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Thermotropic hydrogel sustained-release veterinary drug injection for animal contraception and preparation method thereof

A hydrogel and injection technology, applied in the field of pharmaceutical preparations, can solve problems such as poor compliance, low drug loading, and limited application, and achieve the effects of cost saving, simple synthesis, and prolonged release period

Inactive Publication Date: 2018-05-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the solvent is an organic solvent, there is tissue toxicity, which greatly limits its application in the field of medical devices and veterinary preparations
[0008] Chinese patent (CN 101455644) describes a long-acting contraceptive microsphere for injection, which includes gestodene, estrogen and a biodegradable polymer, which can release the two active ingredients stably and synchronously over a long period of time , which solves the problems of large side effects and poor compliance of existing oral contraceptives
However, because it is an external dressing, the drug loading capacity is low, and it cannot achieve the effect of sustained release for a long time, so it cannot be used as a long-acting contraceptive preparation
[0010] None of the above patents or documents mentioned a long-acting sustained-release system for animal contraception that is minimally invasive, non-biotoxic, simple to prepare, and moderately costly.

Method used

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  • Thermotropic hydrogel sustained-release veterinary drug injection for animal contraception and preparation method thereof
  • Thermotropic hydrogel sustained-release veterinary drug injection for animal contraception and preparation method thereof
  • Thermotropic hydrogel sustained-release veterinary drug injection for animal contraception and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Add 20 g of PEG (1000) into a 250 mL three-necked bottle, set the temperature of the oil bath to 125 °C, vacuum filter at a stirring speed of 70 r / min for 3 h, and change argon 3-4 times during this period. After the flask was cooled down slowly, 43 g and 7 g of D, L-lactide and glycolide respectively in a molar ratio of 5:1 were added. After it was completely dissolved, about 0.25 wt% stannous octoate was added, the temperature of the oil bath was raised to 160 °C, and the reaction was continued for 12 h under an argon atmosphere. After the reaction was completed, the unreacted monomer and low boiling point products in the system were removed by vacuum filtration for 2 h. Finally, the product was transferred to hot water at 80 °C, and the supernatant was poured out after standing for precipitation, repeated washing three times, and vacuum-dried for 48 hours to obtain the BAB type triblock copolymer PLGA-PEG-PLGA with a yield of about 80%. The number-average and weight...

Embodiment 2

[0044] Add 20 g of PEG (1500) into a 250 mL three-necked bottle, set the temperature of the oil bath to 125 °C, vacuum filter at a stirring speed of 70 r / min for 3 h, and change the argon gas 3-4 times during this period. After the flask was cooled down slowly, 42 g and 3.4 g of D, L-lactide and glycolide respectively in a molar ratio of 10:1 were added. After it was completely dissolved, about 0.25 wt% stannous octoate was added, the temperature of the oil bath was raised to 160 °C, and the reaction was continued for 12 h under an argon atmosphere. After the reaction was completed, the unreacted monomer and low boiling point products in the system were removed by vacuum filtration for 2 h. Finally, the product was transferred to hot water at 80 °C, and the supernatant was poured after standing for precipitation, and the washing was repeated 3 times. After vacuum drying for 48 hours, the BAB type triblock copolymer PLGA-PEG-PLGA was obtained with a yield of about 85%. The nu...

Embodiment 3

[0046] Add 20 g of PEG (1500) into a 250 mL three-necked bottle, set the temperature of the oil bath to 125 °C, vacuum filter at a stirring speed of 70 r / min for 3 h, and change the argon gas 3-4 times during this period. After the flask was cooled slowly, 42.6 g and 5.4 g of caprolactone (CL) and glycolide (GA), respectively, were added in a molar ratio of 4:1. After it was completely dissolved, about 0.25 wt% stannous octoate was added, the temperature of the oil bath was raised to 160 °C, and the reaction was continued for 12 h under an argon atmosphere. After the reaction was completed, the unreacted monomer and low boiling point products in the system were removed by vacuum filtration for 2 h. Finally, the product was transferred to hot water at 80 °C, and the supernatant was poured out after standing for precipitation, repeated washing three times, and vacuum-dried for 48 hours to obtain the BAB type triblock copolymer PCGA-PEG-PCGA with a yield of about 76%. The number...

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Abstract

The invention belongs to the field of pharmaceutical preparations, in particular to a thermotropic hydrogel sustained-release veterinary drug injection containing contraception effective components and a preparation method of the thermotropic hydrogel sustained-release veterinary drug injection containing the contraceptive effective components. The injection preparation comprises three parts of anamphiphilic block copolymer, the contraceptive effective components and a solvent together. For the amphiphilic block copolymer, generally polyethylene glycol forms a hydrophilic block, and degradable polyester forms a hydrophobic block. A water system of the amphiphilic block copolymer can be thermally gelatinized when the temperature increases and is fluid liquid at room temperature, and then semi-solid gel can be formed in situ at body temperature after injection and drug administration are performed, thereby being minimally invasive. The preparation is a first thermotropic hydrogel sustained-release preparation special for the animal contraception, and the sustained-release period for one injection can range from several weeks to several months; for the first time, the effective encapsulation of hydrophobic contraceptives is tried to be directly realized with the polymer water system without using organic solvents; the thermotropic hydrogel sustained-release veterinary drug injection for the animal contraception disclosed by the invention is simple in preparation process, low in materials cost and good in development prospects by being taken as the veterinary drug preparation.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a thermotropic hydrogel veterinary drug injection preparation containing contraceptive active ingredients and a preparation method thereof. Background technique [0002] In the animal farming industry, in order to improve the quality of farmed animals or their milk products, it is usually necessary to control animals for contraception and estrus. The means of contraception in mammals mainly include surgical and non-surgical methods. The surgical method is ligation of male animals, which is permanently effective but irreversible, and has problems such as poor animal compliance. Non-surgical methods include oral contraceptives, intrauterine rings, and subcutaneous implants. Oral contraceptives have problems such as easy missed doses, large side effects, and low bioavailability, while intrauterine rings and subcutaneous implants require artificial i...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K31/567A61K31/05A61P15/18
CPCA61K9/06A61K9/0019A61K31/05A61K31/567A61K47/34A61K2300/00
Inventor 俞麟陈曦丁建东俸灵林李芳
Owner FUDAN UNIV
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