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Carnauba wax as a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of highly soluble drugs.
Mater Sci Eng C Mater Biol Appl. 2017 Jan 01; 70(Pt 1):250-257.MS

Abstract

Mini-tablets are a new tendency in solid dosage form design for overcoming therapeutic obstacles such as impaired swallowing and polypharmacy therapy. Among their advantages, these systems offer therapeutic benefits such as dose flexibility and combined drug release patterns. The use of lipids in the formulation has also drawn considerable interest as means to modify the drug release from the dosage form. Therefore, this paper aimed at developing sustained release mini-tablets containing the highly soluble drugs captopril and metformin hydrochloride. Carnauba wax was used as a lipid component in melt granulation, targeting the improvement of the drugs poor flowability and tabletability, as well as to sustain the drug release profiles in association with other excipients. To assist sustaining the drug release, Ethocel™ (EC) and Kollicoat® SR 30D associated with Opadry® II were employed as matrix-forming and reservoir-forming materials, respectively. The neat drugs, granules and the bulk formulations were evaluated for their angle of repose, compressibility index, Hausner ratio and tabletability. Mini-tablets were evaluated for their weight variation, hardness, friability, drug content and in-vitro drug release. The results indicated that melt granulation with carnauba wax improved the flow and the tabletability of the drugs, allowing the preparation of mini-tablets with adequate tensile strength under reduced compaction pressures. All mini-tablet formulations showed acceptable hardness (within the range of 1.16 to 3.93Kp) and friability (<0.1%). The melt-granulated captopril in matrix systems containing 50% EC (45P, 100P or 100FP) and the melt-granulated metformin hydrochloride in reservoir systems coated with Kollicoat® SR 30D and Opadry® II (80:20 with 10% weight gain or 70:30 with 20% weight gain) exhibited release profiles adequate to sustained release formulations, for over 450min. Therefore, carnauba wax proved to be a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of soluble drugs.

Authors+Show Affiliations

Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil.Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis 88040-970, Brazil. Electronic address: hellen.stulzer@ufsc.br.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27770888

Citation

Nart, Viviane, et al. "Carnauba Wax as a Promising Excipient in Melt Granulation Targeting the Preparation of Mini-tablets for Sustained Release of Highly Soluble Drugs." Materials Science & Engineering. C, Materials for Biological Applications, vol. 70, no. Pt 1, 2017, pp. 250-257.
Nart V, Beringhs AO, França MT, et al. Carnauba wax as a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of highly soluble drugs. Mater Sci Eng C Mater Biol Appl. 2017;70(Pt 1):250-257.
Nart, V., Beringhs, A. O., França, M. T., de Espíndola, B., Pezzini, B. R., & Stulzer, H. K. (2017). Carnauba wax as a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of highly soluble drugs. Materials Science & Engineering. C, Materials for Biological Applications, 70(Pt 1), 250-257. https://doi.org/10.1016/j.msec.2016.07.070
Nart V, et al. Carnauba Wax as a Promising Excipient in Melt Granulation Targeting the Preparation of Mini-tablets for Sustained Release of Highly Soluble Drugs. Mater Sci Eng C Mater Biol Appl. 2017 Jan 1;70(Pt 1):250-257. PubMed PMID: 27770888.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Carnauba wax as a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of highly soluble drugs. AU - Nart,Viviane, AU - Beringhs,André O'Reilly, AU - França,Maria Terezinha, AU - de Espíndola,Brenda, AU - Pezzini,Bianca Ramos, AU - Stulzer,Hellen Karine, Y1 - 2016/07/27/ PY - 2016/03/15/received PY - 2016/06/24/revised PY - 2016/07/26/accepted PY - 2016/10/25/pubmed PY - 2017/4/18/medline PY - 2016/10/25/entrez KW - Apparatus 3 KW - Carnauba wax KW - Highly soluble drug KW - Melt granulation KW - Mini-tablets KW - Sustained release SP - 250 EP - 257 JF - Materials science & engineering. C, Materials for biological applications JO - Mater Sci Eng C Mater Biol Appl VL - 70 IS - Pt 1 N2 - Mini-tablets are a new tendency in solid dosage form design for overcoming therapeutic obstacles such as impaired swallowing and polypharmacy therapy. Among their advantages, these systems offer therapeutic benefits such as dose flexibility and combined drug release patterns. The use of lipids in the formulation has also drawn considerable interest as means to modify the drug release from the dosage form. Therefore, this paper aimed at developing sustained release mini-tablets containing the highly soluble drugs captopril and metformin hydrochloride. Carnauba wax was used as a lipid component in melt granulation, targeting the improvement of the drugs poor flowability and tabletability, as well as to sustain the drug release profiles in association with other excipients. To assist sustaining the drug release, Ethocel™ (EC) and Kollicoat® SR 30D associated with Opadry® II were employed as matrix-forming and reservoir-forming materials, respectively. The neat drugs, granules and the bulk formulations were evaluated for their angle of repose, compressibility index, Hausner ratio and tabletability. Mini-tablets were evaluated for their weight variation, hardness, friability, drug content and in-vitro drug release. The results indicated that melt granulation with carnauba wax improved the flow and the tabletability of the drugs, allowing the preparation of mini-tablets with adequate tensile strength under reduced compaction pressures. All mini-tablet formulations showed acceptable hardness (within the range of 1.16 to 3.93Kp) and friability (<0.1%). The melt-granulated captopril in matrix systems containing 50% EC (45P, 100P or 100FP) and the melt-granulated metformin hydrochloride in reservoir systems coated with Kollicoat® SR 30D and Opadry® II (80:20 with 10% weight gain or 70:30 with 20% weight gain) exhibited release profiles adequate to sustained release formulations, for over 450min. Therefore, carnauba wax proved to be a promising excipient in melt granulation targeting the preparation of mini-tablets for sustained release of soluble drugs. SN - 1873-0191 UR - https://www.unboundmedicine.com/medline/citation/27770888/Carnauba_wax_as_a_promising_excipient_in_melt_granulation_targeting_the_preparation_of_mini_tablets_for_sustained_release_of_highly_soluble_drugs_ DB - PRIME DP - Unbound Medicine ER -