ENHANCING THE SOLUBILITY OF BCS CLASS II DRUG RALOXIFENE THROUGH SOLID DISPERSION TECHNIQUES
Sulochana Dutta* and Amitder Nath Chatterjee
ABSTRACT
Improving the solubility and rate of dissolution of Raloxifene Hydrochloride (RLX), a selective estrogen receptor modulator used to prevent and cure postmenopausal osteoporosis, was the aim of the current study. The poor water solubility of RLX, a medication that falls under BCS Class II medicines, restricts its oral bioavailability. In order to tackle this problem, solid RLX dispersions were made in a 1:1 ratio utilizing a variety of hydrophilic carriers, including β-cyclodextrin, Poloxamer 407, PVA, and others, using the solvent evaporation approach.
FTIR spectroscopy and other preformulation studies verified that RLX and the chosen carriers were compatible. Excellent flow characteristics were demonstrated by the generated solid dispersions, which were then directly crushed into tablets.
Weight variation, hardness, friability, disintegration time, and drug content were all evaluated physicochemically and found to be within acceptable pharmacopeial parameters. When compared to the pure medication, dissolution experiments showed a noticeably improved release profile for RLX from solid dispersions and tablet forms. PVA, β-cyclodextrin, and Poloxamer 407 were the carriers that showed the best dissolution enhancement.
The results show that solid dispersion is a viable method for enhancing the bioavailability and solubility of medications that are not very soluble in water, such as RLX. The development of effective, immediate-release oral dosage forms that satisfy quality criteria and have the potential to be scaled for commercial manufacturing is made possible by this formulation technique.
Keywords: FTIR, Raloxifene, Osteoporosis, Solid Dispersions, Solubility.
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