Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Once-weekly oral administration of aripiprazole

a technology of aripiprazole and once-weekly oral administration, which is applied in the direction of drug composition, metabolism disorder, nervous disorder, etc., can solve the problems of time-consuming and expensive supervised administration, patients may consider once-a-day oral administration dosage regime too frequent for many patients, etc., to reduce the indirect human cost of drugs, improve patient convenience and compliance, and increase adverse events

Inactive Publication Date: 2014-02-13
ZYSIS
View PDF1 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention provides new ways to make medicine called compositions. These compositions can be taken once a day, and they can contain more of a drug called aripiprazole than the current daily pill. This means that the medicine can be more effective, but it won't make people sick more often. The medication also releases the drug in a controlled way, which may make it more effective and tolerable. Overall, these compositions can improve patient care and make the drug treatment process more efficient.

Problems solved by technology

There are a number of disadvantages associated with the dosage regimen for aripiprazole described above for treating schizophrenia, bipolar disease and other CNS conditions.
The once daily oral administration dosage regime may be considered too frequent for many patients.
Such patients often require time consuming and expensive supervised administration.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Once-weekly oral administration of aripiprazole
  • Once-weekly oral administration of aripiprazole
  • Once-weekly oral administration of aripiprazole

Examples

Experimental program
Comparison scheme
Effect test

example 1

Aripiprazole Compositions

[0285]30 mg direct compression (DC) and wet granulation (WG) controlled release tablets were manufactured as described below.

[0286]Direct Compression Tablets

[0287]The ingredients set out in Table 1 below were blended together in a planetary mixer for 5 minutes. The blend was compressed on a rotary tabletting machine, using 7.0 mm diameter round n / c punches. The tablet breaking strength was 2.5 kp to 3.5 kp.

TABLE 1Direct Compression CompositionDJ / 1 / 27 / ADCIngredient%tablet mgbatch gAripiprazole2030100Methocel K4M3552.5175Avicel PH 2004466220Sodium Stearyl Fumarate11.55100150500

[0288]Wet Granulation Tablets

[0289]The ingredients set out in Table 2 below except for sodium stearyl fumarate were blended together in planetary mixer for 5 minutes prior to wet granulation with purified water. The moist powders were dried in a fluid bed drier at an inlet temperature of 70° C. for 15 minutes. The dried granule had a loss on drying value of 2.5% w / w. The granules were si...

example 2

In Vitro Release Experiments

[0291]The release profiles of Aripiprazole from the DC and WG tablets described in Example 1 were studied in pH 4.0 phosphate buffer and 0.1M HCl, as described in more detail below.

[0292]Dissolution System

Dissolution medium0.05M Phosphate Buffer (pH 4.0)or 0.1M Hydrochloric AcidApparatusUSP II (Paddles)Volume900 mlSpeed100 rpmTemperature37° C.

[0293]7 litres 0.05M Phosphate buffer (pH 4.0) was prepared by dissolving 47.8 g potassium phosphate in 6.75 litres of water, then adding portions of 60% orthophosphoric acid solution to obtain a pH of 4.0 (+ / −0.05). The solution was made up to 7 litres with water and the pH adjusted as necessary with sodium hydroxide or phosphoric acid).

[0294]The 0.1M HCl was prepared by diluting 3.5 litres of 0.2M hydrochloric acid to 7 litres with purified water.

[0295]Dissolution Procedure

[0296]Aliquots were taken from each dissolution vessel at the indicated (e.g. hourly) hourly intervals. The UV absorbance of each aliquot at 215...

example 3

Pharmacokinetic Modelling

[0303]Multiexponential functions were fitted to the published plasma concentration-time profiles of immediate-release (IR) aripiprazole after repeated once-daily oral doses of 5, 10, 15 and 20 mg (Mallikaarjun S, Salazar D, Braner S, “Pharmacokinetics, tolerability and safety of aripiprazole following multiple oral dosing in normal healthy volunteers”, J. Clin. Pharmacol., 2004; 44:179-187).

[0304]The function (representing first-order absorption with two-compartment disposition) was of the form:

C(t)=A·e−α(t)+B·e−β(t)+C·e−k01(t)

where A, B, α, β and k01 are constants, C=−(A+B) and C(t) is the plasma concentration at time, t.

[0305]The published model (Mallikaarjun et al, see above) was used to simulate plasma concentrations of aripiprazole after various dose regimens of the IR formulation. In addition, various dose regimens of a sustained-release (SR) formulation were simulated assuming that the release was zero-order for examples ranging from 10 h to 18 h. Th...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Timeaaaaaaaaaa
Biodegradabilityaaaaaaaaaa
Login to View More

Abstract

An orally deliverable pharmaceutical composition provides controlled release of aripiprazole. The composition includes a therapeutically effective amount of aripiprazole and at least one pharmaceutically acceptable excipient. The compositions of the invention may exhibit one or more of the release profiles defined in the specification.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a division of co-pending U.S. patent application Ser. No. 12 / 443,036, filed Mar. 26, 2009, which in turn was a Section 371 U.S. National Stage application of International Application No. PCT / GB2007 / 003677, filed Sep. 26, 2007, which was published in the English language on Apr. 3, 2008, under International Publication No. WO / 2008 / 038003 A2, the disclosures of each of which are hereby incorporated herein by reference.BACKGROUND OF THE INVENTION[0002]The invention relates to pharmaceutical formulations comprising aripiprazole. More particularly, the invention relates to orally deliverable pharmaceutical compositions for the controlled release of aripiprazole.[0003]Aripiprazole is 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one and has the following structure:[0004]Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. Partial agonism at...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/38A61K45/06A61K31/496
CPCA61K47/38A61K45/06A61K31/496A61K9/2054A61P1/00A61P11/06A61P19/10A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P43/00A61P3/10A61K9/20
Inventor WILDING, IANPENDLETON, RUSSELL
Owner ZYSIS
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com