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Medicament compound adopting bicyclo-ethanol as active component and preparation thereof

A technology of active ingredients and compositions, which is applied in the field of pharmaceutical compositions and preparations with bicyclol as the active ingredient, can solve the problems of no solid precipitation of bicyclol, improve bioavailability, improve clinical curative effect, enhance absorption effect

Active Publication Date: 2011-05-18
BEIJING UNION PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] 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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  • Medicament compound adopting bicyclo-ethanol as active component and preparation thereof
  • Medicament compound adopting bicyclo-ethanol as active component and preparation thereof
  • Medicament compound adopting bicyclo-ethanol as active component and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] [Prescription composition]

[0074] Bicyclic alcohol 40mg

[0075] LABRAFIL M 1944CS 200mg

[0076] Cremophor RH40 300mg

[0077] Tween-80 300mg

[0078] PEG400 200mg

[0079] Propyl gallate (antioxidant) 0.01%

[0080] [Preparation method] According to the prescription, weigh the auxiliary materials, heat to 60-70°C and mix uniformly; add the prescription amount of bicyclic alcohol, stir and dissolve at 60-70°C to obtain a uniform solution, and get it.

[0081] [Emulsification performance inspection] Method: take the drug solution, add about 20 times 37℃ water, shake or stir, observe the emulsification and dispersion of the drug solution in the water; and use the Nicomp laser particle size analyzer to measure the particle size distribution.

[0082] Result: The pharmaceutical composition showed a light blue transparent microemulsion after adding water, with a particle size distribution range of 20nm-50nm. See attached for particle size distribution figure 1 .

[0083] [Bioavailabil...

Embodiment 2

[0088] [Prescription composition]

[0089] Bicyclic alcohol 40mg

[0090] LABRAFIL M 1944CS 200mg

[0091] Cremophor RH40 400mg

[0092] Tween-80 200mg

[0093] PEG400 100mg

[0094] Propyl gallate (antioxidant) 0.01%

[0095] [Preparation method] Same as Example 1.

[0096] [Emulsification performance inspection] Same as Example 1.

[0097] Result: The pharmaceutical composition showed a light blue transparent microemulsion after adding water, with a particle size distribution range of 20nm-50nm. See attached for particle size distribution image 3 .

Embodiment 3

[0099] [Prescription composition]

[0100] Bicyclic alcohol 40mg

[0101] Tween-80 600mg

[0102] PEG400 200mg

[0103] [Preparation method] Same as Example 1.

[0104] [Emulsification performance inspection] Same as Example 1.

[0105] Results: The pharmaceutical composition became a transparent solution after adding water.

[0106] [Bioavailability experiment] Test purpose: To compare the in vivo pharmacokinetic characteristics of the bicyclic alcohol pharmaceutical composition in Example 3 and the CMC suspension of the micronized bicyclic alcohol raw material drug after oral administration in rats.

[0107] Methods: SD rats were given a single intragastric administration ①The bicyclic alcohol pharmaceutical composition in Example 3 ②The micronized bicyclic alcohol crude drug CMC suspension 100mg / kg, 5min, 15min, 30min, 1h, 2h, 3h after administration , 4h, 6h, 8h, 12h, 24 each time point from the eye canthus vein to take blood, HPLC blood sample determination, draw blood concentration-...

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Abstract

The invention discloses a medicament compound adopting bicyclo-ethanol as an active component and a preparation thereof. The medicament compound is formed by dissolving the bicyclo-ethanol in a medicament carrying substance consisting of one or more of surfactant, cosurfactant and oils, and is in the form of an oily solution or a semisolid object at room temperature. Through different formulas, the medicament compound can form emulsion and microemulsion quickly through gentle agitation. After being taken orally, the medicament compound can be used for enhancing the bicyclo-ethanol absorption of insoluble medicaments through self-emulsification and self-microemulsification, reducing the individual differences, and improving the bioavailability and clinical effects of the bicyclo-ethanol. The medicament compound is simple in preparation technology and is suitable for being prepared into various preparations. The invention further discloses a hard capsule, a soft capsule, a slow control and release type capsule, an osmotic pump type capsule and other suitable preparations, which are made from the medicament compound.

Description

[0001] The present invention is a divisional application of the invention patent application with the application number 200810117846.8 and titled "Bicyclic alcohol surfactant-containing pharmaceutical composition and its preparation". The original application was filed on August 6, 2008. Technical field [0002] The present invention relates to the technical fields related to solubilization, self-emulsification, self-microemulsification and improvement of bioavailability of poorly water-soluble drugs, specifically by dissolving bicyclic alcohol in one of surfactants, co-surfactants, and oils. In a drug-carrying matrix composed of one or several components, a 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 bicyclo The bioavailability and clinical efficacy of alcoh...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61K47/44A61P1/16A61P31/12
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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