Orodispersible dosage forms: biopharmaceutical improvements and regulatory requirements

Cilurzo, Francesco; Franzè, Silvia; Selmin, Francesca; Minghetti, Paola

doi:10.1016/j.drudis.2017.10.003

Cited by 76 publications

(66 citation statements)

References 61 publications

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“…The value of this technic includes convenient administration in every day situations in which it is difficult to get water, for example when the patient is traveling or when he is in a work that can not be interrupt. Moreover, it might be decisive when the administration of the drug is urgent (13,14).…”

Section: Resultsmentioning

confidence: 99%

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

Pinho

Temer

Ribeiro

et al. 2018

Infarma

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Orodispersible tablets are getting popular due to its easy administration which leads to a higher therapeutic adherence. This study aimed to evaluate the state of the art of these drug products based on the scientific literature. Also, orodispersible tablets available in the US, Europe and Brazil markets based on information extracted from the health agencies were analyzed. Those tablets are designed to be placed on the tongue and instantly disintegrated by the fast capitation of the saliva without the additional intake of water. The orodispersible technology enables oral administration of tablets to patients with dysphagia, especially children, and elderlies. Moreover, orodispersible make possible rapid drug intervention and mouth absorption. The drug is partially absorbed in the oral cavity, pharynx, and esophagus without first pass effect, increasing drug bioavailability and reaching faster therapeutic effect. This is a low-cost technology that fits in a conventional solid production area and adds value to the product without requiring high investment. A market analysis showed there is a predominance of antihistamine drugs or medicines for mental disorders using orodispersible matrices. However, the orodispersible technology shows great versatility and potential application to other pharmacological groups. It is expected that in coming years a massive commercial insertion of this tablet technology occurs. In this scenery, it is indispensable that health professionals are prepared with updated technical information for the use of this therapeutic resource safely and efficiently. RESUMOOs comprimidos orodispersíveis têm ganhado popularidade por serem de fácil administração e levarem a uma maior adesão terapêutica. Esse estudo teve como objetivo avaliar o estado da arte desses medicamentos com base na literatura científica. Adicionalmente, foram levantados os comprimidos orodispersíveis disponíveis nos mercados dos EUA, Europa e Brasil com base em informações extraídas das agências sanitárias dessas regiões. Esses comprimidos são concebidos para serem colocados na boca e instantaneamente desintegrados pela captação da saliva, sem a necessidade de água. A tecnologia orodispersível viabiliza a administração oral de comprimidos em usuários com disfagia. Adicionalmente, esses medicamentos possibilitam uma rápida intervenção medicamentosa e absorção bucal, fazendo com que uma fração do fármaco seja absorvido na cavidade oral, faringe e esôfago sem sofrer efeito de primeira passagem, incrementando sua biodispobibilidade e permitindo alcançar um efeito terapêutico mais rápido. O barateamento dessa tecnologia, que se adapta a áreas de produção de sólidos convencionais, agrega valor ao medicamento sem demandar alto investimento.

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Section: Resultsmentioning

confidence: 99%

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

Pinho

Temer

Ribeiro

et al. 2018

Infarma

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“…They are usually taken without water and once in the buccal cavity they disintegrate rapidly in saliva, usually in a matter of seconds. ODTs may be significantly better than conventional dosage forms in terms of drug dissolution, absorption, onset of clinical effect and drug bioavailability [9,10]. In a study done by Shoukri et al it was found that the rate of absorption of nimesulide from ODT was faster than that from the reference tablet.…”

Section: Discussionmentioning

confidence: 99%

Options when anti-depressants cannot be used in conventional ways. Clinical case and review of literature

Das

Obiozor

Elwadhi

et al. 2019

Personalized Medicine in Psychiatry

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“…Technical issues concerning OTDD, ODT, and ODF preparation are beyond the aim of this review, but have been recently presented and discussed in some excellent reviews (Hoffmann et al ., ; Kathpalia & Gupte, ; Sattar et al ., ; Cilurzo et al ., ).…”

Section: Oral Transmucosal Drug Delivery Could Potentially Shorten Tmmentioning

confidence: 97%

“…ODT and ODF formulations have five interesting advantages compared to oral formulations if absorption occurs in the mouth (Kathpalia & Gupte, ; Cilurzo et al ., ): (1) a shorter T max , and T onset , depending on drug physicochemical properties and excipients; (2) an increase in drug bioavailability by preventing catabolism of the drug by the stomach and gut, and through the first passage effect; (3) no need to alter drug dosage compared with liquid formulations; (4) discrete intake of the drug since water is not usually required; and (5) elimination of swallowing issues that is present in the general population, specifically in 22% of patients aged > 50 years (Howden, ), and more evident in special subpopulations such as geriatric patients and those with dysphagia. The advantages of ODT and ODF formulation and, in particular, points 4 and 5, appear to be crucial for improving patient adherence to treatment.…”

Section: Oral Transmucosal Drug Delivery Could Potentially Shorten Tmmentioning

confidence: 99%

The first‐generation phosphodiesterase 5 inhibitors and their pharmacokinetic issue

et al. 2019

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Background Erectile dysfunction (ED) is a relatively frequent disease that negatively impacts the overall quality of life, well‐being, and relationships. Although the use of phosphodiesterase 5 inhibitors (PDE5is) has revolutionized the treatment of ED, a high percentage of ED patients discontinue PDE5i treatment. Objectives (i) To analyze the reasons for patient dissatisfaction leading to PDE5i discontinuation; (ii) analyze the pharmacokinetics of new formulations focusing on the time needed to reach an effective plasma concentration of PDE5is (Tonset) following drug intake; and (iii) summarize the physicochemical properties of sildenafil to understand which excipients may increase the absorption rate. Material and methods An online PubMed literature search was conducted to identify English language publications from inception to January 2019. Results The main reasons for patient dissatisfaction when using PDE5is on demand are the relatively long Tonset after taking vardenafil and sildenafil, including formulations such as film‐coated tablets, fine granules, orally disintegrating tablets (ODTs), and oral thin films (ODFs). The relatively long Tonset, further worsened when accompanied by eating, highlights the following: (i) the need for planning intercourse, determining partner‐related issues; (ii) issues when having sex before the maximum effect of the drug; and (iii) lower drug‐related placebo effects. Some data suggest that sildenafil is a ‘difficult’ molecule, but Tonset can be improved following absorption by buccal mucosa using appropriate excipients. Conclusions We conclude that several ODT and ODF formulations can improve the ‘discretion’ issue because they are taken without water, but they have similar pharmacokinetics to corresponding film‐coated tablet formulations. One ODF formulation of sildenafil was characterized by a shorter Tonset and could potentially increase patient satisfaction following treatment. However, more clinical studies are needed to confirm the findings. Surfactants and ascorbic acid appear to be crucial excipients for achieving a high absorption rate, but more studies are needed.

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Orodispersible dosage forms: biopharmaceutical improvements and regulatory requirements

Cited by 76 publications

References 61 publications

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

Options when anti-depressants cannot be used in conventional ways. Clinical case and review of literature

The first‐generation phosphodiesterase 5 inhibitors and their pharmacokinetic issue

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