Injectable depot compositions and process of preparation of such compositions

An injection composition and composition technology, applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as toxic side effects and unpopular biological active agents

Inactive Publication Date: 2009-09-23
PANACEA BIOTEC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In some cases, this burst release can produce an undesired increase in the level of the bioactive agent, resulting in toxic side effects and / or minimal release of the active agent (drug) after providing a subtherapeutic concentration of the active agent (drug)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] No. Component Amount / Unit Dose

[0090] component 1

[0091] 1. Tamsulosin 12.0mg

[0092] 2. Lactide-glycolide copolymer 50 / 50 400.0mg

[0093] 3. Polyvinyl alcohol 240.0mg (disappears during processing)

[0094] 4. Dichloromethane 10.0ml (disappears during processing)

[0095] 5. Water for injection 24.0ml (disappears during processing)

[0096] 6. Hydroxyethylcellulose 40.0mg

[0097] component 2

[0098] 7. Polyethylene glycol 1.5ml

[0099] 8. Glycerin 0.5ml

[0100] process:

[0101] i) Prepare polyvinyl alcohol solution by dissolving polyvinyl alcohol in hot water for injection with stirring.

[0102] ii) Dissolve tamsulosin and biodegradable polymer in dichloromethane and add it to the polyvinyl alcohol solution under homogenization conditions.

[0103] iii) The emulsion of step (ii) is stirred and optionally vacuum is applied until the dichloromethane is completely removed leaving a suspension of microparticles.

[0104] iv) Wash the microparticles w...

Embodiment 2

[0109] No. Component Amount / Unit Dose

[0110] component 1

[0111] 1. Tamsulosin 12.0mg

[0112] 2. Lactide-glycolide copolymer 50 / 50 120.0mg

[0113] 3. Gelatin 30.0mg (disappears during processing)

[0114] 4. Dichloromethane 2.0ml (disappears during processing)

[0115] 5. Water for injection 5.0ml (disappears during processing)

[0116] 6. Mannitol 7.0mg

[0117] 7. Sodium carboxymethylcellulose 60.0mg

[0118] component 2

[0119] 8. Propylene glycol 1.7ml

[0120] 9. Ethanol 0.3ml

[0121] process:

[0122] i) A solution was prepared by dissolving gelatin in warm (40°C) water for injection with stirring and cooling to room temperature by continuous stirring.

[0123] ii) Tamsulosin and lactide-glycolide copolymer 50 / 50 were dissolved in dichloromethane and this clear solution was added to the gelatin solution under homogenization conditions.

[0124] iii) Stir the emulsion of step (ii) until the dichloromethane is completely evaporated, leaving a suspension o...

Embodiment 3

[0130] No. Component Amount / Unit Dose

[0131] component 1

[0132] 1. Tamsulosin 12.0mg

[0133] 2. Lactide-glycolide copolymer 50 / 50120.0mg

[0134] 3. Polyvinyl alcohol 30.0mg (disappears during processing)

[0135] 4. Dichloromethane 2.0ml (disappears during processing)

[0136] 5. Water for injection 5.0ml (disappears during processing)

[0137] 6. Mannitol 7.0mg

[0138] component 2

[0139] 7. Sodium carboxymethylcellulose 50.0mg

[0140] 8. Propylene glycol 2.2ml

[0141] 9. Ethanol 0.3ml

[0142] process:

[0143] i) Prepare a solution by dissolving polyvinyl alcohol in hot water for injection with stirring and cooling to room temperature by continuous stirring.

[0144] ii) Tamsulosin and lactide-glycolide copolymer 50 / 50 were dissolved in dichloromethane and this clear solution was added to the polyvinyl alcohol solution under homogenization conditions.

[0145] iii) Stir the emulsion of step (ii) until the dichloromethane is completely evaporated, leavin...

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PUM

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Abstract

Novel injectable compositions are provided comprising an active agent which is tarnsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time.; Also described are process for preparation of such novel compositions and method of using them.

Description

technical field [0001] The present invention relates to a novel injectable composition, which comprises an active agent and one or more pharmaceutically acceptable excipients, the active agent being tamsulosin or letrozole or pharmaceutically acceptable salts, derivatives, Isomers, polymorphs, solvates, hydrates, analogs, enantiomers, tautomeric forms or mixtures thereof, wherein the composition is preferably formulated as biodegradable microparticles (microparticles) or Nanoparticles which may optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable composition of the present invention preferably forms a depot when administered in vivo and is in the form of an in situ gelling composition or a monolithic graft composition which provides tamsulosin or extended release of letrozole over an extended period of time. The invention also describes methods of making the novel compositions and methods of using t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/10A61K9/50A61K31/18A61K31/138A61K31/4196A61K47/34A61P35/00
CPCA61K9/1647A61K9/06A61K9/0024A61P13/08A61P35/00A61K9/16A61K47/34B82Y5/00
Inventor 拉杰什·贾殷库尔·昌德·吉恩达尔萨姆帕斯·库马尔·德瓦拉扬
Owner PANACEA BIOTEC
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