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Oral controlled release compositions comprising vitamin d compound and waxy carrier

A technology of vitamins and compounds, applied in the field of controlled-release pharmaceutical compositions, can solve the problems of early detection and treatment of hyperparathyroidism

Active Publication Date: 2010-03-10
OPKO IP HLDG II INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, secondary hyperparathyroidism in CKD is rarely detected and treated early, let alone prevented

Method used

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  • Oral controlled release compositions comprising vitamin d compound and waxy carrier
  • Oral controlled release compositions comprising vitamin d compound and waxy carrier
  • Oral controlled release compositions comprising vitamin d compound and waxy carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] Example 1 - Modified release formulation

[0118] Nine oral vitamin D preparations were prepared according to Table 3 below by uniformly mixing the ingredients in the amounts listed in Table 3, and filling the mixture into hard capsules. Formulation 9 is an immediate release formulation according to the prior art, wherein MIGLYOL 812N is a trade name for caprylic / capric triglyceride, available from CONDEA Chemie GmbH of Cranford, New Jersey, USA. The formulation is formulated with the equivalent of 250 μg of 25-hydroxyvitamin D 3 A single dose of Yucatan minipigs (approximately 10 kg) was administered to groups consisting of 5 animals per group. Equivalent 250 μg 25-hydroxyvitamin D 3 A tenth group of five Yucatan minipigs was administered by intravenous bolus.

[0119]

[0120] Blood was collected before dosing, and at 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 96, 168, 240, 336, 432, 504, 576, and 672 hours after dosing. Serum 25-hydroxyvitamin D 3 Levels were detected b...

Embodiment 2

[0131] Example 2-Pharmacokinetic study of oral capsules in minipigs

[0132] The aim of the study was to evaluate 25-hydroxyvitamin D in male Yucatan pigs (-45kg body weight) 3 systemic absorption, administration is carried out as follows: a) 1×250 μg 25-hydroxyvitamin D 3 Modified release (MR) capsules; b) 2×250 μg MR capsules; c) 4×250 μg MR capsules; d) 1×1000 μg MR capsules; e) 1×250 μg 25-hydroxyvitamin D 3 Immediate release (IR) capsules; and f) 1 x 250 μg MR capsules administered for 3 consecutive days.

[0133] The MR formulation was prepared based on the formulation of Example 1, Group 7 above. Higher concentration of 25-hydroxyvitamin D in the case of 1000 μg MR capsules 3 offset by the relative reduction in ethanol.

[0134] To prepare IR preparations, 25-hydroxyvitamin D 3 (0.12% wt / wt; 250 μg per capsule) dissolved in ethanol USP (2.32% wt / wt; solublizer), mixed with corn oil USP (97.54% / wt, antioxidant) mixed. The corn oil solution (205 mg) was filled int...

Embodiment 3

[0150] Example 3 - Oral Capsule Minipig Systemic Exposure Study

[0151] The aim of this study was to assess systemic 25-hydroxyvitamin D in healthy normal male Yucatan pigs (body weight -50-60kg) maintained on a diet including adequate vitamin D intake, administered daily for 21 days 3 Concentration increases, administered as follows: a) 25 μg immediate release (IR) 25-hydroxyvitamin D 3 Capsules (group 1), b) 25 μg modified-release (MR) 25-hydroxyvitamin D 3 capsules (group 2), and c) 125 μg MR 25-hydroxyvitamin D 3 capsules (group 3).

[0152] The MR formulation was prepared based on the formulation of Example 1, Group 7 above. 25 hydroxyvitamin D 3 Differences in concentrations are offset by relative changes in ethanol.

[0153] For the preparation of IR formulations, 25-hydroxyvitamin D 3 (0.12% wt / wt; 250 μg per capsule) dissolved in ethanol USP (2.32% wt / wt; solublizer) and mixed with corn oil USP (97.54% / wt, antioxidant) mixed. Corn oil solution (205 mg) was f...

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Abstract

A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Patent Application 60 / 913,853, filed April 25, 2007, under 35 U.S.C. § 119(e). technical field [0003] The present invention generally relates to controlled release pharmaceutical compositions. More specifically, the present invention relates to controlled release formulations for oral administration of vitamin D compounds. Background technique [0004] Cholecalciferol and ergocalciferol (collectively "vitamin D") are fat-soluble ring-opened steroid precursors of the provitamin D hormone. 25-Hydroxyvitamin D 2 and 25-hydroxyvitamin D 3 Vitamin D metabolites (collectively referred to as "25-hydroxyvitamin D") are fat-soluble steroid prohormones of the vitamin D hormone, which contribute to maintaining normal levels of calcium and phosphorus in the blood. [0005] Cholecalciferol and ergocalciferol usually exist stably at low concentrations in human blood. Since...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/593A61K47/06A61K47/14A61K47/44
CPCA61K31/59A61K47/14A61K9/4866A61K47/44A61K9/4858A61K47/06A61K31/593A61K47/10A61K9/0019A61P1/00A61P1/02A61P11/00A61P13/00A61P13/12A61P17/00A61P19/00A61P21/00A61P25/00A61P27/00A61P29/00A61P3/00A61P3/02A61P31/00A61P35/00A61P43/00A61P5/00A61P5/18A61P7/00A61P9/00A61K47/50A61K9/48A61K9/0053A61K9/4825
Inventor 萨米尔·P·塔巴什杰伊·A·怀特查理斯·W·比绍夫
Owner OPKO IP HLDG II INC
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