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Porous silica gel as a carrier for liquid technologies

A technology of liquid and liquid materials, applied in the fields of silicon compounds, emulsion delivery, chemical instruments and methods, etc.

Inactive Publication Date: 2015-11-25
WR GRACE & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This makes these materials difficult to process in pharmaceutical manufacturing
In order to have acceptable flowability and compactability, high levels of carrier and coating materials must be added, increasing the weight and bulk of the resulting dosage form

Method used

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  • Porous silica gel as a carrier for liquid technologies
  • Porous silica gel as a carrier for liquid technologies
  • Porous silica gel as a carrier for liquid technologies

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0144]

[0145] The D10, D50 and D90 values ​​indicate the weighted 10th, 50th and 90th percentiles of the particle diameter distribution. These values ​​are obtained from Malvern Instruments Ltd of Malvern TM Mastersizer2000 instrument was obtained. PV: pore volume; SA: surface area; APD: average pore diameter; BETSA: surface area; and relative span was measured using the BJH nitrogen adsorption method at a pressure of 0.995 using the ASAP2420HV accelerated surface area and porosity measurement system available from Micromeretics Instrument Corporation Determination.

[0146] Example 2

[0147] Procedure: Place 2 to 5 g (based on bulk density) of solid carrier material in a 100 ml beaker and add oil or surfactant dropwise from a dropper while mixing with a spatula according to ASTM D281. Continue adding oil or surfactant until a thick paste-like mass forms. Stop adding oil or surfactant when the mass appears to contain excess oil. Record the burette reading when the b...

Embodiment 2

[0149] The table below lists the oil and its adsorption capacity on the sample S1 material and the specific gravity of the oil.

[0150] Table 2

[0151] serial number oil name Specific gravity (g / mL) Adsorption capacity (g / 100g) 1 raw linseed oil 0.930 294 2 Eucalyptus oil 0.915 328 3 lemongrass oil 0.895 287 4 peppermint 0.890 307 5 castor oil 0.960 316 6 sesame oil 0.923 298 7 olive oil 0.920 305 8 clove oil 1.045 390 9 Oleic acid 0.895 300 10 dl-alpha-tocopherol 0.950 292 11 Captex 355 0.940 315 12 Labrafac PG 0.919 304 13 Miglitol 812 0.940 319 14 Capmul MCM 0.995 303

[0152] The table below lists the surfactants and their adsorption capacity on the sample S1 material as well as the specific gravity of the surfactants.

[0153] table 3

[0154] serial number Surfactant name Specific gravity (g / mL) Oil adsorption value S1 (g / ...

Embodiment 3

[0160]

[0161] Bulk density was measured by USP616 Method 1 using a 250ml graduated cylinder (USP30-NF25). Tap density is measured by USP616 method 2 (250 taps per minute) using a 250ml graduated cylinder with an ETD-1020 tap density tester available from Electrolab. The USP grade is an observational measure of powder flow and is rated according to Table 7 below.

[0162] Table 7

[0163] Compressibility Index (%) flow characteristics Hausnaby <10

excellent 1.00-1.11 11-15 good 1.12-1.18 16-20 generally 1.19-1.25 21-25 passable 1.26-1.34 26-31 Difference 1.35-1.45 32-37 very poor 1.46-1.59 >38 extremely bad >1.60

[0164] Example 4

[0165] Following the procedure of Example 2, 10 grams of sample S1 was charged with 16.25 ml of sesame oil, which gave a 1:1.5 ratio of inorganic oxide material to oil. The volume of the mixture was reduced from 65ml to 50ml over a period of 10 hours, as figure 1 The r...

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Abstract

Compositions containing a biologically active ingredient and an inorganic oxide material are disclosed. Methods of making and using compositions containing a biologically active ingredient and an inorganic oxide material are also disclosed. The present invention relates to compositions comprising inorganic oxide porous material containing a biologically active ingredient in liquid form, methods of making such compositions, and methods of using them.

Description

technical field [0001] The present invention relates to compositions comprising inorganic oxide porous materials containing biologically active ingredients in liquid form, methods of making such compositions, and methods of using the same. Background technique [0002] The oral route remains the preferred route of drug administration due to its convenience and good patient compliance. A major problem with oral pharmaceutical formulations is unstable and incomplete absorption throughout the gastrointestinal (GI) tract, resulting in low and variable bioavailability and lack of dose proportionality. These problems are mainly caused by the poor water solubility of the active ingredients. It has been reported that an estimated 40% of existing pharmaceutical active ingredients and an even higher proportion of all newly developed drugs are poorly or insoluble in water. This poses a major challenge to drug development as there is a high need to create suitable formulations to impr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01J20/10
CPCB01J20/10B01J20/28004B01J20/28059B01J20/28073C01B33/193B01J20/103A61K9/1075A61K9/2077A61K9/143A61K9/14
Inventor F.H.蒙苏尔
Owner WR GRACE & CO