Simvastatin-nicotinamide co-crystal: design, preparation and preliminary characterization

Sopyan, Iyan; Fudholi, Achmad; Muchtaridi, Muchtaridi; Sari, Ika Puspita

doi:10.4314/tjpr.v16i2.6

Cited by 19 publications

(23 citation statements)

References 24 publications

(25 reference statements)

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“…Iyan et al developed Simvastatinnicotinamide co-crystals by solvent evaporation to improve the solubility of simvastatin by co-crystallization using nicotinamide as co-crystal agent or co-former and evaluated for solubility. Observation was saturated solubility of co-crystal show a threefold increase compared to raw simvastatin 23 . Chadha et al also improved solubility of efavirenz by cocrystal technique.…”

Section: Solubilitymentioning

confidence: 89%

Co-Crystals: A Review

Chaudhari¹,

Nikam

Khatri³

et al. 2018

J. Drug Delivery Ther.

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In development of new product major constraints are poor aqueous solubility and low oral bioavailability. Crystallization is one the approach has been used for enhancement of solubility of poorly aqueous soluble drugs also helps to improve physicochemical properties such as melting point, tabletability, solubility, stability, bioavailability and permeability with preserving the pharmacological properties of the active pharmaceutical ingredient. Different methods have been used for the synthesis of cocrystal such as grinding, slurry, antisolvent, hot melt extrusion, sonocrystallization, supercritical fluid, spray drying etc. The article highlights the co-crystallization, its methods and significance.

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Section: Solubilitymentioning

confidence: 89%

Co-Crystals: A Review

Chaudhari¹,

Nikam

Khatri³

et al. 2018

J. Drug Delivery Ther.

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“…The highest solubility enhancement was on simvastatin and saccharin cocrystal, i.e. 10-fold than its pure simvastatin (Sopyan et al, 2017a) . Besides the formation of hydrogen bond, it was assumed that cocrystal exhibited the higher intensity of solvent af inity and lower lattice energy of cocrystal (Sopyan, 2016 The solubility of acyclovir-fumaric acid and acyclovir-malonic acid cocrystal increased and were better than acyclovir-tartaric acid.…”

Section: Solubility and Dissolutionmentioning

confidence: 93%

Better in solubility enhancement : salt or cocrystal?

Alfauziah

Sopyan

2019

ijrps

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Nowadays, most of marketed APIs are in the salt form. But not every single API was ionizable. Thus cocrystallization technique arised to overcome the problem. The aim of this review is to compare the solubility profile of salt and cocrystal. Both salt or cocrystal were used to improve the solubility of APIs and claimed for each other, which is the most effective in solubility enhancement. The salt was formed by ionic interaction, whilst cocrystal formed by hydrogen. Both interactions changed the interaction energy and crystal packing, thus changing the physicochemical properties of APIs. Besides, other factors affecting the solubility of the binary system were melting point, particle morphology, and solubility of coformer. The solubility comparison led to understand the underlying mechanism on solubility enhancement of salt and cocrystal itself.

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“…The shifting of diffractogram has exhibited the interaction of material in solid state or changes of internal space group of molecular structure [20][21]. The result of diffractogram showed shifting for several peaks at 2Ɵ angle, it showed the changes in space group of structural [14]. 5) indicated a shifting on spectrum of CTM purely as compared to the CTM in the mixture, its tends to increase the intensity of the sharp, whereas in the un-diluted PCT tend intensity obtained PCT tends not to undergo much change in the intensity of its incorporation in spectrum [22].…”

Section: Fig 1: Pct (A) Ctm (C) and Their Physical Mixture (B)mentioning

confidence: 98%

“…Each pure substance PCT 100 mg and 100 mg and CTM substance a mixture of PCT and CTM weighed in mole comparison; 132:0.5, 200:0.8, 330:1, 400:1.3, and 500:1.5 was dispersed in potassium bromide (KBr), it's made by mixing a sample with a mass of KBr, the infrared spectrum of results obtained with infrared spectrophotometry on a range of wavenumbers 400-4000 cm -1 [14] using fourier transform infrared.…”

Section: Fourier Transform Infrared (Ft-ir) Analysis (Pct Ctm and Mmentioning

confidence: 99%

Solid State Characterization of a Novel Physical Interaction (Paracetamol-Chlorpheniramine Maleate)

2018

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Objective: Interactions of active pharmaceutical ingredients (API) as well as pharmaceutical excipients don't occur in a pharmaceutical dosage form. Base on structures of paracetamol (PCT) and chlorphenamine maleate (CTM), its combination is possible to give a physical interaction in the solid state. This study was conducted to investigate the physical interaction of PCT and CTM in the solid state.Methods: Characterization used the polarization microscope, solubility test, powder x-ray diffraction (PXRD) to observe peak shifting in 2Ɵ angle, and fourier transform infrared spectroscopy (FT-IR) to examine wavenumber shifting. Results:Results of solubility exhibited an increased solubility percentage with increasing concentration. Polarization microscope analysis presented a combination of crystal morphology after the two substances were mixed in an equimolar ratio. The result of melting point determination of each pure substance was 172 °C for PCT, 132 °C for CTM, and 170 °C for the mixture of the two substances in various ratios. Diffractogram showed the shifting at angle 2Ɵ: 20.715, 19.355-23.500 and 21.840, 26.455-20.330 for concentration ratio of PCT: CTM in (132:0.5) and (330:1) respectively and any change in the functional group was observed from infrared spectrum. Conclusion:All evaluation of PCT and CTM in the solid state has exhibited the interaction in solid condition.

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Simvastatin-nicotinamide co-crystal: design, preparation and preliminary characterization

Abstract: Purpose: To improve the solubility of simvastatin (SV) by co-crystallization using nicotinamide (Nic) as co-crystal agent (co-former

Cited by 19 publications

References 24 publications

Co-Crystals: A Review

Co-Crystals: A Review

Better in solubility enhancement : salt or cocrystal?

Solid State Characterization of a Novel Physical Interaction (Paracetamol-Chlorpheniramine Maleate)

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