Better Actali with hydroxypropyl betacyclodextrin
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Better Actali with hydroxypropyl betacyclodextrin

Views: 0     Author: Site Editor     Publish Time: 2022-06-23      Origin: Site

Actarit (Acta) is acetaminophenacetic acid, which is an anti-rheumatic drug developed by Mitsubishi Chemical Industry Corporation of Japan. It has inhibitory effect on delayed allergic reaction and can be improved by reducing serum nitric oxide concentration. The early symptoms of rheumatoid arthritis (RA) are mainly used for the treatment of RA. However, due to the poor water solubility of Acta, its clinical application is limited.

Hydroxypropyl betadex (HPBCD) is a low toxicity, safe and effective drug solubilizer, and has the advantages of high water solubility and improved release rate of the contained drug in vivo. By preparing the inclusion complex of Acta-HP--βCD to increase its solubility in water, and then adding appropriate excipients to fill capsules to achieve a good dissolution effect, providing a theoretical basis for further developing new Acta dosage forms and improving its pharmaceutical properties.

Preparation of Solid Inclusion Compounds Weigh hydroxypropyl beta-cyclodextrin and Acta in a molar ratio of 11 and place them in a beaker, add absolute ethanol to dissolve Acta, and add dropwise to the hydroxypropyl beta-cyclodextrin under stirring conditions. dextrin ethanol solution, stirring was continued for 4h at room temperature. Take it out, take a 60-degree water bath, remove ethanol by rotary evaporation, grind it finely after vacuum drying, and pass it through an 80-mesh sieve to get it.

To determine the content of Acta (Acta) in the inclusion complex, weigh an appropriate amount of Acta, dilute it to an appropriate concentration with anhydrous ethanol solution, take the ethanol solution as a blank, and scan at a wavelength of 200-400 nm. The results show that Acta has the maximum ultraviolet absorption at the wavelength of 245nm, so 245nm is selected as the detection wavelength. During the test, the powder is easy to leak, and it is impossible to ensure that the sample is put into the medium at the same time, so the paddle method is selected. During granulation, it was found that the viscosity of water as a wetting agent was high, which brought certain difficulties to granulation, and 95% ethanol was used as a wetting agent to solve this problem. "Chinese Pharmacopoeia" stipulates that the dissolution rate at 45min should reach 75%. From the results, capsules with different prescriptions are in compliance with the regulations. Individual prescriptions have a slight attenuation phenomenon, which should be related to the continuous replenishment of the medium. The filler has little effect on the dissolution of inclusion compound capsules, which may be because the preparation of inclusion compound itself improves the solubility of Acta and accelerates the dissolution rate of the drug, so that the inclusion compound capsules have good dissolution regardless of the filler used. Effect. If ordinary capsules are prepared, economical starch can be used as an excipient to meet the dissolution requirements; if immediate-release capsules are to be prepared, lactose can be considered as a filler.




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