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A kind of oral self-microemulsion concentrate of spironolactone

A technology of self-microemulsion and concentrated solution, which is applied in the field of medicine, can solve the problems of increasing the microbial contamination of the emulsion, increasing the cost of preparation storage and transportation, reducing the oral compliance of patients and children, and achieving the goal of increasing oral bioavailability and reducing adverse reactions Generate and realize the effect of large-scale industrial production

Active Publication Date: 2022-08-09
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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  • A kind of oral self-microemulsion concentrate of spironolactone
  • A kind of oral self-microemulsion concentrate of spironolactone
  • A kind of oral self-microemulsion concentrate of spironolactone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

[0045] Table 1 Solubility of Spironolactone in Various Excipients

[0046]

[0047]

[0048] Among all the tested excipients, the solubility of spironolactone in medium chain triglyceride (MCT), Solutol HS 15, Cremophor RH40 and absolute ethanol is relatively high, 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] Example 2 Emulsifier results of different oils, emulsifiers, co-emulsifiers

[0050] The selected oil phase, emulsifier and co-emulsifier were tested for compatibility. Soybean oil and medium chain triglyceride (MCT) were used as oil phase, Solutol HS 15 and Tween 80 were used as emulsifier, and ethanol was used as co-emulsifier. . The oil phase, emulsifier and co-emulsifier are mixed uniformly according to a certain proportion, and then 10 times deionized water is added for stirring and emulsification, and the emulsification result is observed. Divide emulsification into

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

[0052]

Embodiment 3

[0053] Example 3 Prescription Screening

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

[0055]

[0056]

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Abstract

The invention discloses a spironolactone oral self-microemulsion concentrate, which is a spironolactone composition with good taste, stable properties and high bioavailability. The composition consists of spironolactone and auxiliary materials. Co-emulsifier, flavoring agent and antioxidant, the weight ratio of each component is spironolactone: oil phase: emulsifier: co-emulsifier: flavoring agent: antioxidant = 0.1%-10%: 10%-30%: 20%-60%: 20%-30%: 0.1%-3%: 0.1%-1%, the self-microemulsion concentrate composition will form an O / W type microemulsion after being diluted with water before use or directly taken. The microemulsion significantly improves the solubility and oral bioavailability of spironolactone, and the spironolactone self-microemulsion composition can improve the bad taste of spironolactone and enhance the administration compliance of patients, especially children.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a kind of oral self-microemulsion composition of spironolactone and a preparation method thereof, that is, the solubility and bioavailability of spironolactone are improved by preparing a self-microemulsion preparation. Background technique [0002] Spironolactone, a synthetic steroid compound, is a potassium-sparing ineffective diuretic. Its chemical structure is shown below. Spironolactone is structurally similar to aldosterone and is a competitive inhibitor of aldosterone. It acts on the distal convoluted tubules and collecting ducts, blocking the exchange of Na+-K+ and Na+-H+, resulting in an increase in the excretion of Na+, C1- and water, and a decrease in the 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 e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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