In-vitro Bioadhesion of a Buccal, Miconazole Slow-release Tablet

Bouckaert, Stefan; Remon, Jean Paul

doi:10.1111/j.2042-7158.1993.tb05588.x

Cited by 68 publications

(18 citation statements)

References 13 publications

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“…The microenvironment pH of different batches showed the acidic nature of CP 940P. 23) Folding endurance was found to more than 300 for each case, indicative of reasonable flexibility of the films.…”

Section: Resultsmentioning

confidence: 91%

In Vitro and in Vivo Evaluation of Buccal Bioadhesive Films Containing Salbutamol Sulphate

Singh

Soni

Rawat

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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The aim of present study was to prepare and evaluate buccal bioadhesive films of salbutamol sulphate (SS) for the treatment of asthma. The films were designed to release the drug for a prolonged period of time so as to reduce the frequency of administration of the available conventional dosage forms of SS. The different proportions of sodium carboxymethylcellulose (SCMC) and Carbopol 940P (CP 940P) were used for the preparation of films. Carbopol was used to incorporate the desired bioadhesiveness in the films. The films were prepared by solvent casting method and evaluated for bioadhesion, in vitro drug release and anti asthmatic effect (bronchoprotection) in histamine induced bronchospasm of guinea pigs. In vitro drug release from the film was determined using a modified Franz diffusion cell while bioadhesiveness was evaluated with a modified two-arm balance using guinea pig buccal mucosa as a model tissue. Films containing SCMC : CP 940P ratio of 76 : 24 was found to be the best with moderate swelling along with favorable bioadhesion force and in vitro drug release. The drug release mechanism was found to follow non-Fickian diffusion as release mechanism. The prolonged in vivo effect (bronchoprotection) obtained from the buccal bioadhesive film of SS administered via buccal route may improve the treatment of asthmatic disorders by reducing the frequency of administration which is associated with the tolerance effect of SS. Additionally for the clinical benefit, it is also expected to reduce the major adverse effects of SS such as tachycardia and arrhythmias via buccal absorption.Key words salbutamol sulphate; buccal bioadhesive film; Carbopol 940P; in vivo effect Chem. Pharm. Bull. 58(3) 307-311 (2010)

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Section: Resultsmentioning

confidence: 91%

In Vitro and in Vivo Evaluation of Buccal Bioadhesive Films Containing Salbutamol Sulphate

Singh

Soni

Rawat

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Comparative observation was obtained by Bouckaert and Remon; [11] 30% miconazole nitrate didn't influence the bioadhesive characteristics of tablets containing thermally modified starch and CP907, whereas a significant decrease in bioadhesion was seen at a concentration of 50% miconazole nitrate. Regarding the bilayer formulae (CP 2 , CP 4 , PC 2 ,PC 4 and C 3 ) no effect on bioadhesion was observed due to the presence of the drug in the outer release layer and the plain layer is in contact with the mucus ( Table 2).…”

Section: Resultsmentioning

confidence: 95%

Mucoadhesive Delivery Systems. II. Formulation and In‐Vitro/In‐Vivo Evaluation of Buccal Mucoadhesive Tablets Containing Water‐Soluble Drugs

Nafee

Ismail

Boraie

et al. 2004

Drug Development and Industrial Pharmacy

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From the previous work (Part I), mucoadhesive formulae containing 5% CP/65% HPMC/30% lactose and 2% PC/68% HPMC/30% mannitol as well as formulae based on sodium carboxymethyl cellulose (SCMC) were selected. Medicated tablets were prepared using diltiazem hydrochloride (DZ) and metclopramide hydrochloride (MP) in two different doses (30 and 60 mg). The effect of drug and dose on the mucoadhesive properties and in-vitro drug release was evaluated. All formulae produced extended drug release (over 8 to 12 h). Polyacrylic acid based matrices (PAA) showed Fickian's diffusion release pattern for both drugs. SCMC ensured zero-order release for DZ, which deviated to anomalous behavior in case of MP. Doubling the dose significantly reduced the bioadhesion strength (p<0.05) with a slight improvement in drug release rate. The formulation of bilayer tablets containing drug-free layer and medicated layer enhanced the drug release without affecting the bioadhesive performance. The bilayer tablet formulated with 2% PC/68% HPMC/30% mannitol (PC2) was selected for studying the in-vivo metoclopramide release in four healthy volunteers. The tablet ensured controlled drug release for 12 h, in addition, good correlation (r=0.9398) was observed between in-vitro and in-vivo data. The effect of ageing on selected formulae containing DZ and MP, respectively, was studied. Storage at 40 degrees C and 75% relative humidity for 6 months didn't influence the mucoadhesive performance, however, an enhanced released rate was observed.

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“…Swine buccal mucosa was chosen as a substrate for the tensile bond strength, because its anatomical and physiological characteristics are similar to the human ones delivery (Squier & Wertz) were surgically removed and stored in a Bio-Freezer at -70ºC (Bouckaert & Remon, 1993. ) until the moment of the assays.…”

Section: Methodsmentioning

confidence: 99%

In vitro Fluoride Release and Tensile Bond Strength of a Polymeric Intra-Buccal Bioadhesive

Pedrazzi¹,

Lara²,

Panzeri³

et al. 2009

Int. J. Morphol.

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SUMMARY:The intra-buccal polymeric bioadhesive systems that can stay adhered to the oral soft tissues for drug programmed release, with the preventive and/or therapeutic purpose has been employed for large clinical situations. A system based on hydroxypropyl methyl cellulose/Carbopol 934'/magnesium stearate (HPMC/Cp/StMg) was developed having the sodium fluoride as active principle. This kind of system was evaluated according to its resistance to the removal by means of physical test of tensile strength. Swine buccal mucosa extracted immediately after animals' sacrifice was employed as substrate for the physical trials, to obtain 16 test bodies. Artificial saliva with or without mucin was used to involve the substrate/bioadhesive system sets during the trials. Artificial salivas viscosity was determined by means of Brookfield viscometer, showing the artificial saliva with mucin 10.0 cP, and the artificial saliva without mucin 7.5 cP. The tensile strength assays showed the following averages: for the group "artificial saliva with mucin" -12.89 Pa, and for the group "without mucin" -12.35 Pa. Statistical analysis showed no significant difference between the assays for both artificial salivas, and it was possible to conclude that the variable mucin did not interfered with the bioadhesion process for the polymeric devices. The device was able to release fluoride in a safe, efficient and constant way up to 8 hours.

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In-vitro Bioadhesion of a Buccal, Miconazole Slow-release Tablet

Cited by 68 publications

References 13 publications

In Vitro and in Vivo Evaluation of Buccal Bioadhesive Films Containing Salbutamol Sulphate

In Vitro and in Vivo Evaluation of Buccal Bioadhesive Films Containing Salbutamol Sulphate

Mucoadhesive Delivery Systems. II. Formulation and In‐Vitro/In‐Vivo Evaluation of Buccal Mucoadhesive Tablets Containing Water‐Soluble Drugs

In vitro Fluoride Release and Tensile Bond Strength of a Polymeric Intra-Buccal Bioadhesive

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