CN112156076A - 一种脂溶性维生素固体颗粒及其制备方法 - Google Patents
一种脂溶性维生素固体颗粒及其制备方法 Download PDFInfo
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Abstract
本发明公开了一种脂溶性维生素固体颗粒及其制备方法,维生素固体颗粒包括脂溶性维生素、乳化剂、抗氧化剂、填充剂;其中,脂溶性维生素的含量为固体颗粒总重量的0.05%‑5%,所述抗氧化剂包含了两种及以上的不同氧化电势的抗氧化剂。本发明所述脂溶性维生素固体颗粒的制备方法如下:(1)将脂溶性维生素溶解于油中或加热使其熔融;(2)将乳化剂、抗氧化剂、填充剂与水混合溶解,得水溶液;(3)将步骤(1)所得溶解或熔融的脂溶性维生素与所述水溶液混合,得到混合溶液;(4)将混合溶液进行喷雾干燥,即得平均粒径小于100μm的脂溶性维生素固体颗粒。
Description
技术领域
本发明涉及药物制剂领域,具体涉及一种脂溶性维生素固体颗粒及其制备方法。
背景技术
脂溶性维生素是一类可维持人体正常机体功能的水不溶性维生素,包括维生素A、维生素D、维生素E、维生素K及其衍生物,可溶解于油脂中且稳定性较差。脂溶性维生素经口服,由胆汁的乳化作用在肠道中被吸收,由淋巴系统进入人体的各个器官,且大部分被储存在脂肪组织中,仅少量被排出体外。
一般而言,人们可从正常膳食中补充每日所需维生素;而部分特殊人群,如婴幼儿、老年人、食物偏好者等,脂溶性维生素的摄入量往往不足,若不额外补充,则会缓慢出现维生素缺乏症状,严重者会诱发或加重部分疾病。除日常饮食外,可额外补充维生素的产品包括药品、保健食品及添加维生素作为营养强化剂的其他食品。但由于人体可储存大量脂溶性维生素,若摄入量过多则存在蓄积中毒的可能性。因此,《GB14880-2012 食品营养强化剂使用标准》及《中国居民膳食营养素参考摄入量》分别对脂溶性维生素的食品添加量及人体每日推荐摄入量有所规定。此外,通过查阅部分市售奶粉、保健食品及药品的说明书可知,脂溶性维生素在产品中的占比多在千分之一、万分之一,添加量极少。
现有市售产品中,脂溶性维生素的添加形式主要分为液体或固体原料及固体颗粒(制剂中间体)两类。受脂溶性维生素稳定性的影响,为确保含量符合下限要求,以原料形式投料时往往会采用过量投料。但过量投料导致成本较高,且同时带来含量超限等安全性问题。而脂溶性维生素固体颗粒这一制剂中间体的性质稳定,生产操作简便,已广泛应用于食品、药品及饲料中。但是,目前市售维生素固体颗粒的粒径较大,多在250 μm左右,且颗粒流动性很好,在与其他物料混合时易聚集分层,导致含量均匀度不合格;另外由于脂溶性维生素的性质较不稳定,制备维生素固体颗粒时往往过量投料导致市售脂溶性维生素颗粒中维生素的相对含量较高,但人体每日摄入的维生素量有限,市售维生素颗粒在使用时加入量极少,增加了混合不均匀的风险。因此市场中急需一种含量较低、粒径较小且性质稳定的维生素固体颗粒,以解决含量不均匀的问题。
发明内容
本发明的主要目的在于提供一种脂溶性维生素固体颗粒及其制备方法,以解决现有技术难题。
本发明的技术方案如下:
本发明提供一种脂溶性维生素固体颗粒,处方组成包括脂溶性维生素、乳化剂、抗氧化剂、填充剂,其特征在于,脂溶性维生素为维生素A及其衍生物、维生素D及其衍生物、维生素E及其衍生物、维生素K及其衍生物中的一种或多种。
基于固体颗粒总重量,脂溶性维生素的含量为0.05% - 5%。优选地,基于固体颗粒总重量,脂溶性维生素的含量为0.10% - 5%。
所述脂溶性维生素固体颗粒的处方中加入了乳化剂,乳化剂可选自食物改性淀粉、磷脂(卵磷脂、大豆磷脂)、蔗糖酯、卡拉胶、抗坏血酸棕榈酯、山梨酯中的一种或多种。
所述脂溶性维生素固体颗粒的处方中加入了抗氧化剂,抗氧化剂可选自生育酚、抗坏血酸及其盐、抗坏血酸棕榈酯、二丁基羟基甲苯(BHT)中的两种或多种。基于固体颗粒总重量,抗氧化剂的总含量为0.05% - 10%。
所述脂溶性维生素固体颗粒的处方中还加入了填充剂,填充剂可选自乳糖、蔗糖、麦芽糊精、葡萄糖。
所述脂溶性维生素固体颗粒的平均粒径小于100 μm。
本发明所述脂溶性维生素固体颗粒包括以下重量百分比的各组分:
脂溶性维生素:0.05% - 5%
乳化剂:20% - 80%
抗氧化剂:0.05% - 10%
填充剂:10% - 20%
油相溶剂:0% - 20%。
本发明提供一种脂溶性维生素固体颗粒的制备方法,步骤如下:
(1)将脂溶性维生素溶解于油中或加热使其熔融;
(2)提供含乳化剂及其他基质组分的水溶液;
(3)混合上述水溶液及上述溶解或熔融的脂溶性维生素;
(4)采用喷雾干燥法,将(3)中的混合溶液制成平均粒径小于100 μm的维生素固体颗粒。
本发明所述脂溶性维生素固体颗粒的制备方法,具体如下:
所述步骤(1)将脂溶性维生素溶解于油中,其中油包括但不限于食用油(大豆油、菜籽油、葵花籽油)、脂肪酸单甘油酯、脂肪酸双甘油酯、脂肪酸聚甘油酯,或加热使其熔融;
所述步骤(2)将乳化剂、填充剂、抗氧化剂溶解于纯化水中;
所述步骤(3)中,采用高速搅拌的方法,混合上述水溶液及上述溶解或熔融的脂溶性维生素,制得分散均匀、稳定的乳液;
所述步骤(4)中,采用喷雾干燥法,将上述乳液制成平均粒径小于100 μm的脂溶性维生素固体颗粒,喷雾干燥方式包括气流式喷雾干燥、压力式喷雾干燥、离心式喷雾干燥;优选地采用离心式喷雾干燥。
本发明所述的脂溶性维生素固体颗粒可用于但不限于片剂、膳食补充剂、食品、食品补充剂、乳品、药物或兽药、饲料或饲料补充剂、饮料的制备。
本发明的优势在于:
本发明提供了一种低含量、小粒径、性质稳定的脂溶性维生素固体颗粒。本发明的制备方法在降低固体颗粒中脂溶性维生素含量的同时,减小了脂溶性维生素固体颗粒的粒径,降低混合工序中含量均匀度不合格风险,填补市场中低含量、小粒径脂溶性维生素固体颗粒的空白,带来良好的经济效益及社会效益。
附图说明
图1 实施例3所获得的维生素D3颗粒与市售维生素D3颗粒稳定性考察对比。
具体实施方式
在下面的描述中阐述了很多具体细节以便于充分理解本发明。但是本发明能够以很多不同于在此描述的其它方式来实施,本领域技术人员可以在不违背本发明内涵的情况下做类似改进,因此本发明不受下面公开的具体实施的限制。
除非另有定义,本文所使用的所有的技术和科学术语与属于本发明的技术领域的技术人员通常理解的含义相同。在本发明的说明书中所使用的术语只是为了描述具体的实施例的目的,不是旨在于限制本发明。
实施例1:
取适量纯化水加热至70 ℃,加入食物改性淀粉、乳糖及抗坏血酸钠在65 ℃ - 70 ℃下搅拌至完全溶解得水相溶液。将维生素A醋酸酯加热至60 ℃熔融,随后加入BHT搅拌至完全溶解得油相溶液。将上述水相溶液与油相溶液在容器中混合均匀并乳化,乳化过程的温度始终保持在65 ℃左右。通过偏光显微镜观察可得,乳化后的乳滴粒径分布均匀。将得到的乳液进行喷雾干燥,终产品呈球形及类球形。通过激光粒度仪(TopSizer)测量的最终产品平均粒度结果如下:D10 = 68μm,D50 = 86μm,D90 = 102μm。
实施例2:
取适量纯化水加热至70 ℃,加入食物改性淀粉、乳糖及抗坏血酸钠在65 ℃ - 70 ℃下搅拌至完全溶解得水相溶液。维生素D3及生育酚溶于中链甘油三酯中得油相溶液。将上述水相溶液与油相溶液在容器中混合均匀并乳化,乳化过程的温度始终保持在65 ℃左右。通过偏光显微镜观察可得,乳化后的乳液粒径分布均匀。将得到的乳液进行喷雾干燥,终产品呈球形及类球形。通过激光粒度仪(TopSizer)测量的最终产品平均粒度结果如下:D10 =63μm,D50 = 94μm,D90 = 106μm。
实施例3:
取适量纯化水加热至70 ℃,加入食物改性淀粉、乳糖及抗坏血酸钠在65 ℃ - 70 ℃下搅拌至完全溶解得水相溶液。维生素D3及生育酚溶于中链甘油三酯中得油相溶液。将上述水相溶液与油相溶液在容器中混合均匀并乳化,乳化过程的温度始终保持在65 ℃左右。通过偏光显微镜观察可得,乳化后的乳液粒径分布均匀。将得到的乳液进行喷雾干燥,终产品呈球形及类球形。通过激光粒度仪(TopSizer)测量的最终产品平均粒度结果如下:D10 =52μm,D50 =73μm,D90 = 89μm。
实施例4:
将实施例3所获得的维生素D3颗粒与市售维生素D3颗粒分别包装与防潮镀铝袋中,一同放置于40 ℃条件下,分别测定放置0、1、2、3、6月后维生素D3的相对含量以进行稳定性考察。结果如下表所示,其中本发明所述维生素D3颗粒0天相对含量为100.2%,在40℃下放置6个月,维生素D3的相对含量仅降低5%,而市售维生素D3颗粒0天的相对含量为128.2%,在40℃下放置6个月后降低了约46%。无论是0天相对含量还是稳定性,本发明提供的维生素D3颗粒均优于市售制剂。综上,本发明提供的脂溶性维生素固体颗粒的稳定性及维生素相对含量均显著优于市售产品。
以上所述实施例仅表达了本发明的几种实施方式,其描述较为具体和详细,但并不能因此而理解为对发明专利范围的限制。应当指出的是,对于本领域的普通技术人员来说,在不脱离本发明构思的前提下,还可以做出若干变形和改进,这些都属于本发明的保护范围。因此,本发明专利的保护范围应以所附权利要求为准。
Claims (10)
1.一种脂溶性维生素固体颗粒,其特征在于,包括脂溶性维生素、乳化剂、抗氧化剂、填充剂;其中,
(1)所述脂溶性维生素的含量为固体颗粒总重量的0.05% - 5%;
(2)至少包含两种不同氧化电势的抗氧化剂,所述抗氧化剂的总含量为固体颗粒总重量的0.05% - 10%;
(3)所述脂溶性维生素固体颗粒的平均粒径小于100 μm。
2.根据权利要求1所述的脂溶性维生素固体颗粒,其特征在于,所述脂溶性维生素的含量为固体颗粒总重量的0.10% - 5%。
3.根据权利要求1所述的脂溶性维生素固体颗粒,其特征在于,所述脂溶性维生素为维生素A及其衍生物、维生素D及其衍生物、维生素E及其衍生物、维生素K及其衍生物中的一种或多种。
4.根据权利要求1所述的脂溶性维生素固体颗粒,其特征在于,所述乳化剂选自食物改性淀粉、磷脂(卵磷脂、大豆磷脂)、蔗糖酯、卡拉胶、抗坏血酸棕榈酯、山梨酯中的一种或多种。
5.根据权利要求1所述的脂溶性维生素固体颗粒,其特征在于,抗氧化剂可选自生育酚、抗坏血酸及其盐、抗坏血酸棕榈酯、二丁基羟基甲苯(BHT)中的两种或多种。
6.根据权利要求1所述的脂溶性维生素固体颗粒,其特征在于,包括以下重量百分比的各组分:
脂溶性维生素:0.05% - 5%;
乳化剂:20% - 80%;
抗氧化剂:0.05% - 10%;
填充剂:10% - 20%;
油相溶剂:0% - 20%。
7.根据权利要求1~6所述的脂溶性维生素固体颗粒,其特征在于,所述颗粒处方组成包含但不限于:
脂溶性维生素:2.5mg/g;
食物改性淀粉:730.5mg/g;
抗氧化剂:50.0mg/g;
乳糖:187.0mg/g;
中链甘油三酯:30.0mg/g。
8.根据权利要求1~6所述的脂溶性维生素固体颗粒,其特征在于,所述颗粒处方组成包含但不限于:
脂溶性维生素:50mg/g;
食物改性淀粉:730mg/g;
抗氧化剂:80.0mg/g;
乳糖:140.0mg/g。
9.一种权利要求1所述脂溶性维生素固体颗粒的制备方法,其特征在于,包括以下步骤:
(1)将脂溶性维生素溶解于油中或加热使其熔融;
(2)将乳化剂、抗氧化剂、填充剂与水混合溶解,得水溶液;
(3)将步骤(1)所得溶解或熔融的脂溶性维生素与所述水溶液混合,得到混合溶液;
(4)将混合溶液进行喷雾干燥,即得。
10.权利要求1~8所述脂溶性维生素固体颗粒在制备膳食补充剂、食品、食品补充剂、乳品、药物或兽药、饲料或饲料补充剂、饮料中的应用。
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