Calcitonin (a peptide consisting of 32 amino acids) is one of the first choice drugs for the treatment of osteoporosis. The advantages of calcitonin are its inhibition of osteoclast activity, reduction of the number of osteoclasts, inhibition of bone resorption, and reduction of bone conversion, as well as the central analgesic effect of calcitonin, which can relieve bone pain. By adding large acidic substances such as dextran carboxylic acid (DEX-COOH) and slow-release polymers such as polyhydroxyacetic acid (PLGA), the local acidic environment caused by the degradation of the above-mentioned reagents can be used to achieve a sharp release of calcitonin within a certain time frame, solving the problem that calcitonin is difficult to be released within the slow-release polymer material. The rapid release period of calcitonin microspheres can be adjusted by the slow release polymer used. The development of calcitonin long-acting sustained release combination microspheres overcomes the disadvantages of protein peptide drugs that are easily adsorbed in the sustained release material and cannot be released; it achieves sustained release with small abrupt release and complete release.
CD Formulation provides professional preparation services for calcitonin long-acting sustained release microspheres. In addition to providing customers with multiple types of formulation services, we can also provide testing services for the microspheres themselves, including morphology characterization, encapsulation rate testing, and in vitro release testing. We can provide you with high quality microsphere products and help you in your drug development.
Calcitonin and acidic dextran are prepared together into a solution or pellets of calcitonin and acidic dextran, and then dispersed in an organic solution containing a slow-release or controlled-release polymer to form a suspension; among them, acidic dextran can be carboxylic acid dextran or sulfate dextran, etc., and calcitonin and acidic dextran solution can be an acetic acid solution or hydrochloric acid solution; in the organic solution of slow-release or controlled-release polymer, the solvent can be selected from dichloromethane, ethyl acetate or any mixture of dichloromethane and ethyl acetate; said calcitonin and acidic dextran to prepare particles can be calcitonin and acidic dextran and polyethylene glycol (PEG) together to form a solution, then put into lyophilization, remove the PEG to get particles.
Adding the suspension to the aqueous phase containing surfactant and forming colostrum microspheres by stirring or vortexing; the ratio of the volume of the suspension and the aqueous phase containing surfactant can be chosen according to common sense in the industry.
The colloidal microspheres are transferred to the salt-containing aqueous phase and cured to obtain microspheres.
The choice of sustained release or controlled release polymers includes:
Polylactic acid (PLA), polylactic acid-polyhydroxyacetic acid (PLGA), polyethylene glycol-polylactic acid (PEG-PLA), polyethylene glycol-polyhydroxyacetic acid (PEG-PLGA), polyhydroxyacetic acid-polyethylene glycol-polyhydroxyacetic acid (PLGA-PEG-PLGA), polylactic acid-polyethylene glycol-polylactic acid (PLA-PEG-PLA), polyethylene glycol-polycaprolactone (PEG-PEG (PEG-PCL), polycaprolactone-polyethylene glycol-polycaprolactone (PCL-PEG-PCL), etc.
The particle size and surface morphology of calcitonin microspheres were observed by scanning electron microscopy.
Using dichloromethane vortex to dissolve the macromolecules, the concentration of the drug is calculated by HPLC, and thus the drug loading capacity of the microspheres is calculated.
Calcitonin microspheres were placed in a release vial, buffer was added, and later placed on a shaker. The release profile of the drug was generated by HPLC.
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