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Exploration of Parteck® SRP 80 and Hypromellose for Chronomodulated Release of LTD4 Receptor Antagonist and Statistical Optimization Using Central Composite Design

  • Research Article
  • Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract
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Abstract

To manage early morning symptoms of nocturnal bronchial asthma, a chronotherapeutic drug delivery system (ChrDDS) of montelukast sodium was designed and developed utilizing non-saccharide, fully synthetic Parteck® SRP 80, and hydrophilic cellulose derivative hydroxypropyl methylcellulose (HPMC). Recurrent lag phase, each followed by the release of a fraction of the drug dose, can be achieved by formulating a “tablets in a capsule” system containing more than one compressed coated tablet encapsulated in an enteric-coated capsule. Lag time in this study was controlled by the compressed coating of HPMC K4M and a blend of ethyl cellulose and Carbopol polymer. Assembly of the system includes two compressed coated tablets encapsulated in a capsule which was further proceeded for enteric coating in a conventional, a novel wax-based, and a Eudracap™ enteric-coated capsule. The optimized formulation of directly compressed tablets of Parteck ® SRP 80 showed a hardness of 8.8 kg/cm2 which is 1.25-fold higher than wet granulated tablets of HPMC. In vitro release data of matrix tablets of Parteck® SRP 80 demonstrated controlled release of drug for a duration of up to 10.8–11 h with changing ratio of polymer and filler. Eudracap™ capsule showed a minimum acid uptake value of 1.75%. The current approach can open a path for the time-regulated release of montelukast that may be beneficial for individuals with episodes of asthma attacks mostly in the early morning.

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Acknowledgements

The authors express gratitude towards Merck Pharmaceuticals Ltd., Mumbai India, Evonik Healthcare, Essen, Germany, and Shin-Etsu Chemical Tylose India Pvt. Ltd., Mumbai, for providing Parteck SRP 80, Eudracap™ ready-to-fill capsule, and HPMC phthalate respectively.

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Authors and Affiliations

  1. Faculty of Pharmaceutical Sciences, PES University, 50 Feet Road, Hanumanthnagar, BSK 1st stage-560050, Bengaluru, India

    Saniya Jawed & Satish CS

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  1. Saniya Jawed
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Saniya Jawed: methodology, carried out formulation and evaluation, writing the original draft. Satish CS: reviewing, editing, and supervision.

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Correspondence to Saniya Jawed.

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Jawed, S., CS, S. Exploration of Parteck® SRP 80 and Hypromellose for Chronomodulated Release of LTD4 Receptor Antagonist and Statistical Optimization Using Central Composite Design. AAPS PharmSciTech 23, 263 (2022). https://doi.org/10.1208/s12249-022-02415-5

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