6 results about "Linaclotide" patented technology

The invention provides a preparation method of linaclotide, which comprises the following steps: cyclizing linear peptide of linaclotide to obtain linaclotide, wherein the cyclization refers to air oxidation in a phosphate and guanidine hydrochloride solution with the pH value of 7.5-8.5.

This invention discloses a method for preparing linaclotide capsules, belonging to the pharmaceutical field. The method involves preparation, coating, drying, and filling to obtain linaclotide capsules. By controlling the acidity of the solution and the proportions of the various components in the formula during the preparation process, the quality content and total impurities of the drug can be controlled. The resulting linaclotide capsules have stable content, low impurities, and good quality.

The invention discloses a method for preparing linaclotide through random oxidation, which comprises the following steps: preparing a linear crude peptide into an aqueous solution, in the presence of copper acetate, regulating the pH value with stronger ammonia water, and standing and oxidizing under temperature control; the method is simple and efficient, three pairs of disulfide bonds can be constructed in one step under high concentration, the obtained crude peptide is high in purity and easy to purify, and the production efficiency of preparing linaclotide through oxidation is greatly improved.

The present application belongs to the technical field of biological macromolecule pharmaceutical chemistry and tumor targeting delivery system, and particularly relates to a polypeptide conjugate based on linaclotide and a preparation method and application thereof. The present application finds through experiments that linaclotide or its derivative has potential in colorectal cancer (CRC) targeting and deep penetration after proper modification, and therefore proposes a new use of the clinical drug linaclotide or its derivative in a tumor targeting drug delivery system, and constructs a polypeptide conjugate based on linaclotide or its derivative and a tumor targeting drug delivery system based thereon. In-vivo and in-vitro experiments prove that the polypeptide conjugate and the tumor targeting drug delivery system of the present application have precise targeting and deep penetration capabilities in colorectal cancer and metastatic tumors, can effectively enhance the accumulation of an antitumor drug at a tumor site, thereby enhancing the efficacy of the antitumor drug, and have a wide application prospect in the drug delivery system of colorectal cancer.

The invention provides a linaclotide capsule preparation and a preparation method thereof. The linaclotide capsule preparation comprises a plurality of linaclotide particles and a capsule shell, the capsule shell is filled with the linaclotide particles, and each linaclotide particle sequentially comprises a medicine carrying bead, a linaclotide coating layer and a protective coating layer from inside to outside. The linaclotide coating layer at least comprises linaclotide, calcium chloride dihydrate, leucine and steric hindrance primary amine. The linaclotide capsule preparation disclosed by the invention is relatively good in drug effect stability.

The application discloses a method for synthesizing a linear linaclotide intermediate and linaclotide in a full liquid phase, and relates to the following process: at least two polypeptide fragments are designed and planned by segmenting a linear linaclotide; amino acid raw materials are selected according to the amino acid sequence order of the planned polypeptide fragments; the target polypeptide fragments are synthesized by using an activating agent one by one; the polypeptide fragments are sequentially connected by step-by-step liquid phase condensation to obtain a fully-protected straight-chain linaclotide; and finally, the side chain and the main chain of the fully-protected straight-chain linaclotide are removed to obtain the linear linaclotide, which is the linaclotide intermediate; and the linaclotide is prepared by further adopting an electrochemical one-step oxidation method. The application provides a method for synthesizing a linear linaclotide intermediate and linaclotide in a full liquid phase, can reduce production cost, improve the quality of linaclotide, is more suitable for industrialized production processes, meets environmental protection and safety requirements, and has better economic benefits and application prospects.