Exenatide enteric capsule and preparation method thereof
An enteric-coated capsule, exenatide technology, applied in the directions of capsule delivery, pharmaceutical formulations, peptide/protein components, etc., can solve the problem of low oral bioavailability of polypeptide drugs, large molecular weight of polypeptide drugs, chemical and conformational instability To achieve the effect of promoting passive intestinal transmembrane transport, improving oral bioavailability and maintaining structural integrity
Inactive Publication Date: 2021-04-02
JIANGSU OCEAN UNIV
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Problems solved by technology
[0004] Exenatide is currently administered clinically by injection. However, due to its short half-life, it needs to be injected once a day before breakfast and dinner. Long-term, twice-a-day administration results in poor patient compliance.
Oral administration is currently the most widely used and more convenient route of administration, but polypeptide drugs have large molecular weight and poor fat solubility, making it difficult to pass through the biofilm barrier of the gastrointestinal tract; there are a large number of peptidases in the gastrointestinal tract, which can degrade polypeptides; Degradable; easily eliminated by the liver after absorption; also chemical and conformational instability issues
Due to the above reasons, the oral bioavailability of peptide drugs is low, and most peptide drugs are seldom or unable to be absorbed through the gastrointestinal tract, which limits their clinical application.
Method used
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Embodiment 1
[0024] Example 1, a preparation experiment of exenatide enteric-coated granules:
[0025] One, the present embodiment is the example of the exenatide enteric-coated capsule of the component of 5 different particle parts:
[0026] 1. Exenatide 5.0%, SNAC 32.5%, microcrystalline cellulose 15.0%, anhydrous lactose 30.0%, sodium carboxymethyl starch 15.0%, sodium stearyl fumarate 1.5%, magnesium stearate 1.0%.
[0027] 2. Exenatide 5.0%, 5-CNAC 32.5%, microcrystalline cellulose 15.0%, anhydrous lactose 30.0%, sodium carboxymethyl starch 15.0%, sodium stearyl fumarate 1.5%, magnesium stearate 1.0%.
[0028] 3. Exenatide 5.0%, 4-CNAB 32.5%, microcrystalline cellulose 15.0%, anhydrous lactose 30.0%, sodium carboxymethyl starch 15.0%, sodium stearyl fumarate 1.5%, magnesium stearate 1.0% %.
[0029] 4. Exenatide 5.0%, SNAC 41.5%, microcrystalline cellulose 12.0%, anhydrous lactose 24.0%, sodium carboxymethyl starch 15.0%, sodium stearyl fumarate 1.5%, magnesium stearate 1.0%.
[0...
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The invention discloses an exenatide enteric capsule and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The exenatide enteric capsule is composed of particles and an enteric capsule shell, wherein the particles comprise the following components in percentage by mass of 1.0%-5.0% of exenatide, 20.0%-60.0% of an absorption enhancer, 20.0%-45.0% of afilling agent, 5.0%-20.0% of a disintegrating agent and 0.25%-4.0% of a lubricating agent. The oral absorption enhancer comprises one or more of N-[8-(2-hydroxy benzoyl) amino] sodium caprylate, N-(5-chloro salicyloyl)-8-amino caprylic acid and 4-[(4-chloro-2-hydroxy benzoyl) amino] sodium butyrate, has a hydrophobic part, and generates a weak non-covalent drug-carrier compound with exenatide, andthe transport of exenatide across gastrointestinal tract biofilms can be promoted. According to the method, exenatide exists in an oral preparation, and a new dosage form selection is provided for clinical treatment of diabetes by exenatide.
Description
technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an exenatide enteric-coated capsule and a preparation method thereof. Background technique [0002] According to the latest data released by the International Diabetes Federation (IDF) in 2019, there are approximately 463 million diabetics worldwide, 90% of whom are type 2 diabetics. Glucagon-like peptide-1 (GLP-1) receptor agonist is a new type of polypeptide drug that has entered the field of type 2 diabetes treatment in recent years. As a new generation of hypoglycemic drugs, its hypoglycemic effect Second only to insulin, it has multiple clinical advantages such as strong hypoglycemic effect, low risk of hypoglycemia, obvious weight loss effect and cardiovascular benefits. At present, many guidelines and consensuses on the prevention and treatment of type 2 diabetes at home and abroad continue to emphasize and improve its role in clinical treatment. impor...
Claims
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IPC IPC(8): A61K9/48A61K38/22A61K47/38A61K47/36A61K47/32A61K47/18A61P3/10
CPCA61K38/22A61K9/1617A61K9/1652A61K9/1635A61P3/10
Inventor沈金阳朱月霞孔丽周冰雪吉敬李姣姣张迪曹志凌秦昆明董自波
OwnerJIANGSU OCEAN UNIV