Drug-containing nanoparticle, process for producing the same and parenterally administered preparation from the nanoparticle

A drug-loading nanometer and nanoparticle technology, which is applied to medical preparations containing active ingredients, nanomedicine, nanotechnology, etc., can solve problems such as failure to achieve practical application, unsatisfactory drug absorption or local irritation, etc. To achieve the effect of good bioavailability, high absorption, good sustained release

Inactive Publication Date: 2007-02-21
LTT BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these preparations are unsatisfactory in terms of drug absorption or local irritation, and have not yet reached practical use.
In addition, no one has known the technology for in vivo absorption through the skin and mucous membranes using nanoparticles containing fat-soluble drugs or fat-soluble water-soluble drugs.

Method used

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  • Drug-containing nanoparticle, process for producing the same and parenterally administered preparation from the nanoparticle
  • Drug-containing nanoparticle, process for producing the same and parenterally administered preparation from the nanoparticle
  • Drug-containing nanoparticle, process for producing the same and parenterally administered preparation from the nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Preparation of Secondary Nanoparticles - Effect of Surfactants

[0076] Add 10 mg of sodium oleate to 0.1 mL of water and dissolve it completely with a bath ultrasonic generator to form micelles. After that, 1 mg of testosterone enanthate or 1 mg of cyclosporine A dissolved in prescribed amounts of Tween80 and ethanol were mixed into the above solution, and the mixture was homogenized for 10 minutes with an ultrasonic generator. Then, by adding a prescribed amount of calcium chloride aqueous solution thereto and stirring for 30 minutes, secondary nanoparticles containing testosterone enanthate or cyclosporine A were prepared. The drug-containing solution thus prepared was centrifuged at 10,000 rpm for 10 minutes, and the contents of testosterone enanthate and cyclosporin A in the supernatant were quantified by HPLC. The results are shown in Table 1 and Table 2.

[0077] The effect of the amount (weight ratio) of calcium and Tween on the formation of micropa...

Embodiment 2

[0084] Example 2: Preparation of Secondary Nanoparticles

[0085] Add 10 mg of sodium oleate to 0.1 mL of water and dissolve it completely with a bath ultrasonic generator to form micelles. Thereafter, 1 mg of betamethasone valerate dissolved in prescribed amounts of Tween 80 and ethanol was mixed into the above solution, and ultrasonic waves were irradiated for 10 minutes. Then, secondary nanoparticles containing betamethasone valerate were prepared by adding 33 μL of 1 M calcium chloride aqueous solution thereto and stirring for 30 minutes. The drug-containing solution thus prepared was centrifuged at 10,000 rpm for 10 minutes, and the content of betamethasone valerate in the supernatant was quantified by HPLC. The results are shown in Table 3.

[0086] Particle Formation of Betamethasone Valerate (BV)

[0087] [table 3]

[0088]

Embodiment 3

[0089] Embodiment 3: the relation of surfactant and particle size

[0090] Mix a predetermined amount of lipid-PEG (phosphatidylethanolamine-PEG (MW: 2000), manufactured by NOF) or Tween80 into 10 mg of sodium oleate, mix well with an ultrasonic generator, and then add 33 μL of 1M chlorine Calcium chloride aqueous solution, measure its particle size. The results are shown in Table 4.

[0091] The Effect of Surfactant Amount on the Particle Size of Surfactant / Oleic Acid Microparticles

[0092] [Table 4]

[0093]

[0094] ND: not determined

[0095] From the results shown in Table 4, it can be clearly seen that the greater the amount of surfactant used, the larger its particle size, and if the amount is too small, it will also aggregate or form large particles, and there is a mixing ratio that forms the smallest particle size.

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Abstract

An external preparation or injectable solution that exerts the effect of enabling percutaneous or transmucous in vivo absorption of fat-soluble drugs and water-soluble drugs not having been satisfactorily attained hitherto and that contains a highly absorbable fat-soluble / water-soluble drug. The injectable solution especially aims at sustained release and target effects. In particular, drug-containing nanoparticles (secondary nanoparticles) are provided by causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a divalent or trivalent metal salt. Further, drug-containing nanoparticles (tertiary nanoparticles) are provided by first causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a divalent or trivalent metal salt to thereby obtain secondary nanoparticles and thereafter causing a monovalent to trivalent basic salt to act on the secondary nanoparticles. Still further, there are provided a process for producing these nanoparticles, and a percutaneous or transmucous external preparation or injectable solution in which these nanoparticles are contained.

Description

technical field [0001] The present invention relates to nanoparticles containing fat-soluble drugs or fat-soluble water-soluble drugs, more specifically, to nanoparticles of fat-soluble drugs or fat-soluble water-soluble drugs and a preparation method thereof, and to nanoparticles containing the same Preparations for parenteral administration suitable for skin and mucous membranes and for injection. Background technique [0002] The purpose of transdermal and transmucosal administration is to improve the shortcomings of oral preparations, for example, (1) poor absorption of drugs through the digestive tract, resulting in irregular absorption and drug inactivation in the liver; (2) rapid drug absorption produces side effects , the side effects are especially serious in the gastrointestinal tract and liver; (3) the sustained release effect of the drug cannot be reached. [0003] Regarding the skin and mucous membrane applicability of drugs, many technologies have been put int...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/06A61K9/08A61K9/10A61K9/20A61K9/70A61K9/72A61K47/02A61K47/04A61K47/10A61K47/12A61K47/24A61K47/34A61K47/36A61K31/07A61K31/122A61K31/198A61P3/02A61K9/51
CPCA61K9/0024A61K31/07A61K31/198A61K9/5123A61K9/5146A61K9/5192A61K31/122A61P3/02A61P5/24A61K9/14B82Y5/00
Inventor 石原务水岛裕铃木润关根准三山口叶子五十岚理慧
Owner LTT BIO PHARMA
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