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Novel recombinant parathyroid hormone (1-34) correlated peptide nose drops

A technology of parathyroid hormone and nasal drops, applied in the field of nasal drops of recombinant parathyroid hormone-related peptides, which can solve the problems of weakening activity, stimulating AC biological activity loss, and activity reduction, so as to achieve good absorption and avoid pain , Ease of use

Inactive Publication Date: 2008-03-12
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] According to the molecular modeling results of the interaction between PTH(1-34) and PTH / PTHrP receptors, the N-terminal Ser1 is one of the two contact points for PTH(1-34) to bind to the receptor, and it must be in the form of free amino acids. The biotinylation or extension of the N-terminal amino acid will significantly weaken its activity, such as: fMet-hPTH (1-84) is only 10% of hPTH (1-84) in the bioassay of osteosarcoma; Connecting Tyr or Tyr-Gly-Gly to the end can significantly reduce its activity; connecting Met-Gly to the N-terminal of hPTH even leads to the loss of its biological activity of stimulating AC

Method used

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  • Novel recombinant parathyroid hormone (1-34) correlated peptide nose drops

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Experimental program
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Effect test

Embodiment 1

[0031] The preparation of embodiment 1 nasal drops

[0032] Pro-Pro-[Arg 11 ]hPTH(1-34)-Pro-Pro 5mg (low), 12.5mg (medium), 25mg (high)

[0033] 2,6-Dimethyl-β-cyclodextrin 400mg

[0034] Polyacrylic acid 25mg

[0035] Citric acid·2H 2 O 84mg

[0036] EDTA 1mg

[0037] Adjust pH to 6.0 with NaOH

[0038] Add water for injection to 10mL

[0039] Get above-mentioned components and prepare Pro-Pro-[Arg 11 ]hPTH(1-34)-Pro-Pro Nasal Drops.

Embodiment 2

[0040] Embodiment 2 nasal drops treat the osteoporosis of ovariectomy rat

[0041] Divide 48 rats of about 200g into 6 groups according to body weight, which are normal control group (Normal), sham operation group (Sham), normal saline group (NS), and high, medium and low dose groups (HhPTH, MhPTH , LhPTH), all rats except the normal control group were subjected to ovariectomy. After feeding for 2 weeks, the high, medium and low dose groups were instilled with 80 μl of nasal drops of corresponding concentration every day, and the normal saline group was instilled with 80 μl of normal saline. After 12 weeks of continuous administration, the BMD of the femur and vertebrae were measured with a dual-energy X-ray absorptiometry instrument produced by Lunar Corporation of the United States. Vertebral bone density measurement results are shown in Figure 1, and bone bone density measurement results are shown in Figure 2. As can be seen from Fig. 1, compared with normal saline, the h...

Embodiment 3

[0042] The toxicity test of embodiment 3 nasal drops to rat nasal mucosa epithelial cells

[0043] The rats in Example 2 were sacrificed, and the nasal mucosa was taken, fixed with 10% formaldehyde, routinely drawn, embedded in paraffin, made into slices (4 μm thick), stained with HE, and observed with an optical microscope. The results are shown in accompanying drawing 3, as can be seen from the figure that Pro-Pro-[Arg 11 ] hPTH(1-34)-Pro-Pro intranasally administered in each dosage group, the nasal mucosa tissue surface of the rats covered with squamous epithelium is complete, no erosion, ulcer formation, edema and inflammatory cell infiltration in the lamina propria, so it can be concluded Conclusion Pro-Pro-[Arg 11 ] hPTH(1-34)-Pro-Pro nasal drops have no toxicity to rat nasal mucosal epithelial cells.

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Abstract

The present invention discloses a human recombinant parathyroid hormone (1-34) related peptide Pro-Pro-[Arg11]hPTH(1-34)-Pro-Pro nasal drop and a production method. The main ingredient of the nasal drop is Pro-Pro-[Arg11]hPTH(1-34)-Pro-Pro, which is made into an aqueous nasal drop added with an appropriate pH buffer, a thickener, a penetration-promoting agent and a preservative. The nasal formulation avoids the pain and adverse effect (fever, etc.) caused by injection, which is especially suitable for the elder. The nasal drop can effectively cure and prevent osteoporosis with a certain value of clinical practice.

Description

Technical field [0001] The invention belongs to the field of biopharmaceuticals, and in particular relates to nasal drops of recombinant parathyroid hormone (1-34) related peptides for treating and preventing osteoporosis and a preparation method thereof. technical background [0002] Osteoporosis is a multidisciplinary public health problem. It refers to a reduction in the amount of bone tissue within each unit. Divided into secondary osteoporosis and primary osteoporosis, the former most commonly include steroid-induced osteoporosis and diabetic osteoporosis, and the latter mainly includes postmenopausal osteoporosis and senile osteoporosis. [0003] Nowadays, osteoporosis has become a common disease that seriously threatens the physical and mental health of the elderly. According to the statistics of the Osteoporosis Society of the Chinese Gerontology Society, the number of osteoporosis patients in my country has reached 80 million, which has constituted a serious public...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/29A61K9/72A61P19/10
Inventor 刘景晶施小明庄志华王春晓吴洁曹荣月李泰明金亮
Owner CHINA PHARM UNIV
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