• Journal of Pharmaceutical Investigation
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• 제41권1호
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• pp.45-50
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• 2011

Nonclassical pathway of crystallization has been utilized to modify the properties and morphologies of inorganic and organic/inorganic materials. In here, the polymer-directed crystallization method has been applied to the pharmaceutical active ingredient to assess the applicability for as a particle engineering tool. The polymer-directed crystallization was successful to modifying the crystal size, habit and morphology, but it was not effective to discover the novel polymorphs of Sibutramine (SB). SB was selected as a model drug and polyacrylic acid (PAA), polyethylene imine (PEI) and chitosan (CHI) were added as a crystallization pathway modifier. SB was crystallized via drowning crystallization using methanol or ethanol as a solvent and water as a non-solvent. The significant interactions between polymer and the drug were confirmed by measuring the solubility of the drug in presence of polymer during the crystallization. The crystal forms of SB are characterized by X-ray diffraction (XRD), scanning electron microscope (SEM) and optical microscope (OM). The polymer-directed crystallization seems to be able to modify the crystal properties of pharmaceutical active ingredient, which is critical in determining the bioavailability, processability, and stability.

• 폴리머
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• 제33권2호
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• pp.124-130
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• 2009

고분자를 저분자 유기물질의 결정화 과정에 사용하면 결정형성과정을 중간 단계, 즉 메조크리스탈 단계에서 멈출 수 있다. 메조크리스탈은 수백 나노미터-수 마이크로미터의 결정들이 스스로 배열되어 결정성을 갖는, 결정과 고분자의 복합초구조로 정의할 수 있다. 본 연구에서는 구아노신일인산의 메조크리스탈 형성에서 고분자의 영향과 그와 관련된 변수들에 대해 알아 보았다. OM과 SEM 분석을 통해 고분자유도 결정화에 의한 GMP 결정은 전형적인 GMP입자와는 다른 모폴로지를 보임을 확인하였고, XRD 분석을 통해 새로운 polymorph를 가짐을 확인하였다. 이러한 결과는 고분자에 의해 GMP의 결정구조가 달라졌음을 의미하며, 결정 안에 함유되는 물의 함량이 달라져 다른 수화물 구조를 보임을 TGA 분석을 통해 확인하였다.