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Formulation and Characterization of Sublingual Tablets of Iloperidone Prepared by Microenvironmental pH Regulated Approach

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Abstract

Purpose

Iloperidone (Ilo) is an antipsychotic drug having low and pH-dependent solubility, hence less bioavailability. Thus, the aim of this study was to prepare and characterize binary (TAPOL B) and ternary complexes (TAPOL T) of drug with Kolliphor P-188 and tartaric acid to improve solubility. Further, sublingual tablets incorporating ternary complex were formulated to improve the dissolution.

Methods

Preliminary screening studies were conducted to select the acidifying agent and polymer based on saturation solubility studies. Binary and ternary complexes were prepared by the melting method. Complexes were characterized by DSC, powder X-ray diffraction (PXRD), FTIR, microenvironmental studies, and in vitro dissolution studies. The sublingual tablets of ternary complexes were prepared by the direct compression method and evaluated for weight variation, disintegration time, and dissolution studies.

Results

Based on solubility studies, Kolliphor P-188 and tartaric acid were selected as polymer and acidifying agents. DSC studies and FTIR spectra showed the interaction of drugs with polymer and acidifying agents. PXRD spectra showed the crystalline nature of complexes. Microenvironmental studies carried out in pH 6.8 showed a drastic decrease in pH with ternary complex as compared with binary complex. Dissolution studies showed an increase in dissolution, TAPOL T > TAPOL B > drug. The sublingual tablets showed disintegration time < 30 s and more than 80% of a drug released within 10 min. Due to the presence of tartaric acid and polymer, solubility of the drug increases tremendously.

Conclusion

The present study demonstrates the increase in solubility and release of Iloperidone due to the microenvironmental pH effect from sublingual tablets. Hence, microenvironmental pH modification is a good approach to increase drug solubility and dissolution.

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Authors and Affiliations

  1. Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’s NMIMS, Vile Parle [W], Mumbai, Maharashtra, 400056, India

    Akshayya Pawar, Vaishali Y. Londhe & Rupali S. Bhadale

Authors
  1. Akshayya Pawar
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  2. Vaishali Y. Londhe
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  3. Rupali S. Bhadale
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Correspondence to Vaishali Y. Londhe.

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Highlights

• Binary and ternary complexes of Ilo were formulated.

• Kolliphor P-188 and tartaric acid were optimized as a polymer and an auxiliary agent.

• Tartaric acid accelerated the dissolution efficiency of the drug due to pH change.

• DC tablets showed ≥ 80% release within 5 min for 12 mg, maximum strength.

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Pawar, A., Londhe, V.Y. & Bhadale, R.S. Formulation and Characterization of Sublingual Tablets of Iloperidone Prepared by Microenvironmental pH Regulated Approach. J Pharm Innov 17, 104–110 (2022). https://doi.org/10.1007/s12247-020-09502-9

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  • DOI: https://doi.org/10.1007/s12247-020-09502-9

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