The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linkermoiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effectorbiomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and / or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Uses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.
Disclosed is a donepezil-containing transdermally absorbable preparation which develops reduced adverse side effects and shows a satisfactory level of therapeutic effect. The preparation comprises an adhesive and a donepezil component (containing crystalline donepezil having type-B crystal polymorphism) and / or a salt thereof, wherein the donepezil component or the salt thereof is contained in an amount of 9 to 50% by mass relative to the total weight of the adhesive. The preparation (particularly, one having a non-aqueous adhesive layer) shows an excellent penetration of donepezil and / or a salt thereof into the skin, retains good stability of the active ingredient therein, and is remarkably reduced in local stimulation and adverse side effects.
The invention discloses self-microemulsifying calcium alginate gel pellets and a preparation method thereof. The preparation method comprises the following steps: uniformly mixing an oil phase, a surfactant and a co-surfactant, adding an indissolvable drug until the indissolvable drug is completely dissolved; uniformly mixing the prepared liquid drug-loading self-microemulsifying preparation and a sodium alginate solution, performing complex crosslinking between the sodium alginate and calcium ions in calciumchloride to prepare the self-microemulsifying calcium alginate gel pellets for loading drugs by an ion gelatinizing method. According to the method, sustained-release and controlled release of a medicine can be controlled by changing the concentration of sodium alginate, the concentration of calcium chloride and other conditions. By virtue of the method, a solid self-microemulsifying preparation can be prepared from the liquid self-microemulsifying preparation, so that various defects of a liquid self-microemulsifying preparation can be effectively avoided. The preparation method is simple in process, low in production cost and easy for industrial production.