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Transdermal absorptive preparation of pennogenin compounds

A technology for transdermal absorption preparations and penenosides, which can be used in medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., and can solve problems such as gastrointestinal discomfort and low bioavailability.

Inactive Publication Date: 2008-12-17
YUNNAN BAIYAO GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmacokinetic studies have shown that the bioavailability of pinanoside compounds is extremely low, and more than 90% of them are excreted from the feces via the gastrointestinal tract in the original form. The main adverse reaction is gastrointestinal discomfort

Method used

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  • Transdermal absorptive preparation of pennogenin compounds
  • Transdermal absorptive preparation of pennogenin compounds
  • Transdermal absorptive preparation of pennogenin compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Grind and dissolve 1 g of pinanoside compounds with 1 g of dimethyl sulfoxide and 1 g of azone, mix evenly with 5 g of glycerin, 6 g of liquid paraffin, and 5 g of lanolin, then add 12 g of stearic acid and 3.5 g of glyceryl monostearate , Vaseline 1g, triethanolamine 0.4g, ethyl p-hydroxybenzoate 0.15g, add distilled water to 100g, stir and emulsify at high speed in a milk homogenizer to form an O / W emulsion. Depending on the severity of the condition, apply 0.3-1g of the emulsion 3-5 days before the onset of menstruation, and the application position is the inner arm and inner thigh. 1 sticker every 1-3 days, up to 7 days. It is used for the treatment of gynecological hyperemia and inflammation, including hemorrhage caused by functional uterine bleeding and family planning measures.

Embodiment 2

[0040] 0.5 g of pinanoside compounds was ground and dissolved with 0.8 g of azone and 8 g of propylene glycol. Take 10001g of polyvinyl alcohol and 1.6g of sodium carboxymethyl cellulose to swell in 10ml of water to obtain auxiliary material A; take 4g of sodium polyacrylate and 2g of glycerin, add 10-20ml of water, and mix well to obtain auxiliary material B. Stir A and B evenly, add pinanoside compounds containing penetration enhancers, add water to 100g, and stir evenly. Apply evenly on the cataplasm applicator, solidify, form, divide, and cover to obtain a cataplasm with a paste thickness of about 50 μm. Application locations are arms, thighs, abdomen and back. Each sticking unit contains 10 mg pinanoside compounds. 1 sticker every 1-3 days, up to 7 days. It is used for the treatment of gynecological hyperemia and inflammation, including hemorrhage caused by functional uterine bleeding and family planning measures.

Embodiment 3

[0042] 3 g of pinanoside compounds, 0.6 g of azone, 0.6 g of dimethyl sulfoxide, 5 g of propylene glycol, and 0.2 g of menthol as penetration enhancers were ground and dissolved. Take carbomer U100.5g, swell with 7-10ml of water, stir at 400r / min in a water bath at 50°C for 30 minutes, and make phase A; mix 6g of sodium polyacrylate, 0.8g of kaolin, and 37g of glycerin evenly, and make phase B ; Dissolve 0.08g of aluminum trichloride and 0.12g of citric acid in 2ml of water, forming phase C. Mix Phase C and Phase B, stir evenly, then add to Phase A at a stirring speed of 200r / min, keep the temperature at 50°C, add the miscible product of drug and penetrant after 10 minutes, and continue stirring for 30 minutes. The viscous semi-solid fluid is obtained, which is evenly coated on the non-woven fabric, left at room temperature, covered with a backing, punched, and packaged to obtain the cataplasm formulation. Application locations are arms, thighs, abdomen and back. Each sticki...

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Abstract

The present invention relates to one special preparation form of pennogenin compounds as active component, and is especially transdermal adsorbed preparation of pennogenin compounds. The transdermal adsorbed preparation of pennogenin compounds consists of pennogenin compounds 0.05-40 wt%, transdermal promoter 1-20 wt%, and medicinal substrate 40-98.5 wt%. The pennogenin compounds have high activity and thus small dosage, and the transdermal adsorbed preparation of pennogenin compounds has no adverse reaction of gastrointestinal tract. The transdermal adsorbed preparation of pennogenin compounds may be prepared into different externally applied preparation forms.

Description

technical field [0001] The invention relates to a special preparation form with pinanoside compounds as active ingredients. Background technique [0002] The distribution of pinanosides in the plant kingdom is not very wide, and the content is relatively low. Chinese patent application No. 02150907.7 discloses a "17-hydroxy C#-[27] steroid compound, its synthesis method and its use", which can be used for the synthesis of pinanoside compounds. Chinese patent 03135589.7 discloses the purification of pinanoside compounds. Chinese Patent No. 85108520 discloses the application of two pinanoside compounds in gynecological anemia. Pharmacokinetic studies have shown that the bioavailability of pinanoside compounds is extremely low, and more than 90% of them are excreted from the feces via the gastrointestinal tract in their original form. The main adverse reaction is gastrointestinal discomfort. Therefore, it is particularly necessary to find new dosage forms of pinanosides. C...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/706A61P15/00
Inventor 唐书明冯有
Owner YUNNAN BAIYAO GROUP