Succinylsulfathiazole Crystal Forms II: Effect of Additives on Kinetics of Interconversion

Ebian, A. R.; Moustafa, M. M.; Khalil, Said A.; Motawi, M M

doi:10.1002/jps.2600640911

Cited by 19 publications

(2 citation statements)

References 9 publications

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“…PVP was selected as an effective inhibitor of crystal transformation and growth and as a solubilizer (Motawi et al, 1982, Crowley & Zography, 2003, Miyazaki et al, 2004. MC is a protective colloid that has been also successfully used to inhibit crystal transformation and growth in pharmaceutical suspensions (Ebian et al, 1975;Raghavan et al, 2001).…”

Section: Dissolution Solubility Studiesmentioning

confidence: 99%

Towards a Universal Dissolution Medium for Carbamazepine

El-Massik

Abdallah

Galal

et al. 2006

Drug Development and Industrial Pharmacy

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The aim of this study was to develop a dissolution medium for assessment of various carbamazepine (CBZ) formulations with different strengths. The design of a system inhibiting transformation of the anhydrous CBZ (CBZ A) to the dihydrate form (CBZ D), with minimum surface-active properties and suitable sink was investigated. The effect of pH, different concentrations of sodium lauryl sulphate (SLS), polyvinylpyrrolidone (PVP), and methyl cellulose (MC) on dissolution rate, solubility, dissolution solubility, and polymorphic transformation of CBZ was assessed. Solution-mediated transformation of CBZ A into CBZ D was monitored using optical microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry. Results showed that different strengths (100, 200, 400 mg) of the same CBZ tablet formulation exhibited different dissolution patterns, in 1% SLS (USP system). Such differences were reduced in 0.5% SLS solution which provided sufficient sink for up to 200 mg CBZ. It was also shown that solubility of CBZ A could not be detected in the media under study (water, SGF, SIF, and SLS solutions) due to its rapid transformation into CBZ D. The use of 3% PVP solution protected CBZ A from conversion for 75 min, while 0.01% MC completely inhibited the transformation up to 24 h. Therefore, a medium consisting of 0.5% SLS and 0.01% MC was selected. The medium provided: a) protection against transformation of CBZ A to CBZ D, b) increased solubility of CBZ A (204 mg % compared to 128 mg % of CBZ D in 0.5% SLS), c) suitable sink for up to 400 mg CBZ and d) overlapping dissolution profiles of various strengths of the same CBZ formulation. The suggested system may be a step in the way of solving CBZ dissolution problems that forced the USP to specify two similar dissolution tests with two different limits for conventional 200 mg CBZ tablets.

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Section: Dissolution Solubility Studiesmentioning

confidence: 99%

Towards a Universal Dissolution Medium for Carbamazepine

El-Massik

Abdallah

Galal

et al. 2006

Drug Development and Industrial Pharmacy

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show abstract

“…Effect of Additives-The effect of additives on the kinetics of interconversion of succinylsulfathiazole crystal forms was investigated (169). These investigations showed that a physically stable aqueous pharmaceutical suspension may be achieved by including a suitable transformation retardant.…”

Section: Dosage Formsmentioning

confidence: 99%