Abstract
Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.
Highlights
The low aqueous solubility of drugs is a major challenge to the design of oral dosage forms [1].It may lead to poor drug bioavailability because of the slow dissolution process before drug molecules can be absorbed into the systemic circulation
A bulk powder of Lor-oxalic acid (Oxa) hydrate was prepared in a similar way, except 4.59 g of Lor (12 mmol) and 0.54 g of Oxa (6 mmol) was dissolved in 15 mL acetone with slight heating to obtain a clear solution before the sample was placed in the cold room
Powder X-ray Diffractometry (PXRD) peaks different from the starting Lor and Oxa were obtained when screening efforts (Table S1)
Summary
The low aqueous solubility of drugs is a major challenge to the design of oral dosage forms [1]. Given the wide use of Lor, a new crystal form of Lor with improved solubility and dissolution rate, which may reduce variability in bioavailability, as well as enhanced powder properties for more efficient pharmaceutical processing, is desired for developing new Lor tablets. Past efforts to improve the solubility of Lorproperty, include the use of stability and mechanical property, [22,23], of both new forms were characterized Their suitability[25], for complexes [20,21], solid dispersion solidcrystal lipid microparticles [24], solid lipid nanoparticles developing a tablet product with a faster and more robust drug-release performance and self microemulsifying particles [26], and coamorphous systems [27].
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