Solubility Enhancement of Poorly Water Soluble Drug Tinidazole by Solid Dispersion Technique

Abstract

Tinidazole is nitro imidazole derivative, anti-parasitic drug against protozoan infection. It is used as tissue amoebic ides for both intestinal and extra intestinal amoebiasis. It has broad spectrum cidal activity against protozoa including giardia lamblia many anaerobic bacteria such as fragilis, fusobacterium, clostridium perfrigens, and helicobacter pylori. But as it is BCS class-II Drug, Dissolution from its dosage form is too low and rate limiting step in absorption of drug. The present study was aimed to increase the solubility of the poorly water soluble drug (Tinidazole) by using hydrophilic polymers (PEG 6000 and Mannitol). Solid dispersions were prepared by hot melt method.Phase solubility study, in-vitro dissolution of pure drug, physical mixtures and solid dispersions were carried out. PEG and Mannitol were found to be effective in increasing the dissolution of Tinidazole in solid dispersions when compared to pure drug. FT-IR spectroscopy studies were carried out in order to characterize the drug and solid dispersion.

An Overview on the Recent Technologies and Advances in Drug Delivery of Poorly Water-Soluble Drugs

“…The drug should be dissolved in gastric or intestinal fluids in order to pass through the membrane of GIT and reach the systemic circulation. Therefore, many attempts were performed by the pharmaceutical researchers to enhance drug bioavailability by improving the solubility and the dissolution rate of low water-soluble drug [7] . Biopharmaceutical Classification System (BCS) based on drug solubility, permeability and dissolution of the dosage form.…”

Preparation and Characterization Phisicochemical Properties of Multi Component Ketoprofen With Co-Former Glutamine

“…Several previous studies have been carried out to increase the solubility of ketoprofen, including the formation of multicomponent ketoprofen with nicotinamide using the solvent evaporation technique which shows an increase in solubility 1.3 times higher than pure ketoprofen (Wicaksono et al, 2018) using the Co Grinding technique using the polymer Hydroxypropyl Methylcellulose E6 with a solubility increase of 6.5 times (Hilaliyati et al, 2017), an increase in solubility with a solid dispersion of ketoprofen-macrogol 6000-KLHT is 3.8 times (Jachowicz et al, 2000), an increase in solubility with a solid dispersion of ketoprofen-polyvinylpyrrolidone (PVP) is a ratio of 1:1.5 providing a faster dissolution rate of ketoprofen than the physical mixture (Patil et al, 2010) with the ketoprofen fusion technique with the coformer used p-amino-salicylate, showing a 14-fold increase in solubility in water (Vaghela et al, 2014) where it can be interpreted that multicomponents can improve physicochemical properties, especially the solubility of ketoprofen.…”

Preparasi dan Karakterisasi Sifat Fisikokimia Multikomponen Ketoprofen dengan Koformer Proline

“…Pada beberapa penelitian sebelumnya telah dilakukan peningkatan kelarutan dari ketoprofen, diantaranya pembentukan multikomponen kristal ketoprofen dengan nikotinamida dengan teknik solvent evaporation menunjukkan peningkatan kelarutan 1,3 kali lebih tinggi dari ketoprofen (Wicaksono et al, 2018), dengan teknik Co Grinding menggunakan polimer Hidroksipropil Metilselulosa E6 dengan peningkatan kelarutan sebesar 6,5 kali (Hilaliyati, 2017), peningkatan kelarutan dengan dispersi padat ketoprofen-macrogol 6000-KLHT adalah 3,8 kali (Jachowicz et al, 2000), peningkatan kelarutan dengan dispersi padat ketoprofen-polivinilpirrolidon (PvP) adalah 1,5 memberikan laju disolusi ketoprofen lebih cepat dibandingkan dengan campuran fisiknya (Patil et al, 2010), dengan teknik fusi ketoprofen dengan koformer dipakai p-amino-salisilat, menunjukkan peningkatan kelarutan 14 kali lipat dalam air (Vaghela et al, 2014), dengan dispersi padat ketoprofen-PVP K-30 dapat meningkatkan profil disolusi pada menit ke-30 persen terdisolusinya adalah 82,376% (tidak kurang dari 80%) (Umar et al, 2014), dispersi padat ketoprofen-PVA pada perbandingan 1:1 dengan kadar ketoprofen yang terdisolusi sebesar 26,6% (Sultan et al, 2019) dimana hal tersebut dapat diartikan multikomponen kristal dapat memperbaiki sifat fisikokimia terutama kelarutan dan profil disolusi dari ketoprofen.…”