Effects of Temperature and Solvent on the Solid-State Transformations of Pranlukast During Mechanical Milling

Xiong, Xiaopeng; Xu, Kailin; Du, Qiaohong; Zeng, Xia; Xiao, Ying; Yang, Hongqin; Li, Hui

doi:10.1016/j.xphs.2017.02.020

Cited by 6 publications

(2 citation statements)

References 40 publications

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“…The apparent solubility of amorphous indomethacin is higher than the γ-crystal API over the temperature range from 5 to 45 • C [18]. Amorphous pranlukast enhanced apparent solubility approximately 5.8 times in water and 19.4 times in phosphate buffered saline, compared with the crystal substance [19]. However, the inherent instability of amorphous solids remains the major concern in terms of its wider adoption in modern medicine.…”

Section: Introductionmentioning

confidence: 99%

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

et al. 2021

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Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs. The enhancement of ASD in the oral absorption of drugs has been mainly attributed to the high apparent drug solubility during the dissolution. In the last decade, with the implementations of new knowledge and advanced analytical techniques, a drug-rich transient metastable phase was frequently highlighted within the supersaturation stage of the ASD dissolution. The extended drug absorption and bioavailability enhancement may be attributed to the metastability of such drug-rich phases. In this paper, we have reviewed (i) the possible theory behind the formation and stabilization of such metastable drug-rich phases, with a focus on non-classical nucleation; (ii) the additional benefits of the ASD-induced drug-rich phases for bioavailability enhancements. It is envisaged that a greater understanding of the non-classical nucleation theory and its application on the ASD design might accelerate the drug product development process in the future.

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Section: Introductionmentioning

confidence: 99%

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

et al. 2021

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“…Pengaruh penggilingan dan kompresi pada stabilitas metoklopramid hidroklorida dan beberapa bentuk kristal laktosa telah diteliti oleh Qiu dkk, 2005. Proses penggilingan dapat meningkatkan luas permukaan, menghasilkan bahan yang amorf dan menyebabkan kerusakan kristal (13,14) . yang digiling, campuran yang telah dikompresi menjadi tablet dengan tekanan tertentu dan tablet setelah dihancurkan kembali.…”

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Pengaruh Disintegran dan Cara Pencampuran Terhadap Sifat Fisika Kimia Telmisartan

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et al. 2021

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Telmisartan (TMS) mempunyai struktur yang padat dan saling mengunci antar unit kristal.Hal ini mengakibatkan zat mempunyai gaya elektrostatik tinggi sehingga ketika dikompresi menjaditablet, TMS mengalami sintering. Salah satu upaya untuk mengatasi sintering pada tablet TMSadalah dengan menambahkan disintegran. Disintegran yang digunakan adalah berasal dari golonganpati: Starch 1500® (S1500) dan sodium starch glikolat (SSG) serta golongan selulosa mikrokristalinselulosa (MCC) dan croscarmellose sodium (CCS). Tujuan penelitian ini adalah melihat pengaruhbeberapa disintegran terhadap sifat fi sikokimia TMS dengan berbagai perlakuan. TMS divariasikandengan masing-masing disintegran dengan perbandingan 1:9% b/b. Perlakuan terhadap campuranbiner TMS dengan berbagai disintegran meliputi campuran fi sik, campuran digiling, campuran yangdikompresi dan campuran dikompresi yang dihancurkan. Karakterisasi dan evaluasi meliputi pengujianPXRD, SEM dan uji disolusi. Karakterisasi PXRD dan SEM pada berbagai perlakuan menunjukkanadanya pengaruh sifat fi sikokimia terhadap campuran biner TMS dengan berbagai macam disintegran.Kombinasi TMS:CCS dengan perbandingan (1:9) menghasilkan laju disolusi tertinggi pada semuaperlakuan Perlakuan campuran yang digiling memberikan disolusi tertinggi dengan DP60 menit yaitusekitar 55,86±2,47%. Penambahan disintegran pada TMS dengan berbagai perlakuan dapat mengurangisintering tetapi masih belum cukup untuk memenuhi persyaratan disolusi TMS yaitu dalam waktu 30menit terdisolusi dalam media dapar fosfat pH 7,5 dengan Q>75%.

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Amorphous Drug Solubility and Absorption Enhancement

et al. 2018

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Effects of Temperature and Solvent on the Solid-State Transformations of Pranlukast During Mechanical Milling

Cited by 6 publications

References 40 publications

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

Pengaruh Disintegran dan Cara Pencampuran Terhadap Sifat Fisika Kimia Telmisartan

Amorphous Drug Solubility and Absorption Enhancement

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