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Spirolactone oral self-microemulsion concentrated solution

A technology of spironolactone and self-microemulsion, which is applied in the field of medicine and can solve the problems of increasing microbial contamination of emulsions, increasing storage and transportation costs of preparations, and reducing oral compliance of patients and children

Active Publication Date: 2021-07-30
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the application prepared spironolactone into a nanoemulsion, the prepared nanoemulsion would reduce the oral compliance of patients, especially children, due to the significant bitterness of the spironolactone bulk drug; (30%-50%), which not only increases the risk of microbial contamination of the emulsion, but also increases the storage and transportation costs of the preparation

Method used

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  • Spirolactone oral self-microemulsion concentrated solution
  • Spirolactone oral self-microemulsion concentrated solution
  • Spirolactone oral self-microemulsion concentrated solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The saturation solubility of embodiment 1 spironolactone in each auxiliary material

[0044] In this study, the saturation solubility of spironolactone in some excipients was compared, and the results are shown in Table 1.

[0045] The solubility of table 1 spironolactone in various excipients

[0046]

[0047]

[0048] Among all the excipients tested, spironolactone has higher solubility in medium-chain triglyceride (MCT), Solutol HS 15, Cremophor RH40, and absolute ethanol, so medium-chain triglyceride (MCT) was initially selected as the oil phase , Solutol HS 15 and / or Cremophor RH40 are emulsifiers, and absolute ethanol is a co-emulsifier.

Embodiment 2

[0049] The emulsifier result of embodiment 2 different oils, emulsifier, co-emulsifier

[0050] Compatibility experiments were carried out on the screened oil phase, emulsifier and co-emulsifier. Soybean oil and medium chain triglyceride (MCT) were used as the oil phase, Solutol HS 15 and Tween 80 were used as emulsifiers, and ethanol was used as co-emulsifier . Mix the oil phase, emulsifier, and co-emulsifier evenly according to a certain ratio, then add 10 times deionized water to stir and emulsify, and observe the emulsification result. The emulsification situation is divided into

[0051] Table 2 Compatibility results of different oils, emulsifiers and co-emulsifiers

[0052]

Embodiment 3

[0053] Embodiment 3 prescription screening

[0054] Prepare from the microemulsion concentrate according to the prescription of table 3, add 10 volumes of water to form a microemulsion, measure the particle size after emulsification, and measure the saturation solubility of spironolactone in each prescription.

[0055]

[0056]

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Abstract

The invention discloses a spirolactone oral self-microemulsion concentrated solution. The concentrated solution is a spirolactone composition with good taste, stable property and high bioavailability, the composition is composed of spirolactone and auxiliary materials, and the auxiliary materials are composed of an oil phase, an emulsifier, a co-emulsifier, a flavoring agent and an antioxidant. The weight ratio of the spirolactone to the oil phase to the emulsifier to the co-emulsifier to the flavoring agent to the antioxidant is (0.1-10%): (10-30%): (20-60%): (20-30%): (0.1-3%): (0.1-1%). The self-microemulsion concentrated solution composition can form O / W type microemulsion after being diluted with water before use or being directly taken. According to the micro-emulsion, the solubility and oral bioavailability of the spirolactone are remarkably improved, and the spirolactone self-micro-emulsion composition can improve the bad taste of the spirolactone and enhance the administration compliance of patients, especially child patients.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a spironolactone oral self-microemulsion composition and a preparation method thereof, that is, the solubility and bioavailability of spironolactone are improved by preparing the self-microemulsion preparation. Background technique [0002] Spironolactone, a synthetic steroid compound, is a potassium-sparing low-efficiency diuretic. Its chemical structure is shown below. Spironolactone is similar in structure to aldosterone and is a competitive inhibitor of aldosterone. It acts on the distal convoluted tubule and collecting duct to block the exchange of Na+-K+ and Na+-H+, resulting in increased excretion of Na+, C1- and water, decreased excretion of K+, Mg2+ and H+, and the effect on Ca2+ is uncertain. Since the drug only acts on the distal convoluted tubule and collecting duct, and has no effect on other segments of the renal tubule, the diuretic effect is weak. In addition, t...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/585A61K47/10A61K47/44A61P7/10
CPCA61K31/585A61K9/1075A61K47/10A61K47/44A61P7/10Y02A50/30
Inventor 王坚成陈鑫王向宇
Owner PEKING UNIV
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