In-vitro evaluation of bioadhesion in particulate systems and possible improvement using interactive mixtures

Bredenberg, Susanne; Nyström, Christer

doi:10.1211/002235702423

Cited by 10 publications

(8 citation statements)

References 60 publications

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“…Camphor and menthol were chosen as sublimable materials, to induce pores into the compressed tablets, as they have the ability to sublimate (i.e., transit from solid phase directly to vapor phase without passing through an intermediate liquid phase). Kollidon CL was included in the formulations as a bioadhesive component in order to increase the contact time of vinpocetine at the sublingual mucosa, thereby reduce the potential intra/inter-individual variability resulting from swallowing the drug [13, 25]. Nevertheless, it is reported that Kollidon CL does not interfere with the rapid disintegration of the tablets [26].…”

Section: Resultsmentioning

confidence: 99%

Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with β-Cyclodextrin and Hydroxy Acid

Aburahma

El-Laithy²,

Hamza³

2010

Sci. Pharm.

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The demand for sublingual tablets has been growing during the previous decades especially for drugs with extensive hepatic first-pass metabolism. Vinpocetine, a widely used neurotropic agent, has low oral bioavailability due to its poor aqueous solubility and marked first-pass metabolism. Accordingly, the aim of this work was to develop tablets for the sublingual delivery of vinpocetine. Initially, the feasibility of improving vinpocetine’s poor aqueous solubility by preparing kneaded solid systems of the drug with β-Cyclodextrin and hydroxy acids (citric acid and tartaric acid) was assessed. The solid system with improved solubility and dissolution properties was incorporated into porous tablets that rapidly disintegrate permitting fast release of vinpocetine into the sublingual cavity. The pores were induced into these tablets by directly compressing the tablets’ excipients with a sublimable material, either camphor or menthol, which was eventually sublimated leaving pores. The obtained results demonstrated that the tablets prepared using camphor attained sufficient mechanical strength for practical use together with rapid disintegration and dissolution. In vivo absorption study performed in rabbits indicated that the sublingual administration of the proposed porous tablets containing vinpocetine solid system with β-Cyclodextrin and tartaric acid could be useful for therapeutic application.

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Section: Resultsmentioning

confidence: 99%

Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with β-Cyclodextrin and Hydroxy Acid

Aburahma

El-Laithy²,

Hamza³

2010

Sci. Pharm.

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“…Another potential benefit to using the disintegrant Ac-DiSol is the mucoadhesivity of this excipient [20]. Although very few studies have been made using mucoadhesive rectal formulations [21], it has been suggested that the addition of mucoadhesive polymers to conventional solid suppositories can increase the bioavailability of certain drugs, particularly those that are sensitive to first passage metabolism [22].…”

Section: Discussion Relating To Suppositoriesmentioning

confidence: 99%

Comparative Drug Release Measurements in Limited Amounts of Liquid: A Suppository Formulation Study

Welch¹,

Ek²,

Strömme

2006

CDD

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A novel method for the investigation of drug formulations in limited liquid volumes is presented. The experimental setup consists of a measurement cell containing an absorbent sponge cloth placed between two parallel electrodes. Conductivity measurements are used to monitor the drug release from the dosage form. By varying the amount of water contained in the absorbent cloth surrounding the dosage form, it is possible to measure the drug release performance of the dosage form in very limited amounts of water. The method was employed to test four different tablet formulations consisting of the model drug NaCl incorporated in excipient matrices of hard fat, polyethylene glycol, microcrystalline cellulose and a mixture of microcrystalline cellulose and croscarmellose sodium (Ac-Di-Sol). The drug release rates of the different formulations in limited water volumes differed markedly from the release rates in an excess of water. Whereas the release rates from all tablet types in an excess of water showed only minor differences among the tablet types, the release rates from the tablets formulated with disintegrating excipients were clearly superior in limited water volumes. The developed method for drug release in limited volumes of liquid should be suitable for evaluation of rectal dosage forms.

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“…The development of the transmucosal tablet has been shown to be an advance in the delivery of fentanyl. This dosage form was designed to encourage retention of the active substance with the mucosa, so as to increase contact time at the absorption site and avoid the potential intraindividual and interindividual variability resulting from swallowing 25. Onset of action is rapid (8–11 minutes after administration), with available preparations showing dose proportionality 26.…”

Section: Approaches To Breakthrough Painmentioning

confidence: 99%

Fentanyl transmucosal tablets: current status in the management of cancer-related breakthrough pain

Prommer¹,

Ficek

2012

PPA

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Breakthrough pain is a newly recognized pain category that was first described by Portenoy and Hagen in 1990. The term describes pain that increases in intensity to “break through” chronic pain that is being controlled by a scheduled opioid regimen. The development of fluctuations in pain intensity is challenging due to their unpredictable nature, rapid onset, and need for rapid treatment intervention. Breakthrough pain has been treated by using an extra opioid dose in addition to the scheduled opioid being used for pain. Recommendations for dose and frequency are based on expert opinion only, and have included dosing based on a percentage of the total opioid dose. Other recommendations include increasing the regularly scheduled opioid dose. Clinical trials have now focused on delivery of opioids that have both potency and a rapid onset of action. Lipophilic opioids have received a substantial amount of study due to their quick absorption and rapid onset of analgesia. Lipophilic opioids that have been studied to date include transmucosal fentanyl, sublingual fentanyl, intranasal sufentanil, and oral and sublingual methadone. Initial clinical trials have established the superiority of transmucosal fentanyl as a breakthrough analgesic when compared with immediate-release oral opioid formulations. Problems with bioavailability have led to a search for newer formulations of transmucosal delivery. Newer formulations, such as fentanyl transmucosal tablets, have been developed to ensure superior delivery for the patient suffering from breakthrough pain. The purpose of this paper is to discuss the current status of transmucosal tablet formulations for cancer breakthrough pain.

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In-vitro evaluation of bioadhesion in particulate systems and possible improvement using interactive mixtures

Cited by 10 publications

References 60 publications

Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with β-Cyclodextrin and Hydroxy Acid

Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with β-Cyclodextrin and Hydroxy Acid

Comparative Drug Release Measurements in Limited Amounts of Liquid: A Suppository Formulation Study

Fentanyl transmucosal tablets: current status in the management of cancer-related breakthrough pain

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