• Title/Summary/Keyword: pharmaceutical formulation

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New Cationic Liposome with Enhanced Stability and Transfection Efficiency for Gene Delivery (안정성 및 Transfection 효율이 우수한 양이온성 리포좀 유전자 전달시스템의 개발)

  • Kim, Kyoung-Mi;Nam, Bang-Hyun;Sohn, Dong-Hwan
    • Journal of Pharmaceutical Investigation
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    • v.28 no.2
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    • pp.93-98
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    • 1998
  • We have developed liposomes which can be easily prepared with inexpensive lipid, have enhanced stability, and can efficiently deliver DNA into the COS-l cells, Liposome formulations were prepared using cationic materials such as dimethyldioctadecyl ammonium bromide (DDAB), cetyltrimethyl ammonium bromide(CTAB), We investigated the effect of cationic liposome formulations on in vitro DNA transfection, DDAB-containing liposomes showed increased transfection efficiency which was 3.2-fold as much as that by $Lipofectin^{\circledR}$, but CTAB-containing liposomes were inactive in gene transfection. The effect of colipid of DDAB-containing liposome was also investegated. As a colipid, dioleylphosphatidylethanolamine(DOPE) and cholesterol did altered the transfection efficiency of DDAB-containing liposomes. And increased DDAB concentration lowered the transfection efficiency. The optimum amount of liposomal formulation was $10\;{\mu}M$ for $1\;{\mu}g$ of DNA. In the experiment of stability, DOPE-containing liposomes formulation showed a broad size distribution and separation of two major peaks on a 5th day of preparation, but liposomes containing cholesterol was stable for 10 days. DDAB-containing liposomal DNA delivery system was prepared easily and was stable.

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Improved Stability against Moisture of Amlodipine Maleate Tablets using Microcrystalline Cellulose and Pregelatinized Starch (미세결정셀룰로오스와 호화전분을 이용한 암로디핀말레이트 정제의 수분에 대한 안정성 개선)

  • Park, Ho-Seock;Hwang, Woo-Sin;Bang, Kyu-Ho;Park, Jeong-Sook;Cho, Cheong-Weon;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.38 no.3
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    • pp.157-162
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    • 2008
  • The aim of the study was to formulate the stable amlodipine maleate tablet by selecting and combining of suitable ingredients. Amlodipine tablets were designed by using different manufacturing methods or formulations. Dissolution rate at 30 min of newly formulated tablets was over 98% in 0.1 M HCl medium. After 4 months storage under accelerated condition, the changes of appearance, loss on drying, content and total impurity were investigated. For long-term stability tests, two formulations of K017 (direct compressed tablets consisting of microcrystalline cellulose and pregelatinized starch) and K018 (wet granulated tablets by OpadryAMB) were stored under $25^{\circ}C$, 60% RH for 24 months. Under the accelerated condition, moisture content in K017 formulation was increased as 5.96% for 4 months, while other formulations with anhydrous monobasic phosphoric potassium or by wet granulation showed higher increase in moisture content compared to K017. In addition, K017 formulation showed a low decrease in contents and total relative substance as 0.8% and 0.7%, respectively. Similar stability of amlodipine in K017 was obtained under the long-term stability test. These results indicate that the K017 combined with microcrystalline cellulose and pregelatinized starch as ingredients is very stable formulation to protect active substance from moisture contact and sustain stability. Therefore, suitable combination of ingredients such as microcrystalline cellulose and pregelatinized starch could attribute to enhance the stability of moisture-labile drug such as amlodipine maleate.

Development of Novel Cosmetic Formulations using Foams (기포를 이용한 차별화된 화장품 제형 개발)

  • Cho, Wan-Goo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.38 no.1
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    • pp.1-13
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    • 2012
  • In this review, the use of air bubbles in the pharmaceutical and cosmetic formulations was discussed. The foam bubbles show different characteristics depending on the foaming agents and foam generating devices. The foam bubbles are generated in the form of dispersion of gas bubbles in a solvent. The assessment of stability and rheological properties of bubbles are the starting point for the formulation to be used. Pharmaceutical and cosmetic uses of bubbles are substantially growing, and the foam formulations of drugs can be used for rectal, vaginal, and dermal symptoms. The foam formulation is used in hair mousse, makeup foundation, and sunscreen cosmetics in basic cosmetics. Recently, a lot of studies and patents have been filed in stabilization of active ingredients and delivery of the active ingredient in terms of foam formulations. In the future, foam formulations are expected to be used as novel cosmeceutical formulations.

Development of New Amlodipine Complex using Ion Exchange Resin (이온교환수지를 이용한 새로운 암로디핀 복합체 개발)

  • Jeong, Sang-Young;Ahn, Ki-Young;Ahn, Geon-Seok;Gil, Young-Sig;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.38 no.1
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    • pp.9-14
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    • 2008
  • Cation exchange resin complex of amlodipine free base has been investigated to improve the stability and dissolution profile. The complex was prepared by reacting amlodipine solution with activated cation exchange resin, and amlodipine content in the complex was 31.6% calculated by HPLC determination. Its product was not physical mixture but the complex formed by ionic bond, which was identified by microscope system, differential scanning calorimetry and X-ray diffractometry. Each tablet containing amlodipine free base(I) and its complex(II) was prepared for the accelerated stability test ($40^{\circ}C$, 75%RH) and dissolution test in the pH 1.2 buffer solution and purified water media. Dissolution patterns of formulation II in both media were similar to those of $Norvasc^{(R)}$ tablet, but the pattern of formulation I in purified water was different. After 6 months storage under stability test, amlodipine content of formulation I, II and $Norvasc^{(R)}$ tablet were $99.3{\pm}1.2%,\;98.9{\pm}1.4%\;and\;83.9{\pm}3.4%$, respectively. While amlodipine free base was unstable at the condition, its complex was not only significantly stable, but also similar in the dissolution pattern. These results suggest the usefulness of complex as a stable carrier for amlodipine free base.

Safety, Efficacy, and Physicochemical Characterization of Tinospora crispa Ointment: A Community-Based Formulation against Pediculus humanus capitis

  • Torre, Gerwin Louis Tapan Dela;Ponsaran, Kerstin Mariae Gonzales;de Guzman, Angelica Louise Dela Pena;Manalo, Richelle Ann Mallapre;Arollado, Erna Custodio
    • Parasites, Hosts and Diseases
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    • v.55 no.4
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    • pp.409-416
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    • 2017
  • The high prevalence of pediculosis capitis, commonly known as head lice (Pediculus humanus capitis) infestation, has led to the preparation of a community-based pediculicidal ointment, which is made of common household items and the extract of Tinospora crispa stem. The present study aimed to evaluate the safety, efficacy, and physicochemical characteristics of the T. crispa pediculicidal ointment. The physicochemical properties of the ointment were characterized, and safety was determined using acute dermal irritation test (OECD 404), while the efficacy was assessed using an in vitro pediculicidal assay. Furthermore, the chemical compounds present in T. crispa were identified using liquid-liquid extraction followed by ultra-performance liquid chromatography quadruple time-of-flight mass spectrometric (UPLC-qTOF/MS) analysis. The community-based ointment formulation was light yellow in color, homogeneous, smooth, with distinct aromatic odor and pH of $6.92{\pm}0.09$. It has spreadability value of $15.04{\pm}0.98g{\cdot}cm/sec$ and has thixotropic behavior. It was also found to be non-irritant, with a primary irritation index value of 0.15. Moreover, it was comparable to the pediculicidal activity of the positive control $Kwell^{(R)}$, a commercially available 1% permethrin shampoo (P>0.05), and was significantly different to the activity of the negative control ointment, a mixture of palm oil and candle wax (P<0.05). These findings suggested that the community-based T. crispa pediculicidal ointment is safe and effective, having acceptable physicochemical characteristics. Its activity can be attributed to the presence of compounds moupinamide and physalin I.

Preparation and Evaluation of Titrated Extract of Centella Asiatica Niosome/W/O System Cream for Site Specific Targeting (니오좀을 이용한 병풀 추출물 외용제의 제조 및 평가)

  • Kim, Dong-Woo;Cho, Mi-Hyun;Park, Sun-Young;Lee, Jong-Hwa;Lee, Gye-Won;Park, Mork-Soon;Park, Jin-Kyu;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.291-297
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    • 2002
  • For preventing and curing the stretching mark, TECA Niosome/W/O system creams were formulated using Titrated Extract of Centella Asiatica (TECA) which is well known for its excellent wound healing effect. The lipid-water partition coefficients and the stabilities of TECA were evaluated and TECA Niosome/W/O system (TECA N/W/O) creams were prepared with different concentrations of cetyl alcohol and ceramide. TECA N/W/O cream was evaluated with respect to their rheological properties, permeation through excised skin of hairless mouse and in vitro and in vivo accumulation in the skin of hairless mouse. In addition, dermal thicknesses of hairless mouse skins were determined following the in vivo application of TECA N/W/O cream and control cream. TECA N/W/O creams showed pseudoplastic flow and hysteresis loop. The permeation of TECA from formulations through excised skin of hairless mouse did not observed. Amount of accumulated drug in the excised skin of hairless mouse was deσeased with an increase in the concentration of cetyl alcohol and showed no relationship with concentration of ceramide. Amount of accumulated drug in formulation A-3 was higher than in niosome suspension and other formulations. In in vivo experiment, amount of accumulated drug in formulation A-2 and A-3 was much higher than that of niosome suspension. Being treated with the N/W/O cream for 8 weeks, the dermal thickness of hairless mouse skin was increased 3.2 times than that of 16 weeks-control group.

Influence of Ointment Base on In Vitro Release Characteristics of Oregonin (오레고닌의 in vitro 방출 특성에 미치는 연고기제의 영향)

  • Im, Tae-Jong;Oh, Il-Young;Park, Young-Mi;Park, Jong-Hyeok;Lee, Min-Won;Cho, Jae-Youl;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.211-216
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    • 2007
  • The bark of Alnus japonica has been used for the treatment of fever, hemorrhage and diarrehea in oriental traditional medicine. Recently, it was revealed that the diarylheptanoids from the bark of Alnus japonica possess anti-inflammatory activity and are expected to be applicable for atopic dermatitis. In this study, oregonin, one of major active components in the bark of Alnus japonica, was developed in the form of semisolid formulations for topical delivery. Oregonin was incorporated into four ointment bases: O/W cream, W/O cream, hydrophilic ointment and lipophilic ointment. Oregonin release from all formulation prepared was evaluated. Franz cell method and immersion method were employed to characterize the release patterns of drug from each formulation based on solvent availability. O/W cream showed a better release profile than the other formulations when evaluated with Franz cell method with an order of O/W cream, hydrophilic ointment, W/O cream and lipophilic ointment. In the immersion method, hydrophilic ointment showed the greatest release rate at times 1 hour exceeding compared to other bases with an order of hydrophilic ointment, O/W cream, W/O cream and lipophilic ointment. Hydrophilicity and solvent availability of formulation seems to significantly influence the release rate of oregonin from ointment bases. In this study, we successfully characterized the oregon in ointment and found that o/w cream is a promising formulation for the topical delivery of oregonin.

Study on Polymorphism of Cimetidine (시메티딘의 다형에 관한 연구)

  • Sohn, Young-Taek;Kim, Ki-Soo
    • Journal of Pharmaceutical Investigation
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    • v.23 no.2
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    • pp.81-87
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    • 1993
  • Five crystalline forms of cimetidine, four anhydrous and a monohydrate, have been prepared, and their thermal behavriours have been studied by differential thermal analysis and thermo-gravimetry. The dissolution rates of the five forms were determined in distilled water at $37^{\circ}C$. The results showed a significant difference in the dissolution rate. Polymorphic transformation occurred spontaneously during storage at room condition and was accelerated by applied energy during formulation process-milling.

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Formulation and Biopharmaceutical Evaluation of Self-Microemulsifying Drug Delivery Systems (SMEDDS) Containing Silymarin

  • Kim, Tae-Seo
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.56-56
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    • 2003
  • Carduus marianus extract (formally called silymarin) have been used mainly as a medicament for hepatobiliary diseases. The major component of silymarin is silybin, which constitutes between 50 and 70% of the drug and is the major active component. Many experiments show the efficacy of silybin parenterally administerated. But, its bioavailability is low after oral administration due to its low solubility in water. (omitted)

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Formulation and Biopharmaceutical Evaluation of Silymarin Using Self-MicroEmulsifying Drug Delivery Systems

  • Kim, Tae-Seo;Park, Jae-Hyun;Chi, Sang-Cheol;Woo, Jong-Soo
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.296.2-296.2
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    • 2003
  • Carduus marianus extract (formally called silymarin) have been used mainly as a medicament for hepatobiliary diseases. The major component of silymarin is silybin, which constitutes between 50 and 70% of the drug and is the major active component. Many experiments show the efficacy of silybin parenterally administerated. But, its bioavalability is low after oral administration due to its low solubility in water. (omitted)

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