of UVB radiation are absorbed by the protective ozone layer in the stratosphere.…”

mentioning

confidence: 99%

“…On the other hand, several papers discussed the lack of photostability testing of pharmaceutical drug substances during or after administration. It is therefore necessary to examine how the existing instruments and existing guidelines aid the understanding of the photostability of topical drugs, which could be exposed to a significant amount of light after application to the skin [10,[17][18][19][20][21].Two main categories of drug products applied topically to the skin are identified: products applied for local action (creams, gels, sprays, solutions) and products applied for systemic effects-transdermal drug delivery systems. The aim of this study was to conduct a systematic review of the photostability of dermatological drugs applied topically to the skin for local effect.…”

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confidence: 99%

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confidence: 99%

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Photostability of Topical Agents Applied to the Skin: A Review

2019

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Topical treatment modalities have multiple advantages starting with the convenient application and non-invasive treatment and ending with the reduction of the risk of the systemic side effects. Active pharmaceutical substances must reach the desired concentration at the target site in order to produce a particular therapeutic effect. In contrast to other dosage forms topical agents applied to the skin may also be susceptible to photodegradation after application. That is why the knowledge of the susceptibility of these topical drugs to UV irradiation, which may contribute to their degradation or changes in chemical structure, is very important. Active pharmaceutical substances used in dermatology may differ both in chemical structure and photostability. Furthermore, various factors-such as light intensity and wavelength, pH, temperature, concentration-can influence the photodegradation process, which is reflected in particular in kinetics of photodegradation of active pharmaceutical substances as well as both the quantitative and qualitative composition of by-products. The aim of this study was to conduct a systematic review of the photostability of dermatological drugs, as well as of other substances commonly applied topically. The photostability of glucocorticosteroids, retinoids, and antifungal drugs as well as non-steroidal anti-inflammatory drugs applied topically and selected UV-filters have been discussed. Furthermore, the impact of photoinstability on the effectiveness of pharmacotherapy and some photostabilization strategies have been also included. the active pharmaceutical ingredient (API) must reach the desired concentration at the target site so that it provides a particular therapeutic effect. Appropriate API concentration will be obtained after the application of the recommended amount of drug product (a finished dosage form) to the skin [4]. The skin is the largest organ of the human body (1.5-2.0 m 2 ) that protects against external environmental factors, and thus is exposed to, among others, UV radiation and xenobiotics. Overcoming the barrier that constitutes the skin is possible for lipophilic substances with log P in the range of 1-3 and those with a low molecular weight (MW < 500 Da) [2]. Therefore, many substances applied topically that penetrate through the stratum corneum, reach the dermis and via dermal microcirculation could get into the systemic circulation causing systemic effects [2,3,5].The stability studies of APIs and drug products are a priority in the research and development of drugs. Information about the stability of the drug is necessary to ensure its appropriate quality, effectiveness, and safety for the patients [6,7]. General rules for conducting stability tests are included in the Guidance for Industry Q1A(R2) Stability Testing of New Drug Substances and Products which was developed by International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use [8]. The ultimate goal of the stability studies is to provide industry...

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Stability Testing

Clapham¹

2017

ICH Quality Guidelines

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Implications of In-Use Photostability: Proposed Guidance for Photostability Testing and Labeling to Support the Administration of Photosensitive Pharmaceutical Products, Part 2: Topical Drug Product

Cited by 27 publications

References 40 publications

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

Photostability of Topical Agents Applied to the Skin: A Review

Stability Testing

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