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Double-cyclitol medicine composition containing surfactant and preparation method thereof

A technology of surfactants and co-surfactants, which is applied in the field of bicyclic alcohol-containing surfactant-containing pharmaceutical compositions and its preparations, can solve the problems of no precipitation of bicyclic alcohol solids, improve bioavailability, and improve clinical efficacy. Curative effect, enhanced absorption effect

Active Publication Date: 2009-03-25
BEIJING UNION PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] In the research, we found that there are still suitable formulas that can form a transparent solution after adding water, and there is no precipitation of bicyclic alcohol solids after diluting with water infinitely

Method used

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  • Double-cyclitol medicine composition containing surfactant and preparation method thereof
  • Double-cyclitol medicine composition containing surfactant and preparation method thereof
  • Double-cyclitol medicine composition containing surfactant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] [Prescription Composition]

[0073] Bicyclol 40mg

[0074] LABRAFIL M 1944CS 200mg

[0075] Cremophor RH40 300mg

[0076] Tween-80 300mg

[0077] PEG400 200mg

[0078] Propyl gallate (antioxidant) 0.01%

[0079] [Preparation method] According to the prescription, weigh the excipients, heat to 60-70°C and mix evenly; add the prescribed amount of bicyclic alcohol, stir and dissolve at 60-70°C to obtain a homogeneous solution.

[0080] [Emulsification performance inspection] Method: Take the liquid medicine, add about 20 times of water at 37°C, shake or stir, observe the emulsification and dispersion of the liquid medicine in water; and measure the particle size distribution with a Nicomp laser particle size analyzer.

[0081] Results: the medicinal composition is light blue transparent microemulsion after adding water, and the particle size distribution range is 20nm-50nm. The particle size distribution chart is attached figure 1 .

[0082] [Bioavailability experime...

Embodiment 2

[0087] [Prescription Composition]

[0088] Bicyclol 40mg

[0089] LABRAFIL M 1944CS 200mg

[0090] Cremophor RH40 400mg

[0091] Tween-80 200mg

[0092] PEG400 100mg

[0093] Propyl gallate (antioxidant) 0.01%

[0094] [Preparation method] with embodiment 1.

[0095] [Emulsification performance inspection] with embodiment 1.

[0096] Results: the medicinal composition is light blue transparent microemulsion after adding water, and the particle size distribution range is 20nm-50nm. The particle size distribution chart is attached image 3 .

Embodiment 3

[0098] [Prescription Composition]

[0099] Bicyclol 40mg

[0100] Tween-80 600mg

[0101] PEG400 200mg

[0102] [Preparation method] with embodiment 1.

[0103] [Emulsification performance inspection] with embodiment 1.

[0104] Result: the pharmaceutical composition becomes a transparent solution after adding water.

[0105] [Bioavailability experiment] Test purpose: To compare the in vivo pharmacokinetic characteristics of rats after oral administration of the bicyclol pharmaceutical composition in Example 3 and bicyclol micronized crude drug CMC suspension.

[0106] Method: Single intragastric administration of SD rats ① Bicyclol pharmaceutical composition in Example 3 ② Bicyclol micronized raw drug CMC suspension 100mg / kg, 5min, 15min, 30min, 1h, 2h, 3h after administration , 4h, 6h, 8h, 12h, 24 each time point from the canthus vein from the blood, HPLC blood sample determination, draw the blood concentration - time curve, calculate the bioavailability.

[0107] Resu...

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Abstract

The invention discloses a bicyclo-ethanol medicine combination which contains surfactant, and the preparation thereof. Bicyclo-ethanol is dissolved in medicine loading substrate which is composed of one or more types of the following ingredients, surfactant, cosurfactant and oil, so as to form the medicine combination which is oily solution or semisolid. The medicine combination in different formulations can be added with water to form emulsion, microemulsion or transparent rapidly. When the medicine combination is taken orally, the absorption of difficult soluble bicyclo-ethanol is enhanced through self-emulsification, self micro-emulsification or solubilization, so as to reduce the individual difference and improve the bioavailability and clinical treatment effect of bicyclo-ethanol. The medicine combination has simple preparation process and is applicable to preparing various preparations. The invention also includes capsules, soft capsules, controlled-release capsule, osmotic pump capsules or other proper types of preparation which are prepared through the medicine combination.

Description

technical field [0001] The present invention relates to the technical field of solubilization, self-emulsification, self-microemulsification and bioavailability improvement of poorly water-soluble drugs. In the drug-loading matrix composed of one or several components, the drug delivery system is prepared, which can be self-emulsified, self-microemulsified or solubilized in the gastrointestinal tract after oral administration, thereby enhancing the absorption of the insoluble drug bicyclol, reducing individual differences, and improving bicyclol. Alcohol bioavailability and clinical efficacy. Background technique [0002] Bicyclol is an innovative anti-hepatitis drug with independent intellectual property rights developed by the Institute of Materia Medica, Chinese Academy of Medical Sciences. The bicyclol raw material and its tablets obtained the new drug certificate and production approval in 2001, and are exclusively produced by Peking Union Medical College Pharmaceutica...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61K9/107A61P1/16A61P31/12
Inventor 吕昭云张颖李强兰培潘显道赵立敏
Owner BEIJING UNION PHARMA FACTORY
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