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CN-121987767-A - Stable cod collagen peptide suppository and preparation method thereof

CN121987767ACN 121987767 ACN121987767 ACN 121987767ACN-121987767-A

Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a stable cod collagen peptide suppository and a preparation method thereof. The suppository comprises active ingredient cod collagen peptide, the matrix is a composition of polyethylene glycol and glycerin, and comprises chitosan serving as an adhesive, polyethylene glycol-40 hydrogenated castor oil serving as a solubilizer, a preservative and an antioxidant. The preparation method comprises melting matrix, mixing with adjuvants, cooling, adding active ingredients, mixing, injection molding, solidifying, and demolding. The invention solves the problems of poor formability of polypeptide suppositories, easy instability of active ingredients in storage and the like through the compounding of specific matrixes and the synergistic effect of functional auxiliary materials, the appearance, hardness and melting time limit of the obtained suppositories are in accordance with the regulations, the stability is obviously improved, and the preparation method is suitable for the local treatment of ulcerative colitis.

Inventors

  • SHEN JINYANG
  • ZHANG YUCHEN
  • CHEN XINYUE
  • YANG FAN
  • DONG XUEHONG
  • HU CHANGJING
  • LI YUXUAN
  • XIE QICHENG
  • XU WENTAO
  • Yi Wanyu
  • HUANG SIYAO

Assignees

  • 江苏海洋大学

Dates

Publication Date
20260508
Application Date
20260123

Claims (10)

  1. 1. The stable cod collagen peptide suppository is characterized by comprising the following components in percentage by mass: 5% -20% of cod collagen peptide; 70% -90% of matrix; 2% -3.5% of adhesive; 1% -3% of solubilizer; 0.1% -1% of an antioxidant; 0.1% -1% of preservative; Wherein the matrix is selected from one of two combinations: (a) Polyethylene glycol 400, polyethylene glycol 4000 and glycerin, or (B) Polyethylene glycol 400, polyethylene glycol 6000 and glycerin; The adhesive is chitosan; the solubilizer is polyoxyethylene (40) hydrogenated castor oil; the sum of the mass percentages of the components is 100 percent.
  2. 2. The stable cod collagen peptide suppository of claim 1, wherein when the matrix is composition (a), the mass ratio of polyethylene glycol 400, polyethylene glycol 4000 and glycerin is (3.5-4): 2.5-4): 1.8-3.5.
  3. 3. The stabilized cod collagen peptide suppository according to claim 2, wherein the mass ratio of polyethylene glycol 400, polyethylene glycol 4000 and glycerin is 4:3:3 or 4:4:2.
  4. 4. The stabilized cod collagen peptide suppository according to claim 1, wherein when the matrix is composition (b), the mass ratio of polyethylene glycol 400, polyethylene glycol 6000 and glycerin is 4:3:3.
  5. 5. The stabilized cod collagen peptide suppository according to any one of claims 1 to 4, wherein the antioxidant is ascorbyl palmitate and the preservative is methylparaben.
  6. 6. The stable cod collagen peptide suppository of claim 5, wherein the suppository is prepared from the following components in percentage by mass: 10% of cod collagen peptide; polyethylene glycol 400.84%; Polyethylene glycol 4000.38%; 25.38% of glycerol; Chitosan 2.5%: polyethylene glycol-40 hydrogenated castor oil 2%; Ascorbyl palmitate 0.5%; Methyl p-hydroxybenzoate 0.4%.
  7. 7. A method for preparing the stable cod collagen peptide suppository according to any one of claims 1 to 6, comprising the steps of s1, melting the matrix by mixing prescribed amounts of matrix components, heating to melt at 65-75 ℃ to obtain a molten matrix; S2, adding auxiliary materials, namely adding preservative, antioxidant, adhesive and solubilizer with the prescribed amount into the molten matrix, and uniformly stirring; s3, adding active ingredients, namely cooling the mixture obtained in the step S2 to 45-50 ℃, adding the cod collagen peptide with the prescription amount, stirring until the cod collagen peptide is dissolved and uniformly mixing to obtain suppository liquid medicine; S4, injection molding and curing, namely injecting the suppository liquid medicine into a suppository mold while the suppository liquid medicine is hot, curing for 10-30 minutes at 2-10 ℃, and demolding to obtain the suppository.
  8. 8. The method of claim 7, wherein in step S3, the temperature is reduced to 48 ℃.
  9. 9. The method according to claim 7 or 8, wherein in step S4, the curing temperature is 4 ℃.
  10. 10. Use of a stabilized cod collagen peptide suppository according to any one of claims 1 to 6 in the manufacture of a medicament for the treatment of ulcerative colitis.

Description

Stable cod collagen peptide suppository and preparation method thereof Technical Field The invention relates to the technical field of pharmaceutical preparations, in particular to a stable cod collagen peptide suppository and a preparation method thereof. Background The cod collagen peptide is a small molecular active peptide prepared by taking deep sea cod as a raw material and adopting an enzymolysis process. Research shows that the compound has remarkable anti-inflammatory and antioxidant activities, and particularly has therapeutic potential in the aspects of intestinal inflammatory diseases such as ulcerative colitis and the like. Animal experiments show that the traditional Chinese medicine can effectively relieve colonitis symptoms of model animals, and the mechanism of the traditional Chinese medicine is related to regulation of inflammatory signal paths such as NF- κB and the like. However, the conversion of the above pharmacological activity to clinical efficacy faces key bottlenecks in dosage form and delivery strategy. At present, related researches on cod collagen peptide are focused on raw material preparation and in-vitro and in-vivo activity evaluation, and the clinical application form of the cod collagen peptide is very limited, and the cod collagen peptide is mainly a conventional oral preparation (such as a cod collagen peptide beverage described in CN 112715813A). For local diseases of ulcerative colitis and the like with lesion sites located on colonic mucosa, oral administration has the problems of obvious first pass effect, low concentration of medicine at the lesion sites, easy damage to gastrointestinal tract environment and the like, and is difficult to realize high-efficiency and accurate local treatment, thereby limiting the full play of bioavailability and curative effect. Therefore, development of a novel cod collagen peptide formulation which can directly reach focus, improve local drug concentration and keep active ingredients stable becomes a technical problem to be solved in order to promote clinical transformation. Suppositories are a classical dosage form for rectal administration, which is expected to deliver the drug directly to the colon area, circumventing the drawbacks of oral administration. However, combining water-soluble polypeptide drugs with suppository bases and ensuring that they remain physically stable, chemically stable, and ideally release during preparation, storage, and use, face a number of prescription and process challenges. At present, no systematic research and optimization report aiming at cod collagen peptide suppositories exists. Disclosure of Invention Aiming at the defects of the prior art, the invention provides a stable cod collagen peptide suppository and a preparation method thereof. The suppository can realize rectal local delivery of medicine, and solves the technical problems of difficult shaping and poor storage stability of polypeptide in suppository matrix. In order to achieve the purpose of the invention, the following technical means are specifically adopted: On the one hand, the invention provides a stable cod collagen peptide suppository which is prepared from the following components, by mass, 5% -20% of cod collagen peptide, 70% -90% of matrix, 2% -3.5% of adhesive, 1% -3% of solubilizer, 0.1% -1% of antioxidant and 0.1% -1% of preservative. The matrix is a composition of polyethylene glycol 400, polyethylene glycol 4000 and glycerin, the adhesive is chitosan, the solubilizer is polyethylene glycol-40 hydrogenated castor oil, and the sum of the mass percentages of the components is 100%. On the other hand, the invention provides a preparation method of the stable cod collagen peptide suppository, which comprises the following steps of mixing, heating and melting the matrix components with the prescription amount, adding a preservative, an antioxidant, an adhesive and a solubilizer, stirring uniformly, cooling the mixture to 45-50 ℃, adding the cod collagen peptide with the prescription amount, stirring until the cod collagen peptide is dissolved and mixed uniformly to obtain a suppository liquid medicine, hot injection molding, solidifying for 10-30 minutes at 2-10 ℃, and demoulding to obtain the suppository liquid medicine. In some embodiments, the matrix may also be a composition of polyethylene glycol 400, polyethylene glycol 6000 and glycerin in a mass ratio of 4:3:3. In other embodiments, the mass ratio of polyethylene glycol 400 to polyethylene glycol 4000 to glycerin is (3.5-4): 2.5-4): 1.8-3.5. More preferably, the mass ratio is 4:3:3 or 4:4:2. In a further embodiment, the antioxidant is ascorbyl palmitate and the preservative is methylparaben. In a specific and preferred embodiment, the suppository is prepared from the following components, by mass, 10% of cod collagen peptide, 40033.84% of polyethylene glycol, 400025.38% of polyethylene glycol, 25.38% of glycerol, 2.5% of chitosan, 2% of polyethylene glycol-40 hydro