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Formulations comprising entrapped active ingredients and uses thereof

A technology of active ingredients and formulas, applied in the field of formulas containing encapsulated active ingredients and their uses, which can solve the problems of low anti-exudation and anti-inflammatory activities

Inactive Publication Date: 2004-05-26
THE SCRIPPS RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antiexudative and anti-inflammatory activities of orally administered GA were lower compared with the corresponding activities of orally administered acetylsalicylate or indomethacin

Method used

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  • Formulations comprising entrapped active ingredients and uses thereof
  • Formulations comprising entrapped active ingredients and uses thereof
  • Formulations comprising entrapped active ingredients and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Preparation of GlcNAc Encapsulated by Liposomes

[0122] 33 μmol DSPC and 33 μmol Chol (or other compositions, see Table 1 below) were dissolved in 3 ml of chloroform:methanol (95:5, v / v) solution in a 100 ml Erlenmeyer flask. The organic solvent was evaporated under vacuum (600 mm Hg) at room temperature. After removing the last visible traces of solvent, the vacuum was maintained for at least 30 minutes.

[0123] 2 ml of GlcNAc (containing a total of 10 μCi of labeled and 5.38 mg of unlabeled GlcNAc in a 0.85% sodium chloride solution, with a final unlabeled to labeled molar ratio of 10000 tol) was added to the flask. The flask was placed in a water bath at 60°C (see Table 1 for temperatures of other compositions) for 5 minutes, and the dry lipid was suspended by vigorous shaking at 2500 rpm for 1 minute. Liposomes were annealed at the same temperature for 45 minutes. The prepared liposomes were then dispensed into four 1.5-ml Eppendorf tubes. Liposomes were dried...

Embodiment 2

[0167] In vitro release of GlcNAc from liposomes

[0168] 100 μl of liposome-encapsulated GlcNAc prepared as described above was suspended in 3 ml of 0.1 M PBS (pH 7.4) in a 50 ml centrifuge tube. Liposomes were incubated at 37°C in a shaking incubator at 60 rpm. After various time points, liposomes were isolated by centrifugation at 20000 rpm for 15 minutes. GlcNAc released in the supernatant ( 3 H activity) was determined by liquid scintillation oscillator. The liposome pellet was resuspended in 3 ml of fresh PBS and incubated under the same conditions. Different types of liposomes [ 3 H] GlcNAc release percentage as a function of time is plotted in figure 1 .

[0169] figure 1 shows the in vitro release of different liposome formulations encapsulated in the presence of 0.1M PBS, pH 7.4 [ 3 H] Dynamic overview of GlcNAc. Determination of [ 3 H] Amount of GlcNAc, calculated as a percentage of initially encapsulated compound released.

[0170] figure 1 show[ 3 The...

Embodiment 3

[0176] In vivo retention of GlcNAc after intra-articular application

[0177] 50 μl of GlcNAc solution (unlabeled 2.69 mg / ml, labeled 5 μCi / ml, unlabeled molecule:labeled molecule 10000:1) was injected into the knee joints of six rats. The animals (2 animals per time point) were sacrificed 0, 30 minutes and 2 hours after application of the GlcNAc solution. Two additional rats were injected with saline as negative controls. All joint specimens were taken and homogenized with 5ml normal saline at 16000rpm for about 30 seconds. 100 μl of tissue homogenate was added to 500 μl of histolytic solution. The solution was incubated at 50°C for 16 hours, mixed with 30 μl of glacial acetic acid and 5 ml of liquid scintillation layer. Determined by liquid scintillation counting [ 3 H] GlcNAc activity.

[0178] Fourteen rats were used for each liposomal formulation. 50 [mu]l of liposomes (1.13 [mu]Ci / ml, GlcNAc concentration 0.61 mg / ml, unlabeled:labeled molecule 10000:1 prepared acco...

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Abstract

Formulations comprising entrapped active ingredients, such as aminosugars, and uses thereof are disclosed. In one embodiment, intra-articular injectable formulations are provided.

Description

field of invention [0001] The present invention generally relates to formulations containing encapsulated active ingredients such as amino sugars and uses thereof. More particularly it relates to formulations containing N-acetylglucosamine which can be injected intra-articularly. Background technique [0002] Osteoarthritis is a common joint disease with a marked social response (Lawrence et al., (1998) Arthritis Rheum. 41: 778; Gabriel et al., (1997) J. Rheumatol. 24: 719; March et al., ( 1997) Baillieres Clin. Rheumatol. 11:817). Drug classes used to treat OA include, nonsteroidal anti-inflammatory drugs (NSAIDS), injectable intra-articular corticosteroids and hyaluronic acid. These drugs primarily relieve pain, but still have not been shown to provide true relief by slowing or stopping the disease process. (Altman et al. (1998) Osteoarthritis Cartilage 6 Suppl. A: 22; Hochberg et al. (1995) Arthritis Rheum. 38: 1535; Hochberg et al. (1995) Arthritis Rheum. 38: 1541). ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/16A61K9/51A61K31/7008A61K31/726A61K47/24A61K47/34A61K47/36A61K47/48A61P19/00A61P19/02A61P29/00
CPCA61K9/0019A61K9/127A61P19/00A61P19/02A61P29/00
Inventor M·洛茨A·R·希赫曼S-B·黄C·胡
Owner THE SCRIPPS RES INST
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