Estradiol transdermal spray and preparation method thereof

An estradiol and spray technology, applied in the field of estradiol transdermal spray and its preparation, can solve problems such as poor drug effect persistence, achieve the effects of less irritation, prolonged drug action time, and convenient use

Inactive Publication Date: 2011-04-20
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This transdermal spray is composed of estradiol, volatile solvent ethanol and ethylhexyl salicylate, but there is a technical problem of relatively poor drug effect persistence

Method used

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  • Estradiol transdermal spray and preparation method thereof
  • Estradiol transdermal spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～13

[0040] Weigh estradiol, polymer, plasticizer and penetration enhancer according to the table below, add ethanol to dissolve to 10g, and put them in a quantitative spray device to prepare estradiol transdermal spray.

[0041] Spray the prepared estradiol transdermal spray on a glass plate, and observe whether it can form spray, film forming speed and properties of film forming.

[0042] Formulation composition and film-forming performance of table 1 spray

[0043]

Embodiment 14

[0045] Weigh 0.1 g of estradiol and 0.5 g of Eudragit RL PO, add ethanol to dissolve to 10 g, and put them in a quantitative spray device to prepare estradiol transdermal spray.

[0046] The obtained estradiol transdermal spray is carried out in vitro percutaneous penetration test:

[0047] TK-12 transdermal diffusion tester was used to investigate the transdermal penetration rate of estradiol spray with suckling pig skin as the skin model. The piglet skin from which the subcutaneous tissue was removed was washed in normal saline. Fix its cuticle upwards between the supply pool and the receiving pool of the diffusion pool, exhaust the air bubbles, and keep the circulating water at (37±0.5) °C. Add pre-degassed receiving medium into the receiving cell, and add a stirring bar at 300r·min -1 stirring speed. Spray estradiol spray on the skin, sample 1ml at 2, 4, 8, 18, 20, 22, and 24 hours respectively, and add an equal amount of receiving solution at the same temperature. The...

Embodiment 15

[0050] Weigh 0.1 g of estradiol and 0.5 g of hydroxypropyl cellulose Klucel EF, add ethanol to dissolve to 10 g, and put them in a quantitative spray device to prepare estradiol transdermal spray.

[0051] The prepared estradiol transdermal spray was subjected to an in vitro transdermal penetration test, and the test method was as in Example 14.

[0052] The steady-state permeation rate of estradiol is 0.053 μg cm -2 h -1 , 24h cumulative permeation amount is 1.43μg·cm -2 .

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Abstract

The invention discloses an estradiol transdermal spray, composed of the following raw materials in percentage by weight: 0.1-10% of estradiol, 0.5-10% of polymer, 0-20% of penetration enhancer, 0-10% of plasticizer and balance of solvent. The estradiol transdermal spray provided by the invention is applied to skin in a spray from, a uniform polymer thin film is formed after the solvent is volatilized, and medicine is dispersed in the film in a molecule form, so that not only the medicine transdermal penetration effect is improved and the blood concentration is sustained and stable, but also the patient compliance is good. The estradiol transdermal spray is filled in a spraying device and can be directly used, thus being easy and simple to use, and the dosage can be freely adjusted as required. The invention also discloses a preparation method of the estradiol transdermal spray, which has strong operability and low technological conditional requirements, and is simple and easy to realize and easy for industrialized production.

Description

technical background [0001] The invention relates to the field of pharmaceutical preparations, in particular to an estradiol transdermal spray and a preparation method thereof. Background technique [0002] Estradiol is an endogenous estrogen, and its main clinical applications include: improving menopausal symptoms (treatment of menopausal syndrome), reducing the risk and mortality of ischemic cardiovascular disease, and preventing Alzheimer's disease , Prevention and treatment of osteoporosis, etc. [0003] Currently, the most commonly used methods of administration of estradiol are oral, vaginal and transdermal administration. Oral administration method, due to the existence of hepatic first-pass effect, the oral bioavailability of estradiol is very low, and the half-life is 1.7h; and estradiol will affect the metabolism of intrahepatic protein, which may lead to cholecystitis and other diseases. Big side effects. The vaginal administration method will cause side effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K31/565A61K47/30A61K47/32A61K47/38A61P15/12A61P9/00A61P9/10A61P19/10A61P15/00A61P25/28
Inventor 梁文权俞振伟梁漪
Owner ZHEJIANG UNIV
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