# Montelukast microsuspension with hypromellose for improved stability and oral absorption.
> ヒプロメロースを用いたモンテルカストマイクロサスペンションの安定性および経口吸収性の向上


## Abstract

Montelukast (MTK), used clinically for asthma and rhinitis and under investigation for Alzheimer's dementia, was formulated as an oral microsuspension (MS) using hypromellose (HPMC) as a polymeric suspending agent. Amorphous MTK particles suspended in aqueous vehicles readily crystallized and aggregated, substantially reducing dissolution rates. Incorporation of HPMC markedly inhibited crystal growth, improving both drug stability and dissolution profiles. Raman spectroscopy confirmed intermolecular hydrogen bonding between MTK particles and HPMC. Pharmaceutical additives such as sucrose and simethicone, as well as storage temperature, significantly influenced crystal growth and dissolution behavior. In rat pharmacokinetic studies, the optimized HPMC-based MS demonstrated bioavailability more than 80% greater than that of a commercially available granule formulation, suggesting this liquid preparation may improve oral absorption and patient compliance.

### Mechanism

HPMC adsorbs onto amorphous MTK particle surfaces and forms intermolecular hydrogen bonds, inhibiting crystal nucleation and growth, which in turn enhances dissolution rate and oral bioavailability in vivo.

## Bibliographic

- **Authors**: Park HJ, Park DW, Ho MJ, Kim DY, Lee H, Kim EJ, et al.
- **Journal**: Int J Biol Macromol
- **Year**: 2021 (2021-07-31)
- **PMID**: [34051251](https://pubmed.ncbi.nlm.nih.gov/34051251/)
- **DOI**: [10.1016/j.ijbiomac.2021.05.151](https://doi.org/10.1016/j.ijbiomac.2021.05.151)
- **Study type**: animal study
- **Delivery route**: not specified
- **Effect reported**: positive

## Delivery context

The delivery route is not clearly identifiable from this paper. For hydrogen intake, inhalation is the most efficient route; inhalation, however, carries explosion risk (empirical LFL of 10%; high-concentration devices are not recommended).

## Safety notes

The delivery route is not clearly identifiable from this paper. For hydrogen intake, inhalation is the most efficient route; inhalation, however, carries explosion risk (empirical LFL of 10%; high-concentration devices are not recommended).

See also:
- [Inhalation concentration and LFL / UFL](https://h2-papers.org/en/safety-notes/inhalation-concentration)
- [Consumer Affairs Agency accident cases](https://h2-papers.org/en/safety-notes/accident-cases)

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> **Cite as**: H2 Papers — PMID 34051251. https://h2-papers.org/en/papers/34051251
> **Source**: PubMed PMID [34051251](https://pubmed.ncbi.nlm.nih.gov/34051251/)