Characterization of cellulosic hot-melt extruded films containing lidocaine

Repka, Michael A.; Gutta, Kavitha; Prodduturi, Suneela; Munjal, Manish; Stodghill, Steven P.

doi:10.1016/j.ejpb.2004.06.008

Cited by 152 publications

(88 citation statements)

References 17 publications

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“…In another study by Repka et al (86), oral mucoadhesive lidocaine-containing films were prepared with a combination of two cellulosic polymers HPC and HPMC, as the matrixforming polymer and drug-release modifier, respectively, using the HME process. Two formulations were prepared with one loaded with only HPC and the other with HPC:HPMC (80:20) and the homogeneous films produced had an average thickness of 0.66±0.01 mm.…”

Section: Filmsmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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Section: Filmsmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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“…Hot-melt processing has been demonstrated to be a viable method for the preparation of drug-incorporated polymeric matrices (8)(9)(10)(11)(12). Hot-melt processing requires a pharmaceutical grade thermoplastic polymer that can be processed at relatively low temperatures (low melting or glass transition temperatures) due to thermal sensitivity of many drugs.…”

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confidence: 99%

Preformulation Studies of a Prodrug of Δ9-Tetrahydrocannabinol

et al. 2008

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Abstract. Preformulation studies were performed on a hemiglutarate ester prodrug of Δ 9 -tetrahydrocannabinol (THC-HG), to facilitate the development of stable formulations by hot-melt methods. The various studies performed included solid-state thermal characterization, pKa, logP, aqueous and pH dependent solubility, pH stability and effect of moisture, temperature and oxygen on solid-state stability. A hot-melt method was utilized to fabricate THC-HG incorporated poly (ethylene oxide) (PEO) matrices and the bioadhesive properties, release profiles and post-processing stability of these matrices were assessed as a function of the polymer molecular weight. The prodrug exhibited a T g close to 0°C, indicating its amorphous nature. Thermogravimetric analysis revealed a rapid weight loss after 170°C. The prodrug exhibited a seven-fold higher aqueous solubility as compared to the parent drug (THC). Also, the solubility of the compound increased with increasing pH, being maximum at pH 8. The prodrug exhibited a v-shaped pH-rate profile, with the degradation rate minimum between pH 3 and 4. The moisture uptake and drug degradation increased with an increase in relative humidity. Solid-state stability indicated that the prodrug was stable at −18°C but demonstrated higher degradation at 4°C, 25°C and 40°C (51.6%, 74.5% and 90.1%, respectively) at the end of 3-months. THC-HG was found to be sensitive to the presence of oxygen. The release of the active from the polymeric matrices decreased, while bioadhesion increased, with an increase in molecular weight of PEO.

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“…Different polymers and drugs have been employed and reported in the literature for obtaining drug loaded hotmelt extruded films for various indications and are summarised in Repka and co-workers have conducted extensive research on the use of HME for the manufacture of mucoadhesive buccal films. They successfully evaluated different matrix formers and additives for the processing of the blend prior to extrusion [61,62,63,64]. In an early investigation, it was found that even though films containing exclusively HPC could not be obtained, the addition of plasticizers, such as triethyl citrate, PEG 2000/8000, or acetyltributyl citrate, allowed for the manufacture of thin, flexible, and stable HPC films [65].…”

Section: Films By Hot-melt Extrusionmentioning

confidence: 99%