183 results about "Exenatide" patented technology

The invention discloses a polypeptide medicament sustained release microsphere or a microcapsule preparation with uniform grain size, a preparation method thereof and application. The average grain size of the microsphere or the microcapsule preparation is between 50 nanometers and 100 microns, and the grain size distribution coefficient CV value is less than 20 percent. The polypeptide medicament has a definite structure, has functions of therapy or adjuvant therapy of type-2 diabetes, and is preferably one or more of GLP-1, Exenatide, Exendin-4 and derivatives and analogs thereof. The microsphere or the microcapsule preparation uses a microsphere or a microcapsule with uniform grain size as a substrate to prepare the polypeptide medicament into a sustained release preparation through an embedding mode, and by changing the grain size of the microsphere or the microcapsule, the sustained release cycle is adjustable between one week and one month, and the microsphere or the microcapsule preparation can be applied to the therapy or the adjuvant therapy of the type-2 diabetes and body weight control. Besides, the microsphere or the microcapsule preparation has the advantages of simple preparation process and mild preparation course, and can protect the biological activity of the embedded polypeptide medicament.

The invention discloses a pharmaceutical preparation containing exenatide. Besides the active constituent exenatide, the pharmaceutical preparation further contains 10-100mm of buffer with pH being 3-7 and adjuvants for enhancing stability of the exenatide. The invention has the advantages of preparing an exenatide preparation which is applicable to clinical application, in particular to injection and can be stably kept by adding a plurality of human acceptable constituents.

The invention provides a medicinal preparation containing exenatide suitable for multi-administration, which contains exenatide, buffer solution, pharmaceutically acceptable accessory and preservative, wherein the buffer solution can keep the pH value of the preparation in an aqueous solution state at 3.0 to 7.0; the accessory may be one or combination of glucose, sucrose, methionine, mannitol or glycine; and the preservative is selected from benzoic acid, sodium benzoate, potassium sorbate or acetone chloroform. The medicinal preparation has the advantages that the stability of physicochemical and biological activities of the exenatide is enhanced by adding a few components capable of being accepted by the human body, and then a preparation suitable for clinical use, particularly injection use is prepared.

The invention provides a pegylated exenatide ramification (Exendin-4-Cys-PEG (polyethylene glycol)) and the use of the pegylated exenatide ramification, belonging to the technical field of the preparation and the application of a polypeptide drug. A preparation method of the pegylated exenatide ramification provided by the invention comprises the following steps of: introducing a cysteine at the C-end of exenatide, and coupling maleic acylamino polyethylene glycol, so that the pegylated exenatide ramification can be formed. The pegylated exenatide ramification provided by the invention has slow clearance rate in the blood circulation and prolonged half-life period, and can be used for preparing the related illness treatment drugs for reducing the blood sugar, reducing the ingestion, reducing the gastrointestinal emptying, increasing the beta cell quantity or reducing the gastrointestinal motility.

A method for preparing exenatide by solid-phase synthesis, including: 1) mixing an Fmoc-Rink amide AM resin with a deprotecting agent to obtain a Rink amide AM resin; 2) condensing an Fmoc-Ser(tBu)-OH with the Rink amide AM resin to obtain an Fmoc-Ser(tBu)-Rink amide AM resin; 3) repeating the Fmoc deprotection and the condensation between an amino acid and a polypeptide on the resin, and condensing an amino acid with a polypeptide on the resin from the C-terminal to the N-terminal, to form a polypeptide resin; and 4) separating the polypeptide and the resin on the polypeptide resin.

Slow release forms of exenatide wherein exenatide is releasably linked to polyethylene glycol carriers are disclosed.

Provided are compounds and methods of making compounds containing two or three groups derived from a peptide, such as enfuvirtide or exenatide, covalently bound to a linker. The compounds may contain polyethylene glycol groups to enhance solubility and pharmacokinetic properties. The compounds are useful for the treatment of diseases or conditions subject to treatment with the parent peptide, such as HIV and AIDS in the case of enfuvirtide, or diabetes in the case of exenatide.

Methods for treating metabolic diseases are described for intranasal delivery of an exenatide, comprising an aqueous mixture of exendin, and a delivery enhancer selected from the group consisting of a solubilizer, a chelator, and a surfactant, and the pharmaceutical formulations used therein.

This invention provides compositions comprising a byetta, fish oil, and a protease inhibitor, method for treating diabetes mellitus, comprising administering same, and methods for oral or rectal administration of a byetta.

Provided herein are pharmaceutical formulations containing exendins, exendin agonists, or exendin analog agonists that are administered at therapeutic plasma concentration levels over a sustained period of time to lower total cholesterol levels; to lower LDL-cholesterol levels; to lower triglyceride levels; to treat dyslipidemia; to treat and slow the progression of atherosclerosis; and to treat, prevent, and reduce the risk of heart attacks and strokes in patients. In the pharmaceutical formulations and methods of the invention, the exendin may be exendin-4, an exendin-4 agonist, or an exendin-4 analog agonist. The pharmaceutical formulations may be polymer-based pharmaceutical formulations that may be administered once weekly. An exemplary pharmaceutical formulation comprises 5% (w / w) of exenatide, about 2% (w / w) of sucrose, and about 93% (w / w) of a poly(lactide-co-glycolide) polymer, wherein the poly(lactide-co-glycolide) polymer is in the form of microshperes encapsulating the exenatide.

The invention discloses a pharmaceutical preparation containing exenatide. Besides the active constituent exenatide, the pharmaceutical preparation further contains 10-100mm of buffer with pH being 3-7 and adjuvants for enhancing stability of the exenatide. The invention has the advantages of preparing an exenatide preparation which is applicable to clinical application, in particular to injection and can be stably kept by adding a plurality of human acceptable constituents.

The invention discloses a solid-phase fragment synthetic method of exenatide. The solid-phase fragment synthetic method comprises the following steps: dividing 39 amino acids of the exenatide into 6 sections of full-protection fragments; firstly respectively synthesizing the 6 sections of the full-protection fragments; sequentially carrying out solid-phase fragment assembling and connection on the 6 sections of the full-protection fragments to obtain exenatide resin; then cutting to obtain an exenatide crude product; and purifying the crude product to obtain an exenatide product. According to the solid-phase fragment synthetic method of the exenatide, the problems that the existing solid-phase exenatide synthesizing process is complicated, is low in efficiency and difficult to purify and scale are solved; the synthesizing efficiency is improved and connection steps are simplified greatly; the accumulation of impurities is reduced; the invention provides a novel method for realizing the large-scale synthesis of the exenatide, improving the product purity and reducing the purification difficulty.

The invention provides a medicinal preparation containing exenatide suitable for multi-administration, which contains exenatide, buffer solution, pharmaceutically acceptable accessory and preservative, wherein the buffer solution can keep the pH value of the preparation in an aqueous solution state at 3.0 to 7.0; the accessory may be one or combination of glucose, sucrose, methionine, mannitol or glycine; and the preservative is selected from benzoic acid, sodium benzoate, potassium sorbate or acetone chloroform. The medicinal preparation has the advantages that the stability of physicochemical and biological activities of the exenatide is enhanced by adding a few components capable of being accepted by the human body, and then a preparation suitable for clinical use, particularly injection use is prepared.