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Enhancement of the Physicochemical Properties of Poorly Soluble Lovastatin by Co-crystallization Techniques - In vivo Studies

Department of Pharmaceutics, Rao׳s College of Pharmacy, Nellore-524320, 1Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Viswa Vidhyalayam, Tirupati-517502, 2A. U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530 003, India

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Department of Pharmaceutics, Rao׳s College of Pharmacy, Nellore-524320, India, E-mail:

To overcome the poor solubility and low bioavailability of lovastatin co-crystallization was attempted. Lovastatin co-crystals were prepared with selected co-former gallic acid by co-grinding method. Characterization was carried out through X-ray diffraction, Fourier Transform infra-red spectroscopy, differential scanning colorimetry and scanning electron microscopy. The Fourier-transform infrared spectroscopy results showed that a hydrogen bond was formed between lovastatin and gallic acid to yield a co-crystal. Micrometric properties, solubility, dissolution studies, pre-compression and post-compression properties were evaluated. Lovastatin co-crystals were formulated into conventional tablets. In vivo and stability studies were performed. Pharmacokinetic parameters and dynamic studies of the formulation were statistically analysed and a value of p<0.05 was considered to be significant. Thus physicochemical properties and bioavailability of lovastatin was improved through co-crystallization.

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