Terlipressin acetate nasal cavity spray and preparation method thereof

A technology of terlipressin and nasal spray, which is applied in aerosol delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., and can solve problems such as inconvenient use, patient pain and high economic burden

Active Publication Date: 2012-05-09
深圳市健翔生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current clinical dosage form of the drug is mainly injections. The use of injections requires a specific environment and

Method used

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  • Terlipressin acetate nasal cavity spray and preparation method thereof
  • Terlipressin acetate nasal cavity spray and preparation method thereof
  • Terlipressin acetate nasal cavity spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 The formulation of terlipressin acetate nasal spray is: 1.0 mg / ml terlipressin acetate, 0.1% w / v disodium edetate, 0.80% w / v sodium chloride, 0.30% w / v chlorobutanol, acetic acid to adjust pH to 5.5.

[0016] Its preparation process is as follows: Accurately weigh 100mg disodium edetate, 800mg sodium chloride, and 300mg chlorobutanol in a 1000ml beaker, add purified water to fully dissolve, then add 1000mg terlipressin acetate, and It is fully dissolved, and an appropriate amount of acetic acid is added to adjust the pH value to 5.5, and the purified water is constant to volume. Filter through a 0.22 μm microporous membrane, fill it into a sterilized spray bottle after passing the inspection, and add a bottle cap with a spray metering pump; label and pack to obtain terlipressin acetate nasal spray.

[0017] Ten sprays of nasal spray containing 1.0 mg / ml terlipressin acetate and ten injections of terlipressin for injection were prepared according to this examp...

Embodiment 2

[0025] Example 2 The formulation of terlipressin acetate nasal spray is: 1.0 mg / ml terlipressin acetate, 0.5% w / v sodium deoxycholate, 1.0% w / v glucose, 0.40% w / v Chlorobutanol, acetic acid regulation pH is 5.5, and its preparation process is as follows:

[0026] The preparation process is as follows: Accurately weigh 500mg sodium deoxycholate, 1000mg glucose, and 400mg chlorobutanol in a 1000ml beaker, add purified water to fully dissolve it, then add 1000mg terlipressin acetate to fully dissolve it, A proper amount of acetic acid was added to adjust the pH to 5.5, and the purified water was made to volume. Filter through a 0.22 μm microporous membrane, fill it into a sterilized spray bottle after passing the inspection, and add a bottle cap with a spray metering pump; label and pack to obtain terlipressin acetate nasal spray.

[0027] Ten sprays of nasal spray containing 1.0 mg / ml terlipressin acetate and ten injections of terlipressin for injection were prepared according ...

Embodiment 3

[0035] Example 3 The formulation of terlipressin acetate nasal spray is: 1.5 mg / ml terlipressin acetate, 0.5% w / v disodium edetate, 0.5% w / v chitosan, 1.0% W / v sodium chloride, 0.30% w / v chlorobutanol, acetic acid to adjust pH to 6.5, its preparation process is as follows:

[0036] The preparation process is as follows: Accurately weigh 500mg disodium EDTA, 500mg chitosan, 1000mg sodium chloride, and 300mg chlorobutanol in a 1000ml beaker, add purified water to fully dissolve, then add 1500mg tertiary acetate For vasopressin, fully dissolve it, add an appropriate amount of acetic acid to adjust the pH to 6.5, and dilute to volume with purified water. Filter through a 0.22 μm microporous membrane, fill it into a sterilized spray bottle after passing the inspection, and add a bottle cap with a spray metering pump; label and pack to obtain terlipressin acetate nasal spray.

[0037] 10 sprays of 1.5 mg / ml terlipressin acetate nasal spray and 10 injections of terlipressin for inje...

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Abstract

The invention relates to a terlipressin acetate nasal cavity spray and a preparation method thereof. The spray is composed by terlipressin acetate, absorption enhancer, osmotic pressure regulator, preservative and pH regulator. The preparation method of the spray mainly comprises raw material preparing, dissolving, bottle washing, filling, packing and the like. The spray has the main functions of contracting smooth muscles of visceral vessels and reducing blood flow volume of the viscera, accordingly, the portal vein blood flow and portal vein pressure are reduced, and meanwhile, the spray can be used for the smooth muscles of the esophagus and the uterus. The spray is convenient to dose, has high bioavailability, and is beneficial to patients to accept.

Description

Technical field: [0001] The invention relates to the field of preparations, in particular to a nasal spray of terlipressin acetate and a preparation method thereof. Background technique: [0002] Terlipressin is a synthetic polypeptide and an analog of the hormone secreted by the posterior pituitary gland. It is a new type of synthetic long-acting vasopressin. It is a prodrug and has no activity itself. After the action of aminopeptidase, the three glycyl residues at the N-terminus are removed, and the active lysine vasopressin is slowly released. The main function of terlipressin is to contract visceral vascular smooth muscle and reduce visceral blood flow, thereby reducing portal vein blood flow and portal vein pressure. It can also act on smooth muscles such as the esophagus and uterus. The clinical dosage form of this drug is mainly injection. The use of injection requires a specific environment and is generally limited to hospitals. It is inconvenient to use, and the p...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K38/11A61P7/12A61K38/095
Inventor 李新宇姚志勇支钦
Owner 深圳市健翔生物制药有限公司
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